TREA

NOVEL FUNCTIONALIZED LACTAMS AS MODULATORS OF THE 5-HYDROXYTRYPTAMINE RECEPTOR 7 AND THEIR METHOD OF USE

Follow

Information

  • Patent Application
  • 20220306629
  • Publication Number
    20220306629
  • Date Filed
    May 10, 2019
    5 years ago
  • Date Published
    September 29, 2022
    2 years ago
Information
Abstract
Pharmaceutical compositions of the invention comprise functionalized lactam derivatives of formula (I) having a disease-modifying action in the treatment of diseases associated with dysregulation of 5-hydroxytryptamine receptor 7 activity. A is selected from a group consisting of (group) and (group)
Description
FIELD OF INVENTION

Embodiments of the invention are directed to novel compounds useful as modulators of 5-hydroxytryptamine receptor 7 (5-HTS) activity and their method of use. Embodiments are further directed to a novel chemotype useful for the treatment diseases that are associated with dysregulation of 5-hydroxytryptamine receptor 7 activity.


BACKGROUND OF THE INVENTION

Serotonin was discovered in the late 1940s and is present in both the peripheral and central nervous systems [Physiol. Res, 60 (2011) 15-25; Psychopharmacology 213 (2011) 167-169]. Serotonin or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter of the indolalkylamine group that acts at synapses of nerve cells. Seven distinct families of serotonin receptors have been identified and at least 20 subpopulations have been cloned on the basis of sequence similarity, signal transduction coupling and pharmacological characteristics. The seven families of 5-HT receptor are named 5-HT1, 5-HT2, 5-HT3, 5-HT4, 5-HT5, 5-HT6, and 5-HT7 and each of these receptors in turn has subfamilies or subpopulations. The signal transduction mechanism for all seven families have been studied and it is known that activation of 5-HT1 and 5-HT5 receptors causes a decrease in intracellular cAMP whereas activation of 5-HT2, 5-HT3, 5-HT4, 5-HT6, and 5-HT7 results in an increase in intracellular IP3 and DAG. The 5-HT pathways in the brain are important targets for drug development in the area of CNS disorders. The neurotransmitter binds to its a G-protein coupled receptor and is involved in a wide variety of actions including cognition, mood, anxiety, attention, appetite, cardiovascular function, vasoconstriction, sleep (ACS Medicinal Chemistry Letters, 2011, 2, 929-932; Physiological Research, 2011, 60, 15-25), inflammatory bowel disease (IBD), and intestinal inflammation (WO 2012058769, Khan, W. I., et. al. Journal of Immunology, 2013, 190, 4795-4804), epilepsy, seizure disorders (Epilepsy Research (2007) 75, 39), drug addiction, and alcohol addiction (Hauser, S. R. et. al. Frontiers in Neuroscience, 2015, 8, 1-9) among others.


SUMMARY OF THE INVENTION

The present invention is directed toward novel 5-hydroxytryptamine receptor 7 (5-HT7) activity modulators, compounds of formula (I),




embedded image


Including enantiomers, diastereomers, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, wherein:

  • A is selected from a group consisting of




embedded image


  • R1 is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl;

  • R2 is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl;

  • Or R1 and R2 are taken together with the atoms to which they are bound to form a ring having from 5 to 7 ring atoms, optionally containing a double bond;

  • Or R1 and R2 are taken together with the atoms to which they are bound to form a ring having from 6 to 8 ring atoms containing a moiety selected from the group consisting of O, S, SO, SO2, and NR7;

  • R3 is selected from the group consisting of optionally substituted phenyl, optionally substituted naphthylen-1-yl, optionally substituted naphthylen-2-yl, optionally substituted 2-pyridyl, optionally substituted 3-pyridyl, optionally substituted 4-pyridyl, and





embedded image


  • R4 is selected from the group consisting of optionally substituted phenyl, optionally substituted naphthylen-1-yl, optionally substituted naphthylen-2-yl, optionally substituted 2-pyridyl, optionally substituted 3-pyridyl, optionally substituted 4-pyridyl and





embedded image


  • R5 is selected from the group consisting of optionally substituted phenyl, optionally substituted naphthylen-1-yl, optionally substituted naphthylen-2-yl, optionally substituted 2-pyridyl, optionally substituted 3-pyridyl, optionally substituted 4-pyridyl and





embedded image


  • R6 is selected from the group consisting of optionally substituted phenyl, optionally substituted naphthylen-1-yl, optionally substituted naphthylen-2-yl, optionally substituted 2-pyridyl, optionally substituted 3-pyridyl, and optionally substituted 4-pyridyl;

  • R7 is selected from the group consisting of H, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, optionally substituted phenyl, optionally substituted benzyl, COR8, CO2R9, CONR10aR10b, SO2NR10aR10b, and SO2R10c;

  • R8 is selected from the group consisting of H, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R9 is selected from the group consisting of C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R10a is selected from the group consisting of H, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R10b is selected from the group consisting of H, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R10c is selected from the group consisting of C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear haloalkyl, C3-7 branched haloalkyl, —(CH2)qCN, —(CH2)qSO2R11, —(CH2)qOR12,





embedded image


  • R11 is selected from the group consisting of C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R12 is selected from the group consisting of C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R1a, R1b, R1c, R1d, and R1e are at each occurrence independently selected from the group consisting of H, OH, NO2, halogen, CN, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, —S(C1-6 linear alkyl), S(C3-7 branched alkyl), —S(C3-7 cycloalkyl), COR13, CO2R14, CONR15aR15b, SO2NR15aR15b, NR16aR16b, NR16aCOR17, NR16aSO2R18, and NR16aSO2NR19dR19b;

  • R13 is at each occurrence independently selected from the group consisting of H, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R14 is at each occurrence independently selected from the group consisting of C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R15a is at each occurrence independently selected from the group consisting of H, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R15b is at each occurrence independently selected from the group consisting of H, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R16a is at each occurrence independently selected from the group consisting of H, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R16b is at each occurrence independently selected from the group consisting of H, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R17 is at each occurrence independently selected from the group consisting of H, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R18 is at each occurrence independently selected from the group consisting of C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R19a is at each occurrence independently selected from the group consisting of C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R19b is at each occurrence independently selected from the group consisting of C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl; n is 1, 2, 3, or 4;

  • m is 1, 2, or 3.



In embodiments, A is




embedded image


In embodiments, n is 1, 2, or 3. In embodiments, n is 1 or 2. In embodiments, n is 1. In embodiments, n is 2. In embodiments, each of R1 and R2 is unsubstituted C1-6 alkyl (e.g., each of R1 and R2 is methyl or each of R1 and R2 is ethyl). In embodiments, R1 and R2 are taken together with the atoms to which they are bound to form a 5- to 8-membered ring (e.g., a C3-C8 cycloalkyl, a C5-C8 cycloalkenyl, or a 5- to 8-membered ring containing a ring atom that is NR7). In embodiments, R1 and R2 are taken together with the atoms to which they are bound to form cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cycloheptenyl, cyclooctyl, cyclooctenyl, pyrrolidinyl, or piperidinyl, wherein the nitrogen atom in said pyrrolidinyl or piperidinyl group is NR7. In embodiments, R7 is an alkylsulfonyl —SO2R10c (e.g., —SO2Me) or an acyl —COR8 (e.g., acetyl). In embodiments, R3 is phenyl or a pyridyl. In embodiments, R3 is unsubstituted. In embodiments, R3 is substituted (e.g., a phenyl substituted by 1, 2, 3, 4, or 5 substituents or a pyridyl substituted by 1, 2, 3, or 4 substituents). In embodiments, substituents are selected from the group consisting of —OH, —F, —Cl, —Br, —I, —CN, —OMe, —OEt, —OnPr, —OiPr, —OCF3, -Me, -Et, —n—iPr, —CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.


In embodiments, A is




embedded image


In embodiments, n is 1, 2, or 3. In embodiments, n is 1 or 2. In embodiments, n is 1. In embodiments, n is 2. In embodiments, each of R1 and R2 is unsubstituted C1-6 alkyl (e.g., each of R1 and R2 is methyl or each of R1 and R2 is ethyl). In embodiments, R1 and R2 are taken together with the atoms to which they are bound to form a 5- to 8-membered ring (e.g., a C3-C8 cycloalkyl, a C5-C8 cycloalkenyl, or a 5- to 8-membered ring containing a ring atom that is NR7). In embodiments, R1 and R2 are taken together with the atoms to which they are bound to form cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cycloheptenyl, cyclooctyl, cyclooctenyl, pyrrolidinyl, or piperidinyl, wherein the nitrogen atom in said pyrrolidinyl or piperidinyl group is NR7. In embodiments, R7 is an alkylsulfonyl —SO2R10c (e.g., —SO2Me) or an acyl —COR8 (e.g., acetyl). In embodiments, R4 is phenyl or a pyridyl. In embodiments, R4 is unsubstituted. In embodiments, R4 is substituted (e.g., a phenyl substituted by 1, 2, 3, 4, or 5 substituents or a pyridyl substituted by 1, 2, 3, or 4 substituents). In embodiments, substituents are selected from the group consisting of —OH, —F, —Cl, —Br, —CN, —OMe, —OEt, —OnPr, —OiPr, —OCF3, -Me, -Et, —nPr, —iPr, —CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.


In embodiments, A is




embedded image


In embodiments, n is 1, 2, or 3. In embodiments, n is 1 or 2. In embodiments, n is 1. In embodiments, n is 2. In embodiments, each of R1 and R2 is unsubstituted C1-6 alkyl (e.g., each of R1 and R2 is methyl or each of R1 and R2 is ethyl). In embodiments, R1 and R2 are taken together with the atoms to which they are bound to form a 5- to 8-membered ring (e.g., a C3-C8 cycloalkyl, a C5-C8 cycloalkenyl, or a 5- to 8-membered ring containing a ring atom that is NR7). In embodiments, R1 and R2 are taken together with the atoms to which they are bound to form cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cycloheptenyl, cyclooctyl, cyclooctenyl, pyrrolidinyl, or piperidinyl, wherein the nitrogen atom in said pyrrolidinyl or piperidinyl group is NR7. In embodiments, R7 is an alkylsulfonyl —SO2R10c (e.g., —SO2Me) or an acyl —COR8 (e.g., acetyl). In embodiments, R5 is phenyl or a pyridyl. In embodiments, R5 is unsubstituted. In embodiments, R5 is substituted (e.g., a phenyl substituted by 1, 2, 3, 4, or 5 substituents or a pyridyl substituted by 1, 2, 3, or 4 substituents). In embodiments, substituents are selected from the group consisting of —OH, —F, —Cl, —Br, —CN, —OMe, —OEt, —OnPr, —OiPr, —OCF3, -Me, -Et, —nPr, —iPr, —CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.


In embodiments, a compound is according to any formula described herein, or a pharmaceutically acceptable salt thereof In embodiments, a compound is any compound described herein or a pharmaceutically acceptable salt thereof (e.g., a compound as described in any of Tables 1-39 described herein, or a pharmaceutically acceptable salt thereof). In embodiments, a compound is any of the compounds described in any of Tables 34-39, or a pharmaceutically acceptable salt thereof.


In embodiments, a compound has the S-configuration at the nitrogen-substituted carbon of the lactam. In embodiments, a compound has the R-configuration at the nitrogen-substituted carbon of the lactam.


The present invention further relates to compositions comprising: an effective amount of one or more compounds according to the present invention and an excipient.


The present invention also relates to a method for treating or preventing diseases that involve dysregulation of 5-hydroxytryptamine receptor 7 activity, including, for example, circadian rhythm disorder, depression, schizophrenia, neurogenic inflammation, hypertension, peripheral, vascular diseases, migraine, neuropathic pain, peripheral pain, allodynia, thermoregulation disorder, learning disorder, memory disorder, hippocampal signaling disorder, sleep disorder, attention deficit/hyperactivity disorder, anxiety, avoidant personality disorder, premature ejaculation, eating disorder, premenstrual syndrome, premenstrual dysphonic disorder, seasonal affective disorder, bipolar disorder, inflammatory bowel disease (IBD), intestinal inflammation, epilepsy, seizure disorders, drug addiction, alcohol addiction, breast cancer, liver fibrosis, chronic liver injury, hepatocellular carcinoma, small intestine neuroendocrine tumors, and lung injury said method comprising administering to a subject an effective amount of a compound or composition according to the present invention.


The present invention yet further relates to a method for treating or preventing diseases that involve dysregulation of 5-hydroxytryptamine receptor 7 activity, including, for example, circadian rhythm disorder, depression, schizophrenia, neurogenic inflammation, hypertension, peripheral, vascular diseases, migraine, neuropathic pain, peripheral pain, allodynia, thermoregulation disorder, learning disorder, memory disorder, hippocampal signaling disorder, sleep disorder, attention deficit/hyperactivity disorder, anxiety, avoidant personality disorder, premature ejaculation, eating disorder, premenstrual syndrome, premenstrual dysphonic disorder, seasonal affective disorder, bipolar, disorder inflammatory bowel disease (IBD), intestinal inflammation, epilepsy, seizure disorders, drug addiction, alcohol addiction breast cancer, liver fibrosis, chronic liver injury, hepatocellular carcinoma, small intestine neuroendocrine tumors, and lung injury wherein said method comprises administering to a subject a composition comprising an effective amount of one or more compounds according to the present invention and an excipient.


The present invention also relates to a method for treating or preventing diseases or conditions associated with circadian rhythm disorder, depression, schizophrenia, neurogenic inflammation, hypertension, peripheral, vascular diseases, migraine, neuropathic pain, peripheral pain, allodynia, thermoregulation disorder, learning disorder, memory disorder, hippocampal signaling disorder, sleep disorder, attention deficit/hyperactivity disorder, anxiety, avoidant personality disorder, premature ejaculation, eating disorder, premenstrual syndrome, premenstrual dysphonic disorder, seasonal affective disorder, bipolar disorder, inflammatory bowel disease (IBD), intestinal inflammation, epilepsy, seizure disorders, drug addiction, alcohol addiction, breast cancer, liver fibrosis, chronic liver injury, hepatocellular carcinoma, small intestine neuroendocrine tumors, and lung injury, and diseases that involve dysregulation of 5-hydroxytryptamine receptor 7 activity. Said methods comprise administering to a subject an effective amount of a compound or composition according to the present invention.


The present invention yet further relates to a method for treating or preventing diseases or conditions associated with circadian rhythm disorder, depression, schizophrenia, neurogenic inflammation, hypertension, peripheral, vascular diseases, migraine, neuropathic pain, peripheral pain, allodynia, thermoregulation disorder, learning disorder, memory disorder, hippocampal signaling disorder, sleep disorder, attention deficit/hyperactivity disorder, anxiety, avoidant personality disorder, premature ejaculation, eating disorder, premenstrual syndrome, premenstrual dysphonic disorder, seasonal affective disorder, and bipolar disorder, inflammatory bowel disease (IBD), intestinal inflammation, epilepsy, seizure disorders, drug addiction, alcohol addiction, breast cancer, liver fibrosis, chronic liver injury, hepatocellular carcinoma, small intestine neuroendocrine tumors, and lung injury, and diseases that involve dysregulation of 5-hydroxytryptamine receptor 7 activity, wherein said method comprises administering to a subject a composition comprising an effective amount of one or more compounds according to the present invention and an excipient.


The present invention also relates to a method for treating or preventing diseases or conditions associated with dysregulation of 5-hydroxytryptamine receptor 7 activity. Said methods comprise administering to a subject an effective amount of a compound or composition according to the present invention.


The present invention yet further relates to a method for treating or preventing diseases or conditions associated with dysregulation of 5-hydroxytryptamine receptor 7 activity, wherein said method comprises administering to a subject a composition comprising an effective amount of one or more compounds according to the present invention and an excipient.


The present invention further relates to a process for preparing the 5-hydroxytryptamine receptor 7 activity modulators of the present invention.


In embodiments, a disease or condition is inflammatory bowel disease (IBD).


These and other objects, features, and advantages will become apparent to those of ordinary skill in the art from a reading of the following detailed description and the appended claims. All percentages, ratios and proportions herein are by weight, unless otherwise specified. All temperatures are in degrees Celsius (° C.) unless otherwise specified. All documents cited are in relevant part, incorporated herein by reference; the citation of any document is not to be construed as an admission that it is prior art with respect to the present invention.







DETAILED DESCRIPTION OF THE INVENTION

There is evidence that suggests a role for the 5-HT7 receptor in a number of medical disorders. 5-HT7 receptor activity modulators are likely to have a beneficial effect on patients suffering from these disorders. The disorders in which 5-HT7 dysregulation plays a role and modulation of 5-HT7 receptor activity by a therapeutic agent may be a viable approach to therapeutic relief include, but are not limited to, circadian rhythm disorder, depression, schizophrenia, neurogenic inflammation, hypertension, peripheral, vascular diseases, migraine (Vanhoenacker, P. et al. Trends in Pharmacological Sciences, 2000, 21, 2, 70-77), neuropathic pain, peripheral pain, allodynia (EP1875899), thermoregulation disorder, learning disorder, memory disorder, hippocampal signaling disorder, sleep disorder (WO20100197700) attention deficit/hyperactivity disorder (ADHD) (WO20100069390), anxiety, avoidant personality disorder, premature ejaculation, eating disorder, premenstrual syndrome, premenstrual dysphonic disorder, seasonal affective disorder, bipolar disorder (WO20040229874), inflammatory bowel disease (IBD), intestinal inflammation (WO 2012058769, Khan, W. I., et. al. Journal of Immunology, 2013, 190, 4795-4804), epilepsy, seizure disorders (Epilepsy Research (2007) 75, 39), drug addiction, alcohol addiction (Hauser, S. R. et. al. Frontiers in Neuroscience, 2015, 8, 1-9), breast cancer (Gautam, J. Molecular Cancer, 2016, 15, 75, 1-14, Gautam, J. Breast Cancer Research and Treatment, 2017, 161, 29-40), liver fibrosis, chronic liver injury (Halici, Z. International Immunopharmacology, 2017, 43, 227-235), hepatocellular carcinoma (Bian, Z. X. Molecular Oncology, 2016, 10, 195-212), small intestine neuroendocrine tumors (Modlin, I. M. Cancer Science, 2013, 104, 7, 844-855), and lung injury (Halici, Z. Immunology, 2013, 1271-1283.).


There is a long felt need for new 5-HT7 modulators that will provide therapeutic relief from patients suffering from diseases associated with dysregulation of 5-hydroxytryptamine receptor 7 activity. The invention addresses the need to identify novel 5-HT7 modulators capable of treating disease associated with dysregulation of 5-hydroxytryptamine receptor 7 activity. The present invention addresses the need to develop new therapeutic agents for the treatment and prevention of circadian rhythm disorder, depression, schizophrenia, neurogenic inflammation, hypertension, peripheral, vascular diseases, migraine, neuropathic pain, peripheral pain, allodynia, thermoregulation disorder, learning disorder, memory disorder, hippocampal signaling disorder, sleep disorder, attention deficit/hyperactivity disorder, anxiety, avoidant personality disorder, premature ejaculation, eating disorder, premenstrual syndrome, premenstrual dysphonic disorder, seasonal affective disorder, bipolar disorder, inflammatory bowel disease (IBD), intestinal inflammation epilepsy, seizure disorders, drug addiction, alcohol addiction, breast cancer, liver fibrosis, chronic liver injury, hepatocellular carcinoma, small intestine neuroendocrine tumors, and lung injury.


The 5-hydroxytryptamine receptor 7 activity modulators of the present invention are capable of treating and preventing diseases associated with dysregulation of 5-hydroxytryptamine receptor 7 activity, for example circadian rhythm disorder, depression, schizophrenia, neurogenic inflammation, hypertension, peripheral, vascular diseases, migraine, neuropathic pain, peripheral pain, allodynia, thermoregulation disorder, learning disorder, memory disorder, hippocampal signaling disorder, sleep disorder, attention deficit/hyperactivity disorder, anxiety, avoidant personality disorder, premature ejaculation, eating disorder, premenstrual syndrome, premenstrual dysphonic disorder, seasonal affective disorder, bipolar disorder, inflammatory bowel disease (IBD), intestinal inflammation, epilepsy, seizure disorders, drug addiction, alcohol addiction, breast cancer, liver fibrosis, chronic liver injury, hepatocellular carcinoma, small intestine neuroendocrine tumors, and lung injury. It has been discovered that the 5-hydroxytryptamine receptor 7 play a role in a number of medical disorders, and therefore, 5-HT7 receptor activity modulators are likely to have a beneficial effect on patients suffering from these disorders. The disorders in which 5-HT7 dysregulation plays a role and modulation of 5-HT7 receptor activity by a therapeutic agent may be a viable approach to therapeutic relief include, but are not limited to, circadian rhythm disorder, depression, schizophrenia, neurogenic inflammation, hypertension, peripheral, vascular diseases, migraine (Vanhoenacker, P.et. al. Trends in Pharmacological Sciences, 2000, 21, 2, 70-77), neuropathic pain, peripheral pain, allodynia (EP1875899), thermoregulation disorder, learning disorder, memory disorder, hippocampal signaling disorder, sleep disorder (WO20100197700) attention deficit/hyperactivity disorder (ADHD) (WO20100069390), anxiety, avoidant personality disorder, premature ejaculation, eating disorder, premenstrual syndrome, premenstrual dysphonic disorder, seasonal affective disorder, bipolar disorder (WO20040229874), inflammatory bowel disease (IBD), intestinal inflammation (WO 2012058769) epilepsy, seizure disorders (Epilepsy Research (2007) 75, 39), drug addiction, alcohol addiction (Hauser, S. R. et. al. Frontiers in Neuroscience, 2015, 8, 1-9), breast cancer (Gautam, J. Molecular Cancer, 2016, 15, 75, 1-14, Gautam, J. Breast Cancer Research and Treatment, 2017, 161, 29-40), liver fibrosis, chronic liver injury (Halici, Z. International Immunopharmacology, 2017, 43, 227-235), hepatocellular carcinoma (Bian, Z. X. Molecular Oncology, 2016, 10, 195-212), small intestine neuroendocrine tumors (Modlin, I. M. ancer Science, 2013, 104, 7, 844-855), and lung injury (Halici, Z. Immunology, 2013, 1271-1283.).


Without wishing to be limited by theory, it is believed that 5-hydroxytryptamine receptor 7 receptor activity modulators of the present invention can ameliorate, abate, otherwise cause to be controlled, diseases associated with dysregulation of 5-hydroxytryptamine receptor 7 activity. The diseases include, but are not limited to circadian rhythm disorder, depression, schizophrenia, neurogenic inflammation, hypertension, peripheral, vascular diseases, migraine, neuropathic pain, peripheral pain, allodynia, thermoregulation disorder, learning disorder, memory disorder, hippocampal signaling disorder, sleep disorder, attention deficit/hyperactivity disorder, anxiety, avoidant personality disorder, premature ejaculation, eating disorder, premenstrual syndrome, premenstrual dysphonic disorder, seasonal affective disorder, bipolar disorder, inflammatory bowel disease (IBD), intestinal inflammation, epilepsy, seizure disorders, drug addiction, alcohol addiction, breast cancer, liver fibrosis, chronic liver injury, hepatocellular carcinoma, small intestine neuroendocrine tumors, and lung injury.


In embodiments, a disease is depression, schizophrenia, anxiety, or bipolar disorder. In embodiments, a disease is depression. In embodiments, a disease is schizophrenia. In embodiments, a disease is anxiety. In embodiments, a disease is bipolar disorder.


In embodiments, a disease is attention deficit/hyperactivity disorder.


In embodiments, a disease is avoidant personality disorder.


In embodiments, a disease is seasonal affective disorder.


In embodiments, a disease is circadian rhythm disorder or hippocampal signaling disorder. In embodiments, a disease is circadian rhythm disorder. In embodiments, a disease is hippocampal signaling disorder.


In embodiments, a disease is neurogenic inflammation.


In embodiments, a disease is neuropathic pain, peripheral pain, or allodynia. In embodiments, a disease is neuropathic pain. In embodiments, a disease is peripheral pain. In embodiments, a disease is allodynia.


In embodiments, a disease is migraine.


In embodiments, a disease is epilepsy or a seizure disorder. In embodiments, a disease is epilepsy. In embodiments, a disease is a seizure disorder.


In embodiments, a disease is a learning disorder or a memory disorder. In embodiments, a disease is a learning disorder. In embodiments, a disease is a memory disorder.


In embodiments, a disease is an eating disorder.


In embodiments, a disease is drug addiction or alcohol addiction.


In embodiments, a disease is a sleep disorder.


In embodiments, a disease is hypertension or peripheral vascular disease. In embodiments, a disease is hypertension. In embodiments, a disease is peripheral vascular disease.


In embodiments, a disease is thermoregulation disorder.


In embodiments, a disease is premature ejaculation.


In embodiments, a disease is premenstrual syndrome or premenstrual dysphonic disorder. In embodiments, a disease is premenstrual syndrome. In embodiments, a disease is premenstrual dysphonic disorder.


In embodiments, a disease is inflammatory bowel disease (IBD) or intestinal inflammation. In embodiments, a disease is inflammatory bowel disease (IBD). In embodiments, a disease is intestinal inflammation.


In embodiments, a disease is breast cancer.


In embodiments, a disease is liver fibrosis, chronic liver injury, or hepatocellular carcinoma. In embodiments, a disease is liver fibrosis. In embodiments, a disease is chronic liver injury. In embodiments, a disease is hepatocellular carcinoma.


In embodiments, a disease is a small intestine neuroendocrine tumor.


In embodiments, a disease is lung injury.


In embodiments, a disease is inflammatory bowel disease (IBD).


In embodiments, a compound described herein is a selective modulator of the serotonin 5HT7 receptor. In embodiments, a compound described herein can more potently bind a serotonin 5HT7 receptor as compared to other targets (e.g., other serotonin receptors). In embodiments, a compound may selectively bind a serotonin 5HT7 receptor in a particular tissue or organ.


In embodiments, compounds described herein may have particularly favorable properties for effective therapy (e.g., of any of the diseases or conditions described herein). For example, in the treatment of CNS or mental disorders, a compound described herein may exhibit favorably effective blood-brain barrier permeability. Alternatively, in the treatment of non-CNS or -mental disorders, a compound described herein will not have high blood-brain barrier permeability (e.g., off-target effects will be reduced). Without being bound by theory, molecular elements of a compound may be an effective strategy for obtaining the desired biological targeting.


For example, a compound described herein may selectively bind serotonin 5HT7 receptors in the intestine of a subject. Accordingly, a compound may be used to treat or prevent inflammatory bowel disease (IBD) or intestinal inflammation.


Throughout the description, where compositions are described as having, including, or comprising specific components, or where processes are described as having, including, or comprising specific process steps, it is contemplated that compositions of the present teachings also consist essentially of, or consist of, the recited components, and that the processes of the present teachings also consist essentially of, or consist of, the recited processing steps.


In the application, where an element or component is said to be included in and/or selected from a list of recited elements or components, it should be understood that the element or component can be any one of the recited elements or components and can be selected from a group consisting of two or more of the recited elements or components.


The use of the singular herein includes the plural (and vice versa) unless specifically stated otherwise. In addition, where the use of the term “about” is before a quantitative value, the present teachings also include the specific quantitative value itself, unless specifically stated otherwise.


It should be understood that the order of steps or order for performing certain actions is immaterial so long as the present teachings remain operable. Moreover, two or more steps or actions can be conducted simultaneously.


As used herein, the term “halogen” shall mean chlorine, bromine, fluorine and iodine.


As used herein, unless otherwise noted, “alkyl” and/or “aliphatic” whether used alone or as part of a substituent group refers to straight and branched carbon chains having 1 to 20 carbon atoms or any number within this range, for example 1 to 6 carbon atoms or 1 to 4 carbon atoms. Designated numbers of carbon atoms (e.g. C1-6) shall refer independently to the number of carbon atoms in an alkyl moiety or to the alkyl portion of a larger alkyl-containing substituent. Non-limiting examples of alkyl groups include methyl, ethyl, n-propyl, iso-propyl, n-butyl, sec-butyl, iso-butyl, tent-butyl, and the like. Alkyl groups can be optionally substituted. Non-limiting examples of substituted alkyl groups include hydroxymethyl, chloromethyl, trifluoromethyl, aminomethyl, 1-chloroethyl, 2-hydroxyethyl, 1,2-difluoroethyl, 3-carboxypropyl, and the like. In substituent groups with multiple alkyl groups such as (C1-6alkyl)2amino, the alkyl groups may be the same or different.


As used herein, the terms “alkenyl” and “alkynyl” groups, whether used alone or as part of a substituent group, refer to straight and branched carbon chains having 2 or more carbon atoms, preferably 2 to 20, wherein an alkenyl chain has at least one double bond in the chain and an alkynyl chain has at least one triple bond in the chain. Alkenyl and alkynyl groups can be optionally substituted. Nonlimiting examples of alkenyl groups include ethenyl, 3-propenyl, 1-propenyl (also 2-methylethenyl), isopropenyl (also 2-methylethen-2-yl), buten-4-yl, and the like. Nonlimiting examples of substituted alkenyl groups include 2-chloroethenyl (also 2-chlorovinyl), 4-hydroxybuten-1-yl, 7-hydroxy-7-methyloct-4-en-2-yl, 7-hydroxy-7-methyloct-3,5-dien-2-yl, and the like. Nonlimiting examples of alkynyl groups include ethynyl, prop-2-ynyl (also propargyl), propyn-1-yl, and 2-methyl-hex-4-yn-1-yl. Nonlimiting examples of substituted alkynyl groups include, 5-hydroxy-5-methylhex-3-ynyl, 6-hydroxy-6-methylhept-3-yn-2-yl, 5-hydroxy-5-ethylhept-3-ynyl, and the like.


As used herein, “cycloalkyl,” whether used alone or as part of another group, refers to a non-aromatic carbon-containing ring including cyclized alkyl, alkenyl, and alkynyl groups, e.g., having from 3 to 14 ring carbon atoms, preferably from 3 to 7 or 3 to 6 ring carbon atoms, or even 3 to 4 ring carbon atoms, and optionally containing one or more (e.g., 1, 2, or 3) double or triple bond. Cycloalkyl groups can be monocyclic (e.g., cyclohexyl) or polycyclic (e.g., containing fused, bridged, and/or spiro ring systems), wherein the carbon atoms are located inside or outside of the ring system. Any suitable ring position of the cycloalkyl group can be covalently linked to the defined chemical structure. Cycloalkyl rings can be optionally substituted. Nonlimiting examples of cycloalkyl groups include: cyclopropyl, 2-methyl-cyclopropyl, cyclopropenyl, cyclobutyl, 2,3-dihydroxycyclobutyl, cyclobutenyl, cyclopentyl, cyclopentenyl, cyclopentadienyl, cyclohexyl, cyclohexenyl, cycloheptyl, cyclooctanyl, decalinyl, 2,5-dimethylcyclopentyl, 3,5-dichlorocyclohexyl, 4-hydroxycyclohexyl, 3,3,5-trimethylcyclohex-1-yl, octahydropentalenyl, octahydro-1H-indenyl, 3a,4,5,6,7,7a-hexahydro-3H-inden-4-yl, decahydroazulenyl; bicyclo[6.2.0]decanyl, decahydronaphthalenyl, and dodecahydro-1H-fluorenyl. The term “cycloalkyl” also includes carbocyclic rings which are bicyclic hydrocarbon rings, non-limiting examples of which include, bicyclo-[2.1.1]hexanyl, bicyclo[2.2.1]heptanyl, bicyclo[3.1.1]heptanyl, 1,3-dimethyl[2.2.1]heptan-2-yl, bicyclo[2.2.2]octanyl, and bicyclo[3.3.3]undecanyl


“Haloalkyl” is intended to include both branched and straight-chain saturated aliphatic hydrocarbon groups having the specified number of carbon atoms, substituted with 1 or more halogen. Haloalkyl groups include perhaloalkyl groups, wherein all hydrogens of an alkyl group have been replaced with halogens (e.g., —CF3, —CF2CF3). Haloalkyl groups can optionally be substituted with one or more substituents in addition to halogen. Examples of haloalkyl groups include, but are not limited to, fluoromethyl, dichloroethyl, trifluoromethyl, trichloromethyl, pentafluoroethyl, and pentachloroethyl groups.


The term “alkoxy” refers to the group —O-alkyl, wherein the alkyl group is as defined above. Alkoxy groups optionally may be substituted. The term C3-C6 cyclic alkoxy refers to a ring containing 3 to 6 carbon atoms and at least one oxygen atom (e.g., tetrahydrofuran, tetrahydro-2H-pyran). C3-C6 cyclic alkoxy groups optionally may be substituted.


The term “haloalkoxy” refers to the group —O-haloalkyl, wherein the haloalkyl group is as defined above. Examples of haloalkoxy groups include, but are not limited to, fluoromethoxy, difluoromethoxy, trifluoromethoxy, and pentafluoroethoxyl.


The term “aryl,” wherein used alone or as part of another group, is defined herein as an unsaturated, aromatic monocyclic ring of 6 carbon members or to an unsaturated, aromatic polycyclic ring of from 10 to 14 carbon members. Aryl rings can be, for example, phenyl or naphthyl ring each optionally substituted with one or more moieties capable of replacing one or more hydrogen atoms. Non-limiting examples of aryl groups include: phenyl, naphthylen-1-yl, naphthylen-2-yl, 4-fluorophenyl, 2-hydroxyphenyl, 3-methylphenyl, 2-amino-4-fluorophenyl, 2-(N,N-diethylamino)phenyl, 2-cyanophenyl, 2,6-di-tert-butylphenyl, 3-methoxyphenyl, 8-hydroxynaphthylen-2-yl 4,5-dimethoxynaphthylen-1-yl, and 6-cyano-naphthylen-1-yl. Aryl groups also include, for example, phenyl or naphthyl rings fused with one or more saturated or partially saturated carbon rings (e.g., bicyclo[4.2.0]octa-1,3,5-trienyl, indanyl), which can be substituted at one or more carbon atoms of the aromatic and/or saturated or partially saturated rings.


The term “arylalkyl” or “aralkyl” refers to the group -alkyl-aryl, where the alkyl and aryl groups are as defined herein. Aralkyl groups of the present invention are optionally substituted. Examples of arylalkyl groups include, for example, benzyl, 1-phenylethyl, 2-phenylethyl, 3-phenylpropyl, 2-phenylpropyl, fluorenylmethyl and the like.


The terms “heterocyclic” and/or “heterocycle” and/or “heterocylyl,” whether used alone or as part of another group, are defined herein as one or more ring having from 3 to 20 atoms wherein at least one atom in at least one ring is a heteroatom selected from nitrogen (N), oxygen (O), or sulfur (S), and wherein further the ring that includes the heteroatom is non-aromatic. In heterocycle groups that include 2 or more fused rings, the non-heteroatom bearing ring may be aryl (e.g., indolinyl, tetrahydroquinolinyl, chromanyl). Exemplary heterocycle groups have from 3 to 14 ring atoms of which from 1 to 5 are heteroatoms independently selected from nitrogen (N), oxygen (O), or sulfur (S). One or more N or S atoms in a heterocycle group can be oxidized. Heterocycle groups can be optionally substituted.


Non-limiting examples of heterocyclic units having a single ring include: diazirinyl, aziridinyl, urazolyl, azetidinyl, pyrazolidinyl, imidazolidinyl, oxazolidinyl, isoxazolinyl, isoxazolyl, thiazolidinyl, isothiazolyl, isothiazolinyl oxathiazolidinonyl, oxazolidinonyl, hydantoinyl, tetrahydrofuranyl, pyrrolidinyl, morpholinyl, piperazinyl, piperidinyl, dihydropyranyl, tetrahydropyranyl, piperidin-2-onyl (valerolactam), 2,3,4,5-tetrahydro-1H-azepinyl, 2,3-dihydro-1H-indole, and 1,2,3,4-tetrahydro-quinoline. Non-limiting examples of heterocyclic units having 2 or more rings include: hexahydro-1H-pyrrolizinyl, 3a,4,5,6,7,7a-hexahydro-1H-benzo[d]imidazolyl, 3a,4,5,6,7,7a-hexahydro-1H-indolyl, 1,2,3,4-tetrahydroquinolinyl, chromanyl, isochromanyl, indolinyl, isoindolinyl, and decahydro-1H-cycloocta[b]pyrrolyl.


The term “heteroaryl,” whether used alone or as part of another group, is defined herein as one or more rings having from 5 to 20 atoms wherein at least one atom in at least one ring is a heteroatom chosen from nitrogen (N), oxygen (O), or sulfur (S), and wherein further at least one of the rings that includes a heteroatom is aromatic. In heteroaryl groups that include 2 or more fused rings, the non-heteroatom bearing ring may be a carbocycle (e.g., 6,7-Dihydro-5H-cyclopentapyrimidine) or aryl (e.g., benzofuranyl, benzothiophenyl, indolyl). Exemplary heteroaryl groups have from 5 to 14 ring atoms and contain from 1 to 5 ring heteroatoms independently selected from nitrogen (N), oxygen (O), or sulfur (S). One or more N or S atoms in a heteroaryl group can be oxidized. Heteroaryl groups can be substituted. Non-limiting examples of heteroaryl rings containing a single ring include: 1,2,3,4-tetrazolyl, [1,2,3]triazolyl, [1,2,4]triazolyl, triazinyl, thiazolyl, 1H-imidazolyl, oxazolyl, furanyl, thiopheneyl, pyrimidinyl, 2-phenylpyrimidinyl, pyridinyl, 3-methylpyridinyl, and 4-dimethylaminopyridinyl. Non-limiting examples of heteroaryl rings containing 2 or more fused rings include: benzofuranyl, benzothiophenyl, benzoxazolyl, benzthiazolyl, benztriazolyl, cinnolinyl, naphthyridinyl, phenanthridinyl, 7H-purinyl, 9H-purinyl, 6-amino-9H-purinyl, 5H-pyrrolo[3,2-d]pyrimidinyl, 7H-pyrrolo[2,3-d]pyrimidinyl, pyrido[2,3-d]pyrimidinyl, 2-phenylbenzo[d]thiazolyl, 1H-indolyl, 4,5,6,7-tetrahydro-1-H-indolyl, quinoxalinyl, 5-methylquinoxalinyl, quinazolinyl, quinolinyl, 8-hydroxy-quinolinyl, 1H-benzo[d]imidazol-2(3H)-onyl, 1H-benzo[d]imidazolyl, and isoquinolinyl.


One non-limiting example of a heteroaryl group as described above is C1-C5 heteroaryl, which has 1 to 5 carbon ring atoms and at least one additional ring atom that is a heteroatom (preferably 1 to 4 additional ring atoms that are heteroatoms) independently selected from nitrogen (N), oxygen (O), or sulfur (S). Examples of C1-C5 heteroaryl include, but are not limited to, triazinyl, thiazol-2-yl, thiazol-4-yl, imidazol-1-yl, 1H-imidazol-2-yl, 1H-imidazol-4-yl, isoxazolin-5-yl, furan-2-yl, furan-3-yl, thiophen-2-yl, thiophen-4-yl, pyrimidin-2-yl, pyrimidin-4-yl, pyrimidin-5-yl, pyridin-2-yl, pyridin-3-yl, and pyridin-4-yl.


Unless otherwise noted, when two substituents are taken together to form a ring having a specified number of ring atoms (e.g., R2 and R3 taken together with the nitrogen (N) to which they are attached to form a ring having from 3 to 7 ring members), the ring can have carbon atoms and optionally one or more (e.g., 1 to 3) additional heteroatoms independently selected from nitrogen (N), oxygen (O), or sulfur (S). The ring can be saturated or partially saturated and can be optionally substituted.


For the purposed of the present invention fused ring units, as well as spirocyclic rings, bicyclic rings and the like, which comprise a single heteroatom will be considered to belong to the cyclic family corresponding to the heteroatom containing ring. For example, 1,2,3,4-tetrahydroquinoline having the formula:




embedded image


is, for the purposes of the present invention, considered a heterocyclic unit. 6,7-Dihydro-5H-cyclopentapyrimidine having the formula:




embedded image


is, for the purposes of the present invention, considered a heteroaryl unit. When a fused ring unit contains heteroatoms in both a saturated and an aryl ring, the aryl ring will predominate and determine the type of category to which the ring is assigned. For example, 1,2,3,4-tetrahydro-[1,8]naphthyridine having the formula:




embedded image


is, for the purposes of the present invention, considered a heteroaryl unit.


Whenever a term or either of their prefix roots appear in a name of a substituent the name is to be interpreted as including those limitations provided herein. For example, whenever the term “alkyl” or “aryl” or either of their prefix roots appear in a name of a substituent (e.g., arylalkyl, alkylamino) the name is to be interpreted as including those limitations given above for “alkyl” and “aryl.”


The term “substituted” is used throughout the specification. The term “substituted” is defined herein as a moiety, whether acyclic or cyclic, which has one or more hydrogen atoms replaced by a substituent or several (e.g., 1 to 10) substituents as defined herein below. The substituents are capable of replacing one or two hydrogen atoms of a single moiety at a time. In addition, these substituents can replace two hydrogen atoms on two adjacent carbons to form said substituent, new moiety or unit. For example, a substituted unit that requires a single hydrogen atom replacement includes halogen, hydroxyl, and the like. A two hydrogen atom replacement includes carbonyl, oximino, and the like. A two hydrogen atom replacement from adjacent carbon atoms includes epoxy, and the like. The term “substituted” is used throughout the present specification to indicate that a moiety can have one or more of the hydrogen atoms replaced by a substituent. When a moiety is described as “substituted” any number of the hydrogen atoms may be replaced. For example, difluoromethyl is a substituted C1 alkyl; trifluoromethyl is a substituted C1 alkyl; 4-hydroxyphenyl is a substituted aromatic ring; (N,N-dimethyl-5-amino)octanyl is a substituted C8 alkyl; 3-guanidinopropyl is a substituted C3 alkyl; and 2-carboxypyridinyl is a substituted heteroaryl.


The variable groups defined herein, e.g., alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, aryloxy, aryl, heterocycle and heteroaryl groups defined herein, whether used alone or as part of another group, can be optionally substituted. Optionally substituted groups will be so indicated.


The following are non-limiting examples of substituents which can substitute for hydrogen atoms on a moiety: halogen (chlorine (Cl), bromine (Br), fluorine (F) and iodine(I)), —CN, —NO2, oxo (═O), —OR26, —SR26, —N(R26)2, —NR26C(O)R26, —SO2R26, —SO2OR26, —SO2N(R26)2, —C(O)R26, —C(O)OR26, —C(O)N(R26)2, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, C2-8 alkenyl, C2-8 alkynyl, C3-14 cycloalkyl, aryl, heterocycle, or heteroaryl, wherein each of the alkyl, haloalkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, aryl, heterocycle, and heteroaryl groups is optionally substituted with 1-10 (e.g., 1-6 or 1-4) groups selected independently from halogen, —CN, —NO2, oxo, and R26; wherein R26, at each occurrence, independently is hydrogen, —OR27, —SR27, —C(O)R27, —C(O)OR27, —C(O)N(R27)2, —SO2R27, —S(O)2OR27, —N(R27)2, —NR27C(O)R27, C1-6 alkyl, C1-6 haloalkyl, C2-8 alkenyl, C2-8 alkynyl, cycloalkyl (e.g., C3-6 cycloalkyl), aryl, heterocycle, or heteroaryl, or two R26 units taken together with the atom(s) to which they are bound form an optionally substituted carbocycle or heterocycle wherein said carbocycle or heterocycle has 3 to 7 ring atoms; wherein R27, at each occurrence, independently is hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-8 alkenyl, C2-8 alkynyl, cycloalkyl (e.g., C3-6 cycloalkyl), aryl, heterocycle, or heteroaryl, or two R27 units taken together with the atom(s) to which they are bound form an optionally substituted carbocycle or heterocycle wherein said carbocycle or heterocycle preferably has 3 to 7 ring atoms.


In some embodiments, the substituents are selected from

    • i) —OR28; for example, —OH, —OCH3, —OCH2CH3, —OCH2CH2CH3;
    • ii) —C(O)R28; for example, —COCH3, —COCH2CH3, —COCH2CH2CH3;
    • iii) —C(O)OR28; for example, —CO2CH3, —CO2CH2CH3, —CO2CH2CH2CH3;
    • iv) —C(O)N(R28)2; for example, —CONH2, —CONHCH3, —CON(CH3)2;
    • v) —N(R28)2; for example, —NH2, —NHCH3, —N(CH3)2, —NH(CH2CH3);
    • vi) halogen: —F, —Cl, —Br, and —I;
    • vii) —CHeXg; wherein X is halogen, m is from 0 to 2, e+g=3; for example, —CH2F, —CHF2, —CF3, —CCl3, or —CBr3;
    • viii) —SO2R28; for example, —SO2H; —SO2CH3; —SO2C6H5;
    • ix) C1-C6 linear, branched, or cyclic alkyl;
    • x) Cyano
    • xi) Nitro;
    • xii) N(R28)C(O)R28;
    • xiii) Oxo (═O);
    • xiv) Heterocycle; and
    • xv) Heteroaryl.


      wherein each R28 is independently hydrogen, optionally substituted C1-C6 linear or branched alkyl (e.g., optionally substituted C1-C4 linear or branched alkyl), or optionally substituted C3-C6 cycloalkyl (e.g optionally substituted C3-C4 cycloalkyl); or two R28 units can be taken together to form a ring comprising 3-7 ring atoms. In certain aspects, each R28 is independently hydrogen, C1-C6 linear or branched alkyl optionally substituted with halogen or C3-C6 cycloalkyl or C3-C6 cycloalkyl.


At various places in the present specification, substituents of compounds are disclosed in groups or in ranges. It is specifically intended that the description include each and every individual subcombination of the members of such groups and ranges. For example, the term “C1-6 alkyl” is specifically intended to individually disclose C1, C2, C3, C4, C5, C6, C1-C6, C1-C5, C1-C4, C1-C3, C1-C2, C2-C6, C2-C5, C2-C4, C2-C3, C3-C6, C3-C5, C3-C4, C4-C6, C4-C5, and C5-C6, alkyl.


For the purposes of the present invention the terms “compound,” “analog,” and “composition of matter” stand equally well for the 5-hydroxytryptamine receptor 7 activity modulators described herein, including all enantiomeric forms, diastereomeric forms, salts, and the like, and the terms “compound,” “analog,” and “composition of matter” are used interchangeably throughout the present specification.


Compounds described herein can contain an asymmetric atom (also referred as a chiral center), and some of the compounds can contain one or more asymmetric atoms or centers, which can thus give rise to optical isomers (enantiomers) and diastereomers. The present teachings and compounds disclosed herein include such enantiomers and diastereomers, as well as the racemic and resolved, enantiomerically pure R and S stereoisomers, as well as other mixtures of the R and S stereoisomers and pharmaceutically acceptable salts thereof. Optical isomers can be obtained in pure form by standard procedures known to those skilled in the art, which include, but are not limited to, diastereomeric salt formation, kinetic resolution, and asymmetric synthesis. The present teachings also encompass cis and trans isomers of compounds containing alkenyl moieties (e.g., alkenes and imines). It is also understood that the present teachings encompass all possible regioisomers, and mixtures thereof, which can be obtained in pure form by standard separation procedures known to those skilled in the art, and include, but are not limited to, column chromatography, thin-layer chromatography, and high-performance liquid chromatography.


Pharmaceutically acceptable salts of compounds of the present teachings, which can have an acidic moiety, can be formed using organic and inorganic bases. Both mono and polyanionic salts are contemplated, depending on the number of acidic hydrogens available for deprotonation. Suitable salts formed with bases include metal salts, such as alkali metal or alkaline earth metal salts, for example sodium, potassium, or magnesium salts; ammonia salts and organic amine salts, such as those formed with morpholine, thiomorpholine, piperidine, pyrrolidine, a mono-, di- or tri-lower alkylamine (e.g., ethyl-tert-butyl-, diethyl-, diisopropyl-, triethyl-, tributyl- or dimethylpropylamine), or a mono-, di-, or trihydroxy lower alkylamine (e.g., mono-, di- or triethanolamine). Specific non-limiting examples of inorganic bases include NaHCO3, Na2CO3, KHCO3, K2CO3, Cs2CO3, LiOH, NaOH, KOH, NaH2PO4, Na2HPO4, and Na3PO4. Internal salts also can be formed. Similarly, when a compound disclosed herein contains a basic moiety, salts can be formed using organic and inorganic acids. For example, salts can be formed from the following acids: acetic, propionic, lactic, benzenesulfonic, benzoic, camphorsulfonic, citric, tartaric, succinic, dichloroacetic, ethenesulfonic, formic, fumaric, gluconic, glutamic, hippuric, hydrobromic, hydrochloric, isethionic, lactic, maleic, malic, malonic, mandelic, methanesulfonic, mucic, napthalenesulfonic, nitric, oxalic, pamoic, pantothenic, phosphoric, phthalic, propionic, succinic, sulfuric, tartaric, toluenesulfonic, and camphorsulfonic as well as other known pharmaceutically acceptable acids.


When any variable occurs more than one time in any constituent or in any formula, its definition in each occurrence is independent of its definition at every other occurrence (e.g., in N(R9)2, each R9 may be the same or different than the other). Combinations of substituents and/or variables are permissible only if such combinations result in stable compounds.


The terms “treat” and “treating” and “treatment” as used herein, refer to partially or completely alleviating, inhibiting, ameliorating and/or relieving a condition from which a patient is suspected to suffer.


As used herein, “therapeutically effective” and “effective dose” refer to a substance or an amount that elicits a desirable biological activity or effect.


Except when noted, the terms “subject” or “patient” are used interchangeably and refer to mammals such as human patients and non-human primates, as well as experimental animals such as rabbits, rats, and mice, and other animals. Accordingly, the term “subject” or “patient” as used herein means any mammalian patient or subject to which the compounds of the invention can be administered. In an exemplary embodiment of the present invention, to identify subject patients for treatment according to the methods of the invention, accepted screening methods are employed to determine risk factors associated with a targeted or suspected disease or condition or to determine the status of an existing disease or condition in a subject. These screening methods include, for example, conventional work-ups to determine risk factors that may be associated with the targeted or suspected disease or condition. These and other routine methods allow the clinician to select patients in need of therapy using the methods and compounds of the present invention.


The 5-Hydroxytryptamine Receptor 7 Activity Modulators


The present invention is directed toward novel 5-hydroxytryptamine receptor 7 (5-HT7) activity modulators, compounds of formula (I),




embedded image


Including enantiomers, diastereomers, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, wherein:


A is selected from a group consisting of




embedded image


R1 is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl;


R2 is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl;


Or R1 and R2 are taken together with the atoms to which they are bound to form a ring having from 5 to 7 ring atoms, optionally containing a double bond;


Or R1 and R2 are taken together with the atoms to which they are bound to form a ring having from 6 to 8 ring atoms containing a moiety selected from the group consisting of O, S, SO, SO2, and NR7;


R3 is selected from the group consisting of optionally substituted phenyl, optionally substituted naphthylen-1-yl, optionally substituted naphthylen-2-yl, optionally substituted 2-pyridyl, optionally substituted 3-pyridyl, optionally substituted 4-pyridyl, and




embedded image


R4 is selected from the group consisting of optionally substituted phenyl, optionally substituted naphthylen-1-yl, optionally substituted naphthylen-2-yl, optionally substituted 2-pyridyl, optionally substituted 3-pyridyl, optionally substituted 4-pyridyl and




embedded image


R5 is selected from the group consisting of optionally substituted phenyl, optionally substituted naphthylen-1-yl, optionally substituted naphthylen-2-yl, optionally substituted 2-pyridyl, optionally substituted 3-pyridyl, optionally substituted 4-pyridyl and




embedded image


R6 is selected from the group consisting of optionally substituted phenyl, optionally substituted naphthylen-1-yl, optionally substituted naphthylen-2-yl, optionally substituted 2-pyridyl, optionally substituted 3-pyridyl, and optionally substituted 4-pyridyl;


R7 is selected from the group consisting of H, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, optionally substituted phenyl, optionally substituted benzyl, COR8, CO2R9, CONR10aR10b, SO2NR10aR10b, and SO2R10c;


R8 is selected from the group consisting of H, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;


R9 is selected from the group consisting of C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;


R10a is selected from the group consisting of H, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;


R10b is selected from the group consisting of H, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;


R10c is selected from the group consisting of C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear haloalkyl, C3-7 branched haloalkyl, —(CH2)qCN, —(CH2)qSO2R11, —(CH2)qOR12,




embedded image


R11 is selected from the group consisting of C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;


R12 is selected from the group consisting of C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;


R1a, R1b, R1c, R1d, and R1e are at each occurrence independently selected from the group consisting of H, OH, NO2, halogen, CN, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, —S(C1-6 linear alkyl), S(C3-7 branched alkyl), —S(C3-7 cycloalkyl), COR13, CO2R14, CONR15aR15b, SO2NR15aR15b, NR16aR16b, NR16aCOR17, NR16aSO2R18, and NR16aSO2NR19aR19b;


R13 is at each occurrence independently selected from the group consisting of H, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;


R14 is at each occurrence independently selected from the group consisting of C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;


R15d is at each occurrence independently selected from the group consisting of H, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;


R15b is at each occurrence independently selected from the group consisting of H, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;


R16a is at each occurrence independently selected from the group consisting of H, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;


R16b is at each occurrence independently selected from the group consisting of H, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;


R17 is at each occurrence independently selected from the group consisting of H, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;


R18 is at each occurrence independently selected from the group consisting of C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;


R19a is at each occurrence independently selected from the group consisting of C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;


R19b is at each occurrence independently selected from the group consisting of C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;


n is 1, 2, 3, or 4;


m is 1, 2, or 3.


In embodiments,


A is




embedded image


each R1 and R2 is independently C1-6 linear alkyl or C3-7 branched alkyl; or R1 and R2 are taken together with the atoms to which they are bound to form a 5- to 8-membered ring,

    • wherein said 5- to 8-membered ring is saturated or comprises a carbon-carbon double bond, and/or a ring atom that is O, S, SO, SO2, or NR7


each R3, R4, and R5 is independently optionally substituted phenyl, optionally optionally substituted 2-pyridyl, optionally substituted 3-pyridyl, or optionally substituted 4-pyridyl;


R6 is independently optionally substituted phenyl, optionally optionally substituted 2-pyridyl, optionally substituted 3-pyridyl, or optionally substituted 4-pyridyl;


R7 is independently H, C1-6 linear alkyl, C3-7 branched alkyl, COR8, or SO2R16c;


R8 is selected from the group consisting of H, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;


R16c is C1-6 linear alkyl or C3-7 branched alkyl;


n is 1, 2, 3, or 4; and


m is 1, 2, or 3.


In embodiments, n is 1, 2, or 3. In embodiments, n is 1. In embodiments, n is 2. In embodiments, n is 3.


The embodiments of the present invention include compounds having formula (II):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof.


In embodiments, a compound has the formula (XLII):




embedded image


or a pharmaceutically acceptable salt thereof.


In embodiments, a compound has the formula (XLIII):




embedded image


or a pharmaceutically acceptable salt thereof.


In embodiments, n is 1, 2, or 3. In embodiments, n is 1. In embodiments, n is 2. In embodiments, n is 3. In embodiments, n is 1 or 2.


In embodiments, each of R1 and R2 is unsubstituted C1-6 alkyl. In embodiments, each of R1 and R2 is ethyl. In embodiments, each of R1 and R2 is methyl.


In embodiments, R1 and R2 are taken together with the atoms to which they are bound to form a 5- to 8-membered ring, optionally containing one carbon-carbon double bonds and/or a ring atom selected from the group consisting of O, S, SO, SO2, and NR7.


In embodiments, R1 and R2 are taken together with the atoms to which they are bound to form a C3-C8 cycloalkyl or a C5-C8 cycloalkenyl.


In embodiments, R1 and R2 are taken together with the atoms to which they are bound to form a C3-C8 cycloalkyl or C5-C8 cycloalkenyl selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cycloheptenyl, cyclooctyl, and cyclooctenyl. In embodiments, said C3-C8 cycloalkyl or C5-C8 cycloalkenyl is unsubstituted. In embodiments, said C3-C8 cycloalkyl or C5-C8 cycloalkenyl is substituted by 1, 2, 3, or 4 substituents (e.g., 1 or 2 substituents as described herein). In embodiments, said substituents are selected from oxo (═O), hydroxyl, halo, cyano, C1-6 alkoxy, C1-6 linear alkyl, C3-7 branched alkyl, C1-6 haloalkyl, C3-8 cycloalkyl, and 3- to 8-membered heterocylyl. In embodiments, the substituents are selected from the group consisting of —OH, —F, —Cl, —Br, ——, —CN, —OMe, —OEt, —OnOPr, —OiPr, —OCF3, -Me, -Et, —nPr, —iPr, —CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.


In embodiments, a compound has a structure according to formula (XXXXIIIa):




embedded image


or


a pharmaceutically acceptable salt thereof, wherein custom-character represents a single or double bond.


In embodiments, custom-character represents a single bond.


In embodiments, custom-character represents a double bond.


In embodiments, the lactam stereocenter substituted by nitrogen has the R-configuration.


In embodiments, the lactam stereocenter substituted by nitrogen has the S-configuration.


In embodiments, R1 and R2 are taken together with the atoms to which they are bound to form a 5- to 8-membered ring containing a ring atom that is NR7. In embodiments, said 5- to 8-membered ring is not further substituted. In embodiments, said 5- to 8-membered ring further comprises 1, 2, 3, or 4 substituents (e.g., 1 or 2 substituents as described herein). In embodiments, said substituents are selected from oxo (═O), hydroxyl, halo, cyano, C1-6 alkoxy, C1-6 linear alkyl, C3-7 branched alkyl, C1-6 haloalkyl, C3-8 cycloalkyl, and 3- to 8-membered heterocylyl. In embodiments, the substituents are selected from the group consisting of —OH, —F, —Cl, —Br, —I, —CN, —OMe, —OEt, —OnPr, —OiPr, —OCF3, -Me, -Et, —nPr, —iPr, —CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.


In embodiments, R1 and R2 are taken together to form a pyrrolidinyl or piperidinyl group where the nitrogen atom is NR7. In embodiments, said pyrrolidinyl or piperidinyl group is not further substituted. In embodiments, said pyrrolidinyl or piperidinyl group further comprises 1, 2, 3, or 4 substituents as described herein.


In embodiments, a compound has the formula (XLIIIb)




embedded image


or a pharmaceutically acceptable salt thereof.


In embodiments, a compound has the formula (XLIV)




embedded image


or a pharmaceutically acceptable salt thereof.


In embodiments, a compound has the formula (XLV)




embedded image


or a pharmaceutically acceptable salt thereof.


In embodiments, n is 1, 2, or 3. In embodiments, n is 1. In embodiments, n is 2. In embodiments, n is 3. In embodiments, n is 1 or 2.


In embodiments, R7 is COR8, and R8 is C1-6 linear alkyl.


In embodiments, R7 is acetyl.


In embodiments, R7 is SO2R10c, and R10c is C1-6 linear alkyl.


In embodiments, R10c is methyl (i.e., R7 is SO2Me).


In embodiments, R3 is unsubstituted phenyl.


In embodiments, R3 is substituted phenyl. In embodiments, R3 is phenyl substituted by 1, 2, 3, 4, or 5 substituents (e.g., phenyl substituted by 1 or 2 substituents as described herein). In embodiments, the substitutents are selected from the group consisting of hydroxyl, halo, cyano, C1-6 alkoxy, C1-6 linear alkyl, C3-7 branched alkyl, C1-6 haloalkyl, C3-8 cycloalkyl, and 3- to 8-membered heterocylyl. In embodiments, the substituents are selected from the group consisting of —OH, —F, —Cl, —Br, —CN, —OMe, —OEt, —OnPr, —OiPr, —OCF3, -Me, -Et, —nPr, —iPr, —CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.


In embodiments, R3 is selected from the group consisting of hydroxylphenyl, fluorophenyl, chlorophenyl, bromophenyl, cyanophenyl, tolyl, methoxylphenyl, difluorophenyl, dichlorophenyl, chloro-fluorophenyl, dimethylphenyl, trifluoromethylphenyl, di(trifluoromethyl)phenyl,


In embodiments, R3 is selected from the group consisting of 4-hydroxyphenyl, 3-fluorophenyl, 4-fluorophenyl, 3-chlorophenyl, 4-chlorophenyl, 3,4-dichlorophenyl, 4-fluoro-3-chlorophenyl, 4-cyanophenyl, 2-methoxyphenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, 2-isopropylphenyl, 4-trifluoromethylphenyl, 2-morpholinophenyl, and 4-methyl-2-morpholinophenyl.


In embodiments, R3 is 2-pyridyl. In embodiments, R3 is 3-pyridyl. In embodiments, R3 is 4-pyridyl. In embodiments, said pyridyl is unsubstituted. In embodiments, said pyridyl is substituted by 1, 2, 3, or 4 substituents (e.g., pyridyl substituted by 1 or 2 substituents as described herein). In embodiments, the substitutents are selected from the group consisting of hydroxyl, halo, cyano, C1-6 alkoxy, C1-6 linear alkyl, C3-7 branched alkyl, C1-6 haloalkyl, C3-8 cycloalkyl, and 3- to 8-membered heterocylyl. In embodiments, the substituents are selected from the group consisting of —OH, —F, —Cl, —Br, —CN, —OMe, —OEt, —OnPr, —OiPr, —OCF3, -Me, -Et, —nPr, —iPr, —CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.


The embodiments of the present invention include compounds having formula (IIa):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, R20d, and R20e are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;



and at least 3 of R20a, R20b, R20c, R20d, and R20e are hydrogen.


The embodiments of the present invention include compounds having formula (IIb):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;


and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIc):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IId):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IId-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IId-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IId-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IId-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IId-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIe):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, and R20d are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 3 of R20a, R20b, R20c, and R20d are hydrogen.



The embodiments of the present invention include compounds having formula (IIf):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIg):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIh):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIh-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIh-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIh-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIh-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIh-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (III):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, and R20e are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl; and at least 2 of R20a, R20b, R20c, and R20e are hydrogen.



The embodiments of the present invention include compounds having formula (IIj):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIk):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIL):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIL-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


    The embodiments of the present invention include compounds having formula (IIL-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIL-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIL-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIL-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIm):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20cd, and R20e are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl; and at least 3 of R20a, R20b, R20c, and R20d are hydrogen.



The embodiments of the present invention include compounds having formula (IIn):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIo):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIp):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIp-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIp-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIp-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIp-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIp-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIq):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, R20d, R20e, R20f, and R20g are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 5 of R20a, R20b, R20c, R20d, R20e, R20f, and R20 are hydrogen.



The embodiments of the present invention include compounds having formula (IIr):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Hs):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIt):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein X1 is selected from the group consisting of O, S, SO, SO2, and NR7;

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIt-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIt-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIt-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIt-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIt-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIu):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, R20d, R20e, R20f, and R20g are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 5 of R20a, R20b, R20c, R20d, R20e, R20f, and R20g are hydrogen.



The embodiments of the present invention include compounds having formula (IIv):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIw):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIx):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIx-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIx-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIx-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIx-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIx-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (III):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof.


The embodiments of the present invention include compounds having formula (IIIa):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, R20d, and R20e are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6

  • linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 3 of R20a, R20b, R20c, R20d, and R20e are hydrogen.



The embodiments of the present invention include compounds having formula (IIIb):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIc):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIId):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein X1 is selected from the group consisting of O, S, SO, SO2, and NR7;

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIId-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIId-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIId-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIId-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIId-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIe):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, and R20d are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 2 of R20a, R20b, R20c, and R20d are hydrogen.



The embodiments of the present invention include compounds having formula (IIIf):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIg):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIh):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIh-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIh-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIh-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIh-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIh-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIi):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, and R20e are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 2 of R20a, R20b, R20c, and R20e are hydrogen.



The embodiments of the present invention include compounds having formula (IIIj):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIk):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIL):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIL-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIL-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIL-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIL-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIL-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20d, and R20e are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 2 of R20a, R20b, R20c, and R20d are hydrogen.



The embodiments of the present invention include compounds having formula (IIIn):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIo):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIp):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIp-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIp-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIp-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIp-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIp-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIq):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, R20d, R20e, R20f, and R20g are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 5 of R20a, R20b, R20c, R20d, R20e, R20f, and R20g are hydrogen.



The embodiments of the present invention include compounds having formula (IIIr):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIs):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIt):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIt-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIt-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIt-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIt-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIt-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIu):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, R20d, R20e, R20f, and R20g are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 5 of R20a, R20b, R20c, R20d, R20e, R20f, and R20g are hydrogen.



The embodiments of the present invention include compounds having formula (IIIv):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIw):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIx):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIx-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIx-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIx-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIx-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IIIx-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IV):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof.


In embodiments, a compound has a structure according to Formula (XLVII),




embedded image


or a pharmaceutically acceptable salt thereof.


In embodiments, a compound has a structure according to Formula (XLVII),




embedded image


or a pharmaceutically acceptable salt thereof.


In embodiments, n is 1, 2, or 3. In embodiments, n is 1. In embodiments, n is 2. In embodiments, n is 1 or 2.


In embodiments, each of R1 and R2 is unsubstituted C1-6 alkyl. In embodiments, each of R1 and R2 is ethyl. In embodiments, each of R1 and R2 is methyl.


In embodiments, R1 and R2 are taken together with the atoms to which they are bound to form a 5- to 8-membered ring, optionally containing one carbon-carbon double bonds and/or a ring atom selected from the group consisting of O, S, SO, SO2, and NR7.


In embodiments, R1 and R2 are taken together with the atoms to which they are bound to form a C3-C8 cycloalkyl or a C5-C8 cycloalkenyl.


In embodiments, R1 and R2 are taken together with the atoms to which they are bound to form a C3-C8 cycloalkyl or C5-C8 cycloalkenyl selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cycloheptenyl, cyclooctyl, and cyclooctenyl. In embodiments, said C3-C8 cycloalkyl or C5-C8 cycloalkenyl is unsubstituted. In embodiments, said C3-C8 cycloalkyl or C5-C8 cycloalkenyl is substituted by 1, 2, 3, or 4 substituents (e.g., 1 or 2 substituents as described herein). In embodiments, said substituents are selected from oxo (═O), hydroxyl, halo, cyano, C1-6 alkoxy, C1-6 linear alkyl, C3-7 branched alkyl, C1-6 haloalkyl, C3-8 cycloalkyl, and 3- to 8-membered heterocylyl. In embodiments, the substituents are selected from the group consisting of—OH, —F, —Cl, —Br, ——, —CN, —OMe, —OEt, —OnPr, —OiPr, —OCF3, -Me, -Et, —nPr, —iPr, —CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.


In embodiments, R1 and R2 are taken together with the atoms to which they are bound to form a 5- to 8-membered ring containing a ring atom that is NR7. In embodiments, said 5- to 8-membered ring is not further substituted. In embodiments, said 5- to 8-membered ring further comprises 1, 2, 3, or 4 substituents (e.g., 1 or 2 substituents as described herein). In embodiments, said substituents are selected from oxo (═O), hydroxyl, halo, cyano, C1-6 alkoxy, C1-6 linear alkyl, C3-7 branched alkyl, C1-6 haloalkyl, C3-8 cycloalkyl, and 3- to 8-membered heterocylyl. In embodiments, the substituents are selected from the group consisting of —OH, —F, —Cl, —Br, —I, —CN, —OMe, —OEt, —OnPr, —OiPr, —OCF3, -Me, -Et, —nPr, —iPr, —CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.


In embodiments, R1 and R2 are taken together to form a pyrrolidinyl or piperidinyl group where the nitrogen atom is NR7. In embodiments, said pyrrolidinyl or piperidinyl group is not further substituted. In embodiments, said pyrrolidinyl or piperidinyl group further comprises 1, 2, 3, or 4 substituents as described herein.


In embodiments, R7 is COR8, and R8 is C1-6 linear alkyl.


In embodiments, R7 is acetyl.


In embodiments, R7 is SO2R10c, and R10c is C1-6 linear alkyl.


In embodiments, R10c is methyl (i.e., R7 is SO2Me).


In embodiments, R4 is phenyl.


In embodiments, R4 is substituted phenyl. In embodiments, R4 is phenyl substituted by 1, 2, 3, 4, or 5 substituents (e.g., phenyl substituted by 1 or 2 substituents as described herein). In embodiments, the substitutents are selected from the group consisting of hydroxyl, halo, cyano, C1-6 alkoxy, C1-6 linear alkyl, C3-7 branched alkyl, C1-6 haloalkyl, C3-8 cycloalkyl, and 3- to 8-membered heterocylyl. In embodiments, the substituents are selected from the group consisting of —OH, —F, —Cl, —Br, —CN, —OMe, —OEt, —OnPr, —OiPr, —OCF3, -Me, -Et, —nPr, —iPr, —CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.


In embodiments, R4 is selected from the group consisting of hydroxylphenyl, fluorophenyl, chlorophenyl, bromophenyl, cyanophenyl, tolyl, methoxylphenyl, difluorophenyl, dichlorophenyl, chloro-fluorophenyl, dimethylphenyl, trifluoromethylphenyl, di(trifluoromethyl)phenyl,


In embodiments, R4 is selected from the group consisting of 4-hydroxyphenyl, 3-fluorophenyl, 4-fluorophenyl, 3-chlorophenyl, 4-chlorophenyl, 3,4-dichlorophenyl, 4-fluoro-3-chlorophenyl, 4-cyanophenyl, 2-methoxyphenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, 2-isopropylphenyl, 4-trifluoromethylphenyl, 2-morpholinophenyl, and 4-methyl-2-morpholinophenyl.


In embodiments, R4 is pyridyl. In embodiments, R4 is 2-pyridyl. In embodiments, R4 is 3-pyridyl. In embodiments, R4 is 4-pyridyl. In embodiments, said pyridyl is unsubstituted. In embodiments, said pyridyl is substituted by 1, 2, 3, or 4 substituents (e.g., pyridyl substituted by 1 or 2 substituents as described herein). In embodiments, the substitutents are selected from the group consisting of hydroxyl, halo, cyano, C1-6 alkoxy, C1-6 linear alkyl, C3-7 branched alkyl, C1-6 haloalkyl, C3-8 cycloalkyl, and 3- to 8-membered heterocylyl. In embodiments, the substituents are selected from the group consisting of —OH, —F, —Cl, —Br, —I, —CN, —OMe, —OEt, —OnPr, —OiPr, —OCF3, -Me, -Et, —nPr, —iPr, —CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.


The embodiments of the present invention include compounds having formula (IVa):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, R20d, and R20e are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 3 of R20a, R20b, R20c, R20d, and R20e are hydrogen.



The embodiments of the present invention include compounds having formula (IVb):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVc):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVd):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVd-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVd-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVd-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVd-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVd-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVe):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, and R20d are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 2 of R20a, R20b, R20c, and R20d are hydrogen.



The embodiments of the present invention include compounds having formula (IVf):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVg):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVh):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein X1 is selected from the group consisting of O, S, SO, SO2, and NR7;

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVh-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVh-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVh-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVh-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVh-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVi):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, and R20e are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 2 of R20a, R20b, R20c, and R20e are hydrogen.



The embodiments of the present invention include compounds having formula (IVj):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVk):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVL):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVL-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVL-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVL-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVL-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVL-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVm):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20d, and R20e are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 2 of R20a, R20b, R20c, and R20d are hydrogen.



The embodiments of the present invention include compounds having formula (IVn):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVo):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVp):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVp-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVp-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVp-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVp-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVp-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVq):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, R20d, R20e, R20f, and R20g are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 5 of R20a, R20b, R20c, R20d, R20e, R20f, and R20g are hydrogen.



The embodiments of the present invention include compounds having formula (IVr):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVs):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVt):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVt-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVt-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVt-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVt-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVt-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVu):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, R20d, R20e, R20f, and R20g are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 5 of R20a, R20b, R20c, R20d, R20e, R20f, and R20g are hydrogen.



The embodiments of the present invention include compounds having formula (IVv):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVw):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVx):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVx-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVx-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVx-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVx-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (IVx-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (V):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof.


The embodiments of the present invention include compounds having formula (Va):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, R20d, and R20e are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23bNHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 3 of R20a, R20b, R20c, R20d, and R20e are hydrogen.



The embodiments of the present invention include compounds having formula (Vb):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vc):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vd):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vd-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vd-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vd-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vd-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vd-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Ve):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, and R20d are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 2 of R20a, R20b, R20c, and R20d are hydrogen.



The embodiments of the present invention include compounds having formula (Vf):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vg):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vh):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vh-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vh-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vh-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vh-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vh-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vi):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, and R20e are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 2 of R20a, R20b, R20c, and R20e are hydrogen.



The embodiments of the present invention include compounds having formula (Vj):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vk):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VL):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VL-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VL-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VL-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VL-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VL-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vm):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20d, and R20e are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 2 of R20a, R20b, R20c, and R20d are hydrogen.



The embodiments of the present invention include compounds having formula (Vn):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vo):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vp):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vp-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vp-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vp-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vp-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vp-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vq):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, R20d, R20e, R20f, and R20g are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 5 of R20a, R20b, R20c, R20d, R20e, R20f, and R20g are hydrogen.



The embodiments of the present invention include compounds having formula (Vr):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vs):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vt):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vt-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vt-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vt-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vt-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vt-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vu):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, R20d, R20e, R20f, and R20g are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;
  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;
  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;
  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;
  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;
  • and at least 5 of R20a, R20b, R20c, R20d, R20e, R20f, and R20g are hydrogen.


The embodiments of the present invention include compounds having formula (Vv):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vw):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vx):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vx-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vx-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vx-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vx-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vx-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VI):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof.


In embodiments, a compound has a structure according to Formula (XLVI)




embedded image


or a pharmaceutically acceptable salt thereof.


In embodiments, a compound has a structure according to Formula (XLVIa)




embedded image


or a pharmaceutically acceptable salt thereof.


In embodiments, n is 1, 2, or 3. In embodiments, n is 1. In embodiments, n is 2. In embodiments, n is 1 or 2.


In embodiments, each of R1 and R2 is unsubstituted C1-6 alkyl. In embodiments, each of R1 and R2 is ethyl. In embodiments, each of R1 and R2 is methyl.


In embodiments, R1 and R2 are taken together with the atoms to which they are bound to form a 5- to 8-membered ring, optionally containing one carbon-carbon double bonds and/or a ring atom selected from the group consisting of O, S, SO, SO2, and NR7.


In embodiments, R1 and R2 are taken together with the atoms to which they are bound to form a C3-C8 cycloalkyl or a C5-C8 cycloalkenyl.


In embodiments, R1 and R2 are taken together with the atoms to which they are bound to form a C3-C8 cycloalkyl or C5-C8 cycloalkenyl selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cycloheptenyl, cyclooctyl, and cyclooctenyl. In embodiments, said C3-C8 cycloalkyl or C5-C8 cycloalkenyl is unsubstituted. In embodiments, said C3-C8 cycloalkyl or C5-C8 cycloalkenyl is substituted by 1, 2, 3, or 4 substituents (e.g., 1 or 2 substituents as described herein). In embodiments, said substituents are selected from oxo (═O), hydroxyl, halo, cyano, C1-6 alkoxy, C1-6 linear alkyl, C3-7 branched alkyl, C1-6 haloalkyl, C3-8 cycloalkyl, and 3- to 8-membered heterocylyl. In embodiments, the substituents are selected from the group consisting of —OH, —F, —Cl, —Br, —I, —CN, —OMe, —OEt, —OnPr, —OiPr, —OCF3, -Me, -Et, —nPr, —iPr, —CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.


In embodiments, R1 and R2 are taken together with the atoms to which they are bound to form a 5- to 8-membered ring containing a ring atom that is NR7. In embodiments, said 5- to 8-membered ring is not further substituted. In embodiments, said 5- to 8-membered ring further comprises 1, 2, 3, or 4 substituents (e.g., 1 or 2 substituents as described herein). In embodiments, said substituents are selected from oxo (═O), hydroxyl, halo, cyano, C1-6 alkoxy, C1-6 linear alkyl, C3-7 branched alkyl, C1-6 haloalkyl, C3-8 cycloalkyl, and 3- to 8-membered heterocylyl. In embodiments, the substituents are selected from the group consisting of —OH, —F, —Cl, —Br, —I, —CN, —OMe, —OEt, —OnPr, —OiPr, —OCF3, -Me, -Et, —nPr, —iPr, —CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.


In embodiments, R1 and R2 are taken together to form a pyrrolidinyl or piperidinyl group where the nitrogen atom is NR7. In embodiments, said pyrrolidinyl or piperidinyl group is not further substituted. In embodiments, said pyrrolidinyl or piperidinyl group further comprises 1, 2, 3, or 4 substituents as described herein.


In embodiments, R7 is COR8, and R8 is C1-6 linear alkyl.


In embodiments, R7 is acetyl.


In embodiments, R7 is SO2R10c, and R10c s C1-6 linear alkyl.


In embodiments, R10c is methyl (i.e., R7 is SO2Me).


In embodiments, R5 is phenyl.


In embodiments, R5 is substituted phenyl. In embodiments, R5 is phenyl substituted by 1, 2, 3, 4, or 5 substituents (e.g., phenyl substituted by 1 or 2 substituents as described herein). In embodiments, the substitutents are selected from the group consisting of hydroxyl, halo, cyano, C1-6 alkoxy, C1-6 linear alkyl, C3-7 branched alkyl, C1-6 haloalkyl, C3-8 cycloalkyl, and 3- to 8-membered heterocylyl. In embodiments, the substituents are selected from the group consisting of —OH, —F, —Cl, —Br, —CN, —OMe, —OEt, —OnPr, —OiPr, —OCF3, -Me, -Et, —nPr, —iPr, —CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.


In embodiments, R5 is selected from the group consisting of hydroxylphenyl, fluorophenyl, chlorophenyl, bromophenyl, cyanophenyl, tolyl, methoxylphenyl, difluorophenyl, dichlorophenyl, chloro-fluorophenyl, dimethylphenyl, trifluoromethylphenyl, di(trifluoromethyl)phenyl,


In embodiments, R5 is selected from the group consisting of 4-hydroxyphenyl, 3-fluorophenyl, 4-fluorophenyl, 3-chlorophenyl, 4-chlorophenyl, 3,4-dichlorophenyl, 4-fluoro-3-chlorophenyl, 4-cyanophenyl, 2-methoxyphenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, 2-isopropylphenyl, 4-trifluoromethylphenyl, 2-morpholinophenyl, and 4-methyl-2-morpholinophenyl.


In embodiments, R5 is pyridyl. In embodiments, R5 is 2-pyridyl. In embodiments, R5 is 3-pyridyl. In embodiments, R5 is 4-pyridyl. In embodiments, said pyridyl is unsubstituted. In embodiments, said pyridyl is substituted by 1, 2, 3, or 4 substituents (e.g., pyridyl substituted by 1 or 2 substituents as described herein). In embodiments, the substitutents are selected from the group consisting of hydroxyl, halo, cyano, C1-6 alkoxy, C1-6 linear alkyl, C3-7 branched alkyl, C1-6 haloalkyl, C3-8 cycloalkyl, and 3- to 8-membered heterocylyl. In embodiments, the substituents are selected from the group consisting of —OH, —F, —Cl, —Br, —I, —CN, —OMe, —OEt, —OnPr, —OiPr, —OCF3, -Me, -Et, —nPr, —iPr, —CF3, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, and morpholino.


The embodiments of the present invention include compounds having formula (VIa):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, R20d, and R20e are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 3 of R20a, R20b, R20c, R20d, and R20e are hydrogen.



The embodiments of the present invention include compounds having formula (VIb):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIc):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VId):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vid-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vid-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vid-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vid-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (Vid-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIe):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, and R20d are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 2 of R20a, R20b, R20c, and R20d are hydrogen.



The embodiments of the present invention include compounds having formula (VIf):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIg):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIh):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein X1 is selected from the group consisting of O, S, SO, SO2, and NR7;

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIh-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIh-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIh-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIh-):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIh-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIi):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, and R20e are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 2 of R20a, R20b, R20c, and R20e are hydrogen.



The embodiments of the present invention include compounds having formula (VIj):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIk):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIL):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIL-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIL-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIL-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIL-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIL-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIm):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20d, and R20e are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 2 of R20a, R20b, R20c, and R20d are hydrogen.



The embodiments of the present invention include compounds having formula (VIn):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIo):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIp):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIp-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIp-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIp-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIp-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIp-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIq):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, R20d, R20e, R20f, and R20g are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 5 of R20a, R20b, R20c, R20d, R20e, R20f, and R20g are hydrogen.



The embodiments of the present invention include compounds having formula (VIr):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIs):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIt):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIt-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIt-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIt-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIt-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIt-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIu):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, R20d, R20e, R20f, and R20g are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 5 of R20a, R20b, R20c, R20d, R20e, R20f, and R20g are hydrogen.



The embodiments of the present invention include compounds having formula (VIv):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIw):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIx):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIx-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIx-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIx-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIx-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIx-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VII):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof


The embodiments of the present invention include compounds having formula (VIIa):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, R20d, and R20e are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 3 of R20a, R20b, R20c, R20d, and R20e are hydrogen.



The embodiments of the present invention include compounds having formula (VIIb):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIc):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIId):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIId-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIId-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIId-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIId-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIId-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIe):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, and R20d are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7 cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 2 of R20a, R20b, R20c, and R20d are hydrogen.



The embodiments of the present invention include compounds having formula (VIIf):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIg):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIh):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIh-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIh-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIh-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIh-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIh-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIII):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, and R20e are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 2 of R20a, R20b, R20c, and R20e are hydrogen.



The embodiments of the present invention include compounds having formula (VIIj):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIk):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIL):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIL-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIL-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIL-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIL-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIL-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIm):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20d, and R20e are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 2 of R20a, R20b, R20c, and R20d are hydrogen.



The embodiments of the present invention include compounds having formula (VIIn):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIo):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIp):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIp-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIp-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIp-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIp-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIp-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIq):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, R20d, R20e, R20f, and R20g are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7cycloalkyl, SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23b, NHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 5 of R20a, R20b, R20c, R20d, R20e, R20f, and R20g are hydrogen.



The embodiments of the present invention include compounds having formula (VIIr):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIs):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIt):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein X1 is selected from the group consisting of O, S, SO, SO2, and NR7;

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIt-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIt-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIt-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIt-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIt-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIu):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • R20a, R20b, R20c, R20d, R20e, R20f, and R20g are independently selected from the group consisting of hydrogen, —CN, —NO2, —OH, halogen, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, C3-7 branched haloalkoxy, SH, SC1-6 linear alkyl, SC3-7 branched alkyl, SC3-7cycloalkyl, SO2C1-6 linear alkyl, SO2C3-7 branched alkyl, SO2C3-7 cycloalkyl SO2NH2, SO2NHR21, NHSO2R22, —NR23aR23bNHC(O)R24, C(O)NHR24, C(O)N(R24)2, morpholino, and




embedded image


  • R21 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R22 at each occurrence is independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23a at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R23b at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R24 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • R25 at each occurrence is independently is selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;

  • and at least 5 of R20a, R20b, R20c, R20d, R20e, R20f, and R20g are hydrogen.



The embodiments of the present invention include compounds having formula (VIIv):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIw):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIx):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • X1 is selected from the group consisting of O, S, SO, SO2, and NR7;
  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIx-1):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIx-2):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIx-3):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIx-4):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


The embodiments of the present invention include compounds having formula (VIIx-5):




embedded image


Including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, and complexes thereof wherein

  • Q1 is 1 or 2;
  • and Q2 is 1 or 2.


In some embodiments A is




embedded image


In some embodiments A is




embedded image


In some embodiments A is




embedded image


In some embodiments R1 is hydrogen.


In some embodiments R1 is C1-6 linear alkyl.


In some embodiments R1 is C3-7 branched alkyl.


In some embodiments R2 is hydrogen.


In some embodiments R2 is C1-6 linear alkyl.


In some embodiments R2 is C3-7 branched alkyl.


In some embodiments R1 and R2 are taken together with the atoms to which they are bound to form a ring having 5 ring atoms.


In some embodiments R1 and R2 are taken together with the atoms to which they are bound to form a ring having 5 ring atoms and containing a double bond.


In some embodiments R1 and R2 are taken together with the atoms to which they are bound to form a ring having 6 ring atoms.


In some embodiments R1 and R2 are taken together with the atoms to which they are bound to form a ring having 6 ring atoms and containing a double bond.


In some embodiments R1 and R2 are taken together with the atoms to which they are bound to form a ring having 7 ring atoms.


In some embodiments R1 and R2 are taken together with the atoms to which they are bound to form a ring having 7 ring atoms and containing a double bond.


In some embodiments R1 and R2 are taken together with the atoms to which they are bound to form a ring having 6 ring atoms containing one of which is O.


In some embodiments R1 and R2 are taken together with the atoms to which they are bound to form a ring having 7 ring atoms containing one of which is O.


In some embodiments R1 and R2 are taken together with the atoms to which they are bound to form a ring having 8 ring atoms containing one of which is O.


In some embodiments R1 and R2 are taken together with the atoms to which they are bound to form a ring having 6 ring atoms containing one of which is S.


In some embodiments R1 and R2 are taken together with the atoms to which they are bound to form a ring having 7 ring atoms containing one of which is S.


In some embodiments R1 and R2 are taken together with the atoms to which they are bound to form a ring having 8 ring atoms containing one of which is S.


In some embodiments R1 and R2 are taken together with the atoms to which they are bound to form a ring having 6 ring atoms containing one of which is SO.


In some embodiments R1 and R2 are taken together with the atoms to which they are bound to form a ring having 7 ring atoms containing one of which is SO.


In some embodiments R1 and R2 are taken together with the atoms to which they are bound to form a ring having 8 ring atoms containing one of which is SO.


In some embodiments R1 and R2 are taken together with the atoms to which they are bound to form a ring having 6 ring atoms containing one of which is SO2.


In some embodiments R1 and R2 are taken together with the atoms to which they are bound to form a ring having 7 ring atoms containing one of which is SO2.


In some embodiments R1 and R2 are taken together with the atoms to which they are bound to form a ring having 8 ring atoms containing one of which is SO2.


In some embodiments R1 and R2 are taken together with the atoms to which they are bound to form a ring having 6 ring atoms containing one of which is NR7.


In some embodiments R1 and R2 are taken together with the atoms to which they are bound to form a ring having 7 ring atoms containing one of which is NR7.


In some embodiments R1 and R2 are taken together with the atoms to which they are bound to form a ring having 8 ring atoms containing one of which is NR7.


In some embodiments R3 is optionally substituted phenyl.


In some embodiments R3 is optionally substituted naphthylen-1-yl.


In some embodiments R3 is optionally substituted naphthylen-2-yl.


In some embodiments R3 is optionally substituted 2-pyridyl


In some embodiments R3 is optionally substituted 3-pyridyl.


In some embodiments R3 is optionally substituted 4-pyridyl.


In some embodiments R3 is




embedded image


In some embodiments R4 is optionally substituted phenyl.


In some embodiments R4 is optionally substituted naphthylen-1-yl.


In some embodiments R4 is optionally substituted naphthylen-2-yl.


In some embodiments R4 is optionally substituted 2-pyridyl


In some embodiments R4 is optionally substituted 3-pyridyl.


In some embodiments R4 is optionally substituted 4-pyridyl.


In some embodiments R4 is




embedded image


In some embodiments R5 is optionally substituted phenyl.


In some embodiments R5 is optionally substituted naphthylen-1-yl.


In some embodiments R5 is optionally substituted naphthylen-2-yl.


In some embodiments R5 is optionally substituted 2-pyridyl


In some embodiments R5 is optionally substituted 3-pyridyl.


In some embodiments R5 is optionally substituted 4-pyridyl.


In some embodiments R5 is




embedded image


In some embodiments R6 is optionally substituted phenyl.


In some embodiments R6 is optionally substituted naphthylen-1-yl.


In some embodiments R6 is optionally substituted naphthylen-2-yl.


In some embodiments R6 is optionally substituted 2-pyridyl


In some embodiments R6 is optionally substituted 3-pyridyl.


In some embodiments R6 is optionally substituted 4-pyridyl.


In some embodiments R7 is H.


In some embodiments R7 is C1-6 linear alkyl.


In some embodiments R7 is C3-7 branched alkyl.


In some embodiments R7 is C3-7 cycloalkyl.


In some embodiments R7 is optionally substituted phenyl.


In some embodiments R7 is optionally substituted benzyl.


In some embodiments R7 is COR8.


In some embodiments R7 is CO2R9.


In some embodiments R7 is CONR10aR10b.


In some embodiments R7 is SO2NR10aR10b.


In some embodiments R7 is SO2R10c.


In some embodiments R8 is selected H.


In some embodiments R8 is C1-6 linear alkyl.


In some embodiments R8 is C3-7 branched alkyl


In some embodiments R8 is C3-7 cycloalkyl.


In some embodiments R9 is C1-6 linear alkyl.


In some embodiments R9 is C3-7 branched alkyl.


In some embodiments R9 is C3-7 cycloalkyl.


In some embodiments R10a is H.


In some embodiments R10a is C1-6 linear alkyl.


In some embodiments R10a is C3-7 branched alkyl.


In some embodiments R10a is C3-7 cycloalkyl.


In some embodiments R10b is H.


In some embodiments R10b is C1-6 linear alkyl.


In some embodiments R10b is C3-7 branched alkyl.


In some embodiments R10b is C3-7 cycloalkyl.


In some embodiments R10c is C1-6 linear alkyl.


In some embodiments R10c is C3-7 branched alkyl.


In some embodiments R10c is C3-7 cycloalkyl.


In some embodiments R10c is C1-6 linear haloalkyl.


In some embodiments R10c is C3-7 branched haloalkyl.


In some embodiments R10c is —(CH2)qCN.


In some embodiments R10c is —(CH2)qSO2R11.


In some embodiments R10c is —(CH2)qOR12.


In some embodiments R10c s




embedded image


In some embodiments R10c s




embedded image


In some embodiments R10c s




embedded image


In some embodiments R10c s




embedded image


In some embodiments R10c s




embedded image


In some embodiments R10c is




embedded image


In some embodiments R10c s




embedded image


In some embodiments R10c is




embedded image


In some embodiments R10c s




embedded image


In some embodiments R10c s




embedded image


In some embodiments R10c is




embedded image


In some embodiments R10c is




embedded image


In some embodiments R11 C1-6 linear alkyl.


In some embodiments R11 C3-7 branched alkyl.


In some embodiments R11 C3-7 cycloalkyl.


In some embodiments R12 is C1-6 linear alkyl.


In some embodiments R12 is C3-7 branched alkyl.


In some embodiments R12 is C3-7 cycloalkyl.


In some embodiments R1a is H.


In some embodiments R1a is OH


In some embodiments R1a is NO2.


In some embodiments R1a is halogen.


In some embodiments R1a is CN.


In some embodiments R1a is C1-6 linear alkyl.


In some embodiments R1a is C3-7 branched alkyl.


In some embodiments R1a is C3-7 cycloalkyl.


In some embodiments R1a is C1-6 linear alkoxy.


In some embodiments R1a is C3-7 branched alkoxy.


In some embodiments R1a is C3-7 cycloalkoxy.


In some embodiments R1a is C1-6 linear haloalkyl.


In some embodiments R1a is C3-7 branched haloalkyl.


In some embodiments R1a is C1-6 linear haloalkoxy.


In some embodiments R1a is —S(C1-6 linear alkyl).


In some embodiments R1a is S(C3-7 branched alkyl).


In some embodiments R1a is —S(C3-7 cycloalkyl).


In some embodiments R1a is COR13.


In some embodiments R1a is CO2R14.


In some embodiments R1a is CONR15aR15b.


In some embodiments R1a is SO2NR15aR15b.


In some embodiments R1a is NR16aR16b.


In some embodiments R1a is NR16aCOR17.


In some embodiments R1a is NR16aSO2R18.


In some embodiments R1a is NR16aSO2NR19aR19b.


In some embodiments R1b is H.


In some embodiments R1b is OH


In some embodiments R1b is NO2.


In some embodiments R1b is halogen.


In some embodiments R1b is CN.


In some embodiments R1b is C1-6 linear alkyl.


In some embodiments R1b is C3-7 branched alkyl.


In some embodiments R1b is C3-7 cycloalkyl.


In some embodiments R1b is C1-6 linear alkoxy.


In some embodiments R1b is C3-7 branched alkoxy.


In some embodiments R1b is C3-7 cycloalkoxy.


In some embodiments R1b is C1-6 linear haloalkyl.


In some embodiments R1b is C3-7 branched haloalkyl.


In some embodiments R1b is C1-6 linear haloalkoxy.


In some embodiments R1b is —S(C1-6 linear alkyl).


In some embodiments R1b is S(C3-7 branched alkyl).


In some embodiments R1b is —S(C3-7 cycloalkyl).


In some embodiments R1b is COR13.


In some embodiments R1b is CO2R14.


In some embodiments R1b is CONR15aR15b.


In some embodiments R1b is SO2NR15aR15b.


In some embodiments R1b is NR16aR16b.


In some embodiments R1b is NR16aCOR17.


In some embodiments R1b is NR16aSO2R18.


In some embodiments R1b is NR16aSO2NR19aR19b.


In some embodiments R1c is H.


In some embodiments R1c is OH


In some embodiments R1c is NO2.


In some embodiments R1c is halogen.


In some embodiments R1c is CN.


In some embodiments R1c is C1-6 linear alkyl.


In some embodiments R1c is C3-7 branched alkyl.


In some embodiments R1c is C3-7 cycloalkyl.


In some embodiments R1c is C1-6 linear alkoxy.


In some embodiments R1c is C3-7 branched alkoxy.


In some embodiments R1c is C3-7 cycloalkoxy.


In some embodiments R1c is C1-6 linear haloalkyl.


In some embodiments R1c is C3-7 branched haloalkyl.


In some embodiments R1c is C1-6 linear haloalkoxy.


In some embodiments R1c is —S(C1-6 linear alkyl).


In some embodiments R1c is S(C3-7 branched alkyl).


In some embodiments R1c is —S(C3-7 cycloalkyl).


In some embodiments R1c is COR13.


In some embodiments R1c is CO2R14.


In some embodiments R1c is CONR15aR15b.


In some embodiments R1c is SO2NR15aR15b.


In some embodiments R1c is NR16aR16b.


In some embodiments R1c is NR16aCOR17.


In some embodiments R1c is NR16aSO2R18.


In some embodiments R1c is NR16aSO2NR19aR19b.


In some embodiments Rid is H.


In some embodiments R1d is OH


In some embodiments R1d is NO2.


In some embodiments R1d is halogen.


In some embodiments R1d is CN.


In some embodiments R1d is C1-6 linear alkyl.


In some embodiments R1d is C3-7 branched alkyl.


In some embodiments R1d is C3-7 cycloalkyl.


In some embodiments R1d is C1-6 linear alkoxy.


In some embodiments R1d is C3-7 branched alkoxy.


In some embodiments R1d is C3-7 cycloalkoxy.


In some embodiments R1d is C1-6 linear haloalkyl.


In some embodiments R1d is C3-7 branched haloalkyl.


In some embodiments R1d is C1-6 linear haloalkoxy.


In some embodiments R1d is —S(C1-6 linear alkyl).


In some embodiments R1d is S(C3-7 branched alkyl).


In some embodiments R1d is —S(C3-7 cycloalkyl).


In some embodiments R1d is COR13.


In some embodiments R1d is CO2R14.


In some embodiments R1d is CONR15aR15b.


In some embodiments R1d is SO2NR15aR15b.


In some embodiments R1d is NR16aR16b.


In some embodiments R1d is NR16aCOR17.


In some embodiments R1d is NR16aSO2R18.


In some embodiments R1d is NR16aSO2NR19aR19b.


In some embodiments R1e is H.


In some embodiments R1e is OH


In some embodiments R1e is NO2.


In some embodiments R1e is halogen.


In some embodiments R1e is CN.


In some embodiments R1e is C1-6 linear alkyl.


In some embodiments R1e is C3-7 branched alkyl.


In some embodiments R1e is C3-7 cycloalkyl.


In some embodiments R1e is C1-6 linear alkoxy.


In some embodiments R1e is C3-7 branched alkoxy.


In some embodiments R1e is C3-7 cycloalkoxy.


In some embodiments R1e is C1-6 linear haloalkyl.


In some embodiments R1e is C3-7 branched haloalkyl.


In some embodiments R1e is C1-6 linear haloalkoxy.


In some embodiments R1e is —S(C1-6 linear alkyl).


In some embodiments R1e is S(C3-7 branched alkyl).


In some embodiments R1e is —S(C3-7 cycloalkyl).


In some embodiments R1e is COR13.


In some embodiments R1e is CO2R14.


In some embodiments R1e is CONR15aR15b.


In some embodiments R1e is SO2NR15aR15b.


In some embodiments R1e is NR16aR16b.


In some embodiments R1e is NR16aCOR17.


In some embodiments R1e is NR16aSO2R18.


In some embodiments R1e is NR16aSO2NR19aR19b.


In some embodiments R13 is H.


In some embodiments R13 is C1-6 linear alkyl.


In some embodiments R13 is C3-7 branched alkyl.


In some embodiments R13 is C3-7 cycloalkyl.


In some embodiments R14 is C1-6 linear alkyl.


In some embodiments R14 is C3-7 branched alkyl.


In some embodiments R14 is C3-7 cycloalkyl.


In some embodiments R15a is H.


In some embodiments R15a is C1-6 linear alkyl.


In some embodiments R15a is C3-7 branched alkyl.


In some embodiments R15a is C3-7 cycloalkyl.


In some embodiments R15b is H.


In some embodiments R15b is C1-6 linear alkyl.


In some embodiments R15bis C3-7 branched alkyl.


In some embodiments R15bis C3-7 cycloalkyl.


In some embodiments R16a is H.


In some embodiments R16a is C1-6 linear alkyl.


In some embodiments R16a is C3-7 branched alkyl.


In some embodiments R16a is C3-7 cycloalkyl.


In some embodiments R16b is H.


In some embodiments R16b is C1-6 linear alkyl.


In some embodiments R16b is C3-7 branched alkyl.


In some embodiments R16b is C3-7 cycloalkyl.


In some embodiments R17 is H.


In some embodiments R17 is C1-6 linear alkyl.


In some embodiments R17 is C3-7 branched alkyl.


In some embodiments R17 is C3-7 cycloalkyl.


In some embodiments R18 is C1-6 linear alkyl.


In some embodiments R18 is C3-7 branched alkyl.


In some embodiments R18 is C3-7 cycloalkyl.


In some embodiments R19a is C1-6 linear alkyl.


In some embodiments R19a is C3-7 branched alkyl.


In some embodiments R19a is C3-7 cycloalkyl.


In some embodiments R19b is C1-6 linear alkyl.


In some embodiments R19b is C3-7 branched alkyl.


In some embodiments R19b is C3-7 cycloalkyl.


In some embodiments n is 1.


In some embodiments n is 2.


In some embodiments n is 3.


In some embodiments n is 4.


In some embodiments m is 1.


In some embodiments m is 2.


In some embodiments m is 3.


In some embodiments R20a is hydrogen.


In some embodiments R20a is —CN.


In some embodiments R20a is —NO2.


In some embodiments R20a is —OH.


In some embodiments R20a is halogen.


In some embodiments R20a is C1-6 linear alkyl.


In some embodiments R20a is C3-7 branched alkyl.


In some embodiments R20a is C3-7 cycloalkyl.


In some embodiments R20a is C1-6 linear alkoxy.


In some embodiments R20a is C3-7 branched alkoxy.


In some embodiments R20a is C3-7 cycloalkoxy.


In some embodiments R20a is C1-6 linear haloalkyl.


In some embodiments R20a is C3-7 branched haloalkyl.


In some embodiments R20a is C1-6 linear haloalkoxy.


In some embodiments R20a is C3-7 branched haloalkoxy.


In some embodiments R20a is SH.


In some embodiments R20a is SC1-6 linear alkyl.


In some embodiments R20a is SC3-7 branched alkyl.


In some embodiments R20a is SC3-7cycloalkyl.


In some embodiments R20a is SO2C1-6 linear alkyl.


In some embodiments R20a is SO2C3-7 branched alkyl.


In some embodiments R20a is SO2C3-7cycloalkyl.


In some embodiments R20a is SO2NH2.


In some embodiments R20a is SO2NHR21.


In some embodiments R20a is NHSO2R22.


In some embodiments R20a is —NR23aR23b.


In some embodiments R20a is NHC(O)R24.


In some embodiments R20a is C(O)NHR24.


In some embodiments R20a is C(O)N(R24)2.


In some embodiments R20a is morpholino.


In some embodiments R20a is




embedded image


In some embodiments R20b is hydrogen.


In some embodiments R20b is —CN.


In some embodiments R20b is —NO2.


In some embodiments R20b is —OH.


In some embodiments R20b is halogen.


In some embodiments R20b is C1-6 linear alkyl.


In some embodiments R20b is C3-7 branched alkyl.


In some embodiments R20b is C3-7 cycloalkyl.


In some embodiments R20b is C1-6 linear alkoxy.


In some embodiments R20b is C3-7 branched alkoxy.


In some embodiments R20b is C3-7 cycloalkoxy.


In some embodiments R20b is C1-6 linear haloalkyl.


In some embodiments R20b is C3-7 branched haloalkyl.


In some embodiments R20b is C1-6 linear haloalkoxy.


In some embodiments R20b is C3-7 branched haloalkoxy.


In some embodiments R20b is SH.


In some embodiments R20b is SC1-6 linear alkyl.


In some embodiments R20b is SC3-7 branched alkyl.


In some embodiments R20b is SC3-7cycloalkyl.


In some embodiments R20b is SO2C1-6 linear alkyl.


In some embodiments R20b is SO2C3-7 branched alkyl.


In some embodiments R20b is SO2C3-7cycloalkyl.


In some embodiments R20b is SO2NH2.


In some embodiments R20b is SO2NHR21.


In some embodiments R20b is NHSO2R22.


In some embodiments R20b is —NR23aR23b.


In some embodiments R20b is NHC(O)R24.


In some embodiments R20b is C(O)NHR24.


In some embodiments R20b is C(O)N(R24)2.


In some embodiments R20b is morpholino.


In some embodiments R20b is




embedded image


In some embodiments R20c is hydrogen.


In some embodiments R20c is —CN.


In some embodiments R20c is —NO2.


In some embodiments R20c is —OH.


In some embodiments R20c is halogen.


In some embodiments R20c is C1-6 linear alkyl.


In some embodiments R20c is C3-7 branched alkyl.


In some embodiments R20c is C3-7 cycloalkyl.


In some embodiments R20c is C1-6 linear alkoxy.


In some embodiments R20c is C3-7 branched alkoxy.


In some embodiments R20c is C3-7 cycloalkoxy.


In some embodiments R20c is C1-6 linear haloalkyl.


In some embodiments R20c is C3-7 branched haloalkyl.


In some embodiments R20c is C1-6 linear haloalkoxy.


In some embodiments R20c is C3-7 branched haloalkoxy.


In some embodiments R20c is SH.


In some embodiments R20c is SC1-6 linear alkyl.


In some embodiments R20c is SC3-7 branched alkyl.


In some embodiments R20c is SC3-7cycloalkyl.


In some embodiments R20c is SO2C1-6 linear alkyl.


In some embodiments R20c is SO2C3-7 branched alkyl.


In some embodiments R20c is SO2C3-7cycloalkyl.


In some embodiments R20c is SO2NH2.


In some embodiments R20c is SO2NHR21.


In some embodiments R20c is NHSO2R22.


In some embodiments R20c is —NR23aR23b.


In some embodiments R20c is NHC(O)R24.


In some embodiments R20c is C(O)NHR24.


In some embodiments R20c is C(O)N(R24)2.


In some embodiments R20c is morpholino.


In some embodiments R20c is




embedded image


In some embodiments R20d is hydrogen.


In some embodiments R20d is —CN.


In some embodiments R20d is —NO2.


In some embodiments R20d is —OH.


In some embodiments R20d is halogen.


In some embodiments R20d is C1-6 linear alkyl.


In some embodiments R20d is C3-7 branched alkyl.


In some embodiments R20d is C3-7 cycloalkyl.


In some embodiments R20d is C1-6 linear alkoxy.


In some embodiments R20d is C3-7 branched alkoxy.


In some embodiments R20d is C3-7 cycloalkoxy.


In some embodiments R20d is C1-6 linear haloalkyl.


In some embodiments R20d is C3-7 branched haloalkyl.


In some embodiments R20d is C1-6 linear haloalkoxy.


In some embodiments R20d is C3-7 branched haloalkoxy.


In some embodiments R20d is SH.


In some embodiments R20d is SC1-6 linear alkyl.


In some embodiments R20d is SC3-7 branched alkyl.


In some embodiments R20d is SC3-7cycloalkyl.


In some embodiments R20d is SO2C1-6 linear alkyl.


In some embodiments R20d is SO2C3-7 branched alkyl.


In some embodiments R20d is SO2C3-7cycloalkyl.


In some embodiments R20d is SO2NH2.


In some embodiments R20d is SO2NHR21.


In some embodiments R20d is NHSO2R22.


In some embodiments R20d is —NR23aR23b.


In some embodiments R20d is NHC(O)R24.


In some embodiments R20d is C(O)NHR24.


In some embodiments R20d is C(O)N(R24)2.


In some embodiments R20d is morpholino.


In some embodiments R20d is




embedded image


In some embodiments R20e is hydrogen.


In some embodiments R20e is —CN.


In some embodiments R20e is —NO2.


In some embodiments R20e is —OH.


In some embodiments R20e is halogen.


In some embodiments R20e is C1-6 linear alkyl.


In some embodiments R20e is C3-7 branched alkyl.


In some embodiments R20e is C3-7 cycloalkyl.


In some embodiments R20e is C1-6 linear alkoxy.


In some embodiments R20e is C3-7 branched alkoxy.


In some embodiments R20e is C3-7 cycloalkoxy.


In some embodiments R20e is C1-6 linear haloalkyl.


In some embodiments R20e is C3-7 branched haloalkyl.


In some embodiments R20e is C1-6 linear haloalkoxy.


In some embodiments R20e is C3-7 branched haloalkoxy.


In some embodiments R20e is SH.


In some embodiments R20e is SC1-6 linear alkyl.


In some embodiments R20e is SC3-7 branched alkyl.


In some embodiments R20e is SC3-7cycloalkyl.


In some embodiments R20e is SO2C1-6 linear alkyl.


In some embodiments R20e is SO2C3-7 branched alkyl.


In some embodiments R20e is SO2C3-7cycloalkyl.


In some embodiments R20e is SO2NH2.


In some embodiments R20e is SO2NHR21.


In some embodiments R20e isNHSO2R22.


In some embodiments R20e is —NR23aR23b.


In some embodiments R20e is NHC(O)R24.


In some embodiments R20e is C(O)NHR24.


In some embodiments R20e is C(O)N(R24)2.


In some embodiments R20e is morpholino.


In some embodiments R20e is




embedded image


In some embodiments R20f is hydrogen.


In some embodiments R20f is —CN.


In some embodiments R20f is —NO2.


In some embodiments R20f is —OH.


In some embodiments R20f is halogen.


In some embodiments R20f is C1-6 linear alkyl.


In some embodiments R20f is C3-7 branched alkyl.


In some embodiments R20f is C3-7 cycloalkyl.


In some embodiments R20f is C1-6 linear alkoxy.


In some embodiments R20f is C3-7 branched alkoxy.


In some embodiments R20f is C3-7 cycloalkoxy.


In some embodiments R20f is C1-6 linear haloalkyl.


In some embodiments R20f is C3-7 branched haloalkyl.


In some embodiments R20f is C1-6 linear haloalkoxy.


In some embodiments R20f is C3-7 branched haloalkoxy.


In some embodiments R20f is SH.


In some embodiments R20f is SC1-6 linear alkyl.


In some embodiments R20f is SC3-7 branched alkyl.


In some embodiments R20f is SC3-7cycloalkyl.


In some embodiments R20f is SO2C1-6 linear alkyl.


In some embodiments R20f is SO2C3-7 branched alkyl.


In some embodiments R20f is SO2C3-7cycloalkyl.


In some embodiments R20f is SO2NH2.


In some embodiments R20f is SO2NHR21.


In some embodiments R20f is NHSO2R22.


In some embodiments R20f is —NR23aR23b.


In some embodiments R20f is NHC(O)R24.


In some embodiments R20f is C(O)NHR24.


In some embodiments R20f is C(O)N(R24)2.


In some embodiments R20f is morpholino.


In some embodiments R20f is




embedded image


In some embodiments R20g is hydrogen.


In some embodiments R20g is —CN.


In some embodiments R20g is —NO2.


In some embodiments R20g is —OH.


In some embodiments R20g is halogen.


In some embodiments R20g is C1-6 linear alkyl.


In some embodiments R20g is C3-7 branched alkyl.


In some embodiments R20g is C3-7 cycloalkyl.


In some embodiments R20g is C1-6 linear alkoxy.


In some embodiments R20g is C3-7 branched alkoxy.


In some embodiments R20g is C3-7 cycloalkoxy.


In some embodiments R20g is C1-6 linear haloalkyl.


In some embodiments R20g is C3-7 branched haloalkyl.


In some embodiments R20g is C1-6 linear haloalkoxy.


In some embodiments R20g is C3-7 branched haloalkoxy.


In some embodiments R20g is SH.


In some embodiments R20g is SC1-6 linear alkyl.


In some embodiments R20g is SC3-7 branched alkyl.


In some embodiments R20g is SC3-7cycloalkyl.


In some embodiments R20g is SO2C1-6 linear alkyl.


In some embodiments R20g is SO2C3-7 branched alkyl.


In some embodiments R20g is SO2C3-7cycloalkyl.


In some embodiments R20g is SO2NH2.


In some embodiments R20g is SO2NHR21.


In some embodiments R20g is NHSO2R22.


In some embodiments R20g is —NR23aR23b


In some embodiments R20g is NHC(O)R24.


In some embodiments R20g is C(O)NHR24.


In some embodiments R20g is C(O)N(R24)2.


In some embodiments R20g is morpholino.


In some embodiments R20g is




embedded image


In some embodiments R21 is hydrogen.


In some embodiments R21 is C1-6 linear alkyl.


In some embodiments R21 is C3-7 branched alkyl.


In some embodiments R21 is C3-7 cycloalkyl.


In some embodiments R22 is hydrogen.


In some embodiments R22 is C1-6 linear alkyl.


In some embodiments R22 is C3-7 branched alkyl.


In some embodiments R22 is C3-7 cycloalkyl.


In some embodiments R23a is hydrogen.


In some embodiments R23a is C1-6 linear alkyl.


In some embodiments R23a is C3-7 branched alkyl.


In some embodiments R23a is C3-7 cycloalkyl.


In some embodiments R23b is hydrogen.


In some embodiments R23b is C1-6 linear alkyl.


In some embodiments R23b is C3-7 branched alkyl.


In some embodiments R23b is C3-7 cycloalkyl.


In some embodiments R24 is hydrogen.


In some embodiments R24 is C1-6 linear alkyl.


In some embodiments R24 is C3-7 branched alkyl.


In some embodiments R24 is C3-7 cycloalkyl.


In some embodiments R25 is hydrogen.


In some embodiments R25 is C1-6 linear alkyl.


In some embodiments R25 is C3-7 branched alkyl.


In some embodiments R25 is C3-7 cycloalkyl.


In some embodiments Q1 is 1.


In some embodiments Q1 is 2.


In some embodiments Q2 is 1.


In some embodiments Q2 is 2.


In some embodiments X1 is 0.


In some embodiments X1 is S.


In some embodiments X1 is SO.


In some embodiments X1 is SO2.


In some embodiments X1 is NR7.


Exemplary Compounds

Exemplary compounds include any of the compounds described herein. In embodiments where the compounds or formulas described herein do not specify the configuration of the lactam stereocenter (i.e., the carbon substituted by the nitrogen of the lactam) is not indicated, said lactam stereocenter can have the R-configuration. In other embodiments, said lactam stereocenter can have the S-configuration.


In embodiments, a compound is any compound described herein or a pharmaceutically acceptable salt thereof. In embodiments, a compound that is described in any one of Tables 1-39, or a pharmaceutically acceptable salt thereof. In embodiments, a compound is a compound described in any one of Tables 34-39, or a pharmaceutically acceptable salt thereof.


Exemplary embodiments include compounds having the formula (II)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 1.













TABLE 1





Entry
R1
R2
n
R3



















1
Methyl
Methyl
1
Phenyl


2
Methyl
Methyl
2
Phenyl


3
Methyl
Methyl
3
Phenyl


4
Methyl
Methyl
4
Phenyl


5
Methyl
Methyl
1
4-OH-Phenyl


6
Methyl
Methyl
2
4-OH-Phenyl


7
Methyl
Methyl
3
4-OH-Phenyl


8
Methyl
Methyl
4
4-OH-Phenyl


9
Methyl
Methyl
1
3-OH-Phenyl


10
Methyl
Methyl
2
3-OH-Phenyl


11
Methyl
Methyl
3
3-OH-Phenyl


12
Methyl
Methyl
4
3-OH-Phenyl


13
Methyl
Methyl
1
2-OH-Phenyl


14
Methyl
Methyl
2
2-OH-Phenyl


15
Methyl
Methyl
3
2-OH-Phenyl


16
Methyl
Methyl
4
2-OH-Phenyl


17
Methyl
Methyl
1
4-OMe-Phenyl


18
Methyl
Methyl
2
4-OMe-Phenyl


19
Methyl
Methyl
3
4-OMe-Phenyl


20
Methyl
Methyl
4
4-OMe-Phenyl


21
Methyl
Methyl
1
3-OMe-Phenyl


22
Methyl
Methyl
2
3-OMe-Phenyl


23
Methyl
Methyl
3
3-OMe-Phenyl


24
Methyl
Methyl
4
3-OMe-Phenyl


25
Methyl
Methyl
1
2-OMe-Phenyl


26
Methyl
Methyl
2
2-OMe-Phenyl


27
Methyl
Methyl
3
2-OMe-Phenyl


28
Methyl
Methyl
4
2-OMe-Phenyl


29
Methyl
Methyl
1
4-CN-Phenyl


30
Methyl
Methyl
2
4-CN-Phenyl


31
Methyl
Methyl
3
4-CN-Phenyl


32
Methyl
Methyl
4
4-CN-Phenyl


33
Methyl
Methyl
1
3-CN-Phenyl


34
Methyl
Methyl
2
3-CN-Phenyl


35
Methyl
Methyl
3
3-CN-Phenyl


36
Methyl
Methyl
4
3-CN-Phenyl


37
Methyl
Methyl
1
2-CN-Phenyl


38
Methyl
Methyl
2
2-CN-Phenyl


39
Methyl
Methyl
3
2-CN-Phenyl


40
Methyl
Methyl
4
2-CN-Phenyl


41
Methyl
Methyl
1
4-Me-Phenyl


42
Methyl
Methyl
2
4-Me-Phenyl


43
Methyl
Methyl
3
4-Me-Phenyl


44
Methyl
Methyl
4
4-Me-Phenyl


45
Methyl
Methyl
1
3-Me-Phenyl


46
Methyl
Methyl
2
3-Me-Phenyl


47
Methyl
Methyl
3
3-Me-Phenyl


48
Methyl
Methyl
4
3-Me-Phenyl


49
Methyl
Methyl
1
2-Me-Phenyl


50
Methyl
Methyl
2
2-Me-Phenyl


51
Methyl
Methyl
3
2-Me-Phenyl


52
Methyl
Methyl
4
2-Me-Phenyl


53
Methyl
Methyl
1
4-F-Phenyl


54
Methyl
Methyl
2
4-F-Phenyl


55
Methyl
Methyl
3
4-F-Phenyl


56
Methyl
Methyl
4
4-F-Phenyl


57
Methyl
Methyl
1
3-F-Phenyl


58
Methyl
Methyl
2
3-F-Phenyl


59
Methyl
Methyl
3
3-F-Phenyl


60
Methyl
Methyl
4
3-F-Phenyl


61
Methyl
Methyl
1
2-F-Phenyl


62
Methyl
Methyl
2
2-F-Phenyl


63
Methyl
Methyl
3
2-F-Phenyl


64
Methyl
Methyl
4
2-F-Phenyl


65
Methyl
Methyl
1
4-Cl-Phenyl


66
Methyl
Methyl
2
4-Cl-Phenyl


67
Methyl
Methyl
3
4-Cl-Phenyl


68
Methyl
Methyl
4
4-Cl-Phenyl


69
Methyl
Methyl
1
3-Cl-Phenyl


70
Methyl
Methyl
2
3-Cl-Phenyl


71
Methyl
Methyl
3
3-Cl-Phenyl


72
Methyl
Methyl
4
3-Cl-Phenyl


73
Methyl
Methyl
1
2-Cl-Phenyl


74
Methyl
Methyl
2
2-Cl-Phenyl


75
Methyl
Methyl
3
2-Cl-Phenyl


76
Methyl
Methyl
4
2-Cl-Phenyl


77
Methyl
Methyl
1
4-Br-Phenyl


78
Methyl
Methyl
2
4-Br-Phenyl


79
Methyl
Methyl
3
4-Br-Phenyl


80
Methyl
Methyl
4
4-Br-Phenyl


81
Methyl
Methyl
1
3-Br-Phenyl


82
Methyl
Methyl
2
3-Br-Phenyl


83
Methyl
Methyl
3
3-Br-Phenyl


84
Methyl
Methyl
4
3-Br-Phenyl


85
Methyl
Methyl
1
2-Br-Phenyl


86
Methyl
Methyl
2
2-Br-Phenyl


87
Methyl
Methyl
3
2-Br-Phenyl


88
Methyl
Methyl
4
2-Br-Phenyl


89
Methyl
Methyl
1
4-CF3-Phenyl


90
Methyl
Methyl
2
4-CF3-Phenyl


91
Methyl
Methyl
3
4-CF3-Phenyl


92
Methyl
Methyl
4
4-CF3-Phenyl


93
Methyl
Methyl
1
3-CF3-Phenyl


94
Methyl
Methyl
2
3-CF3-Phenyl


95
Methyl
Methyl
3
3-CF3-Phenyl


96
Methyl
Methyl
4
3-CF3-Phenyl


97
Methyl
Methyl
1
2-CF3-Phenyl


98
Methyl
Methyl
2
2-CF3-Phenyl


99
Methyl
Methyl
3
2-CF3-Phenyl


100
Methyl
Methyl
4
2-CF3-Phenyl


101
Methyl
Methyl
1
4-iPr-Phenyl


102
Methyl
Methyl
2
4-iPr-Phenyl


103
Methyl
Methyl
3
4-iPr-Phenyl


104
Methyl
Methyl
4
4-iPr-Phenyl


105
Methyl
Methyl
1
3-iPr-Phenyl


106
Methyl
Methyl
2
3-iPr-Phenyl


107
Methyl
Methyl
3
3-iPr-Phenyl


108
Methyl
Methyl
4
3-iPr-Phenyl


109
Methyl
Methyl
1
2-iPr-Phenyl


110
Methyl
Methyl
2
2-iPr-Phenyl


111
Methyl
Methyl
3
2-iPr-Phenyl


112
Methyl
Methyl
4
2-iPr-Phenyl


113
Methyl
Methyl
1
4-NH2-Phenyl


114
Methyl
Methyl
2
4-NH2-Phenyl


115
Methyl
Methyl
3
4-NH2-Phenyl


116
Methyl
Methyl
4
4-NH2-Phenyl


117
Methyl
Methyl
1
3-NH2-Phenyl


118
Methyl
Methyl
2
3-NH2-Phenyl


119
Methyl
Methyl
3
3-NH2-Phenyl


120
Methyl
Methyl
4
3-NH2-Phenyl


121
Methyl
Methyl
1
2-NH2-Phenyl


122
Methyl
Methyl
2
2-NH2-Phenyl


123
Methyl
Methyl
3
2-NH2-Phenyl


124
Methyl
Methyl
4
2-NH2-Phenyl


125
Methyl
Methyl
1
2,3-di-Me-Phenyl


126
Methyl
Methyl
2
2,3-di-Me-Phenyl


127
Methyl
Methyl
3
2,3-di-Me-Phenyl


128
Methyl
Methyl
4
2,3-di-Me-Phenyl


129
Methyl
Methyl
1
2,4-di-Me-Phenyl


130
Methyl
Methyl
2
2,4-di-Me-Phenyl


131
Methyl
Methyl
3
2,4-di-Me-Phenyl


132
Methyl
Methyl
4
2,4-di-Me-Phenyl


133
Methyl
Methyl
1
2,5-di-Me-Phenyl


134
Methyl
Methyl
2
2,5-di-Me-Phenyl


135
Methyl
Methyl
3
2,5-di-Me-Phenyl


136
Methyl
Methyl
4
2,5-di-Me-Phenyl


137
Methyl
Methyl
1
2,6-di-Me-Phenyl


138
Methyl
Methyl
2
2,6-di-Me-Phenyl


139
Methyl
Methyl
3
2,6-di-Me-Phenyl


140
Methyl
Methyl
4
2,6-di-Me-Phenyl


141
Methyl
Methyl
1
2,6-di-iPr-Phenyl


142
Methyl
Methyl
2
2,6-di-iPr-Phenyl


143
Methyl
Methyl
3
2,6-di-iPr-Phenyl


144
Methyl
Methyl
4
2,6-di-iPr-Phenyl


145
Methyl
Methyl
1
2-morpholino-phenyl


146
Methyl
Methyl
2
2-morpholino-phenyl


147
Methyl
Methyl
3
2-morpholino-phenyl


148
Methyl
Methyl
4
2-morpholino-phenyl


149
Methyl
Methyl
1
3-morpholino-phenyl


150
Methyl
Methyl
2
3-morpholino-phenyl


151
Methyl
Methyl
3
3-morpholino-phenyl


152
Methyl
Methyl
4
3-morpholino-phenyl


153
Methyl
Methyl
1
4-morpholino-phenyl


154
Methyl
Methyl
2
4-morpholino-phenyl


155
Methyl
Methyl
3
4-morpholino-phenyl


156
Methyl
Methyl
4
4-morpholino-phenyl


157
Methyl
Methyl
1
4-CN-2-morpholino-phenyl


158
Methyl
Methyl
2
4-CN-2-morpholino-phenyl


159
Methyl
Methyl
3
4-CN-2-morpholino-phenyl


160
Methyl
Methyl
4
4-CN-2-morpholino-phenyl


161
Methyl
Methyl
1
4-CH3-2-morpholino-phenyl


162
Methyl
Methyl
2
4-CH3-2-morpholino-phenyl


163
Methyl
Methyl
3
4-CH3-2-morpholino-phenyl


164
Methyl
Methyl
4
4-CH3-2-morpholino-phenyl


165
Methyl
Methyl
1
4-OH-2-morpholino-phenyl


166
Methyl
Methyl
2
4-OH-2-morpholino-phenyl


167
Methyl
Methyl
3
4-OH-2-morpholino-phenyl


168
Methyl
Methyl
4
4-OH-2-morpholino-phenyl


169
Methyl
Methyl
1
naphthylen-1-yl


170
Methyl
Methyl
2
naphthylen-1-yl


171
Methyl
Methyl
3
naphthylen-1-yl


172
Methyl
Methyl
4
naphthylen-1-yl


173
Methyl
Methyl
1
naphthylen-2-yl


174
Methyl
Methyl
2
naphthylen-2-yl


175
Methyl
Methyl
3
naphthylen-2-yl


176
Methyl
Methyl
4
naphthylen-2-yl


177
Ethyl
Ethyl
1
Phenyl


178
Ethyl
Ethyl
2
Phenyl


179
Ethyl
Ethyl
3
Phenyl


180
Ethyl
Ethyl
4
Phenyl


181
Ethyl
Ethyl
1
4-OH-Phenyl


182
Ethyl
Ethyl
2
4-OH-Phenyl


183
Ethyl
Ethyl
3
4-OH-Phenyl


184
Ethyl
Ethyl
4
4-OH-Phenyl


185
Ethyl
Ethyl
1
3-OH-Phenyl


186
Ethyl
Ethyl
2
3-OH-Phenyl


187
Ethyl
Ethyl
3
3-OH-Phenyl


188
Ethyl
Ethyl
4
3-OH-Phenyl


189
Ethyl
Ethyl
1
2-OH-Phenyl


190
Ethyl
Ethyl
2
2-OH-Phenyl


191
Ethyl
Ethyl
3
2-OH-Phenyl


192
Ethyl
Ethyl
4
2-OH-Phenyl


193
Ethyl
Ethyl
1
4-OMe-Phenyl


194
Ethyl
Ethyl
2
4-OMe-Phenyl


195
Ethyl
Ethyl
3
4-OMe-Phenyl


196
Ethyl
Ethyl
4
4-OMe-Phenyl


197
Ethyl
Ethyl
1
3-OMe-Phenyl


198
Ethyl
Ethyl
2
3-OMe-Phenyl


199
Ethyl
Ethyl
3
3-OMe-Phenyl


200
Ethyl
Ethyl
4
3-OMe-Phenyl


201
Ethyl
Ethyl
1
2-OMe-Phenyl


202
Ethyl
Ethyl
2
2-OMe-Phenyl


203
Ethyl
Ethyl
3
2-OMe-Phenyl


204
Ethyl
Ethyl
4
2-OMe-Phenyl


205
Ethyl
Ethyl
1
4-CN-Phenyl


206
Ethyl
Ethyl
2
4-CN-Phenyl


207
Ethyl
Ethyl
3
4-CN-Phenyl


208
Ethyl
Ethyl
4
4-CN-Phenyl


209
Ethyl
Ethyl
1
3-CN-Phenyl


210
Ethyl
Ethyl
2
3-CN-Phenyl


211
Ethyl
Ethyl
3
3-CN-Phenyl


212
Ethyl
Ethyl
4
3-CN-Phenyl


213
Ethyl
Ethyl
1
2-CN-Phenyl


214
Ethyl
Ethyl
2
2-CN-Phenyl


215
Ethyl
Ethyl
3
2-CN-Phenyl


216
Ethyl
Ethyl
4
2-CN-Phenyl


217
Ethyl
Ethyl
1
4-Me-Phenyl


218
Ethyl
Ethyl
2
4-Me-Phenyl


219
Ethyl
Ethyl
3
4-Me-Phenyl


220
Ethyl
Ethyl
4
4-Me-Phenyl


221
Ethyl
Ethyl
1
3-Me-Phenyl


222
Ethyl
Ethyl
2
3-Me-Phenyl


223
Ethyl
Ethyl
3
3-Me-Phenyl


224
Ethyl
Ethyl
4
3-Me-Phenyl


225
Ethyl
Ethyl
1
2-Me-Phenyl


226
Ethyl
Ethyl
2
2-Me-Phenyl


227
Ethyl
Ethyl
3
2-Me-Phenyl


228
Ethyl
Ethyl
4
2-Me-Phenyl


229
Ethyl
Ethyl
1
4-F-Phenyl


230
Ethyl
Ethyl
2
4-F-Phenyl


231
Ethyl
Ethyl
3
4-F-Phenyl


232
Ethyl
Ethyl
4
4-F-Phenyl


233
Ethyl
Ethyl
1
3-F-Phenyl


234
Ethyl
Ethyl
2
3-F-Phenyl


235
Ethyl
Ethyl
3
3-F-Phenyl


236
Ethyl
Ethyl
4
3-F-Phenyl


237
Ethyl
Ethyl
1
2-F-Phenyl


238
Ethyl
Ethyl
2
2-F-Phenyl


239
Ethyl
Ethyl
3
2-F-Phenyl


240
Ethyl
Ethyl
4
2-F-Phenyl


241
Ethyl
Ethyl
1
4-Cl-Phenyl


242
Ethyl
Ethyl
2
4-Cl-Phenyl


243
Ethyl
Ethyl
3
4-Cl-Phenyl


244
Ethyl
Ethyl
4
4-Cl-Phenyl


245
Ethyl
Ethyl
1
3-Cl-Phenyl


246
Ethyl
Ethyl
2
3-Cl-Phenyl


247
Ethyl
Ethyl
3
3-Cl-Phenyl


248
Ethyl
Ethyl
4
3-Cl-Phenyl


249
Ethyl
Ethyl
1
2-Cl-Phenyl


250
Ethyl
Ethyl
2
2-Cl-Phenyl


251
Ethyl
Ethyl
3
2-Cl-Phenyl


252
Ethyl
Ethyl
4
2-Cl-Phenyl


253
Ethyl
Ethyl
1
4-Br-Phenyl


254
Ethyl
Ethyl
2
4-Br-Phenyl


255
Ethyl
Ethyl
3
4-Br-Phenyl


256
Ethyl
Ethyl
4
4-Br-Phenyl


257
Ethyl
Ethyl
1
3-Br-Phenyl


258
Ethyl
Ethyl
2
3-Br-Phenyl


259
Ethyl
Ethyl
3
3-Br-Phenyl


260
Ethyl
Ethyl
4
3-Br-Phenyl


261
Ethyl
Ethyl
1
2-Br-Phenyl


262
Ethyl
Ethyl
2
2-Br-Phenyl


263
Ethyl
Ethyl
3
2-Br-Phenyl


264
Ethyl
Ethyl
4
2-Br-Phenyl


265
Ethyl
Ethyl
1
4-CF3-Phenyl


266
Ethyl
Ethyl
2
4-CF3-Phenyl


267
Ethyl
Ethyl
3
4-CF3-Phenyl


268
Ethyl
Ethyl
4
4-CF3-Phenyl


269
Ethyl
Ethyl
1
3-CF3-Phenyl


270
Ethyl
Ethyl
2
3-CF3-Phenyl


271
Ethyl
Ethyl
3
3-CF3-Phenyl


272
Ethyl
Ethyl
4
3-CF3-Phenyl


273
Ethyl
Ethyl
1
2-CF3-Phenyl


274
Ethyl
Ethyl
2
2-CF3-Phenyl


275
Ethyl
Ethyl
3
2-CF3-Phenyl


276
Ethyl
Ethyl
4
2-CF3-Phenyl


277
Ethyl
Ethyl
1
4-iPr-Phenyl


278
Ethyl
Ethyl
2
4-iPr-Phenyl


279
Ethyl
Ethyl
3
4-iPr-Phenyl


280
Ethyl
Ethyl
4
4-iPr-Phenyl


281
Ethyl
Ethyl
1
3-iPr-Phenyl


282
Ethyl
Ethyl
2
3-iPr-Phenyl


283
Ethyl
Ethyl
3
3-iPr-Phenyl


284
Ethyl
Ethyl
4
3-iPr-Phenyl


285
Ethyl
Ethyl
1
2-iPr-Phenyl


286
Ethyl
Ethyl
2
2-iPr-Phenyl


287
Ethyl
Ethyl
3
2-iPr-Phenyl


288
Ethyl
Ethyl
4
2-iPr-Phenyl


289
Ethyl
Ethyl
1
4-NH2-Phenyl


290
Ethyl
Ethyl
2
4-NH2-Phenyl


291
Ethyl
Ethyl
3
4-NH2-Phenyl


292
Ethyl
Ethyl
4
4-NH2-Phenyl


293
Ethyl
Ethyl
1
3-NH2-Phenyl


294
Ethyl
Ethyl
2
3-NH2-Phenyl


295
Ethyl
Ethyl
3
3-NH2-Phenyl


296
Ethyl
Ethyl
4
3-NH2-Phenyl


297
Ethyl
Ethyl
1
2-NH2-Phenyl


298
Ethyl
Ethyl
2
2-NH2-Phenyl


299
Ethyl
Ethyl
3
2-NH2-Phenyl


300
Ethyl
Ethyl
4
2-NH2-Phenyl


301
Ethyl
Ethyl
1
2,3-di-Me-Phenyl


302
Ethyl
Ethyl
2
2,3-di-Me-Phenyl


303
Ethyl
Ethyl
3
2,3-di-Me-Phenyl


304
Ethyl
Ethyl
4
2,3-di-Me-Phenyl


305
Ethyl
Ethyl
1
2,4-di-Me-Phenyl


306
Ethyl
Ethyl
2
2,4-di-Me-Phenyl


307
Ethyl
Ethyl
3
2,4-di-Me-Phenyl


308
Ethyl
Ethyl
4
2,4-di-Me-Phenyl


309
Ethyl
Ethyl
1
2,5-di-Me-Phenyl


310
Ethyl
Ethyl
2
2,5-di-Me-Phenyl


311
Ethyl
Ethyl
3
2,5-di-Me-Phenyl


312
Ethyl
Ethyl
4
2,5-di-Me-Phenyl


313
Ethyl
Ethyl
1
2,6-di-Me-Phenyl


314
Ethyl
Ethyl
2
2,6-di-Me-Phenyl


315
Ethyl
Ethyl
3
2,6-di-Me-Phenyl


316
Ethyl
Ethyl
4
2,6-di-Me-Phenyl


317
Ethyl
Ethyl
1
2,6-di-iPr-Phenyl


318
Ethyl
Ethyl
2
2,6-di-iPr-Phenyl


319
Ethyl
Ethyl
3
2,6-di-iPr-Phenyl


320
Ethyl
Ethyl
4
2,6-di-iPr-Phenyl


321
Ethyl
Ethyl
1
2-morpholino-phenyl


322
Ethyl
Ethyl
2
2-morpholino-phenyl


323
Ethyl
Ethyl
3
2-morpholino-phenyl


324
Ethyl
Ethyl
4
2-morpholino-phenyl


325
Ethyl
Ethyl
1
3-morpholino-phenyl


326
Ethyl
Ethyl
2
3-morpholino-phenyl


327
Ethyl
Ethyl
3
3-morpholino-phenyl


328
Ethyl
Ethyl
4
3-morpholino-phenyl


329
Ethyl
Ethyl
1
4-morpholino-phenyl


330
Ethyl
Ethyl
2
4-morpholino-phenyl


331
Ethyl
Ethyl
3
4-morpholino-phenyl


332
Ethyl
Ethyl
4
4-morpholino-phenyl


333
Ethyl
Ethyl
1
4-CN-2-morpholino-phenyl


334
Ethyl
Ethyl
2
4-CN-2-morpholino-phenyl


335
Ethyl
Ethyl
3
4-CN-2-morpholino-phenyl


336
Ethyl
Ethyl
4
4-CN-2-morpholino-phenyl


337
Ethyl
Ethyl
1
4-CH3-2-morpholino-phenyl


338
Ethyl
Ethyl
2
4-CH3-2-morpholino-phenyl


339
Ethyl
Ethyl
3
4-CH3-2-morpholino-phenyl


340
Ethyl
Ethyl
4
4-CH3-2-morpholino-phenyl


341
Ethyl
Ethyl
1
4-OH-2-morpholino-phenyl


342
Ethyl
Ethyl
2
4-OH-2-morpholino-phenyl


343
Ethyl
Ethyl
3
4-OH-2-morpholino-phenyl


344
Ethyl
Ethyl
4
4-OH-2-morpholino-phenyl


345
Ethyl
Ethyl
1
naphthylen-1-yl


346
Ethyl
Ethyl
2
naphthylen-1-yl


347
Ethyl
Ethyl
3
naphthylen-1-yl


348
Ethyl
Ethyl
4
naphthylen-1-yl


349
Ethyl
Ethyl
1
naphthylen-2-yl


350
Ethyl
Ethyl
2
naphthylen-2-yl


351
Ethyl
Ethyl
3
naphthylen-2-yl


352
Ethyl
Ethyl
4
naphthylen-2-yl









Exemplary embodiments include compounds having the formula (VIII)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 2.













TABLE 2







Entry
n
R3




















1
1
Phenyl



2
2
Phenyl



3
3
Phenyl



4
4
Phenyl



5
1
4-OH-Phenyl



6
2
4-OH-Phenyl



7
3
4-OH-Phenyl



8
4
4-OH-Phenyl



9
1
3-OH-Phenyl



10
2
3-OH-Phenyl



11
3
3-OH-Phenyl



12
4
3-OH-Phenyl



13
1
2-OH-Phenyl



14
2
2-OH-Phenyl



15
3
2-OH-Phenyl



16
4
2-OH-Phenyl



17
1
4-OMe-Phenyl



18
2
4-OMe-Phenyl



19
3
4-OMe-Phenyl



20
4
4-OMe-Phenyl



21
1
3-OMe-Phenyl



22
2
3-OMe-Phenyl



23
3
3-OMe-Phenyl



24
4
3-OMe-Phenyl



25
1
2-OMe-Phenyl



26
2
2-OMe-Phenyl



27
3
2-OMe-Phenyl



28
4
2-OMe-Phenyl



29
1
4-CN-Phenyl



30
2
4-CN-Phenyl



31
3
4-CN-Phenyl



32
4
4-CN-Phenyl



33
1
3-CN-Phenyl



34
2
3-CN-Phenyl



35
3
3-CN-Phenyl



36
4
3-CN-Phenyl



37
1
2-CN-Phenyl



38
2
2-CN-Phenyl



39
3
2-CN-Phenyl



40
4
2-CN-Phenyl



41
1
4-Me-Phenyl



42
2
4-Me-Phenyl



43
3
4-Me-Phenyl



44
4
4-Me-Phenyl



45
1
3-Me-Phenyl



46
2
3-Me-Phenyl



47
3
3-Me-Phenyl



48
4
3-Me-Phenyl



49
1
2-Me-Phenyl



50
2
2-Me-Phenyl



51
3
2-Me-Phenyl



52
4
2-Me-Phenyl



53
1
4-F-Phenyl



54
2
4-F-Phenyl



55
3
4-F-Phenyl



56
4
4-F-Phenyl



57
1
3-F-Phenyl



58
2
3-F-Phenyl



59
3
3-F-Phenyl



60
4
3-F-Phenyl



61
1
2-F-Phenyl



62
2
2-F-Phenyl



63
3
2-F-Phenyl



64
4
2-F-Phenyl



65
1
4-Cl-Phenyl



66
2
4-Cl-Phenyl



67
3
4-Cl-Phenyl



68
4
4-Cl-Phenyl



69
1
3-Cl-Phenyl



70
2
3-Cl-Phenyl



71
3
3-Cl-Phenyl



72
4
3-Cl-Phenyl



73
1
2-Cl-Phenyl



74
2
2-Cl-Phenyl



75
3
2-Cl-Phenyl



76
4
2-Cl-Phenyl



77
1
4-Br-Phenyl



78
2
4-Br-Phenyl



79
3
4-Br-Phenyl



80
4
4-Br-Phenyl



81
1
3-Br-Phenyl



82
2
3-Br-Phenyl



83
3
3-Br-Phenyl



84
4
3-Br-Phenyl



85
1
naphthylen-1-yl



86
2
naphthylen-1-yl



87
3
naphthylen-1-yl



88
4
naphthylen-1-yl



89
1
2-Br-Phenyl



90
2
2-Br-Phenyl



91
3
2-Br-Phenyl



92
4
2-Br-Phenyl



93
1
4-CF3-Phenyl



94
2
4-CF3-Phenyl



95
3
4-CF3-Phenyl



96
4
4-CF3-Phenyl



97
1
3-CF3-Phenyl



98
2
3-CF3-Phenyl



99
3
3-CF3-Phenyl



100
4
3-CF3-Phenyl



101
1
2-CF3-Phenyl



102
2
2-CF3-Phenyl



103
3
2-CF3-Phenyl



104
4
2-CF3-Phenyl



105
1
4-iPr-Phenyl



106
2
4-iPr-Phenyl



107
3
4-iPr-Phenyl



108
4
4-iPr-Phenyl



109
1
3-iPr-Phenyl



110
2
3-iPr-Phenyl



111
3
3-iPr-Phenyl



112
4
3-iPr-Phenyl



113
1
2-iPr-Phenyl



114
2
2-iPr-Phenyl



115
3
2-iPr-Phenyl



116
4
2-iPr-Phenyl



117
1
4-NH2-Phenyl



118
2
4-NH2-Phenyl



119
3
4-NH2-Phenyl



120
4
4-NH2-Phenyl



121
1
3-NH2-Phenyl



122
2
3-NH2-Phenyl



123
3
3-NH2-Phenyl



124
4
3-NH2-Phenyl



125
1
2-NH2-Phenyl



126
2
2-NH2-Phenyl



127
3
2-NH2-Phenyl



128
4
2-NH2-Phenyl



129
1
2,3-di-Me-Phenyl



130
2
2,3-di-Me-Phenyl



131
3
2,3-di-Me-Phenyl



132
4
2,3-di-Me-Phenyl



133
1
2,4-di-Me-Phenyl



134
2
2,4-di-Me-Phenyl



135
3
2,4-di-Me-Phenyl



136
4
2,4-di-Me-Phenyl



137
1
2,5-di-Me-Phenyl



138
2
2,5-di-Me-Phenyl



139
3
2,5-di-Me-Phenyl



140
4
2,5-di-Me-Phenyl



141
1
2,6-di-Me-Phenyl



142
2
2,6-di-Me-Phenyl



143
3
2,6-di-Me-Phenyl



144
4
2,6-di-Me-Phenyl



145
1
2,6-di-iPr-Phenyl



146
2
2,6-di-iPr-Phenyl



147
3
2,6-di-iPr-Phenyl



148
4
2,6-di-iPr-Phenyl



149
1
2-morpholino-phenyl



150
2
2-morpholino-phenyl



151
3
2-morpholino-phenyl



152
4
2-morpholino-phenyl



153
1
3-morpholino-phenyl



154
2
3-morpholino-phenyl



155
3
3-morpholino-phenyl



156
4
3-morpholino-phenyl



157
1
4-morpholino-phenyl



158
2
4-morpholino-phenyl



159
3
4-morpholino-phenyl



160
4
4-morpholino-phenyl



161
1
4-CN-2-morpholino-phenyl



162
2
4-CN-2-morpholino-phenyl



163
3
4-CN-2-morpholino-phenyl



164
4
4-CN-2-morpholino-phenyl



165
1
4-CH3-2-morpholino-phenyl



166
2
4-CH3-2-morpholino-phenyl



167
3
4-CH3-2-morpholino-phenyl



168
4
4-CH3-2-morpholino-phenyl



169
1
4-OH-2-morpholino-phenyl



170
2
4-OH-2-morpholino-phenyl



171
3
4-OH-2-morpholino-phenyl



172
4
4-OH-2-morpholino-phenyl



173
1
naphthylen-2-yl



174
2
naphthylen-2-yl



175
3
naphthylen-2-yl



176
4
naphthylen-2-yl










Exemplary embodiments include compounds having the formula (IX)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 3.













TABLE 3







Entry
n
R3




















1
1
Phenyl



2
2
Phenyl



3
3
Phenyl



4
4
Phenyl



5
1
4-OH-Phenyl



6
2
4-OH-Phenyl



7
3
4-OH-Phenyl



8
4
4-OH-Phenyl



9
1
3-OH-Phenyl



10
2
3-OH-Phenyl



11
3
3-OH-Phenyl



12
4
3-OH-Phenyl



13
1
2-OH-Phenyl



14
2
2-OH-Phenyl



15
3
2-OH-Phenyl



16
4
2-OH-Phenyl



17
1
4-OMe-Phenyl



18
2
4-OMe-Phenyl



19
3
4-OMe-Phenyl



20
4
4-OMe-Phenyl



21
1
3-OMe-Phenyl



22
2
3-OMe-Phenyl



23
3
3-OMe-Phenyl



24
4
3-OMe-Phenyl



25
1
2-OMe-Phenyl



26
2
2-OMe-Phenyl



27
3
2-OMe-Phenyl



28
4
2-OMe-Phenyl



29
1
4-CN-Phenyl



30
2
4-CN-Phenyl



31
3
4-CN-Phenyl



32
4
4-CN-Phenyl



33
1
3-CN-Phenyl



34
2
3-CN-Phenyl



35
3
3-CN-Phenyl



36
4
3-CN-Phenyl



37
1
2-CN-Phenyl



38
2
2-CN-Phenyl



39
3
2-CN-Phenyl



40
4
2-CN-Phenyl



41
1
4-Me-Phenyl



42
2
4-Me-Phenyl



43
3
4-Me-Phenyl



44
4
4-Me-Phenyl



45
1
3-Me-Phenyl



46
2
3-Me-Phenyl



47
3
3-Me-Phenyl



48
4
3-Me-Phenyl



49
1
2-Me-Phenyl



50
2
2-Me-Phenyl



51
3
2-Me-Phenyl



52
4
2-Me-Phenyl



53
1
4-F-Phenyl



54
2
4-F-Phenyl



55
3
4-F-Phenyl



56
4
4-F-Phenyl



57
1
3-F-Phenyl



58
2
3-F-Phenyl



59
3
3-F-Phenyl



60
4
3-F-Phenyl



61
1
2-F-Phenyl



62
2
2-F-Phenyl



63
3
2-F-Phenyl



64
4
2-F-Phenyl



65
1
4-Cl-Phenyl



66
2
4-Cl-Phenyl



67
3
4-Cl-Phenyl



68
4
4-Cl-Phenyl



69
1
3-Cl-Phenyl



70
2
3-Cl-Phenyl



71
3
3-Cl-Phenyl



72
4
3-Cl-Phenyl



73
1
2-Cl-Phenyl



74
2
2-Cl-Phenyl



75
3
2-Cl-Phenyl



76
4



77
1



78
2



79
3



80
4



81
1



82
2



83
3



84
4



85
1



86
2



87
3



88
4



89
1
2-Br-Phenyl



90
2
2-Br-Phenyl



91
3
2-Br-Phenyl



92
4
2-Br-Phenyl



93
1
4-CF3-Phenyl



94
2
4-CF3-Phenyl



95
3
4-CF3-Phenyl



96
4
4-CF3-Phenyl



97
1
3-CF3-Phenyl



98
2
3-CF3-Phenyl



99
3
3-CF3-Phenyl



100
4
3-CF3-Phenyl



101
1
2-CF3-Phenyl



102
2
2-CF3-Phenyl



103
3
2-CF3-Phenyl



104
4
2-CF3-Phenyl



105
1
4-iPr-Phenyl



106
2
4-iPr-Phenyl



107
3
4-iPr-Phenyl



108
4
4-iPr-Phenyl



109
1
3-iPr-Phenyl



110
2
3-iPr-Phenyl



111
3
3-iPr-Phenyl



112
4
3-iPr-Phenyl



113
1
2-iPr-Phenyl



114
2
2-iPr-Phenyl



115
3
2-iPr-Phenyl



116
4
2-iPr-Phenyl



117
1
4-NH2-Phenyl



118
2
4-NH2-Phenyl



119
3
4-NH2-Phenyl



120
4
4-NH2-Phenyl



121
1
3-NH2-Phenyl



122
2
3-NH2-Phenyl



123
3
3-NH2-Phenyl



124
4
3-NH2-Phenyl



125
1
2-NH2-Phenyl



126
2
2-NH2-Phenyl



127
3
2-NH2-Phenyl



128
4
2-NH2-Phenyl



129
1
2,3-di-Me-Phenyl



130
2
2,3-di-Me-Phenyl



131
3
2,3-di-Me-Phenyl



132
4
2,3-di-Me-Phenyl



133
1
2,4-di-Me-Phenyl



134
2
2,4-di-Me-Phenyl



135
3
2,4-di-Me-Phenyl



136
4
2,4-di-Me-Phenyl



137
1
2,5-di-Me-Phenyl



138
2
2,5-di-Me-Phenyl



139
3
2,5-di-Me-Phenyl



140
4
2,5-di-Me-Phenyl



141
1
2,6-di-Me-Phenyl



142
2
2,6-di-Me-Phenyl



143
3
2,6-di-Me-Phenyl



144
4
2,6-di-Me-Phenyl



145
1
2,6-di-iPr-Phenyl



146
2
2,6-di-iPr-Phenyl



147
3
2,6-di-iPr-Phenyl



148
4
2,6-di-iPr-Phenyl



149
1
2-morpholino-phenyl



150
2
2-morpholino-phenyl



151
3
2-morpholino-phenyl



152
4
2-morpholino-phenyl



153
1
3-morpholino-phenyl



154
2
3-morpholino-phenyl



155
3
3-morpholino-phenyl



156
4
3-morpholino-phenyl



157
1
4-morpholino-phenyl



158
2
4-morpholino-phenyl



159
3
4-morpholino-phenyl



160
4
4-morpholino-phenyl



161
1
4-CN-2-morpholino-phenyl



162
2
4-CN-2-morpholino-phenyl



163
3
4-CN-2-morpholino-phenyl



164
4
2-Cl-Phenyl



165
1
4-Br-Phenyl



166
2
4-Br-Phenyl



167
3
4-Br-Phenyl



168
4
4-Br-Phenyl



169
1
3-Br-Phenyl



170
2
3-Br-Phenyl



171
3
3-Br-Phenyl



172
4
3-Br-Phenyl



173
1
naphthylen-1-yl



174
2
naphthylen-1-yl



175
3
naphthylen-1-yl



176
4
naphthylen-1-yl










Exemplary embodiments include compounds having the formula (X)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 4.













TABLE 4







Entry
n
R3




















1
1
Phenyl



2
2
Phenyl



3
3
Phenyl



4
4
Phenyl



5
1
4-OH-Phenyl



6
2
4-OH-Phenyl



7
3
4-OH-Phenyl



8
4
4-OH-Phenyl



9
1
3-OH-Phenyl



10
2
3-OH-Phenyl



11
3
3-OH-Phenyl



12
4
3-OH-Phenyl



13
1
2-OH-Phenyl



14
2
2-OH-Phenyl



15
3
2-OH-Phenyl



16
4
2-OH-Phenyl



17
1
4-OMe-Phenyl



18
2
4-OMe-Phenyl



19
3
4-OMe-Phenyl



20
4
4-OMe-Phenyl



21
1
3-OMe-Phenyl



22
2
3-OMe-Phenyl



23
3
3-OMe-Phenyl



24
4
3-OMe-Phenyl



25
1
2-OMe-Phenyl



26
2
2-OMe-Phenyl



27
3
2-OMe-Phenyl



28
4
2-OMe-Phenyl



29
1
4-CN-Phenyl



30
2
4-CN-Phenyl



31
3
4-CN-Phenyl



32
4
4-CN-Phenyl



33
1
3-CN-Phenyl



34
2
3-CN-Phenyl



35
3
3-CN-Phenyl



36
4
3-CN-Phenyl



37
1
2-CN-Phenyl



38
2
2-CN-Phenyl



39
3
2-CN-Phenyl



40
4
2-CN-Phenyl



41
1
4-Me-Phenyl



42
2
4-Me-Phenyl



43
3
4-Me-Phenyl



44
4
4-Me-Phenyl



45
1
3-Me-Phenyl



46
2
3-Me-Phenyl



47
3
3-Me-Phenyl



48
4
3-Me-Phenyl



49
1
2-Me-Phenyl



50
2
2-Me-Phenyl



51
3
2-Me-Phenyl



52
4
2-Me-Phenyl



53
1
4-F-Phenyl



54
2
4-F-Phenyl



55
3
4-F-Phenyl



56
4
4-F-Phenyl



57
1
3-F-Phenyl



58
2
3-F-Phenyl



59
3
3-F-Phenyl



60
4
3-F-Phenyl



61
1
2-F-Phenyl



62
2
2-F-Phenyl



63
3
2-F-Phenyl



64
4
2-F-Phenyl



65
1
4-Cl-Phenyl



66
2
4-Cl-Phenyl



67
3
4-Cl-Phenyl



68
4
4-Cl-Phenyl



69
1
3-Cl-Phenyl



70
2
3-Cl-Phenyl



71
3
3-Cl-Phenyl



72
4
3-Cl-Phenyl



73
1
2-Cl-Phenyl



74
2
2-Cl-Phenyl



75
3
2-Cl-Phenyl



76
4
2-Cl-Phenyl



77
1
4-Br-Phenyl



78
2
4-Br-Phenyl



79
3
4-Br-Phenyl



80
4
4-Br-Phenyl



81
1
3-Br-Phenyl



82
2
3-Br-Phenyl



83
3
3-Br-Phenyl



84
4
3-Br-Phenyl



85
1
naphthylen-1-yl



86
2
naphthylen-1-yl



87
3
naphthylen-1-yl



88
4
naphthylen-1-yl



89
1
2-Br-Phenyl



90
2
2-Br-Phenyl



91
3
2-Br-Phenyl



92
4
2-Br-Phenyl



93
1
4-CF3-Phenyl



94
2
4-CF3-Phenyl



95
3
4-CF3-Phenyl



96
4
4-CF3-Phenyl



97
1
3-CF3-Phenyl



98
2
3-CF3-Phenyl



99
3
3-CF3-Phenyl



100
4
3-CF3-Phenyl



101
1
2-CF3-Phenyl



102
2
2-CF3-Phenyl



103
3
2-CF3-Phenyl



104
4
2-CF3-Phenyl



105
1
4-iPr-Phenyl



106
2
4-iPr-Phenyl



107
3
4-iPr-Phenyl



108
4
4-iPr-Phenyl



109
1
3-iPr-Phenyl



110
2
3-iPr-Phenyl



111
3
3-iPr-Phenyl



112
4
3-iPr-Phenyl



113
1
2-iPr-Phenyl



114
2
2-iPr-Phenyl



115
3
2-iPr-Phenyl



116
4
2-iPr-Phenyl



117
1
4-NH2-Phenyl



118
2
4-NH2-Phenyl



119
3
4-NH2-Phenyl



120
4
4-NH2-Phenyl



121
1
3-NH2-Phenyl



122
2
3-NH2-Phenyl



123
3
3-NH2-Phenyl



124
4
3-NH2-Phenyl



125
1
2-NH2-Phenyl



126
2
2-NH2-Phenyl



127
3
2-NH2-Phenyl



128
4
2-NH2-Phenyl



129
1
2,3-di-Me-Phenyl



130
2
2,3-di-Me-Phenyl



131
3
2,3-di-Me-Phenyl



132
4
2,3-di-Me-Phenyl



133
1
2,4-di-Me-Phenyl



134
2
2,4-di-Me-Phenyl



135
3
2,4-di-Me-Phenyl



136
4
2,4-di-Me-Phenyl



137
1
2,5-di-Me-Phenyl



138
2
2,5-di-Me-Phenyl



139
3
2,5-di-Me-Phenyl



140
4
2,5-di-Me-Phenyl



141
1
2,6-di-Me-Phenyl



142
2
2,6-di-Me-Phenyl



143
3
2,6-di-Me-Phenyl



144
4
2,6-di-Me-Phenyl



145
1
2,6-di-iPr-Phenyl



146
2
2,6-di-iPr-Phenyl



147
3
2,6-di-iPr-Phenyl



148
4
2,6-di-iPr-Phenyl



149
1
2-morpholino-phenyl



150
2
2-morpholino-phenyl



151
3
2-morpholino-phenyl



152
4
2-morpholino-phenyl



153
1
3-morpholino-phenyl



154
2
3-morpholino-phenyl



155
3
3-morpholino-phenyl



156
4
3-morpholino-phenyl



157
1
4-morpholino-phenyl



158
2
4-morpholino-phenyl



159
3
4-morpholino-phenyl



160
4
4-morpholino-phenyl



161
1
4-CN-2-morpholino-phenyl



162
2
4-CN-2-morpholino-phenyl



163
3
4-CN-2-morpholino-phenyl



164
4
4-CN-2-morpholino-phenyl



165
1
4-CH3-2-morpholino-phenyl



166
2
4-CH3-2-morpholino-phenyl



167
3
4-CH3-2-morpholino-phenyl



168
4
4-CH3-2-morpholino-phenyl



169
1
4-OH-2-morpholino-phenyl



170
2
4-OH-2-morpholino-phenyl



171
3
4-OH-2-morpholino-phenyl



172
4
4-OH-2-morpholino-phenyl



173
1
naphthylen-2-yl



174
2
naphthylen-2-yl



175
3
naphthylen-2-yl



176
4
naphthylen-2-yl










Exemplary embodiments include compounds having the formula (XI)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 5.













TABLE 5







Entry
n
R3




















1
1
Phenyl



2
2
Phenyl



3
3
Phenyl



4
4
Phenyl



5
1
4-OH-Phenyl



6
2
4-OH-Phenyl



7
3
4-OH-Phenyl



8
4
4-OH-Phenyl



9
1
3-OH-Phenyl



10
2
3-OH-Phenyl



11
3
3-OH-Phenyl



12
4
3-OH-Phenyl



13
1
2-OH-Phenyl



14
2
2-OH-Phenyl



15
3
2-OH-Phenyl



16
4
2-OH-Phenyl



17
1
4-OMe-Phenyl



18
2
4-OMe-Phenyl



19
3
4-OMe-Phenyl



20
4
4-OMe-Phenyl



21
1
3-OMe-Phenyl



22
2
3-OMe-Phenyl



23
3
3-OMe-Phenyl



24
4
3-OMe-Phenyl



25
1
2-OMe-Phenyl



26
2
2-OMe-Phenyl



27
3
2-OMe-Phenyl



28
4
2-OMe-Phenyl



29
1
4-CN-Phenyl



30
2
4-CN-Phenyl



31
3
4-CN-Phenyl



32
4
4-CN-Phenyl



33
1
3-CN-Phenyl



34
2
3-CN-Phenyl



35
3
3-CN-Phenyl



36
4
3-CN-Phenyl



37
1
2-CN-Phenyl



38
2
2-CN-Phenyl



39
3
2-CN-Phenyl



40
4
2-CN-Phenyl



41
1
4-Me-Phenyl



42
2
4-Me-Phenyl



43
3
4-Me-Phenyl



44
4
4-Me-Phenyl



45
1
3-Me-Phenyl



46
2
3-Me-Phenyl



47
3
3-Me-Phenyl



48
4
3-Me-Phenyl



49
1
2-Me-Phenyl



50
2
2-Me-Phenyl



51
3
2-Me-Phenyl



52
4
2-Me-Phenyl



53
1
4-F-Phenyl



54
2
4-F-Phenyl



55
3
4-F-Phenyl



56
4
4-F-Phenyl



57
1
3-F-Phenyl



58
2
3-F-Phenyl



59
3
3-F-Phenyl



60
4
3-F-Phenyl



61
1
2-F-Phenyl



62
2
2-F-Phenyl



63
3
2-F-Phenyl



64
4
2-F-Phenyl



65
1
4-Cl-Phenyl



66
2
4-Cl-Phenyl



67
3
4-Cl-Phenyl



68
4
4-Cl-Phenyl



69
1
3-Cl-Phenyl



70
2
3-Cl-Phenyl



71
3
3-Cl-Phenyl



72
4
3-Cl-Phenyl



73
1
2-Cl-Phenyl



74
2
2-Cl-Phenyl



75
3
2-Cl-Phenyl



76
4
2-Cl-Phenyl



77
1
4-Br-Phenyl



78
2
4-Br-Phenyl



79
3
4-Br-Phenyl



80
4
4-Br-Phenyl



81
1
3-Br-Phenyl



82
2
3-Br-Phenyl



83
3
3-Br-Phenyl



84
4
3-Br-Phenyl



85
1
naphthylen-1-yl



86
2
naphthylen-1-yl



87
3
naphthylen-1-yl



88
4
naphthylen-1-yl



85
1
2-Br-Phenyl



86
2
2-Br-Phenyl



87
3
2-Br-Phenyl



88
4
2-Br-Phenyl



89
1
4-CF3-Phenyl



90
2
4-CF3-Phenyl



91
3
4-CF3-Phenyl



92
4
4-CF3-Phenyl



93
1
3-CF3-Phenyl



94
2
3-CF3-Phenyl



95
3
3-CF3-Phenyl



96
4
3-CF3-Phenyl



97
1
2-CF3-Phenyl



98
2
2-CF3-Phenyl



99
3
2-CF3-Phenyl



100
4
2-CF3-Phenyl



101
1
4-iPr-Phenyl



102
2
4-iPr-Phenyl



103
3
4-iPr-Phenyl



104
4
4-iPr-Phenyl



105
1
3-iPr-Phenyl



106
2
3-iPr-Phenyl



107
3
3-iPr-Phenyl



108
4
3-iPr-Phenyl



109
1
2-iPr-Phenyl



110
2
2-iPr-Phenyl



111
3
2-iPr-Phenyl



112
4
2-iPr-Phenyl



113
1
4-NH2-Phenyl



114
2
4-NH2-Phenyl



115
3
4-NH2-Phenyl



116
4
4-NH2-Phenyl



117
1
3-NH2-Phenyl



118
2
3-NH2-Phenyl



119
3
3-NH2-Phenyl



120
4
3-NH2-Phenyl



121
1
2-NH2-Phenyl



122
2
2-NH2-Phenyl



123
3
2-NH2-Phenyl



124
4
2-NH2-Phenyl



125
1
2,3-di-Me-Phenyl



126
2
2,3-di-Me-Phenyl



127
3
2,3-di-Me-Phenyl



128
4
2,3-di-Me-Phenyl



129
1
2,4-di-Me-Phenyl



130
2
2,4-di-Me-Phenyl



131
3
2,4-di-Me-Phenyl



132
4
2,4-di-Me-Phenyl



133
1
2,5-di-Me-Phenyl



134
2
2,5-di-Me-Phenyl



135
3
2,5-di-Me-Phenyl



136
4
2,5-di-Me-Phenyl



137
1
2,6-di-Me-Phenyl



138
2
2,6-di-Me-Phenyl



139
3
2,6-di-Me-Phenyl



140
4
2,6-di-Me-Phenyl



141
1
2,6-di-iPr-Phenyl



142
2
2,6-di-iPr-Phenyl



143
3
2,6-di-iPr-Phenyl



144
4
2,6-di-iPr-Phenyl



145
1
2-morpholino-phenyl



146
2
2-morpholino-phenyl



147
3
2-morpholino-phenyl



148
4
2-morpholino-phenyl



149
1
3-morpholino-phenyl



150
2
3-morpholino-phenyl



151
3
3-morpholino-phenyl



152
4
3-morpholino-phenyl



153
1
4-morpholino-phenyl



154
2
4-morpholino-phenyl



155
3
4-morpholino-phenyl



156
4
4-morpholino-phenyl



157
1
4-CN-2-morpholino-phenyl



158
2
4-CN-2-morpholino-phenyl



159
3
4-CN-2-morpholino-phenyl



160
4
4-CN-2-morpholino-phenyl



161
1
4-CH3-2-morpholino-phenyl



162
2
4-CH3-2-morpholino-phenyl



163
3
4-CH3-2-morpholino-phenyl



164
4
4-CH3-2-morpholino-phenyl



165
1
4-OH-2-morpholino-phenyl



166
2
4-OH-2-morpholino-phenyl



167
3
4-OH-2-morpholino-phenyl



168
4
4-OH-2-morpholino-phenyl



173
1
naphthylen-2-yl



174
2
naphthylen-2-yl



175
3
naphthylen-2-yl



176
4
naphthylen-2-yl










Exemplary embodiments include compounds having the formula (XII)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 6.













TABLE 6





Entry
R1
R2
n
R4



















1
Methyl
Methyl
1
Phenyl


2
Methyl
Methyl
2
Phenyl


3
Methyl
Methyl
3
Phenyl


4
Methyl
Methyl
4
Phenyl


5
Methyl
Methyl
1
4-OH-Phenyl


6
Methyl
Methyl
2
4-OH-Phenyl


7
Methyl
Methyl
3
4-OH-Phenyl


8
Methyl
Methyl
4
4-OH-Phenyl


9
Methyl
Methyl
1
3-OH-Phenyl


10
Methyl
Methyl
2
3-OH-Phenyl


11
Methyl
Methyl
3
3-OH-Phenyl


12
Methyl
Methyl
4
3-OH-Phenyl


13
Methyl
Methyl
1
2-OH-Phenyl


14
Methyl
Methyl
2
2-OH-Phenyl


15
Methyl
Methyl
3
2-OH-Phenyl


16
Methyl
Methyl
4
2-OH-Phenyl


17
Methyl
Methyl
1
4-OMe-Phenyl


18
Methyl
Methyl
2
4-OMe-Phenyl


19
Methyl
Methyl
3
4-OMe-Phenyl


20
Methyl
Methyl
4
4-OMe-Phenyl


21
Methyl
Methyl
1
3-OMe-Phenyl


22
Methyl
Methyl
2
3-OMe-Phenyl


23
Methyl
Methyl
3
3-OMe-Phenyl


24
Methyl
Methyl
4
3-OMe-Phenyl


25
Methyl
Methyl
1
2-OMe-Phenyl


26
Methyl
Methyl
2
2-OMe-Phenyl


27
Methyl
Methyl
3
2-OMe-Phenyl


28
Methyl
Methyl
4
2-OMe-Phenyl


29
Methyl
Methyl
1
4-CN-Phenyl


30
Methyl
Methyl
2
4-CN-Phenyl


31
Methyl
Methyl
3
4-CN-Phenyl


32
Methyl
Methyl
4
4-CN-Phenyl


33
Methyl
Methyl
1
3-CN-Phenyl


34
Methyl
Methyl
2
3-CN-Phenyl


35
Methyl
Methyl
3
3-CN-Phenyl


36
Methyl
Methyl
4
3-CN-Phenyl


37
Methyl
Methyl
1
2-CN-Phenyl


38
Methyl
Methyl
2
2-CN-Phenyl


39
Methyl
Methyl
3
2-CN-Phenyl


40
Methyl
Methyl
4
2-CN-Phenyl


41
Methyl
Methyl
1
4-Me-Phenyl


42
Methyl
Methyl
2
4-Me-Phenyl


43
Methyl
Methyl
3
4-Me-Phenyl


44
Methyl
Methyl
4
4-Me-Phenyl


45
Methyl
Methyl
1
3-Me-Phenyl


46
Methyl
Methyl
2
3-Me-Phenyl


47
Methyl
Methyl
3
3-Me-Phenyl


48
Methyl
Methyl
4
3-Me-Phenyl


49
Methyl
Methyl
1
2-Me-Phenyl


50
Methyl
Methyl
2
2-Me-Phenyl


51
Methyl
Methyl
3
2-Me-Phenyl


52
Methyl
Methyl
4
2-Me-Phenyl


53
Methyl
Methyl
1
4-F-Phenyl


54
Methyl
Methyl
2
4-F-Phenyl


55
Methyl
Methyl
3
4-F-Phenyl


56
Methyl
Methyl
4
4-F-Phenyl


57
Methyl
Methyl
1
3-F-Phenyl


58
Methyl
Methyl
2
3-F-Phenyl


59
Methyl
Methyl
3
3-F-Phenyl


60
Methyl
Methyl
4
3-F-Phenyl


61
Methyl
Methyl
1
2-F-Phenyl


62
Methyl
Methyl
2
2-F-Phenyl


63
Methyl
Methyl
3
2-F-Phenyl


64
Methyl
Methyl
4
2-F-Phenyl


65
Methyl
Methyl
1
4-Cl-Phenyl


66
Methyl
Methyl
2
4-Cl-Phenyl


67
Methyl
Methyl
3
4-Cl-Phenyl


68
Methyl
Methyl
4
4-Cl-Phenyl


69
Methyl
Methyl
1
3-Cl-Phenyl


70
Methyl
Methyl
2
3-Cl-Phenyl


71
Methyl
Methyl
3
3-Cl-Phenyl


72
Methyl
Methyl
4
3-Cl-Phenyl


73
Methyl
Methyl
1
2-Cl-Phenyl


74
Methyl
Methyl
2
2-Cl-Phenyl


75
Methyl
Methyl
3
2-Cl-Phenyl


76
Methyl
Methyl
4
2-Cl-Phenyl


77
Methyl
Methyl
1
4-Br-Phenyl


78
Methyl
Methyl
2
4-Br-Phenyl


79
Methyl
Methyl
3
4-Br-Phenyl


80
Methyl
Methyl
4
4-Br-Phenyl


81
Methyl
Methyl
1
3-Br-Phenyl


82
Methyl
Methyl
2
3-Br-Phenyl


83
Methyl
Methyl
3
3-Br-Phenyl


84
Methyl
Methyl
4
3-Br-Phenyl


85
Methyl
Methyl
1
2-Br-Phenyl


86
Methyl
Methyl
2
2-Br-Phenyl


87
Methyl
Methyl
3
2-Br-Phenyl


88
Methyl
Methyl
4
2-Br-Phenyl


89
Methyl
Methyl
1
4-CF3-Phenyl


90
Methyl
Methyl
2
4-CF3-Phenyl


91
Methyl
Methyl
3
4-CF3-Phenyl


92
Methyl
Methyl
4
4-CF3-Phenyl


93
Methyl
Methyl
1
3-CF3-Phenyl


94
Methyl
Methyl
2
3-CF3-Phenyl


95
Methyl
Methyl
3
3-CF3-Phenyl


96
Methyl
Methyl
4
3-CF3-Phenyl


97
Methyl
Methyl
1
2-CF3-Phenyl


98
Methyl
Methyl
2
2-CF3-Phenyl


99
Methyl
Methyl
3
2-CF3-Phenyl


100
Methyl
Methyl
4
2-CF3-Phenyl


101
Methyl
Methyl
1
4-iPr-Phenyl


102
Methyl
Methyl
2
4-iPr-Phenyl


103
Methyl
Methyl
3
4-iPr-Phenyl


104
Methyl
Methyl
4
4-iPr-Phenyl


105
Methyl
Methyl
1
3-iPr-Phenyl


106
Methyl
Methyl
2
3-iPr-Phenyl


107
Methyl
Methyl
3
3-iPr-Phenyl


108
Methyl
Methyl
4
3-iPr-Phenyl


109
Methyl
Methyl
1
2-iPr-Phenyl


110
Methyl
Methyl
2
2-iPr-Phenyl


111
Methyl
Methyl
3
2-iPr-Phenyl


112
Methyl
Methyl
4
2-iPr-Phenyl


113
Methyl
Methyl
1
4-NH2-Phenyl


114
Methyl
Methyl
2
4-NH2-Phenyl


115
Methyl
Methyl
3
4-NH2-Phenyl


116
Methyl
Methyl
4
4-NH2-Phenyl


117
Methyl
Methyl
1
3-NH2-Phenyl


118
Methyl
Methyl
2
3-NH2-Phenyl


119
Methyl
Methyl
3
3-NH2-Phenyl


120
Methyl
Methyl
4
3-NH2-Phenyl


121
Methyl
Methyl
1
2-NH2-Phenyl


122
Methyl
Methyl
2
2-NH2-Phenyl


123
Methyl
Methyl
3
2-NH2-Phenyl


124
Methyl
Methyl
4
2-NH2-Phenyl


125
Methyl
Methyl
1
2,3-di-Me-Phenyl


126
Methyl
Methyl
2
2,3-di-Me-Phenyl


127
Methyl
Methyl
3
2,3-di-Me-Phenyl


128
Methyl
Methyl
4
2,3-di-Me-Phenyl


129
Methyl
Methyl
1
2,4-di-Me-Phenyl


130
Methyl
Methyl
2
2,4-di-Me-Phenyl


131
Methyl
Methyl
3
2,4-di-Me-Phenyl


132
Methyl
Methyl
4
2,4-di-Me-Phenyl


133
Methyl
Methyl
1
2,5-di-Me-Phenyl


134
Methyl
Methyl
2
2,5-di-Me-Phenyl


135
Methyl
Methyl
3
2,5-di-Me-Phenyl


136
Methyl
Methyl
4
2,5-di-Me-Phenyl


137
Methyl
Methyl
1
2,6-di-Me-Phenyl


138
Methyl
Methyl
2
2,6-di-Me-Phenyl


139
Methyl
Methyl
3
2,6-di-Me-Phenyl


140
Methyl
Methyl
4
2,6-di-Me-Phenyl


141
Methyl
Methyl
1
2,6-di-iPr-Phenyl


142
Methyl
Methyl
2
2,6-di-iPr-Phenyl


143
Methyl
Methyl
3
2,6-di-iPr-Phenyl


144
Methyl
Methyl
4
2,6-di-iPr-Phenyl


145
Methyl
Methyl
1
2-morpholino-phenyl


146
Methyl
Methyl
2
2-morpholino-phenyl


147
Methyl
Methyl
3
2-morpholino-phenyl


148
Methyl
Methyl
4
2-morpholino-phenyl


149
Methyl
Methyl
1
3-morpholino-phenyl


150
Methyl
Methyl
2
3-morpholino-phenyl


151
Methyl
Methyl
3
3-morpholino-phenyl


152
Methyl
Methyl
4
3-morpholino-phenyl


153
Methyl
Methyl
1
4-morpholino-phenyl


154
Methyl
Methyl
2
4-morpholino-phenyl


155
Methyl
Methyl
3
4-morpholino-phenyl


156
Methyl
Methyl
4
4-morpholino-phenyl


157
Methyl
Methyl
1
4-CN-2-morpholino-phenyl


158
Methyl
Methyl
2
4-CN-2-morpholino-phenyl


159
Methyl
Methyl
3
4-CN-2-morpholino-phenyl


160
Methyl
Methyl
4
4-CN-2-morpholino-phenyl


161
Methyl
Methyl
1
4-CH3-2-morpholino-phenyl


162
Methyl
Methyl
2
4-CH3-2-morpholino-phenyl


163
Methyl
Methyl
3
4-CH3-2-morpholino-phenyl


164
Methyl
Methyl
4
4-CH3-2-morpholino-phenyl


165
Methyl
Methyl
1
4-OH-2-morpholino-phenyl


166
Methyl
Methyl
2
4-OH-2-morpholino-phenyl


167
Methyl
Methyl
3
4-OH-2-morpholino-phenyl


168
Methyl
Methyl
4
4-OH-2-morpholino-phenyl


169
Methyl
Methyl
1
naphthylen-1-yl


170
Methyl
Methyl
2
naphthylen-1-yl


171
Methyl
Methyl
3
naphthylen-1-yl


172
Methyl
Methyl
4
naphthylen-1-yl


173
Methyl
Methyl
1
naphthylen-2-yl


174
Methyl
Methyl
2
naphthylen-2-yl


175
Methyl
Methyl
3
naphthylen-2-yl


176
Methyl
Methyl
4
naphthylen-2-yl


177
Ethyl
Ethyl
1
Phenyl


178
Ethyl
Ethyl
2
Phenyl


179
Ethyl
Ethyl
3
Phenyl


180
Ethyl
Ethyl
4
Phenyl


181
Ethyl
Ethyl
1
4-OH-Phenyl


182
Ethyl
Ethyl
2
4-OH-Phenyl


183
Ethyl
Ethyl
3
4-OH-Phenyl


184
Ethyl
Ethyl
4
4-OH-Phenyl


185
Ethyl
Ethyl
1
3-OH-Phenyl


186
Ethyl
Ethyl
2
3-OH-Phenyl


187
Ethyl
Ethyl
3
3-OH-Phenyl


188
Ethyl
Ethyl
4
3-OH-Phenyl


189
Ethyl
Ethyl
1
2-OH-Phenyl


190
Ethyl
Ethyl
2
2-OH-Phenyl


191
Ethyl
Ethyl
3
2-OH-Phenyl


192
Ethyl
Ethyl
4
2-OH-Phenyl


193
Ethyl
Ethyl
1
4-OMe-Phenyl


194
Ethyl
Ethyl
2
4-OMe-Phenyl


195
Ethyl
Ethyl
3
4-OMe-Phenyl


196
Ethyl
Ethyl
4
4-OMe-Phenyl


197
Ethyl
Ethyl
1
3-OMe-Phenyl


198
Ethyl
Ethyl
2
3-OMe-Phenyl


199
Ethyl
Ethyl
3
3-OMe-Phenyl


200
Ethyl
Ethyl
4
3-OMe-Phenyl


201
Ethyl
Ethyl
1
2-OMe-Phenyl


202
Ethyl
Ethyl
2
2-OMe-Phenyl


203
Ethyl
Ethyl
3
2-OMe-Phenyl


204
Ethyl
Ethyl
4
2-OMe-Phenyl


205
Ethyl
Ethyl
1
4-CN-Phenyl


206
Ethyl
Ethyl
2
4-CN-Phenyl


207
Ethyl
Ethyl
3
4-CN-Phenyl


208
Ethyl
Ethyl
4
4-CN-Phenyl


209
Ethyl
Ethyl
1
3-CN-Phenyl


210
Ethyl
Ethyl
2
3-CN-Phenyl


211
Ethyl
Ethyl
3
3-CN-Phenyl


212
Ethyl
Ethyl
4
3-CN-Phenyl


213
Ethyl
Ethyl
1
2-CN-Phenyl


214
Ethyl
Ethyl
2
2-CN-Phenyl


215
Ethyl
Ethyl
3
2-CN-Phenyl


216
Ethyl
Ethyl
4
2-CN-Phenyl


217
Ethyl
Ethyl
1
4-Me-Phenyl


218
Ethyl
Ethyl
2
4-Me-Phenyl


219
Ethyl
Ethyl
3
4-Me-Phenyl


220
Ethyl
Ethyl
4
4-Me-Phenyl


221
Ethyl
Ethyl
1
3-Me-Phenyl


222
Ethyl
Ethyl
2
3-Me-Phenyl


223
Ethyl
Ethyl
3
3-Me-Phenyl


224
Ethyl
Ethyl
4
3-Me-Phenyl


225
Ethyl
Ethyl
1
2-Me-Phenyl


226
Ethyl
Ethyl
2
2-Me-Phenyl


227
Ethyl
Ethyl
3
2-Me-Phenyl


228
Ethyl
Ethyl
4
2-Me-Phenyl


229
Ethyl
Ethyl
1
4-F-Phenyl


230
Ethyl
Ethyl
2
4-F-Phenyl


231
Ethyl
Ethyl
3
4-F-Phenyl


232
Ethyl
Ethyl
4
4-F-Phenyl


233
Ethyl
Ethyl
1
3-F-Phenyl


234
Ethyl
Ethyl
2
3-F-Phenyl


235
Ethyl
Ethyl
3
3-F-Phenyl


236
Ethyl
Ethyl
4
3-F-Phenyl


237
Ethyl
Ethyl
1
2-F-Phenyl


238
Ethyl
Ethyl
2
2-F-Phenyl


239
Ethyl
Ethyl
3
2-F-Phenyl


240
Ethyl
Ethyl
4
2-F-Phenyl


241
Ethyl
Ethyl
1
4-Cl-Phenyl


242
Ethyl
Ethyl
2
4-Cl-Phenyl


243
Ethyl
Ethyl
3
4-Cl-Phenyl


244
Ethyl
Ethyl
4
4-Cl-Phenyl


245
Ethyl
Ethyl
1
3-Cl-Phenyl


246
Ethyl
Ethyl
2
3-Cl-Phenyl


247
Ethyl
Ethyl
3
3-Cl-Phenyl


248
Ethyl
Ethyl
4
3-Cl-Phenyl


249
Ethyl
Ethyl
1
2-Cl-Phenyl


250
Ethyl
Ethyl
2
2-Cl-Phenyl


251
Ethyl
Ethyl
3
2-Cl-Phenyl


252
Ethyl
Ethyl
4
2-Cl-Phenyl


253
Ethyl
Ethyl
1
4-Br-Phenyl


254
Ethyl
Ethyl
2
4-Br-Phenyl


255
Ethyl
Ethyl
3
4-Br-Phenyl


256
Ethyl
Ethyl
4
4-Br-Phenyl


257
Ethyl
Ethyl
1
3-Br-Phenyl


258
Ethyl
Ethyl
2
3-Br-Phenyl


259
Ethyl
Ethyl
3
3-Br-Phenyl


260
Ethyl
Ethyl
4
3-Br-Phenyl


261
Ethyl
Ethyl
1
2-Br-Phenyl


262
Ethyl
Ethyl
2
2-Br-Phenyl


263
Ethyl
Ethyl
3
2-Br-Phenyl


264
Ethyl
Ethyl
4
2-Br-Phenyl


265
Ethyl
Ethyl
1
4-CF3-Phenyl


266
Ethyl
Ethyl
2
4-CF3-Phenyl


267
Ethyl
Ethyl
3
4-CF3-Phenyl


268
Ethyl
Ethyl
4
4-CF3-Phenyl


269
Ethyl
Ethyl
1
3-CF3-Phenyl


270
Ethyl
Ethyl
2
3-CF3-Phenyl


271
Ethyl
Ethyl
3
3-CF3-Phenyl


272
Ethyl
Ethyl
4
3-CF3-Phenyl


273
Ethyl
Ethyl
1
2-CF3-Phenyl


274
Ethyl
Ethyl
2
2-CF3-Phenyl


275
Ethyl
Ethyl
3
2-CF3-Phenyl


276
Ethyl
Ethyl
4
2-CF3-Phenyl


277
Ethyl
Ethyl
1
4-iPr-Phenyl


278
Ethyl
Ethyl
2
4-iPr-Phenyl


279
Ethyl
Ethyl
3
4-iPr-Phenyl


280
Ethyl
Ethyl
4
4-iPr-Phenyl


281
Ethyl
Ethyl
1
3-iPr-Phenyl


282
Ethyl
Ethyl
2
3-iPr-Phenyl


283
Ethyl
Ethyl
3
3-iPr-Phenyl


284
Ethyl
Ethyl
4
3-iPr-Phenyl


285
Ethyl
Ethyl
1
2-iPr-Phenyl


286
Ethyl
Ethyl
2
2-iPr-Phenyl


287
Ethyl
Ethyl
3
2-iPr-Phenyl


288
Ethyl
Ethyl
4
2-iPr-Phenyl


289
Ethyl
Ethyl
1
4-NH2-Phenyl


290
Ethyl
Ethyl
2
4-NH2-Phenyl


291
Ethyl
Ethyl
3
4-NH2-Phenyl


292
Ethyl
Ethyl
4
4-NH2-Phenyl


293
Ethyl
Ethyl
1
3-NH2-Phenyl


294
Ethyl
Ethyl
2
3-NH2-Phenyl


295
Ethyl
Ethyl
3
3-NH2-Phenyl


296
Ethyl
Ethyl
4
3-NH2-Phenyl


297
Ethyl
Ethyl
1
2-NH2-Phenyl


298
Ethyl
Ethyl
2
2-NH2-Phenyl


299
Ethyl
Ethyl
3
2-NH2-Phenyl


300
Ethyl
Ethyl
4
2-NH2-Phenyl


301
Ethyl
Ethyl
1
2,3-di-Me-Phenyl


302
Ethyl
Ethyl
2
2,3-di-Me-Phenyl


303
Ethyl
Ethyl
3
2,3-di-Me-Phenyl


304
Ethyl
Ethyl
4
2,3-di-Me-Phenyl


305
Ethyl
Ethyl
1
2,4-di-Me-Phenyl


306
Ethyl
Ethyl
2
2,4-di-Me-Phenyl


307
Ethyl
Ethyl
3
2,4-di-Me-Phenyl


308
Ethyl
Ethyl
4
2,4-di-Me-Phenyl


309
Ethyl
Ethyl
1
2,5-di-Me-Phenyl


310
Ethyl
Ethyl
2
2,5-di-Me-Phenyl


311
Ethyl
Ethyl
3
2,5-di-Me-Phenyl


312
Ethyl
Ethyl
4
2,5-di-Me-Phenyl


313
Ethyl
Ethyl
1
2,6-di-Me-Phenyl


314
Ethyl
Ethyl
2
2,6-di-Me-Phenyl


315
Ethyl
Ethyl
3
2,6-di-Me-Phenyl


316
Ethyl
Ethyl
4
2,6-di-Me-Phenyl


317
Ethyl
Ethyl
1
2,6-di-iPr-Phenyl


318
Ethyl
Ethyl
2
2,6-di-iPr-Phenyl


319
Ethyl
Ethyl
3
2,6-di-iPr-Phenyl


320
Ethyl
Ethyl
4
2,6-di-iPr-Phenyl


321
Ethyl
Ethyl
1
2-morpholino-phenyl


322
Ethyl
Ethyl
2
2-morpholino-phenyl


323
Ethyl
Ethyl
3
2-morpholino-phenyl


324
Ethyl
Ethyl
4
2-morpholino-phenyl


325
Ethyl
Ethyl
1
3-morpholino-phenyl


326
Ethyl
Ethyl
2
3-morpholino-phenyl


327
Ethyl
Ethyl
3
3-morpholino-phenyl


328
Ethyl
Ethyl
4
3-morpholino-phenyl


329
Ethyl
Ethyl
1
4-morpholino-phenyl


330
Ethyl
Ethyl
2
4-morpholino-phenyl


331
Ethyl
Ethyl
3
4-morpholino-phenyl


332
Ethyl
Ethyl
4
4-morpholino-phenyl


333
Ethyl
Ethyl
1
4-CN-2-morpholino-phenyl


334
Ethyl
Ethyl
2
4-CN-2-morpholino-phenyl


335
Ethyl
Ethyl
3
4-CN-2-morpholino-phenyl


336
Ethyl
Ethyl
4
4-CN-2-morpholino-phenyl


337
Ethyl
Ethyl
1
4-CH3-2-morpholino-phenyl


338
Ethyl
Ethyl
2
4-CH3-2-morpholino-phenyl


339
Ethyl
Ethyl
3
4-CH3-2-morpholino-phenyl


340
Ethyl
Ethyl
4
4-CH3-2-morpholino-phenyl


341
Ethyl
Ethyl
1
4-OH-2-morpholino-phenyl


342
Ethyl
Ethyl
2
4-OH-2-morpholino-phenyl


343
Ethyl
Ethyl
3
4-OH-2-morpholino-phenyl


344
Ethyl
Ethyl
4
4-OH-2-morpholino-phenyl


345
Ethyl
Ethyl
1
naphthylen-1-yl


346
Ethyl
Ethyl
2
naphthylen-1-yl


347
Ethyl
Ethyl
3
naphthylen-1-yl


348
Ethyl
Ethyl
4
naphthylen-2-yl


349
Ethyl
Ethyl
1
naphthylen-2-yl


350
Ethyl
Ethyl
2
naphthylen-2-yl


351
Ethyl
Ethyl
3
naphthylen-2-yl


352
Ethyl
Ethyl
4
naphthylen-2-yl









Exemplary embodiments include compounds having the formula (XIII)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 7













TABLE 7







Entry
n
R4




















1
1
Phenyl



2
2
Phenyl



3
3
Phenyl



4
4
Phenyl



5
1
4-OH-Phenyl



6
2
4-OH-Phenyl



7
3
4-OH-Phenyl



8
4
4-OH-Phenyl



9
1
3-OH-Phenyl



10
2
3-OH-Phenyl



11
3
3-OH-Phenyl



12
4
3-OH-Phenyl



13
1
2-OH-Phenyl



14
2
2-OH-Phenyl



15
3
2-OH-Phenyl



16
4
2-OH-Phenyl



17
1
4-OMe-Phenyl



18
2
4-OMe-Phenyl



19
3
4-OMe-Phenyl



20
4
4-OMe-Phenyl



21
1
3-OMe-Phenyl



22
2
3-OMe-Phenyl



23
3
3-OMe-Phenyl



24
4
3-OMe-Phenyl



25
1
2-OMe-Phenyl



26
2
2-OMe-Phenyl



27
3
2-OMe-Phenyl



28
4
2-OMe-Phenyl



29
1
4-CN-Phenyl



30
2
4-CN-Phenyl



31
3
4-CN-Phenyl



32
4
4-CN-Phenyl



33
1
3-CN-Phenyl



34
2
3-CN-Phenyl



35
3
3-CN-Phenyl



36
4
3-CN-Phenyl



37
1
2-CN-Phenyl



38
2
2-CN-Phenyl



39
3
2-CN-Phenyl



40
4
2-CN-Phenyl



41
1
4-Me-Phenyl



42
2
4-Me-Phenyl



43
3
4-Me-Phenyl



44
4
4-Me-Phenyl



45
1
3-Me-Phenyl



46
2
3-Me-Phenyl



47
3
3-Me-Phenyl



48
4
3-Me-Phenyl



49
1
2-Me-Phenyl



50
2
2-Me-Phenyl



51
3
2-Me-Phenyl



52
4
2-Me-Phenyl



53
1
4-F-Phenyl



54
2
4-F-Phenyl



55
3
4-F-Phenyl



56
4
4-F-Phenyl



57
1
3-F-Phenyl



58
2
3-F-Phenyl



59
3
3-F-Phenyl



60
4
3-F-Phenyl



61
1
2-F-Phenyl



62
2
2-F-Phenyl



63
3
2-F-Phenyl



64
4
2-F-Phenyl



65
1
4-Cl-Phenyl



66
2
4-Cl-Phenyl



67
3
4-Cl-Phenyl



68
4
4-Cl-Phenyl



69
1
3-Cl-Phenyl



70
2
3-Cl-Phenyl



71
3
3-Cl-Phenyl



72
4
3-Cl-Phenyl



73
1
2-Cl-Phenyl



74
2
2-Cl-Phenyl



75
3
2-Cl-Phenyl



76
4
2-Cl-Phenyl



77
1
4-Br-Phenyl



78
2
4-Br-Phenyl



79
3
4-Br-Phenyl



80
4
4-Br-Phenyl



81
1
3-Br-Phenyl



82
2
3-Br-Phenyl



83
3
3-Br-Phenyl



84
4
3-Br-Phenyl



85
1
naphthylen-1-yl



86
2
naphthylen-1-yl



87
3
naphthylen-1-yl



88
4
naphthylen-1-yl



85
1
2-Br-Phenyl



86
2
2-Br-Phenyl



87
3
2-Br-Phenyl



88
4
2-Br-Phenyl



89
1
4-CF3-Phenyl



90
2
4-CF3-Phenyl



91
3
4-CF3-Phenyl



92
4
4-CF3-Phenyl



93
1
3-CF3-Phenyl



94
2
3-CF3-Phenyl



95
3
3-CF3-Phenyl



96
4
3-CF3-Phenyl



97
1
2-CF3-Phenyl



98
2
2-CF3-Phenyl



99
3
2-CF3-Phenyl



100
4
2-CF3-Phenyl



101
1
4-iPr-Phenyl



102
2
4-iPr-Phenyl



103
3
4-iPr-Phenyl



104
4
4-iPr-Phenyl



105
1
3-iPr-Phenyl



106
2
3-iPr-Phenyl



107
3
3-iPr-Phenyl



108
4
3-iPr-Phenyl



109
1
2-iPr-Phenyl



110
2
2-iPr-Phenyl



111
3
2-iPr-Phenyl



112
4
2-iPr-Phenyl



113
1
4-NH2-Phenyl



114
2
4-NH2-Phenyl



115
3
4-NH2-Phenyl



116
4
4-NH2-Phenyl



117
1
3-NH2-Phenyl



118
2
3-NH2-Phenyl



119
3
3-NH2-Phenyl



120
4
3-NH2-Phenyl



121
1
2-NH2-Phenyl



122
2
2-NH2-Phenyl



123
3
2-NH2-Phenyl



124
4
2-NH2-Phenyl



125
1
2,3-di-Me-Phenyl



126
2
2,3-di-Me-Phenyl



127
3
2,3-di-Me-Phenyl



128
4
2,3-di-Me-Phenyl



129
1
2,4-di-Me-Phenyl



130
2
2,4-di-Me-Phenyl



131
3
2,4-di-Me-Phenyl



132
4
2,4-di-Me-Phenyl



133
1
2,5-di-Me-Phenyl



134
2
2,5-di-Me-Phenyl



135
3
2,5-di-Me-Phenyl



136
4
2,5-di-Me-Phenyl



137
1
2,6-di-Me-Phenyl



138
2
2,6-di-Me-Phenyl



139
3
2,6-di-Me-Phenyl



140
4
2,6-di-Me-Phenyl



141
1
2,6-di-iPr-Phenyl



142
2
2,6-di-iPr-Phenyl



143
3
2,6-di-iPr-Phenyl



144
4
2,6-di-iPr-Phenyl



145
1
2-morpholino-phenyl



146
2
2-morpholino-phenyl



147
3
2-morpholino-phenyl



148
4
2-morpholino-phenyl



149
1
3-morpholino-phenyl



150
2
3-morpholino-phenyl



151
3
3-morpholino-phenyl



152
4
3-morpholino-phenyl



153
1
4-morpholino-phenyl



154
2
4-morpholino-phenyl



155
3
4-morpholino-phenyl



156
4
4-morpholino-phenyl



157
1
4-CN-2-morpholino-phenyl



158
2
4-CN-2-morpholino-phenyl



159
3
4-CN-2-morpholino-phenyl



160
4
4-CN-2-morpholino-phenyl



161
1
4-CH3-2-morpholino-phenyl



162
2
4-CH3-2-morpholino-phenyl



163
3
4-CH3-2-morpholino-phenyl



164
4
4-CH3-2-morpholino-phenyl



165
1
4-OH-2-morpholino-phenyl



166
2
4-OH-2-morpholino-phenyl



167
3
4-OH-2-morpholino-phenyl



168
4
4-OH-2-morpholino-phenyl



173
1
naphthylen-2-yl



174
2
naphthylen-2-yl



175
3
naphthylen-2-yl



176
4
naphthylen-2-yl










Exemplary embodiments include compounds having the formula (XIV)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 8.













TABLE 8







Entry
n
R4




















1
1
Phenyl



2
2
Phenyl



3
3
Phenyl



4
4
Phenyl



5
1
4-OH-Phenyl



6
2
4-OH-Phenyl



7
3
4-OH-Phenyl



8
4
4-OH-Phenyl



9
1
3-OH-Phenyl



10
2
3-OH-Phenyl



11
3
3-OH-Phenyl



12
4
3-OH-Phenyl



13
1
2-OH-Phenyl



14
2
2-OH-Phenyl



15
3
2-OH-Phenyl



16
4
2-OH-Phenyl



17
1
4-OMe-Phenyl



18
2
4-OMe-Phenyl



19
3
4-OMe-Phenyl



20
4
4-OMe-Phenyl



21
1
3-OMe-Phenyl



22
2
3-OMe-Phenyl



23
3
3-OMe-Phenyl



24
4
3-OMe-Phenyl



25
1
2-OMe-Phenyl



26
2
2-OMe-Phenyl



27
3
2-OMe-Phenyl



28
4
2-OMe-Phenyl



29
1
4-CN-Phenyl



30
2
4-CN-Phenyl



31
3
4-CN-Phenyl



32
4
4-CN-Phenyl



33
1
3-CN-Phenyl



34
2
3-CN-Phenyl



35
3
3-CN-Phenyl



36
4
3-CN-Phenyl



37
1
2-CN-Phenyl



38
2
2-CN-Phenyl



39
3
2-CN-Phenyl



40
4
2-CN-Phenyl



41
1
4-Me-Phenyl



42
2
4-Me-Phenyl



43
3
4-Me-Phenyl



44
4
4-Me-Phenyl



45
1
3-Me-Phenyl



46
2
3-Me-Phenyl



47
3
3-Me-Phenyl



48
4
3-Me-Phenyl



49
1
2-Me-Phenyl



50
2
2-Me-Phenyl



51
3
2-Me-Phenyl



52
4
2-Me-Phenyl



53
1
4-F-Phenyl



54
2
4-F-Phenyl



55
3
4-F-Phenyl



56
4
4-F-Phenyl



57
1
3-F-Phenyl



58
2
3-F-Phenyl



59
3
3-F-Phenyl



60
4
3-F-Phenyl



61
1
2-F-Phenyl



62
2
2-F-Phenyl



63
3
2-F-Phenyl



64
4
2-F-Phenyl



65
1
4-Cl-Phenyl



66
2
4-Cl-Phenyl



67
3
4-Cl-Phenyl



68
4
4-Cl-Phenyl



69
1
3-Cl-Phenyl



70
2
3-Cl-Phenyl



71
3
3-Cl-Phenyl



72
4
3-Cl-Phenyl



73
1
2-Cl-Phenyl



74
2
2-Cl-Phenyl



75
3
2-Cl-Phenyl



76
4
2-Cl-Phenyl



77
1
4-Br-Phenyl



78
2
4-Br-Phenyl



79
3
4-Br-Phenyl



80
4
4-Br-Phenyl



81
1
3-Br-Phenyl



82
2
3-Br-Phenyl



83
3
3-Br-Phenyl



84
4
3-Br-Phenyl



85
1
naphthylen-1-yl



86
2
naphthylen-1-yl



87
3
naphthylen-1-yl



88
4
naphthylen-1-yl



85
1
2-Br-Phenyl



86
2
2-Br-Phenyl



87
3
2-Br-Phenyl



88
4
2-Br-Phenyl



89
1
4-CF3-Phenyl



90
2
4-CF3-Phenyl



91
3
4-CF3-Phenyl



92
4
4-CF3-Phenyl



93
1
3-CF3-Phenyl



94
2
3-CF3-Phenyl



95
3
3-CF3-Phenyl



96
4
3-CF3-Phenyl



97
1
2-CF3-Phenyl



98
2
2-CF3-Phenyl



99
3
2-CF3-Phenyl



100
4
2-CF3-Phenyl



101
1
4-iPr-Phenyl



102
2
4-iPr-Phenyl



103
3
4-iPr-Phenyl



104
4
4-iPr-Phenyl



105
1
3-iPr-Phenyl



106
2
3-iPr-Phenyl



107
3
3-iPr-Phenyl



108
4
3-iPr-Phenyl



109
1
2-iPr-Phenyl



110
2
2-iPr-Phenyl



111
3
2-iPr-Phenyl



112
4
2-iPr-Phenyl



113
1
4-NH2-Phenyl



114
2
4-NH2-Phenyl



115
3
4-NH2-Phenyl



116
4
4-NH2-Phenyl



117
1
3-NH2-Phenyl



118
2
3-NH2-Phenyl



119
3
3-NH2-Phenyl



120
4
3-NH2-Phenyl



121
1
2-NH2-Phenyl



122
2
2-NH2-Phenyl



123
3
2-NH2-Phenyl



124
4
2-NH2-Phenyl



125
1
2,3-di-Me-Phenyl



126
2
2,3-di-Me-Phenyl



127
3
2,3-di-Me-Phenyl



128
4
2,3-di-Me-Phenyl



129
1
2,4-di-Me-Phenyl



130
2
2,4-di-Me-Phenyl



131
3
2,4-di-Me-Phenyl



132
4
2,4-di-Me-Phenyl



133
1
2,5-di-Me-Phenyl



134
2
2,5-di-Me-Phenyl



135
3
2,5-di-Me-Phenyl



136
4
2,5-di-Me-Phenyl



137
1
2,6-di-Me-Phenyl



138
2
2,6-di-Me-Phenyl



139
3
2,6-di-Me-Phenyl



140
4
2,6-di-Me-Phenyl



141
1
2,6-di-iPr-Phenyl



142
2
2,6-di-iPr-Phenyl



143
3
2,6-di-iPr-Phenyl



144
4
2,6-di-iPr-Phenyl



145
1
2-morpholino-phenyl



146
2
2-morpholino-phenyl



147
3
2-morpholino-phenyl



148
4
2-morpholino-phenyl



149
1
3-morpholino-phenyl



150
2
3-morpholino-phenyl



151
3
3-morpholino-phenyl



152
4
3-morpholino-phenyl



153
1
4-morpholino-phenyl



154
2
4-morpholino-phenyl



155
3
4-morpholino-phenyl



156
4
4-morpholino-phenyl



157
1
4-CN-2-morpholino-phenyl



158
2
4-CN-2-morpholino-phenyl



159
3
4-CN-2-morpholino-phenyl



160
4
4-CN-2-morpholino-phenyl



161
1
4-CH3-2-morpholino-phenyl



162
2
4-CH3-2-morpholino-phenyl



163
3
4-CH3-2-morpholino-phenyl



164
4
4-CH3-2-morpholino-phenyl



165
1
4-OH-2-morpholino-phenyl



166
2
4-OH-2-morpholino-phenyl



167
3
4-OH-2-morpholino-phenyl



168
4
4-OH-2-morpholino-phenyl



173
1
naphthylen-2-yl



174
2
naphthylen-2-yl



175
3
naphthylen-2-yl



176
4
naphthylen-2-yl










Exemplary embodiments include compounds having the formula (XV)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 9.













TABLE 9







Entry
n
R4




















1
1
Phenyl



2
2
Phenyl



3
3
Phenyl



4
4
Phenyl



5
1
4-OH-Phenyl



6
2
4-OH-Phenyl



7
3
4-OH-Phenyl



8
4
4-OH-Phenyl



9
1
3-OH-Phenyl



10
2
3-OH-Phenyl



11
3
3-OH-Phenyl



12
4
3-OH-Phenyl



13
1
2-OH-Phenyl



14
2
2-OH-Phenyl



15
3
2-OH-Phenyl



16
4
2-OH-Phenyl



17
1
4-OMe-Phenyl



18
2
4-OMe-Phenyl



19
3
4-OMe-Phenyl



20
4
4-OMe-Phenyl



21
1
3-OMe-Phenyl



22
2
3-OMe-Phenyl



23
3
3-OMe-Phenyl



24
4
3-OMe-Phenyl



25
1
2-OMe-Phenyl



26
2
2-OMe-Phenyl



27
3
2-OMe-Phenyl



28
4
2-OMe-Phenyl



29
1
4-CN-Phenyl



30
2
4-CN-Phenyl



31
3
4-CN-Phenyl



32
4
4-CN-Phenyl



33
1
3-CN-Phenyl



34
2
3-CN-Phenyl



35
3
3-CN-Phenyl



36
4
3-CN-Phenyl



37
1
2-CN-Phenyl



38
2
2-CN-Phenyl



39
3
2-CN-Phenyl



40
4
2-CN-Phenyl



41
1
4-Me-Phenyl



42
2
4-Me-Phenyl



43
3
4-Me-Phenyl



44
4
4-Me-Phenyl



45
1
3-Me-Phenyl



46
2
3-Me-Phenyl



47
3
3-Me-Phenyl



48
4
3-Me-Phenyl



49
1
2-Me-Phenyl



50
2
2-Me-Phenyl



51
3
2-Me-Phenyl



52
4
2-Me-Phenyl



53
1
4-F-Phenyl



54
2
4-F-Phenyl



55
3
4-F-Phenyl



56
4
4-F-Phenyl



57
1
3-F-Phenyl



58
2
3-F-Phenyl



59
3
3-F-Phenyl



60
4
3-F-Phenyl



61
1
2-F-Phenyl



62
2
2-F-Phenyl



63
3
2-F-Phenyl



64
4
2-F-Phenyl



65
1
4-Cl-Phenyl



66
2
4-Cl-Phenyl



67
3
4-Cl-Phenyl



68
4
4-Cl-Phenyl



69
1
3-Cl-Phenyl



70
2
3-Cl-Phenyl



71
3
3-Cl-Phenyl



72
4
3-Cl-Phenyl



73
1
2-Cl-Phenyl



74
2
2-Cl-Phenyl



75
3
2-Cl-Phenyl



76
4
2-Cl-Phenyl



77
1
4-Br-Phenyl



78
2
4-Br-Phenyl



79
3
4-Br-Phenyl



80
4
4-Br-Phenyl



81
1
3-Br-Phenyl



82
2
3-Br-Phenyl



83
3
3-Br-Phenyl



84
4
3-Br-Phenyl



85
1
naphthylen-1-yl



86
2
naphthylen-1-yl



87
3
naphthylen-1-yl



88
4
naphthylen-1-yl



85
1
2-Br-Phenyl



86
2
2-Br-Phenyl



87
3
2-Br-Phenyl



88
4
2-Br-Phenyl



89
1
4-CF3-Phenyl



90
2
4-CF3-Phenyl



91
3
4-CF3-Phenyl



92
4
4-CF3-Phenyl



93
1
3-CF3-Phenyl



94
2
3-CF3-Phenyl



95
3
3-CF3-Phenyl



96
4
3-CF3-Phenyl



97
1
2-CF3-Phenyl



98
2
2-CF3-Phenyl



99
3
2-CF3-Phenyl



100
4
2-CF3-Phenyl



101
1
4-iPr-Phenyl



102
2
4-iPr-Phenyl



103
3
4-iPr-Phenyl



104
4
4-iPr-Phenyl



105
1
3-iPr-Phenyl



106
2
3-iPr-Phenyl



107
3
3-iPr-Phenyl



108
4
3-iPr-Phenyl



109
1
2-iPr-Phenyl



110
2
2-iPr-Phenyl



111
3
2-iPr-Phenyl



112
4
2-iPr-Phenyl



113
1
4-NH2-Phenyl



114
2
4-NH2-Phenyl



115
3
4-NH2-Phenyl



116
4
4-NH2-Phenyl



117
1
3-NH2-Phenyl



118
2
3-NH2-Phenyl



119
3
3-NH2-Phenyl



120
4
3-NH2-Phenyl



121
1
2-NH2-Phenyl



122
2
2-NH2-Phenyl



123
3
2-NH2-Phenyl



124
4
2-NH2-Phenyl



125
1
2,3-di-Me-Phenyl



126
2
2,3-di-Me-Phenyl



127
3
2,3-di-Me-Phenyl



128
4
2,3-di-Me-Phenyl



129
1
2,4-di-Me-Phenyl



130
2
2,4-di-Me-Phenyl



131
3
2,4-di-Me-Phenyl



132
4
2,4-di-Me-Phenyl



133
1
2,5-di-Me-Phenyl



134
2
2,5-di-Me-Phenyl



135
3
2,5-di-Me-Phenyl



136
4
2,5-di-Me-Phenyl



137
1
2,6-di-Me-Phenyl



138
2
2,6-di-Me-Phenyl



139
3
2,6-di-Me-Phenyl



140
4
2,6-di-Me-Phenyl



141
1
2,6-di-iPr-Phenyl



142
2
2,6-di-iPr-Phenyl



143
3
2,6-di-iPr-Phenyl



144
4
2,6-di-iPr-Phenyl



145
1
2-morpholino-phenyl



146
2
2-morpholino-phenyl



147
3
2-morpholino-phenyl



148
4
2-morpholino-phenyl



149
1
3-morpholino-phenyl



150
2
3-morpholino-phenyl



151
3
3-morpholino-phenyl



152
4
3-morpholino-phenyl



153
1
4-morpholino-phenyl



154
2
4-morpholino-phenyl



155
3
4-morpholino-phenyl



156
4
4-morpholino-phenyl



157
1
4-CN-2-morpholino-phenyl



158
2
4-CN-2-morpholino-phenyl



159
3
4-CN-2-morpholino-phenyl



160
4
4-CN-2-morpholino-phenyl



161
1
4-CH3-2-morpholino-phenyl



162
2
4-CH3-2-morpholino-phenyl



163
3
4-CH3-2-morpholino-phenyl



164
4
4-CH3-2-morpholino-phenyl



165
1
4-OH-2-morpholino-phenyl



166
2
4-OH-2-morpholino-phenyl



167
3
4-OH-2-morpholino-phenyl



168
4
4-OH-2-morpholino-phenyl



173
1
naphthylen-2-yl



174
2
naphthylen-2-yl



175
3
naphthylen-2-yl



176
4
naphthylen-2-yl










Exemplary embodiments include compounds having the formula (XVI)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 10.














TABLE 10





Entry
n
R4
Entry
n
R4




















1
1
Phenyl
85
1
2-Br-Phenyl


2
2
Phenyl
86
2
2-Br-Phenyl


3
3
Phenyl
87
3
2-Br-Phenyl


4
4
Phenyl
88
4
2-Br-Phenyl


5
1
4-OH-Phenyl
89
1
4-CF3-Phenyl


6
2
4-OH-Phenyl
90
2
4-CF3-Phenyl


7
3
4-OH-Phenyl
91
3
4-CF3-Phenyl


8
4
4-OH-Phenyl
92
4
4-CF3-Phenyl


9
1
3-OH-Phenyl
93
1
3-CF3-Phenyl


10
2
3-OH-Phenyl
94
2
3-CF3-Phenyl


11
3
3-OH-Phenyl
95
3
3-CF3-Phenyl


12
4
3-OH-Phenyl
96
4
3-CF3-Phenyl


13
1
2-OH-Phenyl
97
1
2-CF3-Phenyl


14
2
2-OH-Phenyl
98
2
2-CF3-Phenyl


15
3
2-OH-Phenyl
99
3
2-CF3-Phenyl


16
4
2-OH-Phenyl
100
4
2-CF3-Phenyl


17
1
4-OMe-Phenyl
101
1
4-iPr-Phenyl


18
2
4-OMe-Phenyl
102
2
4-iPr-Phenyl


19
3
4-OMe-Phenyl
103
3
4-iPr-Phenyl


20
4
4-OMe-Phenyl
104
4
4-iPr-Phenyl


21
1
3-OMe-Phenyl
105
1
3-iPr-Phenyl


22
2
3-OMe-Phenyl
106
2
3-iPr-Phenyl


23
3
3-OMe-Phenyl
107
3
3-iPr-Phenyl


24
4
3-OMe-Phenyl
108
4
3-iPr-Phenyl


25
1
2-OMe-Phenyl
109
1
2-iPr-Phenyl


26
2
2-OMe-Phenyl
110
2
2-iPr-Phenyl


27
3
2-OMe-Phenyl
111
3
2-iPr-Phenyl


28
4
2-OMe-Phenyl
112
4
2-iPr-Phenyl


29
1
4-CN-Phenyl
113
1
4-NH2-Phenyl


30
2
4-CN-Phenyl
114
2
4-NH2-Phenyl


31
3
4-CN-Phenyl
115
3
4-NH2-Phenyl


32
4
4-CN-Phenyl
116
4
4-NH2-Phenyl


33
1
3-CN-Phenyl
117
1
3-NH2-Phenyl


34
2
3-CN-Phenyl
118
2
3-NH2-Phenyl


35
3
3-CN-Phenyl
119
3
3-NH2-Phenyl


36
4
3-CN-Phenyl
120
4
3-NH2-Phenyl


37
1
2-CN-Phenyl
121
1
2-NH2-Phenyl


38
2
2-CN-Phenyl
122
2
2-NH2-Phenyl


39
3
2-CN-Phenyl
123
3
2-NH2-Phenyl


40
4
2-CN-Phenyl
124
4
2-NH2-Phenyl


41
1
4-Me-Phenyl
125
1
2,3-di-Me-Phenyl


42
2
4-Me-Phenyl
126
2
2,3-di-Me-Phenyl


43
3
4-Me-Phenyl
127
3
2,3-di-Me-Phenyl


44
4
4-Me-Phenyl
128
4
2,3-di-Me-Phenyl


45
1
3-Me-Phenyl
129
1
2,4-di-Me-Phenyl


46
2
3-Me-Phenyl
130
2
2,4-di-Me-Phenyl


47
3
3-Me-Phenyl
131
3
2,4-di-Me-Phenyl


48
4
3-Me-Phenyl
132
4
2,4-di-Me-Phenyl


49
1
2-Me-Phenyl
133
1
2,5-di-Me-Phenyl


50
2
2-Me-Phenyl
134
2
2,5-di-Me-Phenyl


51
3
2-Me-Phenyl
135
3
2,5-di-Me-Phenyl


52
4
2-Me-Phenyl
136
4
2,5-di-Me-Phenyl


53
1
4-F-Phenyl
137
1
2,6-di-Me-Phenyl


54
2
4-F-Phenyl
138
2
2,6-di-Me-Phenyl


55
3
4-F-Phenyl
139
3
2,6-di-Me-Phenyl


56
4
4-F-Phenyl
140
4
2,6-di-Me-Phenyl


57
1
3-F-Phenyl
141
1
2,6-di-iPr-Phenyl


58
2
3-F-Phenyl
142
2
2,6-di-iPr-Phenyl


59
3
3-F-Phenyl
143
3
2,6-di-iPr-Phenyl


60
4
3-F-Phenyl
144
4
2,6-di-iPr-Phenyl


61
1
2-F-Phenyl
145
1
2-morpholino-phenyl


62
2
2-F-Phenyl
146
2
2-morpholino-phenyl


63
3
2-F-Phenyl
147
3
2-morpholino-phenyl


64
4
2-F-Phenyl
148
4
2-morpholino-phenyl


65
1
4-Cl-Phenyl
149
1
3-morpholino-phenyl


66
2
4-Cl-Phenyl
150
2
3-morpholino-phenyl


67
3
4-Cl-Phenyl
151
3
3-morpholino-phenyl


68
4
4-Cl-Phenyl
152
4
3-morpholino-phenyl


69
1
3-Cl-Phenyl
153
1
4-morpholino-phenyl


70
2
3-Cl-Phenyl
154
2
4-morpholino-phenyl


71
3
3-Cl-Phenyl
155
3
4-morpholino-phenyl


72
4
3-Cl-Phenyl
156
4
4-morpholino-phenyl


73
1
2-Cl-Phenyl
157
1
4-CN-2-morpholino-phenyl


74
2
2-Cl-Phenyl
158
2
4-CN-2-morpholino-phenyl


75
3
2-Cl-Phenyl
159
3
4-CN-2-morpholino-phenyl


76
4
2-Cl-Phenyl
160
4
4-CN-2-morpholino-phenyl


77
1
4-Br-Phenyl
161
1
4-CH3-2-morpholino-phenyl


78
2
4-Br-Phenyl
162
2
4-CH3-2-morpholino-phenyl


79
3
4-Br-Phenyl
163
3
4-CH3-2-morpholino-phenyl


80
4
4-Br-Phenyl
164
4
4-CH3-2-morpholino-phenyl


81
1
3-Br-Phenyl
165
1
4-OH-2-morpholino-phenyl


82
2
3-Br-Phenyl
166
2
4-OH-2-morpholino-phenyl


83
3
3-Br-Phenyl
167
3
4-OH-2-morpholino-phenyl


84
4
3-Br-Phenyl
168
4
4-OH-2-morpholino-phenyl


85
1
naphthylen-1-yl
173
1
naphthylen-2-yl


86
2
naphthylen-1-yl
174
2
naphthylen-2-yl


87
3
naphthylen-1-yl
175
3
naphthylen-2-yl


88
4
naphthylen-1-yl
176
4
naphthylen-2-yl









Exemplary embodiments include compounds having the formula (XVII)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 11.













TABLE 11





Entry
R1
R2
n
R5



















1
Methyl
Methyl
1
Phenyl


2
Methyl
Methyl
2
Phenyl


3
Methyl
Methyl
3
Phenyl


4
Methyl
Methyl
4
Phenyl


5
Methyl
Methyl
1
4-OH-Phenyl


6
Methyl
Methyl
2
4-OH-Phenyl


7
Methyl
Methyl
3
4-OH-Phenyl


8
Methyl
Methyl
4
4-OH-Phenyl


9
Methyl
Methyl
1
3-OH-Phenyl


10
Methyl
Methyl
2
3-OH-Phenyl


11
Methyl
Methyl
3
3-OH-Phenyl


12
Methyl
Methyl
4
3-OH-Phenyl


13
Methyl
Methyl
1
2-OH-Phenyl


14
Methyl
Methyl
2
2-OH-Phenyl


15
Methyl
Methyl
3
2-OH-Phenyl


16
Methyl
Methyl
4
2-OH-Phenyl


17
Methyl
Methyl
1
4-OMe-Phenyl


18
Methyl
Methyl
2
4-OMe-Phenyl


19
Methyl
Methyl
3
4-OMe-Phenyl


20
Methyl
Methyl
4
4-OMe-Phenyl


21
Methyl
Methyl
1
3-OMe-Phenyl


22
Methyl
Methyl
2
3-OMe-Phenyl


23
Methyl
Methyl
3
3-OMe-Phenyl


24
Methyl
Methyl
4
3-OMe-Phenyl


25
Methyl
Methyl
1
2-OMe-Phenyl


26
Methyl
Methyl
2
2-OMe-Phenyl


27
Methyl
Methyl
3
2-OMe-Phenyl


28
Methyl
Methyl
4
2-OMe-Phenyl


29
Methyl
Methyl
1
4-CN-Phenyl


30
Methyl
Methyl
2
4-CN-Phenyl


31
Methyl
Methyl
3
4-CN-Phenyl


32
Methyl
Methyl
4
4-CN-Phenyl


33
Methyl
Methyl
1
3-CN-Phenyl


34
Methyl
Methyl
2
3-CN-Phenyl


35
Methyl
Methyl
3
3-CN-Phenyl


36
Methyl
Methyl
4
3-CN-Phenyl


37
Methyl
Methyl
1
2-CN-Phenyl


38
Methyl
Methyl
2
2-CN-Phenyl


39
Methyl
Methyl
3
2-CN-Phenyl


40
Methyl
Methyl
4
2-CN-Phenyl


41
Methyl
Methyl
1
4-Me-Phenyl


42
Methyl
Methyl
2
4-Me-Phenyl


43
Methyl
Methyl
3
4-Me-Phenyl


44
Methyl
Methyl
4
4-Me-Phenyl


45
Methyl
Methyl
1
3-Me-Phenyl


46
Methyl
Methyl
2
3-Me-Phenyl


47
Methyl
Methyl
3
3-Me-Phenyl


48
Methyl
Methyl
4
3-Me-Phenyl


49
Methyl
Methyl
1
2-Me-Phenyl


50
Methyl
Methyl
2
2-Me-Phenyl


51
Methyl
Methyl
3
2-Me-Phenyl


52
Methyl
Methyl
4
2-Me-Phenyl


53
Methyl
Methyl
1
4-F-Phenyl


54
Methyl
Methyl
2
4-F-Phenyl


55
Methyl
Methyl
3
4-F-Phenyl


56
Methyl
Methyl
4
4-F-Phenyl


57
Methyl
Methyl
1
3-F-Phenyl


58
Methyl
Methyl
2
3-F-Phenyl


59
Methyl
Methyl
3
3-F-Phenyl


60
Methyl
Methyl
4
3-F-Phenyl


61
Methyl
Methyl
1
2-F-Phenyl


62
Methyl
Methyl
2
2-F-Phenyl


63
Methyl
Methyl
3
2-F-Phenyl


64
Methyl
Methyl
4
2-F-Phenyl


65
Methyl
Methyl
1
4-Cl-Phenyl


66
Methyl
Methyl
2
4-Cl-Phenyl


67
Methyl
Methyl
3
4-Cl-Phenyl


68
Methyl
Methyl
4
4-Cl-Phenyl


69
Methyl
Methyl
1
3-Cl-Phenyl


70
Methyl
Methyl
2
3-Cl-Phenyl


71
Methyl
Methyl
3
3-Cl-Phenyl


72
Methyl
Methyl
4
3-Cl-Phenyl


73
Methyl
Methyl
1
2-Cl-Phenyl


74
Methyl
Methyl
2
2-Cl-Phenyl


75
Methyl
Methyl
3
2-Cl-Phenyl


76
Methyl
Methyl
4
2-Cl-Phenyl


77
Methyl
Methyl
1
4-Br-Phenyl


78
Methyl
Methyl
2
4-Br-Phenyl


79
Methyl
Methyl
3
4-Br-Phenyl


80
Methyl
Methyl
4
4-Br-Phenyl


81
Methyl
Methyl
1
3-Br-Phenyl


82
Methyl
Methyl
2
3-Br-Phenyl


83
Methyl
Methyl
3
3-Br-Phenyl


84
Methyl
Methyl
4
3-Br-Phenyl


85
Methyl
Methyl
1
2-Br-Phenyl


86
Methyl
Methyl
2
2-Br-Phenyl


87
Methyl
Methyl
3
2-Br-Phenyl


88
Methyl
Methyl
4
2-Br-Phenyl


89
Methyl
Methyl
1
4-CF3-Phenyl


90
Methyl
Methyl
2
4-CF3-Phenyl


91
Methyl
Methyl
3
4-CF3-Phenyl


92
Methyl
Methyl
4
4-CF3-Phenyl


93
Methyl
Methyl
1
3-CF3-Phenyl


94
Methyl
Methyl
2
3-CF3-Phenyl


95
Methyl
Methyl
3
3-CF3-Phenyl


96
Methyl
Methyl
4
3-CF3-Phenyl


97
Methyl
Methyl
1
2-CF3-Phenvl


98
Methyl
Methyl
2
2-CF3-Phenvl


99
Methyl
Methyl
3
2-CF3-Phenvl


100
Methyl
Methyl
4
2-CF3-Phenyl


101
Methyl
Methyl
1
4-iPr-Phenyl


102
Methyl
Methyl
2
4-iPr-Phenyl


103
Methyl
Methyl
3
4-iPr-Phenyl


104
Methyl
Methyl
4
4-iPr-Phenyl


105
Methyl
Methyl
1
3-iPr-Phenyl


106
Methyl
Methyl
2
3-iPr-Phenyl


107
Methyl
Methyl
3
3-iPr-Phenyl


108
Methyl
Methyl
4
3-iPr-Phenyl


109
Methyl
Methyl
1
2-iPr-Phenyl


110
Methyl
Methyl
2
2-iPr-Phenyl


111
Methyl
Methyl
3
2-iPr-Phenyl


112
Methyl
Methyl
4
2-iPr-Phenyl


113
Methyl
Methyl
1
4-NH2-Phenyl


114
Methyl
Methyl
2
4-NH2-Phenyl


115
Methyl
Methyl
3
4-NH2-Phenyl


116
Methyl
Methyl
4
4-NH2-Phenyl


117
Methyl
Methyl
1
3-NH2-Phenyl


118
Methyl
Methyl
2
3-NH2-Phenyl


119
Methyl
Methyl
3
3-NH2-Phenyl


120
Methyl
Methyl
4
3-NH2-Phenyl


121
Methyl
Methyl
1
2-NH2-Phenyl


122
Methyl
Methyl
2
2-NH2-Phenyl


123
Methyl
Methyl
3
2-NH2-Phenyl


124
Methyl
Methyl
4
2-NH2-Phenyl


125
Methyl
Methyl
1
2,3-di-Me-Phenyl


126
Methyl
Methyl
2
2,3-di-Me-Phenyl


127
Methyl
Methyl
3
2,3-di-Me-Phenyl


128
Methyl
Methyl
4
2,3-di-Me-Phenyl


129
Methyl
Methyl
1
2,4-di-Me-Phenyl


130
Methyl
Methyl
2
2,4-di-Me-Phenyl


131
Methyl
Methyl
3
2,4-di-Me-Phenyl


132
Methyl
Methyl
4
2,4-di-Me-Phenyl


133
Methyl
Methyl
1
2,5-di-Me-Phenyl


134
Methyl
Methyl
2
2,5-di-Me-Phenyl


135
Methyl
Methyl
3
2,5-di-Me-Phenyl


136
Methyl
Methyl
4
2,5-di-Me-Phenyl


137
Methyl
Methyl
1
2,6-di-Me-Phenyl


138
Methyl
Methyl
2
2,6-di-Me-Phenyl


139
Methyl
Methyl
3
2,6-di-Me-Phenyl


140
Methyl
Methyl
4
2,6-di-Me-Phenyl


141
Methyl
Methyl
1
2,6-di-iPr-Phenyl


142
Methyl
Methyl
2
2,6-di-iPr-Phenyl


143
Methyl
Methyl
3
2,6-di-iPr-Phenyl


144
Methyl
Methyl
4
2,6-di-iPr-Phenyl


145
Methyl
Methyl
1
2-morpholino-phenyl


146
Methyl
Methyl
2
2-morpholino-phenyl


147
Methyl
Methyl
3
2-morpholino-phenyl


148
Methyl
Methyl
4
2-morpholino-phenyl


149
Methyl
Methyl
1
3-morpholino-phenyl


150
Methyl
Methyl
2
3-morpholino-phenyl


151
Methyl
Methyl
3
3-morpholino-phenyl


152
Methyl
Methyl
4
3-morpholino-phenyl


153
Methyl
Methyl
1
4-morpholino-phenyl


154
Methyl
Methyl
2
4-morpholino-phenyl


155
Methyl
Methyl
3
4-morpholino-phenyl


156
Methyl
Methyl
4
4-morpholino-phenyl


157
Methyl
Methyl
1
4-CN-2-morpholino-phenyl


158
Methyl
Methyl
2
4-CN-2-morpholino-phenyl


159
Methyl
Methyl
3
4-CN-2-morpholino-phenyl


160
Methyl
Methyl
4
4-CN-2-morpholino-phenyl


161
Methyl
Methyl
1
4-CH3-2-morpholino-phenyl


162
Methyl
Methyl
2
4-CH3-2-morpholino-phenyl


163
Methyl
Methyl
3
4-CH3-2-morpholino-phenyl


164
Methyl
Methyl
4
4-CH3-2-morpholino-phenyl


165
Methyl
Methyl
1
4-OH-2-morpholino-phenyl


166
Methyl
Methyl
2
4-OH-2-morpholino-phenyl


167
Methyl
Methyl
3
4-OH-2-morpholino-phenyl


168
Methyl
Methyl
4
4-OH-2-morpholino-phenyl


169
Methyl
Methyl
1
naphthylen-1-yl


170
Methyl
Methyl
2
naphthylen-1-yl


171
Methyl
Methyl
3
naphthylen-1-yl


172
Methyl
Methyl
4
naphthylen-1-yl


173
Methyl
Methyl
1
naphthylen-2-yl


174
Methyl
Methyl
2
naphthylen-2-yl


175
Methyl
Methyl
3
naphthylen-2-yl


176
Methyl
Methyl
4
naphthylen-2-yl


177
Ethyl
Ethyl
1
Phenyl


178
Ethyl
Ethyl
2
Phenyl


179
Ethyl
Ethyl
3
Phenyl


180
Ethyl
Ethyl
4
Phenyl


181
Ethyl
Ethyl
1
4-OH-Phenyl


182
Ethyl
Ethyl
2
4-OH-Phenyl


183
Ethyl
Ethyl
3
4-OH-Phenyl


184
Ethyl
Ethyl
4
4-OH-Phenyl


185
Ethyl
Ethyl
1
3-OH-Phenyl


186
Ethyl
Ethyl
2
3-OH-Phenyl


187
Ethyl
Ethyl
3
3-OH-Phenyl


188
Ethyl
Ethyl
4
3-OH-Phenyl


189
Ethyl
Ethyl
1
2-OH-Phenyl


190
Ethyl
Ethyl
2
2-OH-Phenyl


191
Ethyl
Ethyl
3
2-OH-Phenyl


192
Ethyl
Ethyl
4
2-OH-Phenyl


193
Ethyl
Ethyl
1
4-OMe-Phenyl


194
Ethyl
Ethyl
2
4-OMe-Phenyl


195
Ethyl
Ethyl
3
4-OMe-Phenyl


196
Ethyl
Ethyl
4
4-OMe-Phenyl


197
Ethyl
Ethyl
1
3-OMe-Phenyl


198
Ethyl
Ethyl
2
3-OMe-Phenyl


199
Ethyl
Ethyl
3
3-OMe-Phenyl


200
Ethyl
Ethyl
4
3-OMe-Phenyl


201
Ethyl
Ethyl
1
2-OMe-Phenyl


202
Ethyl
Ethyl
2
2-OMe-Phenyl


203
Ethyl
Ethyl
3
2-OMe-Phenyl


204
Ethyl
Ethyl
4
2-OMe-Phenyl


205
Ethyl
Ethyl
1
4-CN-Phenyl


206
Ethyl
Ethyl
2
4-CN-Phenyl


207
Ethyl
Ethyl
3
4-CN-Phenyl


208
Ethyl
Ethyl
4
4-CN-Phenyl


209
Ethyl
Ethyl
1
3-CN-Phenyl


210
Ethyl
Ethyl
2
3-CN-Phenyl


211
Ethyl
Ethyl
3
3-CN-Phenyl


212
Ethyl
Ethyl
4
3-CN-Phenyl


213
Ethyl
Ethyl
1
2-CN-Phenyl


214
Ethyl
Ethyl
2
2-CN-Phenyl


215
Ethyl
Ethyl
3
2-CN-Phenyl


216
Ethyl
Ethyl
4
2-CN-Phenyl


217
Ethyl
Ethyl
1
4-Me-Phenyl


218
Ethyl
Ethyl
2
4-Me-Phenyl


219
Ethyl
Ethyl
3
4-Me-Phenyl


220
Ethyl
Ethyl
4
4-Me-Phenyl


221
Ethyl
Ethyl
1
3-Me-Phenyl


222
Ethyl
Ethyl
2
3-Me-Phenyl


223
Ethyl
Ethyl
3
3-Me-Phenyl


224
Ethyl
Ethyl
4
3-Me-Phenyl


225
Ethyl
Ethyl
1
2-Me-Phenyl


226
Ethyl
Ethyl
2
2-Me-Phenyl


227
Ethyl
Ethyl
3
2-Me-Phenyl


228
Ethyl
Ethyl
4
2-Me-Phenyl


229
Ethyl
Ethyl
1
4-F-Phenyl


230
Ethyl
Ethyl
2
4-F-Phenyl


231
Ethyl
Ethyl
3
4-F-Phenyl


232
Ethyl
Ethyl
4
4-F-Phenyl


233
Ethyl
Ethyl
1
3-F-Phenyl


234
Ethyl
Ethyl
2
3-F-Phenyl


235
Ethyl
Ethyl
3
3-F-Phenyl


236
Ethyl
Ethyl
4
3-F-Phenyl


237
Ethyl
Ethyl
1
2-F-Phenyl


238
Ethyl
Ethyl
2
2-F-Phenyl


239
Ethyl
Ethyl
3
2-F-Phenyl


240
Ethyl
Ethyl
4
2-F-Phenyl


241
Ethyl
Ethyl
1
4-Cl-Phenyl


242
Ethyl
Ethyl
2
4-Cl-Phenyl


243
Ethyl
Ethyl
3
4-Cl-Phenyl


244
Ethyl
Ethyl
4
4-Cl-Phenyl


245
Ethyl
Ethyl
1
3-Cl-Phenyl


246
Ethyl
Ethyl
2
3-Cl-Phenyl


247
Ethyl
Ethyl
3
3-Cl-Phenyl


248
Ethyl
Ethyl
4
3-Cl-Phenyl


249
Ethyl
Ethyl
1
2-Cl-Phenyl


250
Ethyl
Ethyl
2
2-Cl-Phenyl


251
Ethyl
Ethyl
3
2-Cl-Phenyl


252
Ethyl
Ethyl
4
2-Cl-Phenyl


253
Ethyl
Ethyl
1
4-Br-Phenyl


254
Ethyl
Ethyl
2
4-Br-Phenyl


255
Ethyl
Ethyl
3
4-Br-Phenyl


256
Ethyl
Ethyl
4
4-Br-Phenyl


257
Ethyl
Ethyl
1
3-Br-Phenyl


258
Ethyl
Ethyl
2
3-Br-Phenyl


259
Ethyl
Ethyl
3
3-Br-Phenyl


260
Ethyl
Ethyl
4
3-Br-Phenyl


261
Ethyl
Ethyl
1
2-Br-Phenyl


262
Ethyl
Ethyl
2
2-Br-Phenyl


263
Ethyl
Ethyl
3
2-Br-Phenyl


264
Ethyl
Ethyl
4
2-Br-Phenyl


265
Ethyl
Ethyl
1
4-CF3-Phenyl


266
Ethyl
Ethyl
2
4-CF3-Phenyl


267
Ethyl
Ethyl
3
4-CF3-Phenyl


268
Ethyl
Ethyl
4
4-CF3-Phenyl


269
Ethyl
Ethyl
1
3-CF3-Phenyl


270
Ethyl
Ethyl
2
3-CF3-Phenyl


271
Ethyl
Ethyl
3
3-CF3-Phenyl


272
Ethyl
Ethyl
4
3-CF3-Phenyl


273
Ethyl
Ethyl
1
2-CF3-Phenyl


274
Ethyl
Ethyl
2
2-CF3-Phenyl


275
Ethyl
Ethyl
3
2-CF3-Phenyl


276
Ethyl
Ethyl
4
2-CF3-Phenyl


277
Ethyl
Ethyl
1
4-iPr-Phenyl


278
Ethyl
Ethyl
2
4-iPr-Phenyl


279
Ethyl
Ethyl
3
4-iPr-Phenyl


280
Ethyl
Ethyl
4
4-iPr-Phenyl


281
Ethyl
Ethyl
1
3-iPr-Phenyl


282
Ethyl
Ethyl
2
3-iPr-Phenyl


283
Ethyl
Ethyl
3
3-iPr-Phenyl


284
Ethyl
Ethyl
4
3-iPr-Phenyl


285
Ethyl
Ethyl
1
2-iPr-Phenyl


286
Ethyl
Ethyl
2
2-iPr-Phenyl


287
Ethyl
Ethyl
3
2-iPr-Phenyl


288
Ethyl
Ethyl
4
2-iPr-Phenyl


289
Ethyl
Ethyl
1
4-NH2-Phenyl


290
Ethyl
Ethyl
2
4-NH2-Phenyl


291
Ethyl
Ethyl
3
4-NH2-Phenyl


292
Ethyl
Ethyl
4
4-NH2-Phenyl


293
Ethyl
Ethyl
1
3-NH2-Phenyl


294
Ethyl
Ethyl
2
3-NH2-Phenyl


295
Ethyl
Ethyl
3
3-NH2-Phenyl


296
Ethyl
Ethyl
4
3-NH2-Phenyl


297
Ethyl
Ethyl
1
2-NH2-Phenyl


298
Ethyl
Ethyl
2
2-NH2-Phenyl


299
Ethyl
Ethyl
3
2-NH2-Phenyl


300
Ethyl
Ethyl
4
2-NH2-Phenyl


301
Ethyl
Ethyl
1
2.3-di-Me-Phenvl


302
Ethyl
Ethyl
2
2.3-di-Me-Phenyl


303
Ethyl
Ethyl
3
2,3-di-Me-Phenyl


304
Ethyl
Ethyl
4
2,3-di-Me-Phenyl


305
Ethyl
Ethyl
1
2.4-di-Me-Phenyl


306
Ethyl
Ethyl
2
2,4-di-Me-Phenyl


307
Ethyl
Ethyl
3
2,4-di-Me-Phenyl


308
Ethyl
Ethyl
4
2,4-di-Me-Phenyl


309
Ethyl
Ethyl
1
2,5-di-Me-Phenyl


310
Ethyl
Ethyl
2
2,5-di-Me-Phenyl


311
Ethyl
Ethyl
3
2,5-di-Me-Phenyl


312
Ethyl
Ethyl
4
2,5-di-Me-Phenyl


313
Ethyl
Ethyl
1
2,6-di-Me-Phenyl


314
Ethyl
Ethyl
2
2,6-di-Me-Phenyl


315
Ethyl
Ethyl
3
2,6-di-Me-Phenyl


316
Ethyl
Ethyl
4
2,6-di-Me-Phenyl


317
Ethyl
Ethyl
1
2,6-di-iPr-Phenyl


318
Ethyl
Ethyl
2
2,6-di-iPr-Phenyl


319
Ethyl
Ethyl
3
2,6-di-iPr-Phenyl


320
Ethyl
Ethyl
4
2,6-di-iPr-Phenyl


321
Ethyl
Ethyl
1
2-morpholino-phenyl


322
Ethyl
Ethyl
2
2-morpholino-phenyl


323
Ethyl
Ethyl
3
2-morpholino-phenyl


324
Ethyl
Ethyl
4
2-morpholino-phenyl


325
Ethyl
Ethyl
1
3-morpholino-phenyl


326
Ethyl
Ethyl
2
3-morpholino-phenyl


327
Ethyl
Ethyl
3
3-morpholino-phenyl


328
Ethyl
Ethyl
4
3-morpholino-phenyl


329
Ethyl
Ethyl
1
4-morpholino-phenyl


330
Ethyl
Ethyl
2
4-morpholino-phenyl


331
Ethyl
Ethyl
3
4-morpholino-phenyl


332
Ethyl
Ethyl
4
4-morpholino-phenyl


333
Ethyl
Ethyl
1
4-CN-2-morpholino-phenyl


334
Ethyl
Ethyl
2
4-CN-2-morpholino-phenyl


335
Ethyl
Ethyl
3
4-CN-2-morpholino-phenyl


336
Ethyl
Ethyl
4
4-CN-2-morpholino-phenyl


337
Ethyl
Ethyl
1
4-CH3-2-morpholino-phenyl


338
Ethyl
Ethyl
2
4-CH3-2-morpholino-phenyl


339
Ethyl
Ethyl
3
4-CH3-2-morpholino-phenyl


340
Ethyl
Ethyl
4
4-CH3-2-morpholino-phenyl


341
Ethyl
Ethyl
1
4-OH-2-morpholino-phenyl


342
Ethyl
Ethyl
2
4-OH-2-morpholino-phenyl


343
Ethyl
Ethyl
3
4-OH-2-morpholino-phenyl


344
Ethyl
Ethyl
4
4-OH-2-morpholino-phenyl


345
Ethyl
Ethyl
1
naphthylen-1-yl


346
Ethyl
Ethyl
2
naphthylen-1-yl


347
Ethyl
Ethyl
3
naphthylen-1-yl


348
Ethyl
Ethyl
4
naphthylen-1-yl


349
Ethyl
Ethyl
1
naphthylen-2-yl


350
Ethyl
Ethyl
2
naphthylen-2-yl


351
Ethyl
Ethyl
3
naphthylen-2-yl


352
Ethyl
Ethyl
4
naphthylen-2-yl









Exemplary embodiments include compounds having the formula (XVIII)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 12














TABLE 12





Entry
n
R5
Entry
n
R5




















1
1
Phenyl
85
1
2-Br-Phenyl


2
2
Phenyl
86
2
2-Br-Phenyl


3
3
Phenyl
87
3
2-Br-Phenyl


4
4
Phenyl
88
4
2-Br-Phenyl


5
1
4-OH-Phenyl
89
1
4-CF3-Phenyl


6
2
4-OH-Phenyl
90
2
4-CF3-Phenyl


7
3
4-OH-Phenyl
91
3
4-CF3-Phenyl


8
4
4-OH-Phenyl
92
4
4-CF3-Phenyl


9
1
3-OH-Phenyl
93
1
3-CF3-Phenyl


10
2
3-OH-Phenyl
94
2
3-CF3-Phenyl


11
3
3-OH-Phenyl
95
3
3-CF3-Phenyl


12
4
3-OH-Phenyl
96
4
3-CF3-Phenyl


13
1
2-OH-Phenyl
97
1
2-CF3-Phenyl


14
2
2-OH-Phenyl
98
2
2-CF3-Phenyl


15
3
2-OH-Phenyl
99
3
2-CF3-Phenyl


16
4
2-OH-Phenyl
100
4
2-CF3-Phenyl


17
1
4-OMe-Phenyl
101
1
4-iPr-Phenyl


18
2
4-OMe-Phenyl
102
2
4-iPr-Phenyl


19
3
4-OMe-Phenyl
103
3
4-iPr-Phenyl


20
4
4-OMe-Phenyl
104
4
4-iPr-Phenyl


21
1
3-OMe-Phenyl
105
1
3-iPr-Phenyl


22
2
3-OMe-Phenyl
106
2
3-iPr-Phenyl


23
3
3-OMe-Phenyl
107
3
3-iPr-Phenyl


24
4
3-OMe-Phenyl
108
4
3-iPr-Phenyl


25
1
2-OMe-Phenyl
109
1
2-iPr-Phenyl


26
2
2-OMe-Phenyl
110
2
2-iPr-Phenyl


27
3
2-OMe-Phenyl
111
3
2-iPr-Phenyl


28
4
2-OMe-Phenyl
112
4
2-iPr-Phenyl


29
1
4-CN-Phenyl
113
1
4-NH2-Phenyl


30
2
4-CN-Phenyl
114
2
4-NH2-Phenyl


31
3
4-CN-Phenyl
115
3
4-NH2-Phenyl


32
4
4-CN-Phenyl
116
4
4-NH2-Phenyl


33
1
3-CN-Phenyl
117
1
3-NH2-Phenyl


34
2
3-CN-Phenyl
118
2
3-NH2-Phenyl


35
3
3-CN-Phenyl
119
3
3-NH2-Phenyl


36
4
3-CN-Phenyl
120
4
3-NH2-Phenyl


37
1
2-CN-Phenyl
121
1
2-NH2-Phenyl


38
2
2-CN-Phenyl
122
2
2-NH2-Phenyl


39
3
2-CN-Phenyl
123
3
2-NH2-Phenyl


40
4
2-CN-Phenyl
124
4
2-NH2-Phenyl


41
1
4-Me-Phenyl
125
1
2,3-di-Me-Phenyl


42
2
4-Me-Phenyl
126
2
2,3-di-Me-Phenyl


43
3
4-Me-Phenyl
127
3
2,3-di-Me-Phenyl


44
4
4-Me-Phenyl
128
4
2,3-di-Me-Phenyl


45
1
3-Me-Phenyl
129
1
2,4-di-Me-Phenyl


46
2
3-Me-Phenyl
130
2
2,4-di-Me-Phenyl


47
3
3-Me-Phenyl
131
3
2,4-di-Me-Phenyl


48
4
3-Me-Phenyl
132
4
2,4-di-Me-Phenyl


49
1
2-Me-Phenyl
133
1
2,5-di-Me-Phenyl


50
2
2-Me-Phenyl
134
2
2,5-di-Me-Phenyl


51
3
2-Me-Phenyl
135
3
2,5-di-Me-Phenyl


52
4
2-Me-Phenyl
136
4
2,5-di-Me-Phenyl


53
1
4-F-Phenyl
137
1
2,6-di-Me-Phenyl


54
2
4-F-Phenyl
138
2
2,6-di-Me-Phenyl


55
3
4-F-Phenyl
139
3
2,6-di-Me-Phenyl


56
4
4-F-Phenyl
140
4
2,6-di-Me-Phenyl


57
1
3-F-Phenyl
141
1
2,6-di-iPr-Phenyl


58
2
3-F-Phenyl
142
2
2,6-di-iPr-Phenyl


59
3
3-F-Phenyl
143
3
2,6-di-iPr-Phenyl


60
4
3-F-Phenyl
144
4
2,6-di-iPr-Phenyl


61
1
2-F-Phenyl
145
1
2-morpholino-phenyl


62
2
2-F-Phenyl
146
2
2-morpholino-phenyl


63
3
2-F-Phenyl
147
3
2-morpholino-phenyl


64
4
2-F-Phenyl
148
4
2-morpholino-phenyl


65
1
4-Cl-Phenyl
149
1
3-morpholino-phenyl


66
2
4-Cl-Phenyl
150
2
3-morpholino-phenyl


67
3
4-Cl-Phenyl
151
3
3-morpholino-phenyl


68
4
4-Cl-Phenyl
152
4
3-morpholino-phenyl


69
1
3-Cl-Phenyl
153
1
4-morpholino-phenyl


70
2
3-Cl-Phenyl
154
2
4-morpholino-phenyl


71
3
3-Cl-Phenyl
155
3
4-morpholino-phenyl


72
4
3-Cl-Phenyl
156
4
4-morpholino-phenyl


73
1
2-Cl-Phenyl
157
1
4-CN-2-morpholino-phenyl


74
2
2-Cl-Phenyl
158
2
4-CN-2-morpholino-phenyl


75
3
2-Cl-Phenyl
159
3
4-CN-2-morpholino-phenyl


76
4
2-Cl-Phenyl
160
4
4-CN-2-morpholino-phenyl


77
1
4-Br-Phenyl
161
1
4-CH3-2-morpholino-phenyl


78
2
4-Br-Phenyl
162
2
4-CH3-2-morpholino-phenyl


79
3
4-Br-Phenyl
163
3
4-CH3-2-morpholino-phenyl


80
4
4-Br-Phenyl
164
4
4-CH3-2-morpholino-phenyl


81
1
3-Br-Phenyl
165
1
4-OH-2-morpholino-phenyl


82
2
3-Br-Phenyl
166
2
4-OH-2-morpholino-phenyl


83
3
3-Br-Phenyl
167
3
4-OH-2-morpholino-phenyl


84
4
3-Br-Phenyl
168
4
4-OH-2-morpholino-phenyl


85
1
naphthylen-1-yl
173
1
naphthylen-2-yl


86
2
naphthylen-1-yl
174
2
naphthylen-2-yl


87
3
naphthylen-1-yl
175
3
naphthylen-2-yl


88
4
naphthylen-1-yl
176
4
naphthylen-2-yl









Exemplary embodiments include compounds having the formula (XIX)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 13.














TABLE 13





Entry
n
R5
Entry
n
R5




















1
1
Phenyl
85
1
2-Br-Phenyl


2
2
Phenyl
86
2
2-Br-Phenyl


3
3
Phenyl
87
3
2-Br-Phenyl


4
4
Phenyl
88
4
2-Br-Phenyl


5
1
4-OH-Phenyl
89
1
4-CF3-Phenyl


6
2
4-OH-Phenyl
90
2
4-CF3-Phenyl


7
3
4-OH-Phenyl
91
3
4-CF3-Phenyl


8
4
4-OH-Phenyl
92
4
4-CF3-Phenyl


9
1
3-OH-Phenyl
93
1
3-CF3-Phenyl


10
2
3-OH-Phenyl
94
2
3-CF3-Phenyl


11
3
3-OH-Phenyl
95
3
3-CF3-Phenyl


12
4
3-OH-Phenyl
96
4
3-CF3-Phenyl


13
1
2-OH-Phenyl
97
1
2-CF3-Phenyl


14
2
2-OH-Phenyl
98
2
2-CF3-Phenyl


15
3
2-OH-Phenyl
99
3
2-CF3-Phenyl


16
4
2-OH-Phenyl
100
4
2-CF3-Phenyl


17
1
4-OMe-Phenyl
101
1
4-iPr-Phenyl


18
2
4-OMe-Phenyl
102
2
4-iPr-Phenyl


19
3
4-OMe-Phenyl
103
3
4-iPr-Phenyl


20
4
4-OMe-Phenyl
104
4
4-iPr-Phenyl


21
1
3-OMe-Phenyl
105
1
3-iPr-Phenyl


22
2
3-OMe-Phenyl
106
2
3-iPr-Phenyl


23
3
3-OMe-Phenyl
107
3
3-iPr-Phenyl


24
4
3-OMe-Phenyl
108
4
3-iPr-Phenyl


25
1
2-OMe-Phenyl
109
1
2-iPr-Phenyl


26
2
2-OMe-Phenyl
110
2
2-iPr-Phenyl


27
3
2-OMe-Phenyl
111
3
2-iPr-Phenyl


28
4
2-OMe-Phenyl
112
4
2-iPr-Phenyl


29
1
4-CN-Phenyl
113
1
4-NH2-Phenyl


30
2
4-CN-Phenyl
114
2
4-NH2-Phenyl


31
3
4-CN-Phenyl
115
3
4-NH2-Phenyl


32
4
4-CN-Phenyl
116
4
4-NH2-Phenyl


33
1
3-CN-Phenyl
117
1
3-NH2-Phenyl


34
2
3-CN-Phenyl
118
2
3-NH2-Phenyl


35
3
3-CN-Phenyl
119
3
3-NH2-Phenyl


36
4
3-CN-Phenyl
120
4
3-NH2-Phenyl


37
1
2-CN-Phenyl
121
1
2-NH2-Phenyl


38
2
2-CN-Phenyl
122
2
2-NH2-Phenyl


39
3
2-CN-Phenyl
123
3
2-NH2-Phenyl


40
4
2-CN-Phenyl
124
4
2-NH2-Phenyl


41
1
4-Me-Phenyl
125
1
2,3-di-Me-Phenyl


42
2
4-Me-Phenyl
126
2
2,3-di-Me-Phenyl


43
3
4-Me-Phenyl
127
3
2,3-di-Me-Phenyl


44
4
4-Me-Phenyl
128
4
2,3-di-Me-Phenyl


45
1
3-Me-Phenyl
129
1
2,4-di-Me-Phenyl


46
2
3-Me-Phenyl
130
2
2,4-di-Me-Phenyl


47
3
3-Me-Phenyl
131
3
2,4-di-Me-Phenyl


48
4
3-Me-Phenyl
132
4
2,4-di-Me-Phenyl


49
1
2-Me-Phenyl
133
1
2,5-di-Me-Phenyl


50
2
2-Me-Phenyl
134
2
2,5-di-Me-Phenyl


51
3
2-Me-Phenyl
135
3
2,5-di-Me-Phenyl


52
4
2-Me-Phenyl
136
4
2,5-di-Me-Phenyl


53
1
4-F-Phenyl
137
1
2,6-di-Me-Phenyl


54
2
4-F-Phenyl
138
2
2,6-di-Me-Phenyl


55
3
4-F-Phenyl
139
3
2,6-di-Me-Phenyl


56
4
4-F-Phenyl
140
4
2,6-di-Me-Phenyl


57
1
3-F-Phenyl
141
1
2,6-di-iPr-Phenyl


58
2
3-F-Phenyl
142
2
2,6-di-iPr-Phenyl


59
3
3-F-Phenyl
143
3
2,6-di-iPr-Phenyl


60
4
3-F-Phenyl
144
4
2,6-di-iPr-Phenyl


61
1
2-F-Phenyl
145
1
2-morpholino-phenyl


62
2
2-F-Phenyl
146
2
2-morpholino-phenyl


63
3
2-F-Phenyl
147
3
2-morpholino-phenyl


64
4
2-F-Phenyl
148
4
2-morpholino-phenyl


65
1
4-Cl-Phenyl
149
1
3-morpholino-phenyl


66
2
4-Cl-Phenyl
150
2
3-morpholino-phenyl


67
3
4-Cl-Phenyl
151
3
3-morpholino-phenyl


68
4
4-Cl-Phenyl
152
4
3-morpholino-phenyl


69
1
3-Cl-Phenyl
153
1
4-morpholino-phenyl


70
2
3-Cl-Phenyl
154
2
4-morpholino-phenyl


71
3
3-Cl-Phenyl
155
3
4-morpholino-phenyl


72
4
3-Cl-Phenyl
156
4
4-morpholino-phenyl


73
1
2-Cl-Phenyl
157
1
4-CN-2-morpholino-phenyl


74
2
2-Cl-Phenyl
158
2
4-CN-2-morpholino-phenyl


75
3
2-Cl-Phenyl
159
3
4-CN-2-morpholino-phenyl


76
4
2-Cl-Phenyl
160
4
4-CN-2-morpholino-phenyl


77
1
4-Br-Phenyl
161
1
4-CH3-2-morpholino-phenyl


78
2
4-Br-Phenyl
162
2
4-CH3-2-morpholino-phenyl


79
3
4-Br-Phenyl
163
3
4-CH3-2-morpholino-phenyl


80
4
4-Br-Phenyl
164
4
4-CH3-2-morpholino-phenyl


81
1
3-Br-Phenyl
165
1
4-OH-2-morpholino-phenyl


82
2
3-Br-Phenyl
166
2
4-OH-2-morpholino-phenyl


83
3
3-Br-Phenyl
167
3
4-OH-2-morpholino-phenyl


84
4
3-Br-Phenyl
168
4
4-OH-2-morpholino-phenyl


85
1
naphthylen-1-yl
173
1
naphthylen-2-yl


86
2
naphthylen-1-yl
174
2
naphthylen-2-yl


87
3
naphthylen-1-yl
175
3
naphthylen-2-yl


88
4
naphthylen-1-yl
176
4
naphthylen-2-yl









Exemplary embodiments include compounds having the formula (XX)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 14.














TABLE 14





Entry
n
R5
Entry
n
R5




















1
1
Phenyl
85
1
2-Br-Phenyl


2
2
Phenyl
86
2
2-Br-Phenyl


3
3
Phenyl
87
3
2-Br-Phenyl


4
4
Phenyl
88
4
2-Br-Phenyl


5
1
4-OH-Phenyl
89
1
4-CF3-Phenyl


6
2
4-OH-Phenyl
90
2
4-CF3-Phenyl


7
3
4-OH-Phenyl
91
3
4-CF3-Phenyl


8
4
4-OH-Phenyl
92
4
4-CF3-Phenyl


9
1
3-OH-Phenyl
93
1
3-CF3-Phenyl


10
2
3-OH-Phenyl
94
2
3-CF3-Phenyl


11
3
3-OH-Phenyl
95
3
3-CF3-Phenyl


12
4
3-OH-Phenyl
96
4
3-CF3-Phenyl


13
1
2-OH-Phenyl
97
1
2-CF3-Phenyl


14
2
2-OH-Phenyl
98
2
2-CF3-Phenyl


15
3
2-OH-Phenyl
99
3
2-CF3-Phenyl


16
4
2-OH-Phenyl
100
4
2-CF3-Phenyl


17
1
4-OMe-Phenyl
101
1
4-iPr-Phenyl


18
2
4-OMe-Phenyl
102
2
4-iPr-Phenyl


19
3
4-OMe-Phenyl
103
3
4-iPr-Phenyl


20
4
4-OMe-Phenyl
104
4
4-iPr-Phenyl


21
1
3-OMe-Phenyl
105
1
3-iPr-Phenyl


22
2
3-OMe-Phenyl
106
2
3-iPr-Phenyl


23
3
3-OMe-Phenyl
107
3
3-iPr-Phenyl


24
4
3-OMe-Phenyl
108
4
3-iPr-Phenyl


25
1
2-OMe-Phenyl
109
1
2-iPr-Phenyl


26
2
2-OMe-Phenyl
110
2
2-iPr-Phenyl


27
3
2-OMe-Phenyl
111
3
2-iPr-Phenyl


28
4
2-OMe-Phenyl
112
4
2-iPr-Phenyl


29
1
4-CN-Phenyl
113
1
4-NH2-Phenyl


30
2
4-CN-Phenyl
114
2
4-NH2-Phenyl


31
3
4-CN-Phenyl
115
3
4-NH2-Phenyl


32
4
4-CN-Phenyl
116
4
4-NH2-Phenyl


33
1
3-CN-Phenyl
117
1
3-NH2-Phenyl


34
2
3-CN-Phenyl
118
2
3-NH2-Phenyl


35
3
3-CN-Phenyl
119
3
3-NH2-Phenyl


36
4
3-CN-Phenyl
120
4
3-NH2-Phenyl


37
1
2-CN-Phenyl
121
1
2-NH2-Phenyl


38
2
2-CN-Phenyl
122
2
2-NH2-Phenyl


39
3
2-CN-Phenyl
123
3
2-NH2-Phenyl


40
4
2-CN-Phenyl
124
4
2-NH2-Phenyl


41
1
4-Me-Phenyl
125
1
2,3-di-Me-Phenyl


42
2
4-Me-Phenyl
126
2
2,3-di-Me-Phenyl


43
3
4-Me-Phenyl
127
3
2,3-di-Me-Phenyl


44
4
4-Me-Phenyl
128
4
2,3-di-Me-Phenyl


45
1
3-Me-Phenyl
129
1
2,4-di-Me-Phenyl


46
2
3-Me-Phenyl
130
2
2,4-di-Me-Phenyl


47
3
3-Me-Phenyl
131
3
2,4-di-Me-Phenyl


48
4
3-Me-Phenyl
132
4
2,4-di-Me-Phenyl


49
1
2-Me-Phenyl
133
1
2,5-di-Me-Phenyl


50
2
2-Me-Phenyl
134
2
2,5-di-Me-Phenyl


51
3
2-Me-Phenyl
135
3
2,5-di-Me-Phenyl


52
4
2-Me-Phenyl
136
4
2,5-di-Me-Phenyl


53
1
4-F-Phenyl
137
1
2,6-di-Me-Phenyl


54
2
4-F-Phenyl
138
2
2,6-di-Me-Phenyl


55
3
4-F-Phenyl
139
3
2,6-di-Me-Phenyl


56
4
4-F-Phenyl
140
4
2,6-di-Me-Phenyl


57
1
3-F-Phenyl
141
1
2,6-di-iPr-Phenyl


58
2
3-F-Phenyl
142
2
2,6-di-iPr-Phenyl


59
3
3-F-Phenyl
143
3
2,6-di-iPr-Phenyl


60
4
3-F-Phenyl
144
4
2,6-di-iPr-Phenyl


61
1
2-F-Phenyl
145
1
2-morpholino-phenyl


62
2
2-F-Phenyl
146
2
2-morpholino-phenyl


63
3
2-F-Phenyl
147
3
2-morpholino-phenyl


64
4
2-F-Phenyl
148
4
2-morpholino-phenyl


65
1
4-Cl-Phenyl
149
1
3-morpholino-phenyl


66
2
4-Cl-Phenyl
150
2
3-morpholino-phenyl


67
3
4-Cl-Phenyl
151
3
3-morpholino-phenyl


68
4
4-Cl-Phenyl
152
4
3-morpholino-phenyl


69
1
3-Cl-Phenyl
153
1
4-morpholino-phenyl


70
2
3-Cl-Phenyl
154
2
4-morpholino-phenyl


71
3
3-Cl-Phenyl
155
3
4-morpholino-phenyl


72
4
3-Cl-Phenyl
156
4
4-morpholino-phenyl


73
1
2-Cl-Phenyl
157
1
4-CN-2-morpholino-phenyl


74
2
2-Cl-Phenyl
158
2
4-CN-2-morpholino-phenyl


75
3
2-Cl-Phenyl
159
3
4-CN-2-morpholino-phenyl


76
4
2-Cl-Phenyl
160
4
4-CN-2-morpholino-phenyl


77
1
4-Br-Phenyl
161
1
4-CH3-2-morpholino-phenyl


78
2
4-Br-Phenyl
162
2
4-CH3-2-morpholino-phenyl


79
3
4-Br-Phenyl
163
3
4-CH3-2-morpholino-phenyl


80
4
4-Br-Phenyl
164
4
4-CH3-2-morpholino-phenyl


81
1
3-Br-Phenyl
165
1
4-OH-2-morpholino-phenyl


82
2
3-Br-Phenyl
166
2
4-OH-2-morpholino-phenyl


83
3
3-Br-Phenyl
167
3
4-OH-2-morpholino-phenyl


84
4
3-Br-Phenyl
168
4
4-OH-2-morpholino-phenyl


85
1
naphthylen-1-yl
173
1
naphthylen-2-yl


86
2
naphthylen-1-yl
174
2
naphthylen-2-yl


87
3
naphthylen-1-yl
175
3
naphthylen-2-yl


88
4
naphthylen-1-yl
176
4
naphthylen-2-yl









Exemplary embodiments include compounds having the formula (XXI)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 15.














TABLE 15





Entry
n
R5
Entry
n
R5




















1
1
Phenyl
85
1
2-Br-Phenyl


2
2
Phenyl
86
2
2-Br-Phenyl


3
3
Phenyl
87
3
2-Br-Phenyl


4
4
Phenyl
88
4
2-Br-Phenyl


5
1
4-OH-Phenyl
89
1
4-CF3-Phenyl


6
2
4-OH-Phenyl
90
2
4-CF3-Phenyl


7
3
4-OH-Phenyl
91
3
4-CF3-Phenyl


8
4
4-OH-Phenyl
92
4
4-CF3-Phenyl


9
1
3-OH-Phenyl
93
1
3-CF3-Phenyl


10
2
3-OH-Phenyl
94
2
3-CF3-Phenyl


11
3
3-OH-Phenyl
95
3
3-CF3-Phenyl


12
4
3-OH-Phenyl
96
4
3-CF3-Phenyl


13
1
2-OH-Phenyl
97
1
2-CF3-Phenyl


14
2
2-OH-Phenyl
98
2
2-CF3-Phenyl


15
3
2-OH-Phenyl
99
3
2-CF3-Phenyl


16
4
2-OH-Phenyl
100
4
2-CF3-Phenyl


17
1
4-OMe-Phenyl
101
1
4-iPr-Phenyl


18
2
4-OMe-Phenyl
102
2
4-iPr-Phenyl


19
3
4-OMe-Phenyl
103
3
4-iPr-Phenyl


20
4
4-OMe-Phenyl
104
4
4-iPr-Phenyl


21
1
3-OMe-Phenyl
105
1
3-iPr-Phenyl


22
2
3-OMe-Phenyl
106
2
3-iPr-Phenyl


23
3
3-OMe-Phenyl
107
3
3-iPr-Phenyl


24
4
3-OMe-Phenyl
108
4
3-iPr-Phenyl


25
1
2-OMe-Phenyl
109
1
2-iPr-Phenyl


26
2
2-OMe-Phenyl
110
2
2-iPr-Phenyl


27
3
2-OMe-Phenyl
111
3
2-iPr-Phenyl


28
4
2-OMe-Phenyl
112
4
2-iPr-Phenyl


29
1
4-CN-Phenyl
113
1
4-NH2-Phenyl


30
2
4-CN-Phenyl
114
2
4-NH2-Phenyl


31
3
4-CN-Phenyl
115
3
4-NH2-Phenyl


32
4
4-CN-Phenyl
116
4
4-NH2-Phenyl


33
1
3-CN-Phenyl
117
1
3-NH2-Phenyl


34
2
3-CN-Phenyl
118
2
3-NH2-Phenyl


35
3
3-CN-Phenyl
119
3
3-NH2-Phenyl


36
4
3-CN-Phenyl
120
4
3-NH2-Phenyl


37
1
2-CN-Phenyl
121
1
2-NH2-Phenyl


38
2
2-CN-Phenyl
122
2
2-NH2-Phenyl


39
3
2-CN-Phenyl
123
3
2-NH2-Phenyl


40
4
2-CN-Phenyl
124
4
2-NH2-Phenyl


41
1
4-Me-Phenyl
125
1
2,3-di-Me-Phenyl


42
2
4-Me-Phenyl
126
2
2,3-di-Me-Phenyl


43
3
4-Me-Phenyl
127
3
2,3-di-Me-Phenyl


44
4
4-Me-Phenyl
128
4
2,3-di-Me-Phenyl


45
1
3-Me-Phenyl
129
1
2,4-di-Me-Phenyl


46
2
3-Me-Phenyl
130
2
2,4-di-Me-Phenyl


47
3
3-Me-Phenyl
131
3
2,4-di-Me-Phenyl


48
4
3-Me-Phenyl
132
4
2,4-di-Me-Phenyl


49
1
2-Me-Phenyl
133
1
2,5-di-Me-Phenyl


50
2
2-Me-Phenyl
134
2
2,5-di-Me-Phenyl


51
3
2-Me-Phenyl
135
3
2,5-di-Me-Phenyl


52
4
2-Me-Phenyl
136
4
2,5-di-Me-Phenyl


53
1
4-F-Phenyl
137
1
2,6-di-Me-Phenyl


54
2
4-F-Phenyl
138
2
2,6-di-Me-Phenyl


55
3
4-F-Phenyl
139
3
2,6-di-Me-Phenyl


56
4
4-F-Phenyl
140
4
2,6-di-Me-Phenyl


57
1
3-F-Phenyl
141
1
2,6-di-iPr-Phenyl


58
2
3-F-Phenyl
142
2
2,6-di-iPr-Phenyl


59
3
3-F-Phenyl
143
3
2,6-di-iPr-Phenyl


60
4
3-F-Phenyl
144
4
2,6-di-iPr-Phenyl


61
1
2-F-Phenyl
145
1
2-morpholino-phenyl


62
2
2-F-Phenyl
146
2
2-morpholino-phenyl


63
3
2-F-Phenyl
147
3
2-morpholino-phenyl


64
4
2-F-Phenyl
148
4
2-morpholino-phenyl


65
1
4-Cl-Phenyl
149
1
3-morpholino-phenyl


66
2
4-Cl-Phenyl
150
2
3-morpholino-phenyl


67
3
4-Cl-Phenyl
151
3
3-morpholino-phenyl


68
4
4-Cl-Phenyl
152
4
3-morpholino-phenyl


69
1
3-Cl-Phenyl
153
1
4-morpholino-phenyl


70
2
3-Cl-Phenyl
154
2
4-morpholino-phenyl


71
3
3-Cl-Phenyl
155
3
4-morpholino-phenyl


72
4
3-Cl-Phenyl
156
4
4-morpholino-phenyl


73
1
2-Cl-Phenyl
157
1
4-CN-2-morpholino-phenyl


74
2
2-Cl-Phenyl
158
2
4-CN-2-morpholino-phenyl


75
3
2-Cl-Phenyl
159
3
4-CN-2-morpholino-phenyl


76
4
2-Cl-Phenyl
160
4
4-CN-2-morpholino-phenyl


77
1
4-Br-Phenyl
161
1
4-CH3-2-morpholino-phenyl


78
2
4-Br-Phenyl
162
2
4-CH3-2-morpholino-phenyl


79
3
4-Br-Phenyl
163
3
4-CH3-2-morpholino-phenyl


80
4
4-Br-Phenyl
164
4
4-CH3-2-morpholino-phenyl


81
1
3-Br-Phenyl
165
1
4-OH-2-morpholino-phenyl


82
2
3-Br-Phenyl
166
2
4-OH-2-morpholino-phenyl


83
3
3-Br-Phenyl
167
3
4-OH-2-morpholino-phenyl


84
4
3-Br-Phenyl
168
4
4-OH-2-morpholino-phenyl


85
1
naphthylen-1-yl
173
1
naphthylen-2-yl


86
2
naphthylen-1-yl
174
2
naphthylen-2-yl


87
3
naphthylen-1-yl
175
3
naphthylen-2-yl


88
4
naphthylen-1-yl
176
4
naphthylen-2-yl









Exemplary embodiments include compounds having the formula (XXII)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 16.














TABLE 16







Entry
n
R7
R3





















1
1
H
Phenyl



2
2
H
Phenyl



3
3
H
Phenyl



4
4
H
Phenyl



5
1
Me
Phenyl



6
2
Me
Phenyl



7
3
Me
Phenyl



8
4
Me
Phenyl



9
1
CH2Ph
Phenyl



10
2
CH2Ph
Phenyl



11
3
CH2Ph
Phenyl



12
4
CH2Ph
Phenyl



13
1
COMe
Phenyl



14
2
COMe
Phenyl



15
3
COMe
Phenyl



16
4
COMe
Phenyl



17
1
CO2Me
Phenyl



18
2
CO2Me
Phenyl



19
3
CO2Me
Phenyl



20
4
CO2Me
Phenyl



21
1
CO2tBu
Phenyl



22
2
CO2tBu
Phenyl



23
3
CO2tBu
Phenyl



24
4
CO2tBu
Phenyl



25
1
CONHMe
Phenyl



26
2
CONHMe
Phenyl



27
3
CONHMe
Phenyl



28
4
CONHMe
Phenyl



29
1
SO2Me
Phenyl



30
2
SO2Me
Phenyl



31
3
SO2Me
Phenyl



32
4
SO2Me
Phenyl



33
1
SO2NH2
Phenyl



34
2
SO2NH2
Phenyl



35
3
SO2NH2
Phenyl



36
4
SO2NH2
Phenyl



37
1
H
3-OH-Phenyl



38
2
H
3-OH-Phenyl



39
3
H
3-OH-Phenyl



40
4
H
3-OH-Phenyl



41
1
Me
3-OH-Phenyl



42
2
Me
3-OH-Phenyl



43
3
Me
3-OH-Phenyl



44
4
Me
3-OH-Phenyl



45
1
CH2Ph
3-OH-Phenyl



46
2
CH2Ph
3-OH-Phenyl



47
3
CH2Ph
3-OH-Phenyl



48
4
CH2Ph
3-OH-Phenyl



49
1
COMe
3-OH-Phenyl



50
2
COMe
3-OH-Phenyl



51
3
COMe
3-OH-Phenyl



52
4
COMe
3-OH-Phenyl



53
1
CO2Me
3-OH-Phenyl



54
2
CO2Me
3-OH-Phenyl



55
3
CO2Me
3-OH-Phenyl



56
4
CO2Me
3-OH-Phenyl



57
1
CO2tBu
3-OH-Phenyl



58
2
CO2tBu
3-OH-Phenyl



59
3
CO2tBu
3-OH-Phenyl



60
4
CO2tBu
3-OH-Phenyl



61
1
CONHMe
3-OH-Phenyl



62
2
CONHMe
3-OH-Phenyl



63
3
CONHMe
3-OH-Phenyl



64
4
CONHMe
3-OH-Phenyl



65
1
SO2Me
3-OH-Phenyl



66
2
SO2Me
3-OH-Phenyl



67
3
SO2Me
3-OH-Phenyl



68
4
SO2Me
3-OH-Phenyl



69
1
SO2NH2
3-OH-Phenyl



70
2
SO2NH2
3-OH-Phenyl



71
3
SO2NH2
3-OH-Phenyl



72
4
SO2NH2
3-OH-Phenyl



73
1
H
4-NO2-Phenyl



74
2
H
4-NO2-Phenyl



75
3
H
4-NO2-Phenyl



76
4
H
4-NO2-Phenyl



77
1
Me
4-NO2-Phenyl



78
2
Me
4-NO2-Phenyl



79
3
Me
4-NO2-Phenyl



80
4
Me
4-NO2-Phenyl



81
1
CH2Ph
4-NO2-Phenyl



82
2
CH2Ph
4-NO2-Phenyl



83
3
CH2Ph
4-NO2-Phenyl



84
4
CH2Ph
4-NO2-Phenyl



85
1
COMe
4-NO2-Phenyl



86
2
COMe
4-NO2-Phenyl



87
3
COMe
4-NO2-Phenyl



88
4
COMe
4-NO2-Phenyl



89
1
CO2Me
4-NO2-Phenyl



90
2
CO2Me
4-NO2-Phenyl



91
3
CO2Me
4-NO2-Phenyl



92
4
CO2Me
4-NO2-Phenyl



93
1
CO2tBu
4-NO2-Phenyl



94
2
CO2tBu
4-NO2-Phenyl



95
3
CO2tBu
4-NO2-Phenyl



96
4
CO2tBu
4-NO2-Phenyl



97
1
CONHMe
4-NO2-Phenyl



98
2
CONHMe
4-NO2-Phenyl



99
3
CONHMe
4-NO2-Phenyl



100
4
CONHMe
4-NO2-Phenyl



101
1
SO2Me
4-NO2-Phenyl



102
2
SO2Me
4-NO2-Phenyl



103
3
SO2Me
4-NO2-Phenyl



104
4
SO2Me
4-NO2-Phenyl



105
1
SO2NH2
4-NO2-Phenyl



106
2
SO2NH2
4-NO2-Phenyl



107
3
SO2NH2
4-NO2-Phenyl



108
4
SO2NH2
4-NO2-Phenyl



109
1
H
3-OMe-Phenyl



110
2
H
3-OMe-Phenyl



111
3
H
3-OMe-Phenyl



112
4
H
3-OMe-Phenyl



113
1
Me
3-OMe-Phenyl



114
2
Me
3-OMe-Phenyl



115
3
Me
3-OMe-Phenyl



116
4
Me
3-OMe-Phenyl



117
1
CH2Ph
3-OMe-Phenyl



118
2
CH2Ph
3-OMe-Phenyl



119
3
CH2Ph
3-OMe-Phenyl



120
4
CH2Ph
3-OMe-Phenyl



121
1
COMe
3-OMe-Phenyl



122
2
COMe
3-OMe-Phenyl



123
3
COMe
3-OMe-Phenyl



124
4
COMe
3-OMe-Phenyl



125
1
CO2Me
3-OMe-Phenyl



126
2
CO2Me
3-OMe-Phenyl



127
3
CO2Me
3-OMe-Phenyl



128
4
CO2Me
3-OMe-Phenyl



129
1
CO2tBu
3-OMe-Phenyl



130
2
CO2tBu
3-OMe-Phenyl



131
3
CO2tBu
3-OMe-Phenyl



132
4
CO2tBu
3-OMe-Phenyl



133
1
CONHMe
3-OMe-Phenyl



134
2
CONHMe
3-OMe-Phenyl



135
3
CONHMe
3-OMe-Phenyl



136
4
CONHMe
3-OMe-Phenyl



137
1
SO2Me
3-OMe-Phenyl



138
2
SO2Me
3-OMe-Phenyl



139
3
SO2Me
3-OMe-Phenyl



140
4
SO2Me
3-OMe-Phenyl



141
1
SO2NH2
3-OMe-Phenyl



142
2
SO2NH2
3-OMe-Phenyl



143
3
SO2NH2
3-OMe-Phenyl



144
4
SO2NH2
3-OMe-Phenyl



145
1
H
4-CN-Phenyl



146
2
H
4-CN-Phenyl



147
3
H
4-CN-Phenyl



148
4
H
4-CN-Phenyl



149
1
Me
4-CN-Phenyl



150
2
Me
4-CN-Phenyl



151
3
Me
4-CN-Phenyl



152
4
Me
4-CN-Phenyl



153
1
CH2Ph
4-CN-Phenyl



154
2
CH2Ph
4-CN-Phenyl



155
3
CH2Ph
4-CN-Phenyl



156
4
CH2Ph
4-CN-Phenyl



157
1
COMe
4-CN-Phenyl



158
2
COMe
4-CN-Phenyl



159
3
COMe
4-CN-Phenyl



160
4
COMe
4-CN-Phenyl



161
1
CO2Me
4-CN-Phenyl



162
2
CO2Me
4-CN-Phenyl



163
3
CO2Me
4-CN-Phenyl



164
4
CO2Me
4-CN-Phenyl



165
1
CO2tBu
4-CN-Phenyl



166
2
CO2tBu
4-CN-Phenyl



167
3
CO2tBu
4-CN-Phenyl



168
4
CO2tBu
4-CN-Phenyl



169
1
CONHMe
4-CN-Phenyl



170
2
CONHMe
4-CN-Phenyl



171
3
CONHMe
4-CN-Phenyl



172
4
CONHMe
4-CN-Phenyl



173
1
SO2Me
4-CN-Phenyl



174
2
SO2Me
4-CN-Phenyl



175
3
SO2Me
4-CN-Phenyl



176
4
SO2Me
4-CN-Phenyl



177
1
SO2NH2
4-CN-Phenyl



178
2
SO2NH2
4-CN-Phenyl



179
3
SO2NH2
4-CN-Phenyl



180
4
SO2NH2
4-CN-Phenyl



181
1
H
2-CN-Phenyl



182
2
H
2-CN-Phenyl



183
3
H
2-CN-Phenyl



184
4
H
2-CN-Phenyl



185
1
Me
2-CN-Phenyl



186
2
Me
2-CN-Phenyl



187
3
Me
2-CN-Phenyl



188
4
Me
2-CN-Phenyl



189
1
CH2Ph
2-CN-Phenyl



190
2
CH2Ph
2-CN-Phenyl



191
3
CH2Ph
2-CN-Phenyl



192
4
CH2Ph
2-CN-Phenyl



193
1
COMe
2-CN-Phenyl



194
2
COMe
2-CN-Phenyl



195
3
COMe
2-CN-Phenyl



196
4
COMe
2-CN-Phenyl



197
1
CO2Me
2-CN-Phenyl



198
2
CO2Me
2-CN-Phenyl



199
3
CO2Me
2-CN-Phenyl



200
4
CO2Me
2-CN-Phenyl



201
1
CO2tBu
2-CN-Phenyl



202
2
CO2tBu
2-CN-Phenyl



203
3
CO2tBu
2-CN-Phenyl



204
4
CO2tBu
2-CN-Phenyl



205
1
CONHMe
2-CN-Phenyl



206
2
CONHMe
2-CN-Phenyl



207
3
CONHMe
2-CN-Phenyl



208
4
CONHMe
2-CN-Phenyl



209
1
SO2Me
2-CN-Phenyl



210
2
SO2Me
2-CN-Phenyl



211
3
SO2Me
2-CN-Phenyl



212
4
SO2Me
2-CN-Phenyl



213
1
SO2NH2
2-CN-Phenyl



214
2
SO2NH2
2-CN-Phenyl



215
3
SO2NH2
2-CN-Phenyl



216
4
SO2NH2
2-CN-Phenyl



217
1
H
3-Me-Phenyl



218
2
H
3-Me-Phenyl



219
3
H
3-Me-Phenyl



220
4
H
3-Me-Phenyl



221
1
Me
3-Me-Phenyl



222
2
Me
3-Me-Phenyl



223
3
Me
3-Me-Phenyl



224
4
Me
3-Me-Phenyl



225
1
CH2Ph
3-Me-Phenyl



226
2
CH2Ph
3-Me-Phenyl



227
3
CH2Ph
3-Me-Phenyl



228
4
CH2Ph
3-Me-Phenyl



229
1
COMe
3-Me-Phenyl



230
2
COMe
3-Me-Phenyl



231
3
COMe
3-Me-Phenyl



232
4
COMe
3-Me-Phenyl



233
1
CO2Me
3-Me-Phenyl



234
2
CO2Me
3-Me-Phenyl



235
3
CO2Me
3-Me-Phenyl



236
4
CO2Me
3-Me-Phenyl



237
1
CO2tBu
3-Me-Phenyl



238
2
CO2tBu
3-Me-Phenyl



239
3
CO2tBu
3-Me-Phenyl



240
4
CO2tBu
3-Me-Phenyl



241
1
CONHMe
3-Me-Phenyl



242
2
CONHMe
3-Me-Phenyl



243
3
CONHMe
3-Me-Phenyl



244
4
CONHMe
3-Me-Phenyl



245
1
SO2Me
3-Me-Phenyl



246
2
SO2Me
3-Me-Phenyl



247
3
SO2Me
3-Me-Phenyl



248
4
SO2Me
3-Me-Phenyl



249
1
SO2NH2
3-Me-Phenyl



250
2
SO2NH2
3-Me-Phenyl



251
3
SO2NH2
3-Me-Phenyl



252
4
SO2NH2
3-Me-Phenyl



253
1
H
2-F-Phenyl



254
2
H
2-F-Phenyl



255
3
H
2-F-Phenyl



256
4
H
2-F-Phenyl



257
1
Me
2-F-Phenyl



258
2
Me
2-F-Phenyl



259
3
Me
2-F-Phenyl



260
4
Me
2-F-Phenyl



261
1
CH2Ph
2-F-Phenyl



262
2
CH2Ph
2-F-Phenyl



263
3
CH2Ph
2-F-Phenyl



264
4
CH2Ph
2-F-Phenyl



265
1
COMe
2-F-Phenyl



266
2
COMe
2-F-Phenyl



267
3
COMe
2-F-Phenyl



268
4
COMe
2-F-Phenyl



269
1
CO2Me
2-F-Phenyl



270
2
CO2Me
2-F-Phenyl



271
3
CO2Me
2-F-Phenyl



272
4
CO2Me
2-F-Phenyl



273
1
CO2tBu
2-F-Phenyl



274
2
CO2tBu
2-F-Phenyl



275
3
CO2tBu
2-F-Phenyl



276
4
CO2tBu
2-F-Phenyl



277
1
CONHMe
2-F-Phenyl



278
2
CONHMe
2-F-Phenyl



279
3
CONHMe
2-F-Phenyl



280
4
CONHMe
2-F-Phenyl



281
1
SO2Me
2-F-Phenyl



282
2
SO2Me
2-F-Phenyl



283
3
SO2Me
2-F-Phenyl



284
4
SO2Me
2-F-Phenyl



285
1
SO2NH2
2-F-Phenyl



286
2
SO2NH2
2-F-Phenyl



287
3
SO2NH2
2-F-Phenyl



288
4
SO2NH2
2-F-Phenyl



289
1
H
4-F-Phenyl



290
2
H
4-F-Phenyl



291
3
H
4-F-Phenyl



292
4
H
4-F-Phenyl



293
1
Me
4-F-Phenyl



294
2
Me
4-F-Phenyl



295
3
Me
4-F-Phenyl



296
4
Me
4-F-Phenyl



297
1
CH2Ph
4-F-Phenyl



298
2
CH2Ph
4-F-Phenyl



299
3
CH2Ph
4-F-Phenyl



300
4
CH2Ph
4-F-Phenyl



301
1
COMe
4-F-Phenyl



302
2
COMe
4-F-Phenyl



303
3
COMe
4-F-Phenyl



304
4
COMe
4-F-Phenyl



305
1
CO2Me
4-F-Phenyl



306
2
CO2Me
4-F-Phenyl



307
3
CO2Me
4-F-Phenyl



308
4
CO2Me
4-F-Phenyl



309
1
CO2tBu
4-F-Phenyl



310
2
CO2tBu
4-F-Phenyl



311
3
CO2tBu
4-F-Phenyl



312
4
CO2tBu
4-F-Phenyl



313
1
CONHMe
4-F-Phenyl



314
2
CONHMe
4-F-Phenyl



315
3
CONHMe
4-F-Phenyl



316
4
CONHMe
4-F-Phenyl



317
1
SO2Me
4-F-Phenyl



318
2
SO2Me
4-F-Phenyl



319
3
SO2Me
4-F-Phenyl



320
4
SO2Me
4-F-Phenyl



321
1
SO2NH2
4-F-Phenyl



322
2
SO2NH2
4-F-Phenyl



323
3
SO2NH2
4-F-Phenyl



324
4
SO2NH2
4-F-Phenyl



325
1
H
3-Cl-Phenyl



326
2
H
3-Cl-Phenyl



327
3
H
3-Cl-Phenyl



328
4
H
3-Cl-Phenyl



329
1
Me
3-Cl-Phenyl



330
2
Me
3-Cl-Phenyl



331
3
Me
3-Cl-Phenyl



332
4
Me
3-Cl-Phenyl



333
1
CH2Ph
3-Cl-Phenyl



334
2
CH2Ph
3-Cl-Phenyl



335
3
CH2Ph
3-Cl-Phenyl



336
4
CH2Ph
3-Cl-Phenyl



337
1
COMe
3-Cl-Phenyl



338
2
COMe
3-Cl-Phenyl



339
3
COMe
3-Cl-Phenyl



340
4
COMe
3-Cl-Phenyl



341
1
CO2Me
3-Cl-Phenyl



342
2
CO2Me
3-Cl-Phenyl



343
3
CO2Me
3-Cl-Phenyl



344
4
CO2Me
3-Cl-Phenyl



345
1
CO2tBu
3-Cl-Phenyl



346
2
CO2tBu
3-Cl-Phenyl



347
3
CO2tBu
3-Cl-Phenyl



348
4
CO2tBu
3-Cl-Phenyl



349
1
CONHMe
3-Cl-Phenyl



350
2
CONHMe
3-Cl-Phenyl



351
3
CONHMe
3-Cl-Phenyl



352
4
CONHMe
3-Cl-Phenyl



353
1
SO2Me
3-Cl-Phenyl



354
2
SO2Me
3-Cl-Phenyl



355
3
SO2Me
3-Cl-Phenyl



356
4
SO2Me
3-Cl-Phenyl



357
1
SO2NH2
3-Cl-Phenyl



358
2
SO2NH2
3-Cl-Phenyl



359
3
SO2NH2
3-Cl-Phenyl



360
4
SO2NH2
3-Cl-Phenyl



361
1
H
2-Br-Phenyl



362
2
H
2-Br-Phenyl



363
3
H
2-Br-Phenyl



364
4
H
2-Br-Phenyl



365
1
Me
2-Br-Phenyl



366
2
Me
2-Br-Phenyl



367
3
Me
2-Br-Phenyl



368
4
Me
2-Br-Phenyl



369
1
CH2Ph
2-Br-Phenyl



370
2
CH2Ph
2-Br-Phenyl



371
3
CH2Ph
2-Br-Phenyl



372
4
CH2Ph
2-Br-Phenyl



373
1
COMe
2-Br-Phenyl



374
2
COMe
2-Br-Phenyl



375
3
COMe
2-Br-Phenyl



376
4
COMe
2-Br-Phenyl



377
1
CO2Me
2-Br-Phenyl



378
2
CO2Me
2-Br-Phenyl



379
3
CO2Me
2-Br-Phenyl



380
4
CO2Me
2-Br-Phenyl



381
1
CO2tBu
2-Br-Phenyl



382
2
CO2tBu
2-Br-Phenyl



383
3
CO2tBu
2-Br-Phenyl



384
4
CO2tBu
2-Br-Phenyl



385
1
CONHMe
2-Br-Phenyl



386
2
CONHMe
2-Br-Phenyl



387
3
CONHMe
2-Br-Phenyl



388
4
CONHMe
2-Br-Phenyl



389
1
SO2Me
2-Br-Phenyl



390
2
SO2Me
2-Br-Phenyl



391
3
SO2Me
2-Br-Phenyl



392
4
SO2Me
2-Br-Phenyl



393
1
SO2NH2
2-Br-Phenyl



394
2
SO2NH2
2-Br-Phenyl



395
3
SO2NH2
2-Br-Phenyl



396
4
SO2NH2
2-Br-Phenyl



397
1
H
4-Br-Phenyl



398
2
H
4-Br-Phenyl



399
3
H
4-Br-Phenyl



400
4
H
4-Br-Phenyl



401
1
Me
4-Br-Phenyl



402
2
Me
4-Br-Phenyl



403
3
Me
4-Br-Phenyl



404
4
Me
4-Br-Phenyl



405
1
CH2Ph
4-Br-Phenyl



406
2
CH2Ph
4-Br-Phenyl



407
3
CH2Ph
4-Br-Phenyl



408
4
CH2Ph
4-Br-Phenyl



409
1
COMe
4-Br-Phenyl



410
2
COMe
4-Br-Phenyl



411
3
COMe
4-Br-Phenyl



412
4
COMe
4-Br-Phenyl



413
1
CO2Me
4-Br-Phenyl



414
2
CO2Me
4-Br-Phenyl



415
3
CO2Me
4-Br-Phenyl



416
4
CO2Me
4-Br-Phenyl



417
1
CO2tBu
4-Br-Phenyl



418
2
CO2tBu
4-Br-Phenyl



419
3
CO2tBu
4-Br-Phenyl



420
4
CO2tBu
4-Br-Phenyl



421
1
CONHMe
4-Br-Phenyl



422
2
CONHMe
4-Br-Phenyl



423
3
CONHMe
4-Br-Phenyl



424
4
CONHMe
4-Br-Phenyl



425
1
SO2Me
4-Br-Phenyl



426
2
SO2Me
4-Br-Phenyl



427
3
SO2Me
4-Br-Phenyl



428
4
SO2Me
4-Br-Phenyl



429
1
SO2NH2
4-Br-Phenyl



430
2
SO2NH2
4-Br-Phenyl



431
3
SO2NH2
4-Br-Phenyl



432
4
SO2NH2
4-Br-Phenyl



433
1
H
3-CF3-Phenyl



434
2
H
3-CF3-Phenyl



435
3
H
3-CF3-Phenyl



436
4
H
3-CF3-Phenyl



437
1
Me
3-CF3-Phenyl



438
2
Me
3-CF3-Phenyl



439
3
Me
3-CF3-Phenyl



440
4
Me
3-CF3-Phenyl



441
1
CH2Ph
3-CF3-Phenyl



442
2
CH2Ph
3-CF3-Phenyl



443
3
CH2Ph
3-CF3-Phenyl



444
4
CH2Ph
3-CF3-Phenyl



445
1
COMe
3-CF3-Phenyl



446
2
COMe
3-CF3-Phenyl



447
3
COMe
3-CF3-Phenyl



448
4
COMe
3-CF3-Phenyl



449
1
CO2Me
3-CF3-Phenyl



450
2
CO2Me
3-CF3-Phenyl



451
3
CO2Me
3-CF3-Phenyl



452
4
CO2Me
3-CF3-Phenyl



453
1
CO2tBu
3-CF3-Phenyl



454
2
CO2tBu
3-CF3-Phenyl



455
3
CO2tBu
3-CF3-Phenyl



456
4
CO2tBu
3-CF3-Phenyl



457
1
CONHMe
3-CF3-Phenyl



458
2
CONHMe
3-CF3-Phenyl



459
3
CONHMe
3-CF3-Phenyl



460
4
CONHMe
3-CF3-Phenyl



461
1
SO2Me
3-CF3-Phenyl



462
2
SO2Me
3-CF3-Phenyl



463
3
SO2Me
3-CF3-Phenyl



464
4
SO2Me
3-CF3-Phenyl



465
1
SO2NH2
3-CF3-Phenyl



466
2
SO2NH2
3-CF3-Phenyl



467
3
SO2NH2
3-CF3-Phenyl



468
4
SO2NH2
3-CF3-Phenyl



469
1
H
2-iPr-Phenyl



470
2
H
2-iPr-Phenyl



471
3
H
2-iPr-Phenyl



472
4
H
2-iPr-Phenyl



473
1
Me
2-iPr-Phenyl



474
2
Me
2-iPr-Phenyl



475
3
Me
2-iPr-Phenyl



476
4
Me
2-iPr-Phenyl



477
1
CH2Ph
2-iPr-Phenyl



478
2
CH2Ph
2-iPr-Phenyl



479
3
CH2Ph
2-iPr-Phenyl



480
4
CH2Ph
2-iPr-Phenyl



481
1
COMe
2-iPr-Phenyl



482
2
COMe
2-iPr-Phenyl



483
3
COMe
2-iPr-Phenyl



484
4
COMe
2-iPr-Phenyl



485
1
CO2Me
2-iPr-Phenyl



486
2
CO2Me
2-iPr-Phenyl



487
3
CO2Me
2-iPr-Phenyl



488
4
CO2Me
2-iPr-Phenyl



489
1
CO2tBu
2-iPr-Phenyl



490
2
CO2tBu
2-iPr-Phenyl



491
3
CO2tBu
2-iPr-Phenyl



492
4
CO2tBu
2-iPr-Phenyl



493
1
CONHMe
2-iPr-Phenyl



494
2
CONHMe
2-iPr-Phenyl



495
3
CONHMe
2-iPr-Phenyl



496
4
CONHMe
2-iPr-Phenyl



497
1
SO2Me
2-iPr-Phenyl



498
2
SO2Me
2-iPr-Phenyl



499
3
SO2Me
2-iPr-Phenyl



500
4
SO2Me
2-iPr-Phenyl



501
1
SO2NH2
2-iPr-Phenyl



502
2
SO2NH2
2-iPr-Phenyl



503
3
SO2NH2
2-iPr-Phenyl



504
4
SO2NH2
2-iPr-Phenyl



505
1
H
4-iPr-Phenyl



506
2
H
4-iPr-Phenyl



507
3
H
4-iPr-Phenyl



508
4
H
4-iPr-Phenyl



509
1
Me
4-iPr-Phenyl



510
2
Me
4-iPr-Phenyl



511
3
Me
4-iPr-Phenyl



512
4
Me
4-iPr-Phenyl



513
1
CH2Ph
4-iPr-Phenyl



514
2
CH2Ph
4-iPr-Phenyl



515
3
CH2Ph
4-iPr-Phenyl



516
4
CH2Ph
4-iPr-Phenyl



517
1
COMe
4-iPr-Phenyl



518
2
COMe
4-iPr-Phenyl



519
3
COMe
4-iPr-Phenyl



520
4
COMe
4-iPr-Phenyl



521
1
CO2Me
4-iPr-Phenyl



522
2
CO2Me
4-iPr-Phenyl



523
3
CO2Me
4-iPr-Phenyl



524
4
CO2Me
4-iPr-Phenyl



525
1
CO2tBu
4-iPr-Phenyl



526
2
CO2tBu
4-iPr-Phenyl



527
3
CO2tBu
4-iPr-Phenyl



528
4
CO2tBu
4-iPr-Phenyl



529
1
CONHMe
4-iPr-Phenyl



530
2
CONHMe
4-iPr-Phenyl



531
3
CONHMe
4-iPr-Phenyl



532
4
CONHMe
4-iPr-Phenyl



533
1
SO2Me
4-iPr-Phenyl



534
2
SO2Me
4-iPr-Phenyl



535
3
SO2Me
4-iPr-Phenyl



536
4
SO2Me
4-iPr-Phenyl



537
1
SO2NH2
4-iPr-Phenyl



538
2
SO2NH2
4-iPr-Phenyl



539
3
SO2NH2
4-iPr-Phenyl



540
4
SO2NH2
4-iPr-Phenyl



541
1
H
3-NH2-Phenyl



542
2
H
3-NH2-Phenyl



543
3
H
3-NH2-Phenyl



544
4
H
3-NH2-Phenyl



545
1
Me
3-NH2-Phenyl



546
2
Me
3-NH2-Phenyl



547
3
Me
3-NH2-Phenyl



548
4
Me
3-NH2-Phenyl



549
1
CH2Ph
3-NH2-Phenyl



550
2
CH2Ph
3-NH2-Phenyl



551
3
CH2Ph
3-NH2-Phenyl



552
4
CH2Ph
3-NH2-Phenyl



553
1
COMe
3-NH2-Phenyl



554
2
COMe
3-NH2-Phenyl



555
3
COMe
3-NH2-Phenyl



556
4
COMe
3-NH2-Phenyl



557
1
CO2Me
3-NH2-Phenyl



558
2
CO2Me
3-NH2-Phenyl



559
3
CO2Me
3-NH2-Phenyl



560
4
CO2Me
3-NH2-Phenyl



561
1
CO2tBu
3-NH2-Phenyl



562
2
CO2tBu
3-NH2-Phenyl



563
3
CO2tBu
3-NH2-Phenyl



564
4
CO2tBu
3-NH2-Phenyl



565
1
CONHMe
3-NH2-Phenyl



566
2
CONHMe
3-NH2-Phenyl



567
3
CONHMe
3-NH2-Phenyl



568
4
CONHMe
3-NH2-Phenyl



569
1
SO2Me
3-NH2-Phenyl



570
2
SO2Me
3-NH2-Phenyl



571
3
SO2Me
3-NH2-Phenyl



572
4
SO2Me
3-NH2-Phenyl



573
1
SO2NH2
3-NH2-Phenyl



574
2
SO2NH2
3-NH2-Phenyl



575
3
SO2NH2
3-NH2-Phenyl



576
4
SO2NH2
3-NH2-Phenyl



577
1
H
2,4-di-Me-Phenyl



578
2
H
2,4-di-Me-Phenyl



579
3
H
2,4-di-Me-Phenyl



580
4
H
2,4-di-Me-Phenyl



581
1
Me
2,4-di-Me-Phenyl



582
2
Me
2,4-di-Me-Phenyl



583
3
Me
2,4-di-Me-Phenyl



584
4
Me
2,4-di-Me-Phenyl



585
1
CH2Ph
2,4-di-Me-Phenyl



586
2
CH2Ph
2,4-di-Me-Phenyl



587
3
CH2Ph
2,4-di-Me-Phenyl



588
4
CH2Ph
2,4-di-Me-Phenyl



589
1
COMe
2,4-di-Me-Phenyl



590
2
COMe
2,4-di-Me-Phenyl



591
3
COMe
2,4-di-Me-Phenyl



592
4
COMe
2,4-di-Me-Phenyl



593
1
CO2Me
2,4-di-Me-Phenyl



594
2
CO2Me
2,4-di-Me-Phenyl



595
3
CO2Me
2,4-di-Me-Phenyl



596
4
CO2Me
2,4-di-Me-Phenyl



597
1
CO2tBu
2,4-di-Me-Phenyl



598
2
CO2tBu
2,4-di-Me-Phenyl



599
3
CO2tBu
2,4-di-Me-Phenyl



600
4
CO2tBu
2,4-di-Me-Phenyl



601
1
CONHMe
2,4-di-Me-Phenyl



602
2
CONHMe
2,4-di-Me-Phenyl



603
3
CONHMe
2,4-di-Me-Phenyl



604
4
CONHMe
2,4-di-Me-Phenyl



605
1
SO2Me
2,4-di-Me-Phenyl



606
2
SO2Me
2,4-di-Me-Phenyl



607
3
SO2Me
2,4-di-Me-Phenyl



608
4
SO2Me
2,4-di-Me-Phenyl



609
1
SO2NH2
2,4-di-Me-Phenyl



610
2
SO2NH2
2,4-di-Me-Phenyl



611
3
SO2NH2
2,4-di-Me-Phenyl



612
4
SO2NH2
2,4-di-Me-Phenyl



613
1
H
2,6-di-iPr-Phenyl



614
2
H
2,6-di-iPr-Phenyl



615
3
H
2,6-di-iPr-Phenyl



616
4
H
2,6-di-iPr-Phenyl



617
1
Me
2,6-di-iPr-Phenyl



618
2
Me
2,6-di-iPr-Phenyl



619
3
Me
2,6-di-iPr-Phenyl



620
4
Me
2,6-di-iPr-Phenyl



621
1
CH2Ph
2,6-di-iPr-Phenyl



622
2
CH2Ph
2,6-di-iPr-Phenyl



623
3
CH2Ph
2,6-di-iPr-Phenyl



624
3
CH2Ph
2,6-di-iPr-Phenyl



625
1
COMe
2,6-di-iPr-Phenyl



626
2
COMe
2,6-di-iPr-Phenyl



627
3
COMe
2,6-di-iPr-Phenyl



628
4
COMe
2,6-di-iPr-Phenyl



629
1
CO2Me
2,6-di-iPr-Phenyl



630
2
CO2Me
2,6-di-iPr-Phenyl



631
3
CO2Me
2,6-di-iPr-Phenyl



632
4
CO2Me
2,6-di-iPr-Phenyl



633
1
CO2tBu
2,6-di-iPr-Phenyl



634
2
CO2tBu
2,6-di-iPr-Phenyl



635
3
CO2tBu
2,6-di-iPr-Phenyl



636
4
CO2tBu
2,6-di-iPr-Phenyl



637
1
CONHMe
2,6-di-iPr-Phenyl



638
2
CONHMe
2,6-di-iPr-Phenyl



639
3
CONHMe
2,6-di-iPr-Phenyl



640
4
CONHMe
2,6-di-iPr-Phenyl



641
1
SO2Me
2,6-di-iPr-Phenyl



642
2
SO2Me
2,6-di-iPr-Phenyl



643
3
SO2Me
2,6-di-iPr-Phenyl



644
4
SO2Me
2,6-di-iPr-Phenyl



645
1
SO2NH2
2,6-di-iPr-Phenyl



646
2
SO2NH2
2,6-di-iPr-Phenyl



647
3
SO2NH2
2,6-di-iPr-Phenyl



648
4
SO2NH2
2,6-di-iPr-Phenyl



649
1
H
3-Ph-Phenyl



650
2
H
3-Ph-Phenyl



651
3
H
3-Ph-Phenyl



652
4
H
3-Ph-Phenyl



653
1
Me
3-Ph-Phenyl



654
2
Me
3-Ph-Phenyl



655
3
Me
3-Ph-Phenyl



656
4
Me
3-Ph-Phenyl



657
1
CH2Ph
3-Ph-Phenyl



658
2
CH2Ph
3-Ph-Phenyl



659
3
CH2Ph
3-Ph-Phenyl



660
4
CH2Ph
3-Ph-Phenyl



661
1
COMe
3-Ph-Phenyl



662
2
COMe
3-Ph-Phenyl



663
3
COMe
3-Ph-Phenyl



664
4
COMe
3-Ph-Phenyl



665
1
CO2Me
3-Ph-Phenyl



666
2
CO2Me
3-Ph-Phenyl



667
3
CO2Me
3-Ph-Phenyl



668
4
CO2Me
3-Ph-Phenyl



669
1
CO2tBu
3-Ph-Phenyl



670
2
CO2tBu
3-Ph-Phenyl



671
3
CO2tBu
3-Ph-Phenyl



672
4
CO2tBu
3-Ph-Phenyl



673
1
CONHMe
3-Ph-Phenyl



674
2
CONHMe
3-Ph-Phenyl



675
3
CONHMe
3-Ph-Phenyl



676
4
CONHMe
3-Ph-Phenyl



677
1
SO2Me
3-Ph-Phenyl



678
2
SO2Me
3-Ph-Phenyl



679
3
SO2Me
3-Ph-Phenyl



680
4
SO2Me
3-Ph-Phenyl



681
1
SO2NH2
3-Ph-Phenyl



682
2
SO2NH2
3-Ph-Phenyl



683
3
SO2NH2
3-Ph-Phenyl



684
4
SO2NH2
3-Ph-Phenyl



685
1
H
2-morpholino-phenyl



686
2
H
2-morpholino-phenyl



687
3
H
2-morpholino-phenyl



688
4
H
2-morpholino-phenyl



689
1
Me
2-morpholino-phenyl



690
2
Me
2-morpholino-phenyl



691
3
Me
2-morpholino-phenyl



692
4
Me
2-morpholino-phenyl



693
1
CH2Ph
2-morpholino-phenyl



694
2
CH2Ph
2-morpholino-phenyl



695
3
CH2Ph
2-morpholino-phenyl



696
4
CH2Ph
2-morpholino-phenyl



697
1
COMe
2-morpholino-phenyl



698
2
COMe
2-morpholino-phenyl



699
3
COMe
2-morpholino-phenyl



700
4
COMe
2-morpholino-phenyl



701
1
CO2Me
2-morpholino-phenyl



702
2
CO2Me
2-morpholino-phenyl



703
3
CO2Me
2-morpholino-phenyl



704
4
CO2Me
2-morpholino-phenyl



705
1
CO2tBu
2-morpholino-phenyl



706
2
CO2tBu
2-morpholino-phenyl



707
3
CO2tBu
2-morpholino-phenyl



708
4
CO2tBu
2-morpholino-phenyl



709
1
CONHMe
2-morpholino-phenyl



710
2
CONHMe
2-morpholino-phenyl



711
3
CONHMe
2-morpholino-phenyl



712
4
CONHMe
2-morpholino-phenyl



713
1
SO2Me
2-morpholino-phenyl



714
2
SO2Me
2-morpholino-phenyl



715
3
SO2Me
2-morpholino-phenyl



716
4
SO2Me
2-morpholino-phenyl



717
1
SO2NH2
2-morpholino-phenyl



718
2
SO2NH2
2-morpholino-phenyl



719
3
SO2NH2
2-morpholino-phenyl



720
4
SO2NH2
2-morpholino-phenyl



721
1
H
4-morpholino-phenyl



722
2
H
4-morpholino-phenyl



723
3
H
4-morpholino-phenyl



724
4
H
4-morpholino-phenyl



725
1
CH2Ph
4-morpholino-phenyl



726
2
CH2Ph
4-morpholino-phenyl



727
3
CH2Ph
4-morpholino-phenyl



728
4
CH2Ph
4-morpholino-phenyl



729
1
COMe
4-morpholino-phenyl



730
2
COMe
4-morpholino-phenyl



731
3
COMe
4-morpholino-phenyl



732
4
COMe
4-morpholino-phenyl



733
1
CO2Me
4-morpholino-phenyl



734
2
CO2Me
4-morpholino-phenyl



735
3
CO2Me
4-morpholino-phenyl



736
4
CO2Me
4-morpholino-phenyl



737
1
CO2tBu
4-morpholino-phenyl



738
2
CO2tBu
4-morpholino-phenyl



739
3
CO2tBu
4-morpholino-phenyl



740
1
H
naphthylen-1-yl



741
2
H
naphthylen-1-yl



742
3
H
naphthylen-1-yl



743
4
H
naphthylen-1-yl



744
1
Me
naphthylen-1-yl



745
2
Me
naphthylen-1-yl



746
3
Me
naphthylen-1-yl



747
4
Me
naphthylen-1-yl



748
1
CH2Ph
naphthylen-1-yl



749
2
CH2Ph
naphthylen-1-yl



750
3
CH2Ph
naphthylen-1-yl



751
4
CH2Ph
naphthylen-1-yl



752
1
COMe
naphthylen-1-yl



753
2
COMe
naphthylen-1-yl



754
3
COMe
naphthylen-1-yl



755
4
COMe
naphthylen-1-yl



756
1
CO2Me
naphthylen-1-yl



757
2
CO2Me
naphthylen-1-yl



758
3
CO2Me
naphthylen-1-yl



759
4
CO2Me
naphthylen-1-yl



760
1
CO2tBu
naphthylen-1-yl



761
2
CO2tBu
naphthylen-1-yl



762
3
CO2tBu
naphthylen-1-yl



763
4
CO2tBu
naphthylen-1-yl



764
1
CONHMe
naphthylen-1-yl



765
2
CONHMe
naphthylen-1-yl



767
3
CONHMe
naphthylen-1-yl



768
4
CONHMe
naphthylen-1-yl



769
1
SO2Me
naphthylen-1-yl



770
2
SO2Me
naphthylen-1-yl



771
3
SO2Me
naphthylen-1-yl



772
4
SO2Me
naphthylen-1-yl



773
1
SO2NH2
naphthylen-1-yl



774
2
SO2NH2
naphthylen-1-yl



775
3
SO2NH2
naphthylen-1-yl



778
4
SO2NH2
naphthylen-1-yl



779
1
H
4-OH-Phenyl



780
2
H
4-OH-Phenyl



781
3
H
4-OH-Phenyl



782
4
H
4-OH-Phenyl



783
1
Me
4-OH-Phenyl



784
2
Me
4-OH-Phenyl



785
3
Me
4-OH-Phenyl



786
4
Me
4-OH-Phenyl



787
1
CH2Ph
4-OH-Phenyl



788
2
CH2Ph
4-OH-Phenyl



789
3
CH2Ph
4-OH-Phenyl



790
4
CH2Ph
4-OH-Phenyl



791
1
COMe
4-OH-Phenyl



792
2
COMe
4-OH-Phenyl



793
3
COMe
4-OH-Phenyl



794
4
COMe
4-OH-Phenyl



795
1
CO2Me
4-OH-Phenyl



796
2
CO2Me
4-OH-Phenyl



797
3
CO2Me
4-OH-Phenyl



798
4
CO2Me
4-OH-Phenyl



799
1
CO2tBu
4-OH-Phenyl



800
2
CO2tBu
4-OH-Phenyl



801
3
CO2tBu
4-OH-Phenyl



802
4
CO2tBu
4-OH-Phenyl



803
1
CONHMe
4-OH-Phenyl



804
2
CONHMe
4-OH-Phenyl



805
3
CONHMe
4-OH-Phenyl



806
4
CONHMe
4-OH-Phenyl



807
1
SO2Me
4-OH-Phenyl



808
2
SO2Me
4-OH-Phenyl



809
3
SO2Me
4-OH-Phenyl



810
4
SO2Me
4-OH-Phenyl



811
1
SO2NH2
4-OH-Phenyl



812
2
SO2NH2
4-OH-Phenyl



813
3
SO2NH2
4-OH-Phenyl



814
4
SO2NH2
4-OH-Phenyl



815
1
H
2-OH-Phenyl



816
2
H
2-OH-Phenyl



817
3
H
2-OH-Phenyl



818
4
H
2-OH-Phenyl



819
1
Me
2-OH-Phenyl



820
2
Me
2-OH-Phenyl



821
3
Me
2-OH-Phenyl



822
4
Me
2-OH-Phenyl



823
1
CH2Ph
2-OH-Phenyl



824
2
CH2Ph
2-OH-Phenyl



825
3
CH2Ph
2-OH-Phenyl



826
4
CH2Ph
2-OH-Phenyl



827
1
COMe
2-OH-Phenyl



828
2
COMe
2-OH-Phenyl



829
3
COMe
2-OH-Phenyl



830
4
COMe
2-OH-Phenyl



831
1
CO2Me
2-OH-Phenyl



832
2
CO2Me
2-OH-Phenyl



833
3
CO2Me
2-OH-Phenyl



834
4
CO2Me
2-OH-Phenyl



835
1
CO2tBu
2-OH-Phenyl



836
2
CO2tBu
2-OH-Phenyl



837
3
CO2tBu
2-OH-Phenyl



838
4
CO2tBu
2-OH-Phenyl



839
1
CONHMe
2-OH-Phenyl



840
2
CONHMe
2-OH-Phenyl



841
3
CONHMe
2-OH-Phenyl



842
4
CONHMe
2-OH-Phenyl



843
1
SO2Me
2-OH-Phenyl



844
2
SO2Me
2-OH-Phenyl



845
3
SO2Me
2-OH-Phenyl



846
4
SO2Me
2-OH-Phenyl



847
1
SO2NH2
2-OH-Phenyl



848
2
SO2NH2
2-OH-Phenyl



849
3
SO2NH2
2-OH-Phenyl



850
4
SO2NH2
2-OH-Phenyl



851
1
H
4-OMe-Phenyl



852
2
H
4-OMe-Phenyl



853
3
H
4-OMe-Phenyl



854
4
H
4-OMe-Phenyl



855
1
Me
4-OMe-Phenyl



856
2
Me
4-OMe-Phenyl



857
3
Me
4-OMe-Phenyl



858
4
Me
4-OMe-Phenyl



859
1
CH2Ph
4-OMe-Phenyl



860
2
CH2Ph
4-OMe-Phenyl



861
3
CH2Ph
4-OMe-Phenyl



862
4
CH2Ph
4-OMe-Phenyl



863
1
COMe
4-OMe-Phenyl



864
2
COMe
4-OMe-Phenyl



865
3
COMe
4-OMe-Phenyl



866
4
COMe
4-OMe-Phenyl



867
1
CO2Me
4-OMe-Phenyl



868
2
CO2Me
4-OMe-Phenyl



869
3
CO2Me
4-OMe-Phenyl



870
4
CO2Me
4-OMe-Phenyl



871
1
CO2tBu
4-OMe-Phenyl



872
2
CO2tBu
4-OMe-Phenyl



873
3
CO2tBu
4-OMe-Phenyl



874
4
CO2tBu
4-OMe-Phenyl



875
1
CONHMe
4-OMe-Phenyl



876
2
CONHMe
4-OMe-Phenyl



877
3
CONHMe
4-OMe-Phenyl



878
4
CONHMe
4-OMe-Phenyl



879
1
SO2Me
4-OMe-Phenyl



880
2
SO2Me
4-OMe-Phenyl



881
3
SO2Me
4-OMe-Phenyl



882
4
SO2Me
4-OMe-Phenyl



883
1
SO2NH2
4-OMe-Phenyl



884
2
SO2NH2
4-OMe-Phenyl



885
3
SO2NH2
4-OMe-Phenyl



886
4
SO2NH2
4-OMe-Phenyl



887
1
H
2-OMe-Phenyl



888
2
H
2-OMe-Phenyl



889
3
H
2-OMe-Phenyl



890
4
H
2-OMe-Phenyl



891
1
Me
2-OMe-Phenyl



892
2
Me
2-OMe-Phenyl



893
3
Me
2-OMe-Phenyl



894
4
Me
2-OMe-Phenyl



895
1
CH2Ph
2-OMe-Phenyl



896
2
CH2Ph
2-OMe-Phenyl



897
3
CH2Ph
2-OMe-Phenyl



898
4
CH2Ph
2-OMe-Phenyl



899
1
COMe
2-OMe-Phenyl



900
2
COMe
2-OMe-Phenyl



901
3
COMe
2-OMe-Phenyl



902
4
COMe
2-OMe-Phenyl



903
1
CO2Me
2-OMe-Phenyl



904
2
CO2Me
2-OMe-Phenyl



905
3
CO2Me
2-OMe-Phenyl



906
4
CO2Me
2-OMe-Phenyl



907
1
CO2tBu
2-OMe-Phenyl



908
2
CO2tBu
2-OMe-Phenyl



909
3
CO2tBu
2-OMe-Phenyl



910
4
CO2tBu
2-OMe-Phenyl



911
1
CONHMe
2-OMe-Phenyl



912
2
CONHMe
2-OMe-Phenyl



913
3
CONHMe
2-OMe-Phenyl



914
4
CONHMe
2-OMe-Phenyl



915
1
SO2Me
2-OMe-Phenyl



916
2
SO2Me
2-OMe-Phenyl



917
3
SO2Me
2-OMe-Phenyl



918
4
SO2Me
2-OMe-Phenyl



919
1
SO2NH2
2-OMe-Phenyl



920
2
SO2NH2
2-OMe-Phenyl



921
3
SO2NH2
2-OMe-Phenyl



922
4
SO2NH2
2-OMe-Phenyl



923
1
H
3-CN-Phenyl



924
2
H
3-CN-Phenyl



925
3
H
3-CN-Phenyl



926
4
H
3-CN-Phenyl



927
1
Me
3-CN-Phenyl



928
2
Me
3-CN-Phenyl



929
3
Me
3-CN-Phenyl



930
4
Me
3-CN-Phenyl



931
1
CH2Ph
3-CN-Phenyl



932
2
CH2Ph
3-CN-Phenyl



933
3
CH2Ph
3-CN-Phenyl



934
4
CH2Ph
3-CN-Phenyl



935
1
COMe
3-CN-Phenyl



936
2
COMe
3-CN-Phenyl



937
3
COMe
3-CN-Phenyl



938
4
COMe
3-CN-Phenyl



939
1
CO2Me
3-CN-Phenyl



940
2
CO2Me
3-CN-Phenyl



941
3
CO2Me
3-CN-Phenyl



942
4
CO2Me
3-CN-Phenyl



943
1
CO2tBu
3-CN-Phenyl



944
2
CO2tBu
3-CN-Phenyl



945
3
CO2tBu
3-CN-Phenyl



946
4
CO2tBu
3-CN-Phenyl



947
1
CONHMe
3-CN-Phenyl



948
2
CONHMe
3-CN-Phenyl



949
3
CONHMe
3-CN-Phenyl



950
4
CONHMe
3-CN-Phenyl



951
1
SO2Me
3-CN-Phenyl



952
2
SO2Me
3-CN-Phenyl



953
3
SO2Me
3-CN-Phenyl



954
4
SO2Me
3-CN-Phenyl



955
1
SO2NH2
3-CN-Phenyl



956
2
SO2NH2
3-CN-Phenyl



957
3
SO2NH2
3-CN-Phenyl



958
4
SO2NH2
3-CN-Phenyl



959
1
H
2-Me-Phenyl



960
2
H
2-Me-Phenyl



961
3
H
2-Me-Phenyl



962
4
H
2-Me-Phenyl



963
1
Me
2-Me-Phenyl



964
2
Me
2-Me-Phenyl



965
3
Me
2-Me-Phenyl



966
4
Me
2-Me-Phenyl



967
1
CH2Ph
2-Me-Phenyl



968
2
CH2Ph
2-Me-Phenyl



969
3
CH2Ph
2-Me-Phenyl



970
4
CH2Ph
2-Me-Phenyl



971
1
COMe
2-Me-Phenyl



972
2
COMe
2-Me-Phenyl



973
3
COMe
2-Me-Phenyl



974
4
COMe
2-Me-Phenyl



975
1
CO2Me
2-Me-Phenyl



976
2
CO2Me
2-Me-Phenyl



977
3
CO2Me
2-Me-Phenyl



978
4
CO2Me
2-CN-Phenyl



979
1
CO2tBu
2-Me-Phenyl



980
2
CO2tBu
2-Me-Phenyl



981
3
CO2tBu
2-Me-Phenyl



982
4
CO2tBu
2-Me-Phenyl



983
1
CONHMe
2-Me-Phenyl



984
2
CONHMe
2-Me-Phenyl



985
3
CONHMe
2-Me-Phenyl



986
4
CONHMe
2-Me-Phenyl



987
1
SO2Me
2-Me-Phenyl



988
2
SO2Me
2-Me-Phenyl



989
3
SO2Me
2-Me-Phenyl



990
4
SO2Me
2-Me-Phenyl



991
1
SO2NH2
2-Me-Phenyl



992
2
SO2NH2
2-Me-Phenyl



993
3
SO2NH2
2-Me-Phenyl



994
4
SO2NH2
2-Me-Phenyl



995
1
H
4-Me-Phenyl



996
2
H
4-Me-Phenyl



997
3
H
4-Me-Phenyl



998
4
H
4-Me-Phenyl



999
1
Me
4-Me-Phenyl



1000
2
Me
4-Me-Phenyl



1001
3
Me
4-Me-Phenyl



1002
4
Me
4-Me-Phenyl



1003
1
CH2Ph
4-Me-Phenyl



1004
2
CH2Ph
4-Me-Phenyl



1005
3
CH2Ph
4-Me-Phenyl



1006
4
CH2Ph
4-Me-Phenyl



1007
1
COMe
4-Me-Phenyl



1008
2
COMe
4-Me-Phenyl



1009
3
COMe
4-Me-Phenyl



1010
4
COMe
4-Me-Phenyl



1011
1
CO2Me
4-Me-Phenyl



1012
2
CO2Me
4-Me-Phenyl



1013
3
CO2Me
4-Me-Phenyl



1014
4
CO2Me
4-Me-Phenyl



1015
1
CO2tBu
4-Me-Phenyl



1016
2
CO2tBu
4-Me-Phenyl



1017
3
CO2tBu
4-Me-Phenyl



1018
4
CO2tBu
4-Me-Phenyl



1019
1
CONHMe
4-Me-Phenyl



1020
2
CONHMe
4-Me-Phenyl



1021
3
CONHMe
4-Me-Phenyl



1022
4
CONHMe
4-Me-Phenyl



1023
1
SO2Me
4-Me-Phenyl



1024
2
SO2Me
4-Me-Phenyl



1025
3
SO2Me
4-Me-Phenyl



1026
4
SO2Me
4-Me-Phenyl



1027
1
SO2NH2
4-Me-Phenyl



1028
2
SO2NH2
4-Me-Phenyl



1029
3
SO2NH2
4-Me-Phenyl



1030
4
SO2NH2
4-Me-Phenyl



1031
1
H
3-F-Phenyl



1032
2
H
3-F-Phenyl



1033
3
H
3-F-Phenyl



1034
4
H
3-F-Phenyl



1035
1
Me
3-F-Phenyl



1036
2
Me
3-F-Phenyl



1037
3
Me
3-F-Phenyl



1038
4
Me
3-F-Phenyl



1039
1
CH2Ph
3-F-Phenyl



1040
2
CH2Ph
3-F-Phenyl



1041
3
CH2Ph
3-F-Phenyl



1042
4
CH2Ph
3-F-Phenyl



1043
1
COMe
3-F-Phenyl



1044
2
COMe
3-F-Phenyl



1045
3
COMe
3-F-Phenyl



1046
4
COMe
3-F-Phenyl



1047
1
CO2Me
3-F-Phenyl



1048
2
CO2Me
3-F-Phenyl



1049
3
CO2Me
3-F-Phenyl



1050
4
CO2Me
3-F-Phenyl



1051
1
CO2tBu
3-F-Phenyl



1052
2
CO2tBu
3-F-Phenyl



1053
3
CO2tBu
3-F-Phenyl



1054
4
CO2tBu
3-F-Phenyl



1055
1
CONHMe
3-F-Phenyl



1056
2
CONHMe
3-F-Phenyl



1057
3
CONHMe
3-F-Phenyl



1058
4
CONHMe
3-F-Phenyl



1059
1
SO2Me
3-F-Phenyl



1060
2
SO2Me
3-F-Phenyl



1061
3
SO2Me
3-F-Phenyl



1062
4
SO2Me
3-F-Phenyl



1063
1
SO2NH2
3-F-Phenyl



1064
2
SO2NH2
3-F-Phenyl



1065
3
SO2NH2
3-F-Phenyl



1066
4
SO2NH2
3-F-Phenyl



1067
1
H
2-Cl-Phenyl



1068
2
H
2-Cl-Phenyl



1069
3
H
2-Cl-Phenyl



1070
4
H
2-Cl-Phenyl



1071
1
Me
2-Cl-Phenyl



1072
2
Me
2-Cl-Phenyl



1073
3
Me
2-Cl-Phenyl



1074
4
Me
2-Cl-Phenyl



1075
1
CH2Ph
2-Cl-Phenyl



1076
2
CH2Ph
2-Cl-Phenyl



1077
3
CH2Ph
2-Cl-Phenyl



1078
4
CH2Ph
2-Cl-Phenyl



1079
1
COMe
2-Cl-Phenyl



1080
2
COMe
2-Cl-Phenyl



1081
3
COMe
2-Cl-Phenyl



1082
4
COMe
2-Cl-Phenyl



1083
1
CO2Me
2-Cl-Phenyl



1084
2
CO2Me
2-Cl-Phenyl



1085
3
CO2Me
2-Cl-Phenyl



1086
4
CO2Me
2-Cl-Phenyl



1087
1
CO2tBu
2-Cl-Phenyl



1088
2
CO2tBu
2-Cl-Phenyl



1089
3
CO2tBu
2-Cl-Phenyl



1090
4
CO2tBu
2-Cl-Phenyl



1091
1
CONHMe
2-Cl-Phenyl



1092
2
CONHMe
2-Cl-Phenyl



1093
3
CONHMe
2-Cl-Phenyl



1094
4
CONHMe
2-Cl-Phenyl



1095
1
SO2Me
2-Cl-Phenyl



1096
2
SO2Me
2-Cl-Phenyl



1097
3
SO2Me
2-Cl-Phenyl



1098
4
SO2Me
2-Cl-Phenyl



1099
1
SO2NH2
2-Cl-Phenyl



1100
2
SO2NH2
2-Cl-Phenyl



1101
3
SO2NH2
2-Cl-Phenyl



1102
4
SO2NH2
2-Cl-Phenyl



1103
1
H
4-Cl-Phenyl



1104
2
H
4-Cl-Phenyl



1105
3
H
4-Cl-Phenyl



1106
4
H
4-Cl-Phenyl



1107
1
Me
4-Cl-Phenyl



1108
2
Me
4-Cl-Phenyl



1109
3
Me
4-Cl-Phenyl



1110
4
Me
4-Cl-Phenyl



1111
1
CH2Ph
4-Cl-Phenyl



1112
2
CH2Ph
4-Cl-Phenyl



1113
3
CH2Ph
4-Cl-Phenyl



1114
4
CH2Ph
4-Cl-Phenyl



1115
1
COMe
4-Cl-Phenyl



1116
2
COMe
4-Cl-Phenyl



1117
3
COMe
4-Cl-Phenyl



1118
4
COMe
4-Cl-Phenyl



1119
1
CO2Me
4-Cl-Phenyl



1120
2
CO2Me
4-Cl-Phenyl



1121
3
CO2Me
4-Cl-Phenyl



1122
4
CO2Me
4-Cl-Phenyl



1123
1
CO2tBu
4-Cl-Phenyl



1124
2
CO2tBu
4-Cl-Phenyl



1125
3
CO2tBu
4-Cl-Phenyl



1126
4
CO2tBu
4-Cl-Phenyl



1127
1
CONHMe
4-Cl-Phenyl



1128
2
CONHMe
4-Cl-Phenyl



1129
3
CONHMe
4-Cl-Phenyl



1130
4
CONHMe
4-Cl-Phenyl



1131
1
SO2Me
4-Cl-Phenyl



1132
2
SO2Me
4-Cl-Phenyl



1133
3
SO2Me
4-Cl-Phenyl



1134
4
SO2Me
4-Cl-Phenyl



1135
1
SO2NH2
4-Cl-Phenyl



1136
2
SO2NH2
4-Cl-Phenyl



1137
3
SO2NH2
4-Cl-Phenyl



1138
4
SO2NH2
4-Cl-Phenyl



1139
1
H
3-Br-Phenyl



1140
2
H
3-Br-Phenyl



1141
3
H
3-Br-Phenyl



1142
4
H
3-Br-Phenyl



1143
1
Me
3-Br-Phenyl



1144
2
Me
3-Br-Phenyl



1145
3
Me
3-Br-Phenyl



1146
4
Me
3-Br-Phenyl



1147
1
CH2Ph
3-Br-Phenyl



1148
2
CH2Ph
3-Br-Phenyl



1149
3
CH2Ph
3-Br-Phenyl



1150
4
CH2Ph
3-Br-Phenyl



1151
1
COMe
3-Br-Phenyl



1152
2
COMe
3-Br-Phenyl



1153
3
COMe
3-Br-Phenyl



1154
4
COMe
3-Br-Phenyl



1155
1
CO2Me
3-Br-Phenyl



1156
2
CO2Me
3-Br-Phenyl



1157
3
CO2Me
3-Br-Phenyl



1158
4
CO2Me
3-Br-Phenyl



1159
1
CO2tBu
3-Br-Phenyl



1160
2
CO2tBu
3-Br-Phenyl



1161
3
CO2tBu
3-Br-Phenyl



1162
4
CO2tBu
3-Br-Phenyl



1163
1
CONHMe
3-Br-Phenyl



1164
2
CONHMe
3-Br-Phenyl



1165
3
CONHMe
3-Br-Phenyl



1166
4
CONHMe
3-Br-Phenyl



1167
1
SO2Me
3-Br-Phenyl



1168
2
SO2Me
3-Br-Phenyl



1169
3
SO2Me
3-Br-Phenyl



1170
4
SO2Me
3-Br-Phenyl



1171
1
SO2NH2
3-Br-Phenyl



1172
2
SO2NH2
3-Br-Phenyl



1173
3
SO2NH2
3-Br-Phenyl



1174
4
SO2NH2
3-Br-Phenyl



1175
1
H
2-CF3-Phenyl



1176
2
H
2-CF3-Phenyl



1177
3
H
2-CF3-Phenyl



1178
4
H
2-CF3-Phenyl



1179
1
Me
2-CF3-Phenyl



1180
2
Me
2-CF3-Phenyl



1181
3
Me
2-CF3-Phenyl



1182
4
Me
2-CF3-Phenyl



1183
1
CH2Ph
2-CF3-Phenyl



1184
2
CH2Ph
2-CF3-Phenyl



1185
3
CH2Ph
2-CF3-Phenyl



1186
4
CH2Ph
2-CF3-Phenyl



1187
1
COMe
2-CF3-Phenyl



1188
2
COMe
2-CF3-Phenyl



1189
3
COMe
2-CF3-Phenyl



1190
4
COMe
2-CF3-Phenyl



1191
1
CO2Me
2-CF3-Phenyl



1192
2
CO2Me
2-CF3-Phenyl



1193
3
CO2Me
2-CF3-Phenyl



1194
4
CO2Me
2-CF3-Phenyl



1195
1
CO2tBu
2-CF3-Phenyl



1196
2
CO2tBu
2-CF3-Phenyl



1197
3
CO2tBu
2-CF3-Phenyl



1198
4
CO2tBu
2-CF3-Phenyl



1199
1
CONHMe
2-CF3-Phenyl



1200
2
CONHMe
2-CF3-Phenyl



1201
3
CONHMe
2-CF3-Phenyl



1202
4
CONHMe
2-CF3-Phenyl



1203
1
SO2Me
2-CF3-Phenyl



1204
2
SO2Me
2-CF3-Phenyl



1205
3
SO2Me
2-CF3-Phenyl



1206
4
SO2Me
2-CF3-Phenyl



1207
1
SO2NH2
2-CF3-Phenyl



1208
2
SO2NH2
2-CF3-Phenyl



1209
3
SO2NH2
2-CF3-Phenyl



1210
4
SO2NH2
2-CF3-Phenyl



1211
1
H
4-CF3-Phenyl



1212
2
H
4-CF3-Phenyl



1213
3
H
4-CF3-Phenyl



1214
4
H
4-CF3-Phenyl



1215
1
Me
4-CF3-Phenyl



1216
2
Me
4-CF3-Phenyl



1217
3
Me
4-CF3-Phenyl



1218
4
Me
4-CF3-Phenyl



1219
1
CH2Ph
4-CF3-Phenyl



1220
2
CH2Ph
4-CF3-Phenyl



1221
3
CH2Ph
4-CF3-Phenyl



1222
4
CH2Ph
4-CF3-Phenyl



1223
1
COMe
4-CF3-Phenyl



1224
2
COMe
4-CF3-Phenyl



1225
3
COMe
4-CF3-Phenyl



1226
4
COMe
4-CF3-Phenyl



1227
1
CO2Me
4-CF3-Phenyl



1228
2
CO2Me
4-CF3-Phenyl



1229
3
CO2Me
4-CF3-Phenyl



1230
4
CO2Me
4-CF3-Phenyl



1231
1
CO2tBu
4-CF3-Phenyl



1232
2
CO2tBu
4-CF3-Phenyl



1233
3
CO2tBu
4-CF3-Phenyl



1234
4
CO2tBu
4-CF3-Phenyl



1235
1
CONHMe
4-CF3-Phenyl



1236
2
CONHMe
4-CF3-Phenyl



1237
3
CONHMe
4-CF3-Phenyl



1238
4
CONHMe
4-CF3-Phenyl



1239
1
SO2Me
4-CF3-Phenyl



1240
2
SO2Me
4-CF3-Phenyl



1241
3
SO2Me
4-CF3-Phenyl



1242
4
SO2Me
4-CF3-Phenyl



1243
1
SO2NH2
4-CF3-Phenyl



1244
2
SO2NH2
4-CF3-Phenyl



1245
3
SO2NH2
4-CF3-Phenyl



1246
4
SO2NH2
4-CF3-Phenyl



1247
1
H
3-iPr-Phenyl



1248
2
H
3-iPr-Phenyl



1249
3
H
3-iPr-Phenyl



1250
4
H
3-iPr-Phenyl



1251
1
Me
3-iPr-Phenyl



1252
2
Me
3-iPr-Phenyl



1253
3
Me
3-iPr-Phenyl



1254
4
Me
3-iPr-Phenyl



1255
1
CH2Ph
3-iPr-Phenyl



1256
2
CH2Ph
3-iPr-Phenyl



1257
3
CH2Ph
3-iPr-Phenyl



1258
4
CH2Ph
3-iPr-Phenyl



1259
1
COMe
3-iPr-Phenyl



1260
2
COMe
3-iPr-Phenyl



1261
3
COMe
3-iPr-Phenyl



1262
4
COMe
3-iPr-Phenyl



1263
1
CO2Me
3-iPr-Phenyl



1264
2
CO2Me
3-iPr-Phenyl



1265
3
CO2Me
3-iPr-Phenyl



1266
4
CO2Me
3-iPr-Phenyl



1267
1
CO2tBu
3-iPr-Phenyl



1268
2
CO2tBu
3-iPr-Phenyl



1269
3
CO2tBu
3-iPr-Phenyl



1270
4
CO2tBu
3-iPr-Phenyl



1271
1
CONHMe
3-iPr-Phenyl



1272
2
CONHMe
3-iPr-Phenyl



1273
3
CONHMe
3-iPr-Phenyl



1274
4
CONHMe
3-iPr-Phenyl



1275
1
SO2Me
3-iPr-Phenyl



1276
2
SO2Me
3-iPr-Phenyl



1277
3
SO2Me
3-iPr-Phenyl



1278
4
SO2Me
3-iPr-Phenyl



1279
1
SO2NH2
3-iPr-Phenyl



1280
2
SO2NH2
3-iPr-Phenyl



1281
3
SO2NH2
3-iPr-Phenyl



1282
4
SO2NH2
3-iPr-Phenyl



1283
1
H
4-NH2-Phenyl



1284
2
H
4-NH2-Phenyl



1285
3
H
4-NH2-Phenyl



1286
4
H
4-NH2-Phenyl



1287
1
Me
4-NH2-Phenyl



1288
2
Me
4-NH2-Phenyl



1289
3
Me
4-NH2-Phenyl



1290
4
Me
4-NH2-Phenyl



1291
1
CH2Ph
4-NH2-Phenyl



1292
2
CH2Ph
4-NH2-Phenyl



1293
3
CH2Ph
4-NH2-Phenyl



1294
4
CH2Ph
4-NH2-Phenyl



1295
1
COMe
4-NH2-Phenyl



1296
2
COMe
4-NH2-Phenyl



1297
3
COMe
4-NH2-Phenyl



1298
4
COMe
4-NH2-Phenyl



1299
1
CO2Me
4-NH2-Phenyl



1300
2
CO2Me
4-NH2-Phenyl



1301
3
CO2Me
4-NH2-Phenyl



1302
4
CO2Me
4-NH2-Phenyl



1303
1
CO2tBu
4-NH2-Phenyl



1304
2
CO2tBu
4-NH2-Phenyl



1305
3
CO2tBu
4-NH2-Phenyl



1306
4
CO2tBu
4-NH2-Phenyl



1307
1
CONHMe
4-NH2-Phenyl



1308
2
CONHMe
4-NH2-Phenyl



1309
3
CONHMe
4-NH2-Phenyl



1310
4
CONHMe
4-NH2-Phenyl



1311
1
SO2Me
4-NH2-Phenyl



1312
2
SO2Me
4-NH2-Phenyl



1313
3
SO2Me
4-NH2-Phenyl



1314
4
SO2Me
4-NH2-Phenyl



1315
1
SO2NH2
4-NH2-Phenyl



1316
2
SO2NH2
4-NH2-Phenyl



1317
3
SO2NH2
4-NH2-Phenyl



1318
4
SO2NH2
4-NH2-Phenyl



1319
1
H
2-NH2-Phenyl



1320
2
H
2-NH2-Phenyl



1321
3
H
2-NH2-Phenyl



1322
4
H
2-NH2-Phenyl



1323
1
Me
2-NH2-Phenyl



1324
2
Me
2-NH2-Phenyl



1325
3
Me
2-NH2-Phenyl



1326
4
Me
2-NH2-Phenyl



1327
1
CH2Ph
2-NH2-Phenyl



1328
2
CH2Ph
2-NH2-Phenyl



1329
3
CH2Ph
2-NH2-Phenyl



1330
4
CH2Ph
2-NH2-Phenyl



1331
1
COMe
2-NH2-Phenyl



1332
2
COMe
2-NH2-Phenyl



1333
3
COMe
2-NH2-Phenyl



1334
4
COMe
2-NH2-Phenyl



1335
1
CO2Me
2-NH2-Phenyl



1336
2
CO2Me
2-NH2-Phenyl



1337
3
CO2Me
2-NH2-Phenyl



1338
4
CO2Me
2-NH2-Phenyl



1339
1
CO2tBu
2-NH2-Phenyl



1340
2
CO2tBu
2-NH2-Phenyl



1341
3
CO2tBu
2-NH2-Phenyl



1342
4
CO2tBu
2-NH2-Phenyl



1343
1
CONHMe
2-NH2-Phenyl



1344
2
CONHMe
2-NH2-Phenyl



1345
3
CONHMe
2-NH2-Phenyl



1346
4
CONHMe
2-NH2-Phenyl



1347
1
SO2Me
2-NH2-Phenyl



1348
2
SO2Me
2-NH2-Phenyl



1349
3
SO2Me
2-NH2-Phenyl



1350
4
SO2Me
2-NH2-Phenyl



1351
1
SO2NH2
2-NH2-Phenyl



1352
2
SO2NH2
2-NH2-Phenyl



1353
3
SO2NH2
2-NH2-Phenyl



1354
4
SO2NH2
2-NH2-Phenyl



1355
1
H
2,6-di-Me-Phenyl



1356
2
H
2,6-di-Me-Phenyl



1357
3
H
2,6-di-Me-Phenyl



1358
4
H
2,6-di-Me-Phenyl



1359
1
Me
2,6-di-Me-Phenyl



1360
2
Me
2,6-di-Me-Phenyl



1361
3
Me
2,6-di-Me-Phenyl



1362
4
Me
2,6-di-Me-Phenyl



1363
1
CH2Ph
2,6-di-Me-Phenyl



1364
2
CH2Ph
2,6-di-Me-Phenyl



1365
3
CH2Ph
2,6-di-Me-Phenyl



1366
4
CH2Ph
2,6-di-Me-Phenyl



1367
1
COMe
2,6-di-Me-Phenyl



1368
2
COMe
2,6-di-Me-Phenyl



1369
3
COMe
2,6-di-Me-Phenyl



1370
4
COMe
2,6-di-Me-Phenyl



1371
1
CO2Me
2,6-di-Me-Phenyl



1372
2
CO2Me
2,6-di-Me-Phenyl



1373
3
CO2Me
2,6-di-Me-Phenyl



1374
4
CO2Me
2,6-di-Me-Phenyl



1375
1
CO2tBu
2,6-di-Me-Phenyl



1376
2
CO2tBu
2,6-di-Me-Phenyl



1377
3
CO2tBu
2,6-di-Me-Phenyl



1378
4
CO2tBu
2,6-di-Me-Phenyl



1379
1
CONHMe
2,6-di-Me-Phenyl



1380
2
CONHMe
2,6-di-Me-Phenyl



1381
3
CONHMe
2,6-di-Me-Phenyl



1382
4
CONHMe
2,6-di-Me-Phenyl



1383
1
SO2Me
2,6-di-Me-Phenyl



1384
2
SO2Me
2,6-di-Me-Phenyl



1385
3
SO2Me
2,6-di-Me-Phenyl



1386
4
SO2Me
2,6-di-Me-Phenyl



1387
1
SO2NH2
2,6-di-Me-Phenyl



1388
2
SO2NH2
2,6-di-Me-Phenyl



1389
3
SO2NH2
2,6-di-Me-Phenyl



1390
4
SO2NH2
2,6-di-Me-Phenyl



1391
1
H
2-Ph-Phenyl



1392
2
H
2-Ph-Phenyl



1393
3
H
2-Ph-Phenyl



1394
4
H
2-Ph-Phenyl



1395
1
Me
2-Ph-Phenyl



1396
2
Me
2-Ph-Phenyl



1397
3
Me
2-Ph-Phenyl



1398
4
Me
2-Ph-Phenyl



1399
1
CH2Ph
2-Ph-Phenyl



1400
2
CH2Ph
2-Ph-Phenyl



1401
3
CH2Ph
2-Ph-Phenyl



1402
4
CH2Ph
2-Ph-Phenyl



1403
1
COMe
2-Ph-Phenyl



1404
2
COMe
2-Ph-Phenyl



1405
3
COMe
2-Ph-Phenyl



1406
4
COMe
2-Ph-Phenyl



1407
1
CO2Me
2-Ph-Phenyl



1408
2
CO2Me
2-Ph-Phenyl



1409
3
CO2Me
2-Ph-Phenyl



1410
4
CO2Me
2-Ph-Phenyl



1411
1
CO2tBu
2-Ph-Phenyl



1412
2
CO2tBu
2-Ph-Phenyl



1413
3
CO2tBu
2-Ph-Phenyl



1414
4
CO2tBu
2-Ph-Phenyl



1415
1
CONHMe
2-Ph-Phenyl



1416
2
CONHMe
2-Ph-Phenyl



1417
3
CONHMe
2-Ph-Phenyl



1418
4
CONHMe
2-Ph-Phenyl



1419
1
SO2Me
2-Ph-Phenyl



1420
2
SO2Me
2-Ph-Phenyl



1421
3
SO2Me
2-Ph-Phenyl



1422
4
SO2Me
2-Ph-Phenyl



1423
1
SO2NH2
2-Ph-Phenyl



1424
2
SO2NH2
2-Ph-Phenyl



1425
3
SO2NH2
2-Ph-Phenyl



1426
4
SO2NH2
2-Ph-Phenyl



1427
1
H
4-Ph-Phenyl



1428
2
H
4-Ph-Phenyl



1429
3
H
4-Ph-Phenyl



1430
4
H
4-Ph-Phenyl



1431
1
Me
4-Ph-Phenyl



1432
2
Me
4-Ph-Phenyl



1433
3
Me
4-Ph-Phenyl



1434
4
Me
4-Ph-Phenyl



1435
1
CH2Ph
4-Ph-Phenyl



1436
2
CH2Ph
4-Ph-Phenyl



1437
3
CH2Ph
4-Ph-Phenyl



1438
4
CH2Ph
4-Ph-Phenyl



1439
1
COMe
4-Ph-Phenyl



1440
2
COMe
4-Ph-Phenyl



1441
3
COMe
4-Ph-Phenyl



1442
4
COMe
4-Ph-Phenyl



1443
1
CO2Me
4-Ph-Phenyl



1444
2
CO2Me
4-Ph-Phenyl



1445
3
CO2Me
4-Ph-Phenyl



1446
4
CO2Me
4-Ph-Phenyl



1447
1
CO2tBu
4-Ph-Phenyl



1448
2
CO2tBu
4-Ph-Phenyl



1449
3
CO2tBu
4-Ph-Phenyl



1450
4
CO2tBu
4-Ph-Phenyl



1451
1
CONHMe
4-Ph-Phenyl



1452
2
CONHMe
4-Ph-Phenyl



1453
3
CONHMe
4-Ph-Phenyl



1454
4
CONHMe
4-Ph-Phenyl



1455
1
SO2Me
4-Ph-Phenyl



1456
2
SO2Me
4-Ph-Phenyl



1457
3
SO2Me
4-Ph-Phenyl



1458
4
SO2Me
4-Ph-Phenyl



1459
1
SO2NH2
4-Ph-Phenyl



1460
2
SO2NH2
4-Ph-Phenyl



1461
3
SO2NH2
4-Ph-Phenyl



1462
4
SO2NH2
4-Ph-Phenyl



1463
1
H
3-morpholino-phenyl



1464
2
H
3-morpholino-phenyl



1465
3
H
3-morpholino-phenyl



1466
4
H
3-morpholino-phenyl



1467
1
Me
3-morpholino-phenyl



1468
2
Me
3-morpholino-phenyl



1469
3
Me
3-morpholino-phenyl



1470
4
Me
3-morpholino-phenyl



1471
1
CH2Ph
3-morpholino-phenyl



1472
2
CH2Ph
3-morpholino-phenyl



1473
3
CH2Ph
3-morpholino-phenyl



1474
4
CH2Ph
3-morpholino-phenyl



1475
1
COMe
3-morpholino-phenyl



1476
2
COMe
3-morpholino-phenyl



1477
3
COMe
3-morpholino-phenyl



1478
4
COMe
3-morpholino-phenyl



1479
1
CO2Me
3-morpholino-phenyl



1480
2
CO2Me
3-morpholino-phenyl



1481
3
CO2Me
3-morpholino-phenyl



1482
4
CO2Me
3-morpholino-phenyl



1483
1
CO2tBu
3-morpholino-phenyl



1484
2
CO2tBu
3-morpholino-phenyl



1485
3
CO2tBu
3-morpholino-phenyl



1486
4
CO2tBu
3-morpholino-phenyl



1487
1
CONHMe
3-morpholino-phenyl



1488
2
CONHMe
3-morpholino-phenyl



1489
3
CONHMe
3-morpholino-phenyl



1490
4
CONHMe
3-morpholino-phenyl



1491
1
SO2Me
3-morpholino-phenyl



1492
2
SO2Me
3-morpholino-phenyl



1493
3
SO2Me
3-morpholino-phenyl



1494
4
SO2Me
3-morpholino-phenyl



1495
1
SO2NH2
3-morpholino-phenyl



1496
2
SO2NH2
3-morpholino-phenyl



1497
3
SO2NH2
3-morpholino-phenyl



1498
4
SO2NH2
3-morpholino-phenyl



1499
1
Me
4-morpholino-phenyl



1500
2
Me
4-morpholino-phenyl



1501
3
Me
4-morpholino-phenyl



1502
4
Me
4-morpholino-phenyl



103
1
COMe
4-morpholino-phenyl



1504
2
COMe
4-morpholino-phenyl



1505
3
COMe
4-morpholino-phenyl



1506
4
COMe
4-morpholino-phenyl



1507
1
CO2tBu
4-morpholino-phenyl



1508
2
CO2tBu
4-morpholino-phenyl



1509
3
CO2tBu
4-morpholino-phenyl



1510
4
CO2tBu
4-morpholino-phenyl



1511
1
SO2Me
4-morpholino-phenyl



1512
2
SO2Me
4-morpholino-phenyl



1513
3
SO2Me
4-morpholino-phenyl



1514
4
SO2Me
4-morpholino-phenyl



1516
1
H
naphthylen-2-yl



1517
2
H
naphthylen-2-yl



1518
3
H
naphthylen-2-yl



1519
4
H
naphthylen-2-yl



1520
1
Me
naphthylen-2-yl



1521
2
Me
naphthylen-2-yl



1522
3
Me
naphthylen-2-yl



1523
4
Me
naphthylen-2-yl



1524
1
CH2Ph
naphthylen-2-yl



1525
2
CH2Ph
naphthylen-2-yl



1526
3
CH2Ph
naphthylen-2-yl



1527
4
CH2Ph
naphthylen-2-yl



1528
1
COMe
naphthylen-2-yl



1529
2
COMe
naphthylen-2-yl



1530
3
COMe
naphthylen-2-yl



1531
4
COMe
naphthylen-2-yl



1532
1
CO2Me
naphthylen-2-yl



1533
2
CO2Me
naphthylen-2-yl



1534
3
CO2Me
naphthylen-2-yl



1535
4
CO2Me
naphthylen-2-yl



1536
1
CO2tBu
naphthylen-2-yl



1537
2
CO2tBu
naphthylen-2-yl



1538
3
CO2tBu
naphthylen-2-yl



1539
4
CO2tBu
naphthylen-2-yl



1540
1
CONHMe
naphthylen-2-yl



1541
2
CONHMe
naphthylen-2-yl



1542
3
CONHMe
naphthylen-2-yl



1543
4
CONHMe
naphthylen-2-yl



1544
1
SO2Me
naphthylen-2-yl



1545
2
SO2Me
naphthylen-2-yl



1546
3
SO2Me
naphthylen-2-yl



1547
4
SO2Me
naphthylen-2-yl



1548
1
SO2NH2
naphthylen-2-yl



1549
2
SO2NH2
naphthylen-2-yl



1550
3
SO2NH2
naphthylen-2-yl



1551
4
SO2NH2
naphthylen-2-yl










Exemplary embodiments include compounds having the formula (XXIII)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 17.














TABLE 17







Entry
n
R7
R3





















1
1
H
Phenyl



2
2
H
Phenyl



3
3
H
Phenyl



4
4
H
Phenyl



5
1
Me
Phenyl



6
2
Me
Phenyl



7
3
Me
Phenyl



8
4
Me
Phenyl



9
1
CH2Ph
Phenyl



10
2
CH2Ph
Phenyl



11
3
CH2Ph
Phenyl



12
4
CH2Ph
Phenyl



13
1
COMe
Phenyl



14
2
COMe
Phenyl



15
3
COMe
Phenyl



16
4
COMe
Phenyl



17
1
CO2Me
Phenyl



18
2
CO2Me
Phenyl



19
3
CO2Me
Phenyl



20
4
CO2Me
Phenyl



21
1
CO2tBu
Phenyl



22
2
CO2tBu
Phenyl



23
3
CO2tBu
Phenyl



24
4
CO2tBu
Phenyl



25
1
CONHMe
Phenyl



26
2
CONHMe
Phenyl



27
3
CONHMe
Phenyl



28
4
CONHMe
Phenyl



29
1
SO2Me
Phenyl



30
2
SO2Me
Phenyl



31
3
SO2Me
Phenyl



32
4
SO2Me
Phenyl



33
1
SO2NH2
Phenyl



34
2
SO2NH2
Phenyl



35
3
SO2NH2
Phenyl



36
4
SO2NH2
Phenyl



37
1
H
3-OH-Phenyl



38
2
H
3-OH-Phenyl



39
3
H
3-OH-Phenyl



40
4
H
3-OH-Phenyl



41
1
Me
3-OH-Phenyl



42
2
Me
3-OH-Phenyl



43
3
Me
3-OH-Phenyl



44
4
Me
3-OH-Phenyl



45
1
CH2Ph
3-OH-Phenyl



46
2
CH2Ph
3-OH-Phenyl



47
3
CH2Ph
3-OH-Phenyl



48
4
CH2Ph
3-OH-Phenyl



49
1
COMe
3-OH-Phenyl



50
2
COMe
3-OH-Phenyl



51
3
COMe
3-OH-Phenyl



52
4
COMe
3-OH-Phenyl



53
1
CO2Me
3-OH-Phenyl



54
2
CO2Me
3-OH-Phenyl



55
3
CO2Me
3-OH-Phenyl



56
4
CO2Me
3-OH-Phenyl



57
1
CO2tBu
3-OH-Phenyl



58
2
CO2tBu
3-OH-Phenyl



59
3
CO2tBu
3-OH-Phenyl



60
4
CO2tBu
3-OH-Phenyl



61
1
CONHMe
3-OH-Phenyl



62
2
CONHMe
3-OH-Phenyl



63
3
CONHMe
3-OH-Phenyl



64
4
CONHMe
3-OH-Phenyl



65
1
SO2Me
3-OH-Phenyl



66
2
SO2Me
3-OH-Phenyl



67
3
SO2Me
3-OH-Phenyl



68
4
SO2Me
3-OH-Phenyl



69
1
SO2NH2
3-OH-Phenyl



70
2
SO2NH2
3-OH-Phenyl



71
3
SO2NH2
3-OH-Phenyl



72
4
SO2NH2
3-OH-Phenyl



73
1
H
4-NO2-Phenyl



74
2
H
4-NO2-Phenyl



75
3
H
4-NO2-Phenyl



76
4
H
4-NO2-Phenyl



77
1
Me
4-NO2-Phenyl



78
2
Me
4-NO2-Phenyl



79
3
Me
4-NO2-Phenyl



80
4
Me
4-NO2-Phenyl



81
1
CH2Ph
4-NO2-Phenyl



82
2
CH2Ph
4-NO2-Phenyl



83
3
CH2Ph
4-NO2-Phenyl



84
4
CH2Ph
4-NO2-Phenyl



85
1
COMe
4-NO2-Phenyl



86
2
COMe
4-NO2-Phenyl



87
3
COMe
4-NO2-Phenyl



88
4
COMe
4-NO2-Phenyl



89
1
CO2Me
4-NO2-Phenyl



90
2
CO2Me
4-NO2-Phenyl



91
3
CO2Me
4-NO2-Phenyl



92
4
CO2Me
4-NO2-Phenyl



93
1
CO2tBu
4-NO2-Phenyl



94
2
CO2tBu
4-NO2-Phenyl



95
3
CO2tBu
4-NO2-Phenyl



96
4
CO2tBu
4-NO2-Phenyl



97
1
CONHMe
4-NO2-Phenyl



98
2
CONHMe
4-NO2-Phenyl



99
3
CONHMe
4-NO2-Phenyl



100
4
CONHMe
4-NO2-Phenyl



101
1
SO2Me
4-NO2-Phenyl



102
2
SO2Me
4-NO2-Phenyl



103
3
SO2Me
4-NO2-Phenyl



104
4
SO2Me
4-NO2-Phenyl



105
1
SO2NH2
4-NO2-Phenyl



106
2
SO2NH2
4-NO2-Phenyl



107
3
SO2NH2
4-NO2-Phenyl



108
4
SO2NH2
4-NO2-Phenyl



109
1
H
3-OMe-Phenyl



110
2
H
3-OMe-Phenyl



111
3
H
3-OMe-Phenyl



112
4
H
3-OMe-Phenyl



113
1
Me
3-OMe-Phenyl



114
2
Me
3-OMe-Phenyl



115
3
Me
3-OMe-Phenyl



116
4
Me
3-OMe-Phenyl



117
1
CH2Ph
3-OMe-Phenyl



118
2
CH2Ph
3-OMe-Phenyl



119
3
CH2Ph
3-OMe-Phenyl



120
4
CH2Ph
3-OMe-Phenyl



121
1
COMe
3-OMe-Phenyl



122
2
COMe
3-OMe-Phenyl



123
3
COMe
3-OMe-Phenyl



124
4
COMe
3-OMe-Phenyl



125
1
CO2Me
3-OMe-Phenyl



126
2
CO2Me
3-OMe-Phenyl



127
3
CO2Me
3-OMe-Phenyl



128
4
CO2Me
3-OMe-Phenyl



129
1
CO2tBu
3-OMe-Phenyl



130
2
CO2tBu
3-OMe-Phenyl



131
3
CO2tBu
3-OMe-Phenyl



132
4
CO2tBu
3-OMe-Phenyl



133
1
CONHMe
3-OMe-Phenyl



134
2
CONHMe
3-OMe-Phenyl



135
3
CONHMe
3-OMe-Phenyl



136
4
CONHMe
3-OMe-Phenyl



137
1
SO2Me
3-OMe-Phenyl



138
2
SO2Me
3-OMe-Phenyl



139
3
SO2Me
3-OMe-Phenyl



140
4
SO2Me
3-OMe-Phenyl



141
1
SO2NH2
3-OMe-Phenyl



142
2
SO2NH2
3-OMe-Phenyl



143
3
SO2NH2
3-OMe-Phenyl



144
4
SO2NH2
3-OMe-Phenyl



145
1
H
4-CN-Phenyl



146
2
H
4-CN-Phenyl



147
3
H
4-CN-Phenyl



148
4
H
4-CN-Phenyl



149
1
Me
4-CN-Phenyl



150
2
Me
4-CN-Phenyl



151
3
Me
4-CN-Phenyl



152
4
Me
4-CN-Phenyl



153
1
CH2Ph
4-CN-Phenyl



154
2
CH2Ph
4-CN-Phenyl



155
3
CH2Ph
4-CN-Phenyl



156
4
CH2Ph
4-CN-Phenyl



157
1
COMe
4-CN-Phenyl



158
2
COMe
4-CN-Phenyl



159
3
COMe
4-CN-Phenyl



160
4
COMe
4-CN-Phenyl



161
1
CO2Me
4-CN-Phenyl



162
2
CO2Me
4-CN-Phenyl



163
3
CO2Me
4-CN-Phenyl



164
4
CO2Me
4-CN-Phenyl



165
1
CO2tBu
4-CN-Phenyl



166
2
CO2tBu
4-CN-Phenyl



167
3
CO2tBu
4-CN-Phenyl



168
4
CO2tBu
4-CN-Phenyl



169
1
CONHMe
4-CN-Phenyl



170
2
CONHMe
4-CN-Phenyl



171
3
CONHMe
4-CN-Phenyl



172
4
CONHMe
4-CN-Phenyl



173
1
SO2Me
4-CN-Phenyl



174
2
SO2Me
4-CN-Phenyl



175
3
SO2Me
4-CN-Phenyl



176
4
SO2Me
4-CN-Phenyl



177
1
SO2NH2
4-CN-Phenyl



178
2
SO2NH2
4-CN-Phenyl



179
3
SO2NH2
4-CN-Phenyl



180
4
SO2NH2
4-CN-Phenyl



181
1
H
2-CN-Phenyl



182
2
H
2-CN-Phenyl



183
3
H
2-CN-Phenyl



184
4
H
2-CN-Phenyl



185
1
Me
2-CN-Phenyl



186
2
Me
2-CN-Phenyl



187
3
Me
2-CN-Phenyl



188
4
Me
2-CN-Phenyl



189
1
CH2Ph
2-CN-Phenyl



190
2
CH2Ph
2-CN-Phenyl



191
3
CH2Ph
2-CN-Phenyl



192
4
CH2Ph
2-CN-Phenyl



193
1
COMe
2-CN-Phenyl



194
2
COMe
2-CN-Phenyl



195
3
COMe
2-CN-Phenyl



196
4
COMe
2-CN-Phenyl



197
1
CO2Me
2-CN-Phenyl



198
2
CO2Me
2-CN-Phenyl



199
3
CO2Me
2-CN-Phenyl



200
4
CO2Me
2-CN-Phenyl



201
1
CO2tBu
2-CN-Phenyl



202
2
CO2tBu
2-CN-Phenyl



203
3
CO2tBu
2-CN-Phenyl



204
4
CO2tBu
2-CN-Phenyl



205
1
CONHMe
2-CN-Phenyl



206
2
CONHMe
2-CN-Phenyl



207
3
CONHMe
2-CN-Phenyl



208
4
CONHMe
2-CN-Phenyl



209
1
SO2Me
2-CN-Phenyl



210
2
SO2Me
2-CN-Phenyl



211
3
SO2Me
2-CN-Phenyl



212
4
SO2Me
2-CN-Phenyl



213
1
SO2NH2
2-CN-Phenyl



214
2
SO2NH2
2-CN-Phenyl



215
3
SO2NH2
2-CN-Phenyl



216
4
SO2NH2
2-CN-Phenyl



217
1
H
3-Me-Phenyl



218
2
H
3-Me-Phenyl



219
3
H
3-Me-Phenyl



220
4
H
3-Me-Phenyl



221
1
Me
3-Me-Phenyl



222
2
Me
3-Me-Phenyl



223
3
Me
3-Me-Phenyl



224
4
Me
3-Me-Phenyl



225
1
CH2Ph
3-Me-Phenyl



226
2
CH2Ph
3-Me-Phenyl



227
3
CH2Ph
3-Me-Phenyl



228
4
CH2Ph
3-Me-Phenyl



229
1
COMe
3-Me-Phenyl



230
2
COMe
3-Me-Phenyl



231
3
COMe
3-Me-Phenyl



232
4
COMe
3-Me-Phenyl



233
1
CO2Me
3-Me-Phenyl



234
2
CO2Me
3-Me-Phenyl



235
3
CO2Me
3-Me-Phenyl



236
4
CO2Me
3-Me-Phenyl



237
1
CO2tBu
3-Me-Phenyl



238
2
CO2tBu
3-Me-Phenyl



239
3
CO2tBu
3-Me-Phenyl



240
4
CO2tBu
3-Me-Phenyl



241
1
CONHMe
3-Me-Phenyl



242
2
CONHMe
3-Me-Phenyl



243
3
CONHMe
3-Me-Phenyl



244
4
CONHMe
3-Me-Phenyl



245
1
SO2Me
3-Me-Phenyl



246
2
SO2Me
3-Me-Phenyl



247
3
SO2Me
3-Me-Phenyl



248
4
SO2Me
3-Me-Phenyl



249
1
SO2NH2
3-Me-Phenyl



250
2
SO2NH2
3-Me-Phenyl



251
3
SO2NH2
3-Me-Phenyl



252
4
SO2NH2
3-Me-Phenyl



253
1
H
2-F-Phenyl



254
2
H
2-F-Phenyl



255
3
H
2-F-Phenyl



256
4
H
2-F-Phenyl



257
1
Me
2-F-Phenyl



258
2
Me
2-F-Phenyl



259
3
Me
2-F-Phenyl



260
4
Me
2-F-Phenyl



261
1
CH2Ph
2-F-Phenyl



262
2
CH2Ph
2-F-Phenyl



263
3
CH2Ph
2-F-Phenyl



264
4
CH2Ph
2-F-Phenyl



265
1
COMe
2-F-Phenyl



266
2
COMe
2-F-Phenyl



267
3
COMe
2-F-Phenyl



268
4
COMe
2-F-Phenyl



269
1
CO2Me
2-F-Phenyl



270
2
CO2Me
2-F-Phenyl



271
3
CO2Me
2-F-Phenyl



272
4
CO2Me
2-F-Phenyl



273
1
CO2tBu
2-F-Phenyl



274
2
CO2tBu
2-F-Phenyl



275
3
CO2tBu
2-F-Phenyl



276
4
CO2tBu
2-F-Phenyl



277
1
CONHMe
2-F-Phenyl



278
2
CONHMe
2-F-Phenyl



279
3
CONHMe
2-F-Phenyl



280
4
CONHMe
2-F-Phenyl



281
1
SO2Me
2-F-Phenyl



282
2
SO2Me
2-F-Phenyl



283
3
SO2Me
2-F-Phenyl



284
4
SO2Me
2-F-Phenyl



285
1
SO2NH2
2-F-Phenyl



286
2
SO2NH2
2-F-Phenyl



287
3
SO2NH2
2-F-Phenyl



288
4
SO2NH2
2-F-Phenyl



289
1
H
4-F-Phenyl



290
2
H
4-F-Phenyl



291
3
H
4-F-Phenyl



292
4
H
4-F-Phenyl



293
1
Me
4-F-Phenyl



294
2
Me
4-F-Phenyl



295
3
Me
4-F-Phenyl



296
4
Me
4-F-Phenyl



297
1
CH2Ph
4-F-Phenyl



298
2
CH2Ph
4-F-Phenyl



299
3
CH2Ph
4-F-Phenyl



300
4
CH2Ph
4-F-Phenyl



301
1
COMe
4-F-Phenyl



302
2
COMe
4-F-Phenyl



303
3
COMe
4-F-Phenyl



304
4
COMe
4-F-Phenyl



305
1
CO2Me
4-F-Phenyl



306
2
CO2Me
4-F-Phenyl



307
3
CO2Me
4-F-Phenyl



308
4
CO2Me
4-F-Phenyl



309
1
CO2tBu
4-F-Phenyl



310
2
CO2tBu
4-F-Phenyl



311
3
CO2tBu
4-F-Phenyl



312
4
CO2tBu
4-F-Phenyl



313
1
CONHMe
4-F-Phenyl



314
2
CONHMe
4-F-Phenyl



315
3
CONHMe
4-F-Phenyl



316
4
CONHMe
4-F-Phenyl



317
1
SO2Me
4-F-Phenyl



318
2
SO2Me
4-F-Phenyl



319
3
SO2Me
4-F-Phenyl



320
4
SO2Me
4-F-Phenyl



321
1
SO2NH2
4-F-Phenyl



322
2
SO2NH2
4-F-Phenyl



323
3
SO2NH2
4-F-Phenyl



324
4
SO2NH2
4-F-Phenyl



325
1
H
3-Cl-Phenyl



326
2
H
3-Cl-Phenyl



327
3
H
3-Cl-Phenyl



328
4
H
3-Cl-Phenyl



329
1
Me
3-Cl-Phenyl



330
2
Me
3-Cl-Phenyl



331
3
Me
3-Cl-Phenyl



332
4
Me
3-Cl-Phenyl



333
1
CH2Ph
3-Cl-Phenyl



334
2
CH2Ph
3-Cl-Phenyl



335
3
CH2Ph
3-Cl-Phenyl



336
4
CH2Ph
3-Cl-Phenyl



337
1
COMe
3-Cl-Phenyl



338
2
COMe
3-Cl-Phenyl



339
3
COMe
3-Cl-Phenyl



340
4
COMe
3-Cl-Phenyl



341
1
CO2Me
3-Cl-Phenyl



342
2
CO2Me
3-Cl-Phenyl



343
3
CO2Me
3-Cl-Phenyl



344
4
CO2Me
3-Cl-Phenyl



345
1
CO2tBu
3-Cl-Phenyl



346
2
CO2tBu
3-Cl-Phenyl



347
3
CO2tBu
3-Cl-Phenyl



348
4
CO2tBu
3-Cl-Phenyl



349
1
CONHMe
3-Cl-Phenyl



350
2
CONHMe
3-Cl-Phenyl



351
3
CONHMe
3-Cl-Phenyl



352
4
CONHMe
3-Cl-Phenyl



353
1
SO2Me
3-Cl-Phenyl



354
2
SO2Me
3-Cl-Phenyl



355
3
SO2Me
3-Cl-Phenyl



356
4
SO2Me
3-Cl-Phenyl



357
1
SO2NH2
3-Cl-Phenyl



358
2
SO2NH2
3-Cl-Phenyl



359
3
SO2NH2
3-Cl-Phenyl



360
4
SO2NH2
3-Cl-Phenyl



361
1
H
2-Br-Phenyl



362
2
H
2-Br-Phenyl



363
3
H
2-Br-Phenyl



364
4
H
2-Br-Phenyl



365
1
Me
2-Br-Phenyl



366
2
Me
2-Br-Phenyl



367
3
Me
2-Br-Phenyl



368
4
Me
2-Br-Phenyl



369
1
CH2Ph
2-Br-Phenyl



370
2
CH2Ph
2-Br-Phenyl



371
3
CH2Ph
2-Br-Phenyl



372
4
CH2Ph
2-Br-Phenyl



373
1
COMe
2-Br-Phenyl



374
2
COMe
2-Br-Phenyl



375
3
COMe
2-Br-Phenyl



376
4
COMe
2-Br-Phenyl



377
1
CO2Me
2-Br-Phenyl



378
2
CO2Me
2-Br-Phenyl



379
3
CO2Me
2-Br-Phenyl



380
4
CO2Me
2-Br-Phenyl



381
1
CO2tBu
2-Br-Phenyl



382
2
CO2tBu
2-Br-Phenyl



383
3
CO2tBu
2-Br-Phenyl



384
4
CO2tBu
2-Br-Phenyl



385
1
CONHMe
2-Br-Phenyl



386
2
CONHMe
2-Br-Phenyl



387
3
CONHMe
2-Br-Phenyl



388
4
CONHMe
2-Br-Phenyl



389
1
SO2Me
2-Br-Phenyl



390
2
SO2Me
2-Br-Phenyl



391
3
SO2Me
2-Br-Phenyl



392
4
SO2Me
2-Br-Phenyl



393
1
SO2NH2
2-Br-Phenyl



394
2
SO2NH2
2-Br-Phenyl



395
3
SO2NH2
2-Br-Phenyl



396
4
SO2NH2
2-Br-Phenyl



397
1
H
4-Br-Phenyl



398
2
H
4-Br-Phenyl



399
3
H
4-Br-Phenyl



400
4
H
4-Br-Phenyl



401
1
Me
4-Br-Phenyl



402
2
Me
4-Br-Phenyl



403
3
Me
4-Br-Phenyl



404
4
Me
4-Br-Phenyl



405
1
CH2Ph
4-Br-Phenyl



406
2
CH2Ph
4-Br-Phenyl



407
3
CH2Ph
4-Br-Phenyl



408
4
CH2Ph
4-Br-Phenyl



409
1
COMe
4-Br-Phenyl



410
2
COMe
4-Br-Phenyl



411
3
COMe
4-Br-Phenyl



412
4
COMe
4-Br-Phenyl



413
1
CO2Me
4-Br-Phenyl



414
2
CO2Me
4-Br-Phenyl



415
3
CO2Me
4-Br-Phenyl



416
4
CO2Me
4-Br-Phenyl



417
1
CO2tBu
4-Br-Phenyl



418
2
CO2tBu
4-Br-Phenyl



419
3
CO2tBu
4-Br-Phenyl



420
4
CO2tBu
4-Br-Phenyl



421
1
CONHMe
4-Br-Phenyl



422
2
CONHMe
4-Br-Phenyl



423
3
CONHMe
4-Br-Phenyl



424
4
CONHMe
4-Br-Phenyl



425
1
SO2Me
4-Br-Phenyl



426
2
SO2Me
4-Br-Phenyl



427
3
SO2Me
4-Br-Phenyl



428
4
SO2Me
4-Br-Phenyl



429
1
SO2NH2
4-Br-Phenyl



430
2
SO2NH2
4-Br-Phenyl



431
3
SO2NH2
4-Br-Phenyl



432
4
SO2NH2
4-Br-Phenyl



433
1
H
3-CF3-Phenyl



434
2
H
3-CF3-Phenyl



435
3
H
3-CF3-Phenyl



436
4
H
3-CF3-Phenyl



437
1
Me
3-CF3-Phenyl



438
2
Me
3-CF3-Phenyl



439
3
Me
3-CF3-Phenyl



440
4
Me
3-CF3-Phenyl



441
1
CH2Ph
3-CF3-Phenyl



442
2
CH2Ph
3-CF3-Phenyl



443
3
CH2Ph
3-CF3-Phenyl



444
4
CH2Ph
3-CF3-Phenyl



445
1
COMe
3-CF3-Phenyl



446
2
COMe
3-CF3-Phenyl



447
3
COMe
3-CF3-Phenyl



448
4
COMe
3-CF3-Phenyl



449
1
CO2Me
3-CF3-Phenyl



450
2
CO2Me
3-CF3-Phenyl



451
3
CO2Me
3-CF3-Phenyl



452
4
CO2Me
3-CF3-Phenyl



453
1
CO2tBu
3-CF3-Phenyl



454
2
CO2tBu
3-CF3-Phenyl



455
3
CO2tBu
3-CF3-Phenyl



456
4
CO2tBu
3-CF3-Phenyl



457
1
CONHMe
3-CF3-Phenyl



458
2
CONHMe
3-CF3-Phenyl



459
3
CONHMe
3-CF3-Phenyl



460
4
CONHMe
3-CF3-Phenyl



461
1
SO2Me
3-CF3-Phenyl



462
2
SO2Me
3-CF3-Phenyl



463
3
SO2Me
3-CF3-Phenyl



464
4
SO2Me
3-CF3-Phenyl



465
1
SO2NH2
3-CF3-Phenyl



466
2
SO2NH2
3-CF3-Phenyl



467
3
SO2NH2
3-CF3-Phenyl



468
4
SO2NH2
3-CF3-Phenyl



469
1
H
2-iPr-Phenyl



470
2
H
2-iPr-Phenyl



471
3
H
2-iPr-Phenyl



472
4
H
2-iPr-Phenyl



473
1
Me
2-iPr-Phenyl



474
2
Me
2-iPr-Phenyl



475
3
Me
2-iPr-Phenyl



476
4
Me
2-iPr-Phenyl



477
1
CH2Ph
2-iPr-Phenyl



478
2
CH2Ph
2-iPr-Phenyl



479
3
CH2Ph
2-iPr-Phenyl



480
4
CH2Ph
2-iPr-Phenyl



481
1
COMe
2-iPr-Phenyl



482
2
COMe
2-iPr-Phenyl



483
3
COMe
2-iPr-Phenyl



484
4
COMe
2-iPr-Phenyl



485
1
CO2Me
2-iPr-Phenyl



486
2
CO2Me
2-iPr-Phenyl



487
3
CO2Me
2-iPr-Phenyl



488
4
CO2Me
2-iPr-Phenyl



489
1
CO2tBu
2-iPr-Phenyl



490
2
CO2tBu
2-iPr-Phenyl



491
3
CO2tBu
2-iPr-Phenyl



492
4
CO2tBu
2-iPr-Phenyl



493
1
CONHMe
2-iPr-Phenyl



494
2
CONHMe
2-iPr-Phenyl



495
3
CONHMe
2-iPr-Phenyl



496
4
CONHMe
2-iPr-Phenyl



497
1
SO2Me
2-iPr-Phenyl



498
2
SO2Me
2-iPr-Phenyl



499
3
SO2Me
2-iPr-Phenyl



500
4
SO2Me
2-iPr-Phenyl



501
1
SO2NH2
2-iPr-Phenyl



502
2
SO2NH2
2-iPr-Phenyl



503
3
SO2NH2
2-iPr-Phenyl



504
4
SO2NH2
2-iPr-Phenyl



505
1
H
4-iPr-Phenyl



506
2
H
4-iPr-Phenyl



507
3
H
4-iPr-Phenyl



508
4
H
4-iPr-Phenyl



509
1
Me
4-iPr-Phenyl



510
2
Me
4-iPr-Phenyl



511
3
Me
4-iPr-Phenyl



512
4
Me
4-iPr-Phenyl



513
1
CH2Ph
4-iPr-Phenyl



514
2
CH2Ph
4-iPr-Phenyl



515
3
CH2Ph
4-iPr-Phenyl



516
4
CH2Ph
4-iPr-Phenyl



517
1
COMe
4-iPr-Phenyl



518
2
COMe
4-iPr-Phenyl



519
3
COMe
4-iPr-Phenyl



520
4
COMe
4-iPr-Phenyl



521
1
CO2Me
4-iPr-Phenyl



522
2
CO2Me
4-iPr-Phenyl



523
3
CO2Me
4-iPr-Phenyl



524
4
CO2Me
4-iPr-Phenyl



525
1
CO2tBu
4-iPr-Phenyl



526
2
CO2tBu
4-iPr-Phenyl



527
3
CO2tBu
4-iPr-Phenyl



528
4
CO2tBu
4-iPr-Phenyl



529
1
CONHMe
4-iPr-Phenyl



530
2
CONHMe
4-iPr-Phenyl



531
3
CONHMe
4-iPr-Phenyl



532
4
CONHMe
4-iPr-Phenyl



533
1
SO2Me
4-iPr-Phenyl



534
2
SO2Me
4-iPr-Phenyl



535
3
SO2Me
4-iPr-Phenyl



536
4
SO2Me
4-iPr-Phenyl



537
1
SO2NH2
4-iPr-Phenyl



538
2
SO2NH2
4-iPr-Phenyl



539
3
SO2NH2
4-iPr-Phenyl



540
4
SO2NH2
4-iPr-Phenyl



541
1
H
3-NH2-Phenyl



542
2
H
3-NH2-Phenyl



543
3
H
3-NH2-Phenyl



544
4
H
3-NH2-Phenyl



545
1
Me
3-NH2-Phenyl



546
2
Me
3-NH2-Phenyl



547
3
Me
3-NH2-Phenyl



548
4
Me
3-NH2-Phenyl



549
1
CH2Ph
3-NH2-Phenyl



550
2
CH2Ph
3-NH2-Phenyl



551
3
CH2Ph
3-NH2-Phenyl



552
4
CH2Ph
3-NH2-Phenyl



553
1
COMe
3-NH2-Phenyl



554
2
COMe
3-NH2-Phenyl



555
3
COMe
3-NH2-Phenyl



556
4
COMe
3-NH2-Phenyl



557
1
CO2Me
3-NH2-Phenyl



558
2
CO2Me
3-NH2-Phenyl



559
3
CO2Me
3-NH2-Phenyl



560
4
CO2Me
3-NH2-Phenyl



561
1
CO2tBu
3-NH2-Phenyl



562
2
CO2tBu
3-NH2-Phenyl



563
3
CO2tBu
3-NH2-Phenyl



564
4
CO2tBu
3-NH2-Phenyl



565
1
CONHMe
3-NH2-Phenyl



566
2
CONHMe
3-NH2-Phenyl



567
3
CONHMe
3-NH2-Phenyl



568
4
CONHMe
3-NH2-Phenyl



569
1
SO2Me
3-NH2-Phenyl



570
2
SO2Me
3-NH2-Phenyl



571
3
SO2Me
3-NH2-Phenyl



572
4
SO2Me
3-NH2-Phenyl



573
1
SO2NH2
3-NH2-Phenyl



574
2
SO2NH2
3-NH2-Phenyl



575
3
SO2NH2
3-NH2-Phenyl



576
4
SO2NH2
3-NH2-Phenyl



577
1
H
2,4-di-Me-Phenyl



578
2
H
2,4-di-Me-Phenyl



579
3
H
2,4-di-Me-Phenyl



580
4
H
2,4-di-Me-Phenyl



581
1
Me
2,4-di-Me-Phenyl



582
2
Me
2,4-di-Me-Phenyl



583
3
Me
2,4-di-Me-Phenyl



584
4
Me
2,4-di-Me-Phenyl



585
1
CH2Ph
2,4-di-Me-Phenyl



586
2
CH2Ph
2,4-di-Me-Phenyl



587
3
CH2Ph
2,4-di-Me-Phenyl



588
4
CH2Ph
2,4-di-Me-Phenyl



589
1
COMe
2,4-di-Me-Phenyl



590
2
COMe
2,4-di-Me-Phenyl



591
3
COMe
2,4-di-Me-Phenyl



592
4
COMe
2,4-di-Me-Phenyl



593
1
CO2Me
2,4-di-Me-Phenyl



594
2
CO2Me
2,4-di-Me-Phenyl



595
3
CO2Me
2,4-di-Me-Phenyl



596
4
CO2Me
2,4-di-Me-Phenyl



597
1
CO2tBu
2,4-di-Me-Phenyl



598
2
CO2tBu
2,4-di-Me-Phenyl



599
3
CO2tBu
2,4-di-Me-Phenyl



600
4
CO2tBu
2,4-di-Me-Phenyl



601
1
CONHMe
2,4-di-Me-Phenyl



602
2
CONHMe
2,4-di-Me-Phenyl



603
3
CONHMe
2,4-di-Me-Phenyl



604
4
CONHMe
2,4-di-Me-Phenyl



605
1
SO2Me
2,4-di-Me-Phenyl



606
2
SO2Me
2,4-di-Me-Phenyl



607
3
SO2Me
2,4-di-Me-Phenyl



608
4
SO2Me
2,4-di-Me-Phenyl



609
1
SO2NH2
2,4-di-Me-Phenyl



610
2
SO2NH2
2,4-di-Me-Phenyl



611
3
SO2NH2
2,4-di-Me-Phenyl



612
4
SO2NH2
2,4-di-Me-Phenyl



613
1
H
2,6-di-iPr-Phenyl



614
2
H
2,6-di-iPr-Phenyl



615
3
H
2,6-di-iPr-Phenyl



616
4
H
2,6-di-iPr-Phenyl



617
1
Me
2,6-di-iPr-Phenyl



618
2
Me
2,6-di-iPr-Phenyl



619
3
Me
2,6-di-iPr-Phenyl



620
4
Me
2,6-di-iPr-Phenyl



621
1
CH2Ph
2,6-di-iPr-Phenyl



622
2
CH2Ph
2,6-di-iPr-Phenyl



623
3
CH2Ph
2,6-di-iPr-Phenyl



624
3
CH2Ph
2,6-di-iPr-Phenyl



625
1
COMe
2,6-di-iPr-Phenyl



626
2
COMe
2,6-di-iPr-Phenyl



627
3
COMe
2,6-di-iPr-Phenyl



628
4
COMe
2,6-di-iPr-Phenyl



629
1
CO2Me
2,6-di-iPr-Phenyl



630
2
CO2Me
2,6-di-iPr-Phenyl



631
3
CO2Me
2,6-di-iPr-Phenyl



632
4
CO2Me
2,6-di-iPr-Phenyl



633
1
CO2tBu
2,6-di-iPr-Phenyl



634
2
CO2tBu
2,6-di-iPr-Phenyl



635
3
CO2tBu
2,6-di-iPr-Phenyl



636
4
CO2tBu
2,6-di-iPr-Phenyl



637
1
CONHMe
2,6-di-iPr-Phenyl



638
2
CONHMe
2,6-di-iPr-Phenyl



639
3
CONHMe
2,6-di-iPr-Phenyl



640
4
CONHMe
2,6-di-iPr-Phenyl



641
1
SO2Me
2,6-di-iPr-Phenyl



642
2
SO2Me
2,6-di-iPr-Phenyl



643
3
SO2Me
2,6-di-iPr-Phenyl



644
4
SO2Me
2,6-di-iPr-Phenyl



645
1
SO2NH2
2,6-di-iPr-Phenyl



646
2
SO2NH2
2,6-di-iPr-Phenyl



647
3
SO2NH2
2,6-di-iPr-Phenyl



648
4
SO2NH2
2,6-di-iPr-Phenyl



649
1
H
3-Ph-Phenyl



650
2
H
3-Ph-Phenyl



651
3
H
3-Ph-Phenyl



652
4
H
3-Ph-Phenyl



653
1
Me
3-Ph-Phenyl



654
2
Me
3-Ph-Phenyl



655
3
Me
3-Ph-Phenyl



656
4
Me
3-Ph-Phenyl



657
1
CH2Ph
3-Ph-Phenyl



658
2
CH2Ph
3-Ph-Phenyl



659
3
CH2Ph
3-Ph-Phenyl



660
4
CH2Ph
3-Ph-Phenyl



661
1
COMe
3-Ph-Phenyl



662
2
COMe
3-Ph-Phenyl



663
3
COMe
3-Ph-Phenyl



664
4
COMe
3-Ph-Phenyl



665
1
CO2Me
3-Ph-Phenyl



666
2
CO2Me
3-Ph-Phenyl



667
3
CO2Me
3-Ph-Phenyl



668
4
CO2Me
3-Ph-Phenyl



669
1
CO2tBu
3-Ph-Phenyl



670
2
CO2tBu
3-Ph-Phenyl



671
3
CO2tBu
3-Ph-Phenyl



672
4
CO2tBu
3-Ph-Phenyl



673
1
CONHMe
3-Ph-Phenyl



674
2
CONHMe
3-Ph-Phenyl



675
3
CONHMe
3-Ph-Phenyl



676
4
CONHMe
3-Ph-Phenyl



677
1
SO2Me
3-Ph-Phenyl



678
2
SO2Me
3-Ph-Phenyl



679
3
SO2Me
3-Ph-Phenyl



680
4
SO2Me
3-Ph-Phenyl



681
1
SO2NH2
3-Ph-Phenyl



682
2
SO2NH2
3-Ph-Phenyl



683
3
SO2NH2
3-Ph-Phenyl



684
4
SO2NH2
3-Ph-Phenyl



685
1
H
2-morpholino-phenyl



686
2
H
2-morpholino-phenyl



687
3
H
2-morpholino-phenyl



688
4
H
2-morpholino-phenyl



689
1
Me
2-morpholino-phenyl



690
2
Me
2-morpholino-phenyl



691
3
Me
2-morpholino-phenyl



692
4
Me
2-morpholino-phenyl



693
1
CH2Ph
2-morpholino-phenyl



694
2
CH2Ph
2-morpholino-phenyl



695
3
CH2Ph
2-morpholino-phenyl



696
4
CH2Ph
2-morpholino-phenyl



697
1
COMe
2-morpholino-phenyl



698
2
COMe
2-morpholino-phenyl



699
3
COMe
2-morpholino-phenyl



700
4
COMe
2-morpholino-phenyl



701
1
CO2Me
2-morpholino-phenyl



702
2
CO2Me
2-morpholino-phenyl



703
3
CO2Me
2-morpholino-phenyl



704
4
CO2Me
2-morpholino-phenyl



705
1
CO2tBu
2-morpholino-phenyl



706
2
CO2tBu
2-morpholino-phenyl



707
3
CO2tBu
2-morpholino-phenyl



708
4
CO2tBu
2-morpholino-phenyl



709
1
CONHMe
2-morpholino-phenyl



710
2
CONHMe
2-morpholino-phenyl



711
3
CONHMe
2-morpholino-phenyl



712
4
CONHMe
2-morpholino-phenyl



713
1
SO2Me
2-morpholino-phenyl



714
2
SO2Me
2-morpholino-phenyl



715
3
SO2Me
2-morpholino-phenyl



716
4
SO2Me
2-morpholino-phenyl



717
1
SO2NH2
2-morpholino-phenyl



718
2
SO2NH2
2-morpholino-phenyl



719
3
SO2NH2
2-morpholino-phenyl



720
4
SO2NH2
2-morpholino-phenyl



721
1
H
4-morpholino-phenyl



722
2
H
4-morpholino-phenyl



723
3
H
4-morpholino-phenyl



724
4
H
4-morpholino-phenyl



725
1
CH2Ph
4-morpholino-phenyl



726
2
CH2Ph
4-morpholino-phenyl



727
3
CH2Ph
4-morpholino-phenyl



728
4
CH2Ph
4-morpholino-phenyl



729
1
CO2Me
4-morpholino-phenyl



730
2
CO2Me
4-morpholino-phenyl



731
3
CO2Me
4-morpholino-phenyl



732
4
CO2Me
4-morpholino-phenyl



733
1
CONHMe
4-morpholino-phenyl



734
2
CONHMe
4-morpholino-phenyl



735
3
CONHMe
4-morpholino-phenyl



736
4
CONHMe
4-morpholino-phenyl



737
1
SO2NH2
4-morpholino-phenyl



738
2
SO2NH2
4-morpholino-phenyl



739
3
SO2NH2
4-morpholino-phenyl



740
1
H
naphthylen-1-yl



741
2
H
naphthylen-1-yl



742
3
H
naphthylen-1-yl



743
4
H
naphthylen-1-yl



744
1
Me
naphthylen-1-yl



745
2
Me
naphthylen-1-yl



746
3
Me
naphthylen-1-yl



747
4
Me
naphthylen-1-yl



748
1
CH2Ph
naphthylen-1-yl



749
2
CH2Ph
naphthylen-1-yl



750
3
CH2Ph
naphthylen-1-yl



751
4
CH2Ph
naphthylen-1-yl



752
1
COMe
naphthylen-1-yl



753
2
COMe
naphthylen-1-yl



754
3
COMe
naphthylen-1-yl



755
4
COMe
naphthylen-1-yl



756
1
CO2Me
naphthylen-1-yl



757
2
CO2Me
naphthylen-1-yl



758
3
CO2Me
naphthylen-1-yl



759
4
CO2Me
naphthylen-1-yl



760
1
CO2tBu
naphthylen-1-yl



761
2
CO2tBu
naphthylen-1-yl



762
3
CO2tBu
naphthylen-1-yl



763
4
CO2tBu
naphthylen-1-yl



764
1
CONHMe
naphthylen-1-yl



765
2
CONHMe
naphthylen-1-yl



767
3
CONHMe
naphthylen-1-yl



768
4
CONHMe
naphthylen-1-yl



769
1
SO2Me
naphthylen-1-yl



770
2
SO2Me
naphthylen-1-yl



771
3
SO2Me
naphthylen-1-yl



772
4
SO2Me
naphthylen-1-yl



773
1
SO2NH2
naphthylen-1-yl



774
2
SO2NH2
naphthylen-1-yl



775
3
SO2NH2
naphthylen-1-yl



778
4
SO2NH2
naphthylen-1-yl



779
1
H
4-OH-Phenyl



780
2
H
4-OH-Phenyl



781
3
H
4-OH-Phenyl



782
4
H
4-OH-Phenyl



783
1
Me
4-OH-Phenyl



784
2
Me
4-OH-Phenyl



785
3
Me
4-OH-Phenyl



786
4
Me
4-OH-Phenyl



787
1
CH2Ph
4-OH-Phenyl



788
2
CH2Ph
4-OH-Phenyl



789
3
CH2Ph
4-OH-Phenyl



790
4
CH2Ph
4-OH-Phenyl



791
1
COMe
4-OH-Phenyl



792
2
COMe
4-OH-Phenyl



793
3
COMe
4-OH-Phenyl



794
4
COMe
4-OH-Phenyl



795
1
CO2Me
4-OH-Phenyl



796
2
CO2Me
4-OH-Phenyl



797
3
CO2Me
4-OH-Phenyl



798
4
CO2Me
4-OH-Phenyl



799
1
CO2tBu
4-OH-Phenyl



800
2
CO2tBu
4-OH-Phenyl



801
3
CO2tBu
4-OH-Phenyl



802
4
CO2tBu
4-OH-Phenyl



803
1
CONHMe
4-OH-Phenyl



804
2
CONHMe
4-OH-Phenyl



805
3
CONHMe
4-OH-Phenyl



806
4
CONHMe
4-OH-Phenyl



807
1
SO2Me
4-OH-Phenyl



808
2
SO2Me
4-OH-Phenyl



809
3
SO2Me
4-OH-Phenyl



810
4
SO2Me
4-OH-Phenyl



811
1
SO2NH2
4-OH-Phenyl



812
2
SO2NH2
4-OH-Phenyl



813
3
SO2NH2
4-OH-Phenyl



814
4
SO2NH2
4-OH-Phenyl



815
1
H
2-OH-Phenyl



816
2
H
2-OH-Phenyl



817
3
H
2-OH-Phenyl



818
4
H
2-OH-Phenyl



819
1
Me
2-OH-Phenyl



820
2
Me
2-OH-Phenyl



821
3
Me
2-OH-Phenyl



822
4
Me
2-OH-Phenyl



823
1
CH2Ph
2-OH-Phenyl



824
2
CH2Ph
2-OH-Phenyl



825
3
CH2Ph
2-OH-Phenyl



826
4
CH2Ph
2-OH-Phenyl



827
1
COMe
2-OH-Phenyl



828
2
COMe
2-OH-Phenyl



829
3
COMe
2-OH-Phenyl



830
4
COMe
2-OH-Phenyl



831
1
CO2Me
2-OH-Phenyl



832
2
CO2Me
2-OH-Phenyl



833
3
CO2Me
2-OH-Phenyl



834
4
CO2Me
2-OH-Phenyl



835
1
CO2tBu
2-OH-Phenyl



836
2
CO2tBu
2-OH-Phenyl



837
3
CO2tBu
2-OH-Phenyl



838
4
CO2tBu
2-OH-Phenyl



839
1
CONHMe
2-OH-Phenyl



840
2
CONHMe
2-OH-Phenyl



841
3
CONHMe
2-OH-Phenyl



842
4
CONHMe
2-OH-Phenyl



843
1
SO2Me
2-OH-Phenyl



844
2
SO2Me
2-OH-Phenyl



845
3
SO2Me
2-OH-Phenyl



846
4
SO2Me
2-OH-Phenyl



847
1
SO2NH2
2-OH-Phenyl



848
2
SO2NH2
2-OH-Phenyl



849
3
SO2NH2
2-OH-Phenyl



850
4
SO2NH2
2-OH-Phenyl



851
1
H
4-OMe-Phenyl



852
2
H
4-OMe-Phenyl



853
3
H
4-OMe-Phenyl



854
4
H
4-OMe-Phenyl



855
1
Me
4-OMe-Phenyl



856
2
Me
4-OMe-Phenyl



857
3
Me
4-OMe-Phenyl



858
4
Me
4-OMe-Phenyl



859
1
CH2Ph
4-OMe-Phenyl



860
2
CH2Ph
4-OMe-Phenyl



861
3
CH2Ph
4-OMe-Phenyl



862
4
CH2Ph
4-OMe-Phenyl



863
1
COMe
4-OMe-Phenyl



864
2
COMe
4-OMe-Phenyl



865
3
COMe
4-OMe-Phenyl



866
4
COMe
4-OMe-Phenyl



867
1
CO2Me
4-OMe-Phenyl



868
2
CO2Me
4-OMe-Phenyl



869
3
CO2Me
4-OMe-Phenyl



870
4
CO2Me
4-OMe-Phenyl



871
1
CO2tBu
4-OMe-Phenyl



872
2
CO2tBu
4-OMe-Phenyl



873
3
CO2tBu
4-OMe-Phenyl



874
4
CO2tBu
4-OMe-Phenyl



875
1
CONHMe
4-OMe-Phenyl



876
2
CONHMe
4-OMe-Phenyl



877
3
CONHMe
4-OMe-Phenyl



878
4
CONHMe
4-OMe-Phenyl



879
1
SO2Me
4-OMe-Phenyl



880
2
SO2Me
4-OMe-Phenyl



881
3
SO2Me
4-OMe-Phenyl



882
4
SO2Me
4-OMe-Phenyl



883
1
SO2NH2
4-OMe-Phenyl



884
2
SO2NH2
4-OMe-Phenyl



885
3
SO2NH2
4-OMe-Phenyl



886
4
SO2NH2
4-OMe-Phenyl



887
1
H
2-OMe-Phenyl



888
2
H
2-OMe-Phenyl



889
3
H
2-OMe-Phenyl



890
4
H
2-OMe-Phenyl



891
1
Me
2-OMe-Phenyl



892
2
Me
2-OMe-Phenyl



893
3
Me
2-OMe-Phenyl



894
4
Me
2-OMe-Phenyl



895
1
CH2Ph
2-OMe-Phenyl



896
2
CH2Ph
2-OMe-Phenyl



897
3
CH2Ph
2-OMe-Phenyl



898
4
CH2Ph
2-OMe-Phenyl



899
1
COMe
2-OMe-Phenyl



900
2
COMe
2-OMe-Phenyl



901
3
COMe
2-OMe-Phenyl



902
4
COMe
2-OMe-Phenyl



903
1
CO2Me
2-OMe-Phenyl



904
2
CO2Me
2-OMe-Phenyl



905
3
CO2Me
2-OMe-Phenyl



906
4
CO2Me
2-OMe-Phenyl



907
1
CO2tBu
2-OMe-Phenyl



908
2
CO2tBu
2-OMe-Phenyl



909
3
CO2tBu
2-OMe-Phenyl



910
4
CO2tBu
2-OMe-Phenyl



911
1
CONHMe
2-OMe-Phenyl



912
2
CONHMe
2-OMe-Phenyl



913
3
CONHMe
2-OMe-Phenyl



914
4
CONHMe
2-OMe-Phenyl



915
1
SO2Me
2-OMe-Phenyl



916
2
SO2Me
2-OMe-Phenyl



917
3
SO2Me
2-OMe-Phenyl



918
4
SO2Me
2-OMe-Phenyl



919
1
SO2NH2
2-OMe-Phenyl



920
2
SO2NH2
2-OMe-Phenyl



921
3
SO2NH2
2-OMe-Phenyl



922
4
SO2NH2
2-OMe-Phenyl



923
1
H
3-CN-Phenyl



924
2
H
3-CN-Phenyl



925
3
H
3-CN-Phenyl



926
4
H
3-CN-Phenyl



927
1
Me
3-CN-Phenyl



928
2
Me
3-CN-Phenyl



929
3
Me
3-CN-Phenyl



930
4
Me
3-CN-Phenyl



931
1
CH2Ph
3-CN-Phenyl



932
2
CH2Ph
3-CN-Phenyl



933
3
CH2Ph
3-CN-Phenyl



934
4
CH2Ph
3-CN-Phenyl



935
1
COMe
3-CN-Phenyl



936
2
COMe
3-CN-Phenyl



937
3
COMe
3-CN-Phenyl



938
4
COMe
3-CN-Phenyl



939
1
CO2Me
3-CN-Phenyl



940
2
CO2Me
3-CN-Phenyl



941
3
CO2Me
3-CN-Phenyl



942
4
CO2Me
3-CN-Phenyl



943
1
CO2tBu
3-CN-Phenyl



944
2
CO2tBu
3-CN-Phenyl



945
3
CO2tBu
3-CN-Phenyl



946
4
CO2tBu
3-CN-Phenyl



947
1
CONHMe
3-CN-Phenyl



948
2
CONHMe
3-CN-Phenyl



949
3
CONHMe
3-CN-Phenyl



950
4
CONHMe
3-CN-Phenyl



951
1
SO2Me
3-CN-Phenyl



952
2
SO2Me
3-CN-Phenyl



953
3
SO2Me
3-CN-Phenyl



954
4
SO2Me
3-CN-Phenyl



955
1
SO2NH2
3-CN-Phenyl



956
2
SO2NH2
3-CN-Phenyl



957
3
SO2NH2
3-CN-Phenyl



958
4
SO2NH2
3-CN-Phenyl



959
1
H
2-Me-Phenyl



960
2
H
2-Me-Phenyl



961
3
H
2-Me-Phenyl



962
4
H
2-Me-Phenyl



963
1
Me
2-Me-Phenyl



964
2
Me
2-Me-Phenyl



965
3
Me
2-Me-Phenyl



966
4
Me
2-Me-Phenyl



967
1
CH2Ph
2-Me-Phenyl



968
2
CH2Ph
2-Me-Phenyl



969
3
CH2Ph
2-Me-Phenyl



970
4
CH2Ph
2-Me-Phenyl



971
1
COMe
2-Me-Phenyl



972
2
COMe
2-Me-Phenyl



973
3
COMe
2-Me-Phenyl



974
4
COMe
2-Me-Phenyl



975
1
CO2Me
2-Me-Phenyl



976
2
CO2Me
2-Me-Phenyl



977
3
CO2Me
2-Me-Phenyl



978
4
CO2Me
2-CN-Phenyl



979
1
CO2tBu
2-Me-Phenyl



980
2
CO2tBu
2-Me-Phenyl



981
3
CO2tBu
2-Me-Phenyl



982
4
CO2tBu
2-Me-Phenyl



983
1
CONHMe
2-Me-Phenyl



984
2
CONHMe
2-Me-Phenyl



985
3
CONHMe
2-Me-Phenyl



986
4
CONHMe
2-Me-Phenyl



987
1
SO2Me
2-Me-Phenyl



988
2
SO2Me
2-Me-Phenyl



989
3
SO2Me
2-Me-Phenyl



990
4
SO2Me
2-Me-Phenyl



991
1
SO2NH2
2-Me-Phenyl



992
2
SO2NH2
2-Me-Phenyl



993
3
SO2NH2
2-Me-Phenyl



994
4
SO2NH2
2-Me-Phenyl



995
1
H
4-Me-Phenyl



996
2
H
4-Me-Phenyl



997
3
H
4-Me-Phenyl



998
4
H
4-Me-Phenyl



999
1
Me
4-Me-Phenyl



1000
2
Me
4-Me-Phenyl



1001
3
Me
4-Me-Phenyl



1002
4
Me
4-Me-Phenyl



1003
1
CH2Ph
4-Me-Phenyl



1004
2
CH2Ph
4-Me-Phenyl



1005
3
CH2Ph
4-Me-Phenyl



1006
4
CH2Ph
4-Me-Phenyl



1007
1
COMe
4-Me-Phenyl



1008
2
COMe
4-Me-Phenyl



1009
3
COMe
4-Me-Phenyl



1010
4
COMe
4-Me-Phenyl



1011
1
CO2Me
4-Me-Phenyl



1012
2
CO2Me
4-Me-Phenyl



1013
3
CO2Me
4-Me-Phenyl



1014
4
CO2Me
4-Me-Phenyl



1015
1
CO2tBu
4-Me-Phenyl



1016
2
CO2tBu
4-Me-Phenyl



1017
3
CO2tBu
4-Me-Phenyl



1018
4
CO2tBu
4-Me-Phenyl



1019
1
CONHMe
4-Me-Phenyl



1020
2
CONHMe
4-Me-Phenyl



1021
3
CONHMe
4-Me-Phenyl



1022
4
CONHMe
4-Me-Phenyl



1023
1
SO2Me
4-Me-Phenyl



1024
2
SO2Me
4-Me-Phenyl



1025
3
SO2Me
4-Me-Phenyl



1026
4
SO2Me
4-Me-Phenyl



1027
1
SO2NH2
4-Me-Phenyl



1028
2
SO2NH2
4-Me-Phenyl



1029
3
SO2NH2
4-Me-Phenyl



1030
4
SO2NH2
4-Me-Phenyl



1031
1
H
3-F-Phenyl



1032
2
H
3-F-Phenyl



1033
3
H
3-F-Phenyl



1034
4
H
3-F-Phenyl



1035
1
Me
3-F-Phenyl



1036
2
Me
3-F-Phenyl



1037
3
Me
3-F-Phenyl



1038
4
Me
3-F-Phenyl



1039
1
CH2Ph
3-F-Phenyl



1040
2
CH2Ph
3-F-Phenyl



1041
3
CH2Ph
3-F-Phenyl



1042
4
CH2Ph
3-F-Phenyl



1043
1
COMe
3-F-Phenyl



1044
2
COMe
3-F-Phenyl



1045
3
COMe
3-F-Phenyl



1046
4
COMe
3-F-Phenyl



1047
1
CO2Me
3-F-Phenyl



1048
2
CO2Me
3-F-Phenyl



1049
3
CO2Me
3-F-Phenyl



1050
4
CO2Me
3-F-Phenyl



1051
1
CO2tBu
3-F-Phenyl



1052
2
CO2tBu
3-F-Phenyl



1053
3
CO2tBu
3-F-Phenyl



1054
4
CO2tBu
3-F-Phenyl



1055
1
CONHMe
3-F-Phenyl



1056
2
CONHMe
3-F-Phenyl



1057
3
CONHMe
3-F-Phenyl



1058
4
CONHMe
3-F-Phenyl



1059
1
SO2Me
3-F-Phenyl



1060
2
SO2Me
3-F-Phenyl



1061
3
SO2Me
3-F-Phenyl



1062
4
SO2Me
3-F-Phenyl



1063
1
SO2NH2
3-F-Phenyl



1064
2
SO2NH2
3-F-Phenyl



1065
3
SO2NH2
3-F-Phenyl



1066
4
SO2NH2
3-F-Phenyl



1067
1
H
2-Cl-Phenyl



1068
2
H
2-Cl-Phenyl



1069
3
H
2-Cl-Phenyl



1070
4
H
2-Cl-Phenyl



1071
1
Me
2-Cl-Phenyl



1072
2
Me
2-Cl-Phenyl



1073
3
Me
2-Cl-Phenyl



1074
4
Me
2-Cl-Phenyl



1075
1
CH2Ph
2-Cl-Phenyl



1076
2
CH2Ph
2-Cl-Phenyl



1077
3
CH2Ph
2-Cl-Phenyl



1078
4
CH2Ph
2-Cl-Phenyl



1079
1
COMe
2-Cl-Phenyl



1080
2
COMe
2-Cl-Phenyl



1081
3
COMe
2-Cl-Phenyl



1082
4
COMe
2-Cl-Phenyl



1083
1
CO2Me
2-Cl-Phenyl



1084
2
CO2Me
2-Cl-Phenyl



1085
3
CO2Me
2-Cl-Phenyl



1086
4
CO2Me
2-Cl-Phenyl



1087
1
CO2tBu
2-Cl-Phenyl



1088
2
CO2tBu
2-Cl-Phenyl



1089
3
CO2tBu
2-Cl-Phenyl



1090
4
CO2tBu
2-Cl-Phenyl



1091
1
CONHMe
2-Cl-Phenyl



1092
2
CONHMe
2-Cl-Phenyl



1093
3
CONHMe
2-Cl-Phenyl



1094
4
CONHMe
2-Cl-Phenyl



1095
1
SO2Me
2-Cl-Phenyl



1096
2
SO2Me
2-Cl-Phenyl



1097
3
SO2Me
2-Cl-Phenyl



1098
4
SO2Me
2-Cl-Phenyl



1099
1
SO2NH2
2-Cl-Phenyl



1100
2
SO2NH2
2-Cl-Phenyl



1101
3
SO2NH2
2-Cl-Phenyl



1102
4
SO2NH2
2-Cl-Phenyl



1103
1
H
4-Cl-Phenyl



1104
2
H
4-Cl-Phenyl



1105
3
H
4-Cl-Phenyl



1106
4
H
4-Cl-Phenyl



1107
1
Me
4-Cl-Phenyl



1108
2
Me
4-Cl-Phenyl



1109
3
Me
4-Cl-Phenyl



1110
4
Me
4-Cl-Phenyl



1111
1
CH2Ph
4-Cl-Phenyl



1112
2
CH2Ph
4-Cl-Phenyl



1113
3
CH2Ph
4-Cl-Phenyl



1114
4
CH2Ph
4-Cl-Phenyl



1115
1
COMe
4-Cl-Phenyl



1116
2
COMe
4-Cl-Phenyl



1117
3
COMe
4-Cl-Phenyl



1118
4
COMe
4-Cl-Phenyl



1119
1
CO2Me
4-Cl-Phenyl



1120
2
CO2Me
4-Cl-Phenyl



1121
3
CO2Me
4-Cl-Phenyl



1122
4
CO2Me
4-Cl-Phenyl



1123
1
CO2tBu
4-Cl-Phenyl



1124
2
CO2tBu
4-Cl-Phenyl



1125
3
CO2tBu
4-Cl-Phenyl



1126
4
CO2tBu
4-Cl-Phenyl



1127
1
CONHMe
4-Cl-Phenyl



1128
2
CONHMe
4-Cl-Phenyl



1129
3
CONHMe
4-Cl-Phenyl



1130
4
CONHMe
4-Cl-Phenyl



1131
1
SO2Me
4-Cl-Phenyl



1132
2
SO2Me
4-Cl-Phenyl



1133
3
SO2Me
4-Cl-Phenyl



1134
4
SO2Me
4-Cl-Phenyl



1135
1
SO2NH2
4-Cl-Phenyl



1136
2
SO2NH2
4-Cl-Phenyl



1137
3
SO2NH2
4-Cl-Phenyl



1138
4
SO2NH2
4-Cl-Phenyl



1139
1
H
3-Br-Phenyl



1140
2
H
3-Br-Phenyl



1141
3
H
3-Br-Phenyl



1142
4
H
3-Br-Phenyl



1143
1
Me
3-Br-Phenyl



1144
2
Me
3-Br-Phenyl



1145
3
Me
3-Br-Phenyl



1146
4
Me
3-Br-Phenyl



1147
1
CH2Ph
3-Br-Phenyl



1148
2
CH2Ph
3-Br-Phenyl



1149
3
CH2Ph
3-Br-Phenyl



1150
4
CH2Ph
3-Br-Phenyl



1151
1
COMe
3-Br-Phenyl



1152
2
COMe
3-Br-Phenyl



1153
3
COMe
3-Br-Phenyl



1154
4
COMe
3-Br-Phenyl



1155
1
CO2Me
3-Br-Phenyl



1156
2
CO2Me
3-Br-Phenyl



1157
3
CO2Me
3-Br-Phenyl



1158
4
CO2Me
3-Br-Phenyl



1159
1
CO2tBu
3-Br-Phenyl



1160
2
CO2tBu
3-Br-Phenyl



1161
3
CO2tBu
3-Br-Phenyl



1162
4
CO2tBu
3-Br-Phenyl



1163
1
CONHMe
3-Br-Phenyl



1164
2
CONHMe
3-Br-Phenyl



1165
3
CONHMe
3-Br-Phenyl



1166
4
CONHMe
3-Br-Phenyl



1167
1
SO2Me
3-Br-Phenyl



1168
2
SO2Me
3-Br-Phenyl



1169
3
SO2Me
3-Br-Phenyl



1170
4
SO2Me
3-Br-Phenyl



1171
1
SO2NH2
3-Br-Phenyl



1172
2
SO2NH2
3-Br-Phenyl



1173
3
SO2NH2
3-Br-Phenyl



1174
4
SO2NH2
3-Br-Phenyl



1175
1
H
2-CF3-Phenyl



1176
2
H
2-CF3-Phenyl



1177
3
H
2-CF3-Phenyl



1178
4
H
2-CF3-Phenyl



1179
1
Me
2-CF3-Phenyl



1180
2
Me
2-CF3-Phenyl



1181
3
Me
2-CF3-Phenyl



1182
4
Me
2-CF3-Phenyl



1183
1
CH2Ph
2-CF3-Phenyl



1184
2
CH2Ph
2-CF3-Phenyl



1185
3
CH2Ph
2-CF3-Phenyl



1186
4
CH2Ph
2-CF3-Phenyl



1187
1
COMe
2-CF3-Phenyl



1188
2
COMe
2-CF3-Phenyl



1189
3
COMe
2-CF3-Phenyl



1190
4
COMe
2-CF3-Phenyl



1191
1
CO2Me
2-CF3-Phenyl



1192
2
CO2Me
2-CF3-Phenyl



1193
3
CO2Me
2-CF3-Phenyl



1194
4
CO2Me
2-CF3-Phenyl



1195
1
CO2tBu
2-CF3-Phenyl



1196
2
CO2tBu
2-CF3-Phenyl



1197
3
CO2tBu
2-CF3-Phenyl



1198
4
CO2tBu
2-CF3-Phenyl



1199
1
CONHMe
2-CF3-Phenyl



1200
2
CONHMe
2-CF3-Phenyl



1201
3
CONHMe
2-CF3-Phenyl



1202
4
CONHMe
2-CF3-Phenyl



1203
1
SO2Me
2-CF3-Phenyl



1204
2
SO2Me
2-CF3-Phenyl



1205
3
SO2Me
2-CF3-Phenyl



1206
4
SO2Me
2-CF3-Phenyl



1207
1
SO2NH2
2-CF3-Phenyl



1208
2
SO2NH2
2-CF3-Phenyl



1209
3
SO2NH2
2-CF3-Phenyl



1210
4
SO2NH2
2-CF3-Phenyl



1211
1
H
4-CF3-Phenyl



1212
2
H
4-CF3-Phenyl



1213
3
H
4-CF3-Phenyl



1214
4
H
4-CF3-Phenyl



1215
1
Me
4-CF3-Phenyl



1216
2
Me
4-CF3-Phenyl



1217
3
Me
4-CF3-Phenyl



1218
4
Me
4-CF3-Phenyl



1219
1
CH2Ph
4-CF3-Phenyl



1220
2
CH2Ph
4-CF3-Phenyl



1221
3
CH2Ph
4-CF3-Phenyl



1222
4
CH2Ph
4-CF3-Phenyl



1223
1
COMe
4-CF3-Phenyl



1224
2
COMe
4-CF3-Phenyl



1225
3
COMe
4-CF3-Phenyl



1226
4
COMe
4-CF3-Phenyl



1227
1
CO2Me
4-CF3-Phenyl



1228
2
CO2Me
4-CF3-Phenyl



1229
3
CO2Me
4-CF3-Phenyl



1230
4
CO2Me
4-CF3-Phenyl



1231
1
CO2tBu
4-CF3-Phenyl



1232
2
CO2tBu
4-CF3-Phenyl



1233
3
CO2tBu
4-CF3-Phenyl



1234
4
CO2tBu
4-CF3-Phenyl



1235
1
CONHMe
4-CF3-Phenyl



1236
2
CONHMe
4-CF3-Phenyl



1237
3
CONHMe
4-CF3-Phenyl



1238
4
CONHMe
4-CF3-Phenyl



1239
1
SO2Me
4-CF3-Phenyl



1240
2
SO2Me
4-CF3-Phenyl



1241
3
SO2Me
4-CF3-Phenyl



1242
4
SO2Me
4-CF3-Phenyl



1243
1
SO2NH2
4-CF3-Phenyl



1244
2
SO2NH2
4-CF3-Phenyl



1245
3
SO2NH2
4-CF3-Phenyl



1246
4
SO2NH2
4-CF3-Phenyl



1247
1
H
3-iPr-Phenyl



1248
2
H
3-iPr-Phenyl



1249
3
H
3-iPr-Phenyl



1250
4
H
3-iPr-Phenyl



1251
1
Me
3-iPr-Phenyl



1252
2
Me
3-iPr-Phenyl



1253
3
Me
3-iPr-Phenyl



1254
4
Me
3-iPr-Phenyl



1255
1
CH2Ph
3-iPr-Phenyl



1256
2
CH2Ph
3-iPr-Phenyl



1257
3
CH2Ph
3-iPr-Phenyl



1258
4
CH2Ph
3-iPr-Phenyl



1259
1
COMe
3-iPr-Phenyl



1260
2
COMe
3-iPr-Phenyl



1261
3
COMe
3-iPr-Phenyl



1262
4
COMe
3-iPr-Phenyl



1263
1
CO2Me
3-iPr-Phenyl



1264
2
CO2Me
3-iPr-Phenyl



1265
3
CO2Me
3-iPr-Phenyl



1266
4
CO2Me
3-iPr-Phenyl



1267
1
CO2tBu
3-iPr-Phenyl



1268
2
CO2tBu
3-iPr-Phenyl



1269
3
CO2tBu
3-iPr-Phenyl



1270
4
CO2tBu
3-iPr-Phenyl



1271
1
CONHMe
3-iPr-Phenyl



1272
2
CONHMe
3-iPr-Phenyl



1273
3
CONHMe
3-iPr-Phenyl



1274
4
CONHMe
3-iPr-Phenyl



1275
1
SO2Me
3-iPr-Phenyl



1276
2
SO2Me
3-iPr-Phenyl



1277
3
SO2Me
3-iPr-Phenyl



1278
4
SO2Me
3-iPr-Phenyl



1279
1
SO2NH2
3-iPr-Phenyl



1280
2
SO2NH2
3-iPr-Phenyl



1281
3
SO2NH2
3-iPr-Phenyl



1282
4
SO2NH2
3-iPr-Phenyl



1283
1
H
4-NH2-Phenyl



1284
2
H
4-NH2-Phenyl



1285
3
H
4-NH2-Phenyl



1286
4
H
4-NH2-Phenyl



1287
1
Me
4-NH2-Phenyl



1288
2
Me
4-NH2-Phenyl



1289
3
Me
4-NH2-Phenyl



1290
4
Me
4-NH2-Phenyl



1291
1
CH2Ph
4-NH2-Phenyl



1292
2
CH2Ph
4-NH2-Phenyl



1293
3
CH2Ph
4-NH2-Phenyl



1294
4
CH2Ph
4-NH2-Phenyl



1295
1
COMe
4-NH2-Phenyl



1296
2
COMe
4-NH2-Phenyl



1297
3
COMe
4-NH2-Phenyl



1298
4
COMe
4-NH2-Phenyl



1299
1
CO2Me
4-NH2-Phenyl



1300
2
CO2Me
4-NH2-Phenyl



1301
3
CO2Me
4-NH2-Phenyl



1302
4
CO2Me
4-NH2-Phenyl



1303
1
CO2tBu
4-NH2-Phenyl



1304
2
CO2tBu
4-NH2-Phenyl



1305
3
CO2tBu
4-NH2-Phenyl



1306
4
CO2tBu
4-NH2-Phenyl



1307
1
CONHMe
4-NH2-Phenyl



1308
2
CONHMe
4-NH2-Phenyl



1309
3
CONHMe
4-NH2-Phenyl



1310
4
CONHMe
4-NH2-Phenyl



1311
1
SO2Me
4-NH2-Phenyl



1312
2
SO2Me
4-NH2-Phenyl



1313
3
SO2Me
4-NH2-Phenyl



1314
4
SO2Me
4-NH2-Phenyl



1315
1
SO2NH2
4-NH2-Phenyl



1316
2
SO2NH2
4-NH2-Phenyl



1317
3
SO2NH2
4-NH2-Phenyl



1318
4
SO2NH2
4-NH2-Phenyl



1319
1
H
2-NH2-Phenyl



1320
2
H
2-NH2-Phenyl



1321
3
H
2-NH2-Phenyl



1322
4
H
2-NH2-Phenyl



1323
1
Me
2-NH2-Phenyl



1324
2
Me
2-NH2-Phenyl



1325
3
Me
2-NH2-Phenyl



1326
4
Me
2-NH2-Phenyl



1327
1
CH2Ph
2-NH2-Phenyl



1328
2
CH2Ph
2-NH2-Phenyl



1329
3
CH2Ph
2-NH2-Phenyl



1330
4
CH2Ph
2-NH2-Phenyl



1331
1
COMe
2-NH2-Phenyl



1332
2
COMe
2-NH2-Phenyl



1333
3
COMe
2-NH2-Phenyl



1334
4
COMe
2-NH2-Phenyl



1335
1
CO2Me
2-NH2-Phenyl



1336
2
CO2Me
2-NH2-Phenyl



1337
3
CO2Me
2-NH2-Phenyl



1338
4
CO2Me
2-NH2-Phenyl



1339
1
CO2tBu
2-NH2-Phenyl



1340
2
CO2tBu
2-NH2-Phenyl



1341
3
CO2tBu
2-NH2-Phenyl



1342
4
CO2tBu
2-NH2-Phenyl



1343
1
CONHMe
2-NH2-Phenyl



1344
2
CONHMe
2-NH2-Phenyl



1345
3
CONHMe
2-NH2-Phenyl



1346
4
CONHMe
2-NH2-Phenyl



1347
1
SO2Me
2-NH2-Phenyl



1348
2
SO2Me
2-NH2-Phenyl



1349
3
SO2Me
2-NH2-Phenyl



1350
4
SO2Me
2-NH2-Phenyl



1351
1
SO2NH2
2-NH2-Phenyl



1352
2
SO2NH2
2-NH2-Phenyl



1353
3
SO2NH2
2-NH2-Phenyl



1354
4
SO2NH2
2-NH2-Phenyl



1355
1
H
2,6-di-Me-Phenyl



1356
2
H
2,6-di-Me-Phenyl



1357
3
H
2,6-di-Me-Phenyl



1358
4
H
2,6-di-Me-Phenyl



1359
1
Me
2,6-di-Me-Phenyl



1360
2
Me
2,6-di-Me-Phenyl



1361
3
Me
2,6-di-Me-Phenyl



1362
4
Me
2,6-di-Me-Phenyl



1363
1
CH2Ph
2,6-di-Me-Phenyl



1364
2
CH2Ph
2,6-di-Me-Phenyl



1365
3
CH2Ph
2,6-di-Me-Phenyl



1366
4
CH2Ph
2,6-di-Me-Phenyl



1367
1
COMe
2,6-di-Me-Phenyl



1368
2
COMe
2,6-di-Me-Phenyl



1369
3
COMe
2,6-di-Me-Phenyl



1370
4
COMe
2,6-di-Me-Phenyl



1371
1
CO2Me
2,6-di-Me-Phenyl



1372
2
CO2Me
2,6-di-Me-Phenyl



1373
3
CO2Me
2,6-di-Me-Phenyl



1374
4
CO2Me
2,6-di-Me-Phenyl



1375
1
CO2tBu
2,6-di-Me-Phenyl



1376
2
CO2tBu
2,6-di-Me-Phenyl



1377
3
CO2tBu
2,6-di-Me-Phenyl



1378
4
CO2tBu
2,6-di-Me-Phenyl



1379
1
CONHMe
2,6-di-Me-Phenyl



1380
2
CONHMe
2,6-di-Me-Phenyl



1381
3
CONHMe
2,6-di-Me-Phenyl



1382
4
CONHMe
2,6-di-Me-Phenyl



1383
1
SO2Me
2,6-di-Me-Phenyl



1384
2
SO2Me
2,6-di-Me-Phenyl



1385
3
SO2Me
2,6-di-Me-Phenyl



1386
4
SO2Me
2,6-di-Me-Phenyl



1387
1
SO2NH2
2,6-di-Me-Phenyl



1388
2
SO2NH2
2,6-di-Me-Phenyl



1389
3
SO2NH2
2,6-di-Me-Phenyl



1390
4
SO2NH2
2,6-di-Me-Phenyl



1391
1
H
2-Ph-Phenyl



1392
2
H
2-Ph-Phenyl



1393
3
H
2-Ph-Phenyl



1394
4
H
2-Ph-Phenyl



1395
1
Me
2-Ph-Phenyl



1396
2
Me
2-Ph-Phenyl



1397
3
Me
2-Ph-Phenyl



1398
4
Me
2-Ph-Phenyl



1399
1
CH2Ph
2-Ph-Phenyl



1400
2
CH2Ph
2-Ph-Phenyl



1401
3
CH2Ph
2-Ph-Phenyl



1402
4
CH2Ph
2-Ph-Phenyl



1403
1
COMe
2-Ph-Phenyl



1404
2
COMe
2-Ph-Phenyl



1405
3
COMe
2-Ph-Phenyl



1406
4
COMe
2-Ph-Phenyl



1407
1
CO2Me
2-Ph-Phenyl



1408
2
CO2Me
2-Ph-Phenyl



1409
3
CO2Me
2-Ph-Phenyl



1410
4
CO2Me
2-Ph-Phenyl



1411
1
CO2tBu
2-Ph-Phenyl



1412
2
CO2tBu
2-Ph-Phenyl



1413
3
CO2tBu
2-Ph-Phenyl



1414
4
CO2tBu
2-Ph-Phenyl



1415
1
CONHMe
2-Ph-Phenyl



1416
2
CONHMe
2-Ph-Phenyl



1417
3
CONHMe
2-Ph-Phenyl



1418
4
CONHMe
2-Ph-Phenyl



1419
1
SO2Me
2-Ph-Phenyl



1420
2
SO2Me
2-Ph-Phenyl



1421
3
SO2Me
2-Ph-Phenyl



1422
4
SO2Me
2-Ph-Phenyl



1423
1
SO2NH2
2-Ph-Phenyl



1424
2
SO2NH2
2-Ph-Phenyl



1425
3
SO2NH2
2-Ph-Phenyl



1426
4
SO2NH2
2-Ph-Phenyl



1427
1
H
4-Ph-Phenyl



1428
2
H
4-Ph-Phenyl



1429
3
H
4-Ph-Phenyl



1430
4
H
4-Ph-Phenyl



1431
1
Me
4-Ph-Phenyl



1432
2
Me
4-Ph-Phenyl



1433
3
Me
4-Ph-Phenyl



1434
4
Me
4-Ph-Phenyl



1435
1
CH2Ph
4-Ph-Phenyl



1436
2
CH2Ph
4-Ph-Phenyl



1437
3
CH2Ph
4-Ph-Phenyl



1438
4
CH2Ph
4-Ph-Phenyl



1439
1
COMe
4-Ph-Phenyl



1440
2
COMe
4-Ph-Phenyl



1441
3
COMe
4-Ph-Phenyl



1442
4
COMe
4-Ph-Phenyl



1443
1
CO2Me
4-Ph-Phenyl



1444
2
CO2Me
4-Ph-Phenyl



1445
3
CO2Me
4-Ph-Phenyl



1446
4
CO2Me
4-Ph-Phenyl



1447
1
CO2tBu
4-Ph-Phenyl



1448
2
CO2tBu
4-Ph-Phenyl



1449
3
CO2tBu
4-Ph-Phenyl



1450
4
CO2tBu
4-Ph-Phenyl



1451
1
CONHMe
4-Ph-Phenyl



1452
2
CONHMe
4-Ph-Phenyl



1453
3
CONHMe
4-Ph-Phenyl



1454
4
CONHMe
4-Ph-Phenyl



1455
1
SO2Me
4-Ph-Phenyl



1456
2
SO2Me
4-Ph-Phenyl



1457
3
SO2Me
4-Ph-Phenyl



1458
4
SO2Me
4-Ph-Phenyl



1459
1
SO2NH2
4-Ph-Phenyl



1460
2
SO2NH2
4-Ph-Phenyl



1461
3
SO2NH2
4-Ph-Phenyl



1462
4
SO2NH2
4-Ph-Phenyl



1463
1
H
3-morpholino-phenyl



1464
2
H
3-morpholino-phenyl



1465
3
H
3-morpholino-phenyl



1466
4
H
3-morpholino-phenyl



1467
1
Me
3-morpholino-phenyl



1468
2
Me
3-morpholino-phenyl



1469
3
Me
3-morpholino-phenyl



1470
4
Me
3-morpholino-phenyl



1471
1
CH2Ph
3-morpholino-phenyl



1472
2
CH2Ph
3-morpholino-phenyl



1473
3
CH2Ph
3-morpholino-phenyl



1474
4
CH2Ph
3-morpholino-phenyl



1475
1
COMe
3-morpholino-phenyl



1476
2
COMe
3-morpholino-phenyl



1477
3
COMe
3-morpholino-phenyl



1478
4
COMe
3-morpholino-phenyl



1479
1
CO2Me
3-morpholino-phenyl



1480
2
CO2Me
3-morpholino-phenyl



1481
3
CO2Me
3-morpholino-phenyl



1482
4
CO2Me
3-morpholino-phenyl



1483
1
CO2tBu
3-morpholino-phenyl



1484
2
CO2tBu
3-morpholino-phenyl



1485
3
CO2tBu
3-morpholino-phenyl



1486
4
CO2tBu
3-morpholino-phenyl



1487
1
CONHMe
3-morpholino-phenyl



1488
2
CONHMe
3-morpholino-phenyl



1489
3
CONHMe
3-morpholino-phenyl



1490
4
CONHMe
3-morpholino-phenyl



1491
1
SO2Me
3-morpholino-phenyl



1492
2
SO2Me
3-morpholino-phenyl



1493
3
SO2Me
3-morpholino-phenyl



1494
4
SO2Me
3-morpholino-phenyl



1495
1
SO2NH2
3-morpholino-phenyl



1496
2
SO2NH2
3-morpholino-phenyl



1497
3
SO2NH2
3-morpholino-phenyl



1498
4
SO2NH2
3-morpholino-phenyl



1499
1
Me
4-morpholino-phenyl



1500
2
Me
4-morpholino-phenyl



1501
3
Me
4-morpholino-phenyl



1502
4
Me
4-morpholino-phenyl



103
1
COMe
4-morpholino-phenyl



1504
2
COMe
4-morpholino-phenyl



1505
3
COMe
4-morpholino-phenyl



1506
4
COMe
4-morpholino-phenyl



1507
1
CO2tBu
4-morpholino-phenyl



1508
2
CO2tBu
4-morpholino-phenyl



1509
3
CO2tBu
4-morpholino-phenyl



1510
4
CO2tBu
4-morpholino-phenyl



1511
1
SO2Me
4-morpholino-phenyl



1512
2
SO2Me
4-morpholino-phenyl



1513
3
SO2Me
4-morpholino-phenyl



1514
4
SO2Me
4-morpholino-phenyl



1516
1
H
naphthylen-2-yl



1517
2
H
naphthylen-2-yl



1518
3
H
naphthylen-2-yl



1519
4
H
naphthylen-2-yl



1520
1
Me
naphthylen-2-yl



1521
2
Me
naphthylen-2-yl



1522
3
Me
naphthylen-2-yl



1523
4
Me
naphthylen-2-yl



1524
1
CH2Ph
naphthylen-2-yl



1525
2
CH2Ph
naphthylen-2-yl



1526
3
CH2Ph
naphthylen-2-yl



1527
4
CH2Ph
naphthylen-2-yl



1528
1
COMe
naphthylen-2-yl



1529
2
COMe
naphthylen-2-yl



1530
3
COMe
naphthylen-2-yl



1531
4
COMe
naphthylen-2-yl



1532
1
CO2Me
naphthylen-2-yl



1533
2
CO2Me
naphthylen-2-yl



1534
3
CO2Me
naphthylen-2-yl



1535
4
CO2Me
naphthylen-2-yl



1536
1
CO2tBu
naphthylen-2-yl



1537
2
CO2tBu
naphthylen-2-yl



1538
3
CO2tBu
naphthylen-2-yl



1539
4
CO2tBu
naphthylen-2-yl



1540
1
CONHMe
naphthylen-2-yl



1541
2
CONHMe
naphthylen-2-yl



1542
3
CONHMe
naphthylen-2-yl



1543
4
CONHMe
naphthylen-2-yl



1544
1
SO2Me
naphthylen-2-yl



1545
2
SO2Me
naphthylen-2-yl



1546
3
SO2Me
naphthylen-2-yl



1547
4
SO2Me
naphthylen-2-yl



1548
1
SO2NH2
naphthylen-2-yl



1549
2
SO2NH2
naphthylen-2-yl



1550
3
SO2NH2
naphthylen-2-yl



1551
4
SO2NH2
naphthylen-2-yl










Exemplary embodiments include compounds having the formula (XXIV)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 18.














TABLE 18







Entry
n
R7
R3





















1
1
H
Phenyl



2
2
H
Phenyl



3
3
H
Phenyl



4
4
H
Phenyl



5
1
Me
Phenyl



6
2
Me
Phenyl



7
3
Me
Phenyl



8
4
Me
Phenyl



9
1
CH2Ph
Phenyl



10
2
CH2Ph
Phenyl



11
3
CH2Ph
Phenyl



12
4
CH2Ph
Phenyl



13
1
COMe
Phenyl



14
2
COMe
Phenyl



15
3
COMe
Phenyl



16
4
COMe
Phenyl



17
1
CO2Me
Phenyl



18
2
CO2Me
Phenyl



19
3
CO2Me
Phenyl



20
4
CO2Me
Phenyl



21
1
CO2tBu
Phenyl



22
2
CO2tBu
Phenyl



23
3
CO2tBu
Phenyl



24
4
CO2tBu
Phenyl



25
1
CONHMe
Phenyl



26
2
CONHMe
Phenyl



27
3
CONHMe
Phenyl



28
4
CONHMe
Phenyl



29
1
SO2Me
Phenyl



30
2
SO2Me
Phenyl



31
3
SO2Me
Phenyl



32
4
SO2Me
Phenyl



33
1
SO2NH2
Phenyl



34
2
SO2NH2
Phenyl



35
3
SO2NH2
Phenyl



36
4
SO2NH2
Phenyl



37
1
H
3-OH-Phenyl



38
2
H
3-OH-Phenyl



39
3
H
3-OH-Phenyl



40
4
H
3-OH-Phenyl



41
1
Me
3-OH-Phenyl



42
2
Me
3-OH-Phenyl



43
3
Me
3-OH-Phenyl



44
4
Me
3-OH-Phenyl



45
1
CH2Ph
3-OH-Phenyl



46
2
CH2Ph
3-OH-Phenyl



47
3
CH2Ph
3-OH-Phenyl



48
4
CH2Ph
3-OH-Phenyl



49
1
COMe
3-OH-Phenyl



50
2
COMe
3-OH-Phenyl



51
3
COMe
3-OH-Phenyl



52
4
COMe
3-OH-Phenyl



53
1
CO2Me
3-OH-Phenyl



54
2
CO2Me
3-OH-Phenyl



55
3
CO2Me
3-OH-Phenyl



56
4
CO2Me
3-OH-Phenyl



57
1
CO2tBu
3-OH-Phenyl



58
2
CO2tBu
3-OH-Phenyl



59
3
CO2tBu
3-OH-Phenyl



60
4
CO2tBu
3-OH-Phenyl



61
1
CONHMe
3-OH-Phenyl



62
2
CONHMe
3-OH-Phenyl



63
3
CONHMe
3-OH-Phenyl



64
4
CONHMe
3-OH-Phenyl



65
1
SO2Me
3-OH-Phenyl



66
2
SO2Me
3-OH-Phenyl



67
3
SO2Me
3-OH-Phenyl



68
4
SO2Me
3-OH-Phenyl



69
1
SO2NH2
3-OH-Phenyl



70
2
SO2NH2
3-OH-Phenyl



71
3
SO2NH2
3-OH-Phenyl



72
4
SO2NH2
3-OH-Phenyl



73
1
H
4-NO2-Phenyl



74
2
H
4-NO2-Phenyl



75
3
H
4-NO2-Phenyl



76
4
H
4-NO2-Phenyl



77
1
Me
4-NO2-Phenyl



78
2
Me
4-NO2-Phenyl



79
3
Me
4-NO2-Phenyl



80
4
Me
4-NO2-Phenyl



81
1
CH2Ph
4-NO2-Phenyl



82
2
CH2Ph
4-NO2-Phenyl



83
3
CH2Ph
4-NO2-Phenyl



84
4
CH2Ph
4-NO2-Phenyl



85
1
COMe
4-NO2-Phenyl



86
2
COMe
4-NO2-Phenyl



87
3
COMe
4-NO2-Phenyl



88
4
COMe
4-NO2-Phenyl



89
1
CO2Me
4-NO2-Phenyl



90
2
CO2Me
4-NO2-Phenyl



91
3
CO2Me
4-NO2-Phenyl



92
4
CO2Me
4-NO2-Phenyl



93
1
CO2tBu
4-NO2-Phenyl



94
2
CO2tBu
4-NO2-Phenyl



95
3
CO2tBu
4-NO2-Phenyl



96
4
CO2tBu
4-NO2-Phenyl



97
1
CONHMe
4-NO2-Phenyl



98
2
CONHMe
4-NO2-Phenyl



99
3
CONHMe
4-NO2-Phenyl



100
4
CONHMe
4-NO2-Phenyl



101
1
SO2Me
4-NO2-Phenyl



102
2
SO2Me
4-NO2-Phenyl



103
3
SO2Me
4-NO2-Phenyl



104
4
SO2Me
4-NO2-Phenyl



105
1
SO2NH2
4-NO2-Phenyl



106
2
SO2NH2
4-NO2-Phenyl



107
3
SO2NH2
4-NO2-Phenyl



108
4
SO2NH2
4-NO2-Phenyl



109
1
H
3-OMe-Phenyl



110
2
H
3-OMe-Phenyl



111
3
H
3-OMe-Phenyl



112
4
H
3-OMe-Phenyl



113
1
Me
3-OMe-Phenyl



114
2
Me
3-OMe-Phenyl



115
3
Me
3-OMe-Phenyl



116
4
Me
3-OMe-Phenyl



117
1
CH2Ph
3-OMe-Phenyl



118
2
CH2Ph
3-OMe-Phenyl



119
3
CH2Ph
3-OMe-Phenyl



120
4
CH2Ph
3-OMe-Phenyl



121
1
COMe
3-OMe-Phenyl



122
2
COMe
3-OMe-Phenyl



123
3
COMe
3-OMe-Phenyl



124
4
COMe
3-OMe-Phenyl



125
1
CO2Me
3-OMe-Phenyl



126
2
CO2Me
3-OMe-Phenyl



127
3
CO2Me
3-OMe-Phenyl



128
4
CO2Me
3-OMe-Phenyl



129
1
CO2tBu
3-OMe-Phenyl



130
2
CO2tBu
3-OMe-Phenyl



131
3
CO2tBu
3-OMe-Phenyl



132
4
CO2tBu
3-OMe-Phenyl



133
1
CONHMe
3-OMe-Phenyl



134
2
CONHMe
3-OMe-Phenyl



135
3
CONHMe
3-OMe-Phenyl



136
4
CONHMe
3-OMe-Phenyl



137
1
SO2Me
3-OMe-Phenyl



138
2
SO2Me
3-OMe-Phenyl



139
3
SO2Me
3-OMe-Phenyl



140
4
SO2Me
3-OMe-Phenyl



141
1
SO2NH2
3-OMe-Phenyl



142
2
SO2NH2
3-OMe-Phenyl



143
3
SO2NH2
3-OMe-Phenyl



144
4
SO2NH2
3-OMe-Phenyl



145
1
H
4-CN-Phenyl



146
2
H
4-CN-Phenyl



147
3
H
4-CN-Phenyl



148
4
H
4-CN-Phenyl



149
1
Me
4-CN-Phenyl



150
2
Me
4-CN-Phenyl



151
3
Me
4-CN-Phenyl



152
4
Me
4-CN-Phenyl



153
1
CH2Ph
4-CN-Phenyl



154
2
CH2Ph
4-CN-Phenyl



155
3
CH2Ph
4-CN-Phenyl



156
4
CH2Ph
4-CN-Phenyl



157
1
COMe
4-CN-Phenyl



158
2
COMe
4-CN-Phenyl



159
3
COMe
4-CN-Phenyl



160
4
COMe
4-CN-Phenyl



161
1
CO2Me
4-CN-Phenyl



162
2
CO2Me
4-CN-Phenyl



163
3
CO2Me
4-CN-Phenyl



164
4
CO2Me
4-CN-Phenyl



165
1
CO2tBu
4-CN-Phenyl



166
2
CO2tBu
4-CN-Phenyl



167
3
CO2tBu
4-CN-Phenyl



168
4
CO2tBu
4-CN-Phenyl



169
1
CONHMe
4-CN-Phenyl



170
2
CONHMe
4-CN-Phenyl



171
3
CONHMe
4-CN-Phenyl



172
4
CONHMe
4-CN-Phenyl



173
1
SO2Me
4-CN-Phenyl



174
2
SO2Me
4-CN-Phenyl



175
3
SO2Me
4-CN-Phenyl



176
4
SO2Me
4-CN-Phenyl



177
1
SO2NH2
4-CN-Phenyl



178
2
SO2NH2
4-CN-Phenyl



179
3
SO2NH2
4-CN-Phenyl



180
4
SO2NH2
4-CN-Phenyl



181
1
H
2-CN-Phenyl



182
2
H
2-CN-Phenyl



183
3
H
2-CN-Phenyl



184
4
H
2-CN-Phenyl



185
1
Me
2-CN-Phenyl



186
2
Me
2-CN-Phenyl



187
3
Me
2-CN-Phenyl



188
4
Me
2-CN-Phenyl



189
1
CH2Ph
2-CN-Phenyl



190
2
CH2Ph
2-CN-Phenyl



191
3
CH2Ph
2-CN-Phenyl



192
4
CH2Ph
2-CN-Phenyl



193
1
COMe
2-CN-Phenyl



194
2
COMe
2-CN-Phenyl



195
3
COMe
2-CN-Phenyl



196
4
COMe
2-CN-Phenyl



197
1
CO2Me
2-CN-Phenyl



198
2
CO2Me
2-CN-Phenyl



199
3
CO2Me
2-CN-Phenyl



200
4
CO2Me
2-CN-Phenyl



201
1
CO2tBu
2-CN-Phenyl



202
2
CO2tBu
2-CN-Phenyl



203
3
CO2tBu
2-CN-Phenyl



204
4
CO2tBu
2-CN-Phenyl



205
1
CONHMe
2-CN-Phenyl



206
2
CONHMe
2-CN-Phenyl



207
3
CONHMe
2-CN-Phenyl



208
4
CONHMe
2-CN-Phenyl



209
1
SO2Me
2-CN-Phenyl



210
2
SO2Me
2-CN-Phenyl



211
3
SO2Me
2-CN-Phenyl



212
4
SO2Me
2-CN-Phenyl



213
1
SO2NH2
2-CN-Phenyl



214
2
SO2NH2
2-CN-Phenyl



215
3
SO2NH2
2-CN-Phenyl



216
4
SO2NH2
2-CN-Phenyl



217
1
H
3-Me-Phenyl



218
2
H
3-Me-Phenyl



219
3
H
3-Me-Phenyl



220
4
H
3-Me-Phenyl



221
1
Me
3-Me-Phenyl



222
2
Me
3-Me-Phenyl



223
3
Me
3-Me-Phenyl



224
4
Me
3-Me-Phenyl



225
1
CH2Ph
3-Me-Phenyl



226
2
CH2Ph
3-Me-Phenyl



227
3
CH2Ph
3-Me-Phenyl



228
4
CH2Ph
3-Me-Phenyl



229
1
COMe
3-Me-Phenyl



230
2
COMe
3-Me-Phenyl



231
3
COMe
3-Me-Phenyl



232
4
COMe
3-Me-Phenyl



233
1
CO2Me
3-Me-Phenyl



234
2
CO2Me
3-Me-Phenyl



235
3
CO2Me
3-Me-Phenyl



236
4
CO2Me
3-Me-Phenyl



237
1
CO2tBu
3-Me-Phenyl



238
2
CO2tBu
3-Me-Phenyl



239
3
CO2tBu
3-Me-Phenyl



240
4
CO2tBu
3-Me-Phenyl



241
1
CONHMe
3-Me-Phenyl



242
2
CONHMe
3-Me-Phenyl



243
3
CONHMe
3-Me-Phenyl



244
4
CONHMe
3-Me-Phenyl



245
1
SO2Me
3-Me-Phenyl



246
2
SO2Me
3-Me-Phenyl



247
3
SO2Me
3-Me-Phenyl



248
4
SO2Me
3-Me-Phenyl



249
1
SO2NH2
3-Me-Phenyl



250
2
SO2NH2
3-Me-Phenyl



251
3
SO2NH2
3-Me-Phenyl



252
4
SO2NH2
3-Me-Phenyl



253
1
H
2-F-Phenyl



254
2
H
2-F-Phenyl



255
3
H
2-F-Phenyl



256
4
H
2-F-Phenyl



257
1
Me
2-F-Phenyl



258
2
Me
2-F-Phenyl



259
3
Me
2-F-Phenyl



260
4
Me
2-F-Phenyl



261
1
CH2Ph
2-F-Phenyl



262
2
CH2Ph
2-F-Phenyl



263
3
CH2Ph
2-F-Phenyl



264
4
CH2Ph
2-F-Phenyl



265
1
COMe
2-F-Phenyl



266
2
COMe
2-F-Phenyl



267
3
COMe
2-F-Phenyl



268
4
COMe
2-F-Phenyl



269
1
CO2Me
2-F-Phenyl



270
2
CO2Me
2-F-Phenyl



271
3
CO2Me
2-F-Phenyl



272
4
CO2Me
2-F-Phenyl



273
1
CO2tBu
2-F-Phenyl



274
2
CO2tBu
2-F-Phenyl



275
3
CO2tBu
2-F-Phenyl



276
4
CO2tBu
2-F-Phenyl



277
1
CONHMe
2-F-Phenyl



278
2
CONHMe
2-F-Phenyl



279
3
CONHMe
2-F-Phenyl



280
4
CONHMe
2-F-Phenyl



281
1
SO2Me
2-F-Phenyl



282
2
SO2Me
2-F-Phenyl



283
3
SO2Me
2-F-Phenyl



284
4
SO2Me
2-F-Phenyl



285
1
SO2NH2
2-F-Phenyl



286
2
SO2NH2
2-F-Phenyl



287
3
SO2NH2
2-F-Phenyl



288
4
SO2NH2
2-F-Phenyl



289
1
H
4-F-Phenyl



290
2
H
4-F-Phenyl



291
3
H
4-F-Phenyl



292
4
H
4-F-Phenyl



293
1
Me
4-F-Phenyl



294
2
Me
4-F-Phenyl



295
3
Me
4-F-Phenyl



296
4
Me
4-F-Phenyl



297
1
CH2Ph
4-F-Phenyl



298
2
CH2Ph
4-F-Phenyl



299
3
CH2Ph
4-F-Phenyl



300
4
CH2Ph
4-F-Phenyl



301
1
COMe
4-F-Phenyl



302
2
COMe
4-F-Phenyl



303
3
COMe
4-F-Phenyl



304
4
COMe
4-F-Phenyl



305
1
CO2Me
4-F-Phenyl



306
2
CO2Me
4-F-Phenyl



307
3
CO2Me
4-F-Phenyl



308
4
CO2Me
4-F-Phenyl



309
1
CO2tBu
4-F-Phenyl



310
2
CO2tBu
4-F-Phenyl



311
3
CO2tBu
4-F-Phenyl



312
4
CO2tBu
4-F-Phenyl



313
1
CONHMe
4-F-Phenyl



314
2
CONHMe
4-F-Phenyl



315
3
CONHMe
4-F-Phenyl



316
4
CONHMe
4-F-Phenyl



317
1
SO2Me
4-F-Phenyl



318
2
SO2Me
4-F-Phenyl



319
3
SO2Me
4-F-Phenyl



320
4
SO2Me
4-F-Phenyl



321
1
SO2NH2
4-F-Phenyl



322
2
SO2NH2
4-F-Phenyl



323
3
SO2NH2
4-F-Phenyl



324
4
SO2NH2
4-F-Phenyl



325
1
H
3-Cl-Phenyl



326
2
H
3-Cl-Phenyl



327
3
H
3-Cl-Phenyl



328
4
H
3-Cl-Phenyl



329
1
Me
3-Cl-Phenyl



330
2
Me
3-Cl-Phenyl



331
3
Me
3-Cl-Phenyl



332
4
Me
3-Cl-Phenyl



333
1
CH2Ph
3-Cl-Phenyl



334
2
CH2Ph
3-Cl-Phenyl



335
3
CH2Ph
3-Cl-Phenyl



336
4
CH2Ph
3-Cl-Phenyl



337
1
COMe
3-Cl-Phenyl



338
2
COMe
3-Cl-Phenyl



339
3
COMe
3-Cl-Phenyl



340
4
COMe
3-Cl-Phenyl



341
1
CO2Me
3-Cl-Phenyl



342
2
CO2Me
3-Cl-Phenyl



343
3
CO2Me
3-Cl-Phenyl



344
4
CO2Me
3-Cl-Phenyl



345
1
CO2tBu
3-Cl-Phenyl



346
2
CO2tBu
3-Cl-Phenyl



347
3
CO2tBu
3-Cl-Phenyl



348
4
CO2tBu
3-Cl-Phenyl



349
1
CONHMe
3-Cl-Phenyl



350
2
CONHMe
3-Cl-Phenyl



351
3
CONHMe
3-Cl-Phenyl



352
4
CONHMe
3-Cl-Phenyl



353
1
SO2Me
3-Cl-Phenyl



354
2
SO2Me
3-Cl-Phenyl



355
3
SO2Me
3-Cl-Phenyl



356
4
SO2Me
3-Cl-Phenyl



357
1
SO2NH2
3-Cl-Phenyl



358
2
SO2NH2
3-Cl-Phenyl



359
3
SO2NH2
3-Cl-Phenyl



360
4
SO2NH2
3-Cl-Phenyl



361
1
H
2-Br-Phenyl



362
2
H
2-Br-Phenyl



363
3
H
2-Br-Phenyl



364
4
H
2-Br-Phenyl



365
1
Me
2-Br-Phenyl



366
2
Me
2-Br-Phenyl



367
3
Me
2-Br-Phenyl



368
4
Me
2-Br-Phenyl



369
1
CH2Ph
2-Br-Phenyl



370
2
CH2Ph
2-Br-Phenyl



371
3
CH2Ph
2-Br-Phenyl



372
4
CH2Ph
2-Br-Phenyl



373
1
COMe
2-Br-Phenyl



374
2
COMe
2-Br-Phenyl



375
3
COMe
2-Br-Phenyl



376
4
COMe
2-Br-Phenyl



377
1
CO2Me
2-Br-Phenyl



378
2
CO2Me
2-Br-Phenyl



379
3
CO2Me
2-Br-Phenyl



380
4
CO2Me
2-Br-Phenyl



381
1
CO2tBu
2-Br-Phenyl



382
2
CO2tBu
2-Br-Phenyl



383
3
CO2tBu
2-Br-Phenyl



384
4
CO2tBu
2-Br-Phenyl



385
1
CONHMe
2-Br-Phenyl



386
2
CONHMe
2-Br-Phenyl



387
3
CONHMe
2-Br-Phenyl



388
4
CONHMe
2-Br-Phenyl



389
1
SO2Me
2-Br-Phenyl



390
2
SO2Me
2-Br-Phenyl



391
3
SO2Me
2-Br-Phenyl



392
4
SO2Me
2-Br-Phenyl



393
1
SO2NH2
2-Br-Phenyl



394
2
SO2NH2
2-Br-Phenyl



395
3
SO2NH2
2-Br-Phenyl



396
4
SO2NH2
2-Br-Phenyl



397
1
H
4-Br-Phenyl



398
2
H
4-Br-Phenyl



399
3
H
4-Br-Phenyl



400
4
H
4-Br-Phenyl



401
1
Me
4-Br-Phenyl



402
2
Me
4-Br-Phenyl



403
3
Me
4-Br-Phenyl



404
4
Me
4-Br-Phenyl



405
1
CH2Ph
4-Br-Phenyl



406
2
CH2Ph
4-Br-Phenyl



407
3
CH2Ph
4-Br-Phenyl



408
4
CH2Ph
4-Br-Phenyl



409
1
COMe
4-Br-Phenyl



410
2
COMe
4-Br-Phenyl



411
3
COMe
4-Br-Phenyl



412
4
COMe
4-Br-Phenyl



413
1
CO2Me
4-Br-Phenyl



414
2
CO2Me
4-Br-Phenyl



415
3
CO2Me
4-Br-Phenyl



416
4
CO2Me
4-Br-Phenyl



417
1
CO2tBu
4-Br-Phenyl



418
2
CO2tBu
4-Br-Phenyl



419
3
CO2tBu
4-Br-Phenyl



420
4
CO2tBu
4-Br-Phenyl



421
1
CONHMe
4-Br-Phenyl



422
2
CONHMe
4-Br-Phenyl



423
3
CONHMe
4-Br-Phenyl



424
4
CONHMe
4-Br-Phenyl



425
1
SO2Me
4-Br-Phenyl



426
2
SO2Me
4-Br-Phenyl



427
3
SO2Me
4-Br-Phenyl



428
4
SO2Me
4-Br-Phenyl



429
1
SO2NH2
4-Br-Phenyl



430
2
SO2NH2
4-Br-Phenyl



431
3
SO2NH2
4-Br-Phenyl



432
4
SO2NH2
4-Br-Phenyl



433
1
H
3-CF3-Phenyl



434
2
H
3-CF3-Phenyl



435
3
H
3-CF3-Phenyl



436
4
H
3-CF3-Phenyl



437
1
Me
3-CF3-Phenyl



438
2
Me
3-CF3-Phenyl



439
3
Me
3-CF3-Phenyl



440
4
Me
3-CF3-Phenyl



441
1
CH2Ph
3-CF3-Phenyl



442
2
CH2Ph
3-CF3-Phenyl



443
3
CH2Ph
3-CF3-Phenyl



444
4
CH2Ph
3-CF3-Phenyl



445
1
COMe
3-CF3-Phenyl



446
2
COMe
3-CF3-Phenyl



447
3
COMe
3-CF3-Phenyl



448
4
COMe
3-CF3-Phenyl



449
1
CO2Me
3-CF3-Phenyl



450
2
CO2Me
3-CF3-Phenyl



451
3
CO2Me
3-CF3-Phenyl



452
4
CO2Me
3-CF3-Phenyl



453
1
CO2tBu
3-CF3-Phenyl



454
2
CO2tBu
3-CF3-Phenyl



455
3
CO2tBu
3-CF3-Phenyl



456
4
CO2tBu
3-CF3-Phenyl



457
1
CONHMe
3-CF3-Phenyl



458
2
CONHMe
3-CF3-Phenyl



459
3
CONHMe
3-CF3-Phenyl



460
4
CONHMe
3-CF3-Phenyl



461
1
SO2Me
3-CF3-Phenyl



462
2
SO2Me
3-CF3-Phenyl



463
3
SO2Me
3-CF3-Phenyl



464
4
SO2Me
3-CF3-Phenyl



465
1
SO2NH2
3-CF3-Phenyl



466
2
SO2NH2
3-CF3-Phenyl



467
3
SO2NH2
3-CF3-Phenyl



468
4
SO2NH2
3-CF3-Phenyl



469
1
H
2-iPr-Phenyl



470
2
H
2-iPr-Phenyl



471
3
H
2-iPr-Phenyl



472
4
H
2-iPr-Phenyl



473
1
Me
2-iPr-Phenyl



474
2
Me
2-iPr-Phenyl



475
3
Me
2-iPr-Phenyl



476
4
Me
2-iPr-Phenyl



477
1
CH2Ph
2-iPr-Phenyl



478
2
CH2Ph
2-iPr-Phenyl



479
3
CH2Ph
2-iPr-Phenyl



480
4
CH2Ph
2-iPr-Phenyl



481
1
COMe
2-iPr-Phenyl



482
2
COMe
2-iPr-Phenyl



483
3
COMe
2-iPr-Phenyl



484
4
COMe
2-iPr-Phenyl



485
1
CO2Me
2-iPr-Phenyl



486
2
CO2Me
2-iPr-Phenyl



487
3
CO2Me
2-iPr-Phenyl



488
4
CO2Me
2-iPr-Phenyl



489
1
CO2tBu
2-iPr-Phenyl



490
2
CO2tBu
2-iPr-Phenyl



491
3
CO2tBu
2-iPr-Phenyl



492
4
CO2tBu
2-iPr-Phenyl



493
1
CONHMe
2-iPr-Phenyl



494
2
CONHMe
2-iPr-Phenyl



495
3
CONHMe
2-iPr-Phenyl



496
4
CONHMe
2-iPr-Phenyl



497
1
SO2Me
2-iPr-Phenyl



498
2
SO2Me
2-iPr-Phenyl



499
3
SO2Me
2-iPr-Phenyl



500
4
SO2Me
2-iPr-Phenyl



501
1
SO2NH2
2-iPr-Phenyl



502
2
SO2NH2
2-iPr-Phenyl



503
3
SO2NH2
2-iPr-Phenyl



504
4
SO2NH2
2-iPr-Phenyl



505
1
H
4-iPr-Phenyl



506
2
H
4-iPr-Phenyl



507
3
H
4-iPr-Phenyl



508
4
H
4-iPr-Phenyl



509
1
Me
4-iPr-Phenyl



510
2
Me
4-iPr-Phenyl



511
3
Me
4-iPr-Phenyl



512
4
Me
4-iPr-Phenyl



513
1
CH2Ph
4-iPr-Phenyl



514
2
CH2Ph
4-iPr-Phenyl



515
3
CH2Ph
4-iPr-Phenyl



516
4
CH2Ph
4-iPr-Phenyl



517
1
COMe
4-iPr-Phenyl



518
2
COMe
4-iPr-Phenyl



519
3
COMe
4-iPr-Phenyl



520
4
COMe
4-iPr-Phenyl



521
1
CO2Me
4-iPr-Phenyl



522
2
CO2Me
4-iPr-Phenyl



523
3
CO2Me
4-iPr-Phenyl



524
4
CO2Me
4-iPr-Phenyl



525
1
CO2tBu
4-iPr-Phenyl



526
2
CO2tBu
4-iPr-Phenyl



527
3
CO2tBu
4-iPr-Phenyl



528
4
CO2tBu
4-iPr-Phenyl



529
1
CONHMe
4-iPr-Phenyl



530
2
CONHMe
4-iPr-Phenyl



531
3
CONHMe
4-iPr-Phenyl



532
4
CONHMe
4-iPr-Phenyl



533
1
SO2Me
4-iPr-Phenyl



534
2
SO2Me
4-iPr-Phenyl



535
3
SO2Me
4-iPr-Phenyl



536
4
SO2Me
4-iPr-Phenyl



537
1
SO2NH2
4-iPr-Phenyl



538
2
SO2NH2
4-iPr-Phenyl



539
3
SO2NH2
4-iPr-Phenyl



540
4
SO2NH2
4-iPr-Phenyl



541
1
H
3-NH2-Phenyl



542
2
H
3-NH2-Phenyl



543
3
H
3-NH2-Phenyl



544
4
H
3-NH2-Phenyl



545
1
Me
3-NH2-Phenyl



546
2
Me
3-NH2-Phenyl



547
3
Me
3-NH2-Phenyl



548
4
Me
3-NH2-Phenyl



549
1
CH2Ph
3-NH2-Phenyl



550
2
CH2Ph
3-NH2-Phenyl



551
3
CH2Ph
3-NH2-Phenyl



552
4
CH2Ph
3-NH2-Phenyl



553
1
COMe
3-NH2-Phenyl



554
2
COMe
3-NH2-Phenyl



555
3
COMe
3-NH2-Phenyl



556
4
COMe
3-NH2-Phenyl



557
1
CO2Me
3-NH2-Phenyl



558
2
CO2Me
3-NH2-Phenyl



559
3
CO2Me
3-NH2-Phenyl



560
4
CO2Me
3-NH2-Phenyl



561
1
CO2tBu
3-NH2-Phenyl



562
2
CO2tBu
3-NH2-Phenyl



563
3
CO2tBu
3-NH2-Phenyl



564
4
CO2tBu
3-NH2-Phenyl



565
1
CONHMe
3-NH2-Phenyl



566
2
CONHMe
3-NH2-Phenyl



567
3
CONHMe
3-NH2-Phenyl



568
4
CONHMe
3-NH2-Phenyl



569
1
SO2Me
3-NH2-Phenyl



570
2
SO2Me
3-NH2-Phenyl



571
3
SO2Me
3-NH2-Phenyl



572
4
SO2Me
3-NH2-Phenyl



573
1
SO2NH2
3-NH2-Phenyl



574
2
SO2NH2
3-NH2-Phenyl



575
3
SO2NH2
3-NH2-Phenyl



576
4
SO2NH2
3-NH2-Phenyl



577
1
H
2,4-di-Me-Phenyl



578
2
H
2,4-di-Me-Phenyl



579
3
H
2,4-di-Me-Phenyl



580
4
H
2,4-di-Me-Phenyl



581
1
Me
2,4-di-Me-Phenyl



582
2
Me
2,4-di-Me-Phenyl



583
3
Me
2,4-di-Me-Phenyl



584
4
Me
2,4-di-Me-Phenyl



585
1
CH2Ph
2,4-di-Me-Phenyl



586
2
CH2Ph
2,4-di-Me-Phenyl



587
3
CH2Ph
2,4-di-Me-Phenyl



588
4
CH2Ph
2,4-di-Me-Phenyl



589
1
COMe
2,4-di-Me-Phenyl



590
2
COMe
2,4-di-Me-Phenyl



591
3
COMe
2,4-di-Me-Phenyl



592
4
COMe
2,4-di-Me-Phenyl



593
1
CO2Me
2,4-di-Me-Phenyl



594
2
CO2Me
2,4-di-Me-Phenyl



595
3
CO2Me
2,4-di-Me-Phenyl



596
4
CO2Me
2,4-di-Me-Phenyl



597
1
CO2tBu
2,4-di-Me-Phenyl



598
2
CO2tBu
2,4-di-Me-Phenyl



599
3
CO2tBu
2,4-di-Me-Phenyl



600
4
CO2tBu
2,4-di-Me-Phenyl



601
1
CONHMe
2,4-di-Me-Phenyl



602
2
CONHMe
2,4-di-Me-Phenyl



603
3
CONHMe
2,4-di-Me-Phenyl



604
4
CONHMe
2,4-di-Me-Phenyl



605
1
SO2Me
2,4-di-Me-Phenyl



606
2
SO2Me
2,4-di-Me-Phenyl



607
3
SO2Me
2,4-di-Me-Phenyl



608
4
SO2Me
2,4-di-Me-Phenyl



609
1
SO2NH2
2,4-di-Me-Phenyl



610
2
SO2NH2
2,4-di-Me-Phenyl



611
3
SO2NH2
2,4-di-Me-Phenyl



612
4
SO2NH2
2,4-di-Me-Phenyl



613
1
H
2,6-di-iPr-Phenyl



614
2
H
2,6-di-iPr-Phenyl



615
3
H
2,6-di-iPr-Phenyl



616
4
H
2,6-di-iPr-Phenyl



617
1
Me
2,6-di-iPr-Phenyl



618
2
Me
2,6-di-iPr-Phenyl



619
3
Me
2,6-di-iPr-Phenyl



620
4
Me
2,6-di-iPr-Phenyl



621
1
CH2Ph
2,6-di-iPr-Phenyl



622
2
CH2Ph
2,6-di-iPr-Phenyl



623
3
CH2Ph
2,6-di-iPr-Phenyl



624
3
CH2Ph
2,6-di-iPr-Phenyl



625
1
COMe
2,6-di-iPr-Phenyl



626
2
COMe
2,6-di-iPr-Phenyl



627
3
COMe
2,6-di-iPr-Phenyl



628
4
COMe
2,6-di-iPr-Phenyl



629
1
CO2Me
2,6-di-iPr-Phenyl



630
2
CO2Me
2,6-di-iPr-Phenyl



631
3
CO2Me
2,6-di-iPr-Phenyl



632
4
CO2Me
2,6-di-iPr-Phenyl



633
1
CO2tBu
2,6-di-iPr-Phenyl



634
2
CO2tBu
2,6-di-iPr-Phenyl



635
3
CO2tBu
2,6-di-iPr-Phenyl



636
4
CO2tBu
2,6-di-iPr-Phenyl



637
1
CONHMe
2,6-di-iPr-Phenyl



638
2
CONHMe
2,6-di-iPr-Phenyl



639
3
CONHMe
2,6-di-iPr-Phenyl



640
4
CONHMe
2,6-di-iPr-Phenyl



641
1
SO2Me
2,6-di-iPr-Phenyl



642
2
SO2Me
2,6-di-iPr-Phenyl



643
3
SO2Me
2,6-di-iPr-Phenyl



644
4
SO2Me
2,6-di-iPr-Phenyl



645
1
SO2NH2
2,6-di-iPr-Phenyl



646
2
SO2NH2
2,6-di-iPr-Phenyl



647
3
SO2NH2
2,6-di-iPr-Phenyl



648
4
SO2NH2
2,6-di-iPr-Phenyl



649
1
H
3-Ph-Phenyl



650
2
H
3-Ph-Phenyl



651
3
H
3-Ph-Phenyl



652
4
H
3-Ph-Phenyl



653
1
Me
3-Ph-Phenyl



654
2
Me
3-Ph-Phenyl



655
3
Me
3-Ph-Phenyl



656
4
Me
3-Ph-Phenyl



657
1
CH2Ph
3-Ph-Phenyl



658
2
CH2Ph
3-Ph-Phenyl



659
3
CH2Ph
3-Ph-Phenyl



660
4
CH2Ph
3-Ph-Phenyl



661
1
COMe
3-Ph-Phenyl



662
2
COMe
3-Ph-Phenyl



663
3
COMe
3-Ph-Phenyl



664
4
COMe
3-Ph-Phenyl



665
1
CO2Me
3-Ph-Phenyl



666
2
CO2Me
3-Ph-Phenyl



667
3
CO2Me
3-Ph-Phenyl



668
4
CO2Me
3-Ph-Phenyl



669
1
CO2tBu
3-Ph-Phenyl



670
2
CO2tBu
3-Ph-Phenyl



671
3
CO2tBu
3-Ph-Phenyl



672
4
CO2tBu
3-Ph-Phenyl



673
1
CONHMe
3-Ph-Phenyl



674
2
CONHMe
3-Ph-Phenyl



675
3
CONHMe
3-Ph-Phenyl



676
4
CONHMe
3-Ph-Phenyl



677
1
SO2Me
3-Ph-Phenyl



678
2
SO2Me
3-Ph-Phenyl



679
3
SO2Me
3-Ph-Phenyl



680
4
SO2Me
3-Ph-Phenyl



681
1
SO2NH2
3-Ph-Phenyl



682
2
SO2NH2
3-Ph-Phenyl



683
3
SO2NH2
3-Ph-Phenyl



684
4
SO2NH2
3-Ph-Phenyl



685
1
H
2-morpholino-






phenyl



686
2
H
2-morpholino-






phenyl



687
3
H
2-morpholino-






phenyl



688
4
H
2-morpholino-






phenyl



689
1
Me
2-morpholino-






phenyl



690
2
Me
2-morpholino-






phenyl



691
3
Me
2-morpholino-






phenyl



692
4
Me
2-morpholino-






phenyl



693
1
CH2Ph
2-morpholino-






phenyl



694
2
CH2Ph
2-morpholino-






phenyl



695
3
CH2Ph
2-morpholino-






phenyl



696
4
CH2Ph
2-morpholino-






phenyl



697
1
COMe
2-morpholino-






phenyl



698
2
COMe
2-morpholino-






phenyl



699
3
COMe
2-morpholino-






phenyl



700
4
COMe
2-morpholino-






phenyl



701
1
CO2Me
2-morpholino-






phenyl



702
2
CO2Me
2-morpholino-






phenyl



703
3
CO2Me
2-morpholino-






phenyl



704
4
CO2Me
2-morpholino-






phenyl



705
1
CO2tBu
2-morpholino-






phenyl



706
2
CO2tBu
2-morpholino-






phenyl



707
3
CO2tBu
2-morpholino-






phenyl



708
4
CO2tBu
2-morpholino-






phenyl



709
1
CONHMe
2-morpholino-






phenyl



710
2
CONHMe
2-morpholino-






phenyl



711
3
CONHMe
2-morpholino-






phenyl



712
4
CONHMe
2-morpholino-






phenyl



713
1
SO2Me
2-morpholino-






phenyl



714
2
SO2Me
2-morpholino-






phenyl



715
3
SO2Me
2-morpholino-






phenyl



716
4
SO2Me
2-morpholino-






phenyl



717
1
SO2NH2
2-morpholino-






phenyl



718
2
SO2NH2
2-morpholino-






phenyl



719
3
SO2NH2
2-morpholino-






phenyl



720
4
SO2NH2
2-morpholino-






phenyl



721
1
H
4-morpholino-






phenyl



722
2
H
4-morpholino-






phenyl



723
3
H
4-morpholino-






phenyl



724
4
H
4-morpholino-






phenyl



725
1
CH2Ph
4-morpholino-






phenyl



726
2
CH2Ph
4-morpholino-






phenyl



727
3
CH2Ph
4-morpholino-






phenyl



728
4
CH2Ph
4-morpholino-






phenyl



729
1
CO2Me
4-morpholino-






phenyl



730
2
CO2Me
4-morpholino-






phenyl



731
3
CO2Me
4-morpholino-






phenyl



732
4
CO2Me
4-morpholino-






phenyl



733
1
CONHMe
4-morpholino-






phenyl



734
2
CONHMe
4-morpholino-






phenyl



735
3
CONHMe
4-morpholino-






phenyl



736
4
CONHMe
4-morpholino-






phenyl



737
1
SO2NH2
4-morpholino-






phenyl



738
2
SO2NH2
4-morpholino-






phenyl



739
3
SO2NH2
4-morpholino-






phenyl



740
1
H
naphthylen-1-yl



741
2
H
naphthylen-1-yl



742
3
H
naphthylen-1-yl



743
4
H
naphthylen-1-yl



744
1
Me
naphthylen-1-yl



745
2
Me
naphthylen-1-yl



746
3
Me
naphthylen-1-yl



747
4
Me
naphthylen-1-yl



748
1
CH2Ph
naphthylen-1-yl



749
2
CH2Ph
naphthylen-1-yl



750
3
CH2Ph
naphthylen-1-yl



751
4
CH2Ph
naphthylen-1-yl



752
1
COMe
naphthylen-1-yl



753
2
COMe
naphthylen-1-yl



754
3
COMe
naphthylen-1-yl



755
4
COMe
naphthylen-1-yl



756
1
CO2Me
naphthylen-1-yl



757
2
CO2Me
naphthylen-1-yl



758
3
CO2Me
naphthylen-1-yl



759
4
CO2Me
naphthylen-1-yl



760
1
CO2tBu
naphthylen-1-yl



761
2
CO2tBu
naphthylen-1-yl



762
3
CO2tBu
naphthylen-1-yl



763
4
CO2tBu
naphthylen-1-yl



764
1
CONHMe
naphthylen-1-yl



765
2
CONHMe
naphthylen-1-yl



767
3
CONHMe
naphthylen-1-yl



768
4
CONHMe
naphthylen-1-yl



769
1
SO2Me
naphthylen-1-yl



770
2
SO2Me
naphthylen-1-yl



771
3
SO2Me
naphthylen-1-yl



772
4
SO2Me
naphthylen-1-yl



773
1
SO2NH2
naphthylen-1-yl



774
2
SO2NH2
naphthylen-1-yl



775
3
SO2NH2
naphthylen-1-yl



778
4
SO2NH2
naphthylen-1-yl



779
1
H
4-OH-Phenyl



780
2
H
4-OH-Phenyl



781
3
H
4-OH-Phenyl



782
4
H
4-OH-Phenyl



783
1
Me
4-OH-Phenyl



784
2
Me
4-OH-Phenyl



785
3
Me
4-OH-Phenyl



786
4
Me
4-OH-Phenyl



787
1
CH2Ph
4-OH-Phenyl



788
2
CH2Ph
4-OH-Phenyl



789
3
CH2Ph
4-OH-Phenyl



790
4
CH2Ph
4-OH-Phenyl



791
1
COMe
4-OH-Phenyl



792
2
COMe
4-OH-Phenyl



793
3
COMe
4-OH-Phenyl



794
4
COMe
4-OH-Phenyl



795
1
CO2Me
4-OH-Phenyl



796
2
CO2Me
4-OH-Phenyl



797
3
CO2Me
4-OH-Phenyl



798
4
CO2Me
4-OH-Phenyl



799
1
CO2tBu
4-OH-Phenyl



800
2
CO2tBu
4-OH-Phenyl



801
3
CO2tBu
4-OH-Phenyl



802
4
CO2tBu
4-OH-Phenyl



803
1
CONHMe
4-OH-Phenyl



804
2
CONHMe
4-OH-Phenyl



805
3
CONHMe
4-OH-Phenyl



806
4
CONHMe
4-OH-Phenyl



807
1
SO2Me
4-OH-Phenyl



808
2
SO2Me
4-OH-Phenyl



809
3
SO2Me
4-OH-Phenyl



810
4
SO2Me
4-OH-Phenyl



811
1
SO2NH2
4-OH-Phenyl



812
2
SO2NH2
4-OH-Phenyl



813
3
SO2NH2
4-OH-Phenyl



814
4
SO2NH2
4-OH-Phenyl



815
1
H
2-OH-Phenyl



816
2
H
2-OH-Phenyl



817
3
H
2-OH-Phenyl



818
4
H
2-OH-Phenyl



819
1
Me
2-OH-Phenyl



820
2
Me
2-OH-Phenyl



821
3
Me
2-OH-Phenyl



822
4
Me
2-OH-Phenyl



823
1
CH2Ph
2-OH-Phenyl



824
2
CH2Ph
2-OH-Phenyl



825
3
CH2Ph
2-OH-Phenyl



826
4
CH2Ph
2-OH-Phenyl



827
1
COMe
2-OH-Phenyl



828
2
COMe
2-OH-Phenyl



829
3
COMe
2-OH-Phenyl



830
4
COMe
2-OH-Phenyl



831
1
CO2Me
2-OH-Phenyl



832
2
CO2Me
2-OH-Phenyl



833
3
CO2Me
2-OH-Phenyl



834
4
CO2Me
2-OH-Phenyl



835
1
CO2tBu
2-OH-Phenyl



836
2
CO2tBu
2-OH-Phenyl



837
3
CO2tBu
2-OH-Phenyl



838
4
CO2tBu
2-OH-Phenyl



839
1
CONHMe
2-OH-Phenyl



840
2
CONHMe
2-OH-Phenyl



841
3
CONHMe
2-OH-Phenyl



842
4
CONHMe
2-OH-Phenyl



843
1
SO2Me
2-OH-Phenyl



844
2
SO2Me
2-OH-Phenyl



845
3
SO2Me
2-OH-Phenyl



846
4
SO2Me
2-OH-Phenyl



847
1
SO2NH2
2-OH-Phenyl



848
2
SO2NH2
2-OH-Phenyl



849
3
SO2NH2
2-OH-Phenyl



850
4
SO2NH2
2-OH-Phenyl



851
1
H
4-OMe-Phenyl



852
2
H
4-OMe-Phenyl



853
3
H
4-OMe-Phenyl



854
4
H
4-OMe-Phenyl



855
1
Me
4-OMe-Phenyl



856
2
Me
4-OMe-Phenyl



857
3
Me
4-OMe-Phenyl



858
4
Me
4-OMe-Phenyl



859
1
CH2Ph
4-OMe-Phenyl



860
2
CH2Ph
4-OMe-Phenyl



861
3
CH2Ph
4-OMe-Phenyl



862
4
CH2Ph
4-OMe-Phenyl



863
1
COMe
4-OMe-Phenyl



864
2
COMe
4-OMe-Phenyl



865
3
COMe
4-OMe-Phenyl



866
4
COMe
4-OMe-Phenyl



867
1
CO2Me
4-OMe-Phenyl



868
2
CO2Me
4-OMe-Phenyl



869
3
CO2Me
4-OMe-Phenyl



870
4
CO2Me
4-OMe-Phenyl



871
1
CO2tBu
4-OMe-Phenyl



872
2
CO2tBu
4-OMe-Phenyl



873
3
CO2tBu
4-OMe-Phenyl



874
4
CO2tBu
4-OMe-Phenyl



875
1
CONHMe
4-OMe-Phenyl



876
2
CONHMe
4-OMe-Phenyl



877
3
CONHMe
4-OMe-Phenyl



878
4
CONHMe
4-OMe-Phenyl



879
1
SO2Me
4-OMe-Phenyl



880
2
SO2Me
4-OMe-Phenyl



881
3
SO2Me
4-OMe-Phenyl



882
4
SO2Me
4-OMe-Phenyl



883
1
SO2NH2
4-OMe-Phenyl



884
2
SO2NH2
4-OMe-Phenyl



885
3
SO2NH2
4-OMe-Phenyl



886
4
SO2NH2
4-OMe-Phenyl



887
1
H
2-OMe-Phenyl



888
2
H
2-OMe-Phenyl



889
3
H
2-OMe-Phenyl



890
4
H
2-OMe-Phenyl



891
1
Me
2-OMe-Phenyl



892
2
Me
2-OMe-Phenyl



893
3
Me
2-OMe-Phenyl



894
4
Me
2-OMe-Phenyl



895
1
CH2Ph
2-OMe-Phenyl



896
2
CH2Ph
2-OMe-Phenyl



897
3
CH2Ph
2-OMe-Phenyl



898
4
CH2Ph
2-OMe-Phenyl



899
1
COMe
2-OMe-Phenyl



900
2
COMe
2-OMe-Phenyl



901
3
COMe
2-OMe-Phenyl



902
4
COMe
2-OMe-Phenyl



903
1
CO2Me
2-OMe-Phenyl



904
2
CO2Me
2-OMe-Phenyl



905
3
CO2Me
2-OMe-Phenyl



906
4
CO2Me
2-OMe-Phenyl



907
1
CO2tBu
2-OMe-Phenyl



908
2
CO2tBu
2-OMe-Phenyl



909
3
CO2tBu
2-OMe-Phenyl



910
4
CO2tBu
2-OMe-Phenyl



911
1
CONHMe
2-OMe-Phenyl



912
2
CONHMe
2-OMe-Phenyl



913
3
CONHMe
2-OMe-Phenyl



914
4
CONHMe
2-OMe-Phenyl



915
1
SO2Me
2-OMe-Phenyl



916
2
SO2Me
2-OMe-Phenyl



917
3
SO2Me
2-OMe-Phenyl



918
4
SO2Me
2-OMe-Phenyl



919
1
SO2NH2
2-OMe-Phenyl



920
2
SO2NH2
2-OMe-Phenyl



921
3
SO2NH2
2-OMe-Phenyl



922
4
SO2NH2
2-OMe-Phenyl



923
1
H
3-CN-Phenyl



924
2
H
3-CN-Phenyl



925
3
H
3-CN-Phenyl



926
4
H
3-CN-Phenyl



927
1
Me
3-CN-Phenyl



928
2
Me
3-CN-Phenyl



929
3
Me
3-CN-Phenyl



930
4
Me
3-CN-Phenyl



931
1
CH2Ph
3-CN-Phenyl



932
2
CH2Ph
3-CN-Phenyl



933
3
CH2Ph
3-CN-Phenyl



934
4
CH2Ph
3-CN-Phenyl



935
1
COMe
3-CN-Phenyl



936
2
COMe
3-CN-Phenyl



937
3
COMe
3-CN-Phenyl



938
4
COMe
3-CN-Phenyl



939
1
CO2Me
3-CN-Phenyl



940
2
CO2Me
3-CN-Phenyl



941
3
CO2Me
3-CN-Phenyl



942
4
CO2Me
3-CN-Phenyl



943
1
CO2tBu
3-CN-Phenyl



944
2
CO2tBu
3-CN-Phenyl



945
3
CO2tBu
3-CN-Phenyl



946
4
CO2tBu
3-CN-Phenyl



947
1
CONHMe
3-CN-Phenyl



948
2
CONHMe
3-CN-Phenyl



949
3
CONHMe
3-CN-Phenyl



950
4
CONHMe
3-CN-Phenyl



951
1
SO2Me
3-CN-Phenyl



952
2
SO2Me
3-CN-Phenyl



953
3
SO2Me
3-CN-Phenyl



954
4
SO2Me
3-CN-Phenyl



955
1
SO2NH2
3-CN-Phenyl



956
2
SO2NH2
3-CN-Phenyl



957
3
SO2NH2
3-CN-Phenyl



958
4
SO2NH2
3-CN-Phenyl



959
1
H
2-Me-Phenyl



960
2
H
2-Me-Phenyl



961
3
H
2-Me-Phenyl



962
4
H
2-Me-Phenyl



963
1
Me
2-Me-Phenyl



964
2
Me
2-Me-Phenyl



965
3
Me
2-Me-Phenyl



966
4
Me
2-Me-Phenyl



967
1
CH2Ph
2-Me-Phenyl



968
2
CH2Ph
2-Me-Phenyl



969
3
CH2Ph
2-Me-Phenyl



970
4
CH2Ph
2-Me-Phenyl



971
1
COMe
2-Me-Phenyl



972
2
COMe
2-Me-Phenyl



973
3
COMe
2-Me-Phenyl



974
4
COMe
2-Me-Phenyl



975
1
CO2Me
2-Me-Phenyl



976
2
CO2Me
2-Me-Phenyl



977
3
CO2Me
2-Me-Phenyl



978
4
CO2Me
2-CN-Phenyl



979
1
CO2tBu
2-Me-Phenyl



980
2
CO2tBu
2-Me-Phenyl



981
3
CO2tBu
2-Me-Phenyl



982
4
CO2tBu
2-Me-Phenyl



983
1
CONHMe
2-Me-Phenyl



984
2
CONHMe
2-Me-Phenyl



985
3
CONHMe
2-Me-Phenyl



986
4
CONHMe
2-Me-Phenyl



987
1
SO2Me
2-Me-Phenyl



988
2
SO2Me
2-Me-Phenyl



989
3
SO2Me
2-Me-Phenyl



990
4
SO2Me
2-Me-Phenyl



991
1
SO2NH2
2-Me-Phenyl



992
2
SO2NH2
2-Me-Phenyl



993
3
SO2NH2
2-Me-Phenyl



994
4
SO2NH2
2-Me-Phenyl



995
1
H
4-Me-Phenyl



996
2
H
4-Me-Phenyl



997
3
H
4-Me-Phenyl



998
4
H
4-Me-Phenyl



999
1
Me
4-Me-Phenyl



1000
2
Me
4-Me-Phenyl



1001
3
Me
4-Me-Phenyl



1002
4
Me
4-Me-Phenyl



1003
1
CH2Ph
4-Me-Phenyl



1004
2
CH2Ph
4-Me-Phenyl



1005
3
CH2Ph
4-Me-Phenyl



1006
4
CH2Ph
4-Me-Phenyl



1007
1
COMe
4-Me-Phenyl



1008
2
COMe
4-Me-Phenyl



1009
3
COMe
4-Me-Phenyl



1010
4
COMe
4-Me-Phenyl



1011
1
CO2Me
4-Me-Phenyl



1012
2
CO2Me
4-Me-Phenyl



1013
3
CO2Me
4-Me-Phenyl



1014
4
CO2Me
4-Me-Phenyl



1015
1
CO2tBu
4-Me-Phenyl



1016
2
CO2tBu
4-Me-Phenyl



1017
3
CO2tBu
4-Me-Phenyl



1018
4
CO2tBu
4-Me-Phenyl



1019
1
CONHMe
4-Me-Phenyl



1020
2
CONHMe
4-Me-Phenyl



1021
3
CONHMe
4-Me-Phenyl



1022
4
CONHMe
4-Me-Phenyl



1023
1
SO2Me
4-Me-Phenyl



1024
2
SO2Me
4-Me-Phenyl



1025
3
SO2Me
4-Me-Phenyl



1026
4
SO2Me
4-Me-Phenyl



1027
1
SO2NH2
4-Me-Phenyl



1028
2
SO2NH2
4-Me-Phenyl



1029
3
SO2NH2
4-Me-Phenyl



1030
4
SO2NH2
4-Me-Phenyl



1031
1
H
3-F-Phenyl



1032
2
H
3-F-Phenyl



1033
3
H
3-F-Phenyl



1034
4
H
3-F-Phenyl



1035
1
Me
3-F-Phenyl



1036
2
Me
3-F-Phenyl



1037
3
Me
3-F-Phenyl



1038
4
Me
3-F-Phenyl



1039
1
CH2Ph
3-F-Phenyl



1040
2
CH2Ph
3-F-Phenyl



1041
3
CH2Ph
3-F-Phenyl



1042
4
CH2Ph
3-F-Phenyl



1043
1
COMe
3-F-Phenyl



1044
2
COMe
3-F-Phenyl



1045
3
COMe
3-F-Phenyl



1046
4
COMe
3-F-Phenyl



1047
1
CO2Me
3-F-Phenyl



1048
2
CO2Me
3-F-Phenyl



1049
3
CO2Me
3-F-Phenyl



1050
4
CO2Me
3-F-Phenyl



1051
1
CO2tBu
3-F-Phenyl



1052
2
CO2tBu
3-F-Phenyl



1053
3
CO2tBu
3-F-Phenyl



1054
4
CO2tBu
3-F-Phenyl



1055
1
CONHMe
3-F-Phenyl



1056
2
CONHMe
3-F-Phenyl



1057
3
CONHMe
3-F-Phenyl



1058
4
CONHMe
3-F-Phenyl



1059
1
SO2Me
3-F-Phenyl



1060
2
SO2Me
3-F-Phenyl



1061
3
SO2Me
3-F-Phenyl



1062
4
SO2Me
3-F-Phenyl



1063
1
SO2NH2
3-F-Phenyl



1064
2
SO2NH2
3-F-Phenyl



1065
3
SO2NH2
3-F-Phenyl



1066
4
SO2NH2
3-F-Phenyl



1067
1
H
2-Cl-Phenyl



1068
2
H
2-Cl-Phenyl



1069
3
H
2-Cl-Phenyl



1070
4
H
2-Cl-Phenyl



1071
1
Me
2-Cl-Phenyl



1072
2
Me
2-Cl-Phenyl



1073
3
Me
2-Cl-Phenyl



1074
4
Me
2-Cl-Phenyl



1075
1
CH2Ph
2-Cl-Phenyl



1076
2
CH2Ph
2-Cl-Phenyl



1077
3
CH2Ph
2-Cl-Phenyl



1078
4
CH2Ph
2-Cl-Phenyl



1079
1
COMe
2-Cl-Phenyl



1080
2
COMe
2-Cl-Phenyl



1081
3
COMe
2-Cl-Phenyl



1082
4
COMe
2-Cl-Phenyl



1083
1
CO2Me
2-Cl-Phenyl



1084
2
CO2Me
2-Cl-Phenyl



1085
3
CO2Me
2-Cl-Phenyl



1086
4
CO2Me
2-Cl-Phenyl



1087
1
CO2tBu
2-Cl-Phenyl



1088
2
CO2tBu
2-Cl-Phenyl



1089
3
CO2tBu
2-Cl-Phenyl



1090
4
CO2tBu
2-Cl-Phenyl



1091
1
CONHMe
2-Cl-Phenyl



1092
2
CONHMe
2-Cl-Phenyl



1093
3
CONHMe
2-Cl-Phenyl



1094
4
CONHMe
2-Cl-Phenyl



1095
1
SO2Me
2-Cl-Phenyl



1096
2
SO2Me
2-Cl-Phenyl



1097
3
SO2Me
2-Cl-Phenyl



1098
4
SO2Me
2-Cl-Phenyl



1099
1
SO2NH2
2-Cl-Phenyl



1100
2
SO2NH2
2-Cl-Phenyl



1101
3
SO2NH2
2-Cl-Phenyl



1102
4
SO2NH2
2-Cl-Phenyl



1103
1
H
4-Cl-Phenyl



1104
2
H
4-Cl-Phenyl



1105
3
H
4-Cl-Phenyl



1106
4
H
4-Cl-Phenyl



1107
1
Me
4-Cl-Phenyl



1108
2
Me
4-Cl-Phenyl



1109
3
Me
4-Cl-Phenyl



1110
4
Me
4-Cl-Phenyl



1111
1
CH2Ph
4-Cl-Phenyl



1112
2
CH2Ph
4-Cl-Phenyl



1113
3
CH2Ph
4-Cl-Phenyl



1114
4
CH2Ph
4-Cl-Phenyl



1115
1
COMe
4-Cl-Phenyl



1116
2
COMe
4-Cl-Phenyl



1117
3
COMe
4-Cl-Phenyl



1118
4
COMe
4-Cl-Phenyl



1119
1
CO2Me
4-Cl-Phenyl



1120
2
CO2Me
4-Cl-Phenyl



1121
3
CO2Me
4-Cl-Phenyl



1122
4
CO2Me
4-Cl-Phenyl



1123
1
CO2tBu
4-Cl-Phenyl



1124
2
CO2tBu
4-Cl-Phenyl



1125
3
CO2tBu
4-Cl-Phenyl



1126
4
CO2tBu
4-Cl-Phenyl



1127
1
CONHMe
4-Cl-Phenyl



1128
2
CONHMe
4-Cl-Phenyl



1129
3
CONHMe
4-Cl-Phenyl



1130
4
CONHMe
4-Cl-Phenyl



1131
1
SO2Me
4-Cl-Phenyl



1132
2
SO2Me
4-Cl-Phenyl



1133
3
SO2Me
4-Cl-Phenyl



1134
4
SO2Me
4-Cl-Phenyl



1135
1
SO2NH2
4-Cl-Phenyl



1136
2
SO2NH2
4-Cl-Phenyl



1137
3
SO2NH2
4-Cl-Phenyl



1138
4
SO2NH2
4-Cl-Phenyl



1139
1
H
3-Br-Phenyl



1140
2
H
3-Br-Phenyl



1141
3
H
3-Br-Phenyl



1142
4
H
3-Br-Phenyl



1143
1
Me
3-Br-Phenyl



1144
2
Me
3-Br-Phenyl



1145
3
Me
3-Br-Phenyl



1146
4
Me
3-Br-Phenyl



1147
1
CH2Ph
3-Br-Phenyl



1148
2
CH2Ph
3-Br-Phenyl



1149
3
CH2Ph
3-Br-Phenyl



1150
4
CH2Ph
3-Br-Phenyl



1151
1
COMe
3-Br-Phenyl



1152
2
COMe
3-Br-Phenyl



1153
3
COMe
3-Br-Phenyl



1154
4
COMe
3-Br-Phenyl



1155
1
CO2Me
3-Br-Phenyl



1156
2
CO2Me
3-Br-Phenyl



1157
3
CO2Me
3-Br-Phenyl



1158
4
CO2Me
3-Br-Phenyl



1159
1
CO2tBu
3-Br-Phenyl



1160
2
CO2tBu
3-Br-Phenyl



1161
3
CO2tBu
3-Br-Phenyl



1162
4
CO2tBu
3-Br-Phenyl



1163
1
CONHMe
3-Br-Phenyl



1164
2
CONHMe
3-Br-Phenyl



1165
3
CONHMe
3-Br-Phenyl



1166
4
CONHMe
3-Br-Phenyl



1167
1
SO2Me
3-Br-Phenyl



1168
2
SO2Me
3-Br-Phenyl



1169
3
SO2Me
3-Br-Phenyl



1170
4
SO2Me
3-Br-Phenyl



1171
1
SO2NH2
3-Br-Phenyl



1172
2
SO2NH2
3-Br-Phenyl



1173
3
SO2NH2
3-Br-Phenyl



1174
4
SO2NH2
3-Br-Phenyl



1175
1
H
2-CF3-Phenyl



1176
2
H
2-CF3-Phenyl



1177
3
H
2-CF3-Phenyl



1178
4
H
2-CF3-Phenyl



1179
1
Me
2-CF3-Phenyl



1180
2
Me
2-CF3-Phenyl



1181
3
Me
2-CF3-Phenyl



1182
4
Me
2-CF3-Phenyl



1183
1
CH2Ph
2-CF3-Phenyl



1184
2
CH2Ph
2-CF3-Phenyl



1185
3
CH2Ph
2-CF3-Phenyl



1186
4
CH2Ph
2-CF3-Phenyl



1187
1
COMe
2-CF3-Phenyl



1188
2
COMe
2-CF3-Phenyl



1189
3
COMe
2-CF3-Phenyl



1190
4
COMe
2-CF3-Phenyl



1191
1
CO2Me
2-CF3-Phenyl



1192
2
CO2Me
2-CF3-Phenyl



1193
3
CO2Me
2-CF3-Phenyl



1194
4
CO2Me
2-CF3-Phenyl



1195
1
CO2tBu
2-CF3-Phenyl



1196
2
CO2tBu
2-CF3-Phenyl



1197
3
CO2tBu
2-CF3-Phenyl



1198
4
CO2tBu
2-CF3-Phenyl



1199
1
CONHMe
2-CF3-Phenyl



1200
2
CONHMe
2-CF3-Phenyl



1201
3
CONHMe
2-CF3-Phenyl



1202
4
CONHMe
2-CF3-Phenyl



1203
1
SO2Me
2-CF3-Phenyl



1204
2
SO2Me
2-CF3-Phenyl



1205
3
SO2Me
2-CF3-Phenyl



1206
4
SO2Me
2-CF3-Phenyl



1207
1
SO2NH2
2-CF3-Phenyl



1208
2
SO2NH2
2-CF3-Phenyl



1209
3
SO2NH2
2-CF3-Phenyl



1210
4
SO2NH2
2-CF3-Phenyl



1211
1
H
4-CF3-Phenyl



1212
2
H
4-CF3-Phenyl



1213
3
H
4-CF3-Phenyl



1214
4
H
4-CF3-Phenyl



1215
1
Me
4-CF3-Phenyl



1216
2
Me
4-CF3-Phenyl



1217
3
Me
4-CF3-Phenyl



1218
4
Me
4-CF3-Phenyl



1219
1
CH2Ph
4-CF3-Phenyl



1220
2
CH2Ph
4-CF3-Phenyl



1221
3
CH2Ph
4-CF3-Phenyl



1222
4
CH2Ph
4-CF3-Phenyl



1223
1
COMe
4-CF3-Phenyl



1224
2
COMe
4-CF3-Phenyl



1225
3
COMe
4-CF3-Phenyl



1226
4
COMe
4-CF3-Phenyl



1227
1
CO2Me
4-CF3-Phenyl



1228
2
CO2Me
4-CF3-Phenyl



1229
3
CO2Me
4-CF3-Phenyl



1230
4
CO2Me
4-CF3-Phenyl



1231
1
CO2tBu
4-CF3-Phenyl



1232
2
CO2tBu
4-CF3-Phenyl



1233
3
CO2tBu
4-CF3-Phenyl



1234
4
CO2tBu
4-CF3-Phenyl



1235
1
CONHMe
4-CF3-Phenyl



1236
2
CONHMe
4-CF3-Phenyl



1237
3
CONHMe
4-CF3-Phenyl



1238
4
CONHMe
4-CF3-Phenyl



1239
1
SO2Me
4-CF3-Phenyl



1240
2
SO2Me
4-CF3-Phenyl



1241
3
SO2Me
4-CF3-Phenyl



1242
4
SO2Me
4-CF3-Phenyl



1243
1
SO2NH2
4-CF3-Phenyl



1244
2
SO2NH2
4-CF3-Phenyl



1245
3
SO2NH2
4-CF3-Phenyl



1246
4
SO2NH2
4-CF3-Phenyl



1247
1
H
3-iPr-Phenyl



1248
2
H
3-iPr-Phenyl



1249
3
H
3-iPr-Phenyl



1250
4
H
3-iPr-Phenyl



1251
1
Me
3-iPr-Phenyl



1252
2
Me
3-iPr-Phenyl



1253
3
Me
3-iPr-Phenyl



1254
4
Me
3-iPr-Phenyl



1255
1
CH2Ph
3-iPr-Phenyl



1256
2
CH2Ph
3-iPr-Phenyl



1257
3
CH2Ph
3-iPr-Phenyl



1258
4
CH2Ph
3-iPr-Phenyl



1259
1
COMe
3-iPr-Phenyl



1260
2
COMe
3-iPr-Phenyl



1261
3
COMe
3-iPr-Phenyl



1262
4
COMe
3-iPr-Phenyl



1263
1
CO2Me
3-iPr-Phenyl



1264
2
CO2Me
3-iPr-Phenyl



1265
3
CO2Me
3-iPr-Phenyl



1266
4
CO2Me
3-iPr-Phenyl



1267
1
CO2tBu
3-iPr-Phenyl



1268
2
CO2tBu
3-iPr-Phenyl



1269
3
CO2tBu
3-iPr-Phenyl



1270
4
CO2tBu
3-iPr-Phenyl



1271
1
CONHMe
3-iPr-Phenyl



1272
2
CONHMe
3-iPr-Phenyl



1273
3
CONHMe
3-iPr-Phenyl



1274
4
CONHMe
3-iPr-Phenyl



1275
1
SO2Me
3-iPr-Phenyl



1276
2
SO2Me
3-iPr-Phenyl



1277
3
SO2Me
3-iPr-Phenyl



1278
4
SO2Me
3-iPr-Phenyl



1279
1
SO2NH2
3-iPr-Phenyl



1280
2
SO2NH2
3-iPr-Phenyl



1281
3
SO2NH2
3-iPr-Phenyl



1282
4
SO2NH2
3-iPr-Phenyl



1283
1
H
4-NH2-Phenyl



1284
2
H
4-NH2-Phenyl



1285
3
H
4-NH2-Phenyl



1286
4
H
4-NH2-Phenyl



1287
1
Me
4-NH2-Phenyl



1288
2
Me
4-NH2-Phenyl



1289
3
Me
4-NH2-Phenyl



1290
4
Me
4-NH2-Phenyl



1291
1
CH2Ph
4-NH2-Phenyl



1292
2
CH2Ph
4-NH2-Phenyl



1293
3
CH2Ph
4-NH2-Phenyl



1294
4
CH2Ph
4-NH2-Phenyl



1295
1
COMe
4-NH2-Phenyl



1296
2
COMe
4-NH2-Phenyl



1297
3
COMe
4-NH2-Phenyl



1298
4
COMe
4-NH2-Phenyl



1299
1
CO2Me
4-NH2-Phenyl



1300
2
CO2Me
4-NH2-Phenyl



1301
3
CO2Me
4-NH2-Phenyl



1302
4
CO2Me
4-NH2-Phenyl



1303
1
CO2tBu
4-NH2-Phenyl



1304
2
CO2tBu
4-NH2-Phenyl



1305
3
CO2tBu
4-NH2-Phenyl



1306
4
CO2tBu
4-NH2-Phenyl



1307
1
CONHMe
4-NH2-Phenyl



1308
2
CONHMe
4-NH2-Phenyl



1309
3
CONHMe
4-NH2-Phenyl



1310
4
CONHMe
4-NH2-Phenyl



1311
1
SO2Me
4-NH2-Phenyl



1312
2
SO2Me
4-NH2-Phenyl



1313
3
SO2Me
4-NH2-Phenyl



1314
4
SO2Me
4-NH2-Phenyl



1315
1
SO2NH2
4-NH2-Phenyl



1316
2
SO2NH2
4-NH2-Phenyl



1317
3
SO2NH2
4-NH2-Phenyl



1318
4
SO2NH2
4-NH2-Phenyl



1319
1
H
2-NH2-Phenyl



1320
2
H
2-NH2-Phenyl



1321
3
H
2-NH2-Phenyl



1322
4
H
2-NH2-Phenyl



1323
1
Me
2-NH2-Phenyl



1324
2
Me
2-NH2-Phenyl



1325
3
Me
2-NH2-Phenyl



1326
4
Me
2-NH2-Phenyl



1327
1
CH2Ph
2-NH2-Phenyl



1328
2
CH2Ph
2-NH2-Phenyl



1329
3
CH2Ph
2-NH2-Phenyl



1330
4
CH2Ph
2-NH2-Phenyl



1331
1
COMe
2-NH2-Phenyl



1332
2
COMe
2-NH2-Phenyl



1333
3
COMe
2-NH2-Phenyl



1334
4
COMe
2-NH2-Phenyl



1335
1
CO2Me
2-NH2-Phenyl



1336
2
CO2Me
2-NH2-Phenyl



1337
3
CO2Me
2-NH2-Phenyl



1338
4
CO2Me
2-NH2-Phenyl



1339
1
CO2tBu
2-NH2-Phenyl



1340
2
CO2tBu
2-NH2-Phenyl



1341
3
CO2tBu
2-NH2-Phenyl



1342
4
CO2tBu
2-NH2-Phenyl



1343
1
CONHMe
2-NH2-Phenyl



1344
2
CONHMe
2-NH2-Phenyl



1345
3
CONHMe
2-NH2-Phenyl



1346
4
CONHMe
2-NH2-Phenyl



1347
1
SO2Me
2-NH2-Phenyl



1348
2
SO2Me
2-NH2-Phenyl



1349
3
SO2Me
2-NH2-Phenyl



1350
4
SO2Me
2-NH2-Phenyl



1351
1
SO2NH2
2-NH2-Phenyl



1352
2
SO2NH2
2-NH2-Phenyl



1353
3
SO2NH2
2-NH2-Phenyl



1354
4
SO2NH2
2-NH2-Phenyl



1355
1
H
2,6-di-Me-Phenyl



1356
2
H
2,6-di-Me-Phenyl



1357
3
H
2,6-di-Me-Phenyl



1358
4
H
2,6-di-Me-Phenyl



1359
1
Me
2,6-di-Me-Phenyl



1360
2
Me
2,6-di-Me-Phenyl



1361
3
Me
2,6-di-Me-Phenyl



1362
4
Me
2,6-di-Me-Phenyl



1363
1
CH2Ph
2,6-di-Me-Phenyl



1364
2
CH2Ph
2,6-di-Me-Phenyl



1365
3
CH2Ph
2,6-di-Me-Phenyl



1366
4
CH2Ph
2,6-di-Me-Phenyl



1367
1
COMe
2,6-di-Me-Phenyl



1368
2
COMe
2,6-di-Me-Phenyl



1369
3
COMe
2,6-di-Me-Phenyl



1370
4
COMe
2,6-di-Me-Phenyl



1371
1
CO2Me
2,6-di-Me-Phenyl



1372
2
CO2Me
2,6-di-Me-Phenyl



1373
3
CO2Me
2,6-di-Me-Phenyl



1374
4
CO2Me
2,6-di-Me-Phenyl



1375
1
CO2tBu
2,6-di-Me-Phenyl



1376
2
CO2tBu
2,6-di-Me-Phenyl



1377
3
CO2tBu
2,6-di-Me-Phenyl



1378
4
CO2tBu
2,6-di-Me-Phenyl



1379
1
CONHMe
2,6-di-Me-Phenyl



1380
2
CONHMe
2,6-di-Me-Phenyl



1381
3
CONHMe
2,6-di-Me-Phenyl



1382
4
CONHMe
2,6-di-Me-Phenyl



1383
1
SO2Me
2,6-di-Me-Phenyl



1384
2
SO2Me
2,6-di-Me-Phenyl



1385
3
SO2Me
2,6-di-Me-Phenyl



1386
4
SO2Me
2,6-di-Me-Phenyl



1387
1
SO2NH2
2,6-di-Me-Phenyl



1388
2
SO2NH2
2,6-di-Me-Phenyl



1389
3
SO2NH2
2,6-di-Me-Phenyl



1390
4
SO2NH2
2,6-di-Me-Phenyl



1391
1
H
2-Ph-Phenyl



1392
2
H
2-Ph-Phenyl



1393
3
H
2-Ph-Phenyl



1394
4
H
2-Ph-Phenyl



1395
1
Me
2-Ph-Phenyl



1396
2
Me
2-Ph-Phenyl



1397
3
Me
2-Ph-Phenyl



1398
4
Me
2-Ph-Phenyl



1399
1
CH2Ph
2-Ph-Phenyl



1400
2
CH2Ph
2-Ph-Phenyl



1401
3
CH2Ph
2-Ph-Phenyl



1402
4
CH2Ph
2-Ph-Phenyl



1403
1
COMe
2-Ph-Phenyl



1404
2
COMe
2-Ph-Phenyl



1405
3
COMe
2-Ph-Phenyl



1406
4
COMe
2-Ph-Phenyl



1407
1
CO2Me
2-Ph-Phenyl



1408
2
CO2Me
2-Ph-Phenyl



1409
3
CO2Me
2-Ph-Phenyl



1410
4
CO2Me
2-Ph-Phenyl



1411
1
CO2tBu
2-Ph-Phenyl



1412
2
CO2tBu
2-Ph-Phenyl



1413
3
CO2tBu
2-Ph-Phenyl



1414
4
CO2tBu
2-Ph-Phenyl



1415
1
CONHMe
2-Ph-Phenyl



1416
2
CONHMe
2-Ph-Phenyl



1417
3
CONHMe
2-Ph-Phenyl



1418
4
CONHMe
2-Ph-Phenyl



1419
1
SO2Me
2-Ph-Phenyl



1420
2
SO2Me
2-Ph-Phenyl



1421
3
SO2Me
2-Ph-Phenyl



1422
4
SO2Me
2-Ph-Phenyl



1423
1
SO2NH2
2-Ph-Phenyl



1424
2
SO2NH2
2-Ph-Phenyl



1425
3
SO2NH2
2-Ph-Phenyl



1426
4
SO2NH2
2-Ph-Phenyl



1427
1
H
4-Ph-Phenyl



1428
2
H
4-Ph-Phenyl



1429
3
H
4-Ph-Phenyl



1430
4
H
4-Ph-Phenyl



1431
1
Me
4-Ph-Phenyl



1432
2
Me
4-Ph-Phenyl



1433
3
Me
4-Ph-Phenyl



1434
4
Me
4-Ph-Phenyl



1435
1
CH2Ph
4-Ph-Phenyl



1436
2
CH2Ph
4-Ph-Phenyl



1437
3
CH2Ph
4-Ph-Phenyl



1438
4
CH2Ph
4-Ph-Phenyl



1439
1
COMe
4-Ph-Phenyl



1440
2
COMe
4-Ph-Phenyl



1441
3
COMe
4-Ph-Phenyl



1442
4
COMe
4-Ph-Phenyl



1443
1
CO2Me
4-Ph-Phenyl



1444
2
CO2Me
4-Ph-Phenyl



1445
3
CO2Me
4-Ph-Phenyl



1446
4
CO2Me
4-Ph-Phenyl



1447
1
CO2tBu
4-Ph-Phenyl



1448
2
CO2tBu
4-Ph-Phenyl



1449
3
CO2tBu
4-Ph-Phenyl



1450
4
CO2tBu
4-Ph-Phenyl



1451
1
CONHMe
4-Ph-Phenyl



1452
2
CONHMe
4-Ph-Phenyl



1453
3
CONHMe
4-Ph-Phenyl



1454
4
CONHMe
4-Ph-Phenyl



1455
1
SO2Me
4-Ph-Phenyl



1456
2
SO2Me
4-Ph-Phenyl



1457
3
SO2Me
4-Ph-Phenyl



1458
4
SO2Me
4-Ph-Phenyl



1459
1
SO2NH2
4-Ph-Phenyl



1460
2
SO2NH2
4-Ph-Phenyl



1461
3
SO2NH2
4-Ph-Phenyl



1462
4
SO2NH2
4-Ph-Phenyl



1463
1
H
3-morpholino-






phenyl



1464
2
H
3-morpholino-






phenyl



1465
3
H
3-morpholino-






phenyl



1466
4
H
3-morpholino-






phenyl



1467
1
Me
3-morpholino-






phenyl



1468
2
Me
3-morpholino-






phenyl



1469
3
Me
3-morpholino-






phenyl



1470
4
Me
3-morpholino-






phenyl



1471
1
CH2Ph
3-morpholino-






phenyl



1472
2
CH2Ph
3-morpholino-






phenyl



1473
3
CH2Ph
3-morpholino-






phenyl



1474
4
CH2Ph
3-morpholino-






phenyl



1475
1
COMe
3-morpholino-






phenyl



1476
2
COMe
3-morpholino-






phenyl



1477
3
COMe
3-morpholino-






phenyl



1478
4
COMe
3-morpholino-






phenyl



1479
1
CO2Me
3-morpholino-






phenyl



1480
2
CO2Me
3-morpholino-






phenyl



1481
3
CO2Me
3-morpholino-






phenyl



1482
4
CO2Me
3-morpholino-






phenyl



1483
1
CO2tBu
3-morpholino-






phenyl



1484
2
CO2tBu
3-morpholino-






phenyl



1485
3
CO2tBu
3-morpholino-






phenyl



1486
4
CO2tBu
3-morpholino-






phenyl



1487
1
CONHMe
3-morpholino-






phenyl



1488
2
CONHMe
3-morpholino-






phenyl



1489
3
CONHMe
3-morpholino-






phenyl



1490
4
CONHMe
3-morpholino-






phenyl



1491
1
SO2Me
3-morpholino-






phenyl



1492
2
SO2Me
3-morpholino-






phenyl



1493
3
SO2Me
3-morpholino-






phenyl



1494
4
SO2Me
3-morpholino-






phenyl



1495
1
SO2NH2
3-morpholino-






phenyl



1496
2
SO2NH2
3-morpholino-






phenyl



1497
3
SO2NH2
3-morpholino-






phenyl



1498
4
SO2NH2
3-morpholino-






phenyl



1499
1
Me
4-morpholino-






phenyl



1500
2
Me
4-morpholino-






phenyl



1501
3
Me
4-morpholino-






phenyl



1502
4
Me
4-morpholino-






phenyl



103
1
COMe
4-morpholino-






phenyl



1504
2
COMe
4-morpholino-






phenyl



1505
3
COMe
4-morpholino-






phenyl



1506
4
COMe
4-morpholino-






phenyl



1507
1
CO2tBu
4-morpholino-






phenyl



1508
2
CO2tBu
4-morpholino-






phenyl



1509
3
CO2tBu
4-morpholino-






phenyl



1510
4
CO2tBu
4-morpholino-






phenyl



1511
1
SO2Me
4-morpholino-






phenyl



1512
2
SO2Me
4-morpholino-






phenyl



1513
3
SO2Me
4-morpholino-






phenyl



1514
4
SO2Me
4-morpholino-






phenyl



1516
1
H
naphthylen-2-yl



1517
2
H
naphthylen-2-yl



1518
3
H
naphthylen-2-yl



1519
4
H
naphthylen-2-yl



1520
1
Me
naphthylen-2-yl



1521
2
Me
naphthylen-2-yl



1522
3
Me
naphthylen-2-yl



1523
4
Me
naphthylen-2-yl



1524
1
CH2Ph
naphthylen-2-yl



1525
2
CH2Ph
naphthylen-2-yl



1526
3
CH2Ph
naphthylen-2-yl



1527
4
CH2Ph
naphthylen-2-yl



1528
1
COMe
naphthylen-2-yl



1529
2
COMe
naphthylen-2-yl



1530
3
COMe
naphthylen-2-yl



1531
4
COMe
naphthylen-2-yl



1532
1
CO2Me
naphthylen-2-yl



1533
2
CO2Me
naphthylen-2-yl



1534
3
CO2Me
naphthylen-2-yl



1535
4
CO2Me
naphthylen-2-yl



1536
1
CO2tBu
naphthylen-2-yl



1537
2
CO2tBu
naphthylen-2-yl



1538
3
CO2tBu
naphthylen-2-yl



1539
4
CO2tBu
naphthylen-2-yl



1540
1
CONHMe
naphthylen-2-yl



1541
2
CONHMe
naphthylen-2-yl



1542
3
CONHMe
naphthylen-2-yl



1543
4
CONHMe
naphthylen-2-yl



1544
1
SO2Me
naphthylen-2-yl



1545
2
SO2Me
naphthylen-2-yl



1546
3
SO2Me
naphthylen-2-yl



1547
4
SO2Me
naphthylen-2-yl



1548
1
SO2NH2
naphthylen-2-yl



1549
2
SO2NH2
naphthylen-2-yl



1550
3
SO2NH2
naphthylen-2-yl



1551
4
SO2NH2
naphthylen-2-yl










Exemplary embodiments include compounds having the formula (XXV)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 19.

















TABLE 19







Entry
n
R7
R20a
R20b
R20c
R20d
























1
1
H
H
H
H
H



2
2
H
H
H
H
H



3
3
H
H
H
H
H



4
4
H
H
H
H
H



5
1
Me
H
H
H
H



6
2
Me
H
H
H
H



7
3
Me
H
H
H
H



8
4
Me
H
H
H
H



9
1
CH2Ph
H
H
H
H



10
2
CH2Ph
H
H
H
H



11
3
CH2Ph
H
H
H
H



12
4
CH2Ph
H
H
H
H



13
1
COMe
H
H
H
H



14
2
COMe
H
H
H
H



15
3
COMe
H
H
H
H



16
4
COMe
H
H
H
H



17
1
CO2Me
H
H
H
H



18
2
CO2Me
H
H
H
H



19
3
CO2Me
H
H
H
H



20
4
CO2Me
H
H
H
H



21
1
CO2tBu
H
H
H
H



22
2
CO2tBu
H
H
H
H



23
3
CO2tBu
H
H
H
H



24
4
CO2tBu
H
H
H
H



25
1
CONHMe
H
H
H
H



26
2
CONHMe
H
H
H
H



27
3
CONHMe
H
H
H
H



28
4
CONHMe
H
H
H
H



29
1
SO2Me
H
H
H
H



30
2
SO2Me
H
H
H
H



31
3
SO2Me
H
H
H
H



32
4
SO2Me
H
H
H
H



33
1
SO2NH2
H
H
H
H



34
2
SO2NH2
H
H
H
H



35
3
SO2NH2
H
H
H
H



36
4
SO2NH2
H
H
H
H



37
1
H
H
H
OH
H



38
2
H
H
H
OH
H



39
3
H
H
H
OH
H



40
4
H
H
H
OH
H



41
1
Me
H
H
OH
H



42
2
Me
H
H
OH
H



43
3
Me
H
H
OH
H



44
4
Me
H
H
OH
H



45
1
CH2Ph
H
H
OH
H



46
2
CH2Ph
H
H
OH
H



47
3
CH2Ph
H
H
OH
H



48
4
CH2Ph
H
H
OH
H



49
1
COMe
H
H
OH
H



50
2
COMe
H
H
OH
H



51
3
COMe
H
H
OH
H



52
4
COMe
H
H
OH
H



53
1
CO2Me
H
H
OH
H



54
2
CO2Me
H
H
OH
H



55
3
CO2Me
H
H
OH
H



56
4
CO2Me
H
H
OH
H



57
1
CO2tBu
H
H
OH
H



58
2
CO2tBu
H
H
OH
H



59
3
CO2tBu
H
H
OH
H



60
4
CO2tBu
H
H
OH
H



61
1
CONHMe
H
H
OH
H



62
2
CONHMe
H
H
OH
H



63
3
CONHMe
H
H
OH
H



64
4
CONHMe
H
H
OH
H



65
1
SO2Me
H
H
OH
H



66
2
SO2Me
H
H
OH
H



67
3
SO2Me
H
H
OH
H



68
4
SO2Me
H
H
OH
H



69
1
SO2NH2
H
H
OH
H



70
2
SO2NH2
H
H
OH
H



71
3
SO2NH2
H
H
OH
H



72
4
SO2NH2
H
H
OH
H



73
1
H
H
H
OMe
H



74
2
H
H
H
OMe
H



75
3
H
H
H
OMe
H



76
4
H
H
H
OMe
H



77
1
Me
H
H
OMe
H



78
2
Me
H
H
OMe
H



79
3
Me
H
H
OMe
H



80
4
Me
H
H
OMe
H



81
1
CH2Ph
H
H
OMe
H



82
2
CH2Ph
H
H
OMe
H



83
3
CH2Ph
H
H
OMe
H



84
4
CH2Ph
H
H
OMe
H



85
1
COMe
H
H
OMe
H



86
2
COMe
H
H
OMe
H



87
3
COMe
H
H
OMe
H



88
4
COMe
H
H
OMe
H



89
1
CO2Me
H
H
OMe
H



90
2
CO2Me
H
H
OMe
H



91
3
CO2Me
H
H
OMe
H



92
4
CO2Me
H
H
OMe
H



93
1
CO2tBu
H
H
OMe
H



94
2
CO2tBu
H
H
OMe
H



95
3
CO2tBu
H
H
OMe
H



96
1
CO2tBu
H
H
OMe
H



97
1
CONHMe
H
H
OMe
H



98
2
CONHMe
H
H
OMe
H



99
3
CONHMe
H
H
OMe
H



100
4
CONHMe
H
H
OMe
H



101
1
SO2Me
H
H
OMe
H



102
2
SO2Me
H
H
OMe
H



103
3
SO2Me
H
H
OMe
H



104
4
SO2Me
H
H
OMe
H



105
1
SO2NH2
H
H
OMe
H



106
2
SO2NH2
H
H
OMe
H



107
3
SO2NH2
H
H
OMe
H



108
4
SO2NH2
H
H
OMe
H



109
1
H
H
H
Me
H



110
2
H
H
H
Me
H



111
3
H
H
H
Me
H



112
4
H
H
H
Me
H



113
1
Me
H
H
Me
H



114
2
Me
H
H
Me
H



115
3
Me
H
H
Me
H



116
4
Me
H
H
Me
H



117
1
CH2Ph
H
H
Me
H



118
2
CH2Ph
H
H
Me
H



119
3
CH2Ph
H
H
Me
H



120
4
CH2Ph
H
H
Me
H



121
1
COMe
H
H
Me
H



122
2
COMe
H
H
Me
H



123
3
COMe
H
H
Me
H



124
4
COMe
H
H
Me
H



125
1
CO2Me
H
H
Me
H



126
2
CO2Me
H
H
Me
H



127
3
CO2Me
H
H
Me
H



128
4
CO2Me
H
H
Me
H



129
1
CO2tBu
H
H
Me
H



130
2
CO2tBu
H
H
Me
H



131
3
CO2tBu
H
H
Me
H



132
4
CO2tBu
H
H
Me
H



133
1
CONHMe
H
H
Me
H



134
2
CONHMe
H
H
Me
H



135
3
CONHMe
H
H
Me
H



136
4
CONHMe
H
H
Me
H



137
1
SO2Me
H
H
Me
H



138
2
SO2Me
H
H
Me
H



139
3
SO2Me
H
H
Me
H



140
4
SO2Me
H
H
Me
H



141
1
SO2NH2
H
H
Me
H



142
2
SO2NH2
H
H
Me
H



143
3
SO2NH2
H
H
Me
H



144
4
SO2NH2
H
H
Me
H



145
1
H
H
H
CF3
H



146
2
H
H
H
CF3
H



147
3
H
H
H
CF3
H



148
4
H
H
H
CF3
H



149
1
Me
H
H
CF3
H



150
2
Me
H
H
CF3
H



151
3
Me
H
H
CF3
H



152
4
Me
H
H
CF3
H



153
1
CH2Ph
H
H
CF3
H



154
2
CH2Ph
H
H
CF3
H



155
3
CH2Ph
H
H
CF3
H



156
4
CH2Ph
H
H
CF3
H



157
1
COMe
H
H
CF3
H



158
2
COMe
H
H
CF3
H



159
3
COMe
H
H
CF3
H



160
4
COMe
H
H
CF3
H



161
1
CO2Me
H
H
CF3
H



162
2
CO2Me
H
H
CF3
H



163
3
CO2Me
H
H
CF3
H



164
4
CO2Me
H
H
CF3
H



165
1
CO2tBu
H
H
CF3
H



166
2
CO2tBu
H
H
CF3
H



167
3
CO2tBu
H
H
CF3
H



168
4
CO2tBu
H
H
CF3
H



169
1
CONHMe
H
H
CF3
H



170
2
CONHMe
H
H
CF3
H



171
3
CONHMe
H
H
CF3
H



172
4
CONHMe
H
H
CF3
H



173
1
SO2Me
H
H
CF3
H



174
2
SO2Me
H
H
CF3
H



175
3
SO2Me
H
H
CF3
H



176
4
SO2Me
H
H
CF3
H



177
1
SO2NH2
H
H
CF3
H



178
2
SO2NH2
H
H
CF3
H



179
3
SO2NH2
H
H
CF3
H



180
4
SO2NH2
H
H
CF3
H



181
1
H
H
H
F
H



182
2
H
H
H
F
H



183
3
H
H
H
F
H



184
4
H
H
H
F
H



185
1
Me
H
H
F
H



186
2
Me
H
H
F
H



187
3
Me
H
H
F
H



188
4
Me
H
H
F
H



189
1
CH2Ph
H
H
F
H



190
2
CH2Ph
H
H
F
H



191
3
CH2Ph
H
H
F
H



192
4
CH2Ph
H
H
F
H



193
1
COMe
H
H
F
H



194
2
COMe
H
H
F
H



195
3
COMe
H
H
F
H



196
4
COMe
H
H
F
H



197
1
CO2Me
H
H
F
H



198
2
CO2Me
H
H
F
H



199
3
CO2Me
H
H
F
H



200
4
CO2Me
H
H
F
H



201
1
CO2tBu
H
H
F
H



202
2
CO2tBu
H
H
F
H



203
3
CO2tBu
H
H
F
H



204
4
CO2tBu
H
H
F
H



205
1
CONHMe
H
H
F
H



206
2
CONHMe
H
H
F
H



207
3
CONHMe
H
H
F
H



208
4
CONHMe
H
H
F
H



209
1
SO2Me
H
H
F
H



210
2
SO2Me
H
H
F
H



211
3
SO2Me
H
H
F
H



212
4
SO2Me
H
H
F
H



213
1
SO2NH2
H
H
F
H



214
2
SO2NH2
H
H
F
H



215
3
SO2NH2
H
H
F
H



216
4
SO2NH2
H
H
F
H



217
1
H
H
H
Cl
H



218
2
H
H
H
Cl
H



219
3
H
H
H
Cl
H



220
4
H
H
H
Cl
H



221
1
Me
H
H
Cl
H



222
2
Me
H
H
Cl
H



223
3
Me
H
H
Cl
H



224
4
Me
H
H
Cl
H



225
1
CH2Ph
H
H
Cl
H



226
2
CH2Ph
H
H
Cl
H



227
3
CH2Ph
H
H
Cl
H



228
4
CH2Ph
H
H
Cl
H



229
1
COMe
H
H
Cl
H



230
2
COMe
H
H
Cl
H



231
3
COMe
H
H
Cl
H



232
4
COMe
H
H
Cl
H



233
1
CO2Me
H
H
Cl
H



234
2
CO2Me
H
H
Cl
H



235
3
CO2Me
H
H
Cl
H



236
4
CO2Me
H
H
Cl
H



237
1
CO2tBu
H
H
Cl
H



238
2
CO2tBu
H
H
Cl
H



239
3
CO2tBu
H
H
Cl
H



240
4
CO2tBu
H
H
Cl
H



241
1
CONHMe
H
H
Cl
H



242
2
CONHMe
H
H
Cl
H



243
3
CONHMe
H
H
Cl
H



244
4
CONHMe
H
H
Cl
H



245
1
SO2Me
H
H
Cl
H



246
2
SO2Me
H
H
Cl
H



247
3
SO2Me
H
H
Cl
H



248
4
SO2Me
H
H
Cl
H



249
1
SO2NH2
H
H
Cl
H



250
2
SO2NH2
H
H
Cl
H



251
3
SO2NH2
H
H
Cl
H



252
4
SO2NH2
H
H
Cl
H



253
1
H
H
H
CN
H



254
2
H
H
H
CN
H



255
3
H
H
H
CN
H



256
4
H
H
H
CN
H



257
1
Me
H
H
CN
H



258
2
Me
H
H
CN
H



259
3
Me
H
H
CN
H



260
4
Me
H
H
CN
H



261
1
v
H
H
CN
H



262
2
CH2Ph
H
H
CN
H



263
3
CH2Ph
H
H
CN
H



264
4
CH2Ph
H
H
CN
H



265
1
CH2Ph
H
H
CN
H



266
2
COMe
H
H
CN
H



267
3
COMe
H
H
CN
H



268
4
COMe
H
H
CN
H



269
1
COMe
H
H
CN
H



270
2
CO2Me
H
H
CN
H



271
3
CO2Me
H
H
CN
H



272
4
CO2Me
H
H
CN
H



273
1
CO2Me
H
H
CN
H



274
2
CO2tBu
H
H
CN
H



275
3
CO2tBu
H
H
CN
H



276
4
CO2tBu
H
H
CN
H



277
1
CO2tBu
H
H
CN
H



278
2
CONHMe
H
H
CN
H



279
3
CONHMe
H
H
CN
H



280
4
CONHMe
H
H
CN
H



281
1
CONHMe
H
H
CN
H



282
2
SO2Me
H
H
CN
H



283
3
SO2Me
H
H
CN
H



284
4
SO2Me
H
H
CN
H



285
1
SO2Me
H
H
CN
H



286
2
SO2NH2
H
H
CN
H



287
3
SO2NH2
H
H
CN
H



288
4
SO2NH2
H
H
CN
H



289
1
SO2NH2
H
OH
H
H



290
2
H
H
OH
H
H



291
3
H
H
OH
H
H



292
4
H
H
OH
H
H



293
1
Me
H
OH
H
H



294
2
Me
H
OH
H
H



295
3
Me
H
OH
H
H



296
4
Me
H
OH
H
H



297
1
CH2Ph
H
OH
H
H



298
2
CH2Ph
H
OH
H
H



299
3
CH2Ph
H
OH
H
H



300
4
CH2Ph
H
OH
H
H



301
1
COMe
H
OH
H
H



302
2
COMe
H
OH
H
H



303
3
COMe
H
OH
H
H



304
4
COMe
H
OH
H
H



305
1
CO2Me
H
OH
H
H



306
2
CO2Me
H
OH
H
H



307
3
CO2Me
H
OH
H
H



308
4
CO2Me
H
OH
H
H



309
1
CO2tBu
H
OH
H
H



310
2
CO2tBu
H
OH
H
H



311
3
CO2tBu
H
OH
H
H



312
4
CO2tBu
H
OH
H
H



313
1
CONHMe
H
OH
H
H



314
2
CONHMe
H
OH
H
H



315
3
CONHMe
H
OH
H
H



316
4
CONHMe
H
OH
H
H



317
1
SO2Me
H
OH
H
H



318
2
SO2Me
H
OH
H
H



319
3
SO2Me
H
OH
H
H



320
4
SO2Me
H
OH
H
H



321
1
SO2NH2
H
OH
H
H



322
2
SO2NH2
H
OH
H
H



323
3
SO2NH2
H
OH
H
H



324
4
SO2NH2
H
OH
H
H



325
1
H
H
OMe
H
H



326
2
H
H
OMe
H
H



327
3
H
H
OMe
H
H



328
4
H
H
OMe
H
H



329
1
Me
H
OMe
H
H



330
2
Me
H
OMe
H
H



331
3
Me
H
OMe
H
H



332
4
Me
H
OMe
H
H



333
1
CH2Ph
H
OMe
H
H



334
2
CH2Ph
H
OMe
H
H



335
3
CH2Ph
H
OMe
H
H



336
4
CH2Ph
H
OMe
H
H



337
1
COMe
H
OMe
H
H



338
2
COMe
H
OMe
H
H



339
3
COMe
H
OMe
H
H



340
4
COMe
H
OMe
H
H



341
1
CO2Me
H
OMe
H
H



342
2
CO2Me
H
OMe
H
H



343
3
CO2Me
H
OMe
H
H



344
4
CO2Me
H
OMe
H
H



345
1
CO2tBu
H
OMe
H
H



346
2
CO2tBu
H
OMe
H
H



347
3
CO2tBu
H
OMe
H
H



348
4
CO2tBu
H
OMe
H
H



349
1
CONHMe
H
OMe
H
H



350
2
CONHMe
H
OMe
H
H



351
3
CONHMe
H
OMe
H
H



352
4
CONHMe
H
OMe
H
H



353
1
SO2Me
H
OMe
H
H



354
2
SO2Me
H
OMe
H
H



355
3
SO2Me
H
OMe
H
H



356
4
SO2Me
H
OMe
H
H



357
1
SO2NH2
H
OMe
H
H



358
2
SO2NH2
H
OMe
H
H



359
3
SO2NH2
H
OMe
H
H



360
4
SO2NH2
H
OMe
H
H



361
1
H
H
Me
H
H



362
2
H
H
Me
H
H



363
3
H
H
Me
H
H



364
4
H
H
Me
H
H



365
1
Me
H
Me
H
H



366
2
Me
H
Me
H
H



367
3
Me
H
Me
H
H



368
4
Me
H
Me
H
H



369
1
CH2Ph
H
Me
H
H



370
2
CH2Ph
H
Me
H
H



371
3
CH2Ph
H
Me
H
H



372
4
CH2Ph
H
Me
H
H



373
1
COMe
H
Me
H
H



374
2
COMe
H
Me
H
H



375
3
COMe
H
Me
H
H



376
4
COMe
H
Me
H
H



377
1
CO2Me
H
Me
H
H



378
2
CO2Me
H
Me
H
H



379
3
CO2Me
H
Me
H
H



380
4
CO2Me
H
Me
H
H



381
1
CO2tBu
H
Me
H
H



382
2
CO2tBu
H
Me
H
H



383
3
CO2tBu
H
Me
H
H



384
4
CO2tBu
H
Me
H
H



385
1
CONHMe
H
Me
H
H



386
2
CONHMe
H
Me
H
H



387
3
CONHMe
H
Me
H
H



388
4
CONHMe
H
Me
H
H



389
1
SO2Me
H
Me
H
H



390
2
SO2Me
H
Me
H
H



391
3
SO2Me
H
Me
H
H



392
4
SO2Me
H
Me
H
H



393
1
SO2NH2
H
Me
H
H



394
2
SO2NH2
H
Me
H
H



395
3
SO2NH2
H
Me
H
H



396
4
SO2NH2
H
Me
H
H



397
1
H
H
CF3
H
H



398
2
H
H
CF3
H
H



399
3
H
H
CF3
H
H



400
4
H
H
CF3
H
H



401
1
Me
H
CF3
H
H



402
2
Me
H
CF3
H
H



403
3
Me
H
CF3
H
H



404
4
Me
H
CF3
H
H



405
1
CH2Ph
H
CF3
H
H



406
2
CH2Ph
H
CF3
H
H



407
3
CH2Ph
H
CF3
H
H



408
4
CH2Ph
H
CF3
H
H



409
1
COMe
H
CF3
H
H



410
2
COMe
H
CF3
H
H



411
3
COMe
H
CF3
H
H



412
4
COMe
H
CF3
H
H



413
1
CO2Me
H
CF3
H
H



414
2
CO2Me
H
CF3
H
H



415
3
CO2Me
H
CF3
H
H



416
4
CO2Me
H
CF3
H
H



417
1
CO2tBu
H
CF3
H
H



418
2
CO2tBu
H
CF3
H
H



419
3
CO2tBu
H
CF3
H
H



420
4
CO2tBu
H
CF3
H
H



421
1
CONHMe
H
CF3
H
H



422
2
CONHMe
H
CF3
H
H



423
3
CONHMe
H
CF3
H
H



424
4
CONHMe
H
CF3
H
H



425
1
SO2Me
H
CF3
H
H



426
2
SO2Me
H
CF3
H
H



427
3
SO2Me
H
CF3
H
H



428
4
SO2Me
H
CF3
H
H



429
1
SO2NH2
H
CF3
H
H



430
2
SO2NH2
H
CF3
H
H



431
3
SO2NH2
H
CF3
H
H



432
4
SO2NH2
H
CF3
H
H



433
1
H
H
F
H
H



434
2
H
H
F
H
H



435
3
H
H
F
H
H



436
3
H
H
F
H
H



437
1
Me
H
F
H
H



438
2
Me
H
F
H
H



439
3
Me
H
F
H
H



440
4
Me
H
F
H
H



441
1
CH2Ph
H
F
H
H



442
2
CH2Ph
H
F
H
H



443
3
CH2Ph
H
F
H
H



444
4
CH2Ph
H
F
H
H



445
1
COMe
H
F
H
H



446
2
COMe
H
F
H
H



447
3
COMe
H
F
H
H



448
4
COMe
H
F
H
H



449
1
CO2Me
H
F
H
H



450
2
CO2Me
H
F
H
H



451
3
CO2Me
H
F
H
H



452
4
CO2Me
H
F
H
H



453
1
CO2tBu
H
F
H
H



454
2
CO2tBu
H
F
H
H



455
3
CO2tBu
H
F
H
H



456
4
CO2tBu
H
F
H
H



457
1
CONHMe
H
F
H
H



458
2
CONHMe
H
F
H
H



459
3
CONHMe
H
F
H
H



460
4
CONHMe
H
F
H
H



461
1
SO2Me
H
F
H
H



462
2
SO2Me
H
F
H
H



463
3
SO2Me
H
F
H
H



464
4
SO2Me
H
F
H
H



465
1
SO2NH2
H
F
H
H



466
2
SO2NH2
H
F
H
H



467
3
SO2NH2
H
F
H
H



468
4
SO2NH2
H
F
H
H



469
1
H
H
Cl
H
H



470
2
H
H
Cl
H
H



471
3
H
H
Cl
H
H



472
4
H
H
Cl
H
H



473
1
Me
H
Cl
H
H



474
2
Me
H
Cl
H
H



475
3
Me
H
Cl
H
H



476
4
Me
H
Cl
H
H



477
1
CH2Ph
H
Cl
H
H



478
2
CH2Ph
H
Cl
H
H



479
3
CH2Ph
H
Cl
H
H



480
4
CH2Ph
H
Cl
H
H



481
1
COMe
H
Cl
H
H



482
2
COMe
H
Cl
H
H



483
3
COMe
H
Cl
H
H



484
4
COMe
H
Cl
H
H



485
1
CO2Me
H
Cl
H
H



486
2
CO2Me
H
Cl
H
H



487
3
CO2Me
H
Cl
H
H



488
4
CO2Me
H
Cl
H
H



489
1
CO2tBu
H
Cl
H
H



490
2
CO2tBu
H
Cl
H
H



491
3
CO2tBu
H
Cl
H
H



492
4
CO2tBu
H
Cl
H
H



493
1
CONHMe
H
Cl
H
H



494
2
CONHMe
H
Cl
H
H



495
3
CONHMe
H
Cl
H
H



496
4
CONHMe
H
Cl
H
H



497
1
SO2Me
H
Cl
H
H



498
2
SO2Me
H
Cl
H
H



499
3
SO2Me
H
Cl
H
H



500
4
SO2Me
H
Cl
H
H



501
1
SO2NH2
H
Cl
H
H



502
2
SO2NH2
H
Cl
H
H



503
3
SO2NH2
H
Cl
H
H



504
4
SO2NH2
H
Cl
H
H



505
1
H
H
CN
H
H



506
2
H
H
CN
H
H



507
3
H
H
CN
H
H



508
4
H
H
CN
H
H



509
1
Me
H
CN
H
H



510
2
Me
H
CN
H
H



511
3
Me
H
CN
H
H



512
4
Me
H
CN
H
H



513
1
CH2Ph
H
CN
H
H



514
2
CH2Ph
H
CN
H
H



515
3
CH2Ph
H
CN
H
H



516
4
CH2Ph
H
CN
H
H



517
1
COMe
H
CN
H
H



518
2
COMe
H
CN
H
H



519
3
COMe
H
CN
H
H



520
4
COMe
H
CN
H
H



521
1
CO2Me
H
CN
H
H



522
2
CO2Me
H
CN
H
H



523
3
CO2Me
H
CN
H
H



524
4
CO2Me
H
CN
H
H



525
1
CO2tBu
H
CN
H
H



526
2
CO2tBu
H
CN
H
H



527
3
CO2tBu
H
CN
H
H



528
4
CO2tBu
H
CN
H
H



529
1
CONHMe
H
CN
H
H



530
2
CONHMe
H
CN
H
H



531
3
CONHMe
H
CN
H
H



532
4
CONHMe
H
CN
H
H



533
1
SO2Me
H
CN
H
H



534
2
SO2Me
H
CN
H
H



535
3
SO2Me
H
CN
H
H



536
4
SO2Me
H
CN
H
H



537
1
SO2NH2
H
CN
H
H



538
2
SO2NH2
H
CN
H
H



539
3
SO2NH2
H
CN
H
H



540
4
SO2NH2
H
CN
H
H



541
1
H
OH
H
H
H



542
2
H
OH
H
H
H



543
3
H
OH
H
H
H



544
4
H
OH
H
H
H



545
1
Me
OH
H
H
H



546
2
Me
OH
H
H
H



547
3
Me
OH
H
H
H



548
4
Me
OH
H
H
H



549
1
CH2Ph
OH
H
H
H



550
2
CH2Ph
OH
H
H
H



551
3
CH2Ph
OH
H
H
H



552
4
CH2Ph
OH
H
H
H



553
1
COMe
OH
H
H
H



554
2
COMe
OH
H
H
H



555
3
COMe
OH
H
H
H



556
4
COMe
OH
H
H
H



557
1
CO2Me
OH
H
H
H



558
2
CO2Me
OH
H
H
H



559
3
CO2Me
OH
H
H
H



560
4
CO2Me
OH
H
H
H



561
1
CO2tBu
OH
H
H
H



562
2
CO2tBu
OH
H
H
H



563
3
CO2tBu
OH
H
H
H



564
4
CO2tBu
OH
H
H
H



565
1
CONHMe
OH
H
H
H



566
2
CONHMe
OH
H
H
H



567
3
CONHMe
OH
H
H
H



568
4
CONHMe
OH
H
H
H



569
1
SO2Me
OH
H
H
H



570
2
SO2Me
OH
H
H
H



571
3
SO2Me
OH
H
H
H



572
4
SO2Me
OH
H
H
H



573
1
SO2NH2
OH
H
H
H



574
2
SO2NH2
OH
H
H
H



575
3
SO2NH2
OH
H
H
H



576
4
SO2NH2
OH
H
H
H



577
1
H
OMe
H
H
H



578
2
H
OMe
H
H
H



579
3
H
OMe
H
H
H



580
4
H
OMe
H
H
H



581
1
Me
OMe
H
H
H



582
2
Me
OMe
H
H
H



583
3
Me
OMe
H
H
H



584
4
Me
OMe
H
H
H



585
1
CH2Ph
OMe
H
H
H



586
2
CH2Ph
OMe
H
H
H



587
3
CH2Ph
OMe
H
H
H



588
4
CH2Ph
OMe
H
H
H



589
1
COMe
OMe
H
H
H



590
2
COMe
OMe
H
H
H



591
3
COMe
OMe
H
H
H



592
4
COMe
OMe
H
H
H



593
1
CO2Me
OMe
H
H
H



594
2
CO2Me
OMe
H
H
H



595
3
CO2Me
OMe
H
H
H



596
4
CO2Me
OMe
H
H
H



597
1
CO2tBu
OMe
H
H
H



598
2
CO2tBu
OMe
H
H
H



599
3
CO2tBu
OMe
H
H
H



600
4
CO2tBu
OMe
H
H
H



601
1
CONHMe
OMe
H
H
H



602
2
CONHMe
OMe
H
H
H



603
3
CONHMe
OMe
H
H
H



604
4
CONHMe
OMe
H
H
H



605
1
SO2Me
OMe
H
H
H



606
2
SO2Me
OMe
H
H
H



607
3
SO2Me
OMe
H
H
H



608
4
SO2Me
OMe
H
H
H



609
1
SO2NH2
OMe
H
H
H



610
2
SO2NH2
OMe
H
H
H



611
3
SO2NH2
OMe
H
H
H



612
4
SO2NH2
OMe
H
H
H



613
1
H
Me
H
H
H



614
2
H
Me
H
H
H



615
3
H
Me
H
H
H



616
4
H
Me
H
H
H



617
1
Me
Me
H
H
H



618
2
Me
Me
H
H
H



619
3
Me
Me
H
H
H



620
4
Me
Me
H
H
H



621
1
CH2Ph
Me
H
H
H



622
2
CH2Ph
Me
H
H
H



623
3
CH2Ph
Me
H
H
H



624
4
CH2Ph
Me
H
H
H



625
1
COMe
Me
H
H
H



626
2
COMe
Me
H
H
H



627
3
COMe
Me
H
H
H



628
4
COMe
Me
H
H
H



629
1
CO2Me
Me
H
H
H



630
2
CO2Me
Me
H
H
H



631
3
CO2Me
Me
H
H
H



632
4
CO2Me
Me
H
H
H



633
1
CO2tBu
Me
H
H
H



634
2
CO2tBu
Me
H
H
H



635
3
CO2tBu
Me
H
H
H



636
4
CO2tBu
Me
H
H
H



637
1
CONHMe
Me
H
H
H



638
2
CONHMe
Me
H
H
H



639
3
CONHMe
Me
H
H
H



640
4
CONHMe
Me
H
H
H



641
1
SO2Me
Me
H
H
H



642
2
SO2Me
Me
H
H
H



643
3
SO2Me
Me
H
H
H



644
4
SO2Me
Me
H
H
H



645
1
SO2NH2
Me
H
H
H



646
2
SO2NH2
Me
H
H
H



647
3
SO2NH2
Me
H
H
H



648
4
SO2NH2
Me
H
H
H



649
1
H
CF3
H
H
H



650
2
H
CF3
H
H
H



651
3
H
CF3
H
H
H



652
4
H
CF3
H
H
H



653
1
Me
CF3
H
H
H



654
2
Me
CF3
H
H
H



655
3
Me
CF3
H
H
H



656
4
Me
CF3
H
H
H



657
1
CH2Ph
CF3
H
H
H



658
2
CH2Ph
CF3
H
H
H



659
3
CH2Ph
CF3
H
H
H



660
4
CH2Ph
CF3
H
H
H



661
1
COMe
CF3
H
H
H



662
2
COMe
CF3
H
H
H



663
3
COMe
CF3
H
H
H



664
4
COMe
CF3
H
H
H



665
1
CO2Me
CF3
H
H
H



666
2
CO2Me
CF3
H
H
H



667
3
CO2Me
CF3
H
H
H



668
4
CO2Me
CF3
H
H
H



669
1
CO2tBu
CF3
H
H
H



670
2
CO2tBu
CF3
H
H
H



671
3
CO2tBu
CF3
H
H
H



672
4
CO2tBu
CF3
H
H
H



673
1
CONHMe
CF3
H
H
H



674
2
CONHMe
CF3
H
H
H



675
3
CONHMe
CF3
H
H
H



676
4
CONHMe
CF3
H
H
H



677
1
SO2Me
CF3
H
H
H



678
2
SO2Me
CF3
H
H
H



679
3
SO2Me
CF3
H
H
H



680
4
SO2Me
CF3
H
H
H



681
1
SO2NH2
CF3
H
H
H



682
2
SO2NH2
CF3
H
H
H



683
3
SO2NH2
CF3
H
H
H



684
4
SO2NH2
CF3
H
H
H



685
1
H
F
H
H
H



686
2
H
F
H
H
H



687
3
H
F
H
H
H



688
3
H
F
H
H
H



689
1
Me
F
H
H
H



690
2
Me
F
H
H
H



691
3
Me
F
H
H
H



692
4
Me
F
H
H
H



693
1
CH2Ph
F
H
H
H



694
2
CH2Ph
F
H
H
H



695
3
CH2Ph
F
H
H
H



696
4
CH2Ph
F
H
H
H



697
1
COMe
F
H
H
H



698
2
COMe
F
H
H
H



699
3
COMe
F
H
H
H



700
4
COMe
F
H
H
H



701
1
CO2Me
F
H
H
H



702
2
CO2Me
F
H
H
H



703
3
CO2Me
F
H
H
H



704
4
CO2Me
F
H
H
H



705
1
CO2tBu
F
H
H
H



706
2
CO2tBu
F
H
H
H



707
3
CO2tBu
F
H
H
H



708
4
CO2tBu
F
H
H
H



709
1
CONHMe
F
H
H
H



710
2
CONHMe
F
H
H
H



711
3
CONHMe
F
H
H
H



712
4
CONHMe
F
H
H
H



713
1
SO2Me
F
H
H
H



714
2
SO2Me
F
H
H
H



715
3
SO2Me
F
H
H
H



716
4
SO2Me
F
H
H
H



717
1
SO2NH2
F
H
H
H



718
2
SO2NH2
F
H
H
H



719
3
SO2NH2
F
H
H
H



720
4
SO2NH2
F
H
H
H



721
1
H
Cl
H
H
H



722
2
H
Cl
H
H
H



723
3
H
Cl
H
H
H



724
4
H
Cl
H
H
H



725
1
Me
Cl
H
H
H



726
2
Me
Cl
H
H
H



727
3
Me
Cl
H
H
H



728
4
Me
Cl
H
H
H



729
1
CH2Ph
Cl
H
H
H



730
2
CH2Ph
Cl
H
H
H



731
3
CH2Ph
Cl
H
H
H



732
4
CH2Ph
Cl
H
H
H



733
1
COMe
Cl
H
H
H



734
2
COMe
Cl
H
H
H



735
3
COMe
Cl
H
H
H



736
4
COMe
Cl
H
H
H



737
1
CO2Me
Cl
H
H
H



738
2
CO2Me
Cl
H
H
H



739
3
CO2Me
Cl
H
H
H



740
4
CO2Me
Cl
H
H
H



741
1
CO2tBu
Cl
H
H
H



742
2
CO2tBu
Cl
H
H
H



743
3
CO2tBu
Cl
H
H
H



744
4
CO2tBu
Cl
H
H
H



745
1
CONHMe
Cl
H
H
H



746
2
CONHMe
Cl
H
H
H



747
3
CONHMe
Cl
H
H
H



748
4
CONHMe
Cl
H
H
H



749
1
SO2Me
Cl
H
H
H



750
2
SO2Me
Cl
H
H
H



751
3
SO2Me
Cl
H
H
H



752
4
SO2Me
Cl
H
H
H



753
1
SO2NH2
Cl
H
H
H



754
2
SO2NH2
Cl
H
H
H



755
3
SO2NH2
Cl
H
H
H



756
4
SO2NH2
Cl
H
H
H



757
1
H
CN
H
H
H



758
2
H
CN
H
H
H



759
3
H
CN
H
H
H



760
4
H
CN
H
H
H



761
1
Me
CN
H
H
H



762
2
Me
CN
H
H
H



763
3
Me
CN
H
H
H



764
4
Me
CN
H
H
H



765
1
CH2Ph
CN
H
H
H



766
2
CH2Ph
CN
H
H
H



767
3
CH2Ph
CN
H
H
H



768
4
CH2Ph
CN
H
H
H



769
1
COMe
CN
H
H
H



770
2
COMe
CN
H
H
H



771
3
COMe
CN
H
H
H



772
4
COMe
CN
H
H
H



773
1
CO2Me
CN
H
H
H



774
2
CO2Me
CN
H
H
H



775
3
CO2Me
CN
H
H
H



776
4
CO2Me
CN
H
H
H



777
1
CO2tBu
CN
H
H
H



778
2
CO2tBu
CN
H
H
H



779
3
CO2tBu
CN
H
H
H



780
4
CO2tBu
CN
H
H
H



781
1
CONHMe
CN
H
H
H



782
2
CONHMe
CN
H
H
H



783
3
CONHMe
CN
H
H
H



784
4
CONHMe
CN
H
H
H



785
1
SO2Me
CN
H
H
H



786
2
SO2Me
CN
H
H
H



787
3
SO2Me
CN
H
H
H



788
4
SO2Me
CN
H
H
H



789
1
SO2NH2
CN
H
H
H



790
2
SO2NH2
CN
H
H
H



791
3
SO2NH2
CN
H
H
H



792
4
SO2NH2
CN
H
H
H



793
1
H
H
H
H
OH



794
2
H
H
H
H
OH



795
3
H
H
H
H
OH



796
4
H
H
H
H
OH



797
1
Me
H
H
H
OH



798
2
Me
H
H
H
OH



799
3
Me
H
H
H
OH



800
4
Me
H
H
H
OH



801
1
CH2Ph
H
H
H
OH



802
2
CH2Ph
H
H
H
OH



803
3
CH2Ph
H
H
H
OH



804
4
CH2Ph
H
H
H
OH



805
1
COMe
H
H
H
OH



806
2
COMe
H
H
H
OH



807
3
COMe
H
H
H
OH



808
4
COMe
H
H
H
OH



809
1
CO2Me
H
H
H
OH



810
2
CO2Me
H
H
H
OH



811
3
CO2Me
H
H
H
OH



812
4
CO2Me
H
H
H
OH



813
1
CO2tBu
H
H
H
OH



814
2
CO2tBu
H
H
H
OH



815
3
CO2tBu
H
H
H
OH



816
4
CO2tBu
H
H
H
OH



817
1
CONHMe
H
H
H
OH



818
2
CONHMe
H
H
H
OH



819
3
CONHMe
H
H
H
OH



820
4
CONHMe
H
H
H
OH



821
1
SO2Me
H
H
H
OH



822
2
SO2Me
H
H
H
OH



823
3
SO2Me
H
H
H
OH



824
4
SO2Me
H
H
H
OH



825
1
SO2NH2
H
H
H
OH



826
2
SO2NH2
H
H
H
OH



827
3
SO2NH2
H
H
H
OH



828
4
SO2NH2
H
H
H
OH



829
1
H
H
H
H
OMe



830
2
H
H
H
H
OMe



831
3
H
H
H
H
OMe



832
4
H
H
H
H
OMe



833
1
Me
H
H
H
OMe



834
2
Me
H
H
H
OMe



835
3
Me
H
H
H
OMe



836
4
Me
H
H
H
OMe



837
1
CH2Ph
H
H
H
OMe



838
2
CH2Ph
H
H
H
OMe



839
3
CH2Ph
H
H
H
OMe



840
4
CH2Ph
H
H
H
OMe



841
1
COMe
H
H
H
OMe



842
2
COMe
H
H
H
OMe



843
3
COMe
H
H
H
OMe



844
4
COMe
H
H
H
OMe



845
1
CO2Me
H
H
H
OMe



846
2
CO2Me
H
H
H
OMe



847
3
CO2Me
H
H
H
OMe



848
4
CO2Me
H
H
H
OMe



849
1
CO2tBu
H
H
H
OMe



850
2
CO2tBu
H
H
H
OMe



851
3
CO2tBu
H
H
H
OMe



852
4
CO2tBu
H
H
H
OMe



853
1
CONHMe
H
H
H
OMe



854
2
CONHMe
H
H
H
OMe



855
3
CONHMe
H
H
H
OMe



856
4
CONHMe
H
H
H
OMe



857
1
SO2Me
H
H
H
OMe



858
2
SO2Me
H
H
H
OMe



859
3
SO2Me
H
H
H
OMe



860
4
SO2Me
H
H
H
OMe



861
1
SO2NH2
H
H
H
OMe



862
2
SO2NH2
H
H
H
OMe



863
3
SO2NH2
H
H
H
OMe



864
4
SO2NH2
H
H
H
OMe



865
1
H
H
H
H
Me



866
2
H
H
H
H
Me



867
3
H
H
H
H
Me



868
4
H
H
H
H
Me



869
1
Me
H
H
H
Me



870
2
Me
H
H
H
Me



871
3
Me
H
H
H
Me



872
4
Me
H
H
H
Me



873
1
CH2Ph
H
H
H
Me



874
2
CH2Ph
H
H
H
Me



875
3
CH2Ph
H
H
H
Me



876
4
CH2Ph
H
H
H
Me



877
1
COMe
H
H
H
Me



878
2
COMe
H
H
H
Me



879
3
COMe
H
H
H
Me



880
4
COMe
H
H
H
Me



881
1
CO2Me
H
H
H
Me



882
2
CO2Me
H
H
H
Me



883
3
CO2Me
H
H
H
Me



884
4
CO2Me
H
H
H
Me



885
1
CO2tBu
H
H
H
Me



886
2
CO2tBu
H
H
H
Me



887
3
CO2tBu
H
H
H
Me



888
4
CO2tBu
H
H
H
Me



889
1
CONHMe
H
H
H
Me



890
2
CONHMe
H
H
H
Me



891
3
CONHMe
H
H
H
Me



892
4
CONHMe
H
H
H
Me



893
1
SO2Me
H
H
H
Me



894
2
SO2Me
H
H
H
Me



895
3
SO2Me
H
H
H
Me



896
4
SO2Me
H
H
H
Me



897
1
SO2NH2
H
H
H
Me



898
2
SO2NH2
H
H
H
Me



899
3
SO2NH2
H
H
H
Me



900
4
SO2NH2
H
H
H
Me



901
1
H
H
H
H
CF3



902
2
H
H
H
H
CF3



903
3
H
H
H
H
CF3



904
4
H
H
H
H
CF3



905
1
Me
H
H
H
CF3



906
2
Me
H
H
H
CF3



907
3
Me
H
H
H
CF3



908
4
Me
H
H
H
CF3



909
1
CH2Ph
H
H
H
CF3



910
2
CH2Ph
H
H
H
CF3



911
3
CH2Ph
H
H
H
CF3



912
4
CH2Ph
H
H
H
CF3



913
1
COMe
H
H
H
CF3



914
2
COMe
H
H
H
CF3



915
3
COMe
H
H
H
CF3



916
4
COMe
H
H
H
CF3



917
1
CO2Me
H
H
H
CF3



918
2
CO2Me
H
H
H
CF3



919
3
CO2Me
H
H
H
CF3



920
4
CO2Me
H
H
H
CF3



921
1
CO2tBu
H
H
H
CF3



922
2
CO2tBu
H
H
H
CF3



923
3
CO2tBu
H
H
H
CF3



924
4
CO2tBu
H
H
H
CF3



925
1
CONHMe
H
H
H
CF3



926
2
CONHMe
H
H
H
CF3



927
3
CONHMe
H
H
H
CF3



928
4
CONHMe
H
H
H
CF3



929
1
SO2Me
H
H
H
CF3



930
2
SO2Me
H
H
H
CF3



931
3
SO2Me
H
H
H
CF3



932
4
SO2Me
H
H
H
CF3



933
1
SO2NH2
H
H
H
CF3



934
2
SO2NH2
H
H
H
CF3



935
3
SO2NH2
H
H
H
CF3



936
4
SO2NH2
H
H
H
CF3



937
1
H
H
H
H
F



938
2
H
H
H
H
F



939
3
H
H
H
H
F



940
3
H
H
H
H
F



941
1
Me
H
H
H
F



942
2
Me
H
H
H
F



943
3
Me
H
H
H
F



944
4
Me
H
H
H
F



945
1
CH2Ph
H
H
H
F



946
2
CH2Ph
H
H
H
F



947
3
CH2Ph
H
H
H
F



948
4
CH2Ph
H
H
H
F



949
1
COMe
H
H
H
F



950
2
COMe
H
H
H
F



951
3
COMe
H
H
H
F



952
4
COMe
H
H
H
F



953
1
CO2Me
H
H
H
F



954
2
CO2Me
H
H
H
F



955
3
CO2Me
H
H
H
F



956
4
CO2Me
H
H
H
F



957
1
CO2tBu
H
H
H
F



958
2
CO2tBu
H
H
H
F



959
3
CO2tBu
H
H
H
F



960
4
CO2tBu
H
H
H
F



961
1
CONHMe
H
H
H
F



962
2
CONHMe
H
H
H
F



963
3
CONHMe
H
H
H
F



964
4
CONHMe
H
H
H
F



965
1
SO2Me
H
H
H
F



966
2
SO2Me
H
H
H
F



967
3
SO2Me
H
H
H
F



968
4
SO2Me
H
H
H
F



969
1
SO2NH2
H
H
H
F



970
2
SO2NH2
H
H
H
F



971
3
SO2NH2
H
H
H
F



972
4
SO2NH2
H
H
H
F



973
1
H
H
H
H
Cl



974
2
H
H
H
H
Cl



975
3
H
H
H
H
Cl



976
4
H
H
H
H
Cl



977
1
Me
H
H
H
Cl



978
2
Me
H
H
H
Cl



979
3
Me
H
H
H
Cl



980
4
Me
H
H
H
Cl



981
1
CH2Ph
H
H
H
Cl



982
2
CH2Ph
H
H
H
Cl



983
3
CH2Ph
H
H
H
Cl



984
4
CH2Ph
H
H
H
Cl



985
1
COMe
H
H
H
Cl



986
2
COMe
H
H
H
Cl



987
3
COMe
H
H
H
Cl



988
4
COMe
H
H
H
Cl



989
1
CO2Me
H
H
H
Cl



990
2
CO2Me
H
H
H
Cl



991
3
CO2Me
H
H
H
Cl



992
4
CO2Me
H
H
H
Cl



993
1
CO2tBu
H
H
H
Cl



994
2
CO2tBu
H
H
H
Cl



995
3
CO2tBu
H
H
H
Cl



996
4
CO2tBu
H
H
H
Cl



997
1
CONHMe
H
H
H
Cl



998
2
CONHMe
H
H
H
Cl



999
3
CONHMe
H
H
H
Cl



1000
4
CONHMe
H
H
H
Cl



1001
1
SO2Me
H
H
H
Cl



1002
2
SO2Me
H
H
H
Cl



1003
3
SO2Me
H
H
H
Cl



1004
4
SO2Me
H
H
H
Cl



1005
1
SO2NH2
H
H
H
Cl



1006
2
SO2NH2
H
H
H
Cl



1007
3
SO2NH2
H
H
H
Cl



1008
4
SO2NH2
H
H
H
Cl



1009
1
H
H
H
H
CN



1010
2
H
H
H
H
CN



1011
3
H
H
H
H
CN



1012
4
H
H
H
H
CN



1013
1
Me
H
H
H
CN



1014
2
Me
H
H
H
CN



1015
3
Me
H
H
H
CN



1016
4
Me
H
H
H
CN



1017
1
CH2Ph
H
H
H
CN



1018
2
CH2Ph
H
H
H
CN



1019
3
CH2Ph
H
H
H
CN



1020
4
CH2Ph
H
H
H
CN



1021
1
COMe
H
H
H
CN



1022
2
COMe
H
H
H
CN



1023
3
COMe
H
H
H
CN



1024
4
COMe
H
H
H
CN



1025
1
CO2Me
H
H
H
CN



1026
2
CO2Me
H
H
H
CN



1027
3
CO2Me
H
H
H
CN



1028
4
CO2Me
H
H
H
CN



1029
1
CO2tBu
H
H
H
CN



1030
2
CO2tBu
H
H
H
CN



1031
3
CO2tBu
H
H
H
CN



1032
4
CO2tBu
H
H
H
CN



1033
1
CONHMe
H
H
H
CN



1034
2
CONHMe
H
H
H
CN



1035
3
CONHMe
H
H
H
CN



1036
4
CONHMe
H
H
H
CN



1037
1
SO2Me
H
H
H
CN



1038
2
SO2Me
H
H
H
CN



1039
3
SO2Me
H
H
H
CN



1040
4
SO2Me
H
H
H
CN



1041
1
SO2NH2
H
H
H
CN



1042
2
SO2NH2
H
H
H
CN



1043
3
SO2NH2
H
H
H
CN



1044
4
SO2NH2
H
H
H
CN










Exemplary embodiments include compounds having the formula (XXVI)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 20.

















TABLE 20







Entry
n
R7
R20a
R20b
R20c
R20d
























1
1
H
H
H
H
H



2
2
H
H
H
H
H



3
3
H
H
H
H
H



4
4
H
H
H
H
H



5
1
Me
H
H
H
H



6
2
Me
H
H
H
H



7
3
Me
H
H
H
H



8
4
Me
H
H
H
H



9
1
CH2Ph
H
H
H
H



10
2
CH2Ph
H
H
H
H



11
3
CH2Ph
H
H
H
H



12
4
CH2Ph
H
H
H
H



13
1
COMe
H
H
H
H



14
2
COMe
H
H
H
H



15
3
COMe
H
H
H
H



16
4
COMe
H
H
H
H



17
1
CO2Me
H
H
H
H



18
2
CO2Me
H
H
H
H



19
3
CO2Me
H
H
H
H



20
4
CO2Me
H
H
H
H



21
1
CO2tBu
H
H
H
H



22
2
CO2tBu
H
H
H
H



23
3
CO2tBu
H
H
H
H



24
4
CO2tBu
H
H
H
H



25
1
CONHMe
H
H
H
H



26
2
CONHMe
H
H
H
H



27
3
CONHMe
H
H
H
H



28
4
CONHMe
H
H
H
H



29
1
SO2Me
H
H
H
H



30
2
SO2Me
H
H
H
H



31
3
SO2Me
H
H
H
H



32
4
SO2Me
H
H
H
H



33
1
SO2NH2
H
H
H
H



34
2
SO2NH2
H
H
H
H



35
3
SO2NH2
H
H
H
H



36
4
SO2NH2
H
H
H
H



37
1
H
H
H
OH
H



38
2
H
H
H
OH
H



39
3
H
H
H
OH
H



40
4
H
H
H
OH
H



41
1
Me
H
H
OH
H



42
2
Me
H
H
OH
H



43
3
Me
H
H
OH
H



44
4
Me
H
H
OH
H



45
1
CH2Ph
H
H
OH
H



46
2
CH2Ph
H
H
OH
H



47
3
CH2Ph
H
H
OH
H



48
4
CH2Ph
H
H
OH
H



49
1
COMe
H
H
OH
H



50
2
COMe
H
H
OH
H



51
3
COMe
H
H
OH
H



52
4
COMe
H
H
OH
H



53
1
CO2Me
H
H
OH
H



54
2
CO2Me
H
H
OH
H



55
3
CO2Me
H
H
OH
H



56
4
CO2Me
H
H
OH
H



57
1
CO2tBu
H
H
OH
H



58
2
CO2tBu
H
H
OH
H



59
3
CO2tBu
H
H
OH
H



60
4
CO2tBu
H
H
OH
H



61
1
CONHMe
H
H
OH
H



62
2
CONHMe
H
H
OH
H



63
3
CONHMe
H
H
OH
H



64
4
CONHMe
H
H
OH
H



65
1
SO2Me
H
H
OH
H



66
2
SO2Me
H
H
OH
H



67
3
SO2Me
H
H
OH
H



68
4
SO2Me
H
H
OH
H



69
1
SO2NH2
H
H
OH
H



70
2
SO2NH2
H
H
OH
H



71
3
SO2NH2
H
H
OH
H



72
4
SO2NH2
H
H
OH
H



73
1
H
H
H
OMe
H



74
2
H
H
H
OMe
H



75
3
H
H
H
OMe
H



76
4
H
H
H
OMe
H



77
1
Me
H
H
OMe
H



78
2
Me
H
H
OMe
H



79
3
Me
H
H
OMe
H



80
4
Me
H
H
OMe
H



81
1
CH2Ph
H
H
OMe
H



82
2
CH2Ph
H
H
OMe
H



83
3
CH2Ph
H
H
OMe
H



84
4
CH2Ph
H
H
OMe
H



85
1
COMe
H
H
OMe
H



86
2
COMe
H
H
OMe
H



87
3
COMe
H
H
OMe
H



88
4
COMe
H
H
OMe
H



89
1
CO2Me
H
H
OMe
H



90
2
CO2Me
H
H
OMe
H



91
3
CO2Me
H
H
OMe
H



92
4
CO2Me
H
H
OMe
H



93
1
CO2tBu
H
H
OMe
H



94
2
CO2tBu
H
H
OMe
H



95
3
CO2tBu
H
H
OMe
H



96
1
CO2tBu
H
H
OMe
H



97
1
CONHMe
H
H
OMe
H



98
2
CONHMe
H
H
OMe
H



99
3
CONHMe
H
H
OMe
H



100
4
CONHMe
H
H
OMe
H



101
1
SO2Me
H
H
OMe
H



102
2
SO2Me
H
H
OMe
H



103
3
SO2Me
H
H
OMe
H



104
4
SO2Me
H
H
OMe
H



105
1
SO2NH2
H
H
OMe
H



106
2
SO2NH2
H
H
OMe
H



107
3
SO2NH2
H
H
OMe
H



108
4
SO2NH2
H
H
OMe
H



109
1
H
H
H
Me
H



110
2
H
H
H
Me
H



111
3
H
H
H
Me
H



112
4
H
H
H
Me
H



113
1
Me
H
H
Me
H



114
2
Me
H
H
Me
H



115
3
Me
H
H
Me
H



116
4
Me
H
H
Me
H



117
1
CH2Ph
H
H
Me
H



118
2
CH2Ph
H
H
Me
H



119
3
CH2Ph
H
H
Me
H



120
4
CH2Ph
H
H
Me
H



121
1
COMe
H
H
Me
H



122
2
COMe
H
H
Me
H



123
3
COMe
H
H
Me
H



124
4
COMe
H
H
Me
H



125
1
CO2Me
H
H
Me
H



126
2
CO2Me
H
H
Me
H



127
3
CO2Me
H
H
Me
H



128
4
CO2Me
H
H
Me
H



129
1
CO2tBu
H
H
Me
H



130
2
CO2tBu
H
H
Me
H



131
3
CO2tBu
H
H
Me
H



132
4
CO2tBu
H
H
Me
H



133
1
CONHMe
H
H
Me
H



134
2
CONHMe
H
H
Me
H



135
3
CONHMe
H
H
Me
H



136
4
CONHMe
H
H
Me
H



137
1
SO2Me
H
H
Me
H



138
2
SO2Me
H
H
Me
H



139
3
SO2Me
H
H
Me
H



140
4
SO2Me
H
H
Me
H



141
1
SO2NH2
H
H
Me
H



142
2
SO2NH2
H
H
Me
H



143
3
SO2NH2
H
H
Me
H



144
4
SO2NH2
H
H
Me
H



145
1
H
H
H
CF3
H



146
2
H
H
H
CF3
H



147
3
H
H
H
CF3
H



148
4
H
H
H
CF3
H



149
1
Me
H
H
CF3
H



150
2
Me
H
H
CF3
H



151
3
Me
H
H
CF3
H



152
4
Me
H
H
CF3
H



153
1
CH2Ph
H
H
CF3
H



154
2
CH2Ph
H
H
CF3
H



155
3
CH2Ph
H
H
CF3
H



156
4
CH2Ph
H
H
CF3
H



157
1
COMe
H
H
CF3
H



158
2
COMe
H
H
CF3
H



159
3
COMe
H
H
CF3
H



160
4
COMe
H
H
CF3
H



161
1
CO2Me
H
H
CF3
H



162
2
CO2Me
H
H
CF3
H



163
3
CO2Me
H
H
CF3
H



164
4
CO2Me
H
H
CF3
H



165
1
CO2tBu
H
H
CF3
H



166
2
CO2tBu
H
H
CF3
H



167
3
CO2tBu
H
H
CF3
H



168
4
CO2tBu
H
H
CF3
H



169
1
CONHMe
H
H
CF3
H



170
2
CONHMe
H
H
CF3
H



171
3
CONHMe
H
H
CF3
H



172
4
CONHMe
H
H
CF3
H



173
1
SO2Me
H
H
CF3
H



174
2
SO2Me
H
H
CF3
H



175
3
SO2Me
H
H
CF3
H



176
4
SO2Me
H
H
CF3
H



177
1
SO2NH2
H
H
CF3
H



178
2
SO2NH2
H
H
CF3
H



179
3
SO2NH2
H
H
CF3
H



180
4
SO2NH2
H
H
CF3
H



181
1
H
H
H
F
H



182
2
H
H
H
F
H



183
3
H
H
H
F
H



184
4
H
H
H
F
H



185
1
Me
H
H
F
H



186
2
Me
H
H
F
H



187
3
Me
H
H
F
H



188
4
Me
H
H
F
H



189
1
CH2Ph
H
H
F
H



190
2
CH2Ph
H
H
F
H



191
3
CH2Ph
H
H
F
H



192
4
CH2Ph
H
H
F
H



193
1
COMe
H
H
F
H



194
2
COMe
H
H
F
H



195
3
COMe
H
H
F
H



196
4
COMe
H
H
F
H



197
1
CO2Me
H
H
F
H



198
2
CO2Me
H
H
F
H



199
3
CO2Me
H
H
F
H



200
4
CO2Me
H
H
F
H



201
1
CO2tBu
H
H
F
H



202
2
CO2tBu
H
H
F
H



203
3
CO2tBu
H
H
F
H



204
4
CO2tBu
H
H
F
H



205
1
CONHMe
H
H
F
H



206
2
CONHMe
H
H
F
H



207
3
CONHMe
H
H
F
H



208
4
CONHMe
H
H
F
H



209
1
SO2Me
H
H
F
H



210
2
SO2Me
H
H
F
H



211
3
SO2Me
H
H
F
H



212
4
SO2Me
H
H
F
H



213
1
SO2NH2
H
H
F
H



214
2
SO2NH2
H
H
F
H



215
3
SO2NH2
H
H
F
H



216
4
SO2NH2
H
H
F
H



217
1
H
H
H
Cl
H



218
2
H
H
H
Cl
H



219
3
H
H
H
Cl
H



220
4
H
H
H
Cl
H



221
1
Me
H
H
Cl
H



222
2
Me
H
H
Cl
H



223
3
Me
H
H
Cl
H



224
4
Me
H
H
Cl
H



225
1
CH2Ph
H
H
Cl
H



226
2
CH2Ph
H
H
Cl
H



227
3
CH2Ph
H
H
Cl
H



228
4
CH2Ph
H
H
Cl
H



229
1
COMe
H
H
Cl
H



230
2
COMe
H
H
Cl
H



231
3
COMe
H
H
Cl
H



232
4
COMe
H
H
Cl
H



233
1
CO2Me
H
H
Cl
H



234
2
CO2Me
H
H
Cl
H



235
3
CO2Me
H
H
Cl
H



236
4
CO2Me
H
H
Cl
H



237
1
CO2tBu
H
H
Cl
H



238
2
CO2tBu
H
H
Cl
H



239
3
CO2tBu
H
H
Cl
H



240
4
CO2tBu
H
H
Cl
H



241
1
CONHMe
H
H
Cl
H



242
2
CONHMe
H
H
Cl
H



243
3
CONHMe
H
H
Cl
H



244
4
CONHMe
H
H
Cl
H



245
1
SO2Me
H
H
Cl
H



246
2
SO2Me
H
H
Cl
H



247
3
SO2Me
H
H
Cl
H



248
4
SO2Me
H
H
Cl
H



249
1
SO2NH2
H
H
Cl
H



250
2
SO2NH2
H
H
Cl
H



251
3
SO2NH2
H
H
Cl
H



252
4
SO2NH2
H
H
Cl
H



253
1
H
H
H
CN
H



254
2
H
H
H
CN
H



255
3
H
H
H
CN
H



256
4
H
H
H
CN
H



257
1
Me
H
H
CN
H



258
2
Me
H
H
CN
H



259
3
Me
H
H
CN
H



260
4
Me
H
H
CN
H



261
1
CH2Ph
H
H
CN
H



262
2
CH2Ph
H
H
CN
H



263
3
CH2Ph
H
H
CN
H



264
4
CH2Ph
H
H
CN
H



265
1
COMe
H
H
CN
H



266
2
COMe
H
H
CN
H



267
3
COMe
H
H
CN
H



268
4
COMe
H
H
CN
H



269
1
CO2Me
H
H
CN
H



270
2
CO2Me
H
H
CN
H



271
3
CO2Me
H
H
CN
H



272
4
CO2Me
H
H
CN
H



273
1
CO2tBu
H
H
CN
H



274
2
CO2tBu
H
H
CN
H



275
3
CO2tBu
H
H
CN
H



276
4
CO2tBu
H
H
CN
H



277
1
CONHMe
H
H
CN
H



278
2
CONHMe
H
H
CN
H



279
3
CONHMe
H
H
CN
H



280
4
CONHMe
H
H
CN
H



281
1
SO2Me
H
H
CN
H



282
2
SO2Me
H
H
CN
H



283
3
SO2Me
H
H
CN
H



284
4
SO2Me
H
H
CN
H



285
1
SO2NH2
H
H
CN
H



286
2
SO2NH2
H
H
CN
H



287
3
SO2NH2
H
H
CN
H



288
4
SO2NH2
H
H
CN
H



289
1
H
H
OH
H
H



290
2
H
H
OH
H
H



291
3
H
H
OH
H
H



292
4
H
H
OH
H
H



293
1
Me
H
OH
H
H



294
2
Me
H
OH
H
H



295
3
Me
H
OH
H
H



296
4
Me
H
OH
H
H



297
1
CH2Ph
H
OH
H
H



298
2
CH2Ph
H
OH
H
H



299
3
CH2Ph
H
OH
H
H



300
4
CH2Ph
H
OH
H
H



301
1
COMe
H
OH
H
H



302
2
COMe
H
OH
H
H



303
3
COMe
H
OH
H
H



304
4
COMe
H
OH
H
H



305
1
CO2Me
H
OH
H
H



306
2
CO2Me
H
OH
H
H



307
3
CO2Me
H
OH
H
H



308
4
CO2Me
H
OH
H
H



309
1
CO2tBu
H
OH
H
H



310
2
CO2tBu
H
OH
H
H



311
3
CO2tBu
H
OH
H
H



312
4
CO2tBu
H
OH
H
H



313
1
CONHMe
H
OH
H
H



314
2
CONHMe
H
OH
H
H



315
3
CONHMe
H
OH
H
H



316
4
CONHMe
H
OH
H
H



317
1
SO2Me
H
OH
H
H



318
2
SO2Me
H
OH
H
H



319
3
SO2Me
H
OH
H
H



320
4
SO2Me
H
OH
H
H



321
1
SO2NH2
H
OH
H
H



322
2
SO2NH2
H
OH
H
H



323
3
SO2NH2
H
OH
H
H



324
4
SO2NH2
H
OH
H
H



325
1
H
H
OMe
H
H



326
2
H
H
OMe
H
H



327
3
H
H
OMe
H
H



328
4
H
H
OMe
H
H



329
1
Me
H
OMe
H
H



330
2
Me
H
OMe
H
H



331
3
Me
H
OMe
H
H



332
4
Me
H
OMe
H
H



333
1
CH2Ph
H
OMe
H
H



334
2
CH2Ph
H
OMe
H
H



335
3
CH2Ph
H
OMe
H
H



336
4
CH2Ph
H
OMe
H
H



337
1
COMe
H
OMe
H
H



338
2
COMe
H
OMe
H
H



339
3
COMe
H
OMe
H
H



340
4
COMe
H
OMe
H
H



341
1
CO2Me
H
OMe
H
H



342
2
CO2Me
H
OMe
H
H



343
3
CO2Me
H
OMe
H
H



344
4
CO2Me
H
OMe
H
H



345
1
CO2tBu
H
OMe
H
H



346
2
CO2tBu
H
OMe
H
H



347
3
CO2tBu
H
OMe
H
H



348
4
CO2tBu
H
OMe
H
H



349
1
CONHMe
H
OMe
H
H



350
2
CONHMe
H
OMe
H
H



351
3
CONHMe
H
OMe
H
H



352
4
CONHMe
H
OMe
H
H



353
1
SO2Me
H
OMe
H
H



354
2
SO2Me
H
OMe
H
H



355
3
SO2Me
H
OMe
H
H



356
4
SO2Me
H
OMe
H
H



357
1
SO2NH2
H
OMe
H
H



358
2
SO2NH2
H
OMe
H
H



359
3
SO2NH2
H
OMe
H
H



360
4
SO2NH2
H
OMe
H
H



361
1
H
H
Me
H
H



362
2
H
H
Me
H
H



363
3
H
H
Me
H
H



364
4
H
H
Me
H
H



365
1
Me
H
Me
H
H



366
2
Me
H
Me
H
H



367
3
Me
H
Me
H
H



368
4
Me
H
Me
H
H



369
1
CH2Ph
H
Me
H
H



370
2
CH2Ph
H
Me
H
H



371
3
CH2Ph
H
Me
H
H



372
4
CH2Ph
H
Me
H
H



373
1
COMe
H
Me
H
H



374
2
COMe
H
Me
H
H



375
3
COMe
H
Me
H
H



376
4
COMe
H
Me
H
H



377
1
CO2Me
H
Me
H
H



378
2
CO2Me
H
Me
H
H



379
3
CO2Me
H
Me
H
H



380
4
CO2Me
H
Me
H
H



381
1
CO2tBu
H
Me
H
H



382
2
CO2tBu
H
Me
H
H



383
3
CO2tBu
H
Me
H
H



384
4
CO2tBu
H
Me
H
H



385
1
CONHMe
H
Me
H
H



386
2
CONHMe
H
Me
H
H



387
3
CONHMe
H
Me
H
H



388
4
CONHMe
H
Me
H
H



389
1
SO2Me
H
Me
H
H



390
2
SO2Me
H
Me
H
H



391
3
SO2Me
H
Me
H
H



392
4
SO2Me
H
Me
H
H



393
1
SO2NH2
H
Me
H
H



394
2
SO2NH2
H
Me
H
H



395
3
SO2NH2
H
Me
H
H



396
4
SO2NH2
H
Me
H
H



397
1
H
H
CF3
H
H



398
2
H
H
CF3
H
H



399
3
H
H
CF3
H
H



400
4
H
H
CF3
H
H



401
1
Me
H
CF3
H
H



402
2
Me
H
CF3
H
H



403
3
Me
H
CF3
H
H



404
4
Me
H
CF3
H
H



405
1
CH2Ph
H
CF3
H
H



406
2
CH2Ph
H
CF3
H
H



407
3
CH2Ph
H
CF3
H
H



408
4
CH2Ph
H
CF3
H
H



409
1
COMe
H
CF3
H
H



410
2
COMe
H
CF3
H
H



411
3
COMe
H
CF3
H
H



412
4
COMe
H
CF3
H
H



413
1
CO2Me
H
CF3
H
H



414
2
CO2Me
H
CF3
H
H



415
3
CO2Me
H
CF3
H
H



416
4
CO2Me
H
CF3
H
H



417
1
CO2tBu
H
CF3
H
H



418
2
CO2tBu
H
CF3
H
H



419
3
CO2tBu
H
CF3
H
H



420
4
CO2tBu
H
CF3
H
H



421
1
CONHMe
H
CF3
H
H



422
2
CONHMe
H
CF3
H
H



423
3
CONHMe
H
CF3
H
H



424
4
CONHMe
H
CF3
H
H



425
1
SO2Me
H
CF3
H
H



426
2
SO2Me
H
CF3
H
H



427
3
SO2Me
H
CF3
H
H



428
4
SO2Me
H
CF3
H
H



429
1
SO2NH2
H
CF3
H
H



430
2
SO2NH2
H
CF3
H
H



431
3
SO2NH2
H
CF3
H
H



432
4
SO2NH2
H
CF3
H
H



433
1
H
H
F
H
H



434
2
H
H
F
H
H



435
3
H
H
F
H
H



436
3
H
H
F
H
H



437
1
Me
H
F
H
H



438
2
Me
H
F
H
H



439
3
Me
H
F
H
H



440
4
Me
H
F
H
H



441
1
CH2Ph
H
F
H
H



442
2
CH2Ph
H
F
H
H



443
3
CH2Ph
H
F
H
H



444
4
CH2Ph
H
F
H
H



445
1
COMe
H
F
H
H



446
2
COMe
H
F
H
H



447
3
COMe
H
F
H
H



448
4
COMe
H
F
H
H



449
1
CO2Me
H
F
H
H



450
2
CO2Me
H
F
H
H



451
3
CO2Me
H
F
H
H



452
4
CO2Me
H
F
H
H



453
1
CO2tBu
H
F
H
H



454
2
CO2tBu
H
F
H
H



455
3
CO2tBu
H
F
H
H



456
4
CO2tBu
H
F
H
H



457
1
CONHMe
H
F
H
H



458
2
CONHMe
H
F
H
H



459
3
CONHMe
H
F
H
H



460
4
CONHMe
H
F
H
H



461
1
SO2Me
H
F
H
H



462
2
SO2Me
H
F
H
H



463
3
SO2Me
H
F
H
H



464
4
SO2Me
H
F
H
H



465
1
SO2NH2
H
F
H
H



466
2
SO2NH2
H
F
H
H



467
3
SO2NH2
H
F
H
H



468
4
SO2NH2
H
F
H
H



469
1
H
H
Cl
H
H



470
2
H
H
Cl
H
H



471
3
H
H
Cl
H
H



472
4
H
H
Cl
H
H



473
1
Me
H
Cl
H
H



474
2
Me
H
Cl
H
H



475
3
Me
H
Cl
H
H



476
4
Me
H
Cl
H
H



477
1
CH2Ph
H
Cl
H
H



478
2
CH2Ph
H
Cl
H
H



479
3
CH2Ph
H
Cl
H
H



480
4
CH2Ph
H
Cl
H
H



481
1
COMe
H
Cl
H
H



482
2
COMe
H
Cl
H
H



483
3
COMe
H
Cl
H
H



484
4
COMe
H
Cl
H
H



485
1
CO2Me
H
Cl
H
H



486
2
CO2Me
H
Cl
H
H



487
3
CO2Me
H
Cl
H
H



488
4
CO2Me
H
Cl
H
H



489
1
CO2tBu
H
Cl
H
H



490
2
CO2tBu
H
Cl
H
H



491
3
CO2tBu
H
Cl
H
H



492
4
CO2tBu
H
Cl
H
H



493
1
CONHMe
H
Cl
H
H



494
2
CONHMe
H
Cl
H
H



495
3
CONHMe
H
Cl
H
H



496
4
CONHMe
H
Cl
H
H



497
1
SO2Me
H
Cl
H
H



498
2
SO2Me
H
Cl
H
H



499
3
SO2Me
H
Cl
H
H



500
4
SO2Me
H
Cl
H
H



501
1
SO2NH2
H
Cl
H
H



502
2
SO2NH2
H
Cl
H
H



503
3
SO2NH2
H
Cl
H
H



504
4
SO2NH2
H
Cl
H
H



505
1
H
H
CN
H
H



506
2
H
H
CN
H
H



507
3
H
H
CN
H
H



508
4
H
H
CN
H
H



509
1
Me
H
CN
H
H



510
2
Me
H
CN
H
H



511
3
Me
H
CN
H
H



512
4
Me
H
CN
H
H



513
1
CH2Ph
H
CN
H
H



514
2
CH2Ph
H
CN
H
H



515
3
CH2Ph
H
CN
H
H



516
4
CH2Ph
H
CN
H
H



517
1
COMe
H
CN
H
H



518
2
COMe
H
CN
H
H



519
3
COMe
H
CN
H
H



520
4
COMe
H
CN
H
H



521
1
CO2Me
H
CN
H
H



522
2
CO2Me
H
CN
H
H



523
3
CO2Me
H
CN
H
H



524
4
CO2Me
H
CN
H
H



525
1
CO2tBu
H
CN
H
H



526
2
CO2tBu
H
CN
H
H



527
3
CO2tBu
H
CN
H
H



528
4
CO2tBu
H
CN
H
H



529
1
CONHMe
H
CN
H
H



530
2
CONHMe
H
CN
H
H



531
3
CONHMe
H
CN
H
H



532
4
CONHMe
H
CN
H
H



533
1
SO2Me
H
CN
H
H



534
2
SO2Me
H
CN
H
H



535
3
SO2Me
H
CN
H
H



536
4
SO2Me
H
CN
H
H



537
1
SO2NH2
H
CN
H
H



538
2
SO2NH2
H
CN
H
H



539
3
SO2NH2
H
CN
H
H



540
4
SO2NH2
H
CN
H
H



541
1
H
OH
H
H
H



542
2
H
OH
H
H
H



543
3
H
OH
H
H
H



544
4
H
OH
H
H
H



545
1
Me
OH
H
H
H



546
2
Me
OH
H
H
H



547
3
Me
OH
H
H
H



548
4
Me
OH
H
H
H



549
1
CH2Ph
OH
H
H
H



550
2
CH2Ph
OH
H
H
H



551
3
CH2Ph
OH
H
H
H



552
4
CH2Ph
OH
H
H
H



553
1
COMe
OH
H
H
H



554
2
COMe
OH
H
H
H



555
3
COMe
OH
H
H
H



556
4
COMe
OH
H
H
H



557
1
CO2Me
OH
H
H
H



558
2
CO2Me
OH
H
H
H



559
3
CO2Me
OH
H
H
H



560
4
CO2Me
OH
H
H
H



561
1
CO2tBu
OH
H
H
H



562
2
CO2tBu
OH
H
H
H



563
3
CO2tBu
OH
H
H
H



564
4
CO2tBu
OH
H
H
H



565
1
CONHMe
OH
H
H
H



566
2
CONHMe
OH
H
H
H



567
3
CONHMe
OH
H
H
H



568
4
CONHMe
OH
H
H
H



569
1
SO2Me
OH
H
H
H



570
2
SO2Me
OH
H
H
H



571
3
SO2Me
OH
H
H
H



572
4
SO2Me
OH
H
H
H



573
1
SO2NH2
OH
H
H
H



574
2
SO2NH2
OH
H
H
H



575
3
SO2NH2
OH
H
H
H



576
4
SO2NH2
OH
H
H
H



577
1
H
OMe
H
H
H



578
2
H
OMe
H
H
H



579
3
H
OMe
H
H
H



580
4
H
OMe
H
H
H



581
1
Me
OMe
H
H
H



582
2
Me
OMe
H
H
H



583
3
Me
OMe
H
H
H



584
4
Me
OMe
H
H
H



585
1
CH2Ph
OMe
H
H
H



586
2
CH2Ph
OMe
H
H
H



587
3
CH2Ph
OMe
H
H
H



588
4
CH2Ph
OMe
H
H
H



589
1
COMe
OMe
H
H
H



590
2
COMe
OMe
H
H
H



591
3
COMe
OMe
H
H
H



592
4
COMe
OMe
H
H
H



593
1
CO2Me
OMe
H
H
H



594
2
CO2Me
OMe
H
H
H



595
3
CO2Me
OMe
H
H
H



596
4
CO2Me
OMe
H
H
H



597
1
CO2tBu
OMe
H
H
H



598
2
CO2tBu
OMe
H
H
H



599
3
CO2tBu
OMe
H
H
H



600
4
CO2tBu
OMe
H
H
H



601
1
CONHMe
OMe
H
H
H



602
2
CONHMe
OMe
H
H
H



603
3
CONHMe
OMe
H
H
H



604
4
CONHMe
OMe
H
H
H



605
1
SO2Me
OMe
H
H
H



606
2
SO2Me
OMe
H
H
H



607
3
SO2Me
OMe
H
H
H



608
4
SO2Me
OMe
H
H
H



609
1
SO2NH2
OMe
H
H
H



610
2
SO2NH2
OMe
H
H
H



611
3
SO2NH2
OMe
H
H
H



612
4
SO2NH2
OMe
H
H
H



613
1
H
Me
H
H
H



614
2
H
Me
H
H
H



615
3
H
Me
H
H
H



616
4
H
Me
H
H
H



617
1
Me
Me
H
H
H



618
2
Me
Me
H
H
H



619
3
Me
Me
H
H
H



620
4
Me
Me
H
H
H



621
1
CH2Ph
Me
H
H
H



622
2
CH2Ph
Me
H
H
H



623
3
CH2Ph
Me
H
H
H



624
4
CH2Ph
Me
H
H
H



625
1
COMe
Me
H
H
H



626
2
COMe
Me
H
H
H



627
3
COMe
Me
H
H
H



628
4
COMe
Me
H
H
H



629
1
CO2Me
Me
H
H
H



630
2
CO2Me
Me
H
H
H



631
3
CO2Me
Me
H
H
H



632
4
CO2Me
Me
H
H
H



633
1
CO2tBu
Me
H
H
H



634
2
CO2tBu
Me
H
H
H



635
3
CO2tBu
Me
H
H
H



636
4
CO2tBu
Me
H
H
H



637
1
CONHMe
Me
H
H
H



638
2
CONHMe
Me
H
H
H



639
3
CONHMe
Me
H
H
H



640
4
CONHMe
Me
H
H
H



641
1
SO2Me
Me
H
H
H



642
2
SO2Me
Me
H
H
H



643
3
SO2Me
Me
H
H
H



644
4
SO2Me
Me
H
H
H



645
1
SO2NH2
Me
H
H
H



646
2
SO2NH2
Me
H
H
H



647
3
SO2NH2
Me
H
H
H



648
4
SO2NH2
Me
H
H
H



649
1
H
CF3
H
H
H



650
2
H
CF3
H
H
H



651
3
H
CF3
H
H
H



652
4
H
CF3
H
H
H



653
1
Me
CF3
H
H
H



654
2
Me
CF3
H
H
H



655
3
Me
CF3
H
H
H



656
4
Me
CF3
H
H
H



657
1
CH2Ph
CF3
H
H
H



658
2
CH2Ph
CF3
H
H
H



659
3
CH2Ph
CF3
H
H
H



660
4
CH2Ph
CF3
H
H
H



661
1
COMe
CF3
H
H
H



662
2
COMe
CF3
H
H
H



663
3
COMe
CF3
H
H
H



664
4
COMe
CF3
H
H
H



665
1
CO2Me
CF3
H
H
H



666
2
CO2Me
CF3
H
H
H



667
3
CO2Me
CF3
H
H
H



668
4
CO2Me
CF3
H
H
H



669
1
CO2tBu
CF3
H
H
H



670
2
CO2tBu
CF3
H
H
H



671
3
CO2tBu
CF3
H
H
H



672
4
CO2tBu
CF3
H
H
H



673
1
CONHMe
CF3
H
H
H



674
2
CONHMe
CF3
H
H
H



675
3
CONHMe
CF3
H
H
H



676
4
CONHMe
CF3
H
H
H



677
1
SO2Me
CF3
H
H
H



678
2
SO2Me
CF3
H
H
H



679
3
SO2Me
CF3
H
H
H



680
4
SO2Me
CF3
H
H
H



681
1
SO2NH2
CF3
H
H
H



682
2
SO2NH2
CF3
H
H
H



683
3
SO2NH2
CF3
H
H
H



684
4
SO2NH2
CF3
H
H
H



685
1
H
F
H
H
H



686
2
H
F
H
H
H



687
3
H
F
H
H
H



688
3
H
F
H
H
H



689
1
Me
F
H
H
H



690
2
Me
F
H
H
H



691
3
Me
F
H
H
H



692
4
Me
F
H
H
H



693
1
CH2Ph
F
H
H
H



694
2
CH2Ph
F
H
H
H



695
3
CH2Ph
F
H
H
H



696
4
CH2Ph
F
H
H
H



697
1
COMe
F
H
H
H



698
2
COMe
F
H
H
H



699
3
COMe
F
H
H
H



700
4
COMe
F
H
H
H



701
1
CO2Me
F
H
H
H



702
2
CO2Me
F
H
H
H



703
3
CO2Me
F
H
H
H



704
4
CO2Me
F
H
H
H



705
1
CO2tBu
F
H
H
H



706
2
CO2tBu
F
H
H
H



707
3
CO2tBu
F
H
H
H



708
4
CO2tBu
F
H
H
H



709
1
CONHMe
F
H
H
H



710
2
CONHMe
F
H
H
H



711
3
CONHMe
F
H
H
H



712
4
CONHMe
F
H
H
H



713
1
SO2Me
F
H
H
H



714
2
SO2Me
F
H
H
H



715
3
SO2Me
F
H
H
H



716
4
SO2Me
F
H
H
H



717
1
SO2NH2
F
H
H
H



718
2
SO2NH2
F
H
H
H



719
3
SO2NH2
F
H
H
H



720
4
SO2NH2
F
H
H
H



721
1
H
Cl
H
H
H



722
2
H
Cl
H
H
H



723
3
H
Cl
H
H
H



724
4
H
Cl
H
H
H



725
1
Me
Cl
H
H
H



726
2
Me
Cl
H
H
H



727
3
Me
Cl
H
H
H



728
4
Me
Cl
H
H
H



729
1
CH2Ph
Cl
H
H
H



730
2
CH2Ph
Cl
H
H
H



731
3
CH2Ph
Cl
H
H
H



732
4
CH2Ph
Cl
H
H
H



733
1
COMe
Cl
H
H
H



734
2
COMe
Cl
H
H
H



735
3
COMe
Cl
H
H
H



736
4
COMe
Cl
H
H
H



737
1
CO2Me
Cl
H
H
H



738
2
CO2Me
Cl
H
H
H



739
3
CO2Me
Cl
H
H
H



740
4
CO2Me
Cl
H
H
H



741
1
CO2tBu
Cl
H
H
H



742
2
CO2tBu
Cl
H
H
H



743
3
CO2tBu
Cl
H
H
H



744
4
CO2tBu
Cl
H
H
H



745
1
CONHMe
Cl
H
H
H



746
2
CONHMe
Cl
H
H
H



747
3
CONHMe
Cl
H
H
H



748
4
CONHMe
Cl
H
H
H



749
1
SO2Me
Cl
H
H
H



750
2
SO2Me
Cl
H
H
H



751
3
SO2Me
Cl
H
H
H



752
4
SO2Me
Cl
H
H
H



753
1
SO2NH2
Cl
H
H
H



754
2
SO2NH2
Cl
H
H
H



755
3
SO2NH2
Cl
H
H
H



756
4
SO2NH2
Cl
H
H
H



757
1
H
CN
H
H
H



758
2
H
CN
H
H
H



759
3
H
CN
H
H
H



760
4
H
CN
H
H
H



761
1
Me
CN
H
H
H



762
2
Me
CN
H
H
H



763
3
Me
CN
H
H
H



764
4
Me
CN
H
H
H



765
1
CH2Ph
CN
H
H
H



766
2
CH2Ph
CN
H
H
H



767
3
CH2Ph
CN
H
H
H



768
4
CH2Ph
CN
H
H
H



769
1
COMe
CN
H
H
H



770
2
COMe
CN
H
H
H



771
3
COMe
CN
H
H
H



772
4
COMe
CN
H
H
H



773
1
CO2Me
CN
H
H
H



774
2
CO2Me
CN
H
H
H



775
3
CO2Me
CN
H
H
H



776
4
CO2Me
CN
H
H
H



777
1
CO2tBu
CN
H
H
H



778
2
CO2tBu
CN
H
H
H



779
3
CO2tBu
CN
H
H
H



780
4
CO2tBu
CN
H
H
H



781
1
CONHMe
CN
H
H
H



782
2
CONHMe
CN
H
H
H



783
3
CONHMe
CN
H
H
H



784
4
CONHMe
CN
H
H
H



785
1
SO2Me
CN
H
H
H



786
2
SO2Me
CN
H
H
H



787
3
SO2Me
CN
H
H
H



788
4
SO2Me
CN
H
H
H



789
1
SO2NH2
CN
H
H
H



790
2
SO2NH2
CN
H
H
H



791
3
SO2NH2
CN
H
H
H



792
4
SO2NH2
CN
H
H
H



793
1
H
H
H
H
OH



794
2
H
H
H
H
OH



795
3
H
H
H
H
OH



796
4
H
H
H
H
OH



797
1
Me
H
H
H
OH



798
2
Me
H
H
H
OH



799
3
Me
H
H
H
OH



800
4
Me
H
H
H
OH



801
1
CH2Ph
H
H
H
OH



802
2
CH2Ph
H
H
H
OH



803
3
CH2Ph
H
H
H
OH



804
4
CH2Ph
H
H
H
OH



805
1
COMe
H
H
H
OH



806
2
COMe
H
H
H
OH



807
3
COMe
H
H
H
OH



808
4
COMe
H
H
H
OH



809
1
CO2Me
H
H
H
OH



810
2
CO2Me
H
H
H
OH



811
3
CO2Me
H
H
H
OH



812
4
CO2Me
H
H
H
OH



813
1
CO2tBu
H
H
H
OH



814
2
CO2tBu
H
H
H
OH



815
3
CO2tBu
H
H
H
OH



816
4
CO2tBu
H
H
H
OH



817
1
CONHMe
H
H
H
OH



818
2
CONHMe
H
H
H
OH



819
3
CONHMe
H
H
H
OH



820
4
CONHMe
H
H
H
OH



821
1
SO2Me
H
H
H
OH



822
2
SO2Me
H
H
H
OH



823
3
SO2Me
H
H
H
OH



824
4
SO2Me
H
H
H
OH



825
1
SO2NH2
H
H
H
OH



826
2
SO2NH2
H
H
H
OH



827
3
SO2NH2
H
H
H
OH



828
4
SO2NH2
H
H
H
OH



829
1
H
H
H
H
OMe



830
2
H
H
H
H
OMe



831
3
H
H
H
H
OMe



832
4
H
H
H
H
OMe



833
1
Me
H
H
H
OMe



834
2
Me
H
H
H
OMe



835
3
Me
H
H
H
OMe



836
4
Me
H
H
H
OMe



837
1
CH2Ph
H
H
H
OMe



838
2
CH2Ph
H
H
H
OMe



839
3
CH2Ph
H
H
H
OMe



840
4
CH2Ph
H
H
H
OMe



841
1
COMe
H
H
H
OMe



842
2
COMe
H
H
H
OMe



843
3
COMe
H
H
H
OMe



844
4
COMe
H
H
H
OMe



845
1
CO2Me
H
H
H
OMe



846
2
CO2Me
H
H
H
OMe



847
3
CO2Me
H
H
H
OMe



848
4
CO2Me
H
H
H
OMe



849
1
CO2tBu
H
H
H
OMe



850
2
CO2tBu
H
H
H
OMe



851
3
CO2tBu
H
H
H
OMe



852
4
CO2tBu
H
H
H
OMe



853
1
CONHMe
H
H
H
OMe



854
2
CONHMe
H
H
H
OMe



855
3
CONHMe
H
H
H
OMe



856
4
CONHMe
H
H
H
OMe



857
1
SO2Me
H
H
H
OMe



858
2
SO2Me
H
H
H
OMe



859
3
SO2Me
H
H
H
OMe



860
4
SO2Me
H
H
H
OMe



861
1
SO2NH2
H
H
H
OMe



862
2
SO2NH2
H
H
H
OMe



863
3
SO2NH2
H
H
H
OMe



864
4
SO2NH2
H
H
H
OMe



865
1
H
H
H
H
Me



866
2
H
H
H
H
Me



867
3
H
H
H
H
Me



868
4
H
H
H
H
Me



869
1
Me
H
H
H
Me



870
2
Me
H
H
H
Me



871
3
Me
H
H
H
Me



872
4
Me
H
H
H
Me



873
1
CH2Ph
H
H
H
Me



874
2
CH2Ph
H
H
H
Me



875
3
CH2Ph
H
H
H
Me



876
4
CH2Ph
H
H
H
Me



877
1
COMe
H
H
H
Me



878
2
COMe
H
H
H
Me



879
3
COMe
H
H
H
Me



880
4
COMe
H
H
H
Me



881
1
CO2Me
H
H
H
Me



882
2
CO2Me
H
H
H
Me



883
3
CO2Me
H
H
H
Me



884
4
CO2Me
H
H
H
Me



885
1
CO2tBu
H
H
H
Me



886
2
CO2tBu
H
H
H
Me



887
3
CO2tBu
H
H
H
Me



888
4
CO2tBu
H
H
H
Me



889
1
CONHMe
H
H
H
Me



890
2
CONHMe
H
H
H
Me



891
3
CONHMe
H
H
H
Me



892
4
CONHMe
H
H
H
Me



893
1
SO2Me
H
H
H
Me



894
2
SO2Me
H
H
H
Me



895
3
SO2Me
H
H
H
Me



896
4
SO2Me
H
H
H
Me



897
1
SO2NH2
H
H
H
Me



898
2
SO2NH2
H
H
H
Me



899
3
SO2NH2
H
H
H
Me



900
4
SO2NH2
H
H
H
Me



901
1
H
H
H
H
CF3



902
2
H
H
H
H
CF3



903
3
H
H
H
H
CF3



904
4
H
H
H
H
CF3



905
1
Me
H
H
H
CF3



906
2
Me
H
H
H
CF3



907
3
Me
H
H
H
CF3



908
4
Me
H
H
H
CF3



909
1
CH2Ph
H
H
H
CF3



910
2
CH2Ph
H
H
H
CF3



911
3
CH2Ph
H
H
H
CF3



912
4
CH2Ph
H
H
H
CF3



913
1
COMe
H
H
H
CF3



914
2
COMe
H
H
H
CF3



915
3
COMe
H
H
H
CF3



916
4
COMe
H
H
H
CF3



917
1
CO2Me
H
H
H
CF3



918
2
CO2Me
H
H
H
CF3



919
3
CO2Me
H
H
H
CF3



920
4
CO2Me
H
H
H
CF3



921
1
CO2tBu
H
H
H
CF3



922
2
CO2tBu
H
H
H
CF3



923
3
CO2tBu
H
H
H
CF3



924
4
CO2tBu
H
H
H
CF3



925
1
CONHMe
H
H
H
CF3



926
2
CONHMe
H
H
H
CF3



927
3
CONHMe
H
H
H
CF3



928
4
CONHMe
H
H
H
CF3



929
1
SO2Me
H
H
H
CF3



930
2
SO2Me
H
H
H
CF3



931
3
SO2Me
H
H
H
CF3



932
4
SO2Me
H
H
H
CF3



933
1
SO2NH2
H
H
H
CF3



934
2
SO2NH2
H
H
H
CF3



935
3
SO2NH2
H
H
H
CF3



936
4
SO2NH2
H
H
H
CF3



937
1
H
H
H
H
F



938
2
H
H
H
H
F



939
3
H
H
H
H
F



940
3
H
H
H
H
F



941
1
Me
H
H
H
F



942
2
Me
H
H
H
F



943
3
Me
H
H
H
F



944
4
Me
H
H
H
F



945
1
CH2Ph
H
H
H
F



946
2
CH2Ph
H
H
H
F



947
3
CH2Ph
H
H
H
F



948
4
CH2Ph
H
H
H
F



949
1
COMe
H
H
H
F



950
2
COMe
H
H
H
F



951
3
COMe
H
H
H
F



952
4
COMe
H
H
H
F



953
1
CO2Me
H
H
H
F



954
2
CO2Me
H
H
H
F



955
3
CO2Me
H
H
H
F



956
4
CO2Me
H
H
H
F



957
1
CO2tBu
H
H
H
F



958
2
CO2tBu
H
H
H
F



959
3
CO2tBu
H
H
H
F



960
4
CO2tBu
H
H
H
F



961
1
CONHMe
H
H
H
F



962
2
CONHMe
H
H
H
F



963
3
CONHMe
H
H
H
F



964
4
CONHMe
H
H
H
F



965
1
SO2Me
H
H
H
F



966
2
SO2Me
H
H
H
F



967
3
SO2Me
H
H
H
F



968
4
SO2Me
H
H
H
F



969
1
SO2NH2
H
H
H
F



970
2
SO2NH2
H
H
H
F



971
3
SO2NH2
H
H
H
F



972
4
SO2NH2
H
H
H
F



973
1
H
H
H
H
Cl



974
2
H
H
H
H
Cl



975
3
H
H
H
H
Cl



976
4
H
H
H
H
Cl



977
1
Me
H
H
H
Cl



978
2
Me
H
H
H
Cl



979
3
Me
H
H
H
Cl



980
4
Me
H
H
H
Cl



981
1
CH2Ph
H
H
H
Cl



982
2
CH2Ph
H
H
H
Cl



983
3
CH2Ph
H
H
H
Cl



984
4
CH2Ph
H
H
H
Cl



985
1
COMe
H
H
H
Cl



986
2
COMe
H
H
H
Cl



987
3
COMe
H
H
H
Cl



988
4
COMe
H
H
H
Cl



989
1
CO2Me
H
H
H
Cl



990
2
CO2Me
H
H
H
Cl



991
3
CO2Me
H
H
H
Cl



992
4
CO2Me
H
H
H
Cl



993
1
CO2tBu
H
H
H
Cl



994
2
CO2tBu
H
H
H
Cl



995
3
CO2tBu
H
H
H
Cl



996
4
CO2tBu
H
H
H
Cl



997
1
CONHMe
H
H
H
Cl



998
2
CONHMe
H
H
H
Cl



999
3
CONHMe
H
H
H
Cl



1000
4
CONHMe
H
H
H
Cl



1001
1
SO2Me
H
H
H
Cl



1002
2
SO2Me
H
H
H
Cl



1003
3
SO2Me
H
H
H
Cl



1004
4
SO2Me
H
H
H
Cl



1005
1
SO2NH2
H
H
H
Cl



1006
2
SO2NH2
H
H
H
Cl



1007
3
SO2NH2
H
H
H
Cl



1008
4
SO2NH2
H
H
H
Cl



1009
1
H
H
H
H
CN



1010
2
H
H
H
H
CN



1011
3
H
H
H
H
CN



1012
4
H
H
H
H
CN



1013
1
Me
H
H
H
CN



1014
2
Me
H
H
H
CN



1015
3
Me
H
H
H
CN



1016
4
Me
H
H
H
CN



1017
1
CH2Ph
H
H
H
CN



1018
2
CH2Ph
H
H
H
CN



1019
3
CH2Ph
H
H
H
CN



1020
4
CH2Ph
H
H
H
CN



1021
1
COMe
H
H
H
CN



1022
2
COMe
H
H
H
CN



1023
3
COMe
H
H
H
CN



1024
4
COMe
H
H
H
CN



1025
1
CO2Me
H
H
H
CN



1026
2
CO2Me
H
H
H
CN



1027
3
CO2Me
H
H
H
CN



1028
4
CO2Me
H
H
H
CN



1029
1
CO2tBu
H
H
H
CN



1030
2
CO2tBu
H
H
H
CN



1031
3
CO2tBu
H
H
H
CN



1032
4
CO2tBu
H
H
H
CN



1033
1
CONHMe
H
H
H
CN



1034
2
CONHMe
H
H
H
CN



1035
3
CONHMe
H
H
H
CN



1036
4
CONHMe
H
H
H
CN



1037
1
SO2Me
H
H
H
CN



1038
2
SO2Me
H
H
H
CN



1039
3
SO2Me
H
H
H
CN



1040
4
SO2Me
H
H
H
CN



1041
1
SO2NH2
H
H
H
CN



1042
2
SO2NH2
H
H
H
CN



1043
3
SO2NH2
H
H
H
CN



1044
4
SO2NH2
H
H
H
CN










Exemplary embodiments include compounds having the formula (XXVII)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 21.

















TABLE 21







Entry
n
R7
R20a
R20b
R20c
R20d
























1
1
H
H
H
H
H



2
2
H
H
H
H
H



3
3
H
H
H
H
H



4
4
H
H
H
H
H



5
1
Me
H
H
H
H



6
2
Me
H
H
H
H



7
3
Me
H
H
H
H



8
4
Me
H
H
H
H



9
1
CH2Ph
H
H
H
H



10
2
CH2Ph
H
H
H
H



11
3
CH2Ph
H
H
H
H



12
4
CH2Ph
H
H
H
H



13
1
COMe
H
H
H
H



14
2
COMe
H
H
H
H



15
3
COMe
H
H
H
H



16
4
COMe
H
H
H
H



17
1
CO2Me
H
H
H
H



18
2
CO2Me
H
H
H
H



19
3
CO2Me
H
H
H
H



20
4
CO2Me
H
H
H
H



21
1
CO2tBu
H
H
H
H



22
2
CO2tBu
H
H
H
H



23
3
CO2tBu
H
H
H
H



24
4
CO2tBu
H
H
H
H



25
1
CONHMe
H
H
H
H



26
2
CONHMe
H
H
H
H



27
3
CONHMe
H
H
H
H



28
4
CONHMe
H
H
H
H



29
1
SO2Me
H
H
H
H



30
2
SO2Me
H
H
H
H



31
3
SO2Me
H
H
H
H



32
4
SO2Me
H
H
H
H



33
1
SO2NH2
H
H
H
H



34
2
SO2NH2
H
H
H
H



35
3
SO2NH2
H
H
H
H



36
4
SO2NH2
H
H
H
H



37
1
H
H
H
OH
H



38
2
H
H
H
OH
H



39
3
H
H
H
OH
H



40
4
H
H
H
OH
H



41
1
Me
H
H
OH
H



42
2
Me
H
H
OH
H



43
3
Me
H
H
OH
H



44
4
Me
H
H
OH
H



45
1
CH2Ph
H
H
OH
H



46
2
CH2Ph
H
H
OH
H



47
3
CH2Ph
H
H
OH
H



48
4
CH2Ph
H
H
OH
H



49
1
COMe
H
H
OH
H



50
2
COMe
H
H
OH
H



51
3
COMe
H
H
OH
H



52
4
COMe
H
H
OH
H



53
1
CO2Me
H
H
OH
H



54
2
CO2Me
H
H
OH
H



55
3
CO2Me
H
H
OH
H



56
4
CO2Me
H
H
OH
H



57
1
CO2tBu
H
H
OH
H



58
2
CO2tBu
H
H
OH
H



59
3
CO2tBu
H
H
OH
H



60
4
CO2tBu
H
H
OH
H



61
1
CONHMe
H
H
OH
H



62
2
CONHMe
H
H
OH
H



63
3
CONHMe
H
H
OH
H



64
4
CONHMe
H
H
OH
H



65
1
SO2Me
H
H
OH
H



66
2
SO2Me
H
H
OH
H



67
3
SO2Me
H
H
OH
H



68
4
SO2Me
H
H
OH
H



69
1
SO2NH2
H
H
OH
H



70
2
SO2NH2
H
H
OH
H



71
3
SO2NH2
H
H
OH
H



72
4
SO2NH2
H
H
OH
H



73
1
H
H
H
OMe
H



74
2
H
H
H
OMe
H



75
3
H
H
H
OMe
H



76
4
H
H
H
OMe
H



77
1
Me
H
H
OMe
H



78
2
Me
H
H
OMe
H



79
3
Me
H
H
OMe
H



80
4
Me
H
H
OMe
H



81
1
CH2Ph
H
H
OMe
H



82
2
CH2Ph
H
H
OMe
H



83
3
CH2Ph
H
H
OMe
H



84
4
CH2Ph
H
H
OMe
H



85
1
COMe
H
H
OMe
H



86
2
COMe
H
H
OMe
H



87
3
COMe
H
H
OMe
H



88
4
COMe
H
H
OMe
H



89
1
CO2Me
H
H
OMe
H



90
2
CO2Me
H
H
OMe
H



91
3
CO2Me
H
H
OMe
H



92
4
CO2Me
H
H
OMe
H



93
1
CO2tBu
H
H
OMe
H



94
2
CO2tBu
H
H
OMe
H



95
3
CO2tBu
H
H
OMe
H



96
1
CO2tBu
H
H
OMe
H



97
1
CONHMe
H
H
OMe
H



98
2
CONHMe
H
H
OMe
H



99
3
CONHMe
H
H
OMe
H



100
4
CONHMe
H
H
OMe
H



101
1
SO2Me
H
H
OMe
H



102
2
SO2Me
H
H
OMe
H



103
3
SO2Me
H
H
OMe
H



104
4
SO2Me
H
H
OMe
H



105
1
SO2NH2
H
H
OMe
H



106
2
SO2NH2
H
H
OMe
H



107
3
SO2NH2
H
H
OMe
H



108
4
SO2NH2
H
H
OMe
H



109
1
H
H
H
Me
H



110
2
H
H
H
Me
H



111
3
H
H
H
Me
H



112
4
H
H
H
Me
H



113
1
Me
H
H
Me
H



114
2
Me
H
H
Me
H



115
3
Me
H
H
Me
H



116
4
Me
H
H
Me
H



117
1
CH2Ph
H
H
Me
H



118
2
CH2Ph
H
H
Me
H



119
3
CH2Ph
H
H
Me
H



120
4
CH2Ph
H
H
Me
H



121
1
COMe
H
H
Me
H



122
2
COMe
H
H
Me
H



123
3
COMe
H
H
Me
H



124
4
COMe
H
H
Me
H



125
1
CO2Me
H
H
Me
H



126
2
CO2Me
H
H
Me
H



127
3
CO2Me
H
H
Me
H



128
4
CO2Me
H
H
Me
H



129
1
CO2tBu
H
H
Me
H



130
2
CO2tBu
H
H
Me
H



131
3
CO2tBu
H
H
Me
H



132
4
CO2tBu
H
H
Me
H



133
1
CONHMe
H
H
Me
H



134
2
CONHMe
H
H
Me
H



135
3
CONHMe
H
H
Me
H



136
4
CONHMe
H
H
Me
H



137
1
SO2Me
H
H
Me
H



138
2
SO2Me
H
H
Me
H



139
3
SO2Me
H
H
Me
H



140
4
SO2Me
H
H
Me
H



141
1
SO2NH2
H
H
Me
H



142
2
SO2NH2
H
H
Me
H



143
3
SO2NH2
H
H
Me
H



144
4
SO2NH2
H
H
Me
H



145
1
H
H
H
CF3
H



146
2
H
H
H
CF3
H



147
3
H
H
H
CF3
H



148
4
H
H
H
CF3
H



149
1
Me
H
H
CF3
H



150
2
Me
H
H
CF3
H



151
3
Me
H
H
CF3
H



152
4
Me
H
H
CF3
H



153
1
CH2Ph
H
H
CF3
H



154
2
CH2Ph
H
H
CF3
H



155
3
CH2Ph
H
H
CF3
H



156
4
CH2Ph
H
H
CF3
H



157
1
COMe
H
H
CF3
H



158
2
COMe
H
H
CF3
H



159
3
COMe
H
H
CF3
H



160
4
COMe
H
H
CF3
H



161
1
CO2Me
H
H
CF3
H



162
2
CO2Me
H
H
CF3
H



163
3
CO2Me
H
H
CF3
H



164
4
CO2Me
H
H
CF3
H



165
1
CO2tBu
H
H
CF3
H



166
2
CO2tBu
H
H
CF3
H



167
3
CO2tBu
H
H
CF3
H



168
4
CO2tBu
H
H
CF3
H



169
1
CONHMe
H
H
CF3
H



170
2
CONHMe
H
H
CF3
H



171
3
CONHMe
H
H
CF3
H



172
4
CONHMe
H
H
CF3
H



173
1
SO2Me
H
H
CF3
H



174
2
SO2Me
H
H
CF3
H



175
3
SO2Me
H
H
CF3
H



176
4
SO2Me
H
H
CF3
H



177
1
SO2NH2
H
H
CF3
H



178
2
SO2NH2
H
H
CF3
H



179
3
SO2NH2
H
H
CF3
H



180
4
SO2NH2
H
H
CF3
H



181
1
H
H
H
F
H



182
2
H
H
H
F
H



183
3
H
H
H
F
H



184
4
H
H
H
F
H



185
1
Me
H
H
F
H



186
2
Me
H
H
F
H



187
3
Me
H
H
F
H



188
4
Me
H
H
F
H



189
1
CH2Ph
H
H
F
H



190
2
CH2Ph
H
H
F
H



191
3
CH2Ph
H
H
F
H



192
4
CH2Ph
H
H
F
H



193
1
COMe
H
H
F
H



194
2
COMe
H
H
F
H



195
3
COMe
H
H
F
H



196
4
COMe
H
H
F
H



197
1
CO2Me
H
H
F
H



198
2
CO2Me
H
H
F
H



199
3
CO2Me
H
H
F
H



200
4
CO2Me
H
H
F
H



201
1
CO2tBu
H
H
F
H



202
2
CO2tBu
H
H
F
H



203
3
CO2tBu
H
H
F
H



204
4
CO2tBu
H
H
F
H



205
1
CONHMe
H
H
F
H



206
2
CONHMe
H
H
F
H



207
3
CONHMe
H
H
F
H



208
4
CONHMe
H
H
F
H



209
1
SO2Me
H
H
F
H



210
2
SO2Me
H
H
F
H



211
3
SO2Me
H
H
F
H



212
4
SO2Me
H
H
F
H



213
1
SO2NH2
H
H
F
H



214
2
SO2NH2
H
H
F
H



215
3
SO2NH2
H
H
F
H



216
4
SO2NH2
H
H
F
H



217
1
H
H
H
Cl
H



218
2
H
H
H
Cl
H



219
3
H
H
H
Cl
H



220
4
H
H
H
Cl
H



221
1
Me
H
H
Cl
H



222
2
Me
H
H
Cl
H



223
3
Me
H
H
Cl
H



224
4
Me
H
H
Cl
H



225
1
CH2Ph
H
H
Cl
H



226
2
CH2Ph
H
H
Cl
H



227
3
CH2Ph
H
H
Cl
H



228
4
CH2Ph
H
H
Cl
H



229
1
COMe
H
H
Cl
H



230
2
COMe
H
H
Cl
H



231
3
COMe
H
H
Cl
H



232
4
COMe
H
H
Cl
H



233
1
CO2Me
H
H
Cl
H



234
2
CO2Me
H
H
Cl
H



235
3
CO2Me
H
H
Cl
H



236
4
CO2Me
H
H
Cl
H



237
1
CO2tBu
H
H
Cl
H



238
2
CO2tBu
H
H
Cl
H



239
3
CO2tBu
H
H
Cl
H



240
4
CO2tBu
H
H
Cl
H



241
1
CONHMe
H
H
Cl
H



242
2
CONHMe
H
H
Cl
H



243
3
CONHMe
H
H
Cl
H



244
4
CONHMe
H
H
Cl
H



245
1
SO2Me
H
H
Cl
H



246
2
SO2Me
H
H
Cl
H



247
3
SO2Me
H
H
Cl
H



248
4
SO2Me
H
H
Cl
H



249
1
SO2NH2
H
H
Cl
H



250
2
SO2NH2
H
H
Cl
H



251
3
SO2NH2
H
H
Cl
H



252
4
SO2NH2
H
H
Cl
H



253
1
H
H
H
CN
H



254
2
H
H
H
CN
H



255
3
H
H
H
CN
H



256
4
H
H
H
CN
H



257
1
Me
H
H
CN
H



258
2
Me
H
H
CN
H



259
3
Me
H
H
CN
H



260
4
Me
H
H
CN
H



261
1
CH2Ph
H
H
CN
H



262
2
CH2Ph
H
H
CN
H



263
3
CH2Ph
H
H
CN
H



264
4
CH2Ph
H
H
CN
H



265
1
COMe
H
H
CN
H



266
2
COMe
H
H
CN
H



267
3
COMe
H
H
CN
H



268
4
COMe
H
H
CN
H



269
1
CO2Me
H
H
CN
H



270
2
CO2Me
H
H
CN
H



271
3
CO2Me
H
H
CN
H



272
4
CO2Me
H
H
CN
H



273
1
CO2tBu
H
H
CN
H



274
2
CO2tBu
H
H
CN
H



275
3
CO2tBu
H
H
CN
H



276
4
CO2tBu
H
H
CN
H



277
1
CONHMe
H
H
CN
H



278
2
CONHMe
H
H
CN
H



279
3
CONHMe
H
H
CN
H



280
4
CONHMe
H
H
CN
H



281
1
SO2Me
H
H
CN
H



282
2
SO2Me
H
H
CN
H



283
3
SO2Me
H
H
CN
H



284
4
SO2Me
H
H
CN
H



285
1
SO2NH2
H
H
CN
H



286
2
SO2NH2
H
H
CN
H



287
3
SO2NH2
H
H
CN
H



288
4
SO2NH2
H
H
CN
H



289
1
H
H
OH
H
H



290
2
H
H
OH
H
H



291
3
H
H
OH
H
H



292
4
H
H
OH
H
H



293
1
Me
H
OH
H
H



294
2
Me
H
OH
H
H



295
3
Me
H
OH
H
H



296
4
Me
H
OH
H
H



297
1
CH2Ph
H
OH
H
H



298
2
CH2Ph
H
OH
H
H



299
3
CH2Ph
H
OH
H
H



300
4
CH2Ph
H
OH
H
H



301
1
COMe
H
OH
H
H



302
2
COMe
H
OH
H
H



303
3
COMe
H
OH
H
H



304
4
COMe
H
OH
H
H



305
1
CO2Me
H
OH
H
H



306
2
CO2Me
H
OH
H
H



307
3
CO2Me
H
OH
H
H



308
4
CO2Me
H
OH
H
H



309
1
CO2tBu
H
OH
H
H



310
2
CO2tBu
H
OH
H
H



311
3
CO2tBu
H
OH
H
H



312
4
CO2tBu
H
OH
H
H



313
1
CONHMe
H
OH
H
H



314
2
CONHMe
H
OH
H
H



315
3
CONHMe
H
OH
H
H



316
4
CONHMe
H
OH
H
H



317
1
SO2Me
H
OH
H
H



318
2
SO2Me
H
OH
H
H



319
3
SO2Me
H
OH
H
H



320
4
SO2Me
H
OH
H
H



321
1
SO2NH2
H
OH
H
H



322
2
SO2NH2
H
OH
H
H



323
3
SO2NH2
H
OH
H
H



324
4
SO2NH2
H
OH
H
H



325
1
H
H
OMe
H
H



326
2
H
H
OMe
H
H



327
3
H
H
OMe
H
H



328
4
H
H
OMe
H
H



329
1
Me
H
OMe
H
H



330
2
Me
H
OMe
H
H



331
3
Me
H
OMe
H
H



332
4
Me
H
OMe
H
H



333
1
CH2Ph
H
OMe
H
H



334
2
CH2Ph
H
OMe
H
H



335
3
CH2Ph
H
OMe
H
H



336
4
CH2Ph
H
OMe
H
H



337
1
COMe
H
OMe
H
H



338
2
COMe
H
OMe
H
H



339
3
COMe
H
OMe
H
H



340
4
COMe
H
OMe
H
H



341
1
CO2Me
H
OMe
H
H



342
2
CO2Me
H
OMe
H
H



343
3
CO2Me
H
OMe
H
H



344
4
CO2Me
H
OMe
H
H



345
1
CO2tBu
H
OMe
H
H



346
2
CO2tBu
H
OMe
H
H



347
3
CO2tBu
H
OMe
H
H



348
4
CO2tBu
H
OMe
H
H



349
1
CONHMe
H
OMe
H
H



350
2
CONHMe
H
OMe
H
H



351
3
CONHMe
H
OMe
H
H



352
4
CONHMe
H
OMe
H
H



353
1
SO2Me
H
OMe
H
H



354
2
SO2Me
H
OMe
H
H



355
3
SO2Me
H
OMe
H
H



356
4
SO2Me
H
OMe
H
H



357
1
SO2NH2
H
OMe
H
H



358
2
SO2NH2
H
OMe
H
H



359
3
SO2NH2
H
OMe
H
H



360
4
SO2NH2
H
OMe
H
H



361
1
H
H
Me
H
H



362
2
H
H
Me
H
H



363
3
H
H
Me
H
H



364
4
H
H
Me
H
H



365
1
Me
H
Me
H
H



366
2
Me
H
Me
H
H



367
3
Me
H
Me
H
H



368
4
Me
H
Me
H
H



369
1
CH2Ph
H
Me
H
H



370
2
CH2Ph
H
Me
H
H



371
3
CH2Ph
H
Me
H
H



372
4
CH2Ph
H
Me
H
H



373
1
COMe
H
Me
H
H



374
2
COMe
H
Me
H
H



375
3
COMe
H
Me
H
H



376
4
COMe
H
Me
H
H



377
1
CO2Me
H
Me
H
H



378
2
CO2Me
H
Me
H
H



379
3
CO2Me
H
Me
H
H



380
4
CO2Me
H
Me
H
H



381
1
CO2tBu
H
Me
H
H



382
2
CO2tBu
H
Me
H
H



383
3
CO2tBu
H
Me
H
H



384
4
CO2tBu
H
Me
H
H



385
1
CONHMe
H
Me
H
H



386
2
CONHMe
H
Me
H
H



387
3
CONHMe
H
Me
H
H



388
4
CONHMe
H
Me
H
H



389
1
SO2Me
H
Me
H
H



390
2
SO2Me
H
Me
H
H



391
3
SO2Me
H
Me
H
H



392
4
SO2Me
H
Me
H
H



393
1
SO2NH2
H
Me
H
H



394
2
SO2NH2
H
Me
H
H



395
3
SO2NH2
H
Me
H
H



396
4
SO2NH2
H
Me
H
H



397
1
H
H
CF3
H
H



398
2
H
H
CF3
H
H



399
3
H
H
CF3
H
H



400
4
H
H
CF3
H
H



401
1
Me
H
CF3
H
H



402
2
Me
H
CF3
H
H



403
3
Me
H
CF3
H
H



404
4
Me
H
CF3
H
H



405
1
CH2Ph
H
CF3
H
H



406
2
CH2Ph
H
CF3
H
H



407
3
CH2Ph
H
CF3
H
H



408
4
CH2Ph
H
CF3
H
H



409
1
COMe
H
CF3
H
H



410
2
COMe
H
CF3
H
H



411
3
COMe
H
CF3
H
H



412
4
COMe
H
CF3
H
H



413
1
CO2Me
H
CF3
H
H



414
2
CO2Me
H
CF3
H
H



415
3
CO2Me
H
CF3
H
H



416
4
CO2Me
H
CF3
H
H



417
1
CO2tBu
H
CF3
H
H



418
2
CO2tBu
H
CF3
H
H



419
3
CO2tBu
H
CF3
H
H



420
4
CO2tBu
H
CF3
H
H



421
1
CONHMe
H
CF3
H
H



422
2
CONHMe
H
CF3
H
H



423
3
CONHMe
H
CF3
H
H



424
4
CONHMe
H
CF3
H
H



425
1
SO2Me
H
CF3
H
H



426
2
SO2Me
H
CF3
H
H



427
3
SO2Me
H
CF3
H
H



428
4
SO2Me
H
CF3
H
H



429
1
SO2NH2
H
CF3
H
H



430
2
SO2NH2
H
CF3
H
H



431
3
SO2NH2
H
CF3
H
H



432
4
SO2NH2
H
CF3
H
H



433
1
H
H
F
H
H



434
2
H
H
F
H
H



435
3
H
H
F
H
H



436
3
H
H
F
H
H



437
1
Me
H
F
H
H



438
2
Me
H
F
H
H



439
3
Me
H
F
H
H



440
4
Me
H
F
H
H



441
1
CH2Ph
H
F
H
H



442
2
CH2Ph
H
F
H
H



443
3
CH2Ph
H
F
H
H



444
4
CH2Ph
H
F
H
H



445
1
COMe
H
F
H
H



446
2
COMe
H
F
H
H



447
3
COMe
H
F
H
H



448
4
COMe
H
F
H
H



449
1
CO2Me
H
F
H
H



450
2
CO2Me
H
F
H
H



451
3
CO2Me
H
F
H
H



452
4
CO2Me
H
F
H
H



453
1
CO2tBu
H
F
H
H



454
2
CO2tBu
H
F
H
H



455
3
CO2tBu
H
F
H
H



456
4
CO2tBu
H
F
H
H



457
1
CONHMe
H
F
H
H



458
2
CONHMe
H
F
H
H



459
3
CONHMe
H
F
H
H



460
4
CONHMe
H
F
H
H



461
1
SO2Me
H
F
H
H



462
2
SO2Me
H
F
H
H



463
3
SO2Me
H
F
H
H



464
4
SO2Me
H
F
H
H



465
1
SO2NH2
H
F
H
H



466
2
SO2NH2
H
F
H
H



467
3
SO2NH2
H
F
H
H



468
4
SO2NH2
H
F
H
H



469
1
H
H
Cl
H
H



470
2
H
H
Cl
H
H



471
3
H
H
Cl
H
H



472
4
H
H
Cl
H
H



473
1
Me
H
Cl
H
H



474
2
Me
H
Cl
H
H



475
3
Me
H
Cl
H
H



476
4
Me
H
Cl
H
H



477
1
CH2Ph
H
Cl
H
H



478
2
CH2Ph
H
Cl
H
H



479
3
CH2Ph
H
Cl
H
H



480
4
CH2Ph
H
Cl
H
H



481
1
COMe
H
Cl
H
H



482
2
COMe
H
Cl
H
H



483
3
COMe
H
Cl
H
H



484
4
COMe
H
Cl
H
H



485
1
CO2Me
H
Cl
H
H



486
2
CO2Me
H
Cl
H
H



487
3
CO2Me
H
Cl
H
H



488
4
CO2Me
H
Cl
H
H



489
1
CO2tBu
H
Cl
H
H



490
2
CO2tBu
H
Cl
H
H



491
3
CO2tBu
H
Cl
H
H



492
4
CO2tBu
H
Cl
H
H



493
1
CONHMe
H
Cl
H
H



494
2
CONHMe
H
Cl
H
H



495
3
CONHMe
H
Cl
H
H



496
4
CONHMe
H
Cl
H
H



497
1
SO2Me
H
Cl
H
H



498
2
SO2Me
H
Cl
H
H



499
3
SO2Me
H
Cl
H
H



500
4
SO2Me
H
Cl
H
H



501
1
SO2NH2
H
Cl
H
H



502
2
SO2NH2
H
Cl
H
H



503
3
SO2NH2
H
Cl
H
H



504
4
SO2NH2
H
Cl
H
H



505
1
H
H
CN
H
H



506
2
H
H
CN
H
H



507
3
H
H
CN
H
H



508
4
H
H
CN
H
H



509
1
Me
H
CN
H
H



510
2
Me
H
CN
H
H



511
3
Me
H
CN
H
H



512
4
Me
H
CN
H
H



513
1
CH2Ph
H
CN
H
H



514
2
CH2Ph
H
CN
H
H



515
3
CH2Ph
H
CN
H
H



516
4
CH2Ph
H
CN
H
H



517
1
COMe
H
CN
H
H



518
2
COMe
H
CN
H
H



519
3
COMe
H
CN
H
H



520
4
COMe
H
CN
H
H



521
1
CO2Me
H
CN
H
H



522
2
CO2Me
H
CN
H
H



523
3
CO2Me
H
CN
H
H



524
4
CO2Me
H
CN
H
H



525
1
CO2tBu
H
CN
H
H



526
2
CO2tBu
H
CN
H
H



527
3
CO2tBu
H
CN
H
H



528
4
CO2tBu
H
CN
H
H



529
1
CONHMe
H
CN
H
H



530
2
CONHMe
H
CN
H
H



531
3
CONHMe
H
CN
H
H



532
4
CONHMe
H
CN
H
H



533
1
SO2Me
H
CN
H
H



534
2
SO2Me
H
CN
H
H



535
3
SO2Me
H
CN
H
H



536
4
SO2Me
H
CN
H
H



537
1
SO2NH2
H
CN
H
H



538
2
SO2NH2
H
CN
H
H



539
3
SO2NH2
H
CN
H
H



540
4
SO2NH2
H
CN
H
H



541
1
H
OH
H
H
H



542
2
H
OH
H
H
H



543
3
H
OH
H
H
H



544
4
H
OH
H
H
H



545
1
Me
OH
H
H
H



546
2
Me
OH
H
H
H



547
3
Me
OH
H
H
H



548
4
Me
OH
H
H
H



549
1
CH2Ph
OH
H
H
H



550
2
CH2Ph
OH
H
H
H



551
3
CH2Ph
OH
H
H
H



552
4
CH2Ph
OH
H
H
H



553
1
COMe
OH
H
H
H



554
2
COMe
OH
H
H
H



555
3
COMe
OH
H
H
H



556
4
COMe
OH
H
H
H



557
1
CO2Me
OH
H
H
H



558
2
CO2Me
OH
H
H
H



559
3
CO2Me
OH
H
H
H



560
4
CO2Me
OH
H
H
H



561
1
CO2tBu
OH
H
H
H



562
2
CO2tBu
OH
H
H
H



563
3
CO2tBu
OH
H
H
H



564
4
CO2tBu
OH
H
H
H



565
1
CONHMe
OH
H
H
H



566
2
CONHMe
OH
H
H
H



567
3
CONHMe
OH
H
H
H



568
4
CONHMe
OH
H
H
H



569
1
SO2Me
OH
H
H
H



570
2
SO2Me
OH
H
H
H



571
3
SO2Me
OH
H
H
H



572
4
SO2Me
OH
H
H
H



573
1
SO2NH2
OH
H
H
H



574
2
SO2NH2
OH
H
H
H



575
3
SO2NH2
OH
H
H
H



576
4
SO2NH2
OH
H
H
H



577
1
H
OMe
H
H
H



578
2
H
OMe
H
H
H



579
3
H
OMe
H
H
H



580
4
H
OMe
H
H
H



581
1
Me
OMe
H
H
H



582
2
Me
OMe
H
H
H



583
3
Me
OMe
H
H
H



584
4
Me
OMe
H
H
H



585
1
CH2Ph
OMe
H
H
H



586
2
CH2Ph
OMe
H
H
H



587
3
CH2Ph
OMe
H
H
H



588
4
CH2Ph
OMe
H
H
H



589
1
COMe
OMe
H
H
H



590
2
COMe
OMe
H
H
H



591
3
COMe
OMe
H
H
H



592
4
COMe
OMe
H
H
H



593
1
CO2Me
OMe
H
H
H



594
2
CO2Me
OMe
H
H
H



595
3
CO2Me
OMe
H
H
H



596
4
CO2Me
OMe
H
H
H



597
1
CO2tBu
OMe
H
H
H



598
2
CO2tBu
OMe
H
H
H



599
3
CO2tBu
OMe
H
H
H



600
4
CO2tBu
OMe
H
H
H



601
1
CONHMe
OMe
H
H
H



602
2
CONHMe
OMe
H
H
H



603
3
CONHMe
OMe
H
H
H



604
4
CONHMe
OMe
H
H
H



605
1
SO2Me
OMe
H
H
H



606
2
SO2Me
OMe
H
H
H



607
3
SO2Me
OMe
H
H
H



608
4
SO2Me
OMe
H
H
H



609
1
SO2NH2
OMe
H
H
H



610
2
SO2NH2
OMe
H
H
H



611
3
SO2NH2
OMe
H
H
H



612
4
SO2NH2
OMe
H
H
H



613
1
H
Me
H
H
H



614
2
H
Me
H
H
H



615
3
H
Me
H
H
H



616
4
H
Me
H
H
H



617
1
Me
Me
H
H
H



618
2
Me
Me
H
H
H



619
3
Me
Me
H
H
H



620
4
Me
Me
H
H
H



621
1
CH2Ph
Me
H
H
H



622
2
CH2Ph
Me
H
H
H



623
3
CH2Ph
Me
H
H
H



624
4
CH2Ph
Me
H
H
H



625
1
COMe
Me
H
H
H



626
2
COMe
Me
H
H
H



627
3
COMe
Me
H
H
H



628
4
COMe
Me
H
H
H



629
1
CO2Me
Me
H
H
H



630
2
CO2Me
Me
H
H
H



631
3
CO2Me
Me
H
H
H



632
4
CO2Me
Me
H
H
H



633
1
CO2tBu
Me
H
H
H



634
2
CO2tBu
Me
H
H
H



635
3
CO2tBu
Me
H
H
H



636
4
CO2tBu
Me
H
H
H



637
1
CONHMe
Me
H
H
H



638
2
CONHMe
Me
H
H
H



639
3
CONHMe
Me
H
H
H



640
4
CONHMe
Me
H
H
H



641
1
SO2Me
Me
H
H
H



642
2
SO2Me
Me
H
H
H



643
3
SO2Me
Me
H
H
H



644
4
SO2Me
Me
H
H
H



645
1
SO2NH2
Me
H
H
H



646
2
SO2NH2
Me
H
H
H



647
3
SO2NH2
Me
H
H
H



648
4
SO2NH2
Me
H
H
H



649
1
H
CF3
H
H
H



650
2
H
CF3
H
H
H



651
3
H
CF3
H
H
H



652
4
H
CF3
H
H
H



653
1
Me
CF3
H
H
H



654
2
Me
CF3
H
H
H



655
3
Me
CF3
H
H
H



656
4
Me
CF3
H
H
H



657
1
CH2Ph
CF3
H
H
H



658
2
CH2Ph
CF3
H
H
H



659
3
CH2Ph
CF3
H
H
H



660
4
CH2Ph
CF3
H
H
H



661
1
COMe
CF3
H
H
H



662
2
COMe
CF3
H
H
H



663
3
COMe
CF3
H
H
H



664
4
COMe
CF3
H
H
H



665
1
CO2Me
CF3
H
H
H



666
2
CO2Me
CF3
H
H
H



667
3
CO2Me
CF3
H
H
H



668
4
CO2Me
CF3
H
H
H



669
1
CO2tBu
CF3
H
H
H



670
2
CO2tBu
CF3
H
H
H



671
3
CO2tBu
CF3
H
H
H



672
4
CO2tBu
CF3
H
H
H



673
1
CONHMe
CF3
H
H
H



674
2
CONHMe
CF3
H
H
H



675
3
CONHMe
CF3
H
H
H



676
4
CONHMe
CF3
H
H
H



677
1
SO2Me
CF3
H
H
H



678
2
SO2Me
CF3
H
H
H



679
3
SO2Me
CF3
H
H
H



680
4
SO2Me
CF3
H
H
H



681
1
SO2NH2
CF3
H
H
H



682
2
SO2NH2
CF3
H
H
H



683
3
SO2NH2
CF3
H
H
H



684
4
SO2NH2
CF3
H
H
H



685
1
H
F
H
H
H



686
2
H
F
H
H
H



687
3
H
F
H
H
H



688
3
H
F
H
H
H



689
1
Me
F
H
H
H



690
2
Me
F
H
H
H



691
3
Me
F
H
H
H



692
4
Me
F
H
H
H



693
1
CH2Ph
F
H
H
H



694
2
CH2Ph
F
H
H
H



695
3
CH2Ph
F
H
H
H



696
4
CH2Ph
F
H
H
H



697
1
COMe
F
H
H
H



698
2
COMe
F
H
H
H



699
3
COMe
F
H
H
H



700
4
COMe
F
H
H
H



701
1
CO2Me
F
H
H
H



702
2
CO2Me
F
H
H
H



703
3
CO2Me
F
H
H
H



704
4
CO2Me
F
H
H
H



705
1
CO2tBu
F
H
H
H



706
2
CO2tBu
F
H
H
H



707
3
CO2tBu
F
H
H
H



708
4
CO2tBu
F
H
H
H



709
1
CONHMe
F
H
H
H



710
2
CONHMe
F
H
H
H



711
3
CONHMe
F
H
H
H



712
4
CONHMe
F
H
H
H



713
1
SO2Me
F
H
H
H



714
2
SO2Me
F
H
H
H



715
3
SO2Me
F
H
H
H



716
4
SO2Me
F
H
H
H



717
1
SO2NH2
F
H
H
H



718
2
SO2NH2
F
H
H
H



719
3
SO2NH2
F
H
H
H



720
4
SO2NH2
F
H
H
H



721
1
H
Cl
H
H
H



722
2
H
Cl
H
H
H



723
3
H
Cl
H
H
H



724
4
H
Cl
H
H
H



725
1
Me
Cl
H
H
H



726
2
Me
Cl
H
H
H



727
3
Me
Cl
H
H
H



728
4
Me
Cl
H
H
H



729
1
CH2Ph
Cl
H
H
H



730
2
CH2Ph
Cl
H
H
H



731
3
CH2Ph
Cl
H
H
H



732
4
CH2Ph
Cl
H
H
H



733
1
COMe
Cl
H
H
H



734
2
COMe
Cl
H
H
H



735
3
COMe
Cl
H
H
H



736
4
COMe
Cl
H
H
H



737
1
CO2Me
Cl
H
H
H



738
2
CO2Me
Cl
H
H
H



739
3
CO2Me
Cl
H
H
H



740
4
CO2Me
Cl
H
H
H



741
1
CO2tBu
Cl
H
H
H



742
2
CO2tBu
Cl
H
H
H



743
3
CO2tBu
Cl
H
H
H



744
4
CO2tBu
Cl
H
H
H



745
1
CONHMe
Cl
H
H
H



746
2
CONHMe
Cl
H
H
H



747
3
CONHMe
Cl
H
H
H



748
4
CONHMe
Cl
H
H
H



749
1
SO2Me
Cl
H
H
H



750
2
SO2Me
Cl
H
H
H



751
3
SO2Me
Cl
H
H
H



752
4
SO2Me
Cl
H
H
H



753
1
SO2NH2
Cl
H
H
H



754
2
SO2NH2
Cl
H
H
H



755
3
SO2NH2
Cl
H
H
H



756
4
SO2NH2
Cl
H
H
H



757
1
H
CN
H
H
H



758
2
H
CN
H
H
H



759
3
H
CN
H
H
H



760
4
H
CN
H
H
H



761
1
Me
CN
H
H
H



762
2
Me
CN
H
H
H



763
3
Me
CN
H
H
H



764
4
Me
CN
H
H
H



765
1
CH2Ph
CN
H
H
H



766
2
CH2Ph
CN
H
H
H



767
3
CH2Ph
CN
H
H
H



768
4
CH2Ph
CN
H
H
H



769
1
COMe
CN
H
H
H



770
2
COMe
CN
H
H
H



771
3
COMe
CN
H
H
H



772
4
COMe
CN
H
H
H



773
1
CO2Me
CN
H
H
H



774
2
CO2Me
CN
H
H
H



775
3
CO2Me
CN
H
H
H



776
4
CO2Me
CN
H
H
H



777
1
CO2tBu
CN
H
H
H



778
2
CO2tBu
CN
H
H
H



779
3
CO2tBu
CN
H
H
H



780
4
CO2tBu
CN
H
H
H



781
1
CONHMe
CN
H
H
H



782
2
CONHMe
CN
H
H
H



783
3
CONHMe
CN
H
H
H



784
4
CONHMe
CN
H
H
H



785
1
SO2Me
CN
H
H
H



786
2
SO2Me
CN
H
H
H



787
3
SO2Me
CN
H
H
H



788
4
SO2Me
CN
H
H
H



789
1
SO2NH2
CN
H
H
H



790
2
SO2NH2
CN
H
H
H



791
3
SO2NH2
CN
H
H
H



792
4
SO2NH2
CN
H
H
H



793
1
H
H
H
H
OH



794
2
H
H
H
H
OH



795
3
H
H
H
H
OH



796
4
H
H
H
H
OH



797
1
Me
H
H
H
OH



798
2
Me
H
H
H
OH



799
3
Me
H
H
H
OH



800
4
Me
H
H
H
OH



801
1
CH2Ph
H
H
H
OH



802
2
CH2Ph
H
H
H
OH



803
3
CH2Ph
H
H
H
OH



804
4
CH2Ph
H
H
H
OH



805
1
COMe
H
H
H
OH



806
2
COMe
H
H
H
OH



807
3
COMe
H
H
H
OH



808
4
COMe
H
H
H
OH



809
1
CO2Me
H
H
H
OH



810
2
CO2Me
H
H
H
OH



811
3
CO2Me
H
H
H
OH



812
4
CO2Me
H
H
H
OH



813
1
CO2tBu
H
H
H
OH



814
2
CO2tBu
H
H
H
OH



815
3
CO2tBu
H
H
H
OH



816
4
CO2tBu
H
H
H
OH



817
1
CONHMe
H
H
H
OH



818
2
CONHMe
H
H
H
OH



819
3
CONHMe
H
H
H
OH



820
4
CONHMe
H
H
H
OH



821
1
SO2Me
H
H
H
OH



822
2
SO2Me
H
H
H
OH



823
3
SO2Me
H
H
H
OH



824
4
SO2Me
H
H
H
OH



825
1
SO2NH2
H
H
H
OH



826
2
SO2NH2
H
H
H
OH



827
3
SO2NH2
H
H
H
OH



828
4
SO2NH2
H
H
H
OH



829
1
H
H
H
H
OMe



830
2
H
H
H
H
OMe



831
3
H
H
H
H
OMe



832
4
H
H
H
H
OMe



833
1
Me
H
H
H
OMe



834
2
Me
H
H
H
OMe



835
3
Me
H
H
H
OMe



836
4
Me
H
H
H
OMe



837
1
CH2Ph
H
H
H
OMe



838
2
CH2Ph
H
H
H
OMe



839
3
CH2Ph
H
H
H
OMe



840
4
CH2Ph
H
H
H
OMe



841
1
COMe
H
H
H
OMe



842
2
COMe
H
H
H
OMe



843
3
COMe
H
H
H
OMe



844
4
COMe
H
H
H
OMe



845
1
CO2Me
H
H
H
OMe



846
2
CO2Me
H
H
H
OMe



847
3
CO2Me
H
H
H
OMe



848
4
CO2Me
H
H
H
OMe



849
1
CO2tBu
H
H
H
OMe



850
2
CO2tBu
H
H
H
OMe



851
3
CO2tBu
H
H
H
OMe



852
4
CO2tBu
H
H
H
OMe



853
1
CONHMe
H
H
H
OMe



854
2
CONHMe
H
H
H
OMe



855
3
CONHMe
H
H
H
OMe



856
4
CONHMe
H
H
H
OMe



857
1
SO2Me
H
H
H
OMe



858
2
SO2Me
H
H
H
OMe



859
3
SO2Me
H
H
H
OMe



860
4
SO2Me
H
H
H
OMe



861
1
SO2NH2
H
H
H
OMe



862
2
SO2NH2
H
H
H
OMe



863
3
SO2NH2
H
H
H
OMe



864
4
SO2NH2
H
H
H
OMe



865
1
H
H
H
H
Me



866
2
H
H
H
H
Me



867
3
H
H
H
H
Me



868
4
H
H
H
H
Me



869
1
Me
H
H
H
Me



870
2
Me
H
H
H
Me



871
3
Me
H
H
H
Me



872
4
Me
H
H
H
Me



873
1
CH2Ph
H
H
H
Me



874
2
CH2Ph
H
H
H
Me



875
3
CH2Ph
H
H
H
Me



876
4
CH2Ph
H
H
H
Me



877
1
COMe
H
H
H
Me



878
2
COMe
H
H
H
Me



879
3
COMe
H
H
H
Me



880
4
COMe
H
H
H
Me



881
1
CO2Me
H
H
H
Me



882
2
CO2Me
H
H
H
Me



883
3
CO2Me
H
H
H
Me



884
4
CO2Me
H
H
H
Me



885
1
CO2tBu
H
H
H
Me



886
2
CO2tBu
H
H
H
Me



887
3
CO2tBu
H
H
H
Me



888
4
CO2tBu
H
H
H
Me



889
1
CONHMe
H
H
H
Me



890
2
CONHMe
H
H
H
Me



891
3
CONHMe
H
H
H
Me



892
4
CONHMe
H
H
H
Me



893
1
SO2Me
H
H
H
Me



894
2
SO2Me
H
H
H
Me



895
3
SO2Me
H
H
H
Me



896
4
SO2Me
H
H
H
Me



897
1
SO2NH2
H
H
H
Me



898
2
SO2NH2
H
H
H
Me



899
3
SO2NH2
H
H
H
Me



900
4
SO2NH2
H
H
H
Me



901
1
H
H
H
H
CF3



902
2
H
H
H
H
CF3



903
3
H
H
H
H
CF3



904
4
H
H
H
H
CF3



905
1
Me
H
H
H
CF3



906
2
Me
H
H
H
CF3



907
3
Me
H
H
H
CF3



908
4
Me
H
H
H
CF3



909
1
CH2Ph
H
H
H
CF3



910
2
CH2Ph
H
H
H
CF3



911
3
CH2Ph
H
H
H
CF3



912
4
CH2Ph
H
H
H
CF3



913
1
COMe
H
H
H
CF3



914
2
COMe
H
H
H
CF3



915
3
COMe
H
H
H
CF3



916
4
COMe
H
H
H
CF3



917
1
CO2Me
H
H
H
CF3



918
2
CO2Me
H
H
H
CF3



919
3
CO2Me
H
H
H
CF3



920
4
CO2Me
H
H
H
CF3



921
1
CO2tBu
H
H
H
CF3



922
2
CO2tBu
H
H
H
CF3



923
3
CO2tBu
H
H
H
CF3



924
4
CO2tBu
H
H
H
CF3



925
1
CONHMe
H
H
H
CF3



926
2
CONHMe
H
H
H
CF3



927
3
CONHMe
H
H
H
CF3



928
4
CONHMe
H
H
H
CF3



929
1
SO2Me
H
H
H
CF3



930
2
SO2Me
H
H
H
CF3



931
3
SO2Me
H
H
H
CF3



932
4
SO2Me
H
H
H
CF3



933
1
SO2NH2
H
H
H
CF3



934
2
SO2NH2
H
H
H
CF3



935
3
SO2NH2
H
H
H
CF3



936
4
SO2NH2
H
H
H
CF3



937
1
H
H
H
H
F



938
2
H
H
H
H
F



939
3
H
H
H
H
F



940
3
H
H
H
H
F



941
1
Me
H
H
H
F



942
2
Me
H
H
H
F



943
3
Me
H
H
H
F



944
4
Me
H
H
H
F



945
1
CH2Ph
H
H
H
F



946
2
CH2Ph
H
H
H
F



947
3
CH2Ph
H
H
H
F



948
4
CH2Ph
H
H
H
F



949
1
COMe
H
H
H
F



950
2
COMe
H
H
H
F



951
3
COMe
H
H
H
F



952
4
COMe
H
H
H
F



953
1
CO2Me
H
H
H
F



954
2
CO2Me
H
H
H
F



955
3
CO2Me
H
H
H
F



956
4
CO2Me
H
H
H
F



957
1
CO2tBu
H
H
H
F



958
2
CO2tBu
H
H
H
F



959
3
CO2tBu
H
H
H
F



960
4
CO2tBu
H
H
H
F



961
1
CONHMe
H
H
H
F



962
2
CONHMe
H
H
H
F



963
3
CONHMe
H
H
H
F



964
4
CONHMe
H
H
H
F



965
1
SO2Me
H
H
H
F



966
2
SO2Me
H
H
H
F



967
3
SO2Me
H
H
H
F



968
4
SO2Me
H
H
H
F



969
1
SO2NH2
H
H
H
F



970
2
SO2NH2
H
H
H
F



971
3
SO2NH2
H
H
H
F



972
4
SO2NH2
H
H
H
F



973
1
H
H
H
H
Cl



974
2
H
H
H
H
Cl



975
3
H
H
H
H
Cl



976
4
H
H
H
H
Cl



977
1
Me
H
H
H
Cl



978
2
Me
H
H
H
Cl



979
3
Me
H
H
H
Cl



980
4
Me
H
H
H
Cl



981
1
CH2Ph
H
H
H
Cl



982
2
CH2Ph
H
H
H
Cl



983
3
CH2Ph
H
H
H
Cl



984
4
CH2Ph
H
H
H
Cl



985
1
COMe
H
H
H
Cl



986
2
COMe
H
H
H
Cl



987
3
COMe
H
H
H
Cl



988
4
COMe
H
H
H
Cl



989
1
CO2Me
H
H
H
Cl



990
2
CO2Me
H
H
H
Cl



991
3
CO2Me
H
H
H
Cl



992
4
CO2Me
H
H
H
Cl



993
1
CO2tBu
H
H
H
Cl



994
2
CO2tBu
H
H
H
Cl



995
3
CO2tBu
H
H
H
Cl



996
4
CO2tBu
H
H
H
Cl



997
1
CONHMe
H
H
H
Cl



998
2
CONHMe
H
H
H
Cl



999
3
CONHMe
H
H
H
Cl



1000
4
CONHMe
H
H
H
Cl



1001
1
SO2Me
H
H
H
Cl



1002
2
SO2Me
H
H
H
Cl



1003
3
SO2Me
H
H
H
Cl



1004
4
SO2Me
H
H
H
Cl



1005
1
SO2NH2
H
H
H
Cl



1006
2
SO2NH2
H
H
H
Cl



1007
3
SO2NH2
H
H
H
Cl



1008
4
SO2NH2
H
H
H
Cl



1009
1
H
H
H
H
CN



1010
2
H
H
H
H
CN



1011
3
H
H
H
H
CN



1012
4
H
H
H
H
CN



1013
1
Me
H
H
H
CN



1014
2
Me
H
H
H
CN



1015
3
Me
H
H
H
CN



1016
4
Me
H
H
H
CN



1017
1
CH2Ph
H
H
H
CN



1018
2
CH2Ph
H
H
H
CN



1019
3
CH2Ph
H
H
H
CN



1020
4
CH2Ph
H
H
H
CN



1021
1
COMe
H
H
H
CN



1022
2
COMe
H
H
H
CN



1023
3
COMe
H
H
H
CN



1024
4
COMe
H
H
H
CN



1025
1
CO2Me
H
H
H
CN



1026
2
CO2Me
H
H
H
CN



1027
3
CO2Me
H
H
H
CN



1028
4
CO2Me
H
H
H
CN



1029
1
CO2tBu
H
H
H
CN



1030
2
CO2tBu
H
H
H
CN



1031
3
CO2tBu
H
H
H
CN



1032
4
CO2tBu
H
H
H
CN



1033
1
CONHMe
H
H
H
CN



1034
2
CONHMe
H
H
H
CN



1035
3
CONHMe
H
H
H
CN



1036
4
CONHMe
H
H
H
CN



1037
1
SO2Me
H
H
H
CN



1038
2
SO2Me
H
H
H
CN



1039
3
SO2Me
H
H
H
CN



1040
4
SO2Me
H
H
H
CN



1041
1
SO2NH2
H
H
H
CN



1042
2
SO2NH2
H
H
H
CN



1043
3
SO2NH2
H
H
H
CN



1044
4
SO2NH2
H
H
H
CN










Exemplary embodiments include compounds having the formula (XXVIII)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 22.

















TABLE 22







Entry
n
R7
R20a
R20b
R20c
R20e
























1
1
H
H
H
H
H



2
2
H
H
H
H
H



3
3
H
H
H
H
H



4
4
H
H
H
H
H



5
1
Me
H
H
H
H



6
2
Me
H
H
H
H



7
3
Me
H
H
H
H



8
4
Me
H
H
H
H



9
1
CH2Ph
H
H
H
H



10
2
CH2Ph
H
H
H
H



11
3
CH2Ph
H
H
H
H



12
4
CH2Ph
H
H
H
H



13
1
COMe
H
H
H
H



14
2
COMe
H
H
H
H



15
3
COMe
H
H
H
H



16
4
COMe
H
H
H
H



17
1
CO2Me
H
H
H
H



18
2
CO2Me
H
H
H
H



19
3
CO2Me
H
H
H
H



20
4
CO2Me
H
H
H
H



21
1
CO2tBu
H
H
H
H



22
2
CO2tBu
H
H
H
H



23
3
CO2tBu
H
H
H
H



24
4
CO2tBu
H
H
H
H



25
1
CONHMe
H
H
H
H



26
2
CONHMe
H
H
H
H



27
3
CONHMe
H
H
H
H



28
4
CONHMe
H
H
H
H



29
1
SO2Me
H
H
H
H



30
2
SO2Me
H
H
H
H



31
3
SO2Me
H
H
H
H



32
4
SO2Me
H
H
H
H



33
1
SO2NH2
H
H
H
H



34
2
SO2NH2
H
H
H
H



35
3
SO2NH2
H
H
H
H



36
4
SO2NH2
H
H
H
H



37
1
H
H
H
OH
H



38
2
H
H
H
OH
H



39
3
H
H
H
OH
H



40
4
H
H
H
OH
H



41
1
Me
H
H
OH
H



42
2
Me
H
H
OH
H



43
3
Me
H
H
OH
H



44
4
Me
H
H
OH
H



45
1
CH2Ph
H
H
OH
H



46
2
CH2Ph
H
H
OH
H



47
3
CH2Ph
H
H
OH
H



48
4
CH2Ph
H
H
OH
H



49
1
COMe
H
H
OH
H



50
2
COMe
H
H
OH
H



51
3
COMe
H
H
OH
H



52
4
COMe
H
H
OH
H



53
1
CO2Me
H
H
OH
H



54
2
CO2Me
H
H
OH
H



55
3
CO2Me
H
H
OH
H



56
4
CO2Me
H
H
OH
H



57
1
CO2tBu
H
H
OH
H



58
2
CO2tBu
H
H
OH
H



59
3
CO2tBu
H
H
OH
H



60
4
CO2tBu
H
H
OH
H



61
1
CONHMe
H
H
OH
H



62
2
CONHMe
H
H
OH
H



63
3
CONHMe
H
H
OH
H



64
4
CONHMe
H
H
OH
H



65
1
SO2Me
H
H
OH
H



66
2
SO2Me
H
H
OH
H



67
3
SO2Me
H
H
OH
H



68
4
SO2Me
H
H
OH
H



69
1
SO2NH2
H
H
OH
H



70
2
SO2NH2
H
H
OH
H



71
3
SO2NH2
H
H
OH
H



72
4
SO2NH2
H
H
OH
H



73
1
H
H
H
OMe
H



74
2
H
H
H
OMe
H



75
3
H
H
H
OMe
H



76
4
H
H
H
OMe
H



77
1
Me
H
H
OMe
H



78
2
Me
H
H
OMe
H



79
3
Me
H
H
OMe
H



80
4
Me
H
H
OMe
H



81
1
CH2Ph
H
H
OMe
H



82
2
CH2Ph
H
H
OMe
H



83
3
CH2Ph
H
H
OMe
H



84
4
CH2Ph
H
H
OMe
H



85
1
COMe
H
H
OMe
H



86
2
COMe
H
H
OMe
H



87
3
COMe
H
H
OMe
H



88
4
COMe
H
H
OMe
H



89
1
CO2Me
H
H
OMe
H



90
2
CO2Me
H
H
OMe
H



91
3
CO2Me
H
H
OMe
H



92
4
CO2Me
H
H
OMe
H



93
1
CO2tBu
H
H
OMe
H



94
2
CO2tBu
H
H
OMe
H



95
3
CO2tBu
H
H
OMe
H



96
1
CO2tBu
H
H
OMe
H



97
1
CONHMe
H
H
OMe
H



98
2
CONHMe
H
H
OMe
H



99
3
CONHMe
H
H
OMe
H



100
4
CONHMe
H
H
OMe
H



101
1
SO2Me
H
H
OMe
H



102
2
SO2Me
H
H
OMe
H



103
3
SO2Me
H
H
OMe
H



104
4
SO2Me
H
H
OMe
H



105
1
SO2NH2
H
H
OMe
H



106
2
SO2NH2
H
H
OMe
H



107
3
SO2NH2
H
H
OMe
H



108
4
SO2NH2
H
H
OMe
H



109
1
H
H
H
Me
H



110
2
H
H
H
Me
H



111
3
H
H
H
Me
H



112
4
H
H
H
Me
H



113
1
Me
H
H
Me
H



114
2
Me
H
H
Me
H



115
3
Me
H
H
Me
H



116
4
Me
H
H
Me
H



117
1
CH2Ph
H
H
Me
H



118
2
CH2Ph
H
H
Me
H



119
3
CH2Ph
H
H
Me
H



120
4
CH2Ph
H
H
Me
H



121
1
COMe
H
H
Me
H



122
2
COMe
H
H
Me
H



123
3
COMe
H
H
Me
H



124
4
COMe
H
H
Me
H



125
1
CO2Me
H
H
Me
H



126
2
CO2Me
H
H
Me
H



127
3
CO2Me
H
H
Me
H



128
4
CO2Me
H
H
Me
H



129
1
CO2tBu
H
H
Me
H



130
2
CO2tBu
H
H
Me
H



131
3
CO2tBu
H
H
Me
H



132
4
CO2tBu
H
H
Me
H



133
1
CONHMe
H
H
Me
H



134
2
CONHMe
H
H
Me
H



135
3
CONHMe
H
H
Me
H



136
4
CONHMe
H
H
Me
H



137
1
SO2Me
H
H
Me
H



138
2
SO2Me
H
H
Me
H



139
3
SO2Me
H
H
Me
H



140
4
SO2Me
H
H
Me
H



141
1
SO2NH2
H
H
Me
H



142
2
SO2NH2
H
H
Me
H



143
3
SO2NH2
H
H
Me
H



144
4
SO2NH2
H
H
Me
H



145
1
H
H
H
CF3
H



146
2
H
H
H
CF3
H



147
3
H
H
H
CF3
H



148
4
H
H
H
CF3
H



149
1
Me
H
H
CF3
H



150
2
Me
H
H
CF3
H



151
3
Me
H
H
CF3
H



152
4
Me
H
H
CF3
H



153
1
CH2Ph
H
H
CF3
H



154
2
CH2Ph
H
H
CF3
H



155
3
CH2Ph
H
H
CF3
H



156
4
CH2Ph
H
H
CF3
H



157
1
COMe
H
H
CF3
H



158
2
COMe
H
H
CF3
H



159
3
COMe
H
H
CF3
H



160
4
COMe
H
H
CF3
H



161
1
CO2Me
H
H
CF3
H



162
2
CO2Me
H
H
CF3
H



163
3
CO2Me
H
H
CF3
H



164
4
CO2Me
H
H
CF3
H



165
1
CO2tBu
H
H
CF3
H



166
2
CO2tBu
H
H
CF3
H



167
3
CO2tBu
H
H
CF3
H



168
4
CO2tBu
H
H
CF3
H



169
1
CONHMe
H
H
CF3
H



170
2
CONHMe
H
H
CF3
H



171
3
CONHMe
H
H
CF3
H



172
4
CONHMe
H
H
CF3
H



173
1
SO2Me
H
H
CF3
H



174
2
SO2Me
H
H
CF3
H



175
3
SO2Me
H
H
CF3
H



176
4
SO2Me
H
H
CF3
H



177
1
SO2NH2
H
H
CF3
H



178
2
SO2NH2
H
H
CF3
H



179
3
SO2NH2
H
H
CF3
H



180
4
SO2NH2
H
H
CF3
H



181
1
H
H
H
F
H



182
2
H
H
H
F
H



183
3
H
H
H
F
H



184
4
H
H
H
F
H



185
1
Me
H
H
F
H



186
2
Me
H
H
F
H



187
3
Me
H
H
F
H



188
4
Me
H
H
F
H



189
1
CH2Ph
H
H
F
H



190
2
CH2Ph
H
H
F
H



191
3
CH2Ph
H
H
F
H



192
4
CH2Ph
H
H
F
H



193
1
COMe
H
H
F
H



194
2
COMe
H
H
F
H



195
3
COMe
H
H
F
H



196
4
COMe
H
H
F
H



197
1
CO2Me
H
H
F
H



198
2
CO2Me
H
H
F
H



199
3
CO2Me
H
H
F
H



200
4
CO2Me
H
H
F
H



201
1
CO2tBu
H
H
F
H



202
2
CO2tBu
H
H
F
H



203
3
CO2tBu
H
H
F
H



204
4
CO2tBu
H
H
F
H



205
1
CONHMe
H
H
F
H



206
2
CONHMe
H
H
F
H



207
3
CONHMe
H
H
F
H



208
4
CONHMe
H
H
F
H



209
1
SO2Me
H
H
F
H



210
2
SO2Me
H
H
F
H



211
3
SO2Me
H
H
F
H



212
4
SO2Me
H
H
F
H



213
1
SO2NH2
H
H
F
H



214
2
SO2NH2
H
H
F
H



215
3
SO2NH2
H
H
F
H



216
4
SO2NH2
H
H
F
H



217
1
H
H
H
Cl
H



218
2
H
H
H
Cl
H



219
3
H
H
H
Cl
H



220
4
H
H
H
Cl
H



221
1
Me
H
H
Cl
H



222
2
Me
H
H
Cl
H



223
3
Me
H
H
Cl
H



224
4
Me
H
H
Cl
H



225
1
CH2Ph
H
H
Cl
H



226
2
CH2Ph
H
H
Cl
H



227
3
CH2Ph
H
H
Cl
H



228
4
CH2Ph
H
H
Cl
H



229
1
COMe
H
H
Cl
H



230
2
COMe
H
H
Cl
H



231
3
COMe
H
H
Cl
H



232
4
COMe
H
H
Cl
H



233
1
CO2Me
H
H
Cl
H



234
2
CO2Me
H
H
Cl
H



235
3
CO2Me
H
H
Cl
H



236
4
CO2Me
H
H
Cl
H



237
1
CO2tBu
H
H
Cl
H



238
2
CO2tBu
H
H
Cl
H



239
3
CO2tBu
H
H
Cl
H



240
4
CO2tBu
H
H
Cl
H



241
1
CONHMe
H
H
Cl
H



242
2
CONHMe
H
H
Cl
H



243
3
CONHMe
H
H
Cl
H



244
4
CONHMe
H
H
Cl
H



245
1
SO2Me
H
H
Cl
H



246
2
SO2Me
H
H
Cl
H



247
3
SO2Me
H
H
Cl
H



248
4
SO2Me
H
H
Cl
H



249
1
SO2NH2
H
H
Cl
H



250
2
SO2NH2
H
H
Cl
H



251
3
SO2NH2
H
H
Cl
H



252
4
SO2NH2
H
H
Cl
H



253
1
H
H
H
CN
H



254
2
H
H
H
CN
H



255
3
H
H
H
CN
H



256
4
H
H
H
CN
H



257
1
Me
H
H
CN
H



258
2
Me
H
H
CN
H



259
3
Me
H
H
CN
H



260
4
Me
H
H
CN
H



261
1
CH2Ph
H
H
CN
H



262
2
CH2Ph
H
H
CN
H



263
3
CH2Ph
H
H
CN
H



264
4
CH2Ph
H
H
CN
H



265
1
COMe
H
H
CN
H



266
2
COMe
H
H
CN
H



267
3
COMe
H
H
CN
H



268
4
COMe
H
H
CN
H



269
1
CO2Me
H
H
CN
H



270
2
CO2Me
H
H
CN
H



271
3
CO2Me
H
H
CN
H



272
4
CO2Me
H
H
CN
H



273
1
CO2tBu
H
H
CN
H



274
2
CO2tBu
H
H
CN
H



275
3
CO2tBu
H
H
CN
H



276
4
CO2tBu
H
H
CN
H



277
1
CONHMe
H
H
CN
H



278
2
CONHMe
H
H
CN
H



279
3
CONHMe
H
H
CN
H



280
4
CONHMe
H
H
CN
H



281
1
SO2Me
H
H
CN
H



282
2
SO2Me
H
H
CN
H



283
3
SO2Me
H
H
CN
H



284
4
SO2Me
H
H
CN
H



285
1
SO2NH2
H
H
CN
H



286
2
SO2NH2
H
H
CN
H



287
3
SO2NH2
H
H
CN
H



288
4
SO2NH2
H
H
CN
H



289
1
H
H
OH
H
H



290
2
H
H
OH
H
H



291
3
H
H
OH
H
H



292
4
H
H
OH
H
H



293
1
Me
H
OH
H
H



294
2
Me
H
OH
H
H



295
3
Me
H
OH
H
H



296
4
Me
H
OH
H
H



297
1
CH2Ph
H
OH
H
H



298
2
CH2Ph
H
OH
H
H



299
3
CH2Ph
H
OH
H
H



300
4
CH2Ph
H
OH
H
H



301
1
COMe
H
OH
H
H



302
2
COMe
H
OH
H
H



303
3
COMe
H
OH
H
H



304
4
COMe
H
OH
H
H



305
1
CO2Me
H
OH
H
H



306
2
CO2Me
H
OH
H
H



307
3
CO2Me
H
OH
H
H



308
4
CO2Me
H
OH
H
H



309
1
CO2tBu
H
OH
H
H



310
2
CO2tBu
H
OH
H
H



311
3
CO2tBu
H
OH
H
H



312
4
CO2tBu
H
OH
H
H



313
1
CONHMe
H
OH
H
H



314
2
CONHMe
H
OH
H
H



315
3
CONHMe
H
OH
H
H



316
4
CONHMe
H
OH
H
H



317
1
SO2Me
H
OH
H
H



318
2
SO2Me
H
OH
H
H



319
3
SO2Me
H
OH
H
H



320
4
SO2Me
H
OH
H
H



321
1
SO2NH2
H
OH
H
H



322
2
SO2NH2
H
OH
H
H



323
3
SO2NH2
H
OH
H
H



324
4
SO2NH2
H
OH
H
H



325
1
H
H
OMe
H
H



326
2
H
H
OMe
H
H



327
3
H
H
OMe
H
H



328
4
H
H
OMe
H
H



329
1
Me
H
OMe
H
H



330
2
Me
H
OMe
H
H



331
3
Me
H
OMe
H
H



332
4
Me
H
OMe
H
H



333
1
CH2Ph
H
OMe
H
H



334
2
CH2Ph
H
OMe
H
H



335
3
CH2Ph
H
OMe
H
H



336
4
CH2Ph
H
OMe
H
H



337
1
COMe
H
OMe
H
H



338
2
COMe
H
OMe
H
H



339
3
COMe
H
OMe
H
H



340
4
COMe
H
OMe
H
H



341
1
CO2Me
H
OMe
H
H



342
2
CO2Me
H
OMe
H
H



343
3
CO2Me
H
OMe
H
H



344
4
CO2Me
H
OMe
H
H



345
1
CO2tBu
H
OMe
H
H



346
2
CO2tBu
H
OMe
H
H



347
3
CO2tBu
H
OMe
H
H



348
4
CO2tBu
H
OMe
H
H



349
1
CONHMe
H
OMe
H
H



350
2
CONHMe
H
OMe
H
H



351
3
CONHMe
H
OMe
H
H



352
4
CONHMe
H
OMe
H
H



353
1
SO2Me
H
OMe
H
H



354
2
SO2Me
H
OMe
H
H



355
3
SO2Me
H
OMe
H
H



356
4
SO2Me
H
OMe
H
H



357
1
SO2NH2
H
OMe
H
H



358
2
SO2NH2
H
OMe
H
H



359
3
SO2NH2
H
OMe
H
H



360
4
SO2NH2
H
OMe
H
H



361
1
H
H
Me
H
H



362
2
H
H
Me
H
H



363
3
H
H
Me
H
H



364
4
H
H
Me
H
H



365
1
Me
H
Me
H
H



366
2
Me
H
Me
H
H



367
3
Me
H
Me
H
H



368
4
Me
H
Me
H
H



369
1
CH2Ph
H
Me
H
H



370
2
CH2Ph
H
Me
H
H



371
3
CH2Ph
H
Me
H
H



372
4
CH2Ph
H
Me
H
H



373
1
COMe
H
Me
H
H



374
2
COMe
H
Me
H
H



375
3
COMe
H
Me
H
H



376
4
COMe
H
Me
H
H



377
1
CO2Me
H
Me
H
H



378
2
CO2Me
H
Me
H
H



379
3
CO2Me
H
Me
H
H



380
4
CO2Me
H
Me
H
H



381
1
CO2tBu
H
Me
H
H



382
2
CO2tBu
H
Me
H
H



383
3
CO2tBu
H
Me
H
H



384
4
CO2tBu
H
Me
H
H



385
1
CONHMe
H
Me
H
H



386
2
CONHMe
H
Me
H
H



387
3
CONHMe
H
Me
H
H



388
4
CONHMe
H
Me
H
H



389
1
SO2Me
H
Me
H
H



390
2
SO2Me
H
Me
H
H



391
3
SO2Me
H
Me
H
H



392
4
SO2Me
H
Me
H
H



393
1
SO2NH2
H
Me
H
H



394
2
SO2NH2
H
Me
H
H



395
3
SO2NH2
H
Me
H
H



396
4
SO2NH2
H
Me
H
H



397
1
H
H
CF3
H
H



398
2
H
H
CF3
H
H



399
3
H
H
CF3
H
H



400
4
H
H
CF3
H
H



401
1
Me
H
CF3
H
H



402
2
Me
H
CF3
H
H



403
3
Me
H
CF3
H
H



404
4
Me
H
CF3
H
H



405
1
CH2Ph
H
CF3
H
H



406
2
CH2Ph
H
CF3
H
H



407
3
CH2Ph
H
CF3
H
H



408
4
CH2Ph2
H
CF3
H
H



409
1
COMe
H
CF3
H
H



410
2
COMe
H
CF3
H
H



411
3
COMe
H
CF3
H
H



412
4
COMe
H
CF3
H
H



413
1
CO2Me
H
CF3
H
H



414
2
CO2Me
H
CF3
H
H



415
3
CO2Me
H
CF3
H
H



416
4
CO2Me
H
CF3
H
H



417
1
CO2tBu
H
CF3
H
H



418
2
CO2tBu
H
CF3
H
H



419
3
CO2tBu
H
CF3
H
H



420
4
CO2tBu
H
CF3
H
H



421
1
CONHMe
H
CF3
H
H



422
2
CONHMe
H
CF3
H
H



423
3
CONHMe
H
CF3
H
H



424
4
CONHMe
H
CF3
H
H



425
1
SO2Me
H
CF3
H
H



426
2
SO2Me
H
CF3
H
H



427
3
SO2Me
H
CF3
H
H



428
4
SO2Me
H
CF3
H
H



429
1
SO2NH2
H
CF3
H
H



430
2
SO2NH2
H
CF3
H
H



431
3
SO2NH2
H
CF3
H
H



432
4
SO2NH2
H
CF3
H
H



433
1
H
H
F
H
H



434
2
H
H
F
H
H



435
3
H
H
F
H
H



436
3
H
H
F
H
H



437
1
Me
H
F
H
H



438
2
Me
H
F
H
H



439
3
Me
H
F
H
H



440
4
Me
H
F
H
H



441
1
CH2Ph
H
F
H
H



442
2
CH2Ph
H
F
H
H



443
3
CH2Ph
H
F
H
H



444
4
CH2Ph
H
F
H
H



445
1
COMe
H
F
H
H



446
2
COMe
H
F
H
H



447
3
COMe
H
F
H
H



448
4
COMe
H
F
H
H



449
1
CO2Me
H
F
H
H



450
2
CO2Me
H
F
H
H



451
3
CO2Me
H
F
H
H



452
4
CO2Me
H
F
H
H



453
1
CO2tBu
H
F
H
H



454
2
CO2tBu
H
F
H
H



455
3
CO2tBu
H
F
H
H



456
4
CO2tBu
H
F
H
H



457
1
CONHMe
H
F
H
H



458
2
CONHMe
H
F
H
H



459
3
CONHMe
H
F
H
H



460
4
CONHMe
H
F
H
H



461
1
SO2Me
H
F
H
H



462
2
SO2Me
H
F
H
H



463
3
SO2Me
H
F
H
H



464
4
SO2Me
H
F
H
H



465
1
SO2NH2
H
F
H
H



466
2
SO2NH2
H
F
H
H



467
3
SO2NH2
H
F
H
H



468
4
SO2NH2
H
F
H
H



469
1
H
H
Cl
H
H



470
2
H
H
Cl
H
H



471
3
H
H
Cl
H
H



472
4
H
H
Cl
H
H



473
1
Me
H
Cl
H
H



474
2
Me
H
Cl
H
H



475
3
Me
H
Cl
H
H



476
4
Me
H
Cl
H
H



477
1
CH2Ph
H
Cl
H
H



478
2
CH2Ph
H
Cl
H
H



479
3
CH2Ph
H
Cl
H
H



480
4
CH2Ph
H
Cl
H
H



481
1
COMe
H
Cl
H
H



482
2
COMe
H
Cl
H
H



483
3
COMe
H
Cl
H
H



484
4
COMe
H
Cl
H
H



485
1
CO2Me
H
Cl
H
H



486
2
CO2Me
H
Cl
H
H



487
3
CO2Me
H
Cl
H
H



488
4
CO2Me
H
Cl
H
H



489
1
CO2tBu
H
Cl
H
H



490
2
CO2tBu
H
Cl
H
H



491
3
CO2tBu
H
Cl
H
H



492
4
CO2tBu
H
Cl
H
H



493
1
CONHMe
H
Cl
H
H



494
2
CONHMe
H
Cl
H
H



495
3
CONHMe
H
Cl
H
H



496
4
CONHMe
H
Cl
H
H



497
1
SO2Me
H
Cl
H
H



498
2
SO2Me
H
Cl
H
H



499
3
SO2Me
H
Cl
H
H



500
4
SO2Me
H
Cl
H
H



501
1
SO2NH2
H
Cl
H
H



502
2
SO2NH2
H
Cl
H
H



503
3
SO2NH2
H
Cl
H
H



504
4
SO2NH2
H
Cl
H
H



505
1
H
H
CN
H
H



506
2
H
H
CN
H
H



507
3
H
H
CN
H
H



508
4
H
H
CN
H
H



509
1
Me
H
CN
H
H



510
2
Me
H
CN
H
H



511
3
Me
H
CN
H
H



512
4
Me
H
CN
H
H



513
1
CH2Ph
H
CN
H
H



514
2
CH2Ph
H
CN
H
H



515
3
CH2Ph
H
CN
H
H



516
4
CH2Ph
H
CN
H
H



517
1
COMe
H
CN
H
H



518
2
COMe
H
CN
H
H



519
3
COMe
H
CN
H
H



520
4
COMe
H
CN
H
H



521
1
CO2Me
H
CN
H
H



522
2
CO2Me
H
CN
H
H



523
3
CO2Me
H
CN
H
H



524
4
CO2Me
H
CN
H
H



525
1
CO2tBu
H
CN
H
H



526
2
CO2tBu
H
CN
H
H



527
3
CO2tBu
H
CN
H
H



528
4
CO2tBu
H
CN
H
H



529
1
CONHMe
H
CN
H
H



530
2
CONHMe
H
CN
H
H



531
3
CONHMe
H
CN
H
H



532
4
CONHMe
H
CN
H
H



533
1
SO2Me
H
CN
H
H



534
2
SO2Me
H
CN
H
H



535
3
SO2Me
H
CN
H
H



536
4
SO2Me
H
CN
H
H



537
1
SO2NH2
H
CN
H
H



538
2
SO2NH2
H
CN
H
H



539
3
SO2NH2
H
CN
H
H



540
4
SO2NH2
H
CN
H
H



541
1
H
OH
H
H
H



542
2
H
OH
H
H
H



543
3
H
OH
H
H
H



544
4
H
OH
H
H
H



545
1
Me
OH
H
H
H



546
2
Me
OH
H
H
H



547
3
Me
OH
H
H
H



548
4
Me
OH
H
H
H



549
1
CH2Ph
OH
H
H
H



550
2
CH2Ph
OH
H
H
H



551
3
CH2Ph
OH
H
H
H



552
4
CH2Ph
OH
H
H
H



553
1
COMe
OH
H
H
H



554
2
COMe
OH
H
H
H



555
3
COMe
OH
H
H
H



556
4
COMe
OH
H
H
H



557
1
CO2Me
OH
H
H
H



558
2
CO2Me
OH
H
H
H



559
3
CO2Me
OH
H
H
H



560
4
CO2Me
OH
H
H
H



561
1
CO2tBu
OH
H
H
H



562
2
CO2tBu
OH
H
H
H



563
3
CO2tBu
OH
H
H
H



564
4
CO2tBu
OH
H
H
H



565
1
CONHMe
OH
H
H
H



566
2
CONHMe
OH
H
H
H



567
3
CONHMe
OH
H
H
H



568
4
CONHMe
OH
H
H
H



569
1
SO2Me
OH
H
H
H



570
2
SO2Me
OH
H
H
H



571
3
SO2Me
OH
H
H
H



572
4
SO2Me
OH
H
H
H



573
1
SO2NH2
OH
H
H
H



574
2
SO2NH2
OH
H
H
H



575
3
SO2NH2
OH
H
H
H



576
4
SO2NH2
OH
H
H
H



577
1
H
OMe
H
H
H



578
2
H
OMe
H
H
H



579
3
H
OMe
H
H
H



580
4
H
OMe
H
H
H



581
1
Me
OMe
H
H
H



582
2
Me
OMe
H
H
H



583
3
Me
OMe
H
H
H



584
4
Me
OMe
H
H
H



585
1
CH2Ph
OMe
H
H
H



586
2
CH2Ph
OMe
H
H
H



587
3
CH2Ph
OMe
H
H
H



588
4
CH2Ph
OMe
H
H
H



589
1
COMe
OMe
H
H
H



590
2
COMe
OMe
H
H
H



591
3
COMe
OMe
H
H
H



592
4
COMe
OMe
H
H
H



593
1
CO2Me
OMe
H
H
H



594
2
CO2Me
OMe
H
H
H



595
3
CO2Me
OMe
H
H
H



596
4
CO2Me
OMe
H
H
H



597
1
CO2tBu
OMe
H
H
H



598
2
CO2tBu
OMe
H
H
H



599
3
CO2tBu
OMe
H
H
H



600
4
CO2tBu
OMe
H
H
H



601
1
CONHMe
OMe
H
H
H



602
2
CONHMe
OMe
H
H
H



603
3
CONHMe
OMe
H
H
H



604
4
CONHMe
OMe
H
H
H



605
1
SO2Me
OMe
H
H
H



606
2
SO2Me
OMe
H
H
H



607
3
SO2Me
OMe
H
H
H



608
4
SO2Me
OMe
H
H
H



609
1
SO2NH2
OMe
H
H
H



610
2
SO2NH2
OMe
H
H
H



611
3
SO2NH2
OMe
H
H
H



612
4
SO2NH2
OMe
H
H
H



613
1
H
Me
H
H
H



614
2
H
Me
H
H
H



615
3
H
Me
H
H
H



616
4
H
Me
H
H
H



617
1
Me
Me
H
H
H



618
2
Me
Me
H
H
H



619
3
Me
Me
H
H
H



620
4
Me
Me
H
H
H



621
1
CH2Ph
Me
H
H
H



622
2
CH2Ph
Me
H
H
H



623
3
CH2Ph
Me
H
H
H



624
4
CH2Ph
Me
H
H
H



625
1
COMe
Me
H
H
H



626
2
COMe
Me
H
H
H



627
3
COMe
Me
H
H
H



628
4
COMe
Me
H
H
H



629
1
CO2Me
Me
H
H
H



630
2
CO2Me
Me
H
H
H



631
3
CO2Me
Me
H
H
H



632
4
CO2Me
Me
H
H
H



633
1
CO2tBu
Me
H
H
H



634
2
CO2tBu
Me
H
H
H



635
3
CO2tBu
Me
H
H
H



636
4
CO2tBu
Me
H
H
H



637
1
CONHMe
Me
H
H
H



638
2
CONHMe
Me
H
H
H



639
3
CONHMe
Me
H
H
H



640
4
CONHMe
Me
H
H
H



641
1
SO2Me
Me
H
H
H



642
2
SO2Me
Me
H
H
H



643
3
SO2Me
Me
H
H
H



644
4
SO2Me
Me
H
H
H



645
1
SO2NH2
Me
H
H
H



646
2
SO2NH2
Me
H
H
H



647
3
SO2NH2
Me
H
H
H



648
4
SO2NH2
Me
H
H
H



649
1
H
CF3
H
H
H



650
2
H
CF3
H
H
H



651
3
H
CF3
H
H
H



652
4
H
CF3
H
H
H



653
1
Me
CF3
H
H
H



654
2
Me
CF3
H
H
H



655
3
Me
CF3
H
H
H



656
4
Me
CF3
H
H
H



657
1
CH2Ph
CF3
H
H
H



658
2
CH2Ph
CF3
H
H
H



659
3
CH2Ph
CF3
H
H
H



660
4
CH2Ph
CF3
H
H
H



661
1
COMe
CF3
H
H
H



662
2
COMe
CF3
H
H
H



663
3
COMe
CF3
H
H
H



664
4
COMe
CF3
H
H
H



665
1
CO2Me
CF3
H
H
H



666
2
CO2Me
CF3
H
H
H



667
3
CO2Me
CF3
H
H
H



668
4
CO2Me
CF3
H
H
H



669
1
CO2tBu
CF3
H
H
H



670
2
CO2tBu
CF3
H
H
H



671
3
CO2tBu
CF3
H
H
H



672
4
CO2tBu
CF3
H
H
H



673
1
CONHMe
CF3
H
H
H



674
2
CONHMe
CF3
H
H
H



675
3
CONHMe
CF3
H
H
H



676
4
CONHMe
CF3
H
H
H



677
1
SO2Me
CF3
H
H
H



678
2
SO2Me
CF3
H
H
H



679
3
SO2Me
CF3
H
H
H



680
4
SO2Me
CF3
H
H
H



681
1
SO2NH2
CF3
H
H
H



682
2
SO2NH2
CF3
H
H
H



683
3
SO2NH2
CF3
H
H
H



684
4
SO2NH2
CF3
H
H
H



685
1
H
F
H
H
H



686
2
H
F
H
H
H



687
3
H
F
H
H
H



688
3
H
F
H
H
H



689
1
Me
F
H
H
H



690
2
Me
F
H
H
H



691
3
Me
F
H
H
H



692
4
Me
F
H
H
H



693
1
CH2Ph
F
H
H
H



694
2
CH2Ph
F
H
H
H



695
3
CH2Ph
F
H
H
H



696
4
CH2Ph
F
H
H
H



697
1
COMe
F
H
H
H



698
2
COMe
F
H
H
H



699
3
COMe
F
H
H
H



700
4
COMe
F
H
H
H



701
1
CO2Me
F
H
H
H



702
2
CO2Me
F
H
H
H



703
3
CO2Me
F
H
H
H



704
4
CO2Me
F
H
H
H



705
1
CO2tBu
F
H
H
H



706
2
CO2tBu
F
H
H
H



707
3
CO2tBu
F
H
H
H



708
4
CO2tBu
F
H
H
H



709
1
CONHMe
F
H
H
H



710
2
CONHMe
F
H
H
H



711
3
CONHMe
F
H
H
H



712
4
CONHMe
F
H
H
H



713
1
SO2Me
F
H
H
H



714
2
SO2Me
F
H
H
H



715
3
SO2Me
F
H
H
H



716
4
SO2Me
F
H
H
H



717
1
SO2NH2
F
H
H
H



718
2
SO2NH2
F
H
H
H



719
3
SO2NH2
F
H
H
H



720
4
SO2NH2
F
H
H
H



721
1
H
Cl
H
H
H



722
2
H
Cl
H
H
H



723
3
H
Cl
H
H
H



724
4
H
Cl
H
H
H



725
1
Me
Cl
H
H
H



726
2
Me
Cl
H
H
H



727
3
Me
Cl
H
H
H



728
4
Me
Cl
H
H
H



729
1
CH2Ph
Cl
H
H
H



730
2
CH2Ph
Cl
H
H
H



731
3
CH2Ph
Cl
H
H
H



732
4
CH2Ph
Cl
H
H
H



733
1
COMe
Cl
H
H
H



734
2
COMe
Cl
H
H
H



735
3
COMe
Cl
H
H
H



736
4
COMe
Cl
H
H
H



737
1
CO2Me
Cl
H
H
H



738
2
CO2Me
Cl
H
H
H



739
3
CO2Me
Cl
H
H
H



740
4
CO2Me
Cl
H
H
H



741
1
CO2tBu
Cl
H
H
H



742
2
CO2tBu
Cl
H
H
H



743
3
CO2tBu
Cl
H
H
H



744
4
CO2tBu
Cl
H
H
H



745
1
CONHMe
Cl
H
H
H



746
2
CONHMe
Cl
H
H
H



747
3
CONHMe
Cl
H
H
H



748
4
CONHMe
Cl
H
H
H



749
1
SO2Me
Cl
H
H
H



750
2
SO2Me
Cl
H
H
H



751
3
SO2Me
Cl
H
H
H



752
4
SO2Me
Cl
H
H
H



753
1
SO2NH2
Cl
H
H
H



754
2
SO2NH2
Cl
H
H
H



755
3
SO2NH2
Cl
H
H
H



756
4
SO2NH2
Cl
H
H
H



757
1
H
CN
H
H
H



758
2
H
CN
H
H
H



759
3
H
CN
H
H
H



760
4
H
CN
H
H
H



761
1
Me
CN
H
H
H



762
2
Me
CN
H
H
H



763
3
Me
CN
H
H
H



764
4
Me
CN
H
H
H



765
1
CH2Ph
CN
H
H
H



766
2
CH2Ph
CN
H
H
H



767
3
CH2Ph
CN
H
H
H



768
4
CH2Ph
CN
H
H
H



769
1
COMe
CN
H
H
H



770
2
COMe
CN
H
H
H



771
3
COMe
CN
H
H
H



772
4
COMe
CN
H
H
H



773
1
CO2Me
CN
H
H
H



774
2
CO2Me
CN
H
H
H



775
3
CO2Me
CN
H
H
H



776
4
CO2Me
CN
H
H
H



777
1
CO2tBu
CN
H
H
H



778
2
CO2tBu
CN
H
H
H



779
3
CO2tBu
CN
H
H
H



780
4
CO2tBu
CN
H
H
H



781
1
CONHMe
CN
H
H
H



782
2
CONHMe
CN
H
H
H



783
3
CONHMe
CN
H
H
H



784
4
CONHMe
CN
H
H
H



785
1
SO2Me
CN
H
H
H



786
2
SO2Me
CN
H
H
H



787
3
SO2Me
CN
H
H
H



788
4
SO2Me
CN
H
H
H



789
1
SO2NH2
CN
H
H
H



790
2
SO2NH2
CN
H
H
H



791
3
SO2NH2
CN
H
H
H



792
4
SO2NH2
CN
H
H
H



793
1
H
H
H
H
OH



794
2
H
H
H
H
OH



795
3
H
H
H
H
OH



796
4
H
H
H
H
OH



797
1
Me
H
H
H
OH



798
2
Me
H
H
H
OH



799
3
Me
H
H
H
OH



800
4
Me
H
H
H
OH



801
1
CH2Ph
H
H
H
OH



802
2
CH2Ph
H
H
H
OH



803
3
CH2Ph
H
H
H
OH



804
4
CH2Ph
H
H
H
OH



805
1
COMe
H
H
H
OH



806
2
COMe
H
H
H
OH



807
3
COMe
H
H
H
OH



808
4
COMe
H
H
H
OH



809
1
CO2Me
H
H
H
OH



810
2
CO2Me
H
H
H
OH



811
3
CO2Me
H
H
H
OH



812
4
CO2Me
H
H
H
OH



813
1
CO2tBu
H
H
H
OH



814
2
CO2tBu
H
H
H
OH



815
3
CO2tBu
H
H
H
OH



816
4
CO2tBu
H
H
H
OH



817
1
CONHMe
H
H
H
OH



818
2
CONHMe
H
H
H
OH



819
3
CONHMe
H
H
H
OH



820
4
CONHMe
H
H
H
OH



821
1
SO2Me
H
H
H
OH



822
2
SO2Me
H
H
H
OH



823
3
SO2Me
H
H
H
OH



824
4
SO2Me
H
H
H
OH



825
1
SO2NH2
H
H
H
OH



826
2
SO2NH2
H
H
H
OH



827
3
SO2NH2
H
H
H
OH



828
4
SO2NH2
H
H
H
OH



829
1
H
H
H
H
OMe



830
2
H
H
H
H
OMe



831
3
H
H
H
H
OMe



832
4
H
H
H
H
OMe



833
1
Me
H
H
H
OMe



834
2
Me
H
H
H
OMe



835
3
Me
H
H
H
OMe



836
4
Me
H
H
H
OMe



837
1
CH2Ph
H
H
H
OMe



838
2
CH2Ph
H
H
H
OMe



839
3
CH2Ph
H
H
H
OMe



840
4
CH2Ph
H
H
H
OMe



841
1
COMe
H
H
H
OMe



842
2
COMe
H
H
H
OMe



843
3
COMe
H
H
H
OMe



844
4
COMe
H
H
H
OMe



845
1
CO2Me
H
H
H
OMe



846
2
CO2Me
H
H
H
OMe



847
3
CO2Me
H
H
H
OMe



848
4
CO2Me
H
H
H
OMe



849
1
CO2tBu
H
H
H
OMe



850
2
CO2tBu
H
H
H
OMe



851
3
CO2tBu
H
H
H
OMe



852
4
CO2tBu
H
H
H
OMe



853
1
CONHMe
H
H
H
OMe



854
2
CONHMe
H
H
H
OMe



855
3
CONHMe
H
H
H
OMe



856
4
CONHMe
H
H
H
OMe



857
1
SO2Me
H
H
H
OMe



858
2
SO2Me
H
H
H
OMe



859
3
SO2Me
H
H
H
OMe



860
4
SO2Me
H
H
H
OMe



861
1
SO2NH2
H
H
H
OMe



862
2
SO2NH2
H
H
H
OMe



863
3
SO2NH2
H
H
H
OMe



864
4
SO2NH2
H
H
H
OMe



865
1
H
H
H
H
Me



866
2
H
H
H
H
Me



867
3
H
H
H
H
Me



868
4
H
H
H
H
Me



869
1
Me
H
H
H
Me



870
2
Me
H
H
H
Me



871
3
Me
H
H
H
Me



872
4
Me
H
H
H
Me



873
1
CH2Ph
H
H
H
Me



874
2
CH2Ph
H
H
H
Me



875
3
CH2Ph
H
H
H
Me



876
4
CH2Ph
H
H
H
Me



877
1
COMe
H
H
H
Me



878
2
COMe
H
H
H
Me



879
3
COMe
H
H
H
Me



880
4
COMe
H
H
H
Me



881
1
CO2Me
H
H
H
Me



882
2
CO2Me
H
H
H
Me



883
3
CO2Me
H
H
H
Me



884
4
CO2Me
H
H
H
Me



885
1
CO2tBu
H
H
H
Me



886
2
CO2tBu
H
H
H
Me



887
3
CO2tBu
H
H
H
Me



888
4
CO2tBu
H
H
H
Me



889
1
CONHMe
H
H
H
Me



890
2
CONHMe
H
H
H
Me



891
3
CONHMe
H
H
H
Me



892
4
CONHMe
H
H
H
Me



893
1
SO2Me
H
H
H
Me



894
2
SO2Me
H
H
H
Me



895
3
SO2Me
H
H
H
Me



896
4
SO2Me
H
H
H
Me



897
1
SO2NH2
H
H
H
Me



898
2
SO2NH2
H
H
H
Me



899
3
SO2NH2
H
H
H
Me



900
4
SO2NH2
H
H
H
Me



901
1
H
H
H
H
CF3



902
2
H
H
H
H
CF3



903
3
H
H
H
H
CF3



904
4
H
H
H
H
CF3



905
1
Me
H
H
H
CF3



906
2
Me
H
H
H
CF3



907
3
Me
H
H
H
CF3



908
4
Me
H
H
H
CF3



909
1
CH2Ph
H
H
H
CF3



910
2
CH2Ph
H
H
H
CF3



911
3
CH2Ph
H
H
H
CF3



912
4
CH2Ph
H
H
H
CF3



913
1
COMe
H
H
H
CF3



914
2
COMe
H
H
H
CF3



915
3
COMe
H
H
H
CF3



916
4
COMe
H
H
H
CF3



917
1
CO2Me
H
H
H
CF3



918
2
CO2Me
H
H
H
CF3



919
3
CO2Me
H
H
H
CF3



920
4
CO2Me
H
H
H
CF3



921
1
CO2tBu
H
H
H
CF3



922
2
CO2tBu
H
H
H
CF3



923
3
CO2tBu
H
H
H
CF3



924
4
CO2tBu
H
H
H
CF3



925
1
CONHMe
H
H
H
CF3



926
2
CONHMe
H
H
H
CF3



927
3
CONHMe
H
H
H
CF3



928
4
CONHMe
H
H
H
CF3



929
1
SO2Me
H
H
H
CF3



930
2
SO2Me
H
H
H
CF3



931
3
SO2Me
H
H
H
CF3



932
4
SO2Me
H
H
H
CF3



933
1
SO2NH2
H
H
H
CF3



934
2
SO2NH2
H
H
H
CF3



935
3
SO2NH2
H
H
H
CF3



936
4
SO2NH2
H
H
H
CF3



937
1
H
H
H
H
F



938
2
H
H
H
H
F



939
3
H
H
H
H
F



940
3
H
H
H
H
F



941
1
Me
H
H
H
F



942
2
Me
H
H
H
F



943
3
Me
H
H
H
F



944
4
Me
H
H
H
F



945
1
CH2Ph
H
H
H
F



946
2
CH2Ph
H
H
H
F



947
3
CH2Ph
H
H
H
F



948
4
CH2Ph
H
H
H
F



949
1
COMe
H
H
H
F



950
2
COMe
H
H
H
F



951
3
COMe
H
H
H
F



952
4
COMe
H
H
H
F



953
1
CO2Me
H
H
H
F



954
2
CO2Me
H
H
H
F



955
3
CO2Me
H
H
H
F



956
4
CO2Me
H
H
H
F



957
1
CO2tBu
H
H
H
F



958
2
CO2tBu
H
H
H
F



959
3
CO2tBu
H
H
H
F



960
4
CO2tBu
H
H
H
F



961
1
CONHMe
H
H
H
F



962
2
CONHMe
H
H
H
F



963
3
CONHMe
H
H
H
F



964
4
CONHMe
H
H
H
F



965
1
SO2Me
H
H
H
F



966
2
SO2Me
H
H
H
F



967
3
SO2Me
H
H
H
F



968
4
SO2Me
H
H
H
F



969
1
SO2NH2
H
H
H
F



970
2
SO2NH2
H
H
H
F



971
3
SO2NH2
H
H
H
F



972
4
SO2NH2
H
H
H
F



973
1
H
H
H
H
Cl



974
2
H
H
H
H
Cl



975
3
H
H
H
H
Cl



976
4
H
H
H
H
Cl



977
1
Me
H
H
H
Cl



978
2
Me
H
H
H
Cl



979
3
Me
H
H
H
Cl



980
4
Me
H
H
H
Cl



981
1
CH2Ph
H
H
H
Cl



982
2
CH2Ph
H
H
H
Cl



983
3
CH2Ph
H
H
H
Cl



984
4
CH2Ph
H
H
H
Cl



985
1
COMe
H
H
H
Cl



986
2
COMe
H
H
H
Cl



987
3
COMe
H
H
H
Cl



988
4
COMe
H
H
H
Cl



989
1
CO2Me
H
H
H
Cl



990
2
CO2Me
H
H
H
Cl



991
3
CO2Me
H
H
H
Cl



992
4
CO2Me
H
H
H
Cl



993
1
CO2tBu
H
H
H
Cl



994
2
CO2tBu
H
H
H
Cl



995
3
CO2tBu
H
H
H
Cl



996
4
CO2tBu
H
H
H
Cl



997
1
CONHMe
H
H
H
Cl



998
2
CONHMe
H
H
H
Cl



999
3
CONHMe
H
H
H
Cl



1000
4
CONHMe
H
H
H
Cl



1001
1
SO2Me
H
H
H
Cl



1002
2
SO2Me
H
H
H
Cl



1003
3
SO2Me
H
H
H
Cl



1004
4
SO2Me
H
H
H
Cl



1005
1
SO2NH2
H
H
H
Cl



1006
2
SO2NH2
H
H
H
Cl



1007
3
SO2NH2
H
H
H
Cl



1008
4
SO2NH2
H
H
H
Cl



1009
1
H
H
H
H
CN



1010
2
H
H
H
H
CN



1011
3
H
H
H
H
CN



1012
4
H
H
H
H
CN



1013
1
Me
H
H
H
CN



1014
2
Me
H
H
H
CN



1015
3
Me
H
H
H
CN



1016
4
Me
H
H
H
CN



1017
1
CH2Ph
H
H
H
CN



1018
2
CH2Ph
H
H
H
CN



1019
3
CH2Ph
H
H
H
CN



1020
4
CH2Ph
H
H
H
CN



1021
1
COMe
H
H
H
CN



1022
2
COMe
H
H
H
CN



1023
3
COMe
H
H
H
CN



1024
4
COMe
H
H
H
CN



1025
1
CO2Me
H
H
H
CN



1026
2
CO2Me
H
H
H
CN



1027
3
CO2Me
H
H
H
CN



1028
4
CO2Me
H
H
H
CN



1029
1
CO2tBu
H
H
H
CN



1030
2
CO2tBu
H
H
H
CN



1031
3
CO2tBu
H
H
H
CN



1032
4
CO2tBu
H
H
H
CN



1033
1
CONHMe
H
H
H
CN



1034
2
CONHMe
H
H
H
CN



1035
3
CONHMe
H
H
H
CN



1036
4
CONHMe
H
H
H
CN



1037
1
SO2Me
H
H
H
CN



1038
2
SO2Me
H
H
H
CN



1039
3
SO2Me
H
H
H
CN



1040
4
SO2Me
H
H
H
CN



1041
1
SO2NH2
H
H
H
CN



1042
2
SO2NH2
H
H
H
CN



1043
3
SO2NH2
H
H
H
CN



1044
4
SO2NH2
H
H
H
CN










Exemplary embodiments include compounds having the formula (XXIX)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 23.

















TABLE 23







Entry
n
R7
R20a
R20b
R20c
R20e
























1
1
H
H
H
H
H



2
2
H
H
H
H
H



3
3
H
H
H
H
H



4
4
H
H
H
H
H



5
1
Me
H
H
H
H



6
2
Me
H
H
H
H



7
3
Me
H
H
H
H



8
4
Me
H
H
H
H



9
1
CH2Ph
H
H
H
H



10
2
CH2Ph
H
H
H
H



11
3
CH2Ph
H
H
H
H



12
4
CH2Ph
H
H
H
H



13
1
COMe
H
H
H
H



14
2
COMe
H
H
H
H



15
3
COMe
H
H
H
H



16
4
COMe
H
H
H
H



17
1
CO2Me
H
H
H
H



18
2
CO2Me
H
H
H
H



19
3
CO2Me
H
H
H
H



20
4
CO2Me
H
H
H
H



21
1
CO2tBu
H
H
H
H



22
2
CO2tBu
H
H
H
H



23
3
CO2tBu
H
H
H
H



24
4
CO2tBu
H
H
H
H



25
1
CONHMe
H
H
H
H



26
2
CONHMe
H
H
H
H



27
3
CONHMe
H
H
H
H



28
4
CONHMe
H
H
H
H



29
1
SO2Me
H
H
H
H



30
2
SO2Me
H
H
H
H



31
3
SO2Me
H
H
H
H



32
4
SO2Me
H
H
H
H



33
1
SO2NH2
H
H
H
H



34
2
SO2NH2
H
H
H
H



35
3
SO2NH2
H
H
H
H



36
4
SO2NH2
H
H
H
H



37
1
H
H
H
OH
H



38
2
H
H
H
OH
H



39
3
H
H
H
OH
H



40
4
H
H
H
OH
H



41
1
Me
H
H
OH
H



42
2
Me
H
H
OH
H



43
3
Me
H
H
OH
H



44
4
Me
H
H
OH
H



45
1
CH2Ph
H
H
OH
H



46
2
CH2Ph
H
H
OH
H



47
3
CH2Ph
H
H
OH
H



48
4
CH2Ph
H
H
OH
H



49
1
COMe
H
H
OH
H



50
2
COMe
H
H
OH
H



51
3
COMe
H
H
OH
H



52
4
COMe
H
H
OH
H



53
1
CO2Me
H
H
OH
H



54
2
CO2Me
H
H
OH
H



55
3
CO2Me
H
H
OH
H



56
4
CO2Me
H
H
OH
H



57
1
CO2tBu
H
H
OH
H



58
2
CO2tBu
H
H
OH
H



59
3
CO2tBu
H
H
OH
H



60
4
CO2tBu
H
H
OH
H



61
1
CONHMe
H
H
OH
H



62
2
CONHMe
H
H
OH
H



63
3
CONHMe
H
H
OH
H



64
4
CONHMe
H
H
OH
H



65
1
SO2Me
H
H
OH
H



66
2
SO2Me
H
H
OH
H



67
3
SO2Me
H
H
OH
H



68
4
SO2Me
H
H
OH
H



69
1
SO2NH2
H
H
OH
H



70
2
SO2NH2
H
H
OH
H



71
3
SO2NH2
H
H
OH
H



72
4
SO2NH2
H
H
OH
H



73
1
H
H
H
OMe
H



74
2
H
H
H
OMe
H



75
3
H
H
H
OMe
H



76
4
H
H
H
OMe
H



77
1
Me
H
H
OMe
H



78
2
Me
H
H
OMe
H



79
3
Me
H
H
OMe
H



80
4
Me
H
H
OMe
H



81
1
CH2Ph
H
H
OMe
H



82
2
CH2Ph
H
H
OMe
H



83
3
CH2Ph
H
H
OMe
H



84
4
CH2Ph
H
H
OMe
H



85
1
COMe
H
H
OMe
H



86
2
COMe
H
H
OMe
H



87
3
COMe
H
H
OMe
H



88
4
COMe
H
H
OMe
H



89
1
CO2Me
H
H
OMe
H



90
2
CO2Me
H
H
OMe
H



91
3
CO2Me
H
H
OMe
H



92
4
CO2Me
H
H
OMe
H



93
1
CO2tBu
H
H
OMe
H



94
2
CO2tBu
H
H
OMe
H



95
3
CO2tBu
H
H
OMe
H



96
1
CO2tBu
H
H
OMe
H



97
1
CONHMe
H
H
OMe
H



98
2
CONHMe
H
H
OMe
H



99
3
CONHMe
H
H
OMe
H



100
4
CONHMe
H
H
OMe
H



101
1
SO2Me
H
H
OMe
H



102
2
SO2Me
H
H
OMe
H



103
3
SO2Me
H
H
OMe
H



104
4
SO2Me
H
H
OMe
H



105
1
SO2NH2
H
H
OMe
H



106
2
SO2NH2
H
H
OMe
H



107
3
SO2NH2
H
H
OMe
H



108
4
SO2NH2
H
H
OMe
H



109
1
H
H
H
Me
H



110
2
H
H
H
Me
H



111
3
H
H
H
Me
H



112
4
H
H
H
Me
H



113
1
Me
H
H
Me
H



114
2
Me
H
H
Me
H



115
3
Me
H
H
Me
H



116
4
Me
H
H
Me
H



117
1
CH2Ph
H
H
Me
H



118
2
CH2Ph
H
H
Me
H



119
3
CH2Ph
H
H
Me
H



120
4
CH2Ph
H
H
Me
H



121
1
COMe
H
H
Me
H



122
2
COMe
H
H
Me
H



123
3
COMe
H
H
Me
H



124
4
COMe
H
H
Me
H



125
1
CO2Me
H
H
Me
H



126
2
CO2Me
H
H
Me
H



127
3
CO2Me
H
H
Me
H



128
4
CO2Me
H
H
Me
H



129
1
CO2tBu
H
H
Me
H



130
2
CO2tBu
H
H
Me
H



131
3
CO2tBu
H
H
Me
H



132
4
CO2tBu
H
H
Me
H



133
1
CONHMe
H
H
Me
H



134
2
CONHMe
H
H
Me
H



135
3
CONHMe
H
H
Me
H



136
4
CONHMe
H
H
Me
H



137
1
SO2Me
H
H
Me
H



138
2
SO2Me
H
H
Me
H



139
3
SO2Me
H
H
Me
H



140
4
SO2Me
H
H
Me
H



141
1
SO2NH2
H
H
Me
H



142
2
SO2NH2
H
H
Me
H



143
3
SO2NH2
H
H
Me
H



144
4
SO2NH2
H
H
Me
H



145
1
H
H
H
CF3
H



146
2
H
H
H
CF3
H



147
3
H
H
H
CF3
H



148
4
H
H
H
CF3
H



149
1
Me
H
H
CF3
H



150
2
Me
H
H
CF3
H



151
3
Me
H
H
CF3
H



152
4
Me
H
H
CF3
H



153
1
CH2Ph
H
H
CF3
H



154
2
CH2Ph
H
H
CF3
H



155
3
CH2Ph
H
H
CF3
H



156
4
CH2Ph
H
H
CF3
H



157
1
COMe
H
H
CF3
H



158
2
COMe
H
H
CF3
H



159
3
COMe
H
H
CF3
H



160
4
COMe
H
H
CF3
H



161
1
CO2Me
H
H
CF3
H



162
2
CO2Me
H
H
CF3
H



163
3
CO2Me
H
H
CF3
H



164
4
CO2Me
H
H
CF3
H



165
1
CO2tBu
H
H
CF3
H



166
2
CO2tBu
H
H
CF3
H



167
3
CO2tBu
H
H
CF3
H



168
4
CO2tBu
H
H
CF3
H



169
1
CONHMe
H
H
CF3
H



170
2
CONHMe
H
H
CF3
H



171
3
CONHMe
H
H
CF3
H



172
4
CONHMe
H
H
CF3
H



173
1
SO2Me
H
H
CF3
H



174
2
SO2Me
H
H
CF3
H



175
3
SO2Me
H
H
CF3
H



176
4
SO2Me
H
H
CF3
H



177
1
SO2NH2
H
H
CF3
H



178
2
SO2NH2
H
H
CF3
H



179
3
SO2NH2
H
H
CF3
H



180
4
SO2NH2
H
H
CF3
H



181
1
H
H
H
F
H



182
2
H
H
H
F
H



183
3
H
H
H
F
H



184
4
H
H
H
F
H



185
1
Me
H
H
F
H



186
2
Me
H
H
F
H



187
3
Me
H
H
F
H



188
4
Me
H
H
F
H



189
1
CH2Ph
H
H
F
H



190
2
CH2Ph
H
H
F
H



191
3
CH2Ph
H
H
F
H



192
4
CH2Ph
H
H
F
H



193
1
COMe
H
H
F
H



194
2
COMe
H
H
F
H



195
3
COMe
H
H
F
H



196
4
COMe
H
H
F
H



197
1
CO2Me
H
H
F
H



198
2
CO2Me
H
H
F
H



199
3
CO2Me
H
H
F
H



200
4
CO2Me
H
H
F
H



201
1
CO2tBu
H
H
F
H



202
2
CO2tBu
H
H
F
H



203
3
CO2tBu
H
H
F
H



204
4
CO2tBu
H
H
F
H



205
1
CONHMe
H
H
F
H



206
2
CONHMe
H
H
F
H



207
3
CONHMe
H
H
F
H



208
4
CONHMe
H
H
F
H



209
1
SO2Me
H
H
F
H



210
2
SO2Me
H
H
F
H



211
3
SO2Me
H
H
F
H



212
4
SO2Me
H
H
F
H



213
1
SO2NH2
H
H
F
H



214
2
SO2NH2
H
H
F
H



215
3
SO2NH2
H
H
F
H



216
4
SO2NH2
H
H
F
H



217
1
H
H
H
Cl
H



218
2
H
H
H
Cl
H



219
3
H
H
H
Cl
H



220
4
H
H
H
Cl
H



221
1
Me
H
H
Cl
H



222
2
Me
H
H
Cl
H



223
3
Me
H
H
Cl
H



224
4
Me
H
H
Cl
H



225
1
CH2Ph
H
H
Cl
H



226
2
CH2Ph
H
H
Cl
H



227
3
CH2Ph
H
H
Cl
H



228
4
CH2Ph
H
H
Cl
H



229
1
COMe
H
H
Cl
H



230
2
COMe
H
H
Cl
H



231
3
COMe
H
H
Cl
H



232
4
COMe
H
H
Cl
H



233
1
CO2Me
H
H
Cl
H



234
2
CO2Me
H
H
Cl
H



235
3
CO2Me
H
H
Cl
H



236
4
CO2Me
H
H
Cl
H



237
1
CO2tBu
H
H
Cl
H



238
2
CO2tBu
H
H
Cl
H



239
3
CO2tBu
H
H
Cl
H



240
4
CO2tBu
H
H
Cl
H



241
1
CONHMe
H
H
Cl
H



242
2
CONHMe
H
H
Cl
H



243
3
CONHMe
H
H
Cl
H



244
4
CONHMe
H
H
Cl
H



245
1
SO2Me
H
H
Cl
H



246
2
SO2Me
H
H
Cl
H



247
3
SO2Me
H
H
Cl
H



248
4
SO2Me
H
H
Cl
H



249
1
SO2NH2
H
H
Cl
H



250
2
SO2NH2
H
H
Cl
H



251
3
SO2NH2
H
H
Cl
H



252
4
SO2NH2
H
H
Cl
H



253
1
H
H
H
CN
H



254
2
H
H
H
CN
H



255
3
H
H
H
CN
H



256
4
H
H
H
CN
H



257
1
Me
H
H
CN
H



258
2
Me
H
H
CN
H



259
3
Me
H
H
CN
H



260
4
Me
H
H
CN
H



261
1
CH2Ph
H
H
CN
H



262
2
CH2Ph
H
H
CN
H



263
3
CH2Ph
H
H
CN
H



264
4
CH2Ph
H
H
CN
H



265
1
COMe
H
H
CN
H



266
2
COMe
H
H
CN
H



267
3
COMe
H
H
CN
H



268
4
COMe
H
H
CN
H



269
1
CO2Me
H
H
CN
H



270
2
CO2Me
H
H
CN
H



271
3
CO2Me
H
H
CN
H



272
4
CO2Me
H
H
CN
H



273
1
CO2tBu
H
H
CN
H



274
2
CO2tBu
H
H
CN
H



275
3
CO2tBu
H
H
CN
H



276
4
CO2tBu
H
H
CN
H



277
1
CONHMe
H
H
CN
H



278
2
CONHMe
H
H
CN
H



279
3
CONHMe
H
H
CN
H



280
4
CONHMe
H
H
CN
H



281
1
SO2Me
H
H
CN
H



282
2
SO2Me
H
H
CN
H



283
3
SO2Me
H
H
CN
H



284
4
SO2Me
H
H
CN
H



285
1
SO2NH2
H
H
CN
H



286
2
SO2NH2
H
H
CN
H



287
3
SO2NH2
H
H
CN
H



288
4
SO2NH2
H
H
CN
H



289
1
H
H
OH
H
H



290
2
H
H
OH
H
H



291
3
H
H
OH
H
H



292
4
H
H
OH
H
H



293
1
Me
H
OH
H
H



294
2
Me
H
OH
H
H



295
3
Me
H
OH
H
H



296
4
Me
H
OH
H
H



297
1
CH2Ph
H
OH
H
H



298
2
CH2Ph
H
OH
H
H



299
3
CH2Ph
H
OH
H
H



300
4
CH2Ph
H
OH
H
H



301
1
COMe
H
OH
H
H



302
2
COMe
H
OH
H
H



303
3
COMe
H
OH
H
H



304
4
COMe
H
OH
H
H



305
1
CO2Me
H
OH
H
H



306
2
CO2Me
H
OH
H
H



307
3
CO2Me
H
OH
H
H



308
4
CO2Me
H
OH
H
H



309
1
CO2tBu
H
OH
H
H



310
2
CO2tBu
H
OH
H
H



311
3
CO2tBu
H
OH
H
H



312
4
CO2tBu
H
OH
H
H



313
1
CONHMe
H
OH
H
H



314
2
CONHMe
H
OH
H
H



315
3
CONHMe
H
OH
H
H



316
4
CONHMe
H
OH
H
H



317
1
SO2Me
H
OH
H
H



318
2
SO2Me
H
OH
H
H



319
3
SO2Me
H
OH
H
H



320
4
SO2Me
H
OH
H
H



321
1
SO2NH2
H
OH
H
H



322
2
SO2NH2
H
OH
H
H



323
3
SO2NH2
H
OH
H
H



324
4
SO2NH2
H
OH
H
H



325
1
H
H
OMe
H
H



326
2
H
H
OMe
H
H



327
3
H
H
OMe
H
H



328
4
H
H
OMe
H
H



329
1
Me
H
OMe
H
H



330
2
Me
H
OMe
H
H



331
3
Me
H
OMe
H
H



332
4
Me
H
OMe
H
H



333
1
CH2Ph
H
OMe
H
H



334
2
CH2Ph
H
OMe
H
H



335
3
CH2Ph
H
OMe
H
H



336
4
CH2Ph
H
OMe
H
H



337
1
COMe
H
OMe
H
H



338
2
COMe
H
OMe
H
H



339
3
COMe
H
OMe
H
H



340
4
COMe
H
OMe
H
H



341
1
CO2Me
H
OMe
H
H



342
2
CO2Me
H
OMe
H
H



343
3
CO2Me
H
OMe
H
H



344
4
CO2Me
H
OMe
H
H



345
1
CO2tBu
H
OMe
H
H



346
2
CO2tBu
H
OMe
H
H



347
3
CO2tBu
H
OMe
H
H



348
4
CO2tBu
H
OMe
H
H



349
1
CONHMe
H
OMe
H
H



350
2
CONHMe
H
OMe
H
H



351
3
CONHMe
H
OMe
H
H



352
4
CONHMe
H
OMe
H
H



353
1
SO2Me
H
OMe
H
H



354
2
SO2Me
H
OMe
H
H



355
3
SO2Me
H
OMe
H
H



356
4
SO2Me
H
OMe
H
H



357
1
SO2NH2
H
OMe
H
H



358
2
SO2NH2
H
OMe
H
H



359
3
SO2NH2
H
OMe
H
H



360
4
SO2NH2
H
OMe
H
H



361
1
H
H
Me
H
H



362
2
H
H
Me
H
H



363
3
H
H
Me
H
H



364
4
H
H
Me
H
H



365
1
Me
H
Me
H
H



366
2
Me
H
Me
H
H



367
3
Me
H
Me
H
H



368
4
Me
H
Me
H
H



369
1
CH2Ph
H
Me
H
H



370
2
CH2Ph
H
Me
H
H



371
3
CH2Ph
H
Me
H
H



372
4
CH2Ph
H
Me
H
H



373
1
COMe
H
Me
H
H



374
2
COMe
H
Me
H
H



375
3
COMe
H
Me
H
H



376
4
COMe
H
Me
H
H



377
1
CO2Me
H
Me
H
H



378
2
CO2Me
H
Me
H
H



379
3
CO2Me
H
Me
H
H



380
4
CO2Me
H
Me
H
H



381
1
CO2tBu
H
Me
H
H



382
2
CO2tBu
H
Me
H
H



383
3
CO2tBu
H
Me
H
H



384
4
CO2tBu
H
Me
H
H



385
1
CONHMe
H
Me
H
H



386
2
CONHMe
H
Me
H
H



387
3
CONHMe
H
Me
H
H



388
4
CONHMe
H
Me
H
H



389
1
SO2Me
H
Me
H
H



390
2
SO2Me
H
Me
H
H



391
3
SO2Me
H
Me
H
H



392
4
SO2Me
H
Me
H
H



393
1
SO2NH2
H
Me
H
H



394
2
SO2NH2
H
Me
H
H



395
3
SO2NH2
H
Me
H
H



396
4
SO2NH2
H
Me
H
H



397
1
H
H
CF3
H
H



398
2
H
H
CF3
H
H



399
3
H
H
CF3
H
H



400
4
H
H
CF3
H
H



401
1
Me
H
CF3
H
H



402
2
Me
H
CF3
H
H



403
3
Me
H
CF3
H
H



404
4
Me
H
CF3
H
H



405
1
CH2Ph
H
CF3
H
H



406
2
CH2Ph
H
CF3
H
H



407
3
CH2Ph
H
CF3
H
H



408
4
CH2Ph
H
CF3
H
H



409
1
COMe
H
CF3
H
H



410
2
COMe
H
CF3
H
H



411
3
COMe
H
CF3
H
H



412
4
COMe
H
CF3
H
H



413
1
CO2Me
H
CF3
H
H



414
2
CO2Me
H
CF3
H
H



415
3
CO2Me
H
CF3
H
H



416
4
CO2Me
H
CF3
H
H



417
1
CO2tBu
H
CF3
H
H



418
2
CO2tBu
H
CF3
H
H



419
3
CO2tBu
H
CF3
H
H



420
4
CO2tBu
H
CF3
H
H



421
1
CONHMe
H
CF3
H
H



422
2
CONHMe
H
CF3
H
H



423
3
CONHMe
H
CF3
H
H



424
4
CONHMe
H
CF3
H
H



425
1
SO2Me
H
CF3
H
H



426
2
SO2Me
H
CF3
H
H



427
3
SO2Me
H
CF3
H
H



428
4
SO2Me
H
CF3
H
H



429
1
SO2NH2
H
CF3
H
H



430
2
SO2NH2
H
CF3
H
H



431
3
SO2NH2
H
CF3
H
H



432
4
SO2NH2
H
CF3
H
H



433
1
H
H
F
H
H



434
2
H
H
F
H
H



435
3
H
H
F
H
H



436
3
H
H
F
H
H



437
1
Me
H
F
H
H



438
2
Me
H
F
H
H



439
3
Me
H
F
H
H



440
4
Me
H
F
H
H



441
1
CH2Ph
H
F
H
H



442
2
CH2Ph
H
F
H
H



443
3
CH2Ph
H
F
H
H



444
4
CH2Ph
H
F
H
H



445
1
COMe
H
F
H
H



446
2
COMe
H
F
H
H



447
3
COMe
H
F
H
H



448
4
COMe
H
F
H
H



449
1
CO2Me
H
F
H
H



450
2
CO2Me
H
F
H
H



451
3
CO2Me
H
F
H
H



452
4
CO2Me
H
F
H
H



453
1
CO2tBu
H
F
H
H



454
2
CO2tBu
H
F
H
H



455
3
CO2tBu
H
F
H
H



456
4
CO2tBu
H
F
H
H



457
1
CONHMe
H
F
H
H



458
2
CONHMe
H
F
H
H



459
3
CONHMe
H
F
H
H



460
4
CONHMe
H
F
H
H



461
1
SO2Me
H
F
H
H



462
2
SO2Me
H
F
H
H



463
3
SO2Me
H
F
H
H



464
4
SO2Me
H
F
H
H



465
1
SO2NH2
H
F
H
H



466
2
SO2NH2
H
F
H
H



467
3
SO2NH2
H
F
H
H



468
4
SO2NH2
H
F
H
H



469
1
H
H
Cl
H
H



470
2
H
H
Cl
H
H



471
3
H
H
Cl
H
H



472
4
H
H
Cl
H
H



473
1
Me
H
Cl
H
H



474
2
Me
H
Cl
H
H



475
3
Me
H
Cl
H
H



476
4
Me
H
Cl
H
H



477
1
CH2Ph
H
Cl
H
H



478
2
CH2Ph
H
Cl
H
H



479
3
CH2Ph
H
Cl
H
H



480
4
CH2Ph
H
Cl
H
H



481
1
COMe
H
Cl
H
H



482
2
COMe
H
Cl
H
H



483
3
COMe
H
Cl
H
H



484
4
COMe
H
Cl
H
H



485
1
CO2Me
H
Cl
H
H



486
2
CO2Me
H
Cl
H
H



487
3
CO2Me
H
Cl
H
H



488
4
CO2Me
H
Cl
H
H



489
1
CO2tBu
H
Cl
H
H



490
2
CO2tBu
H
Cl
H
H



491
3
CO2tBu
H
Cl
H
H



492
4
CO2tBu
H
Cl
H
H



493
1
CONHMe
H
Cl
H
H



494
2
CONHMe
H
Cl
H
H



495
3
CONHMe
H
Cl
H
H



496
4
CONHMe
H
Cl
H
H



497
1
SO2Me
H
Cl
H
H



498
2
SO2Me
H
Cl
H
H



499
3
SO2Me
H
Cl
H
H



500
4
SO2Me
H
Cl
H
H



501
1
SO2NH2
H
Cl
H
H



502
2
SO2NH2
H
Cl
H
H



503
3
SO2NH2
H
Cl
H
H



504
4
SO2NH2
H
Cl
H
H



505
1
H
H
CN
H
H



506
2
H
H
CN
H
H



507
3
H
H
CN
H
H



508
4
H
H
CN
H
H



509
1
Me
H
CN
H
H



510
2
Me
H
CN
H
H



511
3
Me
H
CN
H
H



512
4
Me
H
CN
H
H



513
1
CH2Ph
H
CN
H
H



514
2
CH2Ph
H
CN
H
H



515
3
CH2Ph
H
CN
H
H



516
4
CH2Ph
H
CN
H
H



517
1
COMe
H
CN
H
H



518
2
COMe
H
CN
H
H



519
3
COMe
H
CN
H
H



520
4
COMe
H
CN
H
H



521
1
CO2Me
H
CN
H
H



522
2
CO2Me
H
CN
H
H



523
3
CO2Me
H
CN
H
H



524
4
CO2Me
H
CN
H
H



525
1
CO2tBu
H
CN
H
H



526
2
CO2tBu
H
CN
H
H



527
3
CO2tBu
H
CN
H
H



528
4
CO2tBu
H
CN
H
H



529
1
CONHMe
H
CN
H
H



530
2
CONHMe
H
CN
H
H



531
3
CONHMe
H
CN
H
H



532
4
CONHMe
H
CN
H
H



533
1
SO2Me
H
CN
H
H



534
2
SO2Me
H
CN
H
H



535
3
SO2Me
H
CN
H
H



536
4
SO2Me
H
CN
H
H



537
1
SO2NH2
H
CN
H
H



538
2
SO2NH2
H
CN
H
H



539
3
SO2NH2
H
CN
H
H



540
4
SO2NH2
H
CN
H
H



541
1
H
OH
H
H
H



542
2
H
OH
H
H
H



543
3
H
OH
H
H
H



544
4
H
OH
H
H
H



545
1
Me
OH
H
H
H



546
2
Me
OH
H
H
H



547
3
Me
OH
H
H
H



548
4
Me
OH
H
H
H



549
1
CH2Ph
OH
H
H
H



550
2
CH2Ph
OH
H
H
H



551
3
CH2Ph
OH
H
H
H



552
4
CH2Ph
OH
H
H
H



553
1
COMe
OH
H
H
H



554
2
COMe
OH
H
H
H



555
3
COMe
OH
H
H
H



556
4
COMe
OH
H
H
H



557
1
CO2Me
OH
H
H
H



558
2
CO2Me
OH
H
H
H



559
3
CO2Me
OH
H
H
H



560
4
CO2Me
OH
H
H
H



561
1
CO2tBu
OH
H
H
H



562
2
CO2tBu
OH
H
H
H



563
3
CO2tBu
OH
H
H
H



564
4
CO2tBu
OH
H
H
H



565
1
CONHMe
OH
H
H
H



566
2
CONHMe
OH
H
H
H



567
3
CONHMe
OH
H
H
H



568
4
CONHMe
OH
H
H
H



569
1
SO2Me
OH
H
H
H



570
2
SO2Me
OH
H
H
H



571
3
SO2Me
OH
H
H
H



572
4
SO2Me
OH
H
H
H



573
1
SO2NH2
OH
H
H
H



574
2
SO2NH2
OH
H
H
H



575
3
SO2NH2
OH
H
H
H



576
4
SO2NH2
OH
H
H
H



577
1
H
OMe
H
H
H



578
2
H
OMe
H
H
H



579
3
H
OMe
H
H
H



580
4
H
OMe
H
H
H



581
1
Me
OMe
H
H
H



582
2
Me
OMe
H
H
H



583
3
Me
OMe
H
H
H



584
4
Me
OMe
H
H
H



585
1
CH2Ph
OMe
H
H
H



586
2
CH2Ph
OMe
H
H
H



587
3
CH2Ph
OMe
H
H
H



588
4
CH2Ph
OMe
H
H
H



589
1
COMe
OMe
H
H
H



590
2
COMe
OMe
H
H
H



591
3
COMe
OMe
H
H
H



592
4
COMe
OMe
H
H
H



593
1
CO2Me
OMe
H
H
H



594
2
CO2Me
OMe
H
H
H



595
3
CO2Me
OMe
H
H
H



596
4
CO2Me
OMe
H
H
H



597
1
CO2tBu
OMe
H
H
H



598
2
CO2tBu
OMe
H
H
H



599
3
CO2tBu
OMe
H
H
H



600
4
CO2tBu
OMe
H
H
H



601
1
CONHMe
OMe
H
H
H



602
2
CONHMe
OMe
H
H
H



603
3
CONHMe
OMe
H
H
H



604
4
CONHMe
OMe
H
H
H



605
1
SO2Me
OMe
H
H
H



606
2
SO2Me
OMe
H
H
H



607
3
SO2Me
OMe
H
H
H



608
4
SO2Me
OMe
H
H
H



609
1
SO2NH2
OMe
H
H
H



610
2
SO2NH2
OMe
H
H
H



611
3
SO2NH2
OMe
H
H
H



612
4
SO2NH2
OMe
H
H
H



613
1
H
Me
H
H
H



614
2
H
Me
H
H
H



615
3
H
Me
H
H
H



616
4
H
Me
H
H
H



617
1
Me
Me
H
H
H



618
2
Me
Me
H
H
H



619
3
Me
Me
H
H
H



620
4
Me
Me
H
H
H



621
1
CH2Ph
Me
H
H
H



622
2
CH2Ph
Me
H
H
H



623
3
CH2Ph
Me
H
H
H



624
4
CH2Ph
Me
H
H
H



625
1
COMe
Me
H
H
H



626
2
COMe
Me
H
H
H



627
3
COMe
Me
H
H
H



628
4
COMe
Me
H
H
H



629
1
CO2Me
Me
H
H
H



630
2
CO2Me
Me
H
H
H



631
3
CO2Me
Me
H
H
H



632
4
CO2Me
Me
H
H
H



633
1
CO2tBu
Me
H
H
H



634
2
CO2tBu
Me
H
H
H



635
3
CO2tBu
Me
H
H
H



636
4
CO2tBu
Me
H
H
H



637
1
CONHMe
Me
H
H
H



638
2
CONHMe
Me
H
H
H



639
3
CONHMe
Me
H
H
H



640
4
CONHMe
Me
H
H
H



641
1
SO2Me
Me
H
H
H



642
2
SO2Me
Me
H
H
H



643
3
SO2Me
Me
H
H
H



644
4
SO2Me
Me
H
H
H



645
1
SO2NH2
Me
H
H
H



646
2
SO2NH2
Me
H
H
H



647
3
SO2NH2
Me
H
H
H



648
4
SO2NH2
Me
H
H
H



649
1
H
CF3
H
H
H



650
2
H
CF3
H
H
H



651
3
H
CF3
H
H
H



652
4
H
CF3
H
H
H



653
1
Me
CF3
H
H
H



654
2
Me
CF3
H
H
H



655
3
Me
CF3
H
H
H



656
4
Me
CF3
H
H
H



657
1
CH2Ph
CF3
H
H
H



658
2
CH2Ph
CF3
H
H
H



659
3
CH2Ph
CF3
H
H
H



660
4
CH2Ph
CF3
H
H
H



661
1
COMe
CF3
H
H
H



662
2
COMe
CF3
H
H
H



663
3
COMe
CF3
H
H
H



664
4
COMe
CF3
H
H
H



665
1
CO2Me
CF3
H
H
H



666
2
CO2Me
CF3
H
H
H



667
3
CO2Me
CF3
H
H
H



668
4
CO2Me
CF3
H
H
H



669
1
CO2tBu
CF3
H
H
H



670
2
CO2tBu
CF3
H
H
H



671
3
CO2tBu
CF3
H
H
H



672
4
CO2tBu
CF3
H
H
H



673
1
CONHMe
CF3
H
H
H



674
2
CONHMe
CF3
H
H
H



675
3
CONHMe
CF3
H
H
H



676
4
CONHMe
CF3
H
H
H



677
1
SO2Me
CF3
H
H
H



678
2
SO2Me
CF3
H
H
H



679
3
SO2Me
CF3
H
H
H



680
4
SO2Me
CF3
H
H
H



681
1
SO2NH2
CF3
H
H
H



682
2
SO2NH2
CF3
H
H
H



683
3
SO2NH2
CF3
H
H
H



684
4
SO2NH2
CF3
H
H
H



685
1
H
F
H
H
H



686
2
H
F
H
H
H



687
3
H
F
H
H
H



688
3
H
F
H
H
H



689
1
Me
F
H
H
H



690
2
Me
F
H
H
H



691
3
Me
F
H
H
H



692
4
Me
F
H
H
H



693
1
CH2Ph
F
H
H
H



694
2
CH2Ph
F
H
H
H



695
3
CH2Ph
F
H
H
H



696
4
CH2Ph
F
H
H
H



697
1
COMe
F
H
H
H



698
2
COMe
F
H
H
H



699
3
COMe
F
H
H
H



700
4
COMe
F
H
H
H



701
1
CO2Me
F
H
H
H



702
2
CO2Me
F
H
H
H



703
3
CO2Me
F
H
H
H



704
4
CO2Me
F
H
H
H



705
1
CO2tBu
F
H
H
H



706
2
CO2tBu
F
H
H
H



707
3
CO2tBu
F
H
H
H



708
4
CO2tBu
F
H
H
H



709
1
CONHMe
F
H
H
H



710
2
CONHMe
F
H
H
H



711
3
CONHMe
F
H
H
H



712
4
CONHMe
F
H
H
H



713
1
SO2Me
F
H
H
H



714
2
SO2Me
F
H
H
H



715
3
SO2Me
F
H
H
H



716
4
SO2Me
F
H
H
H



717
1
SO2NH2
F
H
H
H



718
2
SO2NH2
F
H
H
H



719
3
SO2NH2
F
H
H
H



720
4
SO2NH2
F
H
H
H



721
1
H
Cl
H
H
H



722
2
H
Cl
H
H
H



723
3
H
Cl
H
H
H



724
4
H
Cl
H
H
H



725
1
Me
Cl
H
H
H



726
2
Me
Cl
H
H
H



727
3
Me
Cl
H
H
H



728
4
Me
Cl
H
H
H



729
1
CH2Ph
Cl
H
H
H



730
2
CH2Ph
Cl
H
H
H



731
3
CH2Ph
Cl
H
H
H



732
4
CH2Ph
Cl
H
H
H



733
1
COMe
Cl
H
H
H



734
2
COMe
Cl
H
H
H



735
3
COMe
Cl
H
H
H



736
4
COMe
Cl
H
H
H



737
1
CO2Me
Cl
H
H
H



738
2
CO2Me
Cl
H
H
H



739
3
CO2Me
Cl
H
H
H



740
4
CO2Me
Cl
H
H
H



741
1
CO2tBu
Cl
H
H
H



742
2
CO2tBu
Cl
H
H
H



743
3
CO2tBu
Cl
H
H
H



744
4
CO2tBu
Cl
H
H
H



745
1
CONHMe
Cl
H
H
H



746
2
CONHMe
Cl
H
H
H



747
3
CONHMe
Cl
H
H
H



748
4
CONHMe
Cl
H
H
H



749
1
SO2Me
Cl
H
H
H



750
2
SO2Me
Cl
H
H
H



751
3
SO2Me
Cl
H
H
H



752
4
SO2Me
Cl
H
H
H



753
1
SO2NH2
Cl
H
H
H



754
2
SO2NH2
Cl
H
H
H



755
3
SO2NH2
Cl
H
H
H



756
4
SO2NH2
Cl
H
H
H



757
1
H
CN
H
H
H



758
2
H
CN
H
H
H



759
3
H
CN
H
H
H



760
4
H
CN
H
H
H



761
1
Me
CN
H
H
H



762
2
Me
CN
H
H
H



763
3
Me
CN
H
H
H



764
4
Me
CN
H
H
H



765
1
CH2Ph
CN
H
H
H



766
2
CH2Ph
CN
H
H
H



767
3
CH2Ph
CN
H
H
H



768
4
CH2Ph
CN
H
H
H



769
1
COMe
CN
H
H
H



770
2
COMe
CN
H
H
H



771
3
COMe
CN
H
H
H



772
4
COMe
CN
H
H
H



773
1
CO2Me
CN
H
H
H



774
2
CO2Me
CN
H
H
H



775
3
CO2Me
CN
H
H
H



776
4
CO2Me
CN
H
H
H



777
1
CO2tBu
CN
H
H
H



778
2
CO2tBu
CN
H
H
H



779
3
CO2tBu
CN
H
H
H



780
4
CO2tBu
CN
H
H
H



781
1
CONHMe
CN
H
H
H



782
2
CONHMe
CN
H
H
H



783
3
CONHMe
CN
H
H
H



784
4
CONHMe
CN
H
H
H



785
1
SO2Me
CN
H
H
H



786
2
SO2Me
CN
H
H
H



787
3
SO2Me
CN
H
H
H



788
4
SO2Me
CN
H
H
H



789
1
SO2NH2
CN
H
H
H



790
2
SO2NH2
CN
H
H
H



791
3
SO2NH2
CN
H
H
H



792
4
SO2NH2
CN
H
H
H



793
1
H
H
H
H
OH



794
2
H
H
H
H
OH



795
3
H
H
H
H
OH



796
4
H
H
H
H
OH



797
1
Me
H
H
H
OH



798
2
Me
H
H
H
OH



799
3
Me
H
H
H
OH



800
4
Me
H
H
H
OH



801
1
CH2Ph
H
H
H
OH



802
2
CH2Ph
H
H
H
OH



803
3
CH2Ph
H
H
H
OH



804
4
CH2Ph
H
H
H
OH



805
1
COMe
H
H
H
OH



806
2
COMe
H
H
H
OH



807
3
COMe
H
H
H
OH



808
4
COMe
H
H
H
OH



809
1
CO2Me
H
H
H
OH



810
2
CO2Me
H
H
H
OH



811
3
CO2Me
H
H
H
OH



812
4
CO2Me
H
H
H
OH



813
1
CO2tBu
H
H
H
OH



814
2
CO2tBu
H
H
H
OH



815
3
CO2tBu
H
H
H
OH



816
4
CO2tBu
H
H
H
OH



817
1
CONHMe
H
H
H
OH



818
2
CONHMe
H
H
H
OH



819
3
CONHMe
H
H
H
OH



820
4
CONHMe
H
H
H
OH



821
1
SO2Me
H
H
H
OH



822
2
SO2Me
H
H
H
OH



823
3
SO2Me
H
H
H
OH



824
4
SO2Me
H
H
H
OH



825
1
SO2NH2
H
H
H
OH



826
2
SO2NH2
H
H
H
OH



827
3
SO2NH2
H
H
H
OH



828
4
SO2NH2
H
H
H
OH



829
1
H
H
H
H
OMe



830
2
H
H
H
H
OMe



831
3
H
H
H
H
OMe



832
4
H
H
H
H
OMe



833
1
Me
H
H
H
OMe



834
2
Me
H
H
H
OMe



835
3
Me
H
H
H
OMe



836
4
Me
H
H
H
OMe



837
1
CH2Ph
H
H
H
OMe



838
2
CH2Ph
H
H
H
OMe



839
3
CH2Ph
H
H
H
OMe



840
4
CH2Ph
H
H
H
OMe



841
1
COMe
H
H
H
OMe



842
2
COMe
H
H
H
OMe



843
3
COMe
H
H
H
OMe



844
4
COMe
H
H
H
OMe



845
1
CO2Me
H
H
H
OMe



846
2
CO2Me
H
H
H
OMe



847
3
CO2Me
H
H
H
OMe



848
4
CO2Me
H
H
H
OMe



849
1
CO2tBu
H
H
H
OMe



850
2
CO2tBu
H
H
H
OMe



851
3
CO2tBu
H
H
H
OMe



852
4
CO2tBu
H
H
H
OMe



853
1
CONHMe
H
H
H
OMe



854
2
CONHMe
H
H
H
OMe



855
3
CONHMe
H
H
H
OMe



856
4
CONHMe
H
H
H
OMe



857
1
SO2Me
H
H
H
OMe



858
2
SO2Me
H
H
H
OMe



859
3
SO2Me
H
H
H
OMe



860
4
SO2Me
H
H
H
OMe



861
1
SO2NH2
H
H
H
OMe



862
2
SO2NH2
H
H
H
OMe



863
3
SO2NH2
H
H
H
OMe



864
4
SO2NH2
H
H
H
OMe



865
1
H
H
H
H
Me



866
2
H
H
H
H
Me



867
3
H
H
H
H
Me



868
4
H
H
H
H
Me



869
1
Me
H
H
H
Me



870
2
Me
H
H
H
Me



871
3
Me
H
H
H
Me



872
4
Me
H
H
H
Me



873
1
CH2Ph
H
H
H
Me



874
2
CH2Ph
H
H
H
Me



875
3
CH2Ph
H
H
H
Me



876
4
CH2Ph
H
H
H
Me



877
1
COMe
H
H
H
Me



878
2
COMe
H
H
H
Me



879
3
COMe
H
H
H
Me



880
4
COMe
H
H
H
Me



881
1
CO2Me
H
H
H
Me



882
2
CO2Me
H
H
H
Me



883
3
CO2Me
H
H
H
Me



884
4
CO2Me
H
H
H
Me



885
1
CO2tBu
H
H
H
Me



886
2
CO2tBu
H
H
H
Me



887
3
CO2tBu
H
H
H
Me



888
4
CO2tBu
H
H
H
Me



889
1
CONHMe
H
H
H
Me



890
2
CONHMe
H
H
H
Me



891
3
CONHMe
H
H
H
Me



892
4
CONHMe
H
H
H
Me



893
1
SO2Me
H
H
H
Me



894
2
SO2Me
H
H
H
Me



895
3
SO2Me
H
H
H
Me



896
4
SO2Me
H
H
H
Me



897
1
SO2NH2
H
H
H
Me



898
2
SO2NH2
H
H
H
Me



899
3
SO2NH2
H
H
H
Me



900
4
SO2NH2
H
H
H
Me



901
1
H
H
H
H
CF3



902
2
H
H
H
H
CF3



903
3
H
H
H
H
CF3



904
4
H
H
H
H
CF3



905
1
Me
H
H
H
CF3



906
2
Me
H
H
H
CF3



907
3
Me
H
H
H
CF3



908
4
Me
H
H
H
CF3



909
1
CH2Ph
H
H
H
CF3



910
2
CH2Ph
H
H
H
CF3



911
3
CH2Ph
H
H
H
CF3



912
4
CH2Ph
H
H
H
CF3



913
1
COMe
H
H
H
CF3



914
2
COMe
H
H
H
CF3



915
3
COMe
H
H
H
CF3



916
4
COMe
H
H
H
CF3



917
1
CO2Me
H
H
H
CF3



918
2
CO2Me
H
H
H
CF3



919
3
CO2Me
H
H
H
CF3



920
4
CO2Me
H
H
H
CF3



921
1
CO2tBu
H
H
H
CF3



922
2
CO2tBu
H
H
H
CF3



923
3
CO2tBu
H
H
H
CF3



924
4
CO2tBu
H
H
H
CF3



925
1
CONHMe
H
H
H
CF3



926
2
CONHMe
H
H
H
CF3



927
3
CONHMe
H
H
H
CF3



928
4
CONHMe
H
H
H
CF3



929
1
SO2Me
H
H
H
CF3



930
2
SO2Me
H
H
H
CF3



931
3
SO2Me
H
H
H
CF3



932
4
SO2Me
H
H
H
CF3



933
1
SO2NH2
H
H
H
CF3



934
2
SO2NH2
H
H
H
CF3



935
3
SO2NH2
H
H
H
CF3



936
4
SO2NH2
H
H
H
CF3



937
1
H
H
H
H
F



938
2
H
H
H
H
F



939
3
H
H
H
H
F



940
3
H
H
H
H
F



941
1
Me
H
H
H
F



942
2
Me
H
H
H
F



943
3
Me
H
H
H
F



944
4
Me
H
H
H
F



945
1
CH2Ph
H
H
H
F



946
2
CH2Ph
H
H
H
F



947
3
CH2Ph
H
H
H
F



948
4
CH2Ph
H
H
H
F



949
1
COMe
H
H
H
F



950
2
COMe
H
H
H
F



951
3
COMe
H
H
H
F



952
4
COMe
H
H
H
F



953
1
CO2Me
H
H
H
F



954
2
CO2Me
H
H
H
F



955
3
CO2Me
H
H
H
F



956
4
CO2Me
H
H
H
F



957
1
CO2tBu
H
H
H
F



958
2
CO2tBu
H
H
H
F



959
3
CO2tBu
H
H
H
F



960
4
CO2tBu
H
H
H
F



961
1
CONHMe
H
H
H
F



962
2
CONHMe
H
H
H
F



963
3
CONHMe
H
H
H
F



964
4
CONHMe
H
H
H
F



965
1
SO2Me
H
H
H
F



966
2
SO2Me
H
H
H
F



967
3
SO2Me
H
H
H
F



968
4
SO2Me
H
H
H
F



969
1
SO2NH2
H
H
H
F



970
2
SO2NH2
H
H
H
F



971
3
SO2NH2
H
H
H
F



972
4
SO2NH2
H
H
H
F



973
1
H
H
H
H
Cl



974
2
H
H
H
H
Cl



975
3
H
H
H
H
Cl



976
4
H
H
H
H
Cl



977
1
Me
H
H
H
Cl



978
2
Me
H
H
H
Cl



979
3
Me
H
H
H
Cl



980
4
Me
H
H
H
Cl



981
1
CH2Ph
H
H
H
Cl



982
2
CH2Ph
H
H
H
Cl



983
3
CH2Ph
H
H
H
Cl



984
4
CH2Ph
H
H
H
Cl



985
1
COMe
H
H
H
Cl



986
2
COMe
H
H
H
Cl



987
3
COMe
H
H
H
Cl



988
4
COMe
H
H
H
Cl



989
1
CO2Me
H
H
H
Cl



990
2
CO2Me
H
H
H
Cl



991
3
CO2Me
H
H
H
Cl



992
4
CO2Me
H
H
H
Cl



993
1
CO2tBu
H
H
H
Cl



994
2
CO2tBu
H
H
H
Cl



995
3
CO2tBu
H
H
H
Cl



996
4
CO2tBu
H
H
H
Cl



997
1
CONHMe
H
H
H
Cl



998
2
CONHMe
H
H
H
Cl



999
3
CONHMe
H
H
H
Cl



1000
4
CONHMe
H
H
H
Cl



1001
1
SO2Me
H
H
H
Cl



1002
2
SO2Me
H
H
H
Cl



1003
3
SO2Me
H
H
H
Cl



1004
4
SO2Me
H
H
H
Cl



1005
1
SO2NH2
H
H
H
Cl



1006
2
SO2NH2
H
H
H
Cl



1007
3
SO2NH2
H
H
H
Cl



1008
4
SO2NH2
H
H
H
Cl



1009
1
H
H
H
H
CN



1010
2
H
H
H
H
CN



1011
3
H
H
H
H
CN



1012
4
H
H
H
H
CN



1013
1
Me
H
H
H
CN



1014
2
Me
H
H
H
CN



1015
3
Me
H
H
H
CN



1016
4
Me
H
H
H
CN



1017
1
CH2Ph
H
H
H
CN



1018
2
CH2Ph
H
H
H
CN



1019
3
CH2Ph
H
H
H
CN



1020
4
CH2Ph
H
H
H
CN



1021
1
COMe
H
H
H
CN



1022
2
COMe
H
H
H
CN



1023
3
COMe
H
H
H
CN



1024
4
COMe
H
H
H
CN



1025
1
CO2Me
H
H
H
CN



1026
2
CO2Me
H
H
H
CN



1027
3
CO2Me
H
H
H
CN



1028
4
CO2Me
H
H
H
CN



1029
1
CO2tBu
H
H
H
CN



1030
2
CO2tBu
H
H
H
CN



1031
3
CO2tBu
H
H
H
CN



1032
4
CO2tBu
H
H
H
CN



1033
1
CONHMe
H
H
H
CN



1034
2
CONHMe
H
H
H
CN



1035
3
CONHMe
H
H
H
CN



1036
4
CONHMe
H
H
H
CN



1037
1
SO2Me
H
H
H
CN



1038
2
SO2Me
H
H
H
CN



1039
3
SO2Me
H
H
H
CN



1040
4
SO2Me
H
H
H
CN



1041
1
SO2NH2
H
H
H
CN



1042
2
SO2NH2
H
H
H
CN



1043
3
SO2NH2
H
H
H
CN



1044
4
SO2NH2
H
H
H
CN










Exemplary embodiments include compounds having the formula (XXX)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 24.

















TABLE 24







Entry
n
R7
R20a
R20b
R20c
R20e
























1
1
H
H
H
H
H



2
2
H
H
H
H
H



3
3
H
H
H
H
H



4
4
H
H
H
H
H



5
1
Me
H
H
H
H



6
2
Me
H
H
H
H



7
3
Me
H
H
H
H



8
4
Me
H
H
H
H



9
1
CH2Ph
H
H
H
H



10
2
CH2Ph
H
H
H
H



11
3
CH2Ph
H
H
H
H



12
4
CH2Ph
H
H
H
H



13
1
COMe
H
H
H
H



14
2
COMe
H
H
H
H



15
3
COMe
H
H
H
H



16
4
COMe
H
H
H
H



17
1
CO2Me
H
H
H
H



18
2
CO2Me
H
H
H
H



19
3
CO2Me
H
H
H
H



20
4
CO2Me
H
H
H
H



21
1
CO2tBu
H
H
H
H



22
2
CO2tBu
H
H
H
H



23
3
CO2tBu
H
H
H
H



24
4
CO2tBu
H
H
H
H



25
1
CONHMe
H
H
H
H



26
2
CONHMe
H
H
H
H



27
3
CONHMe
H
H
H
H



28
4
CONHMe
H
H
H
H



29
1
SO2Me
H
H
H
H



30
2
SO2Me
H
H
H
H



31
3
SO2Me
H
H
H
H



32
4
SO2Me
H
H
H
H



33
1
SO2NH2
H
H
H
H



34
2
SO2NH2
H
H
H
H



35
3
SO2NH2
H
H
H
H



36
4
SO2NH2
H
H
H
H



37
1
H
H
H
OH
H



38
2
H
H
H
OH
H



39
3
H
H
H
OH
H



40
4
H
H
H
OH
H



41
1
Me
H
H
OH
H



42
2
Me
H
H
OH
H



43
3
Me
H
H
OH
H



44
4
Me
H
H
OH
H



45
1
CH2Ph
H
H
OH
H



46
2
CH2Ph
H
H
OH
H



47
3
CH2Ph
H
H
OH
H



48
4
CH2Ph
H
H
OH
H



49
1
COMe
H
H
OH
H



50
2
COMe
H
H
OH
H



51
3
COMe
H
H
OH
H



52
4
COMe
H
H
OH
H



53
1
CO2Me
H
H
OH
H



54
2
CO2Me
H
H
OH
H



55
3
CO2Me
H
H
OH
H



56
4
CO2Me
H
H
OH
H



57
1
CO2tBu
H
H
OH
H



58
2
CO2tBu
H
H
OH
H



59
3
CO2tBu
H
H
OH
H



60
4
CO2tBu
H
H
OH
H



61
1
CONHMe
H
H
OH
H



62
2
CONHMe
H
H
OH
H



63
3
CONHMe
H
H
OH
H



64
4
CONHMe
H
H
OH
H



65
1
SO2Me
H
H
OH
H



66
2
SO2Me
H
H
OH
H



67
3
SO2Me
H
H
OH
H



68
4
SO2Me
H
H
OH
H



69
1
SO2NH2
H
H
OH
H



70
2
SO2NH2
H
H
OH
H



71
3
SO2NH2
H
H
OH
H



72
4
SO2NH2
H
H
OH
H



73
1
H
H
H
OMe
H



74
2
H
H
H
OMe
H



75
3
H
H
H
OMe
H



76
4
H
H
H
OMe
H



77
1
Me
H
H
OMe
H



78
2
Me
H
H
OMe
H



79
3
Me
H
H
OMe
H



80
4
Me
H
H
OMe
H



81
1
CH2Ph
H
H
OMe
H



82
2
CH2Ph
H
H
OMe
H



83
3
CH2Ph
H
H
OMe
H



84
4
CH2Ph
H
H
OMe
H



85
1
COMe
H
H
OMe
H



86
2
COMe
H
H
OMe
H



87
3
COMe
H
H
OMe
H



88
4
COMe
H
H
OMe
H



89
1
CO2Me
H
H
OMe
H



90
2
CO2Me
H
H
OMe
H



91
3
CO2Me
H
H
OMe
H



92
4
CO2Me
H
H
OMe
H



93
1
CO2tBu
H
H
OMe
H



94
2
CO2tBu
H
H
OMe
H



95
3
CO2tBu
H
H
OMe
H



96
1
CO2tBu
H
H
OMe
H



97
1
CONHMe
H
H
OMe
H



98
2
CONHMe
H
H
OMe
H



99
3
CONHMe
H
H
OMe
H



100
4
CONHMe
H
H
OMe
H



101
1
SO2Me
H
H
OMe
H



102
2
SO2Me
H
H
OMe
H



103
3
SO2Me
H
H
OMe
H



104
4
SO2Me
H
H
OMe
H



105
1
SO2NH2
H
H
OMe
H



106
2
SO2NH2
H
H
OMe
H



107
3
SO2NH2
H
H
OMe
H



108
4
SO2NH2
H
H
OMe
H



109
1
H
H
H
Me
H



110
2
H
H
H
Me
H



111
3
H
H
H
Me
H



112
4
H
H
H
Me
H



113
1
Me
H
H
Me
H



114
2
Me
H
H
Me
H



115
3
Me
H
H
Me
H



116
4
Me
H
H
Me
H



117
1
CH2Ph
H
H
Me
H



118
2
CH2Ph
H
H
Me
H



119
3
CH2Ph
H
H
Me
H



120
4
CH2Ph
H
H
Me
H



121
1
COMe
H
H
Me
H



122
2
COMe
H
H
Me
H



123
3
COMe
H
H
Me
H



124
4
COMe
H
H
Me
H



125
1
CO2Me
H
H
Me
H



126
2
CO2Me
H
H
Me
H



127
3
CO2Me
H
H
Me
H



128
4
CO2Me
H
H
Me
H



129
1
CO2tBu
H
H
Me
H



130
2
CO2tBu
H
H
Me
H



131
3
CO2tBu
H
H
Me
H



132
4
CO2tBu
H
H
Me
H



133
1
CONHMe
H
H
Me
H



134
2
CONHMe
H
H
Me
H



135
3
CONHMe
H
H
Me
H



136
4
CONHMe
H
H
Me
H



137
1
SO2Me
H
H
Me
H



138
2
SO2Me
H
H
Me
H



139
3
SO2Me
H
H
Me
H



140
4
SO2Me
H
H
Me
H



141
1
SO2NH2
H
H
Me
H



142
2
SO2NH2
H
H
Me
H



143
3
SO2NH2
H
H
Me
H



144
4
SO2NH2
H
H
Me
H



145
1
H
H
H
CF3
H



146
2
H
H
H
CF3
H



147
3
H
H
H
CF3
H



148
4
H
H
H
CF3
H



149
1
Me
H
H
CF3
H



150
2
Me
H
H
CF3
H



151
3
Me
H
H
CF3
H



152
4
Me
H
H
CF3
H



153
1
CH2Ph
H
H
CF3
H



154
2
CH2Ph
H
H
CF3
H



155
3
CH2Ph
H
H
CF3
H



156
4
CH2Ph
H
H
CF3
H



157
1
COMe
H
H
CF3
H



158
2
COMe
H
H
CF3
H



159
3
COMe
H
H
CF3
H



160
4
COMe
H
H
CF3
H



161
1
CO2Me
H
H
CF3
H



162
2
CO2Me
H
H
CF3
H



163
3
CO2Me
H
H
CF3
H



164
4
CO2Me
H
H
CF3
H



165
1
CO2tBu
H
H
CF3
H



166
2
CO2tBu
H
H
CF3
H



167
3
CO2tBu
H
H
CF3
H



168
4
CO2tBu
H
H
CF3
H



169
1
CONHMe
H
H
CF3
H



170
2
CONHMe
H
H
CF3
H



171
3
CONHMe
H
H
CF3
H



172
4
CONHMe
H
H
CF3
H



173
1
SO2Me
H
H
CF3
H



174
2
SO2Me
H
H
CF3
H



175
3
SO2Me
H
H
CF3
H



176
4
SO2Me
H
H
CF3
H



177
1
SO2NH2
H
H
CF3
H



178
2
SO2NH2
H
H
CF3
H



179
3
SO2NH2
H
H
CF3
H



180
4
SO2NH2
H
H
CF3
H



181
1
H
H
H
F
H



182
2
H
H
H
F
H



183
3
H
H
H
F
H



184
4
H
H
H
F
H



185
1
Me
H
H
F
H



186
2
Me
H
H
F
H



187
3
Me
H
H
F
H



188
4
Me
H
H
F
H



189
1
CH2Ph
H
H
F
H



190
2
CH2Ph
H
H
F
H



191
3
CH2Ph
H
H
F
H



192
4
CH2Ph
H
H
F
H



193
1
COMe
H
H
F
H



194
2
COMe
H
H
F
H



195
3
COMe
H
H
F
H



196
4
COMe
H
H
F
H



197
1
CO2Me
H
H
F
H



198
2
CO2Me
H
H
F
H



199
3
CO2Me
H
H
F
H



200
4
CO2Me
H
H
F
H



201
1
CO2tBu
H
H
F
H



202
2
CO2tBu
H
H
F
H



203
3
CO2tBu
H
H
F
H



204
4
CO2tBu
H
H
F
H



205
1
CONHMe
H
H
F
H



206
2
CONHMe
H
H
F
H



207
3
CONHMe
H
H
F
H



208
4
CONHMe
H
H
F
H



209
1
SO2Me
H
H
F
H



210
2
SO2Me
H
H
F
H



211
3
SO2Me
H
H
F
H



212
4
SO2Me
H
H
F
H



213
1
SO2NH2
H
H
F
H



214
2
SO2NH2
H
H
F
H



215
3
SO2NH2
H
H
F
H



216
4
SO2NH2
H
H
F
H



217
1
H
H
H
Cl
H



218
2
H
H
H
Cl
H



219
3
H
H
H
Cl
H



220
4
H
H
H
Cl
H



221
1
Me
H
H
Cl
H



222
2
Me
H
H
Cl
H



223
3
Me
H
H
Cl
H



224
4
Me
H
H
Cl
H



225
1
CH2Ph
H
H
Cl
H



226
2
CH2Ph
H
H
Cl
H



227
3
CH2Ph
H
H
Cl
H



228
4
CH2Ph
H
H
Cl
H



229
1
COMe
H
H
Cl
H



230
2
COMe
H
H
Cl
H



231
3
COMe
H
H
Cl
H



232
4
COMe
H
H
Cl
H



233
1
CO2Me
H
H
Cl
H



234
2
CO2Me
H
H
Cl
H



235
3
CO2Me
H
H
Cl
H



236
4
CO2Me
H
H
Cl
H



237
1
CO2tBu
H
H
Cl
H



238
2
CO2tBu
H
H
Cl
H



239
3
CO2tBu
H
H
Cl
H



240
4
CO2tBu
H
H
Cl
H



241
1
CONHMe
H
H
Cl
H



242
2
CONHMe
H
H
Cl
H



243
3
CONHMe
H
H
Cl
H



244
4
CONHMe
H
H
Cl
H



245
1
SO2Me
H
H
Cl
H



246
2
SO2Me
H
H
Cl
H



247
3
SO2Me
H
H
Cl
H



248
4
SO2Me
H
H
Cl
H



249
1
SO2NH2
H
H
Cl
H



250
2
SO2NH2
H
H
Cl
H



251
3
SO2NH2
H
H
Cl
H



252
4
SO2NH2
H
H
Cl
H



253
1
H
H
H
CN
H



254
2
H
H
H
CN
H



255
3
H
H
H
CN
H



256
4
H
H
H
CN
H



257
1
Me
H
H
CN
H



258
2
Me
H
H
CN
H



259
3
Me
H
H
CN
H



260
4
Me
H
H
CN
H



261
1
CH2Ph
H
H
CN
H



262
2
CH2Ph
H
H
CN
H



263
3
CH2Ph
H
H
CN
H



264
4
CH2Ph
H
H
CN
H



265
1
COMe
H
H
CN
H



266
2
COMe
H
H
CN
H



267
3
COMe
H
H
CN
H



268
4
COMe
H
H
CN
H



269
1
CO2Me
H
H
CN
H



270
2
CO2Me
H
H
CN
H



271
3
CO2Me
H
H
CN
H



272
4
CO2Me
H
H
CN
H



273
1
CO2tBu
H
H
CN
H



274
2
CO2tBu
H
H
CN
H



275
3
CO2tBu
H
H
CN
H



276
4
CO2tBu
H
H
CN
H



277
1
CONHMe
H
H
CN
H



278
2
CONHMe
H
H
CN
H



279
3
CONHMe
H
H
CN
H



280
4
CONHMe
H
H
CN
H



281
1
SO2Me
H
H
CN
H



282
2
SO2Me
H
H
CN
H



283
3
SO2Me
H
H
CN
H



284
4
SO2Me
H
H
CN
H



285
1
SO2NH2
H
H
CN
H



286
2
SO2NH2
H
H
CN
H



287
3
SO2NH2
H
H
CN
H



288
4
SO2NH2
H
H
CN
H



289
1
H
H
OH
H
H



290
2
H
H
OH
H
H



291
3
H
H
OH
H
H



292
4
H
H
OH
H
H



293
1
Me
H
OH
H
H



294
2
Me
H
OH
H
H



295
3
Me
H
OH
H
H



296
4
Me
H
OH
H
H



297
1
CH2Ph
H
OH
H
H



298
2
CH2Ph
H
OH
H
H



299
3
CH2Ph
H
OH
H
H



300
4
CH2Ph
H
OH
H
H



301
1
COMe
H
OH
H
H



302
2
COMe
H
OH
H
H



303
3
COMe
H
OH
H
H



304
4
COMe
H
OH
H
H



305
1
CO2Me
H
OH
H
H



306
2
CO2Me
H
OH
H
H



307
3
CO2Me
H
OH
H
H



308
4
CO2Me
H
OH
H
H



309
1
CO2tBu
H
OH
H
H



310
2
CO2tBu
H
OH
H
H



311
3
CO2tBu
H
OH
H
H



312
4
CO2tBu
H
OH
H
H



313
1
CONHMe
H
OH
H
H



314
2
CONHMe
H
OH
H
H



315
3
CONHMe
H
OH
H
H



316
4
CONHMe
H
OH
H
H



317
1
SO2Me
H
OH
H
H



318
2
SO2Me
H
OH
H
H



319
3
SO2Me
H
OH
H
H



320
4
SO2Me
H
OH
H
H



321
1
SO2NH2
H
OH
H
H



322
2
SO2NH2
H
OH
H
H



323
3
SO2NH2
H
OH
H
H



324
4
SO2NH2
H
OH
H
H



325
1
H
H
OMe
H
H



326
2
H
H
OMe
H
H



327
3
H
H
OMe
H
H



328
4
H
H
OMe
H
H



329
1
Me
H
OMe
H
H



330
2
Me
H
OMe
H
H



331
3
Me
H
OMe
H
H



332
4
Me
H
OMe
H
H



333
1
CH2Ph
H
OMe
H
H



334
2
CH2Ph
H
OMe
H
H



335
3
CH2Ph
H
OMe
H
H



336
4
CH2Ph
H
OMe
H
H



337
1
COMe
H
OMe
H
H



338
2
COMe
H
OMe
H
H



339
3
COMe
H
OMe
H
H



340
4
COMe
H
OMe
H
H



341
1
CO2Me
H
OMe
H
H



342
2
CO2Me
H
OMe
H
H



343
3
CO2Me
H
OMe
H
H



344
4
CO2Me
H
OMe
H
H



345
1
CO2tBu
H
OMe
H
H



346
2
CO2tBu
H
OMe
H
H



347
3
CO2tBu
H
OMe
H
H



348
4
CO2tBu
H
OMe
H
H



349
1
CONHMe
H
OMe
H
H



350
2
CONHMe
H
OMe
H
H



351
3
CONHMe
H
OMe
H
H



352
4
CONHMe
H
OMe
H
H



353
1
SO2Me
H
OMe
H
H



354
2
SO2Me
H
OMe
H
H



355
3
SO2Me
H
OMe
H
H



356
4
SO2Me
H
OMe
H
H



357
1
SO2NH2
H
OMe
H
H



358
2
SO2NH2
H
OMe
H
H



359
3
SO2NH2
H
OMe
H
H



360
4
SO2NH2
H
OMe
H
H



361
1
H
H
Me
H
H



362
2
H
H
Me
H
H



363
3
H
H
Me
H
H



364
4
H
H
Me
H
H



365
1
Me
H
Me
H
H



366
2
Me
H
Me
H
H



367
3
Me
H
Me
H
H



368
4
Me
H
Me
H
H



369
1
CH2Ph
H
Me
H
H



370
2
CH2Ph
H
Me
H
H



371
3
CH2Ph
H
Me
H
H



372
4
CH2Ph
H
Me
H
H



373
1
COMe
H
Me
H
H



374
2
COMe
H
Me
H
H



375
3
COMe
H
Me
H
H



376
4
COMe
H
Me
H
H



377
1
CO2Me
H
Me
H
H



378
2
CO2Me
H
Me
H
H



379
3
CO2Me
H
Me
H
H



380
4
CO2Me
H
Me
H
H



381
1
CO2tBu
H
Me
H
H



382
2
CO2tBu
H
Me
H
H



383
3
CO2tBu
H
Me
H
H



384
4
CO2tBu
H
Me
H
H



385
1
CONHMe
H
Me
H
H



386
2
CONHMe
H
Me
H
H



387
3
CONHMe
H
Me
H
H



388
4
CONHMe
H
Me
H
H



389
1
SO2Me
H
Me
H
H



390
2
SO2Me
H
Me
H
H



391
3
SO2Me
H
Me
H
H



392
4
SO2Me
H
Me
H
H



393
1
SO2NH2
H
Me
H
H



394
2
SO2NH2
H
Me
H
H



395
3
SO2NH2
H
Me
H
H



396
4
SO2NH2
H
Me
H
H



397
1
H
H
CF3
H
H



398
2
H
H
CF3
H
H



399
3
H
H
CF3
H
H



400
4
H
H
CF3
H
H



401
1
Me
H
CF3
H
H



402
2
Me
H
CF3
H
H



403
3
Me
H
CF3
H
H



404
4
Me
H
CF3
H
H



405
1
CH2Ph
H
CF3
H
H



406
2
CH2Ph
H
CF3
H
H



407
3
CH2Ph
H
CF3
H
H



408
4
CH2Ph
H
CF3
H
H



409
1
COMe
H
CF3
H
H



410
2
COMe
H
CF3
H
H



411
3
COMe
H
CF3
H
H



412
4
COMe
H
CF3
H
H



413
1
CO2Me
H
CF3
H
H



414
2
CO2Me
H
CF3
H
H



415
3
CO2Me
H
CF3
H
H



416
4
CO2Me
H
CF3
H
H



417
1
CO2tBu
H
CF3
H
H



418
2
CO2tBu
H
CF3
H
H



419
3
CO2tBu
H
CF3
H
H



420
4
CO2tBu
H
CF3
H
H



421
1
CONHMe
H
CF3
H
H



422
2
CONHMe
H
CF3
H
H



423
3
CONHMe
H
CF3
H
H



424
4
CONHMe
H
CF3
H
H



425
1
SO2Me
H
CF3
H
H



426
2
SO2Me
H
CF3
H
H



427
3
SO2Me
H
CF3
H
H



428
4
SO2Me
H
CF3
H
H



429
1
SO2NH2
H
CF3
H
H



430
2
SO2NH2
H
CF3
H
H



431
3
SO2NH2
H
CF3
H
H



432
4
SO2NH2
H
CF3
H
H



433
1
H
H
F
H
H



434
2
H
H
F
H
H



435
3
H
H
F
H
H



436
3
H
H
F
H
H



437
1
Me
H
F
H
H



438
2
Me
H
F
H
H



439
3
Me
H
F
H
H



440
4
Me
H
F
H
H



441
1
CH2Ph
H
F
H
H



442
2
CH2Ph
H
F
H
H



443
3
CH2Ph
H
F
H
H



444
4
CH2Ph
H
F
H
H



445
1
COMe
H
F
H
H



446
2
COMe
H
F
H
H



447
3
COMe
H
F
H
H



448
4
COMe
H
F
H
H



449
1
CO2Me
H
F
H
H



450
2
CO2Me
H
F
H
H



451
3
CO2Me
H
F
H
H



452
4
CO2Me
H
F
H
H



453
1
CO2tBu
H
F
H
H



454
2
CO2tBu
H
F
H
H



455
3
CO2tBu
H
F
H
H



456
4
CO2tBu
H
F
H
H



457
1
CONHMe
H
F
H
H



458
2
CONHMe
H
F
H
H



459
3
CONHMe
H
F
H
H



460
4
CONHMe
H
F
H
H



461
1
SO2Me
H
F
H
H



462
2
SO2Me
H
F
H
H



463
3
SO2Me
H
F
H
H



464
4
SO2Me
H
F
H
H



465
1
SO2NH2
H
F
H
H



466
2
SO2NH2
H
F
H
H



467
3
SO2NH2
H
F
H
H



468
4
SO2NH2
H
F
H
H



469
1
H
H
Cl
H
H



470
2
H
H
Cl
H
H



471
3
H
H
Cl
H
H



472
4
H
H
Cl
H
H



473
1
Me
H
Cl
H
H



474
2
Me
H
Cl
H
H



475
3
Me
H
Cl
H
H



476
4
Me
H
Cl
H
H



477
1
CH2Ph
H
Cl
H
H



478
2
CH2Ph
H
Cl
H
H



479
3
CH2Ph
H
Cl
H
H



480
4
CH2Ph
H
Cl
H
H



481
1
COMe
H
Cl
H
H



482
2
COMe
H
Cl
H
H



483
3
COMe
H
Cl
H
H



484
4
COMe
H
Cl
H
H



485
1
CO2Me
H
Cl
H
H



486
2
CO2Me
H
Cl
H
H



487
3
CO2Me
H
Cl
H
H



488
4
CO2Me
H
Cl
H
H



489
1
CO2tBu
H
Cl
H
H



490
2
CO2tBu
H
Cl
H
H



491
3
CO2tBu
H
Cl
H
H



492
4
CO2tBu
H
Cl
H
H



493
1
CONHMe
H
Cl
H
H



494
2
CONHMe
H
Cl
H
H



495
3
CONHMe
H
Cl
H
H



496
4
CONHMe
H
Cl
H
H



497
1
SO2Me
H
Cl
H
H



498
2
SO2Me
H
Cl
H
H



499
3
SO2Me
H
Cl
H
H



500
4
SO2Me
H
Cl
H
H



501
1
SO2NH2
H
Cl
H
H



502
2
SO2NH2
H
Cl
H
H



503
3
SO2NH2
H
Cl
H
H



504
4
SO2NH2
H
Cl
H
H



505
1
H
H
CN
H
H



506
2
H
H
CN
H
H



507
3
H
H
CN
H
H



508
4
H
H
CN
H
H



509
1
Me
H
CN
H
H



510
2
Me
H
CN
H
H



511
3
Me
H
CN
H
H



512
4
Me
H
CN
H
H



513
1
CH2Ph
H
CN
H
H



514
2
CH2Ph
H
CN
H
H



515
3
CH2Ph
H
CN
H
H



516
4
CH2Ph
H
CN
H
H



517
1
COMe
H
CN
H
H



518
2
COMe
H
CN
H
H



519
3
COMe
H
CN
H
H



520
4
COMe
H
CN
H
H



521
1
CO2Me
H
CN
H
H



522
2
CO2Me
H
CN
H
H



523
3
CO2Me
H
CN
H
H



524
4
CO2Me
H
CN
H
H



525
1
CO2tBu
H
CN
H
H



526
2
CO2tBu
H
CN
H
H



527
3
CO2tBu
H
CN
H
H



528
4
CO2tBu
H
CN
H
H



529
1
CONHMe
H
CN
H
H



530
2
CONHMe
H
CN
H
H



531
3
CONHMe
H
CN
H
H



532
4
CONHMe
H
CN
H
H



533
1
SO2Me
H
CN
H
H



534
2
SO2Me
H
CN
H
H



535
3
SO2Me
H
CN
H
H



536
4
SO2Me
H
CN
H
H



537
1
SO2NH2
H
CN
H
H



538
2
SO2NH2
H
CN
H
H



539
3
SO2NH2
H
CN
H
H



540
4
SO2NH2
H
CN
H
H



541
1
H
OH
H
H
H



542
2
H
OH
H
H
H



543
3
H
OH
H
H
H



544
4
H
OH
H
H
H



545
1
Me
OH
H
H
H



546
2
Me
OH
H
H
H



547
3
Me
OH
H
H
H



548
4
Me
OH
H
H
H



549
1
CH2Ph
OH
H
H
H



550
2
CH2Ph
OH
H
H
H



551
3
CH2Ph
OH
H
H
H



552
4
CH2Ph
OH
H
H
H



553
1
COMe
OH
H
H
H



554
2
COMe
OH
H
H
H



555
3
COMe
OH
H
H
H



556
4
COMe
OH
H
H
H



557
1
CO2Me
OH
H
H
H



558
2
CO2Me
OH
H
H
H



559
3
CO2Me
OH
H
H
H



560
4
CO2Me
OH
H
H
H



561
1
CO2tBu
OH
H
H
H



562
2
CO2tBu
OH
H
H
H



563
3
CO2tBu
OH
H
H
H



564
4
CO2tBu
OH
H
H
H



565
1
CONHMe
OH
H
H
H



566
2
CONHMe
OH
H
H
H



567
3
CONHMe
OH
H
H
H



568
4
CONHMe
OH
H
H
H



569
1
SO2Me
OH
H
H
H



570
2
SO2Me
OH
H
H
H



571
3
SO2Me
OH
H
H
H



572
4
SO2Me
OH
H
H
H



573
1
SO2NH2
OH
H
H
H



574
2
SO2NH2
OH
H
H
H



575
3
SO2NH2
OH
H
H
H



576
4
SO2NH2
OH
H
H
H



577
1
H
OMe
H
H
H



578
2
H
OMe
H
H
H



579
3
H
OMe
H
H
H



580
4
H
OMe
H
H
H



581
1
Me
OMe
H
H
H



582
2
Me
OMe
H
H
H



583
3
Me
OMe
H
H
H



584
4
Me
OMe
H
H
H



585
1
CH2Ph
OMe
H
H
H



586
2
CH2Ph
OMe
H
H
H



587
3
CH2Ph
OMe
H
H
H



588
4
CH2Ph
OMe
H
H
H



589
1
COMe
OMe
H
H
H



590
2
COMe
OMe
H
H
H



591
3
COMe
OMe
H
H
H



592
4
COMe
OMe
H
H
H



593
1
CO2Me
OMe
H
H
H



594
2
CO2Me
OMe
H
H
H



595
3
CO2Me
OMe
H
H
H



596
4
CO2Me
OMe
H
H
H



597
1
CO2tBu
OMe
H
H
H



598
2
CO2tBu
OMe
H
H
H



599
3
CO2tBu
OMe
H
H
H



600
4
CO2tBu
OMe
H
H
H



601
1
CONHMe
OMe
H
H
H



602
2
CONHMe
OMe
H
H
H



603
3
CONHMe
OMe
H
H
H



604
4
CONHMe
OMe
H
H
H



605
1
SO2Me
OMe
H
H
H



606
2
SO2Me
OMe
H
H
H



607
3
SO2Me
OMe
H
H
H



608
4
SO2Me
OMe
H
H
H



609
1
SO2NH2
OMe
H
H
H



610
2
SO2NH2
OMe
H
H
H



611
3
SO2NH2
OMe
H
H
H



612
4
SO2NH2
OMe
H
H
H



613
1
H
Me
H
H
H



614
2
H
Me
H
H
H



615
3
H
Me
H
H
H



616
4
H
Me
H
H
H



617
1
Me
Me
H
H
H



618
2
Me
Me
H
H
H



619
3
Me
Me
H
H
H



620
4
Me
Me
H
H
H



621
1
CH2Ph
Me
H
H
H



622
2
CH2Ph
Me
H
H
H



623
3
CH2Ph
Me
H
H
H



624
4
CH2Ph
Me
H
H
H



625
1
COMe
Me
H
H
H



626
2
COMe
Me
H
H
H



627
3
COMe
Me
H
H
H



628
4
COMe
Me
H
H
H



629
1
CO2Me
Me
H
H
H



630
2
CO2Me
Me
H
H
H



631
3
CO2Me
Me
H
H
H



632
4
CO2Me
Me
H
H
H



633
1
CO2tBu
Me
H
H
H



634
2
CO2tBu
Me
H
H
H



635
3
CO2tBu
Me
H
H
H



636
4
CO2tBu
Me
H
H
H



637
1
CONHMe
Me
H
H
H



638
2
CONHMe
Me
H
H
H



639
3
CONHMe
Me
H
H
H



640
4
CONHMe
Me
H
H
H



641
1
SO2Me
Me
H
H
H



642
2
SO2Me
Me
H
H
H



643
3
SO2Me
Me
H
H
H



644
4
SO2Me
Me
H
H
H



645
1
SO2NH2
Me
H
H
H



646
2
SO2NH2
Me
H
H
H



647
3
SO2NH2
Me
H
H
H



648
4
SO2NH2
Me
H
H
H



649
1
H
CF3
H
H
H



650
2
H
CF3
H
H
H



651
3
H
CF3
H
H
H



652
4
H
CF3
H
H
H



653
1
Me
CF3
H
H
H



654
2
Me
CF3
H
H
H



655
3
Me
CF3
H
H
H



656
4
Me
CF3
H
H
H



657
1
CH2Ph
CF3
H
H
H



658
2
CH2Ph
CF3
H
H
H



659
3
CH2Ph
CF3
H
H
H



660
4
CH2Ph
CF3
H
H
H



661
1
COMe
CF3
H
H
H



662
2
COMe
CF3
H
H
H



663
3
COMe
CF3
H
H
H



664
4
COMe
CF3
H
H
H



665
1
CO2Me
CF3
H
H
H



666
2
CO2Me
CF3
H
H
H



667
3
CO2Me
CF3
H
H
H



668
4
CO2Me
CF3
H
H
H



669
1
CO2tBu
CF3
H
H
H



670
2
CO2tBu
CF3
H
H
H



671
3
CO2tBu
CF3
H
H
H



672
4
CO2tBu
CF3
H
H
H



673
1
CONHMe
CF3
H
H
H



674
2
CONHMe
CF3
H
H
H



675
3
CONHMe
CF3
H
H
H



676
4
CONHMe
CF3
H
H
H



677
1
SO2Me
CF3
H
H
H



678
2
SO2Me
CF3
H
H
H



679
3
SO2Me
CF3
H
H
H



680
4
SO2Me
CF3
H
H
H



681
1
SO2NH2
CF3
H
H
H



682
2
SO2NH2
CF3
H
H
H



683
3
SO2NH2
CF3
H
H
H



684
4
SO2NH2
CF3
H
H
H



685
1
H
F
H
H
H



686
2
H
F
H
H
H



687
3
H
F
H
H
H



688
3
H
F
H
H
H



689
1
Me
F
H
H
H



690
2
Me
F
H
H
H



691
3
Me
F
H
H
H



692
4
Me
F
H
H
H



693
1
CH2Ph
F
H
H
H



694
2
CH2Ph
F
H
H
H



695
3
CH2Ph
F
H
H
H



696
4
CH2Ph
F
H
H
H



697
1
COMe
F
H
H
H



698
2
COMe
F
H
H
H



699
3
COMe
F
H
H
H



700
4
COMe
F
H
H
H



701
1
CO2Me
F
H
H
H



702
2
CO2Me
F
H
H
H



703
3
CO2Me
F
H
H
H



704
4
CO2Me
F
H
H
H



705
1
CO2tBu
F
H
H
H



706
2
CO2tBu
F
H
H
H



707
3
CO2tBu
F
H
H
H



708
4
CO2tBu
F
H
H
H



709
1
CONHMe
F
H
H
H



710
2
CONHMe
F
H
H
H



711
3
CONHMe
F
H
H
H



712
4
CONHMe
F
H
H
H



713
1
SO2Me
F
H
H
H



714
2
SO2Me
F
H
H
H



715
3
SO2Me
F
H
H
H



716
4
SO2Me
F
H
H
H



717
1
SO2NH2
F
H
H
H



718
2
SO2NH2
F
H
H
H



719
3
SO2NH2
F
H
H
H



720
4
SO2NH2
F
H
H
H



721
1
H
Cl
H
H
H



722
2
H
Cl
H
H
H



723
3
H
Cl
H
H
H



724
4
H
Cl
H
H
H



725
1
Me
Cl
H
H
H



726
2
Me
Cl
H
H
H



727
3
Me
Cl
H
H
H



728
4
Me
Cl
H
H
H



729
1
CH2Ph
Cl
H
H
H



730
2
CH2Ph
Cl
H
H
H



731
3
CH2Ph
Cl
H
H
H



732
4
CH2Ph
Cl
H
H
H



733
1
COMe
Cl
H
H
H



734
2
COMe
Cl
H
H
H



735
3
COMe
Cl
H
H
H



736
4
COMe
Cl
H
H
H



737
1
CO2Me
Cl
H
H
H



738
2
CO2Me
Cl
H
H
H



739
3
CO2Me
Cl
H
H
H



740
4
CO2Me
Cl
H
H
H



741
1
CO2tBu
Cl
H
H
H



742
2
CO2tBu
Cl
H
H
H



743
3
CO2tBu
Cl
H
H
H



744
4
CO2tBu
Cl
H
H
H



745
1
CONHMe
Cl
H
H
H



746
2
CONHMe
Cl
H
H
H



747
3
CONHMe
Cl
H
H
H



748
4
CONHMe
Cl
H
H
H



749
1
SO2Me
Cl
H
H
H



750
2
SO2Me
Cl
H
H
H



751
3
SO2Me
Cl
H
H
H



752
4
SO2Me
Cl
H
H
H



753
1
SO2NH2
Cl
H
H
H



754
2
SO2NH2
Cl
H
H
H



755
3
SO2NH2
Cl
H
H
H



756
4
SO2NH2
Cl
H
H
H



757
1
H
CN
H
H
H



758
2
H
CN
H
H
H



759
3
H
CN
H
H
H



760
4
H
CN
H
H
H



761
1
Me
CN
H
H
H



762
2
Me
CN
H
H
H



763
3
Me
CN
H
H
H



764
4
Me
CN
H
H
H



765
1
CH2Ph
CN
H
H
H



766
2
CH2Ph
CN
H
H
H



767
3
CH2Ph
CN
H
H
H



768
4
CH2Ph
CN
H
H
H



769
1
COMe
CN
H
H
H



770
2
COMe
CN
H
H
H



771
3
COMe
CN
H
H
H



772
4
COMe
CN
H
H
H



773
1
CO2Me
CN
H
H
H



774
2
CO2Me
CN
H
H
H



775
3
CO2Me
CN
H
H
H



776
4
CO2Me
CN
H
H
H



777
1
CO2tBu
CN
H
H
H



778
2
CO2tBu
CN
H
H
H



779
3
CO2tBu
CN
H
H
H



780
4
CO2tBu
CN
H
H
H



781
1
CONHMe
CN
H
H
H



782
2
CONHMe
CN
H
H
H



783
3
CONHMe
CN
H
H
H



784
4
CONHMe
CN
H
H
H



785
1
SO2Me
CN
H
H
H



786
2
SO2Me
CN
H
H
H



787
3
SO2Me
CN
H
H
H



788
4
SO2Me
CN
H
H
H



789
1
SO2NH2
CN
H
H
H



790
2
SO2NH2
CN
H
H
H



791
3
SO2NH2
CN
H
H
H



792
4
SO2NH2
CN
H
H
H



793
1
H
H
H
H
OH



794
2
H
H
H
H
OH



795
3
H
H
H
H
OH



796
4
H
H
H
H
OH



797
1
Me
H
H
H
OH



798
2
Me
H
H
H
OH



799
3
Me
H
H
H
OH



800
4
Me
H
H
H
OH



801
1
CH2Ph
H
H
H
OH



802
2
CH2Ph
H
H
H
OH



803
3
CH2Ph
H
H
H
OH



804
4
CH2Ph
H
H
H
OH



805
1
COMe
H
H
H
OH



806
2
COMe
H
H
H
OH



807
3
COMe
H
H
H
OH



808
4
COMe
H
H
H
OH



809
1
CO2Me
H
H
H
OH



810
2
CO2Me
H
H
H
OH



811
3
CO2Me
H
H
H
OH



812
4
CO2Me
H
H
H
OH



813
1
CO2tBu
H
H
H
OH



814
2
CO2tBu
H
H
H
OH



815
3
CO2tBu
H
H
H
OH



816
4
CO2tBu
H
H
H
OH



817
1
CONHMe
H
H
H
OH



818
2
CONHMe
H
H
H
OH



819
3
CONHMe
H
H
H
OH



820
4
CONHMe
H
H
H
OH



821
1
SO2Me
H
H
H
OH



822
2
SO2Me
H
H
H
OH



823
3
SO2Me
H
H
H
OH



824
4
SO2Me
H
H
H
OH



825
1
SO2NH2
H
H
H
OH



826
2
SO2NH2
H
H
H
OH



827
3
SO2NH2
H
H
H
OH



828
4
SO2NH2
H
H
H
OH



829
1
H
H
H
H
OMe



830
2
H
H
H
H
OMe



831
3
H
H
H
H
OMe



832
4
H
H
H
H
OMe



833
1
Me
H
H
H
OMe



834
2
Me
H
H
H
OMe



835
3
Me
H
H
H
OMe



836
4
Me
H
H
H
OMe



837
1
CH2Ph
H
H
H
OMe



838
2
CH2Ph
H
H
H
OMe



839
3
CH2Ph
H
H
H
OMe



840
4
CH2Ph
H
H
H
OMe



841
1
COMe
H
H
H
OMe



842
2
COMe
H
H
H
OMe



843
3
COMe
H
H
H
OMe



844
4
COMe
H
H
H
OMe



845
1
CO2Me
H
H
H
OMe



846
2
CO2Me
H
H
H
OMe



847
3
CO2Me
H
H
H
OMe



848
4
CO2Me
H
H
H
OMe



849
1
CO2tBu
H
H
H
OMe



850
2
CO2tBu
H
H
H
OMe



851
3
CO2tBu
H
H
H
OMe



852
4
CO2tBu
H
H
H
OMe



853
1
CONHMe
H
H
H
OMe



854
2
CONHMe
H
H
H
OMe



855
3
CONHMe
H
H
H
OMe



856
4
CONHMe
H
H
H
OMe



857
1
SO2Me
H
H
H
OMe



858
2
SO2Me
H
H
H
OMe



859
3
SO2Me
H
H
H
OMe



860
4
SO2Me
H
H
H
OMe



861
1
SO2NH2
H
H
H
OMe



862
2
SO2NH2
H
H
H
OMe



863
3
SO2NH2
H
H
H
OMe



864
4
SO2NH2
H
H
H
OMe



865
1
H
H
H
H
Me



866
2
H
H
H
H
Me



867
3
H
H
H
H
Me



868
4
H
H
H
H
Me



869
1
Me
H
H
H
Me



870
2
Me
H
H
H
Me



871
3
Me
H
H
H
Me



872
4
Me
H
H
H
Me



873
1
CH2Ph
H
H
H
Me



874
2
CH2Ph
H
H
H
Me



875
3
CH2Ph
H
H
H
Me



876
4
CH2Ph
H
H
H
Me



877
1
COMe
H
H
H
Me



878
2
COMe
H
H
H
Me



879
3
COMe
H
H
H
Me



880
4
COMe
H
H
H
Me



881
1
CO2Me
H
H
H
Me



882
2
CO2Me
H
H
H
Me



883
3
CO2Me
H
H
H
Me



884
4
CO2Me
H
H
H
Me



885
1
CO2tBu
H
H
H
Me



886
2
CO2tBu
H
H
H
Me



887
3
CO2tBu
H
H
H
Me



888
4
CO2tBu
H
H
H
Me



889
1
CONHMe
H
H
H
Me



890
2
CONHMe
H
H
H
Me



891
3
CONHMe
H
H
H
Me



892
4
CONHMe
H
H
H
Me



893
1
SO2Me
H
H
H
Me



894
2
SO2Me
H
H
H
Me



895
3
SO2Me
H
H
H
Me



896
4
SO2Me
H
H
H
Me



897
1
SO2NH2
H
H
H
Me



898
2
SO2NH2
H
H
H
Me



899
3
SO2NH2
H
H
H
Me



900
4
SO2NH2
H
H
H
Me



901
1
H
H
H
H
CF3



902
2
H
H
H
H
CF3



903
3
H
H
H
H
CF3



904
4
H
H
H
H
CF3



905
1
Me
H
H
H
CF3



906
2
Me
H
H
H
CF3



907
3
Me
H
H
H
CF3



908
4
Me
H
H
H
CF3



909
1
CH2Ph
H
H
H
CF3



910
2
CH2Ph
H
H
H
CF3



911
3
CH2Ph
H
H
H
CF3



912
4
CH2Ph
H
H
H
CF3



913
1
COMe
H
H
H
CF3



914
2
COMe
H
H
H
CF3



915
3
COMe
H
H
H
CF3



916
4
COMe
H
H
H
CF3



917
1
CO2Me
H
H
H
CF3



918
2
CO2Me
H
H
H
CF3



919
3
CO2Me
H
H
H
CF3



920
4
CO2Me
H
H
H
CF3



921
1
CO2tBu
H
H
H
CF3



922
2
CO2tBu
H
H
H
CF3



923
3
CO2tBu
H
H
H
CF3



924
4
CO2tBu
H
H
H
CF3



925
1
CONHMe
H
H
H
CF3



926
2
CONHMe
H
H
H
CF3



927
3
CONHMe
H
H
H
CF3



928
4
CONHMe
H
H
H
CF3



929
1
SO2Me
H
H
H
CF3



930
2
SO2Me
H
H
H
CF3



931
3
SO2Me
H
H
H
CF3



932
4
SO2Me
H
H
H
CF3



933
1
SO2NH2
H
H
H
CF3



934
2
SO2NH2
H
H
H
CF3



935
3
SO2NH2
H
H
H
CF3



936
4
SO2NH2
H
H
H
CF3



937
1
H
H
H
H
F



938
2
H
H
H
H
F



939
3
H
H
H
H
F



940
3
H
H
H
H
F



941
1
Me
H
H
H
F



942
2
Me
H
H
H
F



943
3
Me
H
H
H
F



944
4
Me
H
H
H
F



945
1
CH2Ph
H
H
H
F



946
2
CH2Ph
H
H
H
F



947
3
CH2Ph
H
H
H
F



948
4
CH2Ph
H
H
H
F



949
1
COMe
H
H
H
F



950
2
COMe
H
H
H
F



951
3
COMe
H
H
H
F



952
4
COMe
H
H
H
F



953
1
CO2Me
H
H
H
F



954
2
CO2Me
H
H
H
F



955
3
CO2Me
H
H
H
F



956
4
CO2Me
H
H
H
F



957
1
CO2tBu
H
H
H
F



958
2
CO2tBu
H
H
H
F



959
3
CO2tBu
H
H
H
F



960
4
CO2tBu
H
H
H
F



961
1
CONHMe
H
H
H
F



962
2
CONHMe
H
H
H
F



963
3
CONHMe
H
H
H
F



964
4
CONHMe
H
H
H
F



965
1
SO2Me
H
H
H
F



966
2
SO2Me
H
H
H
F



967
3
SO2Me
H
H
H
F



968
4
SO2Me
H
H
H
F



969
1
SO2NH2
H
H
H
F



970
2
SO2NH2
H
H
H
F



971
3
SO2NH2
H
H
H
F



972
4
SO2NH2
H
H
H
F



973
1
H
H
H
H
Cl



974
2
H
H
H
H
Cl



975
3
H
H
H
H
Cl



976
4
H
H
H
H
Cl



977
1
Me
H
H
H
Cl



978
2
Me
H
H
H
Cl



979
3
Me
H
H
H
Cl



980
4
Me
H
H
H
Cl



981
1
CH2Ph
H
H
H
Cl



982
2
CH2Ph
H
H
H
Cl



983
3
CH2Ph
H
H
H
Cl



984
4
CH2Ph
H
H
H
Cl



985
1
COMe
H
H
H
Cl



986
2
COMe
H
H
H
Cl



987
3
COMe
H
H
H
Cl



988
4
COMe
H
H
H
Cl



989
1
CO2Me
H
H
H
Cl



990
2
CO2Me
H
H
H
Cl



991
3
CO2Me
H
H
H
Cl



992
4
CO2Me
H
H
H
Cl



993
1
CO2tBu
H
H
H
Cl



994
2
CO2tBu
H
H
H
Cl



995
3
CO2tBu
H
H
H
Cl



996
4
CO2tBu
H
H
H
Cl



997
1
CONHMe
H
H
H
Cl



998
2
CONHMe
H
H
H
Cl



999
3
CONHMe
H
H
H
Cl



1000
4
CONHMe
H
H
H
Cl



1001
1
SO2Me
H
H
H
Cl



1002
2
SO2Me
H
H
H
Cl



1003
3
SO2Me
H
H
H
Cl



1004
4
SO2Me
H
H
H
Cl



1005
1
SO2NH2
H
H
H
Cl



1006
2
SO2NH2
H
H
H
Cl



1007
3
SO2NH2
H
H
H
Cl



1008
4
SO2NH2
H
H
H
Cl



1009
1
H
H
H
H
CN



1010
2
H
H
H
H
CN



1011
3
H
H
H
H
CN



1012
4
H
H
H
H
CN



1013
1
Me
H
H
H
CN



1014
2
Me
H
H
H
CN



1015
3
Me
H
H
H
CN



1016
4
Me
H
H
H
CN



1017
1
CH2Ph
H
H
H
CN



1018
2
CH2Ph
H
H
H
CN



1019
3
CH2Ph
H
H
H
CN



1020
4
CH2Ph
H
H
H
CN



1021
1
COMe
H
H
H
CN



1022
2
COMe
H
H
H
CN



1023
3
COMe
H
H
H
CN



1024
4
COMe
H
H
H
CN



1025
1
CO2Me
H
H
H
CN



1026
2
CO2Me
H
H
H
CN



1027
3
CO2Me
H
H
H
CN



1028
4
CO2Me
H
H
H
CN



1029
1
CO2tBu
H
H
H
CN



1030
2
CO2tBu
H
H
H
CN



1031
3
CO2tBu
H
H
H
CN



1032
4
CO2tBu
H
H
H
CN



1033
1
CONHMe
H
H
H
CN



1034
2
CONHMe
H
H
H
CN



1035
3
CONHMe
H
H
H
CN



1036
4
CONHMe
H
H
H
CN



1037
1
SO2Me
H
H
H
CN



1038
2
SO2Me
H
H
H
CN



1039
3
SO2Me
H
H
H
CN



1040
4
SO2Me
H
H
H
CN



1041
1
SO2NH2
H
H
H
CN



1042
2
SO2NH2
H
H
H
CN



1043
3
SO2NH2
H
H
H
CN



1044
4
SO2NH2
H
H
H
CN










Exemplary embodiments include compounds having the formula (XXXI)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 25.

















TABLE 25







Entry
n
R7
R20a
R20b
R20d
R20e
























1
1
H
H
H
H
H



2
2
H
H
H
H
H



3
3
H
H
H
H
H



4
4
H
H
H
H
H



5
1
Me
H
H
H
H



6
2
Me
H
H
H
H



7
3
Me
H
H
H
H



8
4
Me
H
H
H
H



9
1
CH2Ph
H
H
H
H



10
2
CH2Ph
H
H
H
H



11
3
CH2Ph
H
H
H
H



12
4
CH2Ph
H
H
H
H



13
1
COMe
H
H
H
H



14
2
COMe
H
H
H
H



15
3
COMe
H
H
H
H



16
4
COMe
H
H
H
H



17
1
CO2Me
H
H
H
H



18
2
CO2Me
H
H
H
H



19
3
CO2Me
H
H
H
H



20
4
CO2Me
H
H
H
H



21
1
CO2tBu
H
H
H
H



22
2
CO2tBu
H
H
H
H



23
3
CO2tBu
H
H
H
H



24
4
CO2tBu
H
H
H
H



25
1
CONHMe
H
H
H
H



26
2
CONHMe
H
H
H
H



27
3
CONHMe
H
H
H
H



28
4
CONHMe
H
H
H
H



29
1
SO2Me
H
H
H
H



30
2
SO2Me
H
H
H
H



31
3
SO2Me
H
H
H
H



32
4
SO2Me
H
H
H
H



33
1
SO2NH2
H
H
H
H



34
2
SO2NH2
H
H
H
H



35
3
SO2NH2
H
H
H
H



36
4
SO2NH2
H
H
H
H



37
1
H
H
H
OH
H



38
2
H
H
H
OH
H



39
3
H
H
H
OH
H



40
4
H
H
H
OH
H



41
1
Me
H
H
OH
H



42
2
Me
H
H
OH
H



43
3
Me
H
H
OH
H



44
4
Me
H
H
OH
H



45
1
CH2Ph
H
H
OH
H



46
2
CH2Ph
H
H
OH
H



47
3
CH2Ph
H
H
OH
H



48
4
CH2Ph
H
H
OH
H



49
1
COMe
H
H
OH
H



50
2
COMe
H
H
OH
H



51
3
COMe
H
H
OH
H



52
4
COMe
H
H
OH
H



53
1
CO2Me
H
H
OH
H



54
2
CO2Me
H
H
OH
H



55
3
CO2Me
H
H
OH
H



56
4
CO2Me
H
H
OH
H



57
1
CO2tBu
H
H
OH
H



58
2
CO2tBu
H
H
OH
H



59
3
CO2tBu
H
H
OH
H



60
4
CO2tBu
H
H
OH
H



61
1
CONHMe
H
H
OH
H



62
2
CONHMe
H
H
OH
H



63
3
CONHMe
H
H
OH
H



64
4
CONHMe
H
H
OH
H



65
1
SO2Me
H
H
OH
H



66
2
SO2Me
H
H
OH
H



67
3
SO2Me
H
H
OH
H



68
4
SO2Me
H
H
OH
H



69
1
SO2NH2
H
H
OH
H



70
2
SO2NH2
H
H
OH
H



71
3
SO2NH2
H
H
OH
H



72
4
SO2NH2
H
H
OH
H



73
1
H
H
H
OMe
H



74
2
H
H
H
OMe
H



75
3
H
H
H
OMe
H



76
4
H
H
H
OMe
H



77
1
Me
H
H
OMe
H



78
2
Me
H
H
OMe
H



79
3
Me
H
H
OMe
H



80
4
Me
H
H
OMe
H



81
1
CH2Ph
H
H
OMe
H



82
2
CH2Ph
H
H
OMe
H



83
3
CH2Ph
H
H
OMe
H



84
4
CH2Ph
H
H
OMe
H



85
1
COMe
H
H
OMe
H



86
2
COMe
H
H
OMe
H



87
3
COMe
H
H
OMe
H



88
4
COMe
H
H
OMe
H



89
1
CO2Me
H
H
OMe
H



90
2
CO2Me
H
H
OMe
H



91
3
CO2Me
H
H
OMe
H



92
4
CO2Me
H
H
OMe
H



93
1
CO2tBu
H
H
OMe
H



94
2
CO2tBu
H
H
OMe
H



95
3
CO2tBu
H
H
OMe
H



96
1
CO2tBu
H
H
OMe
H



97
1
CONHMe
H
H
OMe
H



98
2
CONHMe
H
H
OMe
H



99
3
CONHMe
H
H
OMe
H



100
4
CONHMe
H
H
OMe
H



101
1
SO2Me
H
H
OMe
H



102
2
SO2Me
H
H
OMe
H



103
3
SO2Me
H
H
OMe
H



104
4
SO2Me
H
H
OMe
H



105
1
SO2NH2
H
H
OMe
H



106
2
SO2NH2
H
H
OMe
H



107
3
SO2NH2
H
H
OMe
H



108
4
SO2NH2
H
H
OMe
H



109
1
H
H
H
Me
H



110
2
H
H
H
Me
H



111
3
H
H
H
Me
H



112
4
H
H
H
Me
H



113
1
Me
H
H
Me
H



114
2
Me
H
H
Me
H



115
3
Me
H
H
Me
H



116
4
Me
H
H
Me
H



117
1
CH2Ph
H
H
Me
H



118
2
CH2Ph
H
H
Me
H



119
3
CH2Ph
H
H
Me
H



120
4
CH2Ph
H
H
Me
H



121
1
COMe
H
H
Me
H



122
2
COMe
H
H
Me
H



123
3
COMe
H
H
Me
H



124
4
COMe
H
H
Me
H



125
1
CO2Me
H
H
Me
H



126
2
CO2Me
H
H
Me
H



127
3
CO2Me
H
H
Me
H



128
4
CO2Me
H
H
Me
H



129
1
CO2tBu
H
H
Me
H



130
2
CO2tBu
H
H
Me
H



131
3
CO2tBu
H
H
Me
H



132
4
CO2tBu
H
H
Me
H



133
1
CONHMe
H
H
Me
H



134
2
CONHMe
H
H
Me
H



135
3
CONHMe
H
H
Me
H



136
4
CONHMe
H
H
Me
H



137
1
SO2Me
H
H
Me
H



138
2
SO2Me
H
H
Me
H



139
3
SO2Me
H
H
Me
H



140
4
SO2Me
H
H
Me
H



141
1
SO2NH2
H
H
Me
H



142
2
SO2NH2
H
H
Me
H



143
3
SO2NH2
H
H
Me
H



144
4
SO2NH2
H
H
Me
H



145
1
H
H
H
CF3
H



146
2
H
H
H
CF3
H



147
3
H
H
H
CF3
H



148
4
H
H
H
CF3
H



149
1
Me
H
H
CF3
H



150
2
Me
H
H
CF3
H



151
3
Me
H
H
CF3
H



152
4
Me
H
H
CF3
H



153
1
CH2Ph
H
H
CF3
H



154
2
CH2Ph
H
H
CF3
H



155
3
CH2Ph
H
H
CF3
H



156
4
CH2Ph
H
H
CF3
H



157
1
COMe
H
H
CF3
H



158
2
COMe
H
H
CF3
H



159
3
COMe
H
H
CF3
H



160
4
COMe
H
H
CF3
H



161
1
CO2Me
H
H
CF3
H



162
2
CO2Me
H
H
CF3
H



163
3
CO2Me
H
H
CF3
H



164
4
CO2Me
H
H
CF3
H



165
1
CO2tBu
H
H
CF3
H



166
2
CO2tBu
H
H
CF3
H



167
3
CO2tBu
H
H
CF3
H



168
4
CO2tBu
H
H
CF3
H



169
1
CONHMe
H
H
CF3
H



170
2
CONHMe
H
H
CF3
H



171
3
CONHMe
H
H
CF3
H



172
4
CONHMe
H
H
CF3
H



173
1
SO2Me
H
H
CF3
H



174
2
SO2Me
H
H
CF3
H



175
3
SO2Me
H
H
CF3
H



176
4
SO2Me
H
H
CF3
H



177
1
SO2NH2
H
H
CF3
H



178
2
SO2NH2
H
H
CF3
H



179
3
SO2NH2
H
H
CF3
H



180
4
SO2NH2
H
H
CF3
H



181
1
H
H
H
F
H



182
2
H
H
H
F
H



183
3
H
H
H
F
H



184
4
H
H
H
F
H



185
1
Me
H
H
F
H



186
2
Me
H
H
F
H



187
3
Me
H
H
F
H



188
4
Me
H
H
F
H



189
1
CH2Ph
H
H
F
H



190
2
CH2Ph
H
H
F
H



191
3
CH2Ph
H
H
F
H



192
4
CH2Ph
H
H
F
H



193
1
COMe
H
H
F
H



194
2
COMe
H
H
F
H



195
3
COMe
H
H
F
H



196
4
COMe
H
H
F
H



197
1
CO2Me
H
H
F
H



198
2
CO2Me
H
H
F
H



199
3
CO2Me
H
H
F
H



200
4
CO2Me
H
H
F
H



201
1
CO2tBu
H
H
F
H



202
2
CO2tBu
H
H
F
H



203
3
CO2tBu
H
H
F
H



204
4
CO2tBu
H
H
F
H



205
1
CONHMe
H
H
F
H



206
2
CONHMe
H
H
F
H



207
3
CONHMe
H
H
F
H



208
4
CONHMe
H
H
F
H



209
1
SO2Me
H
H
F
H



210
2
SO2Me
H
H
F
H



211
3
SO2Me
H
H
F
H



212
4
SO2Me
H
H
F
H



213
1
SO2NH2
H
H
F
H



214
2
SO2NH2
H
H
F
H



215
3
SO2NH2
H
H
F
H



216
4
SO2NH2
H
H
F
H



217
1
H
H
H
Cl
H



218
2
H
H
H
Cl
H



219
3
H
H
H
Cl
H



220
4
H
H
H
Cl
H



221
1
Me
H
H
Cl
H



222
2
Me
H
H
Cl
H



223
3
Me
H
H
Cl
H



224
4
Me
H
H
Cl
H



225
1
CH2Ph
H
H
Cl
H



226
2
CH2Ph
H
H
Cl
H



227
3
CH2Ph
H
H
Cl
H



228
4
CH2Ph
H
H
Cl
H



229
1
COMe
H
H
Cl
H



230
2
COMe
H
H
Cl
H



231
3
COMe
H
H
Cl
H



232
4
COMe
H
H
Cl
H



233
1
CO2Me
H
H
Cl
H



234
2
CO2Me
H
H
Cl
H



235
3
CO2Me
H
H
Cl
H



236
4
CO2Me
H
H
Cl
H



237
1
CO2tBu
H
H
Cl
H



238
2
CO2tBu
H
H
Cl
H



239
3
CO2tBu
H
H
Cl
H



240
4
CO2tBu
H
H
Cl
H



241
1
CONHMe
H
H
Cl
H



242
2
CONHMe
H
H
Cl
H



243
3
CONHMe
H
H
Cl
H



244
4
CONHMe
H
H
Cl
H



245
1
SO2Me
H
H
Cl
H



246
2
SO2Me
H
H
Cl
H



247
3
SO2Me
H
H
Cl
H



248
4
SO2Me
H
H
Cl
H



249
1
SO2NH2
H
H
Cl
H



250
2
SO2NH2
H
H
Cl
H



251
3
SO2NH2
H
H
Cl
H



252
4
SO2NH2
H
H
Cl
H



253
1
H
H
H
CN
H



254
2
H
H
H
CN
H



255
3
H
H
H
CN
H



256
4
H
H
H
CN
H



257
1
Me
H
H
CN
H



258
2
Me
H
H
CN
H



259
3
Me
H
H
CN
H



260
4
Me
H
H
CN
H



261
1
CH2Ph
H
H
CN
H



262
2
CH2Ph
H
H
CN
H



263
3
CH2Ph
H
H
CN
H



264
4
CH2Ph
H
H
CN
H



265
1
COMe
H
H
CN
H



266
2
COMe
H
H
CN
H



267
3
COMe
H
H
CN
H



268
4
COMe
H
H
CN
H



269
1
CO2Me
H
H
CN
H



270
2
CO2Me
H
H
CN
H



271
3
CO2Me
H
H
CN
H



272
4
CO2Me
H
H
CN
H



273
1
CO2tBu
H
H
CN
H



274
2
CO2tBu
H
H
CN
H



275
3
CO2tBu
H
H
CN
H



276
4
CO2tBu
H
H
CN
H



277
1
CONHMe
H
H
CN
H



278
2
CONHMe
H
H
CN
H



279
3
CONHMe
H
H
CN
H



280
4
CONHMe
H
H
CN
H



281
1
SO2Me
H
H
CN
H



282
2
SO2Me
H
H
CN
H



283
3
SO2Me
H
H
CN
H



284
4
SO2Me
H
H
CN
H



285
1
SO2NH2
H
H
CN
H



286
2
SO2NH2
H
H
CN
H



287
3
SO2NH2
H
H
CN
H



288
4
SO2NH2
H
H
CN
H



289
1
H
H
H
H
OH



290
2
H
H
H
H
OH



291
3
H
H
H
H
OH



292
4
H
H
H
H
OH



293
1
Me
H
H
H
OH



294
2
Me
H
H
H
OH



295
3
Me
H
H
H
OH



296
4
Me
H
H
H
OH



297
1
CH2Ph
H
H
H
OH



298
2
CH2Ph
H
H
H
OH



299
3
CH2Ph
H
H
H
OH



300
4
CH2Ph
H
H
H
OH



301
1
COMe
H
H
H
OH



302
2
COMe
H
H
H
OH



303
3
COMe
H
H
H
OH



304
4
COMe
H
H
H
OH



305
1
CO2Me
H
H
H
OH



306
2
CO2Me
H
H
H
OH



307
3
CO2Me
H
H
H
OH



308
4
CO2Me
H
H
H
OH



309
1
CO2tBu
H
H
H
OH



310
2
CO2tBu
H
H
H
OH



311
3
CO2tBu
H
H
H
OH



312
4
CO2tBu
H
H
H
OH



313
1
CONHMe
H
H
H
OH



314
2
CONHMe
H
H
H
OH



315
3
CONHMe
H
H
H
OH



316
4
CONHMe
H
H
H
OH



317
1
SO2Me
H
H
H
OH



318
2
SO2Me
H
H
H
OH



319
3
SO2Me
H
H
H
OH



320
4
SO2Me
H
H
H
OH



321
1
SO2NH2
H
H
H
OH



322
2
SO2NH2
H
H
H
OH



323
3
SO2NH2
H
H
H
OH



324
4
SO2NH2
H
H
H
OH



325
1
H
H
H
H
OMe



326
2
H
H
H
H
OMe



327
3
H
H
H
H
OMe



328
4
H
H
H
H
OMe



329
1
Me
H
H
H
OMe



330
2
Me
H
H
H
OMe



331
3
Me
H
H
H
OMe



332
4
Me
H
H
H
OMe



333
1
CH2Ph
H
H
H
OMe



334
2
CH2Ph
H
H
H
OMe



335
3
CH2Ph
H
H
H
OMe



336
4
CH2Ph
H
H
H
OMe



337
1
COMe
H
H
H
OMe



338
2
COMe
H
H
H
OMe



339
3
COMe
H
H
H
OMe



340
4
COMe
H
H
H
OMe



341
1
CO2Me
H
H
H
OMe



342
2
CO2Me
H
H
H
OMe



343
3
CO2Me
H
H
H
OMe



344
4
CO2Me
H
H
H
OMe



345
1
CO2tBu
H
H
H
OMe



346
2
CO2tBu
H
H
H
OMe



347
3
CO2tBu
H
H
H
OMe



348
4
CO2tBu
H
H
H
OMe



349
1
CONHMe
H
H
H
OMe



350
2
CONHMe
H
H
H
OMe



351
3
CONHMe
H
H
H
OMe



352
4
CONHMe
H
H
H
OMe



353
1
SO2Me
H
H
H
OMe



354
2
SO2Me
H
H
H
OMe



355
3
SO2Me
H
H
H
OMe



356
4
SO2Me
H
H
H
OMe



357
1
SO2NH2
H
H
H
OMe



358
2
SO2NH2
H
H
H
OMe



359
3
SO2NH2
H
H
H
OMe



360
4
SO2NH2
H
H
H
OMe



361
1
H
H
H
H
Me



362
2
H
H
H
H
Me



363
3
H
H
H
H
Me



364
4
H
H
H
H
Me



365
1
Me
H
H
H
Me



366
2
Me
H
H
H
Me



367
3
Me
H
H
H
Me



368
4
Me
H
H
H
Me



369
1
CH2Ph
H
H
H
Me



370
2
CH2Ph
H
H
H
Me



371
3
CH2Ph
H
H
H
Me



372
4
CH2Ph
H
H
H
Me



373
1
COMe
H
H
H
Me



374
2
COMe
H
H
H
Me



375
3
COMe
H
H
H
Me



376
4
COMe
H
H
H
Me



377
1
CO2Me
H
H
H
Me



378
2
CO2Me
H
H
H
Me



379
3
CO2Me
H
H
H
Me



380
4
CO2Me
H
H
H
Me



381
1
CO2tBu
H
H
H
Me



382
2
CO2tBu
H
H
H
Me



383
3
CO2tBu
H
H
H
Me



384
4
CO2tBu
H
H
H
Me



385
1
CONHMe
H
H
H
Me



386
2
CONHMe
H
H
H
Me



387
3
CONHMe
H
H
H
Me



388
4
CONHMe
H
H
H
Me



389
1
SO2Me
H
H
H
Me



390
2
SO2Me
H
H
H
Me



391
3
SO2Me
H
H
H
Me



392
4
SO2Me
H
H
H
Me



393
1
SO2NH2
H
H
H
Me



394
2
SO2NH2
H
H
H
Me



395
3
SO2NH2
H
H
H
Me



396
4
SO2NH2
H
H
H
Me



397
1
H
H
H
H
CF3



398
2
H
H
H
H
CF3



399
3
H
H
H
H
CF3



400
4
H
H
H
H
CF3



401
1
Me
H
H
H
CF3



402
2
Me
H
H
H
CF3



403
3
Me
H
H
H
CF3



404
4
Me
H
H
H
CF3



405
1
CH2Ph
H
H
H
CF3



406
2
CH2Ph
H
H
H
CF3



407
3
CH2Ph
H
H
H
CF3



408
4
CH2Ph
H
H
H
CF3



409
1
COMe
H
H
H
CF3



410
2
COMe
H
H
H
CF3



411
3
COMe
H
H
H
CF3



412
4
COMe
H
H
H
CF3



413
1
CO2Me
H
H
H
CF3



414
2
CO2Me
H
H
H
CF3



415
3
CO2Me
H
H
H
CF3



416
4
CO2Me
H
H
H
CF3



417
1
CO2tBu
H
H
H
CF3



418
2
CO2tBu
H
H
H
CF3



419
3
CO2tBu
H
H
H
CF3



420
4
CO2tBu
H
H
H
CF3



421
1
CONHMe
H
H
H
CF3



422
2
CONHMe
H
H
H
CF3



423
3
CONHMe
H
H
H
CF3



424
4
CONHMe
H
H
H
CF3



425
1
SO2Me
H
H
H
CF3



426
2
SO2Me
H
H
H
CF3



427
3
SO2Me
H
H
H
CF3



428
4
SO2Me
H
H
H
CF3



429
1
SO2NH2
H
H
H
CF3



430
2
SO2NH2
H
H
H
CF3



431
3
SO2NH2
H
H
H
CF3



432
4
SO2NH2
H
H
H
CF3



433
1
H
H
H
H
F



434
2
H
H
H
H
F



435
3
H
H
H
H
F



436
3
H
H
H
H
F



437
1
Me
H
H
H
F



438
2
Me
H
H
H
F



439
3
Me
H
H
H
F



440
4
Me
H
H
H
F



441
1
CH2Ph
H
H
H
F



442
2
CH2Ph
H
H
H
F



443
3
CH2Ph
H
H
H
F



444
4
CH2Ph
H
H
H
F



445
1
COMe
H
H
H
F



446
2
COMe
H
H
H
F



447
3
COMe
H
H
H
F



448
4
COMe
H
H
H
F



449
1
CO2Me
H
H
H
F



450
2
CO2Me
H
H
H
F



451
3
CO2Me
H
H
H
F



452
4
CO2Me
H
H
H
F



453
1
CO2tBu
H
H
H
F



454
2
CO2tBu
H
H
H
F



455
3
CO2tBu
H
H
H
F



456
4
CO2tBu
H
H
H
F



457
1
CONHMe
H
H
H
F



458
2
CONHMe
H
H
H
F



459
3
CONHMe
H
H
H
F



460
4
CONHMe
H
H
H
F



461
1
SO2Me
H
H
H
F



462
2
SO2Me
H
H
H
F



463
3
SO2Me
H
H
H
F



464
4
SO2Me
H
H
H
F



465
1
SO2NH2
H
H
H
F



466
2
SO2NH2
H
H
H
F



467
3
SO2NH2
H
H
H
F



468
4
SO2NH2
H
H
H
F



469
1
H
H
H
H
Cl



470
2
H
H
H
H
Cl



471
3
H
H
H
H
Cl



472
4
H
H
H
H
Cl



473
1
Me
H
H
H
Cl



474
2
Me
H
H
H
Cl



475
3
Me
H
H
H
Cl



476
4
Me
H
H
H
Cl



477
1
CH2Ph
H
H
H
Cl



478
2
CH2Ph
H
H
H
Cl



479
3
CH2Ph
H
H
H
Cl



480
4
CH2Ph
H
H
H
Cl



481
1
COMe
H
H
H
Cl



482
2
COMe
H
H
H
Cl



483
3
COMe
H
H
H
Cl



484
4
COMe
H
H
H
Cl



485
1
CO2Me
H
H
H
Cl



486
2
CO2Me
H
H
H
Cl



487
3
CO2Me
H
H
H
Cl



488
4
CO2Me
H
H
H
Cl



489
1
CO2tBu
H
H
H
Cl



490
2
CO2tBu
H
H
H
Cl



491
3
CO2tBu
H
H
H
Cl



492
4
CO2tBu
H
H
H
Cl



493
1
CONHMe
H
H
H
Cl



494
2
CONHMe
H
H
H
Cl



495
3
CONHMe
H
H
H
Cl



496
4
CONHMe
H
H
H
Cl



497
1
SO2Me
H
H
H
Cl



498
2
SO2Me
H
H
H
Cl



499
3
SO2Me
H
H
H
Cl



500
4
SO2Me
H
H
H
Cl



501
1
SO2NH2
H
H
H
Cl



502
2
SO2NH2
H
H
H
Cl



503
3
SO2NH2
H
H
H
Cl



504
4
SO2NH2
H
H
H
Cl



505
1
H
H
H
H
CN



506
2
H
H
H
H
CN



507
3
H
H
H
H
CN



508
4
H
H
H
H
CN



509
1
Me
H
H
H
CN



510
2
Me
H
H
H
CN



511
3
Me
H
H
H
CN



512
4
Me
H
H
H
CN



513
1
CH2Ph
H
H
H
CN



514
2
CH2Ph
H
H
H
CN



515
3
CH2Ph
H
H
H
CN



516
4
CH2Ph
H
H
H
CN



517
1
COMe
H
H
H
CN



518
2
COMe
H
H
H
CN



519
3
COMe
H
H
H
CN



520
4
COMe
H
H
H
CN



521
1
CO2Me
H
H
H
CN



522
2
CO2Me
H
H
H
CN



523
3
CO2Me
H
H
H
CN



524
4
CO2Me
H
H
H
CN



525
1
CO2tBu
H
H
H
CN



526
2
CO2tBu
H
H
H
CN



527
3
CO2tBu
H
H
H
CN



528
4
CO2tBu
H
H
H
CN



529
1
CONHMe
H
H
H
CN



530
2
CONHMe
H
H
H
CN



531
3
CONHMe
H
H
H
CN



532
4
CONHMe
H
H
H
CN



533
1
SO2Me
H
H
H
CN



534
2
SO2Me
H
H
H
CN



535
3
SO2Me
H
H
H
CN



536
4
SO2Me
H
H
H
CN



537
1
SO2NH2
H
H
H
CN



538
2
SO2NH2
H
H
H
CN



539
3
SO2NH2
H
H
H
CN



540
4
SO2NH2
H
H
H
CN










Exemplary embodiments include compounds having the formula (XXXII)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 26.

















TABLE26







Entry
n
R7
R20a
R20b
R20d
R20e
























1
1
H
H
H
H
H



2
2
H
H
H
H
H



3
3
H
H
H
H
H



4
4
H
H
H
H
H



5
1
Me
H
H
H
H



6
2
Me
H
H
H
H



7
3
Me
H
H
H
H



8
4
Me
H
H
H
H



9
1
CH2Ph
H
H
H
H



10
2
CH2Ph
H
H
H
H



11
3
CH2Ph
H
H
H
H



12
4
CH2Ph
H
H
H
H



13
1
COMe
H
H
H
H



14
2
COMe
H
H
H
H



15
3
COMe
H
H
H
H



16
4
COMe
H
H
H
H



17
1
CO2Me
H
H
H
H



18
2
CO2Me
H
H
H
H



19
3
CO2Me
H
H
H
H



20
4
CO2Me
H
H
H
H



21
1
CO2tBu
H
H
H
H



22
2
CO2tBu
H
H
H
H



23
3
CO2tBu
H
H
H
H



24
4
CO2tBu
H
H
H
H



25
1
CONHMe
H
H
H
H



26
2
CONHMe
H
H
H
H



27
3
CONHMe
H
H
H
H



28
4
CONHMe
H
H
H
H



29
1
SO2Me
H
H
H
H



30
2
SO2Me
H
H
H
H



31
3
SO2Me
H
H
H
H



32
4
SO2Me
H
H
H
H



33
1
SO2NH2
H
H
H
H



34
2
SO2NH2
H
H
H
H



35
3
SO2NH2
H
H
H
H



36
4
SO2NH2
H
H
H
H



37
1
H
H
H
OH
H



38
2
H
H
H
OH
H



39
3
H
H
H
OH
H



40
4
H
H
H
OH
H



41
1
Me
H
H
OH
H



42
2
Me
H
H
OH
H



43
3
Me
H
H
OH
H



44
4
Me
H
H
OH
H



45
1
CH2Ph
H
H
OH
H



46
2
CH2Ph
H
H
OH
H



47
3
CH2Ph
H
H
OH
H



48
4
CH2Ph
H
H
OH
H



49
1
COMe
H
H
OH
H



50
2
COMe
H
H
OH
H



51
3
COMe
H
H
OH
H



52
4
COMe
H
H
OH
H



53
1
CO2Me
H
H
OH
H



54
2
CO2Me
H
H
OH
H



55
3
CO2Me
H
H
OH
H



56
4
CO2Me
H
H
OH
H



57
1
CO2tBu
H
H
OH
H



58
2
CO2tBu
H
H
OH
H



59
3
CO2tBu
H
H
OH
H



60
4
CO2tBu
H
H
OH
H



61
1
CONHMe
H
H
OH
H



62
2
CONHMe
H
H
OH
H



63
3
CONHMe
H
H
OH
H



64
4
CONHMe
H
H
OH
H



65
1
SO2Me
H
H
OH
H



66
2
SO2Me
H
H
OH
H



67
3
SO2Me
H
H
OH
H



68
4
SO2Me
H
H
OH
H



69
1
SO2NH2
H
H
OH
H



70
2
SO2NH2
H
H
OH
H



71
3
SO2NH2
H
H
OH
H



72
4
SO2NH2
H
H
OH
H



73
1
H
H
H
OMe
H



74
2
H
H
H
OMe
H



75
3
H
H
H
OMe
H



76
4
H
H
H
OMe
H



77
1
Me
H
H
OMe
H



78
2
Me
H
H
OMe
H



79
3
Me
H
H
OMe
H



80
4
Me
H
H
OMe
H



81
1
CH2Ph
H
H
OMe
H



82
2
CH2Ph
H
H
OMe
H



83
3
CH2Ph
H
H
OMe
H



84
4
CH2Ph
H
H
OMe
H



85
1
COMe
H
H
OMe
H



86
2
COMe
H
H
OMe
H



87
3
COMe
H
H
OMe
H



88
4
COMe
H
H
OMe
H



89
1
CO2Me
H
H
OMe
H



90
2
CO2Me
H
H
OMe
H



91
3
CO2Me
H
H
OMe
H



92
4
CO2Me
H
H
OMe
H



93
1
CO2tBu
H
H
OMe
H



94
2
CO2tBu
H
H
OMe
H



95
3
CO2tBu
H
H
OMe
H



96
1
CO2tBu
H
H
OMe
H



97
1
CONHMe
H
H
OMe
H



98
2
CONHMe
H
H
OMe
H



99
3
CONHMe
H
H
OMe
H



100
4
CONHMe
H
H
OMe
H



101
1
SO2Me
H
H
OMe
H



102
2
SO2Me
H
H
OMe
H



103
3
SO2Me
H
H
OMe
H



104
4
SO2Me
H
H
OMe
H



105
1
SO2NH2
H
H
OMe
H



106
2
SO2NH2
H
H
OMe
H



107
3
SO2NH2
H
H
OMe
H



108
4
SO2NH2
H
H
OMe
H



109
1
H
H
H
Me
H



110
2
H
H
H
Me
H



111
3
H
H
H
Me
H



112
4
H
H
H
Me
H



113
1
Me
H
H
Me
H



114
2
Me
H
H
Me
H



115
3
Me
H
H
Me
H



116
4
Me
H
H
Me
H



117
1
CH2Ph
H
H
Me
H



118
2
CH2Ph
H
H
Me
H



119
3
CH2Ph
H
H
Me
H



120
4
CH2Ph
H
H
Me
H



121
1
COMe
H
H
Me
H



122
2
COMe
H
H
Me
H



123
3
COMe
H
H
Me
H



124
4
COMe
H
H
Me
H



125
1
CO2Me
H
H
Me
H



126
2
CO2Me
H
H
Me
H



127
3
CO2Me
H
H
Me
H



128
4
CO2Me
H
H
Me
H



129
1
CO2tBu
H
H
Me
H



130
2
CO2tBu
H
H
Me
H



131
3
CO2tBu
H
H
Me
H



132
4
CO2tBu
H
H
Me
H



133
1
CONHMe
H
H
Me
H



134
2
CONHMe
H
H
Me
H



135
3
CONHMe
H
H
Me
H



136
4
CONHMe
H
H
Me
H



137
1
SO2Me
H
H
Me
H



138
2
SO2Me
H
H
Me
H



139
3
SO2Me
H
H
Me
H



140
4
SO2Me
H
H
Me
H



141
1
SO2NH2
H
H
Me
H



142
2
SO2NH2
H
H
Me
H



143
3
SO2NH2
H
H
Me
H



144
4
SO2NH2
H
H
Me
H



145
1
H
H
H
CF3
H



146
2
H
H
H
CF3
H



147
3
H
H
H
CF3
H



148
4
H
H
H
CF3
H



149
1
Me
H
H
CF3
H



150
2
Me
H
H
CF3
H



151
3
Me
H
H
CF3
H



152
4
Me
H
H
CF3
H



153
1
CH2Ph
H
H
CF3
H



154
2
CH2Ph
H
H
CF3
H



155
3
CH2Ph
H
H
CF3
H



156
4
CH2Ph
H
H
CF3
H



157
1
COMe
H
H
CF3
H



158
2
COMe
H
H
CF3
H



159
3
COMe
H
H
CF3
H



160
4
COMe
H
H
CF3
H



161
1
CO2Me
H
H
CF3
H



162
2
CO2Me
H
H
CF3
H



163
3
CO2Me
H
H
CF3
H



164
4
CO2Me
H
H
CF3
H



165
1
CO2tBu
H
H
CF3
H



166
2
CO2tBu
H
H
CF3
H



167
3
CO2tBu
H
H
CF3
H



168
4
CO2tBu
H
H
CF3
H



169
1
CONHMe
H
H
CF3
H



170
2
CONHMe
H
H
CF3
H



171
3
CONHMe
H
H
CF3
H



172
4
CONHMe
H
H
CF3
H



173
1
SO2Me
H
H
CF3
H



174
2
SO2Me
H
H
CF3
H



175
3
SO2Me
H
H
CF3
H



176
4
SO2Me
H
H
CF3
H



177
1
SO2NH2
H
H
CF3
H



178
2
SO2NH2
H
H
CF3
H



179
3
SO2NH2
H
H
CF3
H



180
4
SO2NH2
H
H
CF3
H



181
1
H
H
H
F
H



182
2
H
H
H
F
H



183
3
H
H
H
F
H



184
4
H
H
H
F
H



185
1
Me
H
H
F
H



186
2
Me
H
H
F
H



187
3
Me
H
H
F
H



188
4
Me
H
H
F
H



189
1
CH2Ph
H
H
F
H



190
2
CH2Ph
H
H
F
H



191
3
CH2Ph
H
H
F
H



192
4
CH2Ph
H
H
F
H



193
1
COMe
H
H
F
H



194
2
COMe
H
H
F
H



195
3
COMe
H
H
F
H



196
4
COMe
H
H
F
H



197
1
CO2Me
H
H
F
H



198
2
CO2Me
H
H
F
H



199
3
CO2Me
H
H
F
H



200
4
CO2Me
H
H
F
H



201
1
CO2tBu
H
H
F
H



202
2
CO2tBu
H
H
F
H



203
3
CO2tBu
H
H
F
H



204
4
CO2tBu
H
H
F
H



205
1
CONHMe
H
H
F
H



206
2
CONHMe
H
H
F
H



207
3
CONHMe
H
H
F
H



208
4
CONHMe
H
H
F
H



209
1
SO2Me
H
H
F
H



210
2
SO2Me
H
H
F
H



211
3
SO2Me
H
H
F
H



212
4
SO2Me
H
H
F
H



213
1
SO2NH2
H
H
F
H



214
2
SO2NH2
H
H
F
H



215
3
SO2NH2
H
H
F
H



216
4
SO2NH2
H
H
F
H



217
1
H
H
H
Cl
H



218
2
H
H
H
Cl
H



219
3
H
H
H
Cl
H



220
4
H
H
H
Cl
H



221
1
Me
H
H
Cl
H



222
2
Me
H
H
Cl
H



223
3
Me
H
H
Cl
H



224
4
Me
H
H
Cl
H



225
1
CH2Ph
H
H
Cl
H



226
2
CH2Ph
H
H
Cl
H



227
3
CH2Ph
H
H
Cl
H



228
4
CH2Ph
H
H
Cl
H



229
1
COMe
H
H
Cl
H



230
2
COMe
H
H
Cl
H



231
3
COMe
H
H
Cl
H



232
4
COMe
H
H
Cl
H



233
1
CO2Me
H
H
Cl
H



234
2
CO2Me
H
H
Cl
H



235
3
CO2Me
H
H
Cl
H



236
4
CO2Me
H
H
Cl
H



237
1
CO2tBu
H
H
Cl
H



238
2
CO2tBu
H
H
Cl
H



239
3
CO2tBu
H
H
Cl
H



240
4
CO2tBu
H
H
Cl
H



241
1
CONHMe
H
H
Cl
H



242
2
CONHMe
H
H
Cl
H



243
3
CONHMe
H
H
Cl
H



244
4
CONHMe
H
H
Cl
H



245
1
SO2Me
H
H
Cl
H



246
2
SO2Me
H
H
Cl
H



247
3
SO2Me
H
H
Cl
H



248
4
SO2Me
H
H
Cl
H



249
1
SO2NH2
H
H
Cl
H



250
2
SO2NH2
H
H
Cl
H



251
3
SO2NH2
H
H
Cl
H



252
4
SO2NH2
H
H
Cl
H



253
1
H
H
H
CN
H



254
2
H
H
H
CN
H



255
3
H
H
H
CN
H



256
4
H
H
H
CN
H



257
1
Me
H
H
CN
H



258
2
Me
H
H
CN
H



259
3
Me
H
H
CN
H



260
4
Me
H
H
CN
H



261
1
CH2Ph
H
H
CN
H



262
2
CH2Ph
H
H
CN
H



263
3
CH2Ph
H
H
CN
H



264
4
CH2Ph
H
H
CN
H



265
1
COMe
H
H
CN
H



266
2
COMe
H
H
CN
H



267
3
COMe
H
H
CN
H



268
4
COMe
H
H
CN
H



269
1
CO2Me
H
H
CN
H



270
2
CO2Me
H
H
CN
H



271
3
CO2Me
H
H
CN
H



272
4
CO2Me
H
H
CN
H



273
1
CO2tBu
H
H
CN
H



274
2
CO2tBu
H
H
CN
H



275
3
CO2tBu
H
H
CN
H



276
4
CO2tBu
H
H
CN
H



277
1
CONHMe
H
H
CN
H



278
2
CONHMe
H
H
CN
H



279
3
CONHMe
H
H
CN
H



280
4
CONHMe
H
H
CN
H



281
1
SO2Me
H
H
CN
H



282
2
SO2Me
H
H
CN
H



283
3
SO2Me
H
H
CN
H



284
4
SO2Me
H
H
CN
H



285
1
SO2NH2
H
H
CN
H



286
2
SO2NH2
H
H
CN
H



287
3
SO2NH2
H
H
CN
H



288
4
SO2NH2
H
H
CN
H



289
1
H
H
H
H
OH



290
2
H
H
H
H
OH



291
3
H
H
H
H
OH



292
4
H
H
H
H
OH



293
1
Me
H
H
H
OH



294
2
Me
H
H
H
OH



295
3
Me
H
H
H
OH



296
4
Me
H
H
H
OH



297
1
CH2Ph
H
H
H
OH



298
2
CH2Ph
H
H
H
OH



299
3
CH2Ph
H
H
H
OH



300
4
CH2Ph
H
H
H
OH



301
1
COMe
H
H
H
OH



302
2
COMe
H
H
H
OH



303
3
COMe
H
H
H
OH



304
4
COMe
H
H
H
OH



305
1
CO2Me
H
H
H
OH



306
2
CO2Me
H
H
H
OH



307
3
CO2Me
H
H
H
OH



308
4
CO2Me
H
H
H
OH



309
1
CO2tBu
H
H
H
OH



310
2
CO2tBu
H
H
H
OH



311
3
CO2tBu
H
H
H
OH



312
4
CO2tBu
H
H
H
OH



313
1
CONHMe
H
H
H
OH



314
2
CONHMe
H
H
H
OH



315
3
CONHMe
H
H
H
OH



316
4
CONHMe
H
H
H
OH



317
1
SO2Me
H
H
H
OH



318
2
SO2Me
H
H
H
OH



319
3
SO2Me
H
H
H
OH



320
4
SO2Me
H
H
H
OH



321
1
SO2NH2
H
H
H
OH



322
2
SO2NH2
H
H
H
OH



323
3
SO2NH2
H
H
H
OH



324
4
SO2NH2
H
H
H
OH



325
1
H
H
H
H
OMe



326
2
H
H
H
H
OMe



327
3
H
H
H
H
OMe



328
4
H
H
H
H
OMe



329
1
Me
H
H
H
OMe



330
2
Me
H
H
H
OMe



331
3
Me
H
H
H
OMe



332
4
Me
H
H
H
OMe



333
1
CH2Ph
H
H
H
OMe



334
2
CH2Ph
H
H
H
OMe



335
3
CH2Ph
H
H
H
OMe



336
4
CH2Ph
H
H
H
OMe



337
1
COMe
H
H
H
OMe



338
2
COMe
H
H
H
OMe



339
3
COMe
H
H
H
OMe



340
4
COMe
H
H
H
OMe



341
1
CO2Me
H
H
H
OMe



342
2
CO2Me
H
H
H
OMe



343
3
CO2Me
H
H
H
OMe



344
4
CO2Me
H
H
H
OMe



345
1
CO2tBu
H
H
H
OMe



346
2
CO2tBu
H
H
H
OMe



347
3
CO2tBu
H
H
H
OMe



348
4
CO2tBu
H
H
H
OMe



349
1
CONHMe
H
H
H
OMe



350
2
CONHMe
H
H
H
OMe



351
3
CONHMe
H
H
H
OMe



352
4
CONHMe
H
H
H
OMe



353
1
SO2Me
H
H
H
OMe



354
2
SO2Me
H
H
H
OMe



355
3
SO2Me
H
H
H
OMe



356
4
SO2Me
H
H
H
OMe



357
1
SO2NH2
H
H
H
OMe



358
2
SO2NH2
H
H
H
OMe



359
3
SO2NH2
H
H
H
OMe



360
4
SO2NH2
H
H
H
OMe



361
1
H
H
H
H
Me



362
2
H
H
H
H
Me



363
3
H
H
H
H
Me



364
4
H
H
H
H
Me



365
1
Me
H
H
H
Me



366
2
Me
H
H
H
Me



367
3
Me
H
H
H
Me



368
4
Me
H
H
H
Me



369
1
CH2Ph
H
H
H
Me



370
2
CH2Ph
H
H
H
Me



371
3
CH2Ph
H
H
H
Me



372
4
CH2Ph
H
H
H
Me



373
1
COMe
H
H
H
Me



374
2
COMe
H
H
H
Me



375
3
COMe
H
H
H
Me



376
4
COMe
H
H
H
Me



377
1
CO2Me
H
H
H
Me



378
2
CO2Me
H
H
H
Me



379
3
CO2Me
H
H
H
Me



380
4
CO2Me
H
H
H
Me



381
1
CO2tBu
H
H
H
Me



382
2
CO2tBu
H
H
H
Me



383
3
CO2tBu
H
H
H
Me



384
4
CO2tBu
H
H
H
Me



385
1
CONHMe
H
H
H
Me



386
2
CONHMe
H
H
H
Me



387
3
CONHMe
H
H
H
Me



388
4
CONHMe
H
H
H
Me



389
1
SO2Me
H
H
H
Me



390
2
SO2Me
H
H
H
Me



391
3
SO2Me
H
H
H
Me



392
4
SO2Me
H
H
H
Me



393
1
SO2NH2
H
H
H
Me



394
2
SO2NH2
H
H
H
Me



395
3
SO2NH2
H
H
H
Me



396
4
SO2NH2
H
H
H
Me



397
1
H
H
H
H
CF3



398
2
H
H
H
H
CF3



399
3
H
H
H
H
CF3



400
4
H
H
H
H
CF3



401
1
Me
H
H
H
CF3



402
2
Me
H
H
H
CF3



403
3
Me
H
H
H
CF3



404
4
Me
H
H
H
CF3



405
1
CH2Ph
H
H
H
CF3



406
2
CH2Ph
H
H
H
CF3



407
3
CH2Ph
H
H
H
CF3



408
4
CH2Ph
H
H
H
CF3



409
1
COMe
H
H
H
CF3



410
2
COMe
H
H
H
CF3



411
3
COMe
H
H
H
CF3



412
4
COMe
H
H
H
CF3



413
1
CO2Me
H
H
H
CF3



414
2
CO2Me
H
H
H
CF3



415
3
CO2Me
H
H
H
CF3



416
4
CO2Me
H
H
H
CF3



417
1
CO2tBu
H
H
H
CF3



418
2
CO2tBu
H
H
H
CF3



419
3
CO2tBu
H
H
H
CF3



420
4
CO2tBu
H
H
H
CF3



421
1
CONHMe
H
H
H
CF3



422
2
CONHMe
H
H
H
CF3



423
3
CONHMe
H
H
H
CF3



424
4
CONHMe
H
H
H
CF3



425
1
SO2Me
H
H
H
CF3



426
2
SO2Me
H
H
H
CF3



427
3
SO2Me
H
H
H
CF3



428
4
SO2Me
H
H
H
CF3



429
1
SO2NH2
H
H
H
CF3



430
2
SO2NH2
H
H
H
CF3



431
3
SO2NH2
H
H
H
CF3



432
4
SO2NH2
H
H
H
CF3



433
1
H
H
H
H
F



434
2
H
H
H
H
F



435
3
H
H
H
H
F



436
3
H
H
H
H
F



437
1
Me
H
H
H
F



438
2
Me
H
H
H
F



439
3
Me
H
H
H
F



440
4
Me
H
H
H
F



441
1
CH2Ph
H
H
H
F



442
2
CH2Ph
H
H
H
F



443
3
CH2Ph
H
H
H
F



444
4
CH2Ph
H
H
H
F



445
1
COMe
H
H
H
F



446
2
COMe
H
H
H
F



447
3
COMe
H
H
H
F



448
4
COMe
H
H
H
F



449
1
CO2Me
H
H
H
F



450
2
CO2Me
H
H
H
F



451
3
CO2Me
H
H
H
F



452
4
CO2Me
H
H
H
F



453
1
CO2tBu
H
H
H
F



454
2
CO2tBu
H
H
H
F



455
3
CO2tBu
H
H
H
F



456
4
CO2tBu
H
H
H
F



457
1
CONHMe
H
H
H
F



458
2
CONHMe
H
H
H
F



459
3
CONHMe
H
H
H
F



460
4
CONHMe
H
H
H
F



461
1
SO2Me
H
H
H
F



462
2
SO2Me
H
H
H
F



463
3
SO2Me
H
H
H
F



464
4
SO2Me
H
H
H
F



465
1
SO2NH2
H
H
H
F



466
2
SO2NH2
H
H
H
F



467
3
SO2NH2
H
H
H
F



468
4
SO2NH2
H
H
H
F



469
1
H
H
H
H
Cl



470
2
H
H
H
H
Cl



471
3
H
H
H
H
Cl



472
4
H
H
H
H
Cl



473
1
Me
H
H
H
Cl



474
2
Me
H
H
H
Cl



475
3
Me
H
H
H
Cl



476
4
Me
H
H
H
Cl



477
1
CH2Ph
H
H
H
Cl



478
2
CH2Ph
H
H
H
Cl



479
3
CH2Ph
H
H
H
Cl



480
4
CH2Ph
H
H
H
Cl



481
1
COMe
H
H
H
Cl



482
2
COMe
H
H
H
Cl



483
3
COMe
H
H
H
Cl



484
4
COMe
H
H
H
Cl



485
1
CO2Me
H
H
H
Cl



486
2
CO2Me
H
H
H
Cl



487
3
CO2Me
H
H
H
Cl



488
4
CO2Me
H
H
H
Cl



489
1
CO2tBu
H
H
H
Cl



490
2
CO2tBu
H
H
H
Cl



491
3
CO2tBu
H
H
H
Cl



492
4
CO2tBu
H
H
H
Cl



493
1
CONHMe
H
H
H
Cl



494
2
CONHMe
H
H
H
Cl



495
3
CONHMe
H
H
H
Cl



496
4
CONHMe
H
H
H
Cl



497
1
SO2Me
H
H
H
Cl



498
2
SO2Me
H
H
H
Cl



499
3
SO2Me
H
H
H
Cl



500
4
SO2Me
H
H
H
Cl



501
1
SO2NH2
H
H
H
Cl



502
2
SO2NH2
H
H
H
Cl



503
3
SO2NH2
H
H
H
Cl



504
4
SO2NH2
H
H
H
Cl



505
1
H
H
H
H
CN



506
2
H
H
H
H
CN



507
3
H
H
H
H
CN



508
4
H
H
H
H
CN



509
1
Me
H
H
H
CN



510
2
Me
H
H
H
CN



511
3
Me
H
H
H
CN



512
4
Me
H
H
H
CN



513
1
CH2Ph
H
H
H
CN



514
2
CH2Ph
H
H
H
CN



515
3
CH2Ph
H
H
H
CN



516
4
CH2Ph
H
H
H
CN



517
1
COMe
H
H
H
CN



518
2
COMe
H
H
H
CN



519
3
COMe
H
H
H
CN



520
4
COMe
H
H
H
CN



521
1
CO2Me
H
H
H
CN



522
2
CO2Me
H
H
H
CN



523
3
CO2Me
H
H
H
CN



524
4
CO2Me
H
H
H
CN



525
1
CO2tBu
H
H
H
CN



526
2
CO2tBu
H
H
H
CN



527
3
CO2tBu
H
H
H
CN



528
4
CO2tBu
H
H
H
CN



529
1
CONHMe
H
H
H
CN



530
2
CONHMe
H
H
H
CN



531
3
CONHMe
H
H
H
CN



532
4
CONHMe
H
H
H
CN



533
1
SO2Me
H
H
H
CN



534
2
SO2Me
H
H
H
CN



535
3
SO2Me
H
H
H
CN



536
4
SO2Me
H
H
H
CN



537
1
SO2NH2
H
H
H
CN



538
2
SO2NH2
H
H
H
CN



539
3
SO2NH2
H
H
H
CN



540
4
SO2NH2
H
H
H
CN










Exemplary embodiments include compounds having the formula (XXXIV)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 27.

















TABLE27







Entry
n
R7
R20a
R20b
R20d
R20e
























1
1
H
H
H
H
H



2
2
H
H
H
H
H



3
3
H
H
H
H
H



4
4
H
H
H
H
H



5
1
Me
H
H
H
H



6
2
Me
H
H
H
H



7
3
Me
H
H
H
H



8
4
Me
H
H
H
H



9
1
CH2Ph
H
H
H
H



10
2
CH2Ph
H
H
H
H



11
3
CH2Ph
H
H
H
H



12
4
CH2Ph
H
H
H
H



13
1
COMe
H
H
H
H



14
2
COMe
H
H
H
H



15
3
COMe
H
H
H
H



16
4
COMe
H
H
H
H



17
1
CO2Me
H
H
H
H



18
2
CO2Me
H
H
H
H



19
3
CO2Me
H
H
H
H



20
4
CO2Me
H
H
H
H



21
1
CO2tBu
H
H
H
H



22
2
CO2tBu
H
H
H
H



23
3
CO2tBu
H
H
H
H



24
4
CO2tBu
H
H
H
H



25
1
CONHMe
H
H
H
H



26
2
CONHMe
H
H
H
H



27
3
CONHMe
H
H
H
H



28
4
CONHMe
H
H
H
H



29
1
SO2Me
H
H
H
H



30
2
SO2Me
H
H
H
H



31
3
SO2Me
H
H
H
H



32
4
SO2Me
H
H
H
H



33
1
SO2NH2
H
H
H
H



34
2
SO2NH2
H
H
H
H



35
3
SO2NH2
H
H
H
H



36
4
SO2NH2
H
H
H
H



37
1
H
H
H
OH
H



38
2
H
H
H
OH
H



39
3
H
H
H
OH
H



40
4
H
H
H
OH
H



41
1
Me
H
H
OH
H



42
2
Me
H
H
OH
H



43
3
Me
H
H
OH
H



44
4
Me
H
H
OH
H



45
1
CH2Ph
H
H
OH
H



46
2
CH2Ph
H
H
OH
H



47
3
CH2Ph
H
H
OH
H



48
4
CH2Ph
H
H
OH
H



49
1
COMe
H
H
OH
H



50
2
COMe
H
H
OH
H



51
3
COMe
H
H
OH
H



52
4
COMe
H
H
OH
H



53
1
CO2Me
H
H
OH
H



54
2
CO2Me
H
H
OH
H



55
3
CO2Me
H
H
OH
H



56
4
CO2Me
H
H
OH
H



57
1
CO2tBu
H
H
OH
H



58
2
CO2tBu
H
H
OH
H



59
3
CO2tBu
H
H
OH
H



60
4
CO2tBu
H
H
OH
H



61
1
CONHMe
H
H
OH
H



62
2
CONHMe
H
H
OH
H



63
3
CONHMe
H
H
OH
H



64
4
CONHMe
H
H
OH
H



65
1
SO2Me
H
H
OH
H



66
2
SO2Me
H
H
OH
H



67
3
SO2Me
H
H
OH
H



68
4
SO2Me
H
H
OH
H



69
1
SO2NH2
H
H
OH
H



70
2
SO2NH2
H
H
OH
H



71
3
SO2NH2
H
H
OH
H



72
4
SO2NH2
H
H
OH
H



73
1
H
H
H
OMe
H



74
2
H
H
H
OMe
H



75
3
H
H
H
OMe
H



76
4
H
H
H
OMe
H



77
1
Me
H
H
OMe
H



78
2
Me
H
H
OMe
H



79
3
Me
H
H
OMe
H



80
4
Me
H
H
OMe
H



81
1
CH2Ph
H
H
OMe
H



82
2
CH2Ph
H
H
OMe
H



83
3
CH2Ph
H
H
OMe
H



84
4
CH2Ph
H
H
OMe
H



85
1
COMe
H
H
OMe
H



86
2
COMe
H
H
OMe
H



87
3
COMe
H
H
OMe
H



88
4
COMe
H
H
OMe
H



89
1
CO2Me
H
H
OMe
H



90
2
CO2Me
H
H
OMe
H



91
3
CO2Me
H
H
OMe
H



92
4
CO2Me
H
H
OMe
H



93
1
CO2tBu
H
H
OMe
H



94
2
CO2tBu
H
H
OMe
H



95
3
CO2tBu
H
H
OMe
H



96
1
CO2tBu
H
H
OMe
H



97
1
CONHMe
H
H
OMe
H



98
2
CONHMe
H
H
OMe
H



99
3
CONHMe
H
H
OMe
H



100
4
CONHMe
H
H
OMe
H



101
1
SO2Me
H
H
OMe
H



102
2
SO2Me
H
H
OMe
H



103
3
SO2Me
H
H
OMe
H



104
4
SO2Me
H
H
OMe
H



105
1
SO2NH2
H
H
OMe
H



106
2
SO2NH2
H
H
OMe
H



107
3
SO2NH2
H
H
OMe
H



108
4
SO2NH2
H
H
OMe
H



109
1
H
H
H
Me
H



110
2
H
H
H
Me
H



111
3
H
H
H
Me
H



112
4
H
H
H
Me
H



113
1
Me
H
H
Me
H



114
2
Me
H
H
Me
H



115
3
Me
H
H
Me
H



116
4
Me
H
H
Me
H



117
1
CH2Ph
H
H
Me
H



118
2
CH2Ph
H
H
Me
H



119
3
CH2Ph
H
H
Me
H



120
4
CH2Ph
H
H
Me
H



121
1
COMe
H
H
Me
H



122
2
COMe
H
H
Me
H



123
3
COMe
H
H
Me
H



124
4
COMe
H
H
Me
H



125
1
CO2Me
H
H
Me
H



126
2
CO2Me
H
H
Me
H



127
3
CO2Me
H
H
Me
H



128
4
CO2Me
H
H
Me
H



129
1
CO2tBu
H
H
Me
H



130
2
CO2tBu
H
H
Me
H



131
3
CO2tBu
H
H
Me
H



132
4
CO2tBu
H
H
Me
H



133
1
CONHMe
H
H
Me
H



134
2
CONHMe
H
H
Me
H



135
3
CONHMe
H
H
Me
H



136
4
CONHMe
H
H
Me
H



137
1
SO2Me
H
H
Me
H



138
2
SO2Me
H
H
Me
H



139
3
SO2Me
H
H
Me
H



140
4
SO2Me
H
H
Me
H



141
1
SO2NH2
H
H
Me
H



142
2
SO2NH2
H
H
Me
H



143
3
SO2NH2
H
H
Me
H



144
4
SO2NH2
H
H
Me
H



145
1
H
H
H
CF3
H



146
2
H
H
H
CF3
H



147
3
H
H
H
CF3
H



148
4
H
H
H
CF3
H



149
1
Me
H
H
CF3
H



150
2
Me
H
H
CF3
H



151
3
Me
H
H
CF3
H



152
4
Me
H
H
CF3
H



153
1
CH2Ph
H
H
CF3
H



154
2
CH2Ph
H
H
CF3
H



155
3
CH2Ph
H
H
CF3
H



156
4
CH2Ph
H
H
CF3
H



157
1
COMe
H
H
CF3
H



158
2
COMe
H
H
CF3
H



159
3
COMe
H
H
CF3
H



160
4
COMe
H
H
CF3
H



161
1
CO2Me
H
H
CF3
H



162
2
CO2Me
H
H
CF3
H



163
3
CO2Me
H
H
CF3
H



164
4
CO2Me
H
H
CF3
H



165
1
CO2tBu
H
H
CF3
H



166
2
CO2tBu
H
H
CF3
H



167
3
CO2tBu
H
H
CF3
H



168
4
CO2tBu
H
H
CF3
H



169
1
CONHMe
H
H
CF3
H



170
2
CONHMe
H
H
CF3
H



171
3
CONHMe
H
H
CF3
H



172
4
CONHMe
H
H
CF3
H



173
1
SO2Me
H
H
CF3
H



174
2
SO2Me
H
H
CF3
H



175
3
SO2Me
H
H
CF3
H



176
4
SO2Me
H
H
CF3
H



177
1
SO2NH2
H
H
CF3
H



178
2
SO2NH2
H
H
CF3
H



179
3
SO2NH2
H
H
CF3
H



180
4
SO2NH2
H
H
CF3
H



181
1
H
H
H
F
H



182
2
H
H
H
F
H



183
3
H
H
H
F
H



184
4
H
H
H
F
H



185
1
Me
H
H
F
H



186
2
Me
H
H
F
H



187
3
Me
H
H
F
H



188
4
Me
H
H
F
H



189
1
CH2Ph
H
H
F
H



190
2
CH2Ph
H
H
F
H



191
3
CH2Ph
H
H
F
H



192
4
CH2Ph
H
H
F
H



193
1
COMe
H
H
F
H



194
2
COMe
H
H
F
H



195
3
COMe
H
H
F
H



196
4
COMe
H
H
F
H



197
1
CO2Me
H
H
F
H



198
2
CO2Me
H
H
F
H



199
3
CO2Me
H
H
F
H



200
4
CO2Me
H
H
F
H



201
1
CO2tBu
H
H
F
H



202
2
CO2tBu
H
H
F
H



203
3
CO2tBu
H
H
F
H



204
4
CO2tBu
H
H
F
H



205
1
CONHMe
H
H
F
H



206
2
CONHMe
H
H
F
H



207
3
CONHMe
H
H
F
H



208
4
CONHMe
H
H
F
H



209
1
SO2Me
H
H
F
H



210
2
SO2Me
H
H
F
H



211
3
SO2Me
H
H
F
H



212
4
SO2Me
H
H
F
H



213
1
SO2NH2
H
H
F
H



214
2
SO2NH2
H
H
F
H



215
3
SO2NH2
H
H
F
H



216
4
SO2NH2
H
H
F
H



217
1
H
H
H
Cl
H



218
2
H
H
H
Cl
H



219
3
H
H
H
Cl
H



220
4
H
H
H
Cl
H



221
1
Me
H
H
Cl
H



222
2
Me
H
H
Cl
H



223
3
Me
H
H
Cl
H



224
4
Me
H
H
Cl
H



225
1
CH2Ph
H
H
Cl
H



226
2
CH2Ph
H
H
Cl
H



227
3
CH2Ph
H
H
Cl
H



228
4
CH2Ph
H
H
Cl
H



229
1
COMe
H
H
Cl
H



230
2
COMe
H
H
Cl
H



231
3
COMe
H
H
Cl
H



232
4
COMe
H
H
Cl
H



233
1
CO2Me
H
H
Cl
H



234
2
CO2Me
H
H
Cl
H



235
3
CO2Me
H
H
Cl
H



236
4
CO2Me
H
H
Cl
H



237
1
CO2tBu
H
H
Cl
H



238
2
CO2tBu
H
H
Cl
H



239
3
CO2tBu
H
H
Cl
H



240
4
CO2tBu
H
H
Cl
H



241
1
CONHMe
H
H
Cl
H



242
2
CONHMe
H
H
Cl
H



243
3
CONHMe
H
H
Cl
H



244
4
CONHMe
H
H
Cl
H



245
1
SO2Me
H
H
Cl
H



246
2
SO2Me
H
H
Cl
H



247
3
SO2Me
H
H
Cl
H



248
4
SO2Me
H
H
Cl
H



249
1
SO2NH2
H
H
Cl
H



250
2
SO2NH2
H
H
Cl
H



251
3
SO2NH2
H
H
Cl
H



252
4
SO2NH2
H
H
Cl
H



253
1
H
H
H
CN
H



254
2
H
H
H
CN
H



255
3
H
H
H
CN
H



256
4
H
H
H
CN
H



257
1
Me
H
H
CN
H



258
2
Me
H
H
CN
H



259
3
Me
H
H
CN
H



260
4
Me
H
H
CN
H



261
1
CH2Ph
H
H
CN
H



262
2
CH2Ph
H
H
CN
H



263
3
CH2Ph
H
H
CN
H



264
4
CH2Ph
H
H
CN
H



265
1
COMe
H
H
CN
H



266
2
COMe
H
H
CN
H



267
3
COMe
H
H
CN
H



268
4
COMe
H
H
CN
H



269
1
CO2Me
H
H
CN
H



270
2
CO2Me
H
H
CN
H



271
3
CO2Me
H
H
CN
H



272
4
CO2Me
H
H
CN
H



273
1
CO2tBu
H
H
CN
H



274
2
CO2tBu
H
H
CN
H



275
3
CO2tBu
H
H
CN
H



276
4
CO2tBu
H
H
CN
H



277
1
CONHMe
H
H
CN
H



278
2
CONHMe
H
H
CN
H



279
3
CONHMe
H
H
CN
H



280
4
CONHMe
H
H
CN
H



281
1
SO2Me
H
H
CN
H



282
2
SO2Me
H
H
CN
H



283
3
SO2Me
H
H
CN
H



284
4
SO2Me
H
H
CN
H



285
1
SO2NH2
H
H
CN
H



286
2
SO2NH2
H
H
CN
H



287
3
SO2NH2
H
H
CN
H



288
4
SO2NH2
H
H
CN
H



289
1
H
H
H
H
OH



290
2
H
H
H
H
OH



291
3
H
H
H
H
OH



292
4
H
H
H
H
OH



293
1
Me
H
H
H
OH



294
2
Me
H
H
H
OH



295
3
Me
H
H
H
OH



296
4
Me
H
H
H
OH



297
1
CH2Ph
H
H
H
OH



298
2
CH2Ph
H
H
H
OH



299
3
CH2Ph
H
H
H
OH



300
4
CH2Ph
H
H
H
OH



301
1
COMe
H
H
H
OH



302
2
COMe
H
H
H
OH



303
3
COMe
H
H
H
OH



304
4
COMe
H
H
H
OH



305
1
CO2Me
H
H
H
OH



306
2
CO2Me
H
H
H
OH



307
3
CO2Me
H
H
H
OH



308
4
CO2Me
H
H
H
OH



309
1
CO2tBu
H
H
H
OH



310
2
CO2tBu
H
H
H
OH



311
3
CO2tBu
H
H
H
OH



312
4
CO2tBu
H
H
H
OH



313
1
CONHMe
H
H
H
OH



314
2
CONHMe
H
H
H
OH



315
3
CONHMe
H
H
H
OH



316
4
CONHMe
H
H
H
OH



317
1
SO2Me
H
H
H
OH



318
2
SO2Me
H
H
H
OH



319
3
SO2Me
H
H
H
OH



320
4
SO2Me
H
H
H
OH



321
1
SO2NH2
H
H
H
OH



322
2
SO2NH2
H
H
H
OH



323
3
SO2NH2
H
H
H
OH



324
4
SO2NH2
H
H
H
OH



325
1
H
H
H
H
OMe



326
2
H
H
H
H
OMe



327
3
H
H
H
H
OMe



328
4
H
H
H
H
OMe



329
1
Me
H
H
H
OMe



330
2
Me
H
H
H
OMe



331
3
Me
H
H
H
OMe



332
4
Me
H
H
H
OMe



333
1
CH2Ph
H
H
H
OMe



334
2
CH2Ph
H
H
H
OMe



335
3
CH2Ph
H
H
H
OMe



336
4
CH2Ph
H
H
H
OMe



337
1
COMe
H
H
H
OMe



338
2
COMe
H
H
H
OMe



339
3
COMe
H
H
H
OMe



340
4
COMe
H
H
H
OMe



341
1
CO2Me
H
H
H
OMe



342
2
CO2Me
H
H
H
OMe



343
3
CO2Me
H
H
H
OMe



344
4
CO2Me
H
H
H
OMe



345
1
CO2tBu
H
H
H
OMe



346
2
CO2tBu
H
H
H
OMe



347
3
CO2tBu
H
H
H
OMe



348
4
CO2tBu
H
H
H
OMe



349
1
CONHMe
H
H
H
OMe



350
2
CONHMe
H
H
H
OMe



351
3
CONHMe
H
H
H
OMe



352
4
CONHMe
H
H
H
OMe



353
1
SO2Me
H
H
H
OMe



354
2
SO2Me
H
H
H
OMe



355
3
SO2Me
H
H
H
OMe



356
4
SO2Me
H
H
H
OMe



357
1
SO2NH2
H
H
H
OMe



358
2
SO2NH2
H
H
H
OMe



359
3
SO2NH2
H
H
H
OMe



360
4
SO2NH2
H
H
H
OMe



361
1
H
H
H
H
Me



362
2
H
H
H
H
Me



363
3
H
H
H
H
Me



364
4
H
H
H
H
Me



365
1
Me
H
H
H
Me



366
2
Me
H
H
H
Me



367
3
Me
H
H
H
Me



368
4
Me
H
H
H
Me



369
1
CH2Ph
H
H
H
Me



370
2
CH2Ph
H
H
H
Me



371
3
CH2Ph
H
H
H
Me



372
4
CH2Ph
H
H
H
Me



373
1
COMe
H
H
H
Me



374
2
COMe
H
H
H
Me



375
3
COMe
H
H
H
Me



376
4
COMe
H
H
H
Me



377
1
CO2Me
H
H
H
Me



378
2
CO2Me
H
H
H
Me



379
3
CO2Me
H
H
H
Me



380
4
CO2Me
H
H
H
Me



381
1
CO2tBu
H
H
H
Me



382
2
CO2tBu
H
H
H
Me



383
3
CO2tBu
H
H
H
Me



384
4
CO2tBu
H
H
H
Me



385
1
CONHMe
H
H
H
Me



386
2
CONHMe
H
H
H
Me



387
3
CONHMe
H
H
H
Me



388
4
CONHMe
H
H
H
Me



389
1
SO2Me
H
H
H
Me



390
2
SO2Me
H
H
H
Me



391
3
SO2Me
H
H
H
Me



392
4
SO2Me
H
H
H
Me



393
1
SO2NH2
H
H
H
Me



394
2
SO2NH2
H
H
H
Me



395
3
SO2NH2
H
H
H
Me



396
4
SO2NH2
H
H
H
Me



397
1
H
H
H
H
CF3



398
2
H
H
H
H
CF3



399
3
H
H
H
H
CF3



400
4
H
H
H
H
CF3



401
1
Me
H
H
H
CF3



402
2
Me
H
H
H
CF3



403
3
Me
H
H
H
CF3



404
4
Me
H
H
H
CF3



405
1
CH2Ph
H
H
H
CF3



406
2
CH2Ph
H
H
H
CF3



407
3
CH2Ph
H
H
H
CF3



408
4
CH2Ph
H
H
H
CF3



409
1
COMe
H
H
H
CF3



410
2
COMe
H
H
H
CF3



411
3
COMe
H
H
H
CF3



412
4
COMe
H
H
H
CF3



413
1
CO2Me
H
H
H
CF3



414
2
CO2Me
H
H
H
CF3



415
3
CO2Me
H
H
H
CF3



416
4
CO2Me
H
H
H
CF3



417
1
CO2tBu
H
H
H
CF3



418
2
CO2tBu
H
H
H
CF3



419
3
CO2tBu
H
H
H
CF3



420
4
CO2tBu
H
H
H
CF3



421
1
CONHMe
H
H
H
CF3



422
2
CONHMe
H
H
H
CF3



423
3
CONHMe
H
H
H
CF3



424
4
CONHMe
H
H
H
CF3



425
1
SO2Me
H
H
H
CF3



426
2
SO2Me
H
H
H
CF3



427
3
SO2Me
H
H
H
CF3



428
4
SO2Me
H
H
H
CF3



429
1
SO2NH2
H
H
H
CF3



430
2
SO2NH2
H
H
H
CF3



431
3
SO2NH2
H
H
H
CF3



432
4
SO2NH2
H
H
H
CF3



433
1
H
H
H
H
F



434
2
H
H
H
H
F



435
3
H
H
H
H
F



436
3
H
H
H
H
F



437
1
Me
H
H
H
F



438
2
Me
H
H
H
F



439
3
Me
H
H
H
F



440
4
Me
H
H
H
F



441
1
CH2Ph
H
H
H
F



442
2
CH2Ph
H
H
H
F



443
3
CH2Ph
H
H
H
F



444
4
CH2Ph
H
H
H
F



445
1
COMe
H
H
H
F



446
2
COMe
H
H
H
F



447
3
COMe
H
H
H
F



448
4
COMe
H
H
H
F



449
1
CO2Me
H
H
H
F



450
2
CO2Me
H
H
H
F



451
3
CO2Me
H
H
H
F



452
4
CO2Me
H
H
H
F



453
1
CO2tBu
H
H
H
F



454
2
CO2tBu
H
H
H
F



455
3
CO2tBu
H
H
H
F



456
4
CO2tBu
H
H
H
F



457
1
CONHMe
H
H
H
F



458
2
CONHMe
H
H
H
F



459
3
CONHMe
H
H
H
F



460
4
CONHMe
H
H
H
F



461
1
SO2Me
H
H
H
F



462
2
SO2Me
H
H
H
F



463
3
SO2Me
H
H
H
F



464
4
SO2Me
H
H
H
F



465
1
SO2NH2
H
H
H
F



466
2
SO2NH2
H
H
H
F



467
3
SO2NH2
H
H
H
F



468
4
SO2NH2
H
H
H
F



469
1
H
H
H
H
Cl



470
2
H
H
H
H
Cl



471
3
H
H
H
H
Cl



472
4
H
H
H
H
Cl



473
1
Me
H
H
H
Cl



474
2
Me
H
H
H
Cl



475
3
Me
H
H
H
Cl



476
4
Me
H
H
H
Cl



477
1
CH2Ph
H
H
H
Cl



478
2
CH2Ph
H
H
H
Cl



479
3
CH2Ph
H
H
H
Cl



480
4
CH2Ph
H
H
H
Cl



481
1
COMe
H
H
H
Cl



482
2
COMe
H
H
H
Cl



483
3
COMe
H
H
H
Cl



484
4
COMe
H
H
H
Cl



485
1
CO2Me
H
H
H
Cl



486
2
CO2Me
H
H
H
Cl



487
3
CO2Me
H
H
H
Cl



488
4
CO2Me
H
H
H
Cl



489
1
CO2tBu
H
H
H
Cl



490
2
CO2tBu
H
H
H
Cl



491
3
CO2tBu
H
H
H
Cl



492
4
CO2tBu
H
H
H
Cl



493
1
CONHMe
H
H
H
Cl



494
2
CONHMe
H
H
H
Cl



495
3
CONHMe
H
H
H
Cl



496
4
CONHMe
H
H
H
Cl



497
1
SO2Me
H
H
H
Cl



498
2
SO2Me
H
H
H
Cl



499
3
SO2Me
H
H
H
Cl



500
4
SO2Me
H
H
H
Cl



501
1
SO2NH2
H
H
H
Cl



502
2
SO2NH2
H
H
H
Cl



503
3
SO2NH2
H
H
H
Cl



504
4
SO2NH2
H
H
H
Cl



505
1
H
H
H
H
CN



506
2
H
H
H
H
CN



507
3
H
H
H
H
CN



508
4
H
H
H
H
CN



509
1
Me
H
H
H
CN



510
2
Me
H
H
H
CN



511
3
Me
H
H
H
CN



512
4
Me
H
H
H
CN



513
1
CH2Ph
H
H
H
CN



514
2
CH2Ph
H
H
H
CN



515
3
CH2Ph
H
H
H
CN



516
4
CH2Ph
H
H
H
CN



517
1
COMe
H
H
H
CN



518
2
COMe
H
H
H
CN



519
3
COMe
H
H
H
CN



520
4
COMe
H
H
H
CN



521
1
CO2Me
H
H
H
CN



522
2
CO2Me
H
H
H
CN



523
3
CO2Me
H
H
H
CN



524
4
CO2Me
H
H
H
CN



525
1
CO2tBu
H
H
H
CN



526
2
CO2tBu
H
H
H
CN



527
3
CO2tBu
H
H
H
CN



528
4
CO2tBu
H
H
H
CN



529
1
CONHMe
H
H
H
CN



530
2
CONHMe
H
H
H
CN



531
3
CONHMe
H
H
H
CN



532
4
CONHMe
H
H
H
CN



533
1
SO2Me
H
H
H
CN



534
2
SO2Me
H
H
H
CN



535
3
SO2Me
H
H
H
CN



536
4
SO2Me
H
H
H
CN



537
1
SO2NH2
H
H
H
CN



538
2
SO2NH2
H
H
H
CN



539
3
SO2NH2
H
H
H
CN



540
4
SO2NH2
H
H
H
CN










Exemplary embodiments include compounds having the formula (XXXV)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 28.













TABLE 28






Entry
n
X
R3




















1
1
O
Phenyl



2
2
O
Phenyl



3
3
O
Phenyl



4
4
O
Phenyl



5
1
S
Phenyl



6
2
S
Phenyl



7
3
S
Phenyl



8
4
S
Phenyl



9
1
SO
Phenyl



10
2
SO
Phenyl



11
3
SO
Phenyl



12
4
SO
Phenyl



13
1
SO2
Phenyl



14
2
SO2
Phenyl



15
3
SO2
Phenyl



16
4
SO2
Phenyl



17
1
O
3-OH-Phenyl



18
2
O
3-OH-Phenyl



19
3
O
3-OH-Phenyl



20
4
O
3-OH-Phenyl



21
1
S
3-OH-Phenyl



22
2
S
3-OH-Phenyl



23
3
S
3-OH-Phenyl



24
4
S
3-OH-Phenyl



25
1
SO
3-OH-Phenyl



26
2
SO
3-OH-Phenyl



27
3
SO
3-OH-Phenyl



28
4
SO
3-OH-Phenyl



29
1
SO2
3-OH-Phenyl



30
2
SO2
3-OH-Phenyl



31
3
SO2
3-OH-Phenyl



32
4
SO2
3-OH-Phenyl



33
1
O
4-NO2-Phenyl



34
2
O
4-NO2-Phenyl



35
3
O
4-NO2-Phenyl



36
4
O
4-NO2-Phenyl



37
1
S
4-NO2-Phenyl



38
2
S
4-NO2-Phenyl



39
3
S
4-NO2-Phenyl



40
4
S
4-NO2-Phenyl



41
1
SO
4-NO2-Phenyl



42
2
SO
4-NO2-Phenyl



43
3
SO
4-NO2-Phenyl



44
4
SO
4-NO2-Phenyl



45
1
SO2
4-NO2-Phenyl



46
2
SO2
4-NO2-Phenyl



47
3
SO2
4-NO2-Phenyl



48
4
SO2
4-NO2-Phenyl



49
1
O
3-OMe-Phenyl



50
2
O
3-OMe-Phenyl



51
3
O
3-OMe-Phenyl



52
4
O
3-OMe-Phenyl



53
1
S
3-OMe-Phenyl



54
2
S
3-OMe-Phenyl



55
3
S
3-OMe-Phenyl



56
4
S
3-OMe-Phenyl



57
1
SO
3-OMe-Phenyl



58
2
SO
3-OMe-Phenyl



59
3
SO
3-OMe-Phenyl



60
4
SO
3-OMe-Phenyl



61
1
SO2
3-OMe-Phenyl



62
2
SO2
3-OMe-Phenyl



63
3
SO2
3-OMe-Phenyl



64
4
SO2
3-OMe-Phenyl



65
1
O
4-CN-Phenyl



66
2
O
4-CN-Phenyl



67
3
O
4-CN-Phenyl



68
4
O
4-CN-Phenyl



69
1
S
4-CN-Phenyl



70
2
S
4-CN-Phenyl



71
3
S
4-CN-Phenyl



72
4
S
4-CN-Phenyl



73
1
SO
4-CN-Phenyl



74
2
SO
4-CN-Phenyl



75
3
SO
4-CN-Phenyl



76
4
SO
4-CN-Phenyl



77
1
SO2
4-CN-Phenyl



78
2
SO2
4-CN-Phenyl



79
3
SO2
4-CN-Phenyl



80
4
SO2
4-CN-Phenyl



81
1
O
2-CN-Phenyl



82
2
O
2-CN-Phenyl



83
3
O
2-CN-Phenyl



84
4
O
2-CN-Phenyl



85
1
S
2-CN-Phenyl



86
2
S
2-CN-Phenyl



87
3
S
2-CN-Phenyl



88
4
S
2-CN-Phenyl



89
1
SO
2-CN-Phenyl



90
2
SO
2-CN-Phenyl



91
3
SO
2-CN-Phenyl



92
4
SO
2-CN-Phenyl



93
1
SO2
2-CN-Phenyl



94
2
SO2
2-CN-Phenyl



95
3
SO2
2-CN-Phenyl



96
4
SO2
2-CN-Phenyl



97
1
O
3-Me-Phenyl



98
2
O
3-Me-Phenyl



99
3
O
3-Me-Phenyl



100
4
O
3-Me-Phenyl



101
1
S
3-Me-Phenyl



102
2
S
3-Me-Phenyl



103
3
S
3-Me-Phenyl



104
4
S
3-Me-Phenyl



105
1
SO
3-Me-Phenyl



106
2
SO
3-Me-Phenyl



107
3
SO
3-Me-Phenyl



108
4
SO
3-Me-Phenyl



109
1
SO2
3-Me-Phenyl



110
2
SO2
3-Me-Phenyl



111
3
SO2
3-Me-Phenyl



112
4
SO2
3-Me-Phenyl



113
1
O
2-F-Phenyl



114
2
O
2-F-Phenyl



115
3
O
2-F-Phenyl



116
4
O
2-F-Phenyl



117
1
S
2-F-Phenyl



118
2
S
2-F-Phenyl



119
3
S
2-F-Phenyl



120
4
S
2-F-Phenyl



121
1
SO
2-F-Phenyl



122
2
SO
2-F-Phenyl



123
3
SO
2-F-Phenyl



124
4
SO
2-F-Phenyl



125
1
SO2
2-F-Phenyl



126
2
SO2
2-F-Phenyl



127
3
SO2
2-F-Phenyl



128
4
SO2
2-F-Phenyl



129
1
O
4-F-Phenyl



130
2
O
4-F-Phenyl



131
3
O
4-F-Phenyl



132
4
O
4-F-Phenyl



133
1
S
4-F-Phenyl



134
2
S
4-F-Phenyl



135
3
S
4-F-Phenyl



136
4
S
4-F-Phenyl



137
1
SO
4-F-Phenyl



138
2
SO
4-F-Phenyl



139
3
SO
4-F-Phenyl



140
4
SO
4-F-Phenyl



141
1
SO2
4-F-Phenyl



142
2
SO2
4-F-Phenyl



143
3
SO2
4-F-Phenyl



144
4
SO2
4-F-Phenyl



145
1
O
3-Cl-Phenyl



146
2
O
3-Cl-Phenyl



147
3
O
3-Cl-Phenyl



148
4
O
3-Cl-Phenyl



149
1
S
3-Cl-Phenyl



150
2
S
3-Cl-Phenyl



151
3
S
3-Cl-Phenyl



152
4
S
3-Cl-Phenyl



153
1
SO
3-Cl-Phenyl



154
2
SO
3-Cl-Phenyl



155
3
SO
3-Cl-Phenyl



156
4
SO
3-Cl-Phenyl



157
1
SO2
3-Cl-Phenyl



158
2
SO2
3-Cl-Phenyl



159
3
SO2
3-Cl-Phenyl



160
4
SO2
3-Cl-Phenyl



161
1
O
2-Br-Phenyl



162
2
O
2-Br-Phenyl



163
3
O
2-Br-Phenyl



164
4
O
2-Br-Phenyl



165
1
S
2-Br-Phenyl



166
2
S
2-Br-Phenyl



167
3
S
2-Br-Phenyl



168
4
S
2-Br-Phenyl



169
1
SO
2-Br-Phenyl



170
2
SO
2-Br-Phenyl



171
3
SO
2-Br-Phenyl



172
4
SO
2-Br-Phenyl



173
1
SO2
2-Br-Phenyl



174
2
SO2
2-Br-Phenyl



175
3
SO2
2-Br-Phenyl



176
4
SO2
2-Br-Phenyl



177
1
O
4-Br-Phenyl



178
2
O
4-Br-Phenyl



179
3
O
4-Br-Phenyl



180
4
O
4-Br-Phenyl



181
1
S
4-Br-Phenyl



182
2
S
4-Br-Phenyl



183
3
S
4-Br-Phenyl



184
4
S
4-Br-Phenyl



185
1
SO
4-Br-Phenyl



186
2
SO
4-Br-Phenyl



187
3
SO
4-Br-Phenyl



188
4
SO
4-Br-Phenyl



189
1
SO2
4-Br-Phenyl



190
2
SO2
4-Br-Phenyl



191
3
SO2
4-Br-Phenyl



192
4
SO2
4-Br-Phenyl



193
1
O
3-CF3-Phenyl



194
2
O
3-CF3-Phenyl



195
3
O
3-CF3-Phenyl



196
4
O
3-CF3-Phenyl



197
1
S
3-CF3-Phenyl



198
2
S
3-CF3-Phenyl



199
3
S
3-CF3-Phenyl



200
4
S
3-CF3-Phenyl



201
1
SO
3-CF3-Phenyl



202
2
SO
3-CF3-Phenyl



203
3
SO
3-CF3-Phenyl



204
4
SO
3-CF3-Phenyl



205
1
SO2
3-CF3-Phenyl



206
2
SO2
3-CF3-Phenyl



207
3
SO2
3-CF3-Phenyl



208
4
SO2
3-CF3-Phenyl



209
1
O
2-iPr-Phenyl



210
2
O
2-iPr-Phenyl



211
3
O
2-iPr-Phenyl



212
4
O
2-iPr-Phenyl



213
1
S
2-iPr-Phenyl



214
2
S
2-iPr-Phenyl



215
3
S
2-iPr-Phenyl



216
4
S
2-iPr-Phenyl



217
1
SO
2-iPr-Phenyl



218
2
SO
2-iPr-Phenyl



219
3
SO
2-iPr-Phenyl



220
4
SO
2-iPr-Phenyl



221
1
SO2
2-iPr-Phenyl



222
2
SO2
2-iPr-Phenyl



223
3
SO2
2-iPr-Phenyl



224
4
SO2
2-iPr-Phenyl



225
1
O
4-iPr-Phenyl



226
2
O
4-iPr-Phenyl



227
3
O
4-iPr-Phenyl



228
4
O
4-iPr-Phenyl



229
1
S
4-iPr-Phenyl



230
2
S
4-iPr-Phenyl



231
3
S
4-iPr-Phenyl



232
4
S
4-iPr-Phenyl



233
1
SO
4-iPr-Phenyl



234
2
SO
4-iPr-Phenyl



235
3
SO
4-iPr-Phenyl



236
4
SO
4-iPr-Phenyl



237
1
SO2
4-iPr-Phenyl



238
2
SO2
4-iPr-Phenyl



239
3
SO2
4-iPr-Phenyl



240
4
SO2
4-iPr-Phenyl



241
1
O
3-NH2-Phenyl



242
2
O
3-NH2-Phenyl



243
3
O
3-NH2-Phenyl



244
4
O
3-NH2-Phenyl



245
1
S
3-NH2-Phenyl



246
2
S
3-NH2-Phenyl



247
3
S
3-NH2-Phenyl



248
1
S
3-NH2-Phenyl



249
2
SO
3-NH2-Phenyl



250
3
SO
3-NH2-Phenyl



251
4
SO
3-NH2-Phenyl



252
1
SO
3-NH2-Phenyl



253
2
SO2
3-NH2-Phenyl



254
3
SO2
3-NH2-Phenyl



255
4
SO2
3-NH2-Phenyl



256
1
O
2,4-di-Me-Phenyl



257
2
O
2,4-di-Me-Phenyl



258
3
O
2,4-di-Me-Phenyl



259
4
O
2,4-di-Me-Phenyl



260
1
S
2,4-di-Me-Phenyl



261
2
S
2,4-di-Me-Phenyl



262
3
S
2,4-di-Me-Phenyl



263
4
S
2,4-di-Me-Phenyl



264
1
SO
2,4-di-Me-Phenyl



265
2
SO
2,4-di-Me-Phenyl



266
3
SO
2,4-di-Me-Phenyl



267
4
SO
2,4-di-Me-Phenyl



268
1
SO2
2,4-di-Me-Phenyl



269
2
SO2
2,4-di-Me-Phenyl



270
3
SO2
2,4-di-Me-Phenyl



271
4
SO2
2,4-di-Me-Phenyl



272
1
O
2,6-di-iPr-Phenyl



273
2
O
2,6-di-iPr-Phenyl



274
3
O
2,6-di-iPr-Phenyl



275
4
O
2,6-di-iPr-Phenyl



276
1
S
2,6-di-iPr-Phenyl



277
2
S
2,6-di-iPr-Phenyl



278
3
S
2,6-di-iPr-Phenyl



279
4
S
2,6-di-iPr-Phenyl



280
1
SO
2,6-di-iPr-Phenyl



281
2
SO
2,6-di-iPr-Phenyl



282
3
SO
2,6-di-iPr-Phenyl



283
4
SO
2,6-di-iPr-Phenyl



284
1
SO2
2,6-di-iPr-Phenyl



285
2
SO2
2,6-di-iPr-Phenyl



286
3
SO2
2,6-di-iPr-Phenyl



287
4
SO2
2,6-di-iPr-Phenyl



288
1
O
3-Ph-Phenyl



289
2
O
3-Ph-Phenyl



290
3
O
3-Ph-Phenyl



291
4
O
3-Ph-Phenyl



292
1
S
3-Ph-Phenyl



293
2
S
3-Ph-Phenyl



294
3
S
3-Ph-Phenyl



295
4
S
3-Ph-Phenyl



296
1
SO
3-Ph-Phenyl



297
2
SO
3-Ph-Phenyl



298
3
SO
3-Ph-Phenyl



299
4
SO
3-Ph-Phenyl



300
1
SO2
3-Ph-Phenyl



301
2
SO2
3-Ph-Phenyl



302
3
SO2
3-Ph-Phenyl



303
4
SO2
3-Ph-Phenyl



304
1
O
2-morpholino-phenyl



305
2
O
2-morpholino-phenyl



306
3
O
2-morpholino-phenyl



307
4
O
2-morpholino-phenyl



308
1
S
2-morpholino-phenyl



309
2
S
2-morpholino-phenyl



310
3
S
2-morpholino-phenyl



311
4
S
2-morpholino-phenyl



312
1
SO
2-morpholino-phenyl



313
2
SO
2-morpholino-phenyl



314
3
SO
2-morpholino-phenyl



315
4
SO
2-morpholino-phenyl



316
1
SO2
2-morpholino-phenyl



317
2
SO2
2-morpholino-phenyl



318
3
SO2
2-morpholino-phenyl



319
4
SO2
2-morpholino-phenyl



320
1
O
4-morpholino-phenyl



321
2
O
4-morpholino-phenyl



322
3
O
4-morpholino-phenyl



323
4
O
4-morpholino-phenyl



324
1
SO
4-morpholino-phenyl



325
2
SO
4-morpholino-phenyl



326
3
SO
4-morpholino-phenyl



327
4
SO
4-morpholino-phenyl



328
1
O
naphthylen-1-yl



329
2
O
naphthylen-1-yl



330
3
O
naphthylen-1-yl



331
4
O
naphthylen-1-yl



332
1
S
naphthylen-1-yl



333
2
S
naphthylen-1-yl



334
3
S
naphthylen-1-yl



335
4
S
naphthylen-1-yl



336
1
SO
naphthylen-1-yl



337
2
SO
naphthylen-1-yl



338
3
SO
naphthylen-1-yl



339
4
SO
naphthylen-1-yl



340
1
SO2
naphthylen-1-yl



341
2
SO2
naphthylen-1-yl



342
3
SO2
naphthylen-1-yl



343
4
SO2
naphthylen-1-yl



344
1
O
4-OH-Phenyl



345
2
O
4-OH-Phenyl



346
3
O
4-OH-Phenyl



347
4
O
4-OH-Phenyl



348
1
S
4-OH-Phenyl



349
2
S
4-OH-Phenyl



350
3
S
4-OH-Phenyl



351
4
S
4-OH-Phenyl



352
1
SO
4-OH-Phenyl



353
2
SO
4-OH-Phenyl



354
3
SO
4-OH-Phenyl



355
4
SO
4-OH-Phenyl



356
1
SO2
4-OH-Phenyl



357
2
SO2
4-OH-Phenyl



358
3
SO2
4-OH-Phenyl



359
4
SO2
4-OH-Phenyl



360
1
O
2-OH-Phenyl



361
2
O
2-OH-Phenyl



362
3
O
2-OH-Phenyl



363
4
O
2-OH-Phenyl



364
1
S
2-OH-Phenyl



365
2
S
2-OH-Phenyl



366
3
S
2-OH-Phenyl



367
4
S
2-OH-Phenyl



368
1
SO
2-OH-Phenyl



369
2
SO
2-OH-Phenyl



370
3
SO
2-OH-Phenyl



371
4
SO
2-OH-Phenyl



372
1
SO2
2-OH-Phenyl



373
2
SO2
2-OH-Phenyl



374
3
SO2
2-OH-Phenyl



375
4
SO2
2-OH-Phenyl



376
1
O
4-OMe-Phenyl



377
2
O
4-OMe-Phenyl



378
3
O
4-OMe-Phenyl



379
4
O
4-OMe-Phenyl



380
1
S
4-OMe-Phenyl



381
2
S
4-OMe-Phenyl



382
3
S
4-OMe-Phenyl



383
4
S
4-OMe-Phenyl



384
1
SO
4-OMe-Phenyl



385
2
SO
4-OMe-Phenyl



386
3
SO
4-OMe-Phenyl



387
4
SO
4-OMe-Phenyl



388
1
SO2
4-OMe-Phenyl



389
2
SO2
4-OMe-Phenyl



390
3
SO2
4-OMe-Phenyl



391
4
SO2
4-OMe-Phenyl



392
1
O
2-OMe-Phenyl



393
2
O
2-OMe-Phenyl



394
3
O
2-OMe-Phenyl



395
4
O
2-OMe-Phenyl



396
1
S
2-OMe-Phenyl



397
2
S
2-OMe-Phenyl



398
3
S
2-OMe-Phenyl



399
4
S
2-OMe-Phenyl



400
1
SO
2-OMe-Phenyl



401
2
SO
2-OMe-Phenyl



402
3
SO
2-OMe-Phenyl



403
4
SO
2-OMe-Phenyl



404
1
SO2
2-OMe-Phenyl



405
2
SO2
2-OMe-Phenyl



406
3
SO2
2-OMe-Phenyl



407
4
SO2
2-OMe-Phenyl



408
1
O
3-CN-Phenyl



409
2
O
3-CN-Phenyl



410
3
O
3-CN-Phenyl



411
4
O
3-CN-Phenyl



412
1
S
3-CN-Phenyl



413
2
S
3-CN-Phenyl



414
3
S
3-CN-Phenyl



415
4
S
3-CN-Phenyl



416
1
SO
3-CN-Phenyl



417
2
SO
3-CN-Phenyl



418
3
SO
3-CN-Phenyl



419
4
SO
3-CN-Phenyl



420
1
SO2
3-CN-Phenyl



421
2
SO2
3-CN-Phenyl



422
3
SO2
3-CN-Phenyl



423
4
SO2
3-CN-Phenyl



424
1
O
2-Me-Phenyl



425
2
O
2-Me-Phenyl



426
3
O
2-Me-Phenyl



427
4
O
2-Me-Phenyl



428
1
S
2-Me-Phenyl



429
2
S
2-Me-Phenyl



430
3
S
2-Me-Phenyl



431
4
S
2-Me-Phenyl



432
1
SO
2-Me-Phenyl



433
2
SO
2-Me-Phenyl



434
3
SO
2-Me-Phenyl



435
4
SO
2-Me-Phenyl



436
1
SO2
2-Me-Phenyl



437
2
SO2
2-Me-Phenyl



438
3
SO2
2-Me-Phenyl



439
4
SO2
2-Me-Phenyl



440
1
O
4-Me-Phenyl



441
2
O
4-Me-Phenyl



442
3
O
4-Me-Phenyl



443
4
O
4-Me-Phenyl



444
1
S
4-Me-Phenyl



445
2
S
4-Me-Phenyl



446
3
S
4-Me-Phenyl



447
4
S
4-Me-Phenyl



448
1
SO
4-Me-Phenyl



449
2
SO
4-Me-Phenyl



450
3
SO
4-Me-Phenyl



451
4
SO
4-Me-Phenyl



452
1
SO2
4-Me-Phenyl



453
2
SO2
4-Me-Phenyl



454
3
SO2
4-Me-Phenyl



455
4
SO2
4-Me-Phenyl



456
1
O
3-F-Phenyl



457
2
O
3-F-Phenyl



458
3
O
3-F-Phenyl



459
4
O
3-F-Phenyl



460
1
S
3-F-Phenyl



461
2
S
3-F-Phenyl



462
3
S
3-F-Phenyl



463
4
S
3-F-Phenyl



464
1
SO
3-F-Phenyl



465
2
SO
3-F-Phenyl



466
3
SO
3-F-Phenyl



467
4
SO
3-F-Phenyl



468
1
SO2
3-F-Phenyl



469
2
SO2
3-F-Phenyl



470
3
SO2
3-F-Phenyl



471
4
SO2
3-F-Phenyl



472
1
O
2-Cl-Phenyl



473
2
O
2-Cl-Phenyl



474
3
O
2-Cl-Phenyl



475
4
O
2-Cl-Phenyl



476
1
S
2-Cl-Phenyl



477
2
S
2-Cl-Phenyl



478
3
S
2-Cl-Phenyl



479
4
S
2-Cl-Phenyl



480
1
SO
2-Cl-Phenyl



481
2
SO
2-Cl-Phenyl



482
3
SO
2-Cl-Phenyl



483
4
SO
2-Cl-Phenyl



484
1
SO2
2-Cl-Phenyl



485
2
SO2
2-Cl-Phenyl



486
3
SO2
2-Cl-Phenyl



487
4
SO2
2-Cl-Phenyl



488
1
O
4-Cl-Phenyl



489
2
O
4-Cl-Phenyl



490
3
O
4-Cl-Phenyl



491
4
O
4-Cl-Phenyl



492
1
S
4-Cl-Phenyl



493
2
S
4-Cl-Phenyl



494
3
S
4-Cl-Phenyl



495
4
S
4-Cl-Phenyl



496
1
SO
4-Cl-Phenyl



497
2
SO
4-Cl-Phenyl



498
3
SO
4-Cl-Phenyl



499
4
SO
4-Cl-Phenyl



500
1
SO2
4-Cl-Phenyl



501
2
SO2
4-Cl-Phenyl



502
3
SO2
4-Cl-Phenyl



503
4
SO2
4-Cl-Phenyl



504
1
O
3-Br-Phenyl



505
2
O
3-Br-Phenyl



506
3
O
3-Br-Phenyl



507
4
O
3-Br-Phenyl



508
1
S
3-Br-Phenyl



509
2
S
3-Br-Phenyl



510
3
S
3-Br-Phenyl



511
4
S
3-Br-Phenyl



512
1
SO
3-Br-Phenyl



513
2
SO
3-Br-Phenyl



514
3
SO
3-Br-Phenyl



515
4
SO
3-Br-Phenyl



516
1
SO2
3-Br-Phenyl



517
2
SO2
3-Br-Phenyl



518
3
SO2
3-Br-Phenyl



519
4
SO2
3-Br-Phenyl



520
1
O
2-CF3-Phenyl



521
2
O
2-CF3-Phenyl



522
3
O
2-CF3-Phenyl



523
4
O
2-CF3-Phenyl



524
1
S
2-CF3-Phenyl



525
2
S
2-CF3-Phenyl



526
3
S
2-CF3-Phenyl



527
4
S
2-CF3-Phenyl



528
1
SO
2-CF3-Phenyl



529
2
SO
2-CF3-Phenyl



530
3
SO
2-CF3-Phenyl



531
4
SO
2-CF3-Phenyl



532
1
SO2
2-CF3-Phenyl



533
2
SO2
2-CF3-Phenyl



534
3
SO2
2-CF3-Phenyl



535
4
SO2
2-CF3-Phenyl



536
1
O
4-CF3-Phenyl



537
2
O
4-CF3-Phenyl



538
3
O
4-CF3-Phenyl



539
4
O
4-CF3-Phenyl



540
1
S
4-CF3-Phenyl



541
2
S
4-CF3-Phenyl



542
3
S
4-CF3-Phenyl



543
4
S
4-CF3-Phenyl



544
1
SO
4-CF3-Phenyl



545
2
SO
4-CF3-Phenyl



546
3
SO
4-CF3-Phenyl



547
4
SO
4-CF3-Phenyl



548
1
SO2
4-CF3-Phenyl



549
2
SO2
4-CF3-Phenyl



550
3
SO2
4-CF3-Phenyl



551
4
SO2
4-CF3-Phenyl



552
1
O
3-iPr-Phenyl



553
2
O
3-iPr-Phenyl



554
3
O
3-iPr-Phenyl



555
4
O
3-iPr-Phenyl



556
1
S
3-iPr-Phenyl



557
2
S
3-iPr-Phenyl



558
3
S
3-iPr-Phenyl



559
4
S
3-iPr-Phenyl



560
1
SO
3-iPr-Phenyl



561
2
SO
3-iPr-Phenyl



562
3
SO
3-iPr-Phenyl



563
4
SO
3-iPr-Phenyl



564
1
SO2
3-iPr-Phenyl



565
2
SO2
3-iPr-Phenyl



566
3
SO2
3-iPr-Phenyl



567
4
SO2
3-iPr-Phenyl



568
1
O
4-NH2-Phenyl



569
2
O
4-NH2-Phenyl



570
3
O
4-NH2-Phenyl



571
4
O
4-NH2-Phenyl



572
1
S
4-NH2-Phenyl



573
2
S
4-NH2-Phenyl



574
3
S
4-NH2-Phenyl



575
4
S
4-NH2-Phenyl



576
1
SO
4-NH2-Phenyl



577
2
SO
4-NH2-Phenyl



578
3
SO
4-NH2-Phenyl



579
4
SO
4-NH2-Phenyl



580
1
SO2
4-NH2-Phenyl



581
2
SO2
4-NH2-Phenyl



582
3
SO2
4-NH2-Phenyl



583
4
SO2
4-NH2-Phenyl



584
1
O
2-NH2-Phenyl



585
2
O
2-NH2-Phenyl



586
3
O
2-NH2-Phenyl



587
4
O
2-NH2-Phenyl



588
1
S
2-NH2-Phenyl



589
2
S
2-NH2-Phenyl



590
3
S
2-NH2-Phenyl



591
1
S
2-NH2-Phenyl



592
2
SO
2-NH2-Phenyl



593
3
SO
2-NH2-Phenyl



594
4
SO
2-NH2-Phenyl



595
1
SO
2-NH2-Phenyl



596
2
SO2
2-NH2-Phenyl



597
3
SO2
2-NH2-Phenyl



598
4
SO2
2-NH2-Phenyl



599
1
O
2,6-di-Me-Phenyl



600
2
O
2,6-di-Me-Phenyl



601
3
O
2,6-di-Me-Phenyl



602
4
O
2,6-di-Me-Phenyl



603
1
S
2,6-di-Me-Phenyl



604
2
S
2,6-di-Me-Phenyl



605
3
S
2,6-di-Me-Phenyl



606
4
S
2,6-di-Me-Phenyl



607
1
SO
2,6-di-Me-Phenyl



608
2
SO
2,6-di-Me-Phenyl



609
3
SO
2,6-di-Me-Phenyl



610
4
SO
2,6-di-Me-Phenyl



611
1
SO2
2,6-di-Me-Phenyl



612
2
SO2
2,6-di-Me-Phenyl



613
3
SO2
2,6-di-Me-Phenyl



614
4
SO2
2,6-di-Me-Phenyl



615
1
O
2-Ph-Phenyl



616
2
O
2-Ph-Phenyl



617
3
O
2-Ph-Phenyl



618
4
O
2-Ph-Phenyl



619
1
S
2-Ph-Phenyl



620
2
S
2-Ph-Phenyl



621
3
S
2-Ph-Phenyl



622
4
S
2-Ph-Phenyl



623
1
SO
2-Ph-Phenyl



624
2
SO
2-Ph-Phenyl



625
3
SO
2-Ph-Phenyl



626
4
SO
2-Ph-Phenyl



627
1
SO2
2-Ph-Phenyl



628
2
SO2
2-Ph-Phenyl



629
3
SO2
2-Ph-Phenyl



630
4
SO2
2-Ph-Phenyl



631
1
O
4-Ph-Phenyl



632
2
O
4-Ph-Phenyl



633
3
O
4-Ph-Phenyl



634
4
O
4-Ph-Phenyl



635
1
S
4-Ph-Phenyl



636
2
S
4-Ph-Phenyl



637
3
S
4-Ph-Phenyl



638
4
S
4-Ph-Phenyl



639
1
SO
4-Ph-Phenyl



640
2
SO
4-Ph-Phenyl



641
3
SO
4-Ph-Phenyl



642
4
SO
4-Ph-Phenyl



643
1
SO2
4-Ph-Phenyl



644
2
SO2
4-Ph-Phenyl



645
3
SO2
4-Ph-Phenyl



646
4
SO2
4-Ph-Phenyl



647
1
O
3-morpholino-phenyl



648
2
O
3-morpholino-phenyl



649
3
O
3-morpholino-phenyl



650
4
O
3-morpholino-phenyl



651
1
S
3-morpholino-phenyl



652
2
S
3-morpholino-phenyl



653
3
S
3-morpholino-phenyl



654
4
S
3-morpholino-phenyl



655
1
SO
3-morpholino-phenyl



656
2
SO
3-morpholino-phenyl



657
3
SO
3-morpholino-phenyl



658
4
SO
3-morpholino-phenyl



659
1
SO2
3-morpholino-phenyl



660
2
SO2
3-morpholino-phenyl



661
3
SO2
3-morpholino-phenyl



662
4
SO2
3-morpholino-phenyl



663
1
S
4-morpholino-phenyl



664
2
S
4-morpholino-phenyl



665
3
S
4-morpholino-phenyl



667
4
S
4-morpholino-phenyl



668
1
SO2
4-morpholino-phenyl



669
2
SO2
4-morpholino-phenyl



670
3
SO2
4-morpholino-phenyl



671
4
SO2
4-morpholino-phenyl



672
1
O
naphthylen-2-yl



673
2
O
naphthylen-2-yl



674
3
O
naphthylen-2-yl



675
4
O
naphthylen-2-yl



676
1
S
naphthylen-2-yl



678
2
S
naphthylen-2-yl



679
3
S
naphthylen-2-yl



680
4
S
naphthylen-2-yl



681
1
SO
naphthylen-2-yl



682
2
SO
naphthylen-2-yl



683
3
SO
naphthylen-2-yl



684
4
SO
naphthylen-2-yl



685
1
SO2
naphthylen-2-yl



686
2
SO2
naphthylen-2-yl



687
3
SO2
naphthylen-2-yl



688
4
SO2
naphthylen-2-yl









Exemplary embodiments include compounds having the formula (XXXXVI)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 29.

















Entry
n
X
R3




















1
1
O
Phenyl



2
2
O
Phenyl



3
3
O
Phenyl



4
4
O
Phenyl



5
1
S
Phenyl



6
2
S
Phenyl



7
3
S
Phenyl



8
4
S
Phenyl



9
1
SO
Phenyl



10
2
SO
Phenyl



11
3
SO
Phenyl



12
4
SO
Phenyl



13
1
SO2
Phenyl



14
2
SO2
Phenyl



15
3
SO2
Phenyl



16
4
SO2
Phenyl



17
1
O
3-OH-Phenyl



18
2
O
3-OH-Phenyl



19
3
O
3-OH-Phenyl



20
4
O
3-OH-Phenyl



21
1
S
3-OH-Phenyl



22
2
S
3-OH-Phenyl



23
3
S
3-OH-Phenyl



24
4
S
3-OH-Phenyl



25
1
SO
3-OH-Phenyl



26
2
SO
3-OH-Phenyl



27
3
SO
3-OH-Phenyl



28
4
SO
3-OH-Phenyl



29
1
SO2
3-OH-Phenyl



30
2
SO2
3-OH-Phenyl



31
3
SO2
3-OH-Phenyl



32
4
SO2
3-OH-Phenyl



33
1
O
4-NO2-Phenyl



34
2
O
4-NO2-Phenyl



35
3
O
4-NO2-Phenyl



36
4
O
4-NO2-Phenyl



37
1
S
4-NO2-Phenyl



38
2
S
4-NO2-Phenyl



39
3
S
4-NO2-Phenyl



40
4
S
4-NO2-Phenyl



41
1
SO
4-NO2-Phenyl



42
2
SO
4-NO2-Phenyl



43
3
SO
4-NO2-Phenyl



44
4
SO
4-NO2-Phenyl



45
1
SO2
4-NO2-Phenyl



46
2
SO2
4-NO2-Phenyl



47
3
SO2
4-NO2-Phenyl



48
4
SO2
4-NO2-Phenyl



49
1
O
3-OMe-Phenyl



50
2
O
3-OMe-Phenyl



51
3
O
3-OMe-Phenyl



52
4
O
3-OMe-Phenyl



53
1
S
3-OMe-Phenyl



54
2
S
3-OMe-Phenyl



55
3
S
3-OMe-Phenyl



56
4
S
3-OMe-Phenyl



57
1
SO
3-OMe-Phenyl



58
2
SO
3-OMe-Phenyl



59
3
SO
3-OMe-Phenyl



60
4
SO
3-OMe-Phenyl



61
1
SO2
3-OMe-Phenyl



62
2
SO2
3-OMe-Phenyl



63
3
SO2
3-OMe-Phenyl



64
4
SO2
3-OMe-Phenyl



65
1
O
4-CN-Phenyl



66
2
O
4-CN-Phenyl



67
3
O
4-CN-Phenyl



68
4
O
4-CN-Phenyl



69
1
S
4-CN-Phenyl



70
2
S
4-CN-Phenyl



71
3
S
4-CN-Phenyl



72
4
S
4-CN-Phenyl



73
1
SO
4-CN-Phenyl



74
2
SO
4-CN-Phenyl



75
3
SO
4-CN-Phenyl



76
4
SO
4-CN-Phenyl



77
1
SO2
4-CN-Phenyl



78
2
SO2
4-CN-Phenyl



79
3
SO2
4-CN-Phenyl



80
4
SO2
4-CN-Phenyl



81
1
O
2-CN-Phenyl



82
2
O
2-CN-Phenyl



83
3
O
2-CN-Phenyl



84
4
O
2-CN-Phenyl



85
1
S
2-CN-Phenyl



86
2
S
2-CN-Phenyl



87
3
S
2-CN-Phenyl



88
4
S
2-CN-Phenyl



89
1
SO
2-CN-Phenyl



90
2
SO
2-CN-Phenyl



91
3
SO
2-CN-Phenyl



92
4
SO
2-CN-Phenyl



93
1
SO2
2-CN-Phenyl



94
2
SO2
2-CN-Phenyl



95
3
SO2
2-CN-Phenyl



96
4
SO2
2-CN-Phenyl



97
1
O
3-Me-Phenyl



98
2
O
3-Me-Phenyl



99
3
O
3-Me-Phenyl



100
4
O
3-Me-Phenyl



101
1
S
3-Me-Phenyl



102
2
S
3-Me-Phenyl



103
3
S
3-Me-Phenyl



104
4
S
3-Me-Phenyl



105
1
SO
3-Me-Phenyl



106
2
SO
3-Me-Phenyl



107
3
SO
3-Me-Phenyl



108
4
SO
3-Me-Phenyl



109
1
SO2
3-Me-Phenyl



110
2
SO2
3-Me-Phenyl



111
3
SO2
3-Me-Phenyl



112
4
SO2
3-Me-Phenyl



113
1
O
2-F-Phenyl



114
2
O
2-F-Phenyl



115
3
O
2-F-Phenyl



116
4
O
2-F-Phenyl



117
1
S
2-F-Phenyl



118
2
S
2-F-Phenyl



119
3
S
2-F-Phenyl



120
4
S
2-F-Phenyl



121
1
SO
2-F-Phenyl



122
2
SO
2-F-Phenyl



123
3
SO
2-F-Phenyl



124
4
SO
2-F-Phenyl



125
1
SO2
2-F-Phenyl



126
2
SO2
2-F-Phenyl



127
3
SO2
2-F-Phenyl



128
4
SO2
2-F-Phenyl



129
1
O
4-F-Phenyl



130
2
O
4-F-Phenyl



131
3
O
4-F-Phenyl



132
4
O
4-F-Phenyl



133
1
S
4-F-Phenyl



134
2
S
4-F-Phenyl



135
3
S
4-F-Phenyl



136
4
S
4-F-Phenyl



137
1
SO
4-F-Phenyl



138
2
SO
4-F-Phenyl



139
3
SO
4-F-Phenyl



140
4
SO
4-F-Phenyl



141
1
SO2
4-F-Phenyl



142
2
SO2
4-F-Phenyl



143
3
SO2
4-F-Phenyl



144
4
SO2
4-F-Phenyl



145
1
O
3-Cl-Phenyl



146
2
O
3-Cl-Phenyl



147
3
O
3-Cl-Phenyl



148
4
O
3-Cl-Phenyl



149
1
S
3-Cl-Phenyl



150
2
S
3-Cl-Phenyl



151
3
S
3-Cl-Phenyl



152
4
S
3-Cl-Phenyl



153
1
SO
3-Cl-Phenyl



154
2
SO
3-Cl-Phenyl



155
3
SO
3-Cl-Phenyl



156
4
SO
3-Cl-Phenyl



157
1
SO2
3-Cl-Phenyl



158
2
SO2
3-Cl-Phenyl



159
3
SO2
3-Cl-Phenyl



160
4
SO2
3-Cl-Phenyl



161
1
O
2-Br-Phenyl



162
2
O
2-Br-Phenyl



163
3
O
2-Br-Phenyl



164
4
O
2-Br-Phenyl



165
1
S
2-Br-Phenyl



166
2
S
2-Br-Phenyl



167
3
S
2-Br-Phenyl



168
4
S
2-Br-Phenyl



169
1
SO
2-Br-Phenyl



170
2
SO
2-Br-Phenyl



171
3
SO
2-Br-Phenyl



172
4
SO
2-Br-Phenyl



173
1
SO2
2-Br-Phenyl



174
2
SO2
2-Br-Phenyl



175
3
SO2
2-Br-Phenyl



176
4
SO2
2-Br-Phenyl



177
1
O
4-Br-Phenyl



178
2
O
4-Br-Phenyl



179
3
O
4-Br-Phenyl



180
4
O
4-Br-Phenyl



181
1
S
4-Br-Phenyl



182
2
S
4-Br-Phenyl



183
3
S
4-Br-Phenyl



184
4
S
4-Br-Phenyl



185
1
SO
4-Br-Phenyl



186
2
SO
4-Br-Phenyl



187
3
SO
4-Br-Phenyl



188
4
SO
4-Br-Phenyl



189
1
SO2
4-Br-Phenyl



190
2
SO2
4-Br-Phenyl



191
3
SO2
4-Br-Phenyl



192
4
SO2
4-Br-Phenyl



193
1
O
3-CF3-Phenyl



194
2
O
3-CF3-Phenyl



195
3
O
3-CF3-Phenyl



196
4
O
3-CF3-Phenyl



197
1
S
3-CF3-Phenyl



198
2
S
3-CF3-Phenyl



199
3
S
3-CF3-Phenyl



200
4
S
3-CF3-Phenyl



201
1
SO
3-CF3-Phenyl



202
2
SO
3-CF3-Phenyl



203
3
SO
3-CF3-Phenyl



204
4
SO
3-CF3-Phenyl



205
1
SO2
3-CF3-Phenyl



206
2
SO2
3-CF3-Phenyl



207
3
SO2
3-CF3-Phenyl



208
4
SO2
3-CF3-Phenyl



209
1
O
2-iPr-Phenyl



210
2
O
2-iPr-Phenyl



211
3
O
2-iPr-Phenyl



212
4
O
2-iPr-Phenyl



213
1
S
2-iPr-Phenyl



214
2
S
2-iPr-Phenyl



215
3
S
2-iPr-Phenyl



216
4
S
2-iPr-Phenyl



217
1
SO
2-iPr-Phenyl



218
2
SO
2-iPr-Phenyl



219
3
SO
2-iPr-Phenyl



220
4
SO
2-iPr-Phenyl



221
1
SO2
2-iPr-Phenyl



222
2
SO2
2-iPr-Phenyl



223
3
SO2
2-iPr-Phenyl



224
4
SO2
2-iPr-Phenyl



225
1
O
4-iPr-Phenyl



226
2
O
4-iPr-Phenyl



227
3
O
4-iPr-Phenyl



228
4
O
4-iPr-Phenyl



229
1
S
4-iPr-Phenyl



230
2
S
4-iPr-Phenyl



231
3
S
4-iPr-Phenyl



232
4
S
4-iPr-Phenyl



233
1
SO
4-iPr-Phenyl



234
2
SO
4-iPr-Phenyl



235
3
SO
4-iPr-Phenyl



236
4
SO
4-iPr-Phenyl



237
1
SO2
4-iPr-Phenyl



238
2
SO2
4-iPr-Phenyl



239
3
SO2
4-iPr-Phenyl



240
4
SO2
4-iPr-Phenyl



241
1
O
3-NH2-Phenyl



242
2
O
3-NH2-Phenyl



243
3
O
3-NH2-Phenyl



244
4
O
3-NH2-Phenyl



245
1
S
3-NH2-Phenyl



246
2
S
3-NH2-Phenyl



247
3
S
3-NH2-Phenyl



248
1
S
3-NH2-Phenyl



249
2
SO
3-NH2-Phenyl



250
3
SO
3-NH2-Phenyl



251
4
SO
3-NH2-Phenyl



252
1
SO
3-NH2-Phenyl



253
2
SO2
3-NH2-Phenyl



254
3
SO2
3-NH2-Phenyl



255
4
SO2
3-NH2-Phenyl



256
1
O
2,4-di-Me-Phenyl



257
2
O
2,4-di-Me-Phenyl



258
3
O
2,4-di-Me-Phenyl



259
4
O
2,4-di-Me-Phenyl



260
1
S
2,4-di-Me-Phenyl



261
2
S
2,4-di-Me-Phenyl



262
3
S
2,4-di-Me-Phenyl



263
4
S
2,4-di-Me-Phenyl



264
1
SO
2,4-di-Me-Phenyl



265
2
SO
2,4-di-Me-Phenyl



266
3
SO
2,4-di-Me-Phenyl



267
4
SO
2,4-di-Me-Phenyl



268
1
SO2
2,4-di-Me-Phenyl



269
2
SO2
2,4-di-Me-Phenyl



270
3
SO2
2,4-di-Me-Phenyl



271
4
SO2
2,4-di-Me-Phenyl



272
1
O
2,6-di-iPr-Phenyl



273
2
O
2,6-di-iPr-Phenyl



274
3
O
2,6-di-iPr-Phenyl



275
4
O
2,6-di-iPr-Phenyl



276
1
S
2,6-di-iPr-Phenyl



277
2
S
2,6-di-iPr-Phenyl



278
3
S
2,6-di-iPr-Phenyl



279
4
S
2,6-di-iPr-Phenyl



280
1
SO
2,6-di-iPr-Phenyl



281
2
SO
2,6-di-iPr-Phenyl



282
3
SO
2,6-di-iPr-Phenyl



283
4
SO
2,6-di-iPr-Phenyl



284
1
SO2
2,6-di-iPr-Phenyl



285
2
SO2
2,6-di-iPr-Phenyl



286
3
SO2
2,6-di-iPr-Phenyl



287
4
SO2
2,6-di-iPr-Phenyl



288
1
O
3-Ph-Phenyl



289
2
O
3-Ph-Phenyl



290
3
O
3-Ph-Phenyl



291
4
O
3-Ph-Phenyl



292
1
S
3-Ph-Phenyl



293
2
S
3-Ph-Phenyl



294
3
S
3-Ph-Phenyl



295
4
S
3-Ph-Phenyl



296
1
SO
3-Ph-Phenyl



297
2
SO
3-Ph-Phenyl



298
3
SO
3-Ph-Phenyl



299
4
SO
3-Ph-Phenyl



300
1
SO2
3-Ph-Phenyl



301
2
SO2
3-Ph-Phenyl



302
3
SO2
3-Ph-Phenyl



303
4
SO2
3-Ph-Phenyl



304
1
O
2-morpholino-phenyl



305
2
O
2-morpholino-phenyl



306
3
O
2-morpholino-phenyl



307
4
O
2-morpholino-phenyl



308
1
S
2-morpholino-phenyl



309
2
S
2-morpholino-phenyl



310
3
S
2-morpholino-phenyl



311
4
S
2-morpholino-phenyl



312
1
SO
2-morpholino-phenyl



313
2
SO
2-morpholino-phenyl



314
3
SO
2-morpholino-phenyl



315
4
SO
2-morpholino-phenyl



316
1
SO2
2-morpholino-phenyl



317
2
SO2
2-morpholino-phenyl



318
3
SO2
2-morpholino-phenyl



319
4
SO2
2-morpholino-phenyl



320
1
O
4-morpholino-phenyl



321
2
O
4-morpholino-phenyl



322
3
O
4-morpholino-phenyl



323
4
O
4-morpholino-phenyl



324
1
SO
4-morpholino-phenyl



325
2
SO
4-morpholino-phenyl



326
3
SO
4-morpholino-phenyl



327
4
SO
4-morpholino-phenyl



328
1
O
naphthylen-1-yl



329
2
O
naphthylen-1-yl



330
3
O
naphthylen-1-yl



331
4
O
naphthylen-1-yl



332
1
S
naphthylen-1-yl



333
2
S
naphthylen-1-yl



334
3
S
naphthylen-1-yl



335
4
S
naphthylen-1-yl



336
1
SO
naphthylen-1-yl



337
2
SO
naphthylen-1-yl



338
3
SO
naphthylen-1-yl



339
4
SO
naphthylen-1-yl



340
1
SO2
naphthylen-1-yl



341
2
SO2
naphthylen-1-yl



342
3
SO2
naphthylen-1-yl



343
4
SO2
naphthylen-1-yl



344
1
O
4-OH-Phenyl



345
2
O
4-OH-Phenyl



346
3
O
4-OH-Phenyl



347
4
O
4-OH-Phenyl



348
1
S
4-OH-Phenyl



349
2
S
4-OH-Phenyl



350
3
S
4-OH-Phenyl



351
4
S
4-OH-Phenyl



352
1
SO
4-OH-Phenyl



353
2
SO
4-OH-Phenyl



354
3
SO
4-OH-Phenyl



355
4
SO
4-OH-Phenyl



356
1
SO2
4-OH-Phenyl



357
2
SO2
4-OH-Phenyl



358
3
SO2
4-OH-Phenyl



359
4
SO2
4-OH-Phenyl



360
1
O
2-OH-Phenyl



361
2
O
2-OH-Phenyl



362
3
O
2-OH-Phenyl



363
4
O
2-OH-Phenyl



364
1
S
2-OH-Phenyl



365
2
S
2-OH-Phenyl



366
3
S
2-OH-Phenyl



367
4
S
2-OH-Phenyl



368
1
SO
2-OH-Phenyl



369
2
SO
2-OH-Phenyl



370
3
SO
2-OH-Phenyl



371
4
SO
2-OH-Phenyl



372
1
SO2
2-OH-Phenyl



373
2
SO2
2-OH-Phenyl



374
3
SO2
2-OH-Phenyl



375
4
SO2
2-OH-Phenyl



376
1
O
4-OMe-Phenyl



377
2
O
4-OMe-Phenyl



378
3
O
4-OMe-Phenyl



379
4
O
4-OMe-Phenyl



380
1
S
4-OMe-Phenyl



381
2
S
4-OMe-Phenyl



382
3
S
4-OMe-Phenyl



383
4
S
4-OMe-Phenyl



384
1
SO
4-OMe-Phenyl



385
2
SO
4-OMe-Phenyl



386
3
SO
4-OMe-Phenyl



387
4
SO
4-OMe-Phenyl



388
1
SO2
4-OMe-Phenyl



389
2
SO2
4-OMe-Phenyl



390
3
SO2
4-OMe-Phenyl



391
4
SO2
4-OMe-Phenyl



392
1
O
2-OMe-Phenyl



393
2
O
2-OMe-Phenyl



394
3
O
2-OMe-Phenyl



395
4
O
2-OMe-Phenyl



396
1
S
2-OMe-Phenyl



397
2
S
2-OMe-Phenyl



398
3
S
2-OMe-Phenyl



399
4
S
2-OMe-Phenyl



400
1
SO
2-OMe-Phenyl



401
2
SO
2-OMe-Phenyl



402
3
SO
2-OMe-Phenyl



403
4
SO
2-OMe-Phenyl



404
1
SO2
2-OMe-Phenyl



405
2
SO2
2-OMe-Phenyl



406
3
SO2
2-OMe-Phenyl



407
4
SO2
2-OMe-Phenyl



408
1
O
3-CN-Phenyl



409
2
O
3-CN-Phenyl



410
3
O
3-CN-Phenyl



411
4
O
3-CN-Phenyl



412
1
S
3-CN-Phenyl



413
2
S
3-CN-Phenyl



414
3
S
3-CN-Phenyl



415
4
S
3-CN-Phenyl



416
1
SO
3-CN-Phenyl



417
2
SO
3-CN-Phenyl



418
3
SO
3-CN-Phenyl



419
4
SO
3-CN-Phenyl



420
1
SO2
3-CN-Phenyl



421
2
SO2
3-CN-Phenyl



422
3
SO2
3-CN-Phenyl



423
4
SO2
3-CN-Phenyl



424
1
O
2-Me-Phenyl



425
2
O
2-Me-Phenyl



426
3
O
2-Me-Phenyl



427
4
O
2-Me-Phenyl



428
1
S
2-Me-Phenyl



429
2
S
2-Me-Phenyl



430
3
S
2-Me-Phenyl



431
4
S
2-Me-Phenyl



432
1
SO
2-Me-Phenyl



433
2
SO
2-Me-Phenyl



434
3
SO
2-Me-Phenyl



435
4
SO
2-Me-Phenyl



436
1
SO2
2-Me-Phenyl



437
2
SO2
2-Me-Phenyl



438
3
SO2
2-Me-Phenyl



439
4
SO2
2-Me-Phenyl



440
1
O
4-Me-Phenyl



441
2
O
4-Me-Phenyl



442
3
O
4-Me-Phenyl



443
4
O
4-Me-Phenyl



444
1
S
4-Me-Phenyl



445
2
S
4-Me-Phenyl



446
3
S
4-Me-Phenyl



447
4
S
4-Me-Phenyl



448
1
SO
4-Me-Phenyl



449
2
SO
4-Me-Phenyl



450
3
SO
4-Me-Phenyl



451
4
SO
4-Me-Phenyl



452
1
SO2
4-Me-Phenyl



453
2
SO2
4-Me-Phenyl



454
3
SO2
4-Me-Phenyl



455
4
SO2
4-Me-Phenyl



456
1
O
3-F-Phenyl



457
2
O
3-F-Phenyl



458
3
O
3-F-Phenyl



459
4
O
3-F-Phenyl



460
1
S
3-F-Phenyl



461
2
S
3-F-Phenyl



462
3
S
3-F-Phenyl



463
4
S
3-F-Phenyl



464
1
SO
3-F-Phenyl



465
2
SO
3-F-Phenyl



466
3
SO
3-F-Phenyl



467
4
SO
3-F-Phenyl



468
1
SO2
3-F-Phenyl



469
2
SO2
3-F-Phenyl



470
3
SO2
3-F-Phenyl



471
4
SO2
3-F-Phenyl



472
1
O
2-Cl-Phenyl



473
2
O
2-Cl-Phenyl



474
3
O
2-Cl-Phenyl



475
4
O
2-Cl-Phenyl



476
1
S
2-Cl-Phenyl



477
2
S
2-Cl-Phenyl



478
3
S
2-Cl-Phenyl



479
4
S
2-Cl-Phenyl



480
1
SO
2-Cl-Phenyl



481
2
SO
2-Cl-Phenyl



482
3
SO
2-Cl-Phenyl



483
4
SO
2-Cl-Phenyl



484
1
SO2
2-Cl-Phenyl



485
2
SO2
2-Cl-Phenyl



486
3
SO2
2-Cl-Phenyl



487
4
SO2
2-Cl-Phenyl



488
1
O
4-Cl-Phenyl



489
2
O
4-Cl-Phenyl



490
3
O
4-Cl-Phenyl



491
4
O
4-Cl-Phenyl



492
1
S
4-Cl-Phenyl



493
2
S
4-Cl-Phenyl



494
3
S
4-Cl-Phenyl



495
4
S
4-Cl-Phenyl



496
1
SO
4-Cl-Phenyl



497
2
SO
4-Cl-Phenyl



498
3
SO
4-Cl-Phenyl



499
4
SO
4-Cl-Phenyl



500
1
SO2
4-Cl-Phenyl



501
2
SO2
4-Cl-Phenyl



502
3
SO2
4-Cl-Phenyl



503
4
SO2
4-Cl-Phenyl



504
1
O
3-Br-Phenyl



505
2
O
3-Br-Phenyl



506
3
O
3-Br-Phenyl



507
4
O
3-Br-Phenyl



508
1
S
3-Br-Phenyl



509
2
S
3-Br-Phenyl



510
3
S
3-Br-Phenyl



511
4
S
3-Br-Phenyl



512
1
SO
3-Br-Phenyl



513
2
SO
3-Br-Phenyl



514
3
SO
3-Br-Phenyl



515
4
SO
3-Br-Phenyl



516
1
SO2
3-Br-Phenyl



517
2
SO2
3-Br-Phenyl



518
3
SO2
3-Br-Phenyl



519
4
SO2
3-Br-Phenyl



520
1
O
2-CF3-Phenyl



521
2
O
2-CF3-Phenyl



522
3
O
2-CF3-Phenyl



523
4
O
2-CF3-Phenyl



524
1
S
2-CF3-Phenyl



525
2
S
2-CF3-Phenyl



526
3
S
2-CF3-Phenyl



527
4
S
2-CF3-Phenyl



528
1
SO
2-CF3-Phenyl



529
2
SO
2-CF3-Phenyl



530
3
SO
2-CF3-Phenyl



531
4
SO
2-CF3-Phenyl



532
1
SO2
2-CF3-Phenyl



533
2
SO2
2-CF3-Phenyl



534
3
SO2
2-CF3-Phenyl



535
4
SO2
2-CF3-Phenyl



536
1
O
4-CF3-Phenyl



537
2
O
4-CF3-Phenyl



538
3
O
4-CF3-Phenyl



539
4
O
4-CF3-Phenyl



540
1
S
4-CF3-Phenyl



541
2
S
4-CF3-Phenyl



542
3
S
4-CF3-Phenyl



543
4
S
4-CF3-Phenyl



544
1
SO
4-CF3-Phenyl



545
2
SO
4-CF3-Phenyl



546
3
SO
4-CF3-Phenyl



547
4
SO
3-CF3-Phenyl



548
1
SO2
4-CF3-Phenyl



549
2
SO2
4-CF3-Phenyl



550
3
SO2
4-CF3-Phenyl



551
4
SO2
4-CF3-Phenyl



552
1
O
3-iPr-Phenyl



553
2
O
3-iPr-Phenyl



554
3
O
3-iPr-Phenyl



555
4
O
3-iPr-Phenyl



556
1
S
3-iPr-Phenyl



557
2
S
3-iPr-Phenyl



558
3
S
3-iPr-Phenyl



559
4
S
3-iPr-Phenyl



560
1
SO
3-iPr-Phenyl



561
2
SO
3-iPr-Phenyl



562
3
SO
3-iPr-Phenyl



563
4
SO
3-iPr-Phenyl



564
1
SO2
3-iPr-Phenyl



565
2
SO2
3-iPr-Phenyl



566
3
SO2
3-iPr-Phenyl



567
4
SO2
3-iPr-Phenyl



568
1
O
4-NH2-Phenyl



569
2
O
4-NH2-Phenyl



570
3
O
4-NH2-Phenyl



571
4
O
4-NH2-Phenyl



572
1
S
4-NH2-Phenyl



573
2
S
4-NH2-Phenyl



574
3
S
4-NH2-Phenyl



575
4
S
4-NH2-Phenyl



576
1
SO
4-NH2-Phenyl



577
2
SO
4-NH2-Phenyl



578
3
SO
4-NH2-Phenyl



579
4
SO
4-NH2-Phenyl



580
1
SO2
4-NH2-Phenyl



581
2
SO2
4-NH2-Phenyl



582
3
SO2
4-NH2-Phenyl



583
4
SO2
4-NH2-Phenyl



584
1
O
2-NH2-Phenyl



585
2
O
2-NH2-Phenyl



586
3
O
2-NH2-Phenyl



587
4
O
2-NH2-Phenyl



588
1
S
2-NH2-Phenyl



589
2
S
2-NH2-Phenyl



590
3
S
2-NH2-Phenyl



591
1
S
2-NH2-Phenyl



592
2
SO
2-NH2-Phenyl



593
3
SO
2-NH2-Phenyl



594
4
SO
2-NH2-Phenyl



595
1
SO
2-NH2-Phenyl



596
2
SO2
2-NH2-Phenyl



597
3
SO2
2-NH2-Phenyl



598
4
SO2
2-NH2-Phenyl



599
1
O
2,6-di-Me-Phenyl



600
2
O
2,6-di-Me-Phenyl



601
3
O
2,6-di-Me-Phenyl



602
4
O
2,6-di-Me-Phenyl



603
1
S
2,6-di-Me-Phenyl



604
2
S
2,6-di-Me-Phenyl



605
3
S
2,6-di-Me-Phenyl



606
4
S
2,6-di-Me-Phenyl



607
1
SO
2,6-di-Me-Phenyl



608
2
SO
2,6-di-Me-Phenyl



609
3
SO
2,6-di-Me-Phenyl



610
4
SO
2,6-di-Me-Phenyl



611
1
SO2
2,6-di-Me-Phenyl



612
2
SO2
2,6-di-Me-Phenyl



613
3
SO2
2,6-di-Me-Phenyl



614
4
SO2
2,6-di-Me-Phenyl



615
1
O
2-Ph-Phenyl



616
2
O
2-Ph-Phenyl



617
3
O
2-Ph-Phenyl



618
4
O
2-Ph-Phenyl



619
1
S
2-Ph-Phenyl



620
2
S
2-Ph-Phenyl



621
3
S
2-Ph-Phenyl



622
4
S
2-Ph-Phenyl



623
1
SO
2-Ph-Phenyl



624
2
SO
2-Ph-Phenyl



625
3
SO
2-Ph-Phenyl



626
4
SO
2-Ph-Phenyl



627
1
SO2
2-Ph-Phenyl



628
2
SO2
2-Ph-Phenyl



629
3
SO2
2-Ph-Phenyl



630
4
SO2
2-Ph-Phenyl



631
1
O
4-Ph-Phenyl



632
2
O
4-Ph-Phenyl



633
3
O
4-Ph-Phenyl



634
4
O
4-Ph-Phenyl



635
1
S
4-Ph-Phenyl



636
2
S
4-Ph-Phenyl



637
3
S
4-Ph-Phenyl



638
4
S
4-Ph-Phenyl



639
1
SO
4-Ph-Phenyl



640
2
SO
4-Ph-Phenyl



641
3
SO
4-Ph-Phenyl



642
4
SO
4-Ph-Phenyl



643
1
SO2
4-Ph-Phenyl



644
2
SO2
4-Ph-Phenyl



645
3
SO2
4-Ph-Phenyl



646
4
SO2
4-Ph-Phenyl



647
1
O
3-morpholino-phenyl



648
2
O
3-morpholino-phenyl



649
3
O
3-morpholino-phenyl



650
4
O
3-morpholino-phenyl



651
1
S
3-morpholino-phenyl



652
2
S
3-morpholino-phenyl



653
3
S
3-morpholino-phenyl



654
4
S
3-morpholino-phenyl



655
1
SO
3-morpholino-phenyl



656
2
SO
3-morpholino-phenyl



657
3
SO
3-morpholino-phenyl



658
4
SO
3-morpholino-phenyl



659
1
SO2
3-morpholino-phenyl



660
2
SO2
3-morpholino-phenyl



661
3
SO2
3-morpholino-phenyl



662
4
SO2
3-morpholino-phenyl



663
1
S
4-morpholino-phenyl



664
2
S
4-morpholino-phenyl



665
3
S
4-morpholino-phenyl



667
4
S
4-morpholino-phenyl



668
1
SO2
4-morpholino-phenyl



669
2
SO2
4-morpholino-phenyl



670
3
SO2
4-morpholino-phenyl



671
4
SO2
4-morpholino-phenyl



672
1
O
naphthylen-2-yl



673
2
O
naphthylen-2-yl



674
3
O
naphthylen-2-yl



675
4
O
naphthylen-2-yl



676
1
S
naphthylen-2-yl



678
2
S
naphthylen-2-yl



679
3
S
naphthylen-2-yl



680
4
S
naphthylen-2-yl



681
1
SO
naphthylen-2-yl



682
2
SO
naphthylen-2-yl



683
3
SO
naphthylen-2-yl



684
4
SO
naphthylen-2-yl



685
1
SO2
naphthylen-2-yl



686
2
SO2
naphthylen-2-yl



687
3
SO2
naphthylen-2-yl



688
4
SO2
naphthylen-2-yl









Exemplary embodiments include compounds having the formula (XXXVII)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 30.














TABLE 30







Entry
n
X
R3





















1
1
O
Phenyl



2
2
O
Phenyl



3
3
O
Phenyl



4
4
O
Phenyl



5
1
S
Phenyl



6
2
S
Phenyl



7
3
S
Phenyl



8
4
S
Phenyl



9
1
SO
Phenyl



10
2
SO
Phenyl



11
3
SO
Phenyl



12
4
SO
Phenyl



13
1
SO2
Phenyl



14
2
SO2
Phenyl



15
3
SO2
Phenyl



16
4
SO2
Phenyl



17
1
O
3-OH-Phenyl



18
2
O
3-OH-Phenyl



19
3
O
3-OH-Phenyl



20
4
O
3-OH-Phenyl



21
1
S
3-OH-Phenyl



22
2
S
3-OH-Phenyl



23
3
S
3-OH-Phenyl



24
4
S
3-OH-Phenyl



25
1
SO
3-OH-Phenyl



26
2
SO
3-OH-Phenyl



27
3
SO
3-OH-Phenyl



28
4
SO
3-OH-Phenyl



29
1
SO2
3-OH-Phenyl



30
2
SO2
3-OH-Phenyl



31
3
SO2
3-OH-Phenyl



32
4
SO2
3-OH-Phenyl



33
1
O
4-NO2-Phenyl



34
2
O
4-NO2-Phenyl



35
3
O
4-NO2-Phenyl



36
4
O
4-NO2-Phenyl



37
1
S
4-NO2-Phenyl



38
2
S
4-NO2-Phenyl



39
3
S
4-NO2-Phenyl



40
4
S
4-NO2-Phenyl



41
1
SO
4-NO2-Phenyl



42
2
SO
4-NO2-Phenyl



43
3
SO
4-NO2-Phenyl



44
4
SO
4-NO2-Phenyl



45
1
SO2
4-NO2-Phenyl



46
2
SO2
4-NO2-Phenyl



47
3
SO2
4-NO2-Phenyl



48
4
SO2
4-NO2-Phenyl



49
1
O
3-OMe-Phenyl



50
2
O
3-OMe-Phenyl



51
3
O
3-OMe-Phenyl



52
4
O
3-OMe-Phenyl



53
1
S
3-OMe-Phenyl



54
2
S
3-OMe-Phenyl



55
3
S
3-OMe-Phenyl



56
4
S
3-OMe-Phenyl



57
1
SO
3-OMe-Phenyl



58
2
SO
3-OMe-Phenyl



59
3
SO
3-OMe-Phenyl



60
4
SO
3-OMe-Phenyl



61
1
SO2
3-OMe-Phenyl



62
2
SO2
3-OMe-Phenyl



63
3
SO2
3-OMe-Phenyl



64
4
SO2
3-OMe-Phenyl



65
1
O
4-CN-Phenyl



66
2
O
4-CN-Phenyl



67
3
O
4-CN-Phenyl



68
4
O
4-CN-Phenyl



69
1
S
4-CN-Phenyl



70
2
S
4-CN-Phenyl



71
3
S
4-CN-Phenyl



72
4
S
4-CN-Phenyl



73
1
SO
4-CN-Phenyl



74
2
SO
4-CN-Phenyl



75
3
SO
4-CN-Phenyl



76
4
SO
4-CN-Phenyl



77
1
SO2
4-CN-Phenyl



78
2
SO2
4-CN-Phenyl



79
3
SO2
4-CN-Phenyl



80
4
SO2
4-CN-Phenyl



81
1
O
2-CN-Phenyl



82
2
O
2-CN-Phenyl



83
3
O
2-CN-Phenyl



84
4
O
2-CN-Phenyl



85
1
S
2-CN-Phenyl



86
2
S
2-CN-Phenyl



87
3
S
2-CN-Phenyl



88
4
S
2-CN-Phenyl



89
1
SO
2-CN-Phenyl



90
2
SO
2-CN-Phenyl



91
3
SO
2-CN-Phenyl



92
4
SO
2-CN-Phenyl



93
1
SO2
2-CN-Phenyl



94
2
SO2
2-CN-Phenyl



95
3
SO2
2-CN-Phenyl



96
4
SO2
2-CN-Phenyl



97
1
O
3-Me-Phenyl



98
2
O
3-Me-Phenyl



99
3
O
3-Me-Phenyl



100
4
O
3-Me-Phenyl



101
1
S
3-Me-Phenyl



102
2
S
3-Me-Phenyl



103
3
S
3-Me-Phenyl



104
4
S
3-Me-Phenyl



105
1
SO
3-Me-Phenyl



106
2
SO
3-Me-Phenyl



107
3
SO
3-Me-Phenyl



108
4
SO
3-Me-Phenyl



109
1
SO2
3-Me-Phenyl



110
2
SO2
3-Me-Phenyl



111
3
SO2
3-Me-Phenyl



112
4
SO2
3-Me-Phenyl



113
1
O
2-F-Phenyl



114
2
O
2-F-Phenyl



115
3
O
2-F-Phenyl



116
4
O
2-F-Phenyl



117
1
S
2-F-Phenyl



118
2
S
2-F-Phenyl



119
3
S
2-F-Phenyl



120
4
S
2-F-Phenyl



121
1
SO
2-F-Phenyl



122
2
SO
2-F-Phenyl



123
3
SO
2-F-Phenyl



124
4
SO
2-F-Phenyl



125
1
SO2
2-F-Phenyl



126
2
SO2
2-F-Phenyl



127
3
SO2
2-F-Phenyl



128
4
SO2
2-F-Phenyl



129
1
O
4-F-Phenyl



130
2
O
4-F-Phenyl



131
3
O
4-F-Phenyl



132
4
O
4-F-Phenyl



133
1
O
4-F-Phenyl



134
2
S
4-F-Phenyl



135
3
S
4-F-Phenyl



136
4
S
4-F-Phenyl



137
1
S
4-F-Phenyl



138
2
SO
4-F-Phenyl



139
3
SO
4-F-Phenyl



140
4
SO
4-F-Phenyl



141
1
SO
4-F-Phenyl



142
2
SO2
4-F-Phenyl



143
3
SO2
4-F-Phenyl



144
4
SO2
4-F-Phenyl



145
1
O
3-Cl-Phenyl



146
2
O
3-Cl-Phenyl



147
3
O
3-Cl-Phenyl



148
4
O
3-Cl-Phenyl



149
1
S
3-Cl-Phenyl



150
2
S
3-Cl-Phenyl



151
3
S
3-Cl-Phenyl



152
4
S
3-Cl-Phenyl



153
1
SO
3-Cl-Phenyl



154
2
SO
3-Cl-Phenyl



155
3
SO
3-Cl-Phenyl



156
4
SO
3-Cl-Phenyl



157
1
SO2
3-Cl-Phenyl



158
2
SO2
3-Cl-Phenyl



159
3
SO2
3-Cl-Phenyl



160
4
SO2
3-Cl-Phenyl



161
1
O
2-Br-Phenyl



162
2
O
2-Br-Phenyl



163
3
O
2-Br-Phenyl



164
4
O
2-Br-Phenyl



165
1
S
2-Br-Phenyl



166
2
S
2-Br-Phenyl



167
3
S
2-Br-Phenyl



168
4
S
2-Br-Phenyl



169
1
SO
2-Br-Phenyl



170
2
SO
2-Br-Phenyl



171
3
SO
2-Br-Phenyl



172
4
SO
2-Br-Phenyl



173
1
SO2
2-Br-Phenyl



174
2
SO2
2-Br-Phenyl



175
3
SO2
2-Br-Phenyl



176
4
SO2
2-Br-Phenyl



177
1
O
4-Br-Phenyl



178
2
O
4-Br-Phenyl



179
3
O
4-Br-Phenyl



180
4
O
4-Br-Phenyl



181
1
S
4-Br-Phenyl



182
2
S
4-Br-Phenyl



183
3
S
4-Br-Phenyl



184
4
S
4-Br-Phenyl



185
1
SO
4-Br-Phenyl



186
2
SO
4-Br-Phenyl



187
3
SO
4-Br-Phenyl



188
4
SO
4-Br-Phenyl



189
1
SO2
4-Br-Phenyl



190
2
SO2
4-Br-Phenyl



191
3
SO2
4-Br-Phenyl



192
4
SO2
4-Br-Phenyl



193
1
O
3-CF3-Phenyl



194
2
O
3-CF3-Phenyl



195
3
O
3-CF3-Phenyl



196
4
O
3-CF3-Phenyl



197
1
S
3-CF3-Phenyl



198
2
S
3-CF3-Phenyl



199
3
S
3-CF3-Phenyl



200
4
S
3-CF3-Phenyl



201
1
SO
3-CF3-Phenyl



202
2
SO
3-CF3-Phenyl



203
3
SO
3-CF3-Phenyl



204
4
SO
3-CF3-Phenyl



205
1
SO2
3-CF3-Phenyl



206
2
SO2
3-CF3-Phenyl



207
3
SO2
3-CF3-Phenyl



208
4
SO2
3-CF3-Phenyl



209
1
O
2-iPr-Phenyl



210
2
O
2-iPr-Phenyl



211
3
O
2-iPr-Phenyl



212
4
O
2-iPr-Phenyl



213
1
S
2-iPr-Phenyl



214
2
S
2-iPr-Phenyl



215
3
S
2-iPr-Phenyl



216
4
S
2-iPr-Phenyl



217
1
SO
2-iPr-Phenyl



218
2
SO
2-iPr-Phenyl



219
3
SO
2-iPr-Phenyl



220
4
SO
2-iPr-Phenyl



221
1
SO2
2-iPr-Phenyl



222
2
SO2
2-iPr-Phenyl



223
3
SO2
2-iPr-Phenyl



224
4
SO2
2-iPr-Phenyl



225
1
O
4-iPr-Phenyl



226
2
O
4-iPr-Phenyl



227
3
O
4-iPr-Phenyl



228
4
O
4-iPr-Phenyl



229
1
S
4-iPr-Phenyl



230
2
S
4-iPr-Phenyl



231
3
S
4-iPr-Phenyl



232
4
S
4-iPr-Phenyl



233
1
SO
4-iPr-Phenyl



234
2
SO
4-iPr-Phenyl



235
3
SO
4-iPr-Phenyl



236
4
SO
4-iPr-Phenyl



237
1
SO2
4-iPr-Phenyl



238
2
SO2
4-iPr-Phenyl



239
3
SO2
4-iPr-Phenyl



240
4
SO2
4-iPr-Phenyl



241
1
O
3-NH2-Phenyl



242
2
O
3-NH2-Phenyl



243
3
O
3-NH2-Phenyl



244
4
O
3-NH2-Phenyl



245
1
S
3-NH2-Phenyl



246
2
S
3-NH2-Phenyl



247
3
S
3-NH2-Phenyl



248
1
S
3-NH2-Phenyl



249
2
SO
3-NH2-Phenyl



250
3
SO
3-NH2-Phenyl



251
4
SO
3-NH2-Phenyl



252
1
SO
3-NH2-Phenyl



253
2
SO2
3-NH2-Phenyl



254
3
SO2
3-NH2-Phenyl



255
4
SO2
3-NH2-Phenyl



256
1
O
2,4-di-Me-Phenyl



257
2
O
2,4-di-Me-Phenyl



258
3
O
2,4-di-Me-Phenyl



259
4
O
2,4-di-Me-Phenyl



260
1
S
2,4-di-Me-Phenyl



261
2
S
2,4-di-Me-Phenyl



262
3
S
2,4-di-Me-Phenyl



263
4
S
2,4-di-Me-Phenyl



264
1
SO
2,4-di-Me-Phenyl



265
2
SO
2,4-di-Me-Phenyl



266
3
SO
2,4-di-Me-Phenyl



267
4
SO
2,4-di-Me-Phenyl



268
1
SO2
2,4-di-Me-Phenyl



269
2
SO2
2,4-di-Me-Phenyl



270
3
SO2
2,4-di-Me-Phenyl



271
4
SO2
2,4-di-Me-Phenyl



272
1
O
2,6-di-iPr-Phenyl



273
2
O
2,6-di-iPr-Phenyl



274
3
O
2,6-di-iPr-Phenyl



275
4
O
2,6-di-iPr-Phenyl



276
1
S
2,6-di-iPr-Phenyl



277
2
S
2,6-di-iPr-Phenyl



278
3
S
2,6-di-iPr-Phenyl



279
4
S
2,6-di-iPr-Phenyl



280
1
SO
2,6-di-iPr-Phenyl



281
2
SO
2,6-di-iPr-Phenyl



282
3
SO
2,6-di-iPr-Phenyl



283
4
SO
2,6-di-iPr-Phenyl



284
1
SO2
2,6-di-iPr-Phenyl



285
2
SO2
2,6-di-iPr-Phenyl



286
3
SO2
2,6-di-iPr-Phenyl



287
4
SO2
2,6-di-iPr-Phenyl



288
1
O
3-Ph-Phenyl



289
2
O
3-Ph-Phenyl



290
3
O
3-Ph-Phenyl



291
4
O
3-Ph-Phenyl



292
1
S
3-Ph-Phenyl



293
2
S
3-Ph-Phenyl



294
3
S
3-Ph-Phenyl



295
4
S
3-Ph-Phenyl



296
1
SO
3-Ph-Phenyl



297
2
SO
3-Ph-Phenyl



298
3
SO
3-Ph-Phenyl



299
4
SO
3-Ph-Phenyl



300
1
SO2
3-Ph-Phenyl



301
2
SO2
3-Ph-Phenyl



302
3
SO2
3-Ph-Phenyl



303
4
SO2
3-Ph-Phenyl



304
1
O
2-morpholino-phenyl



305
2
O
2-morpholino-phenyl



306
3
O
2-morpholino-phenyl



307
4
O
2-morpholino-phenyl



308
1
S
2-morpholino-phenyl



309
2
S
2-morpholino-phenyl



310
3
S
2-morpholino-phenyl



311
4
S
2-morpholino-phenyl



312
1
SO
2-morpholino-phenyl



313
2
SO
2-morpholino-phenyl



314
3
SO
2-morpholino-phenyl



315
4
SO
2-morpholino-phenyl



316
1
SO2
2-morpholino-phenyl



317
2
SO2
2-morpholino-phenyl



318
3
SO2
2-morpholino-phenyl



319
4
SO2
2-morpholino-phenyl



320
1
O
4-morpholino-phenyl



321
2
O
4-morpholino-phenyl



322
3
O
4-morpholino-phenyl



323
4
O
4-morpholino-phenyl



324
1
SO
4-morpholino-phenyl



325
2
SO
4-morpholino-phenyl



326
3
SO
4-morpholino-phenyl



327
4
SO
4-morpholino-phenyl



328
1
O
naphthylen-1-yl



329
2
O
naphthylen-1-yl



330
3
O
naphthylen-1-yl



331
4
O
naphthylen-1-yl



332
1
S
naphthylen-1-yl



333
2
S
naphthylen-1-yl



334
3
S
naphthylen-1-yl



335
4
S
naphthylen-1-yl



336
1
SO
naphthylen-1-yl



337
2
SO
naphthylen-1-yl



338
3
SO
naphthylen-1-yl



339
4
SO
naphthylen-1-yl



340
1
SO2
naphthylen-1-yl



341
2
SO2
naphthylen-1-yl



342
3
SO2
naphthylen-1-yl



343
4
SO2
naphthylen-1-yl



344
1
O
4-OH-Phenyl



345
2
O
4-OH-Phenyl



346
3
O
4-OH-Phenyl



347
4
O
4-OH-Phenyl



348
1
S
4-OH-Phenyl



349
2
S
4-OH-Phenyl



350
3
S
4-OH-Phenyl



351
4
S
4-OH-Phenyl



352
1
SO
4-OH-Phenyl



353
2
SO
4-OH-Phenyl



354
3
SO
4-OH-Phenyl



355
4
SO
4-OH-Phenyl



356
1
SO2
4-OH-Phenyl



357
2
SO2
4-OH-Phenyl



358
3
SO2
4-OH-Phenyl



359
4
SO2
4-OH-Phenyl



360
1
O
2-OH-Phenyl



361
2
O
2-OH-Phenyl



362
3
O
2-OH-Phenyl



363
4
O
2-OH-Phenyl



364
1
S
2-OH-Phenyl



365
2
S
2-OH-Phenyl



366
3
S
2-OH-Phenyl



367
4
S
2-OH-Phenyl



368
1
SO
2-OH-Phenyl



369
2
SO
2-OH-Phenyl



370
3
SO
2-OH-Phenyl



371
4
SO
2-OH-Phenyl



372
1
SO2
2-OH-Phenyl



373
2
SO2
2-OH-Phenyl



374
3
SO2
2-OH-Phenyl



375
4
SO2
2-OH-Phenyl



376
1
O
4-OMe-Phenyl



377
2
O
4-OMe-Phenyl



378
3
O
4-OMe-Phenyl



379
4
O
4-OMe-Phenyl



380
1
S
4-OMe-Phenyl



381
2
S
4-OMe-Phenyl



382
3
S
4-OMe-Phenyl



383
4
S
4-OMe-Phenyl



384
1
SO
4-OMe-Phenyl



385
2
SO
4-OMe-Phenyl



386
3
SO
4-OMe-Phenyl



387
4
SO
4-OMe-Phenyl



388
1
SO2
4-OMe-Phenyl



389
2
SO2
4-OMe-Phenyl



390
3
SO2
4-OMe-Phenyl



391
4
SO2
4-OMe-Phenyl



392
1
O
2-OMe-Phenyl



393
2
O
2-OMe-Phenyl



394
3
O
2-OMe-Phenyl



395
4
O
2-OMe-Phenyl



396
1
S
2-OMe-Phenyl



397
2
S
2-OMe-Phenyl



398
3
S
2-OMe-Phenyl



399
4
S
2-OMe-Phenyl



400
1
SO
2-OMe-Phenyl



401
2
SO
2-OMe-Phenyl



402
3
SO
2-OMe-Phenyl



403
4
SO
2-OMe-Phenyl



404
1
SO2
2-OMe-Phenyl



405
2
SO2
2-OMe-Phenyl



406
3
SO2
2-OMe-Phenyl



407
4
SO2
2-OMe-Phenyl



408
1
O
3-CN-Phenyl



409
2
O
3-CN-Phenyl



410
3
O
3-CN-Phenyl



411
4
O
3-CN-Phenyl



412
1
S
3-CN-Phenyl



413
2
S
3-CN-Phenyl



414
3
S
3-CN-Phenyl



415
4
S
3-CN-Phenyl



416
1
SO
3-CN-Phenyl



417
2
SO
3-CN-Phenyl



418
3
SO
3-CN-Phenyl



419
4
SO
3-CN-Phenyl



420
1
SO2
3-CN-Phenyl



421
2
SO2
3-CN-Phenyl



422
3
SO2
3-CN-Phenyl



423
4
SO2
3-CN-Phenyl



424
1
O
2-Me-Phenyl



425
2
O
2-Me-Phenyl



426
3
O
2-Me-Phenyl



427
4
O
2-Me-Phenyl



428
1
S
2-Me-Phenyl



429
2
S
2-Me-Phenyl



430
3
S
2-Me-Phenyl



431
4
S
2-Me-Phenyl



432
1
SO
2-Me-Phenyl



433
2
SO
2-Me-Phenyl



434
3
SO
2-Me-Phenyl



435
4
SO
2-Me-Phenyl



436
1
SO2
2-Me-Phenyl



437
2
SO2
2-Me-Phenyl



438
3
SO2
2-Me-Phenyl



439
4
SO2
2-Me-Phenyl



440
1
O
4-Me-Phenyl



441
2
O
4-Me-Phenyl



442
3
O
4-Me-Phenyl



443
4
O
4-Me-Phenyl



444
1
S
4-Me-Phenyl



445
2
S
4-Me-Phenyl



446
3
S
4-Me-Phenyl



447
4
S
4-Me-Phenyl



448
1
SO
4-Me-Phenyl



449
2
SO
4-Me-Phenyl



450
3
SO
4-Me-Phenyl



451
4
SO
4-Me-Phenyl



452
1
SO2
4-Me-Phenyl



453
2
SO2
4-Me-Phenyl



454
3
SO2
4-Me-Phenyl



455
4
SO2
4-Me-Phenyl



456
1
O
3-F-Phenyl



457
2
O
3-F-Phenyl



458
3
O
3-F-Phenyl



459
4
O
3-F-Phenyl



460
1
S
3-F-Phenyl



461
2
S
3-F-Phenyl



462
3
S
3-F-Phenyl



463
4
S
3-F-Phenyl



464
1
SO
3-F-Phenyl



465
2
SO
3-F-Phenyl



466
3
SO
3-F-Phenyl



467
4
SO
3-F-Phenyl



468
1
SO2
3-F-Phenyl



469
2
SO2
3-F-Phenyl



470
3
SO2
3-F-Phenyl



471
4
SO2
3-F-Phenyl



472
1
O
2-Cl-Phenyl



473
2
O
2-Cl-Phenyl



474
3
O
2-Cl-Phenyl



475
4
O
2-Cl-Phenyl



476
1
S
2-Cl-Phenyl



477
2
S
2-Cl-Phenyl



478
3
S
2-Cl-Phenyl



479
4
S
2-Cl-Phenyl



480
1
SO
2-Cl-Phenyl



481
2
SO
2-Cl-Phenyl



482
3
SO
2-Cl-Phenyl



483
4
SO
2-Cl-Phenyl



484
1
SO2
2-Cl-Phenyl



485
2
SO2
2-Cl-Phenyl



486
3
SO2
2-Cl-Phenyl



487
4
SO2
2-Cl-Phenyl



488
1
O
4-Cl-Phenyl



489
2
O
4-Cl-Phenyl



490
3
O
4-Cl-Phenyl



491
4
O
4-Cl-Phenyl



492
1
S
4-Cl-Phenyl



493
2
S
4-Cl-Phenyl



494
3
S
4-Cl-Phenyl



495
4
S
4-Cl-Phenyl



496
1
SO
4-Cl-Phenyl



497
2
SO
4-Cl-Phenyl



498
3
SO
4-Cl-Phenyl



499
4
SO
4-Cl-Phenyl



500
1
SO2
4-Cl-Phenyl



501
2
SO2
4-Cl-Phenyl



502
3
SO2
4-Cl-Phenyl



503
4
SO2
4-Cl-Phenyl



504
1
O
3-Br-Phenyl



505
2
O
3-Br-Phenyl



506
3
O
3-Br-Phenyl



507
4
O
3-Br-Phenyl



508
1
S
3-Br-Phenyl



509
2
S
3-Br-Phenyl



510
3
S
3-Br-Phenyl



511
4
S
3-Br-Phenyl



512
1
SO
3-Br-Phenyl



513
2
SO
3-Br-Phenyl



514
3
SO
3-Br-Phenyl



515
4
SO
3-Br-Phenyl



516
1
SO2
3-Br-Phenyl



517
2
SO2
3-Br-Phenyl



518
3
SO2
3-Br-Phenyl



519
4
SO2
3-Br-Phenyl



520
1
O
2-CF3-Phenyl



521
2
O
2-CF3-Phenyl



522
3
O
2-CF3-Phenyl



523
4
O
2-CF3-Phenyl



524
1
S
2-CF3-Phenyl



525
2
S
2-CF3-Phenyl



526
3
S
2-CF3-Phenyl



527
4
S
2-CF3-Phenyl



528
1
SO
2-CF3-Phenyl



529
2
SO
2-CF3-Phenyl



530
3
SO
2-CF3-Phenyl



531
4
SO
2-CF3-Phenyl



532
1
SO2
2-CF3-Phenyl



533
2
SO2
2-CF3-Phenyl



534
3
SO2
2-CF3-Phenyl



535
4
SO2
2-CF3-Phenyl



536
1
O
4-CF3-Phenyl



537
2
O
4-CF3-Phenyl



538
3
O
4-CF3-Phenyl



539
4
O
4-CF3-Phenyl



540
1
S
4-CF3-Phenyl



541
2
S
4-CF3-Phenyl



542
3
S
4-CF3-Phenyl



543
4
S
4-CF3-Phenyl



544
1
SO
4-CF3-Phenyl



545
2
SO
4-CF3-Phenyl



546
3
SO
4-CF3-Phenyl



547
4
SO
3-CF3-Phenyl



548
1
SO2
4-CF3-Phenyl



549
2
SO2
4-CF3-Phenyl



550
3
SO2
4-CF3-Phenyl



551
4
SO2
4-CF3-Phenyl



552
1
O
3-iPr-Phenyl



553
2
O
3-iPr-Phenyl



554
3
O
3-iPr-Phenyl



555
4
O
3-iPr-Phenyl



556
1
S
3-iPr-Phenyl



557
2
S
3-iPr-Phenyl



558
3
S
3-iPr-Phenyl



559
4
S
3-iPr-Phenyl



560
1
SO
3-iPr-Phenyl



561
2
SO
3-iPr-Phenyl



562
3
SO
3-iPr-Phenyl



563
4
SO
3-iPr-Phenyl



564
1
SO2
3-iPr-Phenyl



565
2
SO2
3-iPr-Phenyl



566
3
SO2
3-iPr-Phenyl



567
4
SO2
3-iPr-Phenyl



568
1
O
4-NH2-Phenyl



569
2
O
4-NH2-Phenyl



570
3
O
4-NH2-Phenyl



571
4
O
4-NH2-Phenyl



572
1
S
4-NH2-Phenyl



573
2
S
4-NH2-Phenyl



574
3
S
4-NH2-Phenyl



575
4
S
4-NH2-Phenyl



576
1
SO
4-NH2-Phenyl



577
2
SO
4-NH2-Phenyl



578
3
SO
4-NH2-Phenyl



579
4
SO
4-NH2-Phenyl



580
1
SO2
4-NH2-Phenyl



581
2
SO2
4-NH2-Phenyl



582
3
SO2
4-NH2-Phenyl



583
4
SO2
4-NH2-Phenyl



584
1
O
2-NH2-Phenyl



585
2
O
2-NH2-Phenyl



586
3
O
2-NH2-Phenyl



587
4
O
2-NH2-Phenyl



588
1
S
2-NH2-Phenyl



589
2
S
2-NH2-Phenyl



590
3
S
2-NH2-Phenyl



591
1
S
2-NH2-Phenyl



592
2
SO
2-NH2-Phenyl



593
3
SO
2-NH2-Phenyl



594
4
SO
2-NH2-Phenyl



595
1
SO
2-NH2-Phenyl



596
2
SO2
2-NH2-Phenyl



597
3
SO2
2-NH2-Phenyl



598
4
SO2
2-NH2-Phenyl



599
1
O
2,6-di-Me-Phenyl



600
2
O
2,6-di-Me-Phenyl



601
3
O
2,6-di-Me-Phenyl



602
4
O
2,6-di-Me-Phenyl



603
1
S
2,6-di-Me-Phenyl



604
2
S
2,6-di-Me-Phenyl



605
3
S
2,6-di-Me-Phenyl



606
4
S
2,6-di-Me-Phenyl



607
1
SO
2,6-di-Me-Phenyl



608
2
SO
2,6-di-Me-Phenyl



609
3
SO
2,6-di-Me-Phenyl



610
4
SO
2,6-di-Me-Phenyl



611
1
SO2
2,6-di-Me-Phenyl



612
2
SO2
2,6-di-Me-Phenyl



613
3
SO2
2,6-di-Me-Phenyl



614
4
SO2
2,6-di-Me-Phenyl



615
1
O
2-Ph-Phenyl



616
2
O
2-Ph-Phenyl



617
3
O
2-Ph-Phenyl



618
4
O
2-Ph-Phenyl



619
1
S
2-Ph-Phenyl



620
2
S
2-Ph-Phenyl



621
3
S
2-Ph-Phenyl



622
4
S
2-Ph-Phenyl



623
1
SO
2-Ph-Phenyl



624
2
SO
2-Ph-Phenyl



625
3
SO
2-Ph-Phenyl



626
4
SO
2-Ph-Phenyl



627
1
SO2
2-Ph-Phenyl



628
2
SO2
2-Ph-Phenyl



629
3
SO2
2-Ph-Phenyl



630
4
SO2
2-Ph-Phenyl



631
1
O
4-Ph-Phenyl



632
2
O
4-Ph-Phenyl



633
3
O
4-Ph-Phenyl



634
4
O
4-Ph-Phenyl



635
1
S
4-Ph-Phenyl



636
2
S
4-Ph-Phenyl



637
3
S
4-Ph-Phenyl



638
4
S
4-Ph-Phenyl



639
1
SO
4-Ph-Phenyl



640
2
SO
4-Ph-Phenyl



641
3
SO
4-Ph-Phenyl



642
4
SO
4-Ph-Phenyl



643
1
SO2
4-Ph-Phenyl



644
2
SO2
4-Ph-Phenyl



645
3
SO2
4-Ph-Phenyl



646
4
SO2
4-Ph-Phenyl



647
1
O
3-morpholino-phenyl



648
2
O
3-morpholino-phenyl



649
3
O
3-morpholino-phenyl



650
4
O
3-morpholino-phenyl



651
1
S
3-morpholino-phenyl



652
2
S
3-morpholino-phenyl



653
3
S
3-morpholino-phenyl



654
4
S
3-morpholino-phenyl



655
1
SO
3-morpholino-phenyl



656
2
SO
3-morpholino-phenyl



657
3
SO
3-morpholino-phenyl



658
4
SO
3-morpholino-phenyl



659
1
SO2
3-morpholino-phenyl



660
2
SO2
3-morpholino-phenyl



661
3
SO2
3-morpholino-phenyl



662
4
SO2
3-morpholino-phenyl



663
1
S
4-morpholino-phenyl



664
2
S
4-morpholino-phenyl



665
3
S
4-morpholino-phenyl



667
4
S
4-morpholino-phenyl



668
1
SO2
4-morpholino-phenyl



669
2
SO2
4-morpholino-phenyl



670
3
SO2
4-morpholino-phenyl



671
4
SO2
4-morpholino-phenyl



672
1
O
naphthylen-2-yl



673
2
O
naphthylen-2-yl



674
3
O
naphthylen-2-yl



675
4
O
naphthylen-2-yl



676
1
S
naphthylen-2-yl



678
2
S
naphthylen-2-yl



679
3
S
naphthylen-2-yl



680
4
S
naphthylen-2-yl



681
1
SO
naphthylen-2-yl



682
2
SO
naphthylen-2-yl



683
3
SO
naphthylen-2-yl



684
4
SO
naphthylen-2-yl



685
1
SO2
naphthylen-2-yl



686
2
SO2
naphthylen-2-yl



687
3
SO2
naphthylen-2-yl



688
4
SO2
naphthylen-2-yl










Exemplary embodiments include compounds having the formula (XXXVIII)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 31












TABLE 31





Entry
n
R3
R10c


















1
1
4-CH3-phenyl
Ethyl


2
1
4-CH3-phenyl
n-propyl


3
1
4-CH3-phenyl
Isopropyl


4
1
4-CH3-phenyl
—CH2CH(CH3)2


5
1
4-CH3-phenyl
CF3


6
1
4-CH3-phenyl
—CH2CF3


7
1
4-CH3-phenyl
—CH2CH2CF3


8
1
4-CH3-phenyl
Cyclopropyl


9
1
4-CH3-phenyl
Cyclobutyl


10
1
4-CH3-phenyl
Cyclopentyl


11
1
4-CH3-phenyl
Cyclohexyl


12
1
4-CH3-phenyl
3-pyridyl


13
1
4-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


14
1
4-CH3-phenyl
1H-imidazol-4-yl


15
1
4-CH3-phenyl
2-furanyl


16
1
4-CH3-phenyl
Ethyl


17
1
4-CH3-phenyl
n-propyl


18
1
4-CH3-phenyl
Isopropyl


19
1
4-CH3-phenyl
—CH2CH(CH3)2


20
1
4-CH3-phenyl
CF3


21
1
4-CH3-phenyl
—CH2CF3


22
1
4-CH3-phenyl
—CH2CH2CF3


23
1
4-CH3-phenyl
Cyclopropyl


24
1
4-CH3-phenyl
Cyclobutyl


25
1
4-CH3-phenyl
Cyclopentyl


26
1
4-CH3-phenyl
Cyclohexyl


27
1
4-CH3-phenyl
3-pyridyl


28
1
4-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


29
1
4-CH3-phenyl
1H-imidazol-4-yl


30
1
4-CH3-phenyl
2-furanyl


31
1
3-OH-Phenyl
Ethyl


32
1
3-OH-Phenyl
n-propyl


33
1
3-OH-Phenyl
Isopropyl


34
1
3-OH-Phenyl
—CH2CH(CH3)2


35
1
3-OH-Phenyl
CF3


36
1
3-OH-Phenyl
—CH2CF3


37
1
3-OH-Phenyl
—CH2CH2CF3


38
1
3-OH-Phenyl
Cyclopropyl


39
1
3-OH-Phenyl
Cyclobutyl


40
1
3-OH-Phenyl
Cyclopentyl


41
1
3-OH-Phenyl
Cyclohexyl


42
1
3-OH-Phenyl
3-pyridyl


43
1
3-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


44
1
3-OH-Phenyl
1H-imidazol-4-yl


45
1
3-OH-Phenyl
2-furanyl


46
1
4-OMe-Phenyl
Ethyl


47
1
4-OMe-Phenyl
n-propyl


48
1
4-OMe-Phenyl
Isopropyl


49
1
4-OMe-Phenyl
—CH2CH(CH3)2


50
1
4-OMe-Phenyl
CF3


51
1
4-OMe-Phenyl
—CH2CF3


52
1
4-OMe-Phenyl
—CH2CH2CF3


53
1
4-OMe-Phenyl
Cyclopropyl


54
1
4-OMe-Phenyl
Cyclobutyl


55
1
4-OMe-Phenyl
Cyclopentyl


56
1
4-OMe-Phenyl
Cyclohexyl


57
1
4-OMe-Phenyl
3-pyridyl


58
1
4-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


59
1
4-OMe-Phenyl
1H-imidazol-4-yl


60
1
4-OMe-Phenyl
2-furanyl


61
1
2-OMe-Phenyl
Ethyl


62
1
2-OMe-Phenyl
n-propyl


63
1
2-OMe-Phenyl
Isopropyl


64
1
2-OMe-Phenyl
—CH2CH(CH3)2


65
1
2-OMe-Phenyl
CF3


66
1
2-OMe-Phenyl
—CH2CF3


67
1
2-OMe-Phenyl
—CH2CH2CF3


68
1
2-OMe-Phenyl
Cyclopropyl


69
1
2-OMe-Phenyl
Cyclobutyl


70
1
2-OMe-Phenyl
Cyclopentyl


71
1
2-OMe-Phenyl
Cyclohexyl


72
1
2-OMe-Phenyl
3-pyridyl


73
1
2-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


74
1
2-OMe-Phenyl
1H-imidazol-4-yl


75
1
2-OMe-Phenyl
2-furanyl


76
1
3-CN-Phenyl
Ethyl


77
1
3-CN-Phenyl
n-propyl


78
1
3-CN-Phenyl
Isopropyl


79
1
3-CN-Phenyl
—CH2CH(CH3)2


80
1
3-CN-Phenyl
CF3


81
1
3-CN-Phenyl
—CH2CF3


82
1
3-CN-Phenyl
—CH2CH2CF3


83
1
3-CN-Phenyl
Cyclopropyl


84
1
3-CN-Phenyl
Cyclobutyl


85
1
3-CN-Phenyl
Cyclopentyl


86
1
3-CN-Phenyl
Cyclohexyl


87
1
3-CN-Phenyl
3-pyridyl


88
1
3-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


89
1
3-CN-Phenyl
1H-imidazol-4-yl


90
1
3-CN-Phenyl
2-furanyl


91
1
2-F-Phenyl
Ethyl


92
1
2-F-Phenyl
n-propyl


93
1
2-F-Phenyl
Isopropyl


94
1
2-F-Phenyl
—CH2CH(CH3)2


95
1
2-F-Phenyl
CF3


96
1
2-F-Phenyl
—CH2CF3


97
1
2-F-Phenyl
—CH2CH2CF3


98
1
2-F-Phenyl
Cyclopropyl


99
1
2-F-Phenyl
Cyclobutyl


100
1
2-F-Phenyl
Cyclopentyl


101
1
2-F-Phenyl
Cyclohexyl


102
1
2-F-Phenyl
3-pyridyl


103
1
2-F-Phenyl
1-methyl-1H-pyrazol-4-yl


104
1
2-F-Phenyl
1H-imidazol-4-yl


105
1
2-F-Phenyl
2-furanyl


106
1
4-F-Phenyl
Ethyl


107
1
4-F-Phenyl
n-propyl


108
1
4-F-Phenyl
Isopropyl


109
1
4-F-Phenyl
—CH2CH(CH3)2


110
1
4-F-Phenyl
CF3


111
1
4-F-Phenyl
—CH2CF3


112
1
4-F-Phenyl
—CH2CH2CF3


113
1
4-F-Phenyl
Cyclopropyl


114
1
4-F-Phenyl
Cyclobutyl


115
1
4-F-Phenyl
Cyclopentyl


116
1
4-F-Phenyl
Cyclohexyl


117
1
4-F-Phenyl
3-pyridyl


118
1
4-F-Phenyl
1-methyl-1H-pyrazol-4-yl


119
1
4-F-Phenyl
1H-imidazol-4-yl


120
1
4-F-Phenyl
2-furanyl


121
1
3-Cl-Phenyl
Ethyl


122
1
3-Cl-Phenyl
n-propyl


123
1
3-Cl-Phenyl
Isopropyl


124
1
3-Cl-Phenyl
—CH2CH(CH3)2


125
1
3-Cl-Phenyl
CF3


126
1
3-Cl-Phenyl
—CH2CF3


127
1
3-Cl-Phenyl
—CH2CH2CF3


128
1
3-Cl-Phenyl
Cyclopropyl


129
1
3-Cl-Phenyl
Cyclobutyl


130
1
3-Cl-Phenyl
Cyclopentyl


131
1
3-Cl-Phenyl
Cyclohexyl


132
1
3-Cl-Phenyl
3-pyridyl


133
1
3-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


134
1
3-Cl-Phenyl
1H-imidazol-4-yl


135
1
3-Cl-Phenyl
2-furanyl


136
1
2-Br-Phenyl
ethyl


137
1
2-Br-Phenyl
n-propyl


138
1
2-Br-Phenyl
isopropyl


139
1
2-Br-Phenyl
—CH2CH(CH3)2


140
1
2-Br-Phenyl
CF3


141
1
2-Br-Phenyl
—CH2CF3


142
1
2-Br-Phenyl
—CH2CH2CF3


143
1
2-Br-Phenyl
cyclopropyl


144
1
2-Br-Phenyl
Cyclobutyl


145
1
2-Br-Phenyl
cyclopentyl


146
1
2-Br-Phenyl
cyclohexyl


147
1
2-Br-Phenyl
3-pyridyl


148
1
2-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


149
1
2-Br-Phenyl
1H-imidazol-4-yl


150
1
2-Br-Phenyl
2-furanyl


151
1
4-Br-Phenyl
ethyl


152
1
4-Br-Phenyl
n-propyl


153
1
4-Br-Phenyl
isopropyl


154
1
4-Br-Phenyl
—CH2CH(CH3)2


155
1
4-Br-Phenyl
CF3


156
1
4-Br-Phenyl
—CH2CF3


157
1
4-Br-Phenyl
—CH2CH2CF3


158
1
4-Br-Phenyl
cyclopropyl


159
1
4-Br-Phenyl
Cyclobutyl


160
1
4-Br-Phenyl
cyclopentyl


161
1
4-Br-Phenyl
cyclohexyl


162
1
4-Br-Phenyl
3-pyridyl


163
1
4-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


164
1
4-Br-Phenyl
1H-imidazol-4-yl


165
1
4-Br-Phenyl
2-furanyl


166
1
3-CF3-Phenyl
ethyl


167
1
3-CF3-Phenyl
n-propyl


168
1
3-CF3-Phenyl
isopropyl


169
1
3-CF3-Phenyl
—CH2CH(CH3)2


170
1
3-CF3-Phenyl
CF3


171
1
3-CF3-Phenyl
—CH2CF3


172
1
3-CF3-Phenyl
—CH2CH2CF3


173
1
3-CF3-Phenyl
cyclopropyl


174
1
3-CF3-Phenyl
Cyclobutyl


175
1
3-CF3-Phenyl
cyclopentyl


176
1
3-CF3-Phenyl
cyclohexyl


177
1
3-CF3-Phenyl
3-pyridyl


178
1
3-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


179
1
3-CF3-Phenyl
1H-imidazol-4-yl


180
1
3-CF3-Phenyl
2-furanyl


181
1
2-iPr-Phenyl
ethyl


182
1
2-iPr-Phenyl
n-propyl


183
1
2-iPr-Phenyl
isopropyl


184
1
2-iPr-Phenyl
—CH2CH(CH3)2


185
1
2-iPr-Phenyl
CF3


186
1
2-iPr-Phenyl
—CH2CF3


187
1
2-iPr-Phenyl
—CH2CH2CF3


188
1
2-iPr-Phenyl
cyclopropyl


189
1
2-iPr-Phenyl
Cyclobutyl


190
1
2-iPr-Phenyl
cyclopentyl


191
1
2-iPr-Phenyl
cyclohexyl


192
1
2-iPr-Phenyl
3-pyridyl


193
1
2-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


194
1
2-iPr-Phenyl
1H-imidazol-4-yl


195
1
2-iPr-Phenyl
2-furanyl


196
1
4-iPr-Phenyl
ethyl


197
1
4-iPr-Phenyl
n-propyl


198
1
4-iPr-Phenyl
isopropyl


199
1
4-iPr-Phenyl
—CH2CH(CH3)2


200
1
4-iPr-Phenyl
CF3


201
1
4-iPr-Phenyl
—CH2CF3


202
1
4-iPr-Phenyl
—CH2CH2CF3


203
1
4-iPr-Phenyl
cyclopropyl


204
1
4-iPr-Phenyl
Cyclobutyl


205
1
4-iPr-Phenyl
cyclopentyl


206
1
4-iPr-Phenyl
cyclohexyl


207
1
4-iPr-Phenyl
3-pyridyl


208
1
4-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


209
1
4-iPr-Phenyl
1H-imidazol-4-yl


210
1
4-iPr-Phenyl
2-furanyl


211
1
3-morpholino-phenyl
ethyl


212
1
3-morpholino-phenyl
n-propyl


213
1
3-morpholino-phenyl
isopropyl


214
1
3-morpholino-phenyl
—CH2CH(CH3)2


215
1
3-morpholino-phenyl
CF3


216
1
3-morpholino-phenyl
—CH2CF3


217
1
3-morpholino-phenyl
—CH2CH2CF3


218
1
3-morpholino-phenyl
cyclopropyl


219
1
3-morpholino-phenyl
Cyclobutyl


220
1
3-morpholino-phenyl
cyclopentyl


221
1
3-morpholino-phenyl
cyclohexyl


222
1
3-morpholino-phenyl
3-pyridyl


223
1
3-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


224
1
3-morpholino-phenyl
1H-imidazol-4-yl


225
1
3-morpholino-phenyl
2-furanyl


226
1
4-cyano-2-morpholino-phenyl
ethyl


227
1
4-cyano-2-morpholino-phenyl
n-propyl


228
1
4-cyano-2-morpholino-phenyl
isopropyl


229
1
4-cyano-2-morpholino-phenyl
—CH2CH(CH3)2


230
1
4-cyano-2-morpholino-phenyl
CF3


231
1
4-cyano-2-morpholino-phenyl
—CH2CF3


232
1
4-cyano-2-morpholino-phenyl
—CH2CH2CF3


233
1
4-cyano-2-morpholino-phenyl
cyclopropyl


234
1
4-cyano-2-morpholino-phenyl
Cyclobutyl


235
1
4-cyano-2-morpholino-phenyl
cyclopentyl


236
1
4-cyano-2-morpholino-phenyl
cyclohexyl


237
1
4-cyano-2-morpholino-phenyl
3-pyridyl


238
1
4-cyano-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


239
1
4-cyano-2-morpholino-phenyl
1H-imidazol-4-yl


240
1
4-cyano-2-morpholino-phenyl
2-furanyl


241
1
4-hydroxy-2-morpholino-phenyl
ethyl


242
1
4-hydroxy-2-morpholino-phenyl
n-propyl


243
1
4-hydroxy-2-morpholino-phenyl
isopropyl


244
1
4-hydroxy-2-morpholino-phenyl
—CH2CH(CH3)2


245
1
4-hydroxy-2-morpholino-phenyl
CF3


246
1
4-hydroxy-2-morpholino-phenyl
—CH2CF3


247
1
4-hydroxy-2-morpholino-phenyl
—CH2CH2CF3


248
1
4-hydroxy-2-morpholino-phenyl
cyclopropyl


249
1
4-hydroxy-2-morpholino-phenyl
Cyclobutyl


250
1
4-hydroxy-2-morpholino-phenyl
cyclopentyl


251
1
4-hydroxy-2-morpholino-phenyl
cyclohexyl


252
1
4-hydroxy-2-morpholino-phenyl
3-pyridyl


253
1
4-hydroxy-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


254
1
4-hydroxy-2-morpholino-phenyl
1H-imidazol-4-yl


255
1
4-hydroxy-2-morpholino-phenyl
2-furanyl


256
1
2-CH3-phenyl
Ethyl


257
1
2-CH3-phenyl
n-propyl


258
1
2-CH3-phenyl
Isopropyl


259
1
2-CH3-phenyl
—CH2CH(CH3)2


260
1
2-CH3-phenyl
CF3


261
1
2-CH3-phenyl
—CH2CF3


262
1
2-CH3-phenyl
—CH2CH2CF3


263
1
2-CH3-phenyl
cyclopropyl


264
1
2-CH3-phenyl
Cyclobutyl


265
1
2-CH3-phenyl
cyclopentyl


266
1
2-CH3-phenyl
cyclohexyl


267
1
2-CH3-phenyl
3-pyridyl


268
1
2-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


269
1
2-CH3-phenyl
1H-imidazol-4-yl


270
1
2-CH3-phenyl
2-furanyl


271
1
4-OH-Phenyl
Ethyl


272
1
4-OH-Phenyl
n-propyl


273
1
4-OH-Phenyl
Isopropyl


274
1
4-OH-Phenyl
—CH2CH(CH3)2


275
1
4-OH-Phenyl
CF3


276
1
4-OH-Phenyl
—CH2CF3


277
1
4-OH-Phenyl
—CH2CH2CF3


278
1
4-OH-Phenyl
cyclopropyl


279
1
4-OH-Phenyl
Cyclobutyl


280
1
4-OH-Phenyl
cyclopentyl


281
1
4-OH-Phenyl
cyclohexyl


282
1
4-OH-Phenyl
3-pyridyl


283
1
4-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


284
1
4-OH-Phenyl
1H-imidazol-4-yl


285
1
4-OH-Phenyl
2-furanyl


286
1
2-OH-Phenyl
Ethyl


287
1
2-OH-Phenyl
n-propyl


288
1
2-OH-Phenyl
Isopropyl


289
1
2-OH-Phenyl
—CH2CH(CH3)2


290
1
2-OH-Phenyl
CF3


291
1
2-OH-Phenyl
—CH2CF3


292
1
2-OH-Phenyl
—CH2CH2CF3


293
1
2-OH-Phenyl
cyclopropyl


294
1
2-OH-Phenyl
Cyclobutyl


295
1
2-OH-Phenyl
cyclopentyl


296
1
2-OH-Phenyl
cyclohexyl


297
1
2-OH-Phenyl
3-pyridyl


298
1
2-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


299
1
2-OH-Phenyl
1H-imidazol-4-yl


300
1
2-OH-Phenyl
2-furanyl


301
1
3-OMe-Phenyl
Ethyl


302
1
3-OMe-Phenyl
n-propyl


303
1
3-OMe-Phenyl
Isopropyl


304
1
3-OMe-Phenyl
—CH2CH(CH3)2


305
1
3-OMe-Phenyl
CF3


306
1
3-OMe-Phenyl
—CH2CF3


307
1
3-OMe-Phenyl
—CH2CH2CF3


308
1
3-OMe-Phenyl
cyclopropyl


309
1
3-OMe-Phenyl
Cyclobutyl


310
1
3-OMe-Phenyl
cyclopentyl


311
1
3-OMe-Phenyl
cyclohexyl


312
1
3-OMe-Phenyl
3-pyridyl


313
1
3-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


314
1
3-OMe-Phenyl
1H-imidazol-4-yl


315
1
3-OMe-Phenyl
2-furanyl


316
1
4-CN-Phenyl
Ethyl


317
1
4-CN-Phenyl
n-propyl


318
1
4-CN-Phenyl
Isopropyl


319
1
4-CN-Phenyl
—CH2CH(CH3)2


320
1
4-CN-Phenyl
CF3


321
1
4-CN-Phenyl
—CH2CF3


322
1
4-CN-Phenyl
—CH2CH2CF3


323
1
4-CN-Phenyl
cyclopropyl


324
1
4-CN-Phenyl
Cyclobutyl


325
1
4-CN-Phenyl
cyclopentyl


326
1
4-CN-Phenyl
cyclohexyl


327
1
4-CN-Phenyl
3-pyridyl


328
1
4-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


329
1
4-CN-Phenyl
1H-imidazol-4-yl


330
1
4-CN-Phenyl
2-furanyl


331
1
2-CN-Phenyl
Ethyl


332
1
2-CN-Phenyl
n-propyl


333
1
2-CN-Phenyl
Isopropyl


334
1
2-CN-Phenyl
—CH2CH(CH3)2


335
1
2-CN-Phenyl
CF3


336
1
2-CN-Phenyl
—CH2CF3


337
1
2-CN-Phenyl
—CH2CH2CF3


338
1
2-CN-Phenyl
cyclopropyl


339
1
2-CN-Phenyl
Cyclobutyl


340
1
2-CN-Phenyl
cyclopentyl


341
1
2-CN-Phenyl
cyclohexyl


342
1
2-CN-Phenyl
3-pyridyl


343
1
2-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


344
1
2-CN-Phenyl
1H-imidazol-4-yl


345
1
2-CN-Phenyl
2-furanyl


346
1
3-F-Phenyl
Ethyl


347
1
3-F-Phenyl
n-propyl


348
1
3-F-Phenyl
Isopropyl


349
1
3-F-Phenyl
—CH2CH(CH3)2


350
1
3-F-Phenyl
CF3


351
1
3-F-Phenyl
—CH2CF3


352
1
3-F-Phenyl
—CH2CH2CF3


353
1
3-F-Phenyl
cyclopropyl


354
1
3-F-Phenyl
Cyclobutyl


355
1
3-F-Phenyl
cyclopentyl


356
1
3-F-Phenyl
cyclohexyl


357
1
3-F-Phenyl
3-pyridyl


358
1
3-F-Phenyl
1-methyl-1H-pyrazol-4-yl


359
1
3-F-Phenyl
1H-imidazol-4-yl


360
1
3-F-Phenyl
2-furanyl


361
1
2-Cl-Phenyl
Ethyl


362
1
2-Cl-Phenyl
n-propyl


363
1
2-Cl-Phenyl
Isopropyl


364
1
2-Cl-Phenyl
—CH2CH(CH3)2


365
1
2-Cl-Phenyl
CF3


366
1
2-Cl-Phenyl
—CH2CF3


367
1
2-Cl-Phenyl
—CH2CH2CF3


368
1
2-Cl-Phenyl
cyclopropyl


369
1
2-Cl-Phenyl
Cyclobutyl


370
1
2-Cl-Phenyl
cyclopentyl


371
1
2-Cl-Phenyl
cyclohexyl


372
1
2-Cl-Phenyl
3-pyridyl


373
1
2-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


374
1
2-Cl-Phenyl
1H-imidazol-4-yl


375
1
2-Cl-Phenyl
2-furanyl


376
1
4-Cl-Phenyl
Ethyl


377
1
4-Cl-Phenyl
n-propyl


378
1
4-Cl-Phenyl
Isopropyl


379
1
4-Cl-Phenyl
—CH2CH(CH3)2


380
1
4-Cl-Phenyl
CF3


381
1
4-Cl-Phenyl
—CH2CF3


382
1
4-Cl-Phenyl
—CH2CH2CF3


383
1
4-Cl-Phenyl
cyclopropyl


384
1
4-Cl-Phenyl
Cyclobutyl


385
1
4-Cl-Phenyl
cyclopentyl


386
1
4-Cl-Phenyl
cyclohexyl


387
1
4-Cl-Phenyl
3-pyridyl


388
1
4-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


389
1
4-Cl-Phenyl
1H-imidazol-4-yl


390
1
4-Cl-Phenyl
2-furanyl


391
1
3-Br-Phenyl
Ethyl


392
1
3-Br-Phenyl
n-propyl


393
1
3-Br-Phenyl
Isopropyl


394
1
3-Br-Phenyl
—CH2CH(CH3)2


395
1
3-Br-Phenyl
CF3


396
1
3-Br-Phenyl
—CH2CF3


397
1
3-Br-Phenyl
—CH2CH2CF3


398
1
3-Br-Phenyl
cyclopropyl


399
1
3-Br-Phenyl
Cyclobutyl


400
1
3-Br-Phenyl
cyclopentyl


401
1
3-Br-Phenyl
cyclohexyl


402
1
3-Br-Phenyl
3-pyridyl


403
1
3-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


404
1
3-Br-Phenyl
1H-imidazol-4-yl


405
1
3-Br-Phenyl
2-furanyl


406
1
2-CF3-Phenyl
Ethyl


407
1
2-CF3-Phenyl
n-propyl


408
1
2-CF3-Phenyl
Isopropyl


409
1
2-CF3-Phenyl
—CH2CH(CH3)2


410
1
2-CF3-Phenyl
CF3


411
1
2-CF3-Phenyl
—CH2CF3


412
1
2-CF3-Phenyl
—CH2CH2CF3


413
1
2-CF3-Phenyl
cyclopropyl


414
1
2-CF3-Phenyl
Cyclobutyl


415
1
2-CF3-Phenyl
cyclopentyl


416
1
2-CF3-Phenyl
cyclohexyl


417
1
2-CF3-Phenyl
3-pyridyl


418
1
2-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


419
1
2-CF3-Phenyl
1H-imidazol-4-yl


420
1
2-CF3-Phenyl
2-furanyl


421
1
4-CF3-Phenyl
Ethyl


422
1
4-CF3-Phenyl
n-propyl


423
1
4-CF3-Phenyl
Isopropyl


424
1
4-CF3-Phenyl
—CH2CH(CH3)2


425
1
4-CF3-Phenyl
CF3


426
1
4-CF3-Phenyl
—CH2CF3


427
1
4-CF3-Phenyl
—CH2CH2CF3


428
1
4-CF3-Phenyl
cyclopropyl


429
1
4-CF3-Phenyl
Cyclobutyl


430
1
4-CF3-Phenyl
cyclopentyl


431
1
4-CF3-Phenyl
cyclohexyl


432
1
4-CF3-Phenyl
3-pyridyl


433
1
4-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


434
1
4-CF3-Phenyl
1H-imidazol-4-yl


435
1
4-CF3-Phenyl
2-furanyl


436
1
3-iPr-Phenyl
Ethyl


437
1
3-iPr-Phenyl
n-propyl


438
1
3-iPr-Phenyl
Isopropyl


439
1
3-iPr-Phenyl
—CH2CH(CH3)2


440
1
3-iPr-Phenyl
CF3


441
1
3-iPr-Phenyl
—CH2CF3


442
1
3-iPr-Phenyl
—CH2CH2CF3


443
1
3-iPr-Phenyl
cyclopropyl


444
1
3-iPr-Phenyl
Cyclobutyl


445
1
3-iPr-Phenyl
cyclopentyl


446
1
3-iPr-Phenyl
cyclohexyl


447
1
3-iPr-Phenyl
3-pyridyl


448
1
3-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


449
1
3-iPr-Phenyl
1H-imidazol-4-yl


450
1
3-iPr-Phenyl
2-furanyl


451
1
2-morpholino-phenyl
Ethyl


452
1
2-morpholino-phenyl
n-propyl


453
1
2-morpholino-phenyl
isopropyl


454
1
2-morpholino-phenyl
—CH2CH(CH3)2


455
1
2-morpholino-phenyl
CF3


456
1
2-morpholino-phenyl
—CH2CF3


457
1
2-morpholino-phenyl
—CH2CH2CF3


458
1
2-morpholino-phenyl
cyclopropyl


459
1
2-morpholino-phenyl
Cyclobutyl


460
1
2-morpholino-phenyl
cyclopentyl


461
1
2-morpholino-phenyl
cyclohexyl


462
1
2-morpholino-phenyl
3-pyridyl


463
1
2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


464
1
2-morpholino-phenyl
1H-imidazol-4-yl


465
1
2-morpholino-phenyl
2-furanyl


466
1
4-morpholino-phenyl
ethyl


467
1
4-morpholino-phenyl
n-propyl


468
1
4-morpholino-phenyl
isopropyl


469
1
4-morpholino-phenyl
—CH2CH(CH3)2


470
1
4-morpholino-phenyl
CF3


471
1
4-morpholino-phenyl
—CH2CF3


472
1
4-morpholino-phenyl
—CH2CH2CF3


473
1
4-morpholino-phenyl
cyclopropyl


474
1
4-morpholino-phenyl
Cyclobutyl


475
1
4-morpholino-phenyl
cyclopentyl


476
1
4-morpholino-phenyl
cyclohexyl


477
1
4-morpholino-phenyl
3-pyridyl


478
1
4-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


479
1
4-morpholino-phenyl
1H-imidazol-4-yl


480
1
4-morpholino-phenyl
2-furanyl


481
1
4-methyl-2-morpholino-phenyl
ethyl


482
1
4-methyl-2-morpholino-phenyl
n-propyl


483
1
4-methyl-2-morpholino-phenyl
isopropyl


484
1
4-methyl-2-morpholino-phenyl
—CH2CH(CH3)2


485
1
4-methyl-2-morpholino-phenyl
CF3


486
1
4-methyl-2-morpholino-phenyl
—CH2CF3


487
1
4-methyl-2-morpholino-phenyl
—CH2CH2CF3


488
1
4-methyl-2-morpholino-phenyl
cyclopropyl


489
1
4-methyl-2-morpholino-phenyl
Cyclobutyl


490
1
4-methyl-2-morpholino-phenyl
cyclopentyl


491
1
4-methyl-2-morpholino-phenyl
cyclohexyl


492
1
4-methyl-2-morpholino-phenyl
3-pyridyl


493
1
4-methyl-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


494
1
4-methyl-2-morpholino-phenyl
1H-imidazol-4-yl


495
1
4-methyl-2-morpholino-phenyl
2-furanyl


496
2
4-CH3-phenyl
ethyl


497
2
4-CH3-phenyl
n-propyl


498
2
4-CH3-phenyl
isopropyl


499
2
4-CH3-phenyl
—CH2CH(CH3)2


500
2
4-CH3-phenyl
CF3


501
2
4-CH3-phenyl
—CH2CF3


502
2
4-CH3-phenyl
—CH2CH2CF3


503
2
4-CH3-phenyl
cyclopropyl


504
2
4-CH3-phenyl
Cyclobutyl


505
2
4-CH3-phenyl
cyclopentyl


506
2
4-CH3-phenyl
cyclohexyl


507
2
4-CH3-phenyl
3-pyridyl


508
2
4-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


509
2
4-CH3-phenyl
1H-imidazol-4-yl


510
2
4-CH3-phenyl
2-furanyl


511
2
3-CH3-phenyl
ethyl


512
2
3-CH3-phenyl
n-propyl


513
2
3-CH3-phenyl
isopropyl


514
2
3-CH3-phenyl
—CH2CH(CH3)2


515
2
3-CH3-phenyl
CF3


516
2
3-CH3-phenyl
—CH2CF3


517
2
3-CH3-phenyl
—CH2CH2CF3


518
2
3-CHs-phenyl
cyclopropyl


519
2
3-CH3-phenyl
Cyclobutyl


520
2
3-CH3-phenyl
cyclopentyl


521
2
3-CH3-phenyl
cyclohexyl


522
2
3-CH3-phenyl
3-pyridyl


523
2
3-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


524
2
3-CH3-phenyl
1H-imidazol-4-yl


525
2
3-CH3-phenyl
2-furanyl


526
2
3-OH-Phenyl
ethyl


527
2
3-OH-Phenyl
n-propyl


528
2
3-OH-Phenyl
isopropyl


529
2
3-OH-Phenyl
—CH2CH(CH3)2


530
2
3-OH-Phenyl
CF3


531
2
3-OH-Phenyl
—CH2CF3


532
2
3-OH-Phenyl
—CH2CH2CF3


533
2
3-OH-Phenyl
cyclopropyl


534
2
3-OH-Phenyl
Cyclobutyl


535
2
3-OH-Phenyl
cyclopentyl


536
2
3-OH-Phenyl
cyclohexyl


537
2
3-OH-Phenyl
3-pyridyl


538
2
3-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


539
2
3-OH-Phenyl
1H-imidazol-4-yl


540
2
3-OH-Phenyl
2-furanyl


541
2
4-OMe-Phenyl
ethyl


542
2
4-OMe-Phenyl
n-propyl


543
2
4-OMe-Phenyl
isopropyl


544
2
4-OMe-Phenyl
—CH2CH(CH3)2


545
2
4-OMe-Phenyl
CF3


546
2
4-OMe-Phenyl
—CH2CF3


547
2
4-OMe-Phenyl
—CH2CH2CF3


548
2
4-OMe-Phenyl
cyclopropyl


549
2
4-OMe-Phenyl
Cyclobutyl


550
2
4-OMe-Phenyl
cyclopentyl


551
2
4-OMe-Phenyl
cyclohexyl


552
2
4-OMe-Phenyl
3-pyridyl


553
2
4-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


554
2
4-OMe-Phenyl
1H-imidazol-4-yl


555
2
4-OMe-Phenyl
2-furanyl


556
2
2-OMe-Phenyl
ethyl


557
2
2-OMe-Phenyl
n-propyl


558
2
2-OMe-Phenyl
isopropyl


559
2
2-OMe-Phenyl
—CH2CH(CH3)2


560
2
2-OMe-Phenyl
CF3


561
2
2-OMe-Phenyl
—CH2CF3


562
2
2-OMe-Phenyl
—CH2CH2CF3


563
2
2-OMe-Phenyl
cyclopropyl


564
2
2-OMe-Phenyl
Cyclobutyl


565
2
2-OMe-Phenyl
cyclopentyl


566
2
2-OMe-Phenyl
cyclohexyl


567
2
2-OMe-Phenyl
3-pyridyl


568
2
2-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


569
2
2-OMe-Phenyl
1H-imidazol-4-yl


570
2
2-OMe-Phenyl
2-furanyl


571
2
3-CN-Phenyl
ethyl


572
2
3-CN-Phenyl
n-propyl


573
2
3-CN-Phenyl
isopropyl


574
2
3-CN-Phenyl
—CH2CH(CH3)2


575
2
3-CN-Phenyl
CF3


576
2
3-CN-Phenyl
—CH2CF3


577
2
3-CN-Phenyl
—CH2CH2CF3


578
2
3-CN-Phenyl
cyclopropyl


579
2
3-CN-Phenyl
Cyclobutyl


580
2
3-CN-Phenyl
cyclopentyl


581
2
3-CN-Phenyl
cyclohexyl


582
2
3-CN-Phenyl
3-pyridyl


583
2
3-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


584
2
3-CN-Phenyl
1H-imidazol-4-yl


585
2
3-CN-Phenyl
2-furanyl


586
2
2-F-Phenyl
ethyl


587
2
2-F-Phenyl
n-propyl


588
2
2-F-Phenyl
isopropyl


589
2
2-F-Phenyl
—CH2CH(CH3)2


590
2
2-F-Phenyl
CF3


591
2
2-F-Phenyl
—CH2CF3


592
2
2-F-Phenyl
—CH2CH2CF3


593
2
2-F-Phenyl
cyclopropyl


594
2
2-F-Phenyl
Cyclobutyl


595
2
2-F-Phenyl
cyclopentyl


596
2
2-F-Phenyl
cyclohexyl


597
2
2-F-Phenyl
3-pyridyl


598
2
2-F-Phenyl
1-methyl-1H-pyrazol-4-yl


599
2
2-F-Phenyl
1H-imidazol-4-yl


600
2
2-F-Phenyl
2-furanyl


601
2
4-F-Phenyl
ethyl


602
2
4-F-Phenyl
n-propyl


603
2
4-F-Phenyl
isopropyl


604
2
4-F-Phenyl
—CH2CH(CH3)2


605
2
4-F-Phenyl
CF3


606
2
4-F-Phenyl
—CH2CF3


607
2
4-F-Phenyl
—CH2CH2CF3


608
2
4-F-Phenyl
cyclopropyl


609
2
4-F-Phenyl
Cyclobutyl


610
2
4-F-Phenyl
cyclopentyl


611
2
4-F-Phenyl
cyclohexyl


612
2
4-F-Phenyl
3-pyridyl


613
2
4-F-Phenyl
1-methyl-1H-pyrazol-4-yl


614
2
4-F-Phenyl
1H-imidazol-4-yl


615
2
4-F-Phenyl
2-furanyl


616
2
3-Cl-Phenyl
ethyl


617
2
3-Cl-Phenyl
n-propyl


618
2
3-Cl-Phenyl
isopropyl


619
2
3-Cl-Phenyl
—CH2CH(CH3)2


620
2
3-Cl-Phenyl
CF3


621
2
3-Cl-Phenyl
—CH2CF3


622
2
3-Cl-Phenyl
—CH2CH2CF3


623
2
3-Cl-Phenyl
cyclopropyl


624
2
3-Cl-Phenyl
Cyclobutyl


625
2
3-Cl-Phenyl
cyclopentyl


626
2
3-Cl-Phenyl
cyclohexyl


627
2
3-Cl-Phenyl
3-pyridyl


628
2
3-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


629
2
3-Cl-Phenyl
1H-imidazol-4-yl


630
2
3-Cl-Phenyl
2-furanyl


631
2
2-Br-Phenyl
ethyl


632
2
2-Br-Phenyl
n-propyl


633
2
2-Br-Phenyl
isopropyl


634
2
2-Br-Phenyl
—CH2CH(CH3)2


635
2
2-Br-Phenyl
CF3


636
2
2-Br-Phenyl
—CH2CF3


637
2
2-Br-Phenyl
—CH2CH2CF3


638
2
2-Br-Phenyl
cyclopropyl


639
2
2-Br-Phenyl
Cyclobutyl


640
2
2-Br-Phenyl
cyclopentyl


641
2
2-Br-Phenyl
cyclohexyl


642
2
2-Br-Phenyl
3-pyridyl


643
2
2-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


644
2
2-Br-Phenyl
1H-imidazol-4-yl


645
2
2-Br-Phenyl
2-furanyl


646
2
4-Br-Phenyl
ethyl


647
2
4-Br-Phenyl
n-propyl


648
2
4-Br-Phenyl
isopropyl


649
2
4-Br-Phenyl
—CH2CH(CH3)2


650
2
4-Br-Phenyl
CF3


651
2
4-Br-Phenyl
—CH2CF3


652
2
4-Br-Phenyl
—CH2CH2CF3


653
2
4-Br-Phenyl
cyclopropyl


654
2
4-Br-Phenyl
Cyclobutyl


655
2
4-Br-Phenyl
cyclopentyl


656
2
4-Br-Phenyl
cyclohexyl


657
2
4-Br-Phenyl
3-pyridyl


658
2
4-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


659
2
4-Br-Phenyl
1H-imidazol-4-yl


660
2
4-Br-Phenyl
2-furanyl


661
2
3-CF3-Phenyl
ethyl


662
2
3-CF3-Phenyl
n-propyl


663
2
3-CF3-Phenyl
isopropyl


664
2
3-CF3-Phenyl
—CH2CH(CH3)2


665
2
3-CF3-Phenyl
CF3


666
2
3-CF3-Phenyl
—CH2CF3


667
2
3-CF3-Phenyl
—CH2CH2CF3


668
2
3-CF3-Phenyl
cyclopropyl


669
2
3-CF3-Phenyl
Cyclobutyl


670
2
3-CF3-Phenyl
cyclopentyl


671
2
3-CF3-Phenyl
cyclohexyl


672
2
3-CF3-Phenyl
3-pyridyl


673
2
3-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


674
2
3-CF3-Phenyl
1H-imidazol-4-yl


675
2
3-CF3-Phenyl
2-furanyl


676
2
2-iPr-Phenyl
ethyl


677
2
2-iPr-Phenyl
n-propyl


678
2
2-iPr-Phenyl
isopropyl


679
2
2-iPr-Phenyl
—CH2CH(CH3)2


680
2
2-iPr-Phenyl
CF3


681
2
2-iPr-Phenyl
—CH2CF3


682
2
2-iPr-Phenyl
—CH2CH2CF3


683
2
2-iPr-Phenyl
cyclopropyl


684
2
2-iPr-Phenyl
Cyclobutyl


685
2
2-iPr-Phenyl
cyclopentyl


686
2
2-iPr-Phenyl
cyclohexyl


687
2
2-iPr-Phenyl
3-pyridyl


688
2
2-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


689
2
2-iPr-Phenyl
1H-imidazol-4-yl


690
2
2-iPr-Phenyl
2-furanyl


691
2
4-iPr-Phenyl
ethyl


692
2
4-iPr-Phenyl
n-propyl


693
2
4-iPr-Phenyl
isopropyl


694
2
4-iPr-Phenyl
—CH2CH(CH3)2


695
2
4-iPr-Phenyl
CF3


696
2
4-iPr-Phenyl
—CH2CF3


697
2
4-iPr-Phenyl
—CH2CH2CF3


698
2
4-iPr-Phenyl
cyclopropyl


699
2
4-iPr-Phenyl
Cyclobutyl


700
2
4-iPr-Phenyl
cyclopentyl


701
2
4-iPr-Phenyl
cyclohexyl


702
2
4-iPr-Phenyl
3-pyridyl


703
2
4-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


704
2
4-iPr-Phenyl
1H-imidazol-4-yl


705
2
4-iPr-Phenyl
2-furanyl


706
2
3-morpholino-phenyl
ethyl


707
2
3-morpholino-phenyl
n-propyl


708
2
3-morpholino-phenyl
isopropyl


709
2
3-morpholino-phenyl
—CH2CH(CH3)2


710
2
3-morpholino-phenyl
CF3


711
2
3-morpholino-phenyl
—CH2CF3


712
2
3-morpholino-phenyl
—CH2CH2CF3


713
2
3-morpholino-phenyl
cyclopropyl


714
2
3-morpholino-phenyl
Cyclobutyl


715
2
3-morpholino-phenyl
cyclopentyl


716
2
3-morpholino-phenyl
cyclohexyl


717
2
3-morpholino-phenyl
3-pyridyl


718
2
3-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


719
2
3-morpholino-phenyl
1H-imidazol-4-yl


720
2
3-morpholino-phenyl
2-furanyl


721
2
4-cyano-2-morpholino-phenyl
ethyl


722
2
4-cyano-2-morpholino-phenyl
n-propyl


723
2
4-cyano-2-morpholino-phenyl
isopropyl


724
2
4-cyano-2-morpholino-phenyl
—CH2CH(CH3)2


725
2
4-cyano-2-morpholino-phenyl
CF3


726
2
4-cyano-2-morpholino-phenyl
—CH2CF3


727
2
4-cyano-2-morpholino-phenyl
—CH2CH2CF3


728
2
4-cyano-2-morpholino-phenyl
cyclopropyl


729
2
4-cyano-2-morpholino-phenyl
Cyclobutyl


730
2
4-cyano-2-morpholino-phenyl
cyclopentyl


731
2
4-cyano-2-morpholino-phenyl
cyclohexyl


732
2
4-cyano-2-morpholino-phenyl
3-pyridyl


733
2
4-cyano-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


734
2
4-cyano-2-morpholino-phenyl
1H-imidazol-4-yl


735
2
4-cyano-2-morpholino-phenyl
2-furanyl


736
2
4-hydroxy-2-morpholino-phenyl
ethyl


737
2
4-hydroxy-2-morpholino-phenyl
n-propyl


738
2
4-hydroxy-2-morpholino-phenyl
isopropyl


739
2
4-hydroxy-2-morpholino-phenyl
—CH2CH(CH3)2


740
2
4-hydroxy-2-morpholino-phenyl
CF3


741
2
4-hydroxy-2-morpholino-phenyl
—CH2CF3


742
2
4-hydroxy-2-morpholino-phenyl
—CH2CH2CF3


743
2
4-hydroxy-2-morpholino-phenyl
cyclopropyl


744
2
4-hydroxy-2-morpholino-phenyl
Cyclobutyl


745
2
4-hydroxy-2-morpholino-phenyl
cyclopentyl


746
2
4-hydroxy-2-morpholino-phenyl
cyclohexyl


747
2
4-hydroxy-2-morpholino-phenyl
3-pyridyl


748
2
4-hydroxy-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


749
2
4-hydroxy-2-morpholino-phenyl
1H-imidazol-4-yl


750
2
4-hydroxy-2-morpholino-phenyl
2-furanyl


751
2
2-CH3-phenyl
Ethyl


752
2
2-CH3-phenyl
n-propyl


753
2
2-CH3-phenyl
Isopropyl


754
2
2-CH3-phenyl
—CH2CH(CH3)2


755
2
2-CH3-phenyl
CF3


756
2
2-CH3-phenyl
—CH2CF3


757
2
2-CH3-phenyl
—CH2CH2CF3


758
2
2-CH3-phenyl
cyclopropyl


759
2
2-CH3-phenyl
Cyclobutyl


760
2
2-CH3-phenyl
cyclopentyl


761
2
2-CH3-phenyl
cyclohexyl


762
2
2-CH3-phenyl
3-pyridyl


763
2
2-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


764
2
2-CH3-phenyl
1H-imidazol-4-yl


765
2
2-CH3-phenyl
2-furanyl


766
2
4-OH-Phenyl
Ethyl


767
2
4-OH-Phenyl
n-propyl


768
2
4-OH-Phenyl
Isopropyl


769
2
4-OH-Phenyl
—CH2CH(CH3)2


770
2
4-OH-Phenyl
CF3


771
2
4-OH-Phenyl
—CH2CF3


772
2
4-OH-Phenyl
—CH2CH2CF3


773
2
4-OH-Phenyl
cyclopropyl


774
2
4-OH-Phenyl
Cyclobutyl


775
2
4-OH-Phenyl
cyclopentyl


776
2
4-OH-Phenyl
cyclohexyl


777
2
4-OH-Phenyl
3-pyridyl


778
2
4-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


779
2
4-OH-Phenyl
1H-imidazol-4-yl


780
2
4-OH-Phenyl
2-furanyl


781
2
2-OH-Phenyl
Ethyl


782
2
2-OH-Phenyl
n-propyl


783
2
2-OH-Phenyl
Isopropyl


784
2
2-OH-Phenyl
—CH2CH(CH3)2


785
2
2-OH-Phenyl
CF3


786
2
2-OH-Phenyl
—CH2CF3


787
2
2-OH-Phenyl
—CH2CH2CF3


788
2
2-OH-Phenyl
cyclopropyl


789
2
2-OH-Phenyl
Cyclobutyl


790
2
2-OH-Phenyl
cyclopentyl


791
2
2-OH-Phenyl
cyclohexyl


792
2
2-OH-Phenyl
3-pyridyl


793
2
2-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


794
2
2-OH-Phenyl
1H-imidazol-4-yl


795
2
2-OH-Phenyl
2-furanyl


796
2
3-OMe-Phenyl
Ethyl


797
2
3-OMe-Phenyl
n-propyl


798
2
3-OMe-Phenyl
Isopropyl


799
2
3-OMe-Phenyl
—CH2CH(CH3)2


800
2
3-OMe-Phenyl
CF3


801
2
3-OMe-Phenyl
—CH2CF3


802
2
3-OMe-Phenyl
—CH2CH2CF3


803
2
3-OMe-Phenyl
cyclopropyl


804
2
3-OMe-Phenyl
Cyclobutyl


805
2
3-OMe-Phenyl
cyclopentyl


806
2
3-OMe-Phenyl
cyclohexyl


807
2
3-OMe-Phenyl
3-pyridyl


808
2
3-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


809
2
3-OMe-Phenyl
1H-imidazol-4-yl


810
2
3-OMe-Phenyl
2-furanyl


811
2
4-CN-Phenyl
Ethyl


812
2
4-CN-Phenyl
n-propyl


813
2
4-CN-Phenyl
Isopropyl


814
2
4-CN-Phenyl
—CH2CH(CH3)2


815
2
4-CN-Phenyl
CF3


816
2
4-CN-Phenyl
—CH2CF3


817
2
4-CN-Phenyl
—CH2CH2CF3


818
2
4-CN-Phenyl
cyclopropyl


819
2
4-CN-Phenyl
Cyclobutyl


820
2
4-CN-Phenyl
cyclopentyl


821
2
4-CN-Phenyl
cyclohexyl


822
2
4-CN-Phenyl
3-pyridyl


823
2
4-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


824
2
4-CN-Phenyl
1H-imidazol-4-yl


825
2
4-CN-Phenyl
2-furanyl


826
2
2-CN-Phenyl
Ethyl


827
2
2-CN-Phenyl
n-propyl


828
2
2-CN-Phenyl
Isopropyl


829
2
2-CN-Phenyl
—CH2CH(CH3)2


830
2
2-CN-Phenyl
CF3


831
2
2-CN-Phenyl
—CH2CF3


832
2
2-CN-Phenyl
—CH2CH2CF3


833
2
2-CN-Phenyl
cyclopropyl


834
2
2-CN-Phenyl
Cyclobutyl


835
2
2-CN-Phenyl
cyclopentyl


836
2
2-CN-Phenyl
cyclohexyl


837
2
2-CN-Phenyl
3-pyridyl


838
2
2-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


839
2
2-CN-Phenyl
1H-imidazol-4-yl


840
2
2-CN-Phenyl
2-furanyl


841
2
3-F-Phenyl
Ethyl


842
2
3-F-Phenyl
n-propyl


843
2
3-F-Phenyl
Isopropyl


844
2
3-F-Phenyl
—CH2CH(CH3)2


845
2
3-F-Phenyl
CF3


846
2
3-F-Phenyl
—CH2CF3


847
2
3-F-Phenyl
—CH2CH2CF3


848
2
3-F-Phenyl
cyclopropyl


849
2
3-F-Phenyl
Cyclobutyl


850
2
3-F-Phenyl
cyclopentyl


851
2
3-F-Phenyl
cyclohexyl


852
2
3-F-Phenyl
3-pyridyl


853
2
3-F-Phenyl
1-methyl-1H-pyrazol-4-yl


854
2
3-F-Phenyl
1H-imidazol-4-yl


855
2
3-F-Phenyl
2-furanyl


856
2
2-Cl-Phenyl
Ethyl


857
2
2-Cl-Phenyl
n-propyl


858
2
2-Cl-Phenyl
Isopropyl


859
2
2-Cl-Phenyl
—CH2CH(CH3)2


860
2
2-Cl-Phenyl
CF3


861
2
2-Cl-Phenyl
—CH2CF3


862
2
2-Cl-Phenyl
—CH2CH2CF3


863
2
2-Cl-Phenyl
cyclopropyl


864
2
2-Cl-Phenyl
Cyclobutyl


865
2
2-Cl-Phenyl
cyclopentyl


866
2
2-Cl-Phenyl
cyclohexyl


867
2
2-Cl-Phenyl
3-pyridyl


868
2
2-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


869
2
2-Cl-Phenyl
1H-imidazol-4-yl


870
2
2-Cl-Phenyl
2-furanyl


871
2
4-Cl-Phenyl
Ethyl


872
2
4-Cl-Phenyl
n-propyl


873
2
4-Cl-Phenyl
Isopropyl


874
2
4-Cl-Phenyl
—CH2CH(CH3)2


875
2
4-Cl-Phenyl
CF3


876
2
4-Cl-Phenyl
—CH2CF3


877
2
4-Cl-Phenyl
—CH2CH2CF3


878
2
4-Cl-Phenyl
cyclopropyl


879
2
4-Cl-Phenyl
Cyclobutyl


880
2
4-Cl-Phenyl
cyclopentyl


881
2
4-Cl-Phenyl
cyclohexyl


882
2
4-Cl-Phenyl
3-pyridyl


883
2
4-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


884
2
4-Cl-Phenyl
1H-imidazol-4-yl


885
2
4-Cl-Phenyl
2-furanyl


886
2
3-Br-Phenyl
Ethyl


887
2
3-Br-Phenyl
n-propyl


888
2
3-Br-Phenyl
Isopropyl


889
2
3-Br-Phenyl
—CH2CH(CH3)2


890
2
3-Br-Phenyl
CF3


891
2
3-Br-Phenyl
—CH2CF3


892
2
3-Br-Phenyl
—CH2CH2CF3


893
2
3-Br-Phenyl
cyclopropyl


894
2
3-Br-Phenyl
Cyclobutyl


895
2
3-Br-Phenyl
cyclopentyl


896
2
3-Br-Phenyl
cyclohexyl


897
2
3-Br-Phenyl
3-pyridyl


898
2
3-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


899
2
3-Br-Phenyl
1H-imidazol-4-yl


900
2
3-Br-Phenyl
2-furanyl


901
2
2-CF3-Phenyl
Ethyl


902
2
2-CF3-Phenyl
n-propyl


903
2
2-CF3-Phenyl
Isopropyl


904
2
2-CF3-Phenyl
—CH2CH(CH3)2


905
2
2-CF3-Phenyl
CF3


906
2
2-CF3-Phenyl
—CH2CF3


907
2
2-CF3-Phenyl
—CH2CH2CF3


908
2
2-CF3-Phenyl
cyclopropyl


909
2
2-CF3-Phenyl
Cyclobutyl


910
2
2-CF3-Phenyl
cyclopentyl


911
2
2-CF3-Phenyl
cyclohexyl


912
2
2-CF3-Phenyl
3-pyridyl


913
2
2-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


914
2
2-CF3-Phenyl
1H-imidazol-4-yl


915
2
2-CF3-Phenyl
2-furanyl


916
2
4-CF3-Phenyl
Ethyl


917
2
4-CF3-Phenyl
n-propyl


918
2
4-CF3-Phenyl
Isopropyl


919
2
4-CF3-Phenyl
—CH2CH(CH3)2


920
2
4-CF3-Phenyl
CF3


921
2
4-CF3-Phenyl
—CH2CF3


922
2
4-CF3-Phenyl
—CH2CH2CF3


923
2
4-CF3-Phenyl
cyclopropyl


924
2
4-CF3-Phenyl
Cyclobutyl


925
2
4-CF3-Phenyl
cyclopentyl


926
2
4-CF3-Phenyl
cyclohexyl


927
2
4-CF3-Phenyl
3-pyridyl


928
2
4-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


929
2
4-CF3-Phenyl
1H-imidazol-4-yl


930
2
4-CF3-Phenyl
2-furanyl


931
2
3-iPr-Phenyl
Ethyl


932
2
3-iPr-Phenyl
n-propyl


933
2
3-iPr-Phenyl
Isopropyl


934
2
3-iPr-Phenyl
—CH2CH(CH3)2


935
2
3-iPr-Phenyl
CF3


936
2
3-iPr-Phenyl
—CH2CF3


937
2
3-iPr-Phenyl
—CH2CH2CF3


938
2
3-iPr-Phenyl
cyclopropyl


939
2
3-iPr-Phenyl
Cyclobutyl


940
2
3-iPr-Phenyl
cyclopentyl


941
2
3-iPr-Phenyl
cyclohexyl


942
2
3-iPr-Phenyl
3-pyridyl


943
2
3-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


944
2
3-iPr-Phenyl
1H-imidazol-4-yl


945
2
3-iPr-Phenyl
2-furanyl


946
2
2-morpholino-phenyl
Ethyl


947
2
2-morpholino-phenyl
n-propyl


948
2
2-morpholino-phenyl
isopropyl


949
2
2-morpholino-phenyl
—CH2CH(CH3)2


950
2
2-morpholino-phenyl
CF3


951
2
2-morpholino-phenyl
—CH2CF3


952
2
2-morpholino-phenyl
—CH2CH2CF3


953
2
2-morpholino-phenyl
cyclopropyl


954
2
2-morpholino-phenyl
Cyclobutyl


955
2
2-morpholino-phenyl
cyclopentyl


956
2
2-morpholino-phenyl
cyclohexyl


957
2
2-morpholino-phenyl
3-pyridyl


958
2
2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


959
2
2-morpholino-phenyl
1H-imidazol-4-yl


960
2
2-morpholino-phenyl
2-furanyl


961
2
4-morpholino-phenyl
ethyl


962
2
4-morpholino-phenyl
n-propyl


963
2
4-morpholino-phenyl
isopropyl


964
2
4-morpholino-phenyl
—CH2CH(CH3)2


965
2
4-morpholino-phenyl
CF3


966
2
4-morpholino-phenyl
—CH2CF3


967
2
4-morpholino-phenyl
—CH2CH2CF3


968
2
4-morpholino-phenyl
cyclopropyl


969
2
4-morpholino-phenyl
Cyclobutyl


970
2
4-morpholino-phenyl
cyclopentyl


971
2
4-morpholino-phenyl
cyclohexyl


972
2
4-morpholino-phenyl
3-pyridyl


973
2
4-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


974
2
4-morpholino-phenyl
1H-imidazol-4-yl


975
2
4-morpholino-phenyl
2-furanyl


976
2
4-methyl-2-morpholino-phenyl
ethyl


977
2
4-methyl-2-morpholino-phenyl
n-propyl


978
2
4-methyl-2-morpholino-phenyl
isopropyl


979
2
4-methyl-2-morpholino-phenyl
—CH2CH(CH3)2


980
2
4-methyl-2-morpholino-phenyl
CF3


981
2
4-methyl-2-morpholino-phenyl
—CH2CF3


982
2
4-methyl-2-morpholino-phenyl
—CH2CH2CF3


983
2
4-methyl-2-morpholino-phenyl
cyclopropyl


984
2
4-methyl-2-morpholino-phenyl
Cyclobutyl


985
2
4-methyl-2-morpholino-phenyl
cyclopentyl


986
2
4-methyl-2-morpholino-phenyl
cyclohexyl


987
2
4-methyl-2-morpholino-phenyl
3-pyridyl


988
2
4-methyl-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


989
2
4-methyl-2-morpholino-phenyl
1H-imidazol-4-yl


990
2
4-methyl-2-morpholino-phenyl
2-furanyl


991
3
4-CH3-phenyl
ethyl


992
3
4-CH3-phenyl
n-propyl


993
3
4-CH3-phenyl
isopropyl


994
3
4-CH3-phenyl
—CH2CH(CH3)2


995
3
4-CH3-phenyl
CF3


996
3
4-CH3-phenyl
—CH2CF3


997
3
4-CH3-phenyl
—CH2CH2CF3


998
3
4-CH3-phenyl
cyclopropyl


999
3
4-CH3-phenyl
Cyclobutyl


1000
3
4-CH3-phenyl
cyclopentyl


1001
3
4-CH3-phenyl
cyclohexyl


1002
3
4-CH3-phenyl
3-pyridyl


1003
3
4-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


1004
3
4-CH3-phenyl
1H-imidazol-4-yl


1005
3
4-CH3-phenyl
2-furanyl


1006
3
3-CH3-phenyl
ethyl


1007
3
3-CH3-phenyl
n-propyl


1008
3
3-CH3-phenyl
isopropyl


1009
3
3-CH3-phenyl
—CH2CH(CH3)2


1010
3
3-CH3-phenyl
CF3


1011
3
3-CH3-phenyl
—CH2CF3


1012
3
3-CH3-phenyl
—CH2CH2CF3


1013
3
3-CH3-phenyl
cyclopropyl


1014
3
3-CHs-phenyl
Cyclobutyl


1015
3
3-CH3-phenyl
cyclopentyl


1016
3
3-CH3-phenyl
cyclohexyl


1017
3
3-CH3-phenyl
3-pyridyl


1018
3
3-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


1019
3
3-CH3-phenyl
1H-imidazol-4-yl


1020
3
3-CH3-phenyl
2-furanyl


1021
3
3-OH-Phenyl
ethyl


1022
3
3-OH-Phenyl
n-propyl


1023
3
3-OH-Phenyl
isopropyl


1024
3
3-OH-Phenyl
—CH2CH(CH3)2


1025
3
3-OH-Phenyl
CF3


1026
3
3-OH-Phenyl
—CH2CF3


1027
3
3-OH-Phenyl
—CH2CH2CF3


1028
3
3-OH-Phenyl
cyclopropyl


1029
3
3-OH-Phenyl
Cyclobutyl


1030
3
3-OH-Phenyl
cyclopentyl


1031
3
3-OH-Phenyl
cyclohexyl


1032
3
3-OH-Phenyl
3-pyridyl


1033
3
3-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


1034
3
3-OH-Phenyl
1H-imidazol-4-yl


1035
3
3-OH-Phenyl
2-furanyl


1036
3
4-OMe-Phenyl
ethyl


1037
3
4-OMe-Phenyl
n-propyl


1038
3
4-OMe-Phenyl
isopropyl


1039
3
4-OMe-Phenyl
—CH2CH(CH3)2


1040
3
4-OMe-Phenyl
CF3


1041
3
4-OMe-Phenyl
—CH2CF3


1042
3
4-OMe-Phenyl
—CH2CH2CF3


1043
3
4-OMe-Phenyl
cyclopropyl


1044
3
4-OMe-Phenyl
Cyclobutyl


1045
3
4-OMe-Phenyl
cyclopentyl


1046
3
4-OMe-Phenyl
cyclohexyl


1047
3
4-OMe-Phenyl
3-pyridyl


1048
3
4-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


1049
3
4-OMe-Phenyl
1H-imidazol-4-yl


1050
3
4-OMe-Phenyl
2-furanyl


1051
3
2-OMe-Phenyl
ethyl


1052
3
2-OMe-Phenyl
n-propyl


1053
3
2-OMe-Phenyl
isopropyl


1054
3
2-OMe-Phenyl
—CH2CH(CH3)2


1055
3
2-OMe-Phenyl
CF3


1056
3
2-OMe-Phenyl
—CH2CF3


1057
3
2-OMe-Phenyl
—CH2CH2CF3


1058
3
2-OMe-Phenyl
cyclopropyl


1059
3
2-OMe-Phenyl
Cyclobutyl


1060
3
2-OMe-Phenyl
cyclopentyl


1061
3
2-OMe-Phenyl
cyclohexyl


1062
3
2-OMe-Phenyl
3-pyridyl


1063
3
2-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


1064
3
2-OMe-Phenyl
1H-imidazol-4-yl


1065
3
2-OMe-Phenyl
2-furanyl


1066
3
3-CN-Phenyl
ethyl


1067
3
3-CN-Phenyl
n-propyl


1068
3
3-CN-Phenyl
isopropyl


1069
3
3-CN-Phenyl
—CH2CH(CH3)2


1070
3
3-CN-Phenyl
CF3


1071
3
3-CN-Phenyl
—CH2CF3


1072
3
3-CN-Phenyl
—CH2CH2CF3


1073
3
3-CN-Phenyl
cyclopropyl


1074
3
3-CN-Phenyl
Cyclobutyl


1075
3
3-CN-Phenyl
cyclopentyl


1076
3
3-CN-Phenyl
cyclohexyl


1077
3
3-CN-Phenyl
3-pyridyl


1078
3
3-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


1079
3
3-CN-Phenyl
1H-imidazol-4-yl


1080
3
3-CN-Phenyl
2-furanyl


1081
3
2-F-Phenyl
ethyl


1082
3
2-F-Phenyl
n-propyl


1083
3
2-F-Phenyl
isopropyl


1084
3
2-F-Phenyl
—CH2CH(CH3)2


1085
3
2-F-Phenyl
CF3


1086
3
2-F-Phenyl
—CH2CF3


1087
3
2-F-Phenyl
—CH2CH2CF3


1088
3
2-F-Phenyl
cyclopropyl


1089
3
2-F-Phenyl
Cyclobutyl


1090
3
2-F-Phenyl
cyclopentyl


1091
3
2-F-Phenyl
cyclohexyl


1092
3
2-F-Phenyl
3-pyridyl


1093
3
2-F-Phenyl
1-methyl-1H-pyrazol-4-yl


1094
3
2-F-Phenyl
1H-imidazol-4-yl


1095
3
2-F-Phenyl
2-furanyl


1096
3
4-F-Phenyl
ethyl


1097
3
4-F-Phenyl
n-propyl


1098
3
4-F-Phenyl
isopropyl


1099
3
4-F-Phenyl
—CH2CH(CH3)2


1100
3
4-F-Phenyl
CF3


1101
3
4-F-Phenyl
—CH2CF3


1102
3
4-F-Phenyl
—CH2CH2CF3


1103
3
4-F-Phenyl
cyclopropyl


1104
3
4-F-Phenyl
Cyclobutyl


1105
3
4-F-Phenyl
cyclopentyl


1106
3
4-F-Phenyl
cyclohexyl


1107
3
4-F-Phenyl
3-pyridyl


1108
3
4-F-Phenyl
1-methyl-1H-pyrazol-4-yl


1109
3
4-F-Phenyl
1H-imidazol-4-yl


1110
3
4-F-Phenyl
2-furanyl


1111
3
3-Cl-Phenyl
ethyl


1112
3
3-Cl-Phenyl
n-propyl


1113
3
3-Cl-Phenyl
isopropyl


1114
3
3-Cl-Phenyl
—CH2CH(CH3)2


1115
3
3-Cl-Phenyl
CF3


1116
3
3-Cl-Phenyl
—CH2CF3


1117
3
3-Cl-Phenyl
—CH2CH2CF3


1118
3
3-Cl-Phenyl
cyclopropyl


1119
3
3-Cl-Phenyl
Cyclobutyl


1120
3
3-Cl-Phenyl
cyclopentyl


1121
3
3-Cl-Phenyl
cyclohexyl


1122
3
3-Cl-Phenyl
3-pyridyl


1123
3
3-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


1124
3
3-Cl-Phenyl
1H-imidazol-4-yl


1125
3
3-Cl-Phenyl
2-furanyl


1126
3
2-Br-Phenyl
ethyl


1127
3
2-Br-Phenyl
n-propyl


1128
3
2-Br-Phenyl
isopropyl


1129
3
2-Br-Phenyl
—CH2CH(CH3)2


1130
3
2-Br-Phenyl
CF3


1131
3
2-Br-Phenyl
—CH2CF3


1132
3
2-Br-Phenyl
—CH2CH2CF3


1133
3
2-Br-Phenyl
cyclopropyl


1134
3
2-Br-Phenyl
Cyclobutyl


1135
3
2-Br-Phenyl
cyclopentyl


1136
3
2-Br-Phenyl
cyclohexyl


1137
3
2-Br-Phenyl
3-pyridyl


1138
3
2-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


1139
3
2-Br-Phenyl
1H-imidazol-4-yl


1140
3
2-Br-Phenyl
2-furanyl


1141
3
4-Br-Phenyl
ethyl


1142
3
4-Br-Phenyl
n-propyl


1143
3
4-Br-Phenyl
isopropyl


1144
3
4-Br-Phenyl
—CH2CH(CH3)2


1145
3
4-Br-Phenyl
CF3


1146
3
4-Br-Phenyl
—CH2CF3


1147
3
4-Br-Phenyl
—CH2CH2CF3


1148
3
4-Br-Phenyl
cyclopropyl


1149
3
4-Br-Phenyl
Cyclobutyl


1150
3
4-Br-Phenyl
cyclopentyl


1151
3
4-Br-Phenyl
cyclohexyl


1152
3
4-Br-Phenyl
3-pyridyl


1153
3
4-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


1154
3
4-Br-Phenyl
1H-imidazol-4-yl


1155
3
4-Br-Phenyl
2-furanyl


1156
3
3-CF3-Phenyl
ethyl


1157
3
3-CF3-Phenyl
n-propyl


1158
3
3-CF3-Phenyl
isopropyl


1159
3
3-CF3-Phenyl
—CH2CH(CH3)2


1160
3
3-CF3-Phenyl
CF3


1161
3
3-CF3-Phenyl
—CH2CF3


1162
3
3-CF3-Phenyl
—CH2CH2CF3


1163
3
3-CF3-Phenyl
cyclopropyl


1164
3
3-CF3-Phenyl
Cyclobutyl


1165
3
3-CF3-Phenyl
cyclopentyl


1166
3
3-CF3-Phenyl
cyclohexyl


1167
3
3-CF3-Phenyl
3-pyridyl


1168
3
3-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


1169
3
3-CF3-Phenyl
1H-imidazol-4-yl


1170
3
3-CF3-Phenyl
2-furanyl


1171
3
2-iPr-Phenyl
ethyl


1172
3
2-iPr-Phenyl
n-propyl


1173
3
2-iPr-Phenyl
isopropyl


1174
3
2-iPr-Phenyl
—CH2CH(CH3)2


1175
3
2-iPr-Phenyl
CF3


1176
3
2-iPr-Phenyl
—CH2CF3


1177
3
2-iPr-Phenyl
—CH2CH2CF3


1178
3
2-iPr-Phenyl
cyclopropyl


1179
3
2-iPr-Phenyl
Cyclobutyl


1180
3
2-iPr-Phenyl
cyclopentyl


1181
3
2-iPr-Phenyl
cyclohexyl


1182
3
2-iPr-Phenyl
3-pyridyl


1183
3
2-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


1184
3
2-iPr-Phenyl
1H-imidazol-4-yl


1185
3
2-iPr-Phenyl
2-furanyl


1186
3
4-iPr-Phenyl
ethyl


1187
3
4-iPr-Phenyl
n-propyl


1188
3
4-iPr-Phenyl
isopropyl


1189
3
4-iPr-Phenyl
—CH2CH(CH3)2


1190
3
4-iPr-Phenyl
CF3


1191
3
4-iPr-Phenyl
—CH2CF3


1192
3
4-iPr-Phenyl
—CH2CH2CF3


1193
3
4-iPr-Phenyl
cyclopropyl


1194
3
4-iPr-Phenyl
Cyclobutyl


1195
3
4-iPr-Phenyl
cyclopentyl


1196
3
4-iPr-Phenyl
cyclohexyl


1197
3
4-iPr-Phenyl
3-pyridyl


1198
3
4-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


1199
3
4-iPr-Phenyl
1H-imidazol-4-yl


1200
3
4-iPr-Phenyl
2-furanyl


1201
3
3-morpholino-phenyl
ethyl


1202
3
3-morpholino-phenyl
n-propyl


1203
3
3-morpholino-phenyl
isopropyl


1204
3
3-morpholino-phenyl
—CH2CH(CH3)2


1205
3
3-morpholino-phenyl
CF3


1206
3
3-morpholino-phenyl
—CH2CF3


1207
3
3-morpholino-phenyl
—CH2CH2CF3


1208
3
3-morpholino-phenyl
cyclopropyl


1209
3
3-morpholino-phenyl
Cyclobutyl


1210
3
3-morpholino-phenyl
cyclopentyl


1211
3
3-morpholino-phenyl
cyclohexyl


1212
3
3-morpholino-phenyl
3-pyridyl


1213
3
3-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1214
3
3-morpholino-phenyl
1H-imidazol-4-yl


1215
3
3-morpholino-phenyl
2-furanyl


1216
3
4-cyano-2-morpholino-phenyl
ethyl


1217
3
4-cyano-2-morpholino-phenyl
n-propyl


1218
3
4-cyano-2-morpholino-phenyl
isopropyl


1219
3
4-cyano-2-morpholino-phenyl
—CH2CH(CH3)2


1220
3
4-cyano-2-morpholino-phenyl
CF3


1221
3
4-cyano-2-morpholino-phenyl
—CH2CF3


1222
3
4-cyano-2-morpholino-phenyl
—CH2CH2CF3


1223
3
4-cyano-2-morpholino-phenyl
cyclopropyl


1224
3
4-cyano-2-morpholino-phenyl
Cyclobutyl


1225
3
4-cyano-2-morpholino-phenyl
cyclopentyl


1226
3
4-cyano-2-morpholino-phenyl
cyclohexyl


1227
3
4-cyano-2-morpholino-phenyl
3-pyridyl


1228
3
4-cyano-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1229
3
4-cyano-2-morpholino-phenyl
1H-imidazol-4-yl


1230
3
4-cyano-2-morpholino-phenyl
2-furanyl


1231
3
4-hydroxy-2-morpholino-phenyl
ethyl


1232
3
4-hydroxy-2-morpholino-phenyl
n-propyl


1233
3
4-hydroxy-2-morpholino-phenyl
isopropyl


1234
3
4-hydroxy-2-morpholino-phenyl
—CH2CH(CH3)2


1235
3
4-hydroxy-2-morpholino-phenyl
CF3


1236
3
4-hydroxy-2-morpholino-phenyl
—CH2CF3


1237
3
4-hydroxy-2-morpholino-phenyl
—CH2CH2CF3


1238
3
4-hydroxy-2-morpholino-phenyl
cyclopropyl


1239
3
4-hydroxy-2-morpholino-phenyl
Cyclobutyl


1240
3
4-hydroxy-2-morpholino-phenyl
cyclopentyl


1241
3
4-hydroxy-2-morpholino-phenyl
cyclohexyl


1242
3
4-hydroxy-2-morpholino-phenyl
3-pyridyl


1243
3
4-hydroxy-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1244
3
4-hydroxy-2-morpholino-phenyl
1H-imidazol-4-yl


1245
3
4-hydroxy-2-morpholino-phenyl
2-furanyl


1246
3
2-CH3-phenyl
Ethyl


1247
3
2-CH3-phenyl
n-propyl


1248
3
2-CH3-phenyl
Isopropyl


1249
3
2-CH3-phenyl
—CH2CH(CH3)2


1250
3
2-CH3-phenyl
CF3


1251
3
2-CH3-phenyl
—CH2CF3


1252
3
2-CH3-phenyl
—CH2CH2CF3


1253
3
2-CH3-phenyl
cyclopropyl


1254
3
2-CH3-phenyl
Cyclobutyl


1255
3
2-CH3-phenyl
cyclopentyl


1256
3
2-CH3-phenyl
cyclohexyl


1257
3
2-CH3-phenyl
3-pyridyl


1258
3
2-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


1259
3
2-CH3-phenyl
1H-imidazol-4-yl


1260
3
2-CH3-phenyl
2-furanyl


1261
3
4-OH-Phenyl
Ethyl


1262
3
4-OH-Phenyl
n-propyl


1263
3
4-OH-Phenyl
Isopropyl


1264
3
4-OH-Phenyl
—CH2CH(CH3)2


1265
3
4-OH-Phenyl
CF3


1266
3
4-OH-Phenyl
—CH2CF3


1267
3
4-OH-Phenyl
—CH2CH2CF3


1268
3
4-OH-Phenyl
cyclopropyl


1269
3
4-OH-Phenyl
Cyclobutyl


1270
3
4-OH-Phenyl
cyclopentyl


1271
3
4-OH-Phenyl
cyclohexyl


1272
3
4-OH-Phenyl
3-pyridyl


1273
3
4-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


1274
3
4-OH-Phenyl
1H-imidazol-4-yl


1275
3
4-OH-Phenyl
2-furanyl


1276
3
2-OH-Phenyl
Ethyl


1277
3
2-OH-Phenyl
n-propyl


1278
3
2-OH-Phenyl
Isopropyl


1279
3
2-OH-Phenyl
—CH2CH(CH3)2


1280
3
2-OH-Phenyl
CF3


1281
3
2-OH-Phenyl
—CH2CF3


1282
3
2-OH-Phenyl
—CH2CH2CF3


1283
3
2-OH-Phenyl
cyclopropyl


1284
3
2-OH-Phenyl
Cyclobutyl


1285
3
2-OH-Phenyl
cyclopentyl


1286
3
2-OH-Phenyl
cyclohexyl


1287
3
2-OH-Phenyl
3-pyridyl


1288
3
2-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


1289
3
2-OH-Phenyl
1H-imidazol-4-yl


1290
3
2-OH-Phenyl
2-furanyl


1291
3
3-OMe-Phenyl
Ethyl


1292
3
3-OMe-Phenyl
n-propyl


1293
3
3-OMe-Phenyl
Isopropyl


1294
3
3-OMe-Phenyl
—CH2CH(CH3)2


1295
3
3-OMe-Phenyl
CF3


1296
3
3-OMe-Phenyl
—CH2CF3


1297
3
3-OMe-Phenyl
—CH2CH2CF3


1298
3
3-OMe-Phenyl
cyclopropyl


1299
3
3-OMe-Phenyl
Cyclobutyl


1300
3
3-OMe-Phenyl
cyclopentyl


1301
3
3-OMe-Phenyl
cyclohexyl


1302
3
3-OMe-Phenyl
3-pyridyl


1303
3
3-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


1304
3
3-OMe-Phenyl
1H-imidazol-4-yl


1305
3
3-OMe-Phenyl
2-furanyl


1306
3
4-CN-Phenyl
Ethyl


1307
3
4-CN-Phenyl
n-propyl


1308
3
4-CN-Phenyl
Isopropyl


1309
3
4-CN-Phenyl
—CH2CH(CH3)2


1310
3
4-CN-Phenyl
CF3


1311
3
4-CN-Phenyl
—CH2CF3


1312
3
4-CN-Phenyl
—CH2CH2CF3


1313
3
4-CN-Phenyl
cyclopropyl


1314
3
4-CN-Phenyl
Cyclobutyl


1315
3
4-CN-Phenyl
cyclopentyl


1316
3
4-CN-Phenyl
cyclohexyl


1317
3
4-CN-Phenyl
3-pyridyl


1318
3
4-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


1319
3
4-CN-Phenyl
1H-imidazol-4-yl


1320
3
4-CN-Phenyl
2-furanyl


1321
3
2-CN-Phenyl
Ethyl


1322
3
2-CN-Phenyl
n-propyl


1323
3
2-CN-Phenyl
Isopropyl


1324
3
2-CN-Phenyl
—CH2CH(CH3)2


1325
3
2-CN-Phenyl
CF3


1326
3
2-CN-Phenyl
—CH2CF3


1327
3
2-CN-Phenyl
—CH2CH2CF3


1328
3
2-CN-Phenyl
cyclopropyl


1329
3
2-CN-Phenyl
Cyclobutyl


1330
3
2-CN-Phenyl
cyclopentyl


1331
3
2-CN-Phenyl
cyclohexyl


1332
3
2-CN-Phenyl
3-pyridyl


1333
3
2-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


1334
3
2-CN-Phenyl
1H-imidazol-4-yl


1335
3
2-CN-Phenyl
2-furanyl


1336
3
3-F-Phenyl
Ethyl


1337
3
3-F-Phenyl
n-propyl


1338
3
3-F-Phenyl
Isopropyl


1339
3
3-F-Phenyl
—CH2CH(CH3)2


1340
3
3-F-Phenyl
CF3


1341
3
3-F-Phenyl
—CH2CF3


1342
3
3-F-Phenyl
—CH2CH2CF3


1343
3
3-F-Phenyl
cyclopropyl


1344
3
3-F-Phenyl
Cyclobutyl


1345
3
3-F-Phenyl
cyclopentyl


1346
3
3-F-Phenyl
cyclohexyl


1347
3
3-F-Phenyl
3-pyridyl


1348
3
3-F-Phenyl
1-methyl-1H-pyrazol-4-yl


1349
3
3-F-Phenyl
1H-imidazol-4-yl


1350
3
3-F-Phenyl
2-furanyl


1351
3
2-Cl-Phenyl
Ethyl


1352
3
2-Cl-Phenyl
n-propyl


1353
3
2-Cl-Phenyl
Isopropyl


1354
3
2-Cl-Phenyl
—CH2CH(CH3)2


1355
3
2-Cl-Phenyl
CF3


1356
3
2-Cl-Phenyl
—CH2CF3


1357
3
2-Cl-Phenyl
—CH2CH2CF3


1358
3
2-Cl-Phenyl
cyclopropyl


1359
3
2-Cl-Phenyl
Cyclobutyl


1360
3
2-Cl-Phenyl
cyclopentyl


1361
3
2-Cl-Phenyl
cyclohexyl


1362
3
2-Cl-Phenyl
3-pyridyl


1363
3
2-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


1364
3
2-Cl-Phenyl
1H-imidazol-4-yl


1365
3
2-Cl-Phenyl
2-furanyl


1366
3
4-Cl-Phenyl
Ethyl


1367
3
4-Cl-Phenyl
n-propyl


1368
3
4-Cl-Phenyl
Isopropyl


1369
3
4-Cl-Phenyl
—CH2CH(CH3)2


1370
3
4-Cl-Phenyl
CF3


1371
3
4-Cl-Phenyl
—CH2CF3


1372
3
4-Cl-Phenyl
—CH2CH2CF3


1373
3
4-Cl-Phenyl
cyclopropyl


1374
3
4-Cl-Phenyl
Cyclobutyl


1375
3
4-Cl-Phenyl
cyclopentyl


1376
3
4-Cl-Phenyl
cyclohexyl


1377
3
4-Cl-Phenyl
3-pyridyl


1378
3
4-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


1379
3
4-Cl-Phenyl
1H-imidazol-4-yl


1380
3
4-Cl-Phenyl
2-furanyl


1381
3
3-Br-Phenyl
Ethyl


1382
3
3-Br-Phenyl
n-propyl


1383
3
3-Br-Phenyl
Isopropyl


1384
3
3-Br-Phenyl
—CH2CH(CH3)2


1385
3
3-Br-Phenyl
CF3


1386
3
3-Br-Phenyl
—CH2CF3


1387
3
3-Br-Phenyl
—CH2CH2CF3


1388
3
3-Br-Phenyl
cyclopropyl


1389
3
3-Br-Phenyl
Cyclobutyl


1390
3
3-Br-Phenyl
cyclopentyl


1391
3
3-Br-Phenyl
cyclohexyl


1392
3
3-Br-Phenyl
3-pyridyl


1393
3
3-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


1394
3
3-Br-Phenyl
1H-imidazol-4-yl


1395
3
3-Br-Phenyl
2-furanyl


1396
3
2-CF3-Phenyl
Ethyl


1397
3
2-CF3-Phenyl
n-propyl


1398
3
2-CF3-Phenyl
Isopropyl


1399
3
2-CF3-Phenyl
—CH2CH(CH3)2


1400
3
2-CF3-Phenyl
CF3


1401
3
2-CF3-Phenyl
—CH2CF3


1402
3
2-CF3-Phenyl
—CH2CH2CF3


1403
3
2-CF3-Phenyl
cyclopropyl


1404
3
2-CF3-Phenyl
Cyclobutyl


1405
3
2-CF3-Phenyl
cyclopentyl


1406
3
2-CF3-Phenyl
cyclohexyl


1407
3
2-CF3-Phenyl
3-pyridyl


1408
3
2-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


1409
3
2-CF3-Phenyl
1H-imidazol-4-yl


1410
3
2-CF3-Phenyl
2-furanyl


1411
3
4-CF3-Phenyl
Ethyl


1412
3
4-CF3-Phenyl
n-propyl


1413
3
4-CF3-Phenyl
Isopropyl


1414
3
4-CF3-Phenyl
—CH2CH(CH3)2


1415
3
4-CF3-Phenyl
CF3


1416
3
4-CF3-Phenyl
—CH2CF3


1417
3
4-CF3-Phenyl
—CH2CH2CF3


1418
3
4-CF3-Phenyl
cyclopropyl


1419
3
4-CF3-Phenyl
Cyclobutyl


1420
3
4-CF3-Phenyl
cyclopentyl


1421
3
4-CF3-Phenyl
cyclohexyl


1422
3
4-CF3-Phenyl
3-pyridyl


1423
3
4-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


1424
3
4-CF3-Phenyl
1H-imidazol-4-yl


1425
3
4-CF3-Phenyl
2-furanyl


1426
3
3-iPr-Phenyl
Ethyl


1427
3
3-iPr-Phenyl
n-propyl


1428
3
3-iPr-Phenyl
Isopropyl


1429
3
3-iPr-Phenyl
—CH2CH(CH3)2


1430
3
3-iPr-Phenyl
CF3


1431
3
3-iPr-Phenyl
—CH2CF3


1432
3
3-iPr-Phenyl
—CH2CH2CF3


1433
3
3-iPr-Phenyl
cyclopropyl


1434
3
3-iPr-Phenyl
Cyclobutyl


1435
3
3-iPr-Phenyl
cyclopentyl


1436
3
3-iPr-Phenyl
cyclohexyl


1437
3
3-iPr-Phenyl
3-pyridyl


1438
3
3-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


1439
3
3-iPr-Phenyl
1H-imidazol-4-yl


1440
3
3-iPr-Phenyl
2-furanyl


1441
3
2-morpholino-phenyl
Ethyl


1442
3
2-morpholino-phenyl
n-propyl


1443
3
2-morpholino-phenyl
isopropyl


1444
3
2-morpholino-phenyl
—CH2CH(CH3)2


1445
3
2-morpholino-phenyl
CF3


1446
3
2-morpholino-phenyl
—CH2CF3


1447
3
2-morpholino-phenyl
—CH2CH2CF3


1448
3
2-morpholino-phenyl
cyclopropyl


1449
3
2-morpholino-phenyl
Cyclobutyl


1450
3
2-morpholino-phenyl
cyclopentyl


1451
3
2-morpholino-phenyl
cyclohexyl


1452
3
2-morpholino-phenyl
3-pyridyl


1453
3
2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1454
3
2-morpholino-phenyl
1H-imidazol-4-yl


1455
3
2-morpholino-phenyl
2-furanyl


1456
3
4-morpholino-phenyl
ethyl


1457
3
4-morpholino-phenyl
n-propyl


1458
3
4-morpholino-phenyl
isopropyl


1459
3
4-morpholino-phenyl
—CH2CH(CH3)2


1460
3
4-morpholino-phenyl
CF3


1461
3
4-morpholino-phenyl
—CH2CF3


1462
3
4-morpholino-phenyl
—CH2CH2CF3


1463
3
4-morpholino-phenyl
cyclopropyl


1464
3
4-morpholino-phenyl
Cyclobutyl


1465
3
4-morpholino-phenyl
cyclopentyl


1466
3
4-morpholino-phenyl
cyclohexyl


1467
3
4-morpholino-phenyl
3-pyridyl


1468
3
4-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1469
3
4-morpholino-phenyl
1H-imidazol-4-yl


1470
3
4-morpholino-phenyl
2-furanyl


1471
3
4-methyl-2-morpholino-phenyl
ethyl


1472
3
4-methyl-2-morpholino-phenyl
n-propyl


1473
3
4-methyl-2-morpholino-phenyl
isopropyl


1474
3
4-methyl-2-morpholino-phenyl
—CH2CH(CH3)2


1475
3
4-methyl-2-morpholino-phenyl
CF3


1476
3
4-methyl-2-morpholino-phenyl
—CH2CF3


1477
3
4-methyl-2-morpholino-phenyl
—CH2CH2CF3


1478
3
4-methyl-2-morpholino-phenyl
cyclopropyl


1479
3
4-methyl-2-morpholino-phenyl
Cyclobutyl


1480
3
4-methyl-2-morpholino-phenyl
cyclopentyl


1481
3
4-methyl-2-morpholino-phenyl
cyclohexyl


1482
3
4-methyl-2-morpholino-phenyl
3-pyridyl


1483
3
4-methyl-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1484
3
4-methyl-2-morpholino-phenyl
1H-imidazol-4-yl


1485
3
4-methyl-2-morpholino-phenyl
2-furanyl


1486
4
4-CH3-phenyl
ethyl


1487
4
4-CH3-phenyl
n-propyl


1488
4
4-CH3-phenyl
isopropyl


1489
4
4-CH3-phenyl
—CH2CH(CH3)2


1490
4
4-CH3-phenyl
CF3


1491
4
4-CH3-phenyl
—CH2CF3


1492
4
4-CH3-phenyl
—CH2CH2CF3


1493
4
4-CH3-phenyl
cyclopropyl


1494
4
4-CH3-phenyl
Cyclobutyl


1495
4
4-CH3-phenyl
cyclopentyl


1496
4
4-CH3-phenyl
cyclohexyl


1497
4
4-CH3-phenyl
3-pyridyl


1498
4
4-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


1499
4
4-CH3-phenyl
1H-imidazol-4-yl


1500
4
4-CH3-phenyl
2-furanyl


1501
4
3-CH3-phenyl
ethyl


1502
4
3-CH3-phenyl
n-propyl


1503
4
3-CH3-phenyl
isopropyl


1504
4
3-CH3-phenyl
—CH2CH(CH3)2


1505
4
3-CH3-phenyl
CF3


1506
4
3-CH3-phenyl
—CH2CF3


1507
4
3-CH3-phenyl
—CH2CH2CF3


1508
4
3-CH3-phenyl
cyclopropyl


1509
4
3-CH3-phenyl
Cyclobutyl


1510
4
3-CHs-phenyl
cyclopentyl


1511
4
3-CH3-phenyl
cyclohexyl


1512
4
3-CH3-phenyl
3-pyridyl


1513
4
3-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


1514
4
3-CH3-phenyl
1H-imidazol-4-yl


1515
4
3-CH3-phenyl
2-furanyl


1516
4
3-OH-Phenyl
ethyl


1517
4
3-OH-Phenyl
n-propyl


1518
4
3-OH-Phenyl
isopropyl


1519
4
3-OH-Phenyl
—CH2CH(CH3)2


1520
4
3-OH-Phenyl
CF3


1521
4
3-OH-Phenyl
—CH2CF3


1522
4
3-OH-Phenyl
—CH2CH2CF3


1523
4
3-OH-Phenyl
cyclopropyl


1524
4
3-OH-Phenyl
Cyclobutyl


1525
4
3-OH-Phenyl
cyclopentyl


1526
4
3-OH-Phenyl
cyclohexyl


1527
4
3-OH-Phenyl
3-pyridyl


1528
4
3-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


1529
4
3-OH-Phenyl
1H-imidazol-4-yl


1530
4
3-OH-Phenyl
2-furanyl


1531
4
4-OMe-Phenyl
ethyl


1532
4
4-OMe-Phenyl
n-propyl


1533
4
4-OMe-Phenyl
isopropyl


1534
4
4-OMe-Phenyl
—CH2CH(CH3)2


1535
4
4-OMe-Phenyl
CF3


1536
4
4-OMe-Phenyl
—CH2CF3


1537
4
4-OMe-Phenyl
—CH2CH2CF3


1538
4
4-OMe-Phenyl
cyclopropyl


1539
4
4-OMe-Phenyl
Cyclobutyl


1540
4
4-OMe-Phenyl
cyclopentyl


1541
4
4-OMe-Phenyl
cyclohexyl


1542
4
4-OMe-Phenyl
3-pyridyl


1543
4
4-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


1544
4
4-OMe-Phenyl
1H-imidazol-4-yl


1545
4
4-OMe-Phenyl
2-furanyl


1546
4
2-OMe-Phenyl
ethyl


1547
4
2-OMe-Phenyl
n-propyl


1548
4
2-OMe-Phenyl
isopropyl


1549
4
2-OMe-Phenyl
—CH2CH(CH3)2


1550
4
2-OMe-Phenyl
CF3


1551
4
2-OMe-Phenyl
—CH2CF3


1552
4
2-OMe-Phenyl
—CH2CH2CF3


1553
4
2-OMe-Phenyl
cyclopropyl


1554
4
2-OMe-Phenyl
Cyclobutyl


1555
4
2-OMe-Phenyl
cyclopentyl


1556
4
2-OMe-Phenyl
cyclohexyl


1557
4
2-OMe-Phenyl
3-pyridyl


1558
4
2-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


1559
4
2-OMe-Phenyl
1H-imidazol-4-yl


1560
4
2-OMe-Phenyl
2-furanyl


1561
4
3-CN-Phenyl
ethyl


1562
4
3-CN-Phenyl
n-propyl


1563
4
3-CN-Phenyl
isopropyl


1564
4
3-CN-Phenyl
—CH2CH(CH3)2


1565
4
3-CN-Phenyl
CF3


1566
4
3-CN-Phenyl
—CH2CF3


1567
4
3-CN-Phenyl
—CH2CH2CF3


1568
4
3-CN-Phenyl
cyclopropyl


1569
4
3-CN-Phenyl
Cyclobutyl


1570
4
3-CN-Phenyl
cyclopentyl


1571
4
3-CN-Phenyl
cyclohexyl


1572
4
3-CN-Phenyl
3-pyridyl


1573
4
3-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


1574
4
3-CN-Phenyl
1H-imidazol-4-yl


1575
4
3-CN-Phenyl
2-furanyl


1576
4
2-F-Phenyl
ethyl


1577
4
2-F-Phenyl
n-propyl


1578
4
2-F-Phenyl
isopropyl


1579
4
2-F-Phenyl
—CH2CH(CH3)2


1580
4
2-F-Phenyl
CF3


1581
4
2-F-Phenyl
—CH2CF3


1582
4
2-F-Phenyl
—CH2CH2CF3


1583
4
2-F-Phenyl
cyclopropyl


1584
4
2-F-Phenyl
Cyclobutyl


1585
4
2-F-Phenyl
cyclopentyl


1586
4
2-F-Phenyl
cyclohexyl


1587
4
2-F-Phenyl
3-pyridyl


1588
4
2-F-Phenyl
1-methyl-1H-pyrazol-4-yl


1589
4
2-F-Phenyl
1H-imidazol-4-yl


1590
4
2-F-Phenyl
2-furanyl


1591
4
4-F-Phenyl
ethyl


1592
4
4-F-Phenyl
n-propyl


1593
4
4-F-Phenyl
isopropyl


1594
4
4-F-Phenyl
—CH2CH(CH3)2


1595
4
4-F-Phenyl
CF3


1596
4
4-F-Phenyl
—CH2CF3


1597
4
4-F-Phenyl
—CH2CH2CF3


1598
4
4-F-Phenyl
cyclopropyl


1599
4
4-F-Phenyl
Cyclobutyl


1600
4
4-F-Phenyl
cyclopentyl


1601
4
4-F-Phenyl
cyclohexyl


1602
4
4-F-Phenyl
3-pyridyl


1603
4
4-F-Phenyl
1-methyl-1H-pyrazol-4-yl


1604
4
4-F-Phenyl
1H-imidazol-4-yl


1605
4
4-F-Phenyl
2-furanyl


1606
4
3-Cl-Phenyl
ethyl


1607
4
3-Cl-Phenyl
n-propyl


1608
4
3-Cl-Phenyl
isopropyl


1609
4
3-Cl-Phenyl
—CH2CH(CH3)2


1610
4
3-Cl-Phenyl
CF3


1611
4
3-Cl-Phenyl
—CH2CF3


1612
4
3-Cl-Phenyl
—CH2CH2CF3


1613
4
3-Cl-Phenyl
cyclopropyl


1614
4
3-Cl-Phenyl
Cyclobutyl


1615
4
3-Cl-Phenyl
cyclopentyl


1616
4
3-Cl-Phenyl
cyclohexyl


1617
4
3-Cl-Phenyl
3-pyridyl


1618
4
3-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


1619
4
3-Cl-Phenyl
1H-imidazol-4-yl


1620
4
3-Cl-Phenyl
2-furanyl


1621
4
2-Br-Phenyl
ethyl


1622
4
2-Br-Phenyl
n-propyl


1623
4
2-Br-Phenyl
isopropyl


1624
4
2-Br-Phenyl
—CH2CH(CH3)2


1625
4
2-Br-Phenyl
CF3


1626
4
2-Br-Phenyl
—CH2CF3


1627
4
2-Br-Phenyl
—CH2CH2CF3


1628
4
2-Br-Phenyl
cyclopropyl


1629
4
2-Br-Phenyl
Cyclobutyl


1630
4
2-Br-Phenyl
cyclopentyl


1631
4
2-Br-Phenyl
cyclohexyl


1632
4
2-Br-Phenyl
3-pyridyl


1633
4
2-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


1634
4
2-Br-Phenyl
1H-imidazol-4-yl


1635
4
2-Br-Phenyl
2-furanyl


1636
4
4-Br-Phenyl
ethyl


1637
4
4-Br-Phenyl
n-propyl


1638
4
4-Br-Phenyl
isopropyl


1639
4
4-Br-Phenyl
—CH2CH(CH3)2


1640
4
4-Br-Phenyl
CF3


1641
4
4-Br-Phenyl
—CH2CF3


1642
4
4-Br-Phenyl
—CH2CH2CF3


1643
4
4-Br-Phenyl
cyclopropyl


1644
4
4-Br-Phenyl
Cyclobutyl


1645
4
4-Br-Phenyl
cyclopentyl


1646
4
4-Br-Phenyl
cyclohexyl


1647
4
4-Br-Phenyl
3-pyridyl


1648
4
4-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


1649
4
4-Br-Phenyl
1H-imidazol-4-yl


1650
4
4-Br-Phenyl
2-furanyl


1651
4
3-CF3-Phenyl
ethyl


1652
4
3-CF3-Phenyl
n-propyl


1653
4
3-CF3-Phenyl
isopropyl


1654
4
3-CF3-Phenyl
—CH2CH(CH3)2


1655
4
3-CF3-Phenyl
CF3


1656
4
3-CF3-Phenyl
—CH2CF3


1657
4
3-CF3-Phenyl
—CH2CH2CF3


1658
4
3-CF3-Phenyl
cyclopropyl


1659
4
3-CF3-Phenyl
Cyclobutyl


1660
4
3-CF3-Phenyl
cyclopentyl


1661
4
3-CF3-Phenyl
cyclohexyl


1662
4
3-CF3-Phenyl
3-pyridyl


1663
4
3-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


1664
4
3-CF3-Phenyl
1H-imidazol-4-yl


1665
4
3-CF3-Phenyl
2-furanyl


1666
4
2-iPr-Phenyl
ethyl


1667
4
2-iPr-Phenyl
n-propyl


1668
4
2-iPr-Phenyl
isopropyl


1669
4
2-iPr-Phenyl
—CH2CH(CH3)2


1670
4
2-iPr-Phenyl
CF3


1671
4
2-iPr-Phenyl
—CH2CF3


1672
4
2-iPr-Phenyl
—CH2CH2CF3


1673
4
2-iPr-Phenyl
cyclopropyl


1674
4
2-iPr-Phenyl
Cyclobutyl


1675
4
2-iPr-Phenyl
cyclopentyl


1676
4
2-iPr-Phenyl
cyclohexyl


1677
4
2-iPr-Phenyl
3-pyridyl


1678
4
2-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


1679
4
2-iPr-Phenyl
1H-imidazol-4-yl


1680
4
2-iPr-Phenyl
2-furanyl


1681
4
4-iPr-Phenyl
ethyl


1682
4
4-iPr-Phenyl
n-propyl


1683
4
4-iPr-Phenyl
isopropyl


1684
4
4-iPr-Phenyl
—CH2CH(CH3)2


1685
4
4-iPr-Phenyl
CF3


1686
4
4-iPr-Phenyl
—CH2CF3


1687
4
4-iPr-Phenyl
—CH2CH2CF3


1688
4
4-iPr-Phenyl
cyclopropyl


1689
4
4-iPr-Phenyl
Cyclobutyl


1690
4
4-iPr-Phenyl
cyclopentyl


1691
4
4-iPr-Phenyl
cyclohexyl


1692
4
4-iPr-Phenyl
3-pyridyl


1693
4
4-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


1694
4
4-iPr-Phenyl
1H-imidazol-4-yl


1695
4
4-iPr-Phenyl
2-furanyl


1696
4
3-morpholino-phenyl
ethyl


1697
4
3-morpholino-phenyl
n-propyl


1698
4
3-morpholino-phenyl
isopropyl


1699
4
3-morpholino-phenyl
—CH2CH(CH3)2


1700
4
3-morpholino-phenyl
CF3


1701
4
3-morpholino-phenyl
—CH2CF3


1702
4
3-morpholino-phenyl
—CH2CH2CF3


1703
4
3-morpholino-phenyl
cyclopropyl


1704
4
3-morpholino-phenyl
Cyclobutyl


1705
4
3-morpholino-phenyl
cyclopentyl


1706
4
3-morpholino-phenyl
cyclohexyl


1707
4
3-morpholino-phenyl
3-pyridyl


1708
4
3-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1709
4
3-morpholino-phenyl
1H-imidazol-4-yl


1710
4
3-morpholino-phenyl
2-furanyl


1711
4
4-cyano-2-morpholino-phenyl
ethyl


1712
4
4-cyano-2-morpholino-phenyl
n-propyl


1713
4
4-cyano-2-morpholino-phenyl
isopropyl


1714
4
4-cyano-2-morpholino-phenyl
—CH2CH(CH3)2


1715
4
4-cyano-2-morpholino-phenyl
CF3


1716
4
4-cyano-2-morpholino-phenyl
—CH2CF3


1717
4
4-cyano-2-morpholino-phenyl
—CH2CH2CF3


1718
4
4-cyano-2-morpholino-phenyl
cyclopropyl


1719
4
4-cyano-2-morpholino-phenyl
Cyclobutyl


1720
4
4-cyano-2-morpholino-phenyl
cyclopentyl


1721
4
4-cyano-2-morpholino-phenyl
cyclohexyl


1722
4
4-cyano-2-morpholino-phenyl
3-pyridyl


1723
4
4-cyano-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1724
4
4-cyano-2-morpholino-phenyl
1H-imidazol-4-yl


1725
4
4-cyano-2-morpholino-phenyl
2-furanyl


1726
4
4-hydroxy-2-morpholino-phenyl
ethyl


1727
4
4-hydroxy-2-morpholino-phenyl
n-propyl


1728
4
4-hydroxy-2-morpholino-phenyl
isopropyl


1729
4
4-hydroxy-2-morpholino-phenyl
—CH2CH(CH3)2


1730
4
4-hydroxy-2-morpholino-phenyl
CF3


1731
4
4-hydroxy-2-morpholino-phenyl
—CH2CF3


1732
4
4-hydroxy-2-morpholino-phenyl
—CH2CH2CF3


1733
4
4-hydroxy-2-morpholino-phenyl
cyclopropyl


1734
4
4-hydroxy-2-morpholino-phenyl
Cyclobutyl


1735
4
4-hydroxy-2-morpholino-phenyl
cyclopentyl


1736
4
4-hydroxy-2-morpholino-phenyl
cyclohexyl


1737
4
4-hydroxy-2-morpholino-phenyl
3-pyridyl


1738
4
4-hydroxy-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1739
4
4-hydroxy-2-morpholino-phenyl
1H-imidazol-4-yl


1740
4
4-hydroxy-2-morpholino-phenyl
2-furanyl


1741
4
2-CH3-phenyl
Ethyl


1742
4
2-CH3-phenyl
n-propyl


1743
4
2-CH3-phenyl
Isopropyl


1744
4
2-CH3-phenyl
—CH2CH(CH3)2


1745
4
2-CH3-phenyl
CF3


1746
4
2-CH3-phenyl
—CH2CF3


1747
4
2-CH3-phenyl
—CH2CH2CF3


1748
4
2-CH3-phenyl
cyclopropyl


1749
4
2-CH3-phenyl
Cyclobutyl


1750
4
2-CH3-phenyl
cyclopentyl


1751
4
2-CH3-phenyl
cyclohexyl


1752
4
2-CH3-phenyl
3-pyridyl


1753
4
2-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


1754
4
2-CH3-phenyl
1H-imidazol-4-yl


1755
4
2-CH3-phenyl
2-furanyl


1756
4
4-OH-Phenyl
Ethyl


1757
4
4-OH-Phenyl
n-propyl


1758
4
4-OH-Phenyl
Isopropyl


1759
4
4-OH-Phenyl
—CH2CH(CH3)2


1760
4
4-OH-Phenyl
CF3


1761
4
4-OH-Phenyl
—CH2CF3


1762
4
4-OH-Phenyl
—CH2CH2CF3


1763
4
4-OH-Phenyl
cyclopropyl


1764
4
4-OH-Phenyl
Cyclobutyl


1765
4
4-OH-Phenyl
cyclopentyl


1766
4
4-OH-Phenyl
cyclohexyl


1767
4
4-OH-Phenyl
3-pyridyl


1768
4
4-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


1769
4
4-OH-Phenyl
1H-imidazol-4-yl


1770
4
4-OH-Phenyl
2-furanyl


1771
4
2-OH-Phenyl
Ethyl


1772
4
2-OH-Phenyl
n-propyl


1773
4
2-OH-Phenyl
Isopropyl


1774
4
2-OH-Phenyl
—CH2CH(CH3)2


1775
4
2-OH-Phenyl
CF3


1776
4
2-OH-Phenyl
—CH2CF3


1777
4
2-OH-Phenyl
—CH2CH2CF3


1778
4
2-OH-Phenyl
cyclopropyl


1779
4
2-OH-Phenyl
Cyclobutyl


1780
4
2-OH-Phenyl
cyclopentyl


1781
4
2-OH-Phenyl
cyclohexyl


1782
4
2-OH-Phenyl
3-pyridyl


1783
4
2-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


1784
4
2-OH-Phenyl
1H-imidazol-4-yl


1785
4
2-OH-Phenyl
2-furanyl


1786
4
3-OMe-Phenyl
Ethyl


1787
4
3-OMe-Phenyl
n-propyl


1788
4
3-OMe-Phenyl
Isopropyl


1789
4
3-OMe-Phenyl
—CH2CH(CH3)2


1790
4
3-OMe-Phenyl
CF3


1791
4
3-OMe-Phenyl
—CH2CF3


1792
4
3-OMe-Phenyl
—CH2CH2CF3


1793
4
3-OMe-Phenyl
cyclopropyl


1794
4
3-OMe-Phenyl
Cyclobutyl


1795
4
3-OMe-Phenyl
cyclopentyl


1796
4
3-OMe-Phenyl
cyclohexyl


1797
4
3-OMe-Phenyl
3-pyridyl


1798
4
3-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


1799
4
3-OMe-Phenyl
1H-imidazol-4-yl


1800
4
3-OMe-Phenyl
2-furanyl


1801
4
4-CN-Phenyl
Ethyl


1802
4
4-CN-Phenyl
n-propyl


1803
4
4-CN-Phenyl
Isopropyl


1804
4
4-CN-Phenyl
—CH2CH(CH3)2


1805
4
4-CN-Phenyl
CF3


1806
4
4-CN-Phenyl
—CH2CF3


1807
4
4-CN-Phenyl
—CH2CH2CF3


1808
4
4-CN-Phenyl
cyclopropyl


1809
4
4-CN-Phenyl
Cyclobutyl


1810
4
4-CN-Phenyl
cyclopentyl


1811
4
4-CN-Phenyl
cyclohexyl


1812
4
4-CN-Phenyl
3-pyridyl


1813
4
4-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


1814
4
4-CN-Phenyl
1H-imidazol-4-yl


1815
4
4-CN-Phenyl
2-furanyl


1816
4
2-CN-Phenyl
Ethyl


1817
4
2-CN-Phenyl
n-propyl


1818
4
2-CN-Phenyl
Isopropyl


1819
4
2-CN-Phenyl
—CH2CH(CH3)2


1820
4
2-CN-Phenyl
CF3


1821
4
2-CN-Phenyl
—CH2CF3


1822
4
2-CN-Phenyl
—CH2CH2CF3


1823
4
2-CN-Phenyl
cyclopropyl


1824
4
2-CN-Phenyl
Cyclobutyl


1825
4
2-CN-Phenyl
cyclopentyl


1826
4
2-CN-Phenyl
cyclohexyl


1827
4
2-CN-Phenyl
3-pyridyl


1828
4
2-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


1829
4
2-CN-Phenyl
1H-imidazol-4-yl


1830
4
2-CN-Phenyl
2-furanyl


1831
4
3-F-Phenyl
Ethyl


1832
4
3-F-Phenyl
n-propyl


1833
4
3-F-Phenyl
Isopropyl


1834
4
3-F-Phenyl
—CH2CH(CH3)2


1835
4
3-F-Phenyl
CF3


1836
4
3-F-Phenyl
—CH2CF3


1837
4
3-F-Phenyl
—CH2CH2CF3


1838
4
3-F-Phenyl
cyclopropyl


1839
4
3-F-Phenyl
Cyclobutyl


1840
4
3-F-Phenyl
cyclopentyl


1841
4
3-F-Phenyl
cyclohexyl


1842
4
3-F-Phenyl
3-pyridyl


1843
4
3-F-Phenyl
1-methyl-1H-pyrazol-4-yl


1844
4
3-F-Phenyl
1H-imidazol-4-yl


1845
4
3-F-Phenyl
2-furanyl


1846
4
2-Cl-Phenyl
Ethyl


1847
4
2-Cl-Phenyl
n-propyl


1848
4
2-Cl-Phenyl
Isopropyl


1849
4
2-Cl-Phenyl
—CH2CH(CH3)2


1850
4
2-Cl-Phenyl
CF3


1851
4
2-Cl-Phenyl
—CH2CF3


1852
4
2-Cl-Phenyl
—CH2CH2CF3


1853
4
2-Cl-Phenyl
cyclopropyl


1854
4
2-Cl-Phenyl
Cyclobutyl


1855
4
2-Cl-Phenyl
cyclopentyl


1856
4
2-Cl-Phenyl
cyclohexyl


1857
4
2-Cl-Phenyl
3-pyridyl


1858
4
2-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


1859
4
2-Cl-Phenyl
1H-imidazol-4-yl


1860
4
2-Cl-Phenyl
2-furanyl


1861
4
4-Cl-Phenyl
Ethyl


1862
4
4-Cl-Phenyl
n-propyl


1863
4
4-Cl-Phenyl
Isopropyl


1864
4
4-Cl-Phenyl
—CH2CH(CH3)2


1865
4
4-Cl-Phenyl
CF3


1866
4
4-Cl-Phenyl
—CH2CF3


1867
4
4-Cl-Phenyl
—CH2CH2CF3


1868
4
4-Cl-Phenyl
cyclopropyl


1869
4
4-Cl-Phenyl
Cyclobutyl


1870
4
4-Cl-Phenyl
cyclopentyl


1871
4
4-Cl-Phenyl
cyclohexyl


1872
4
4-Cl-Phenyl
3-pyridyl


1873
4
4-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


1874
4
4-Cl-Phenyl
1H-imidazol-4-yl


1875
4
4-Cl-Phenyl
2-furanyl


1876
4
3-Br-Phenyl
Ethyl


1877
4
3-Br-Phenyl
n-propyl


1878
4
3-Br-Phenyl
Isopropyl


1879
4
3-Br-Phenyl
—CH2CH(CH3)2


1880
4
3-Br-Phenyl
CF3


1881
4
3-Br-Phenyl
—CH2CF3


1882
4
3-Br-Phenyl
—CH2CH2CF3


1883
4
3-Br-Phenyl
cyclopropyl


1884
4
3-Br-Phenyl
Cyclobutyl


1885
4
3-Br-Phenyl
cyclopentyl


1886
4
3-Br-Phenyl
cyclohexyl


1887
4
3-Br-Phenyl
3-pyridyl


1888
4
3-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


1889
4
3-Br-Phenyl
1H-imidazol-4-yl


1890
4
3-Br-Phenyl
2-furanyl


1891
4
2-CF3-Phenyl
Ethyl


1892
4
2-CF3-Phenyl
n-propyl


1893
4
2-CF3-Phenyl
Isopropyl


1894
4
2-CF3-Phenyl
—CH2CH(CH3)2


1895
4
2-CF3-Phenyl
CF3


1896
4
2-CF3-Phenyl
—CH2CF3


1897
4
2-CF3-Phenyl
—CH2CH2CF3


1898
4
2-CF3-Phenyl
cyclopropyl


1899
4
2-CF3-Phenyl
Cyclobutyl


1900
4
2-CF3-Phenyl
cyclopentyl


1901
4
2-CF3-Phenyl
cyclohexyl


1902
4
2-CF3-Phenyl
3-pyridyl


1903
4
2-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


1904
4
2-CF3-Phenyl
1H-imidazol-4-yl


1905
4
2-CF3-Phenyl
2-furanyl


1906
4
4-CF3-Phenyl
Ethyl


1907
4
4-CF3-Phenyl
n-propyl


1908
4
4-CF3-Phenyl
Isopropyl


1909
4
4-CF3-Phenyl
—CH2CH(CH3)2


1910
4
4-CF3-Phenyl
CF3


1911
4
4-CF3-Phenyl
—CH2CF3


1912
4
4-CF3-Phenyl
—CH2CH2CF3


1913
4
4-CF3-Phenyl
cyclopropyl


1914
4
4-CF3-Phenyl
Cyclobutyl


1915
4
4-CF3-Phenyl
cyclopentyl


1916
4
4-CF3-Phenyl
cyclohexyl


1917
4
4-CF3-Phenyl
3-pyridyl


1918
4
4-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


1919
4
4-CF3-Phenyl
1H-imidazol-4-yl


1920
4
4-CF3-Phenyl
2-furanyl


1921
4
3-iPr-Phenyl
Ethyl


1922
4
3-iPr-Phenyl
n-propyl


1923
4
3-iPr-Phenyl
Isopropyl


1924
4
3-iPr-Phenyl
—CH2CH(CH3)2


1925
4
3-iPr-Phenyl
CF3


1926
4
3-iPr-Phenyl
—CH2CF3


1927
4
3-iPr-Phenyl
—CH2CH2CF3


1928
4
3-iPr-Phenyl
cyclopropyl


1929
4
3-iPr-Phenyl
Cyclobutyl


1930
4
3-iPr-Phenyl
cyclopentyl


1931
4
3-iPr-Phenyl
cyclohexyl


1932
4
3-iPr-Phenyl
3-pyridyl


1933
4
3-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


1934
4
3-iPr-Phenyl
1H-imidazol-4-yl


1935
4
3-iPr-Phenyl
2-furanyl


1936
4
2-morpholino-phenyl
Ethyl


1937
4
2-morpholino-phenyl
n-propyl


1938
4
2-morpholino-phenyl
isopropyl


1939
4
2-morpholino-phenyl
—CH2CH(CH3)2


1940
4
2-morpholino-phenyl
CF3


1941
4
2-morpholino-phenyl
—CH2CF3


1942
4
2-morpholino-phenyl
—CH2CH2CF3


1943
4
2-morpholino-phenyl
cyclopropyl


1944
4
2-morpholino-phenyl
Cyclobutyl


1945
4
2-morpholino-phenyl
cyclopentyl


1946
4
2-morpholino-phenyl
cyclohexyl


1947
4
2-morpholino-phenyl
3-pyridyl


1948
4
2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1949
4
2-morpholino-phenyl
1H-imidazol-4-yl


1950
4
2-morpholino-phenyl
2-furanyl


1951
4
4-morpholino-phenyl
ethyl


1952
4
4-morpholino-phenyl
n-propyl


1953
4
4-morpholino-phenyl
isopropyl


1954
4
4-morpholino-phenyl
—CH2CH(CH3)2


1955
4
4-morpholino-phenyl
CF3


1956
4
4-morpholino-phenyl
—CH2CF3


1957
4
4-morpholino-phenyl
—CH2CH2CF3


1958
4
4-morpholino-phenyl
cyclopropyl


1959
4
4-morpholino-phenyl
Cyclobutyl


1960
4
4-morpholino-phenyl
cyclopentyl


1961
4
4-morpholino-phenyl
cyclohexyl


1962
4
4-morpholino-phenyl
3-pyridyl


1963
4
4-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1964
4
4-morpholino-phenyl
1H-imidazol-4-yl


1965
4
4-morpholino-phenyl
2-furanyl


1966
4
4-methyl-2-morpholino-phenyl
ethyl


1967
4
4-methyl-2-morpholino-phenyl
n-propyl


1968
4
4-methyl-2-morpholino-phenyl
isopropyl


1969
4
4-methyl-2-morpholino-phenyl
—CH2CH(CH3)2


1970
4
4-methyl-2-morpholino-phenyl
CF3


1971
4
4-methyl-2-morpholino-phenyl
—CH2CF3


1972
4
4-methyl-2-morpholino-phenyl
—CH2CH2CF3


1973
4
4-methyl-2-morpholino-phenyl
cyclopropyl


1974
4
4-methyl-2-morpholino-phenyl
Cyclobutyl


1975
4
4-methyl-2-morpholino-phenyl
cyclopentyl


1976
4
4-methyl-2-morpholino-phenyl
cyclohexyl


1977
4
4-methyl-2-morpholino-phenyl
3-pyridyl


1978
4
4-methyl-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1979
4
4-methyl-2-morpholino-phenyl
1H-imidazol-4-yl


1980
4
4-methyl-2-morpholino-phenyl
2-furanyl


1981
1
naphthylen-1-yl
Ethyl


1982
1
naphthylen-1-yl
n-propyl


1983
1
naphthylen-1-yl
Isopropyl


1984
1
naphthylen-1-yl
—CH2CH(CH3)2


1985
1
naphthylen-1-yl
CF3


1986
1
naphthylen-1-yl
—CH2CF3


1987
1
naphthylen-1-yl
—CH2CH2CF3


1988
1
naphthylen-1-yl
Cyclopropyl


1989
1
naphthylen-1-yl
Cyclobutyl


1990
1
naphthylen-1-yl
Cyclopentyl


1991
1
naphthylen-1-yl
Cyclohexyl


1992
1
naphthylen-1-yl
3-pyridyl


1993
1
naphthylen-1-yl
1-methyl-1H-pyrazol-4-yl


1994
1
naphthylen-1-yl
1H-imidazol-4-yl


1995
1
naphthylen-1-yl
2-furanyl


1996
1
naphthylen-2-yl
Ethyl


1997
1
naphthylen-2-yl
n-propyl


1998
1
naphthylen-2-yl
Isopropyl


1999
1
naphthylen-2-yl
—CH2CH(CH3)2


2000
1
naphthylen-2-yl
CF3


2001
1
naphthylen-2-yl
—CH2CF3


2002
1
naphthylen-2-yl
—CH2CH2CF3


2003
1
naphthylen-2-yl
Cyclopropyl


2004
1
naphthylen-2-yl
Cyclobutyl


2005
1
naphthylen-2-yl
Cyclopentyl


2006
1
naphthylen-2-yl
Cyclohexyl


2007
1
naphthylen-2-yl
3-pyridyl


2008
1
naphthylen-2-yl
1-methyl-1H-pyrazol-4-yl


2009
1
naphthylen-2-yl
1H-imidazol-4-yl


2010
1
naphthylen-2-yl
2-furanyl


2011
2
naphthylen-1-yl
Ethyl


2012
2
naphthylen-1-yl
n-propyl


2013
2
naphthylen-1-yl
Isopropyl


2014
2
naphthylen-1-yl
—CH2CH(CH3)2


2015
2
naphthylen-1-yl
CF3


2016
2
naphthylen-1-yl
—CH2CF3


2017
2
naphthylen-1-yl
—CH2CH2CF3


2018
2
naphthylen-1-yl
Cyclopropyl


2019
2
naphthylen-1-yl
Cyclobutyl


2020
2
naphthylen-1-yl
Cyclopentyl


2021
2
naphthylen-1-yl
Cyclohexyl


2022
2
naphthylen-1-yl
3-pyridyl


2023
2
naphthylen-1-yl
1-methyl-1H-pyrazol-4-yl


2024
2
naphthylen-1-yl
1H-imidazol-4-yl


2025
2
naphthylen-1-yl
2-furanyl


2026
2
naphthylen-2-yl
Ethyl


2027
2
naphthylen-2-yl
n-propyl


2028
2
naphthylen-2-yl
Isopropyl


2029
2
naphthylen-2-yl
—CH2CH(CH3)2


2030
2
naphthylen-2-yl
CF3


2031
2
naphthylen-2-yl
—CH2CF3


2032
2
naphthylen-2-yl
—CH2CH2CF3


2033
2
naphthylen-2-yl
Cyclopropyl


2034
2
naphthylen-2-yl
Cyclobutyl


2035
2
naphthylen-2-yl
Cyclopentyl


2036
2
naphthylen-2-yl
Cyclohexyl


2037
2
naphthylen-2-yl
3-pyridyl


2038
2
naphthylen-2-yl
1-methyl-1H-pyrazol-4-yl


2039
2
naphthylen-2-yl
1H-imidazol-4-yl


2040
2
naphthylen-2-yl
2-furanyl


2041
3
naphthylen-1-yl
Ethyl


2042
3
naphthylen-1-yl
n-propyl


2043
3
naphthylen-1-yl
Isopropyl


2044
3
naphthylen-1-yl
—CH2CH(CH3)2


2045
3
naphthylen-1-yl
CF3


2046
3
naphthylen-1-yl
—CH2CF3


2047
3
naphthylen-1-yl
—CH2CH2CF3


2048
3
naphthylen-1-yl
Cyclopropyl


2049
3
naphthylen-1-yl
Cyclobutyl


2050
3
naphthylen-1-yl
Cyclopentyl


2051
3
naphthylen-1-yl
Cyclohexyl


2052
3
naphthylen-1-yl
3-pyridyl


2053
3
naphthylen-1-yl
1-methyl-1H-pyrazol-4-yl


2054
3
naphthylen-1-yl
1H-imidazol-4-yl


2055
3
naphthylen-1-yl
2-furanyl


2056
3
naphthylen-2-yl
Ethyl


2057
3
naphthylen-2-yl
n-propyl


2058
3
naphthylen-2-yl
Isopropyl


2059
3
naphthylen-2-yl
—CH2CH(CH3)2


2060
3
naphthylen-2-yl
CF3


2061
3
naphthylen-2-yl
—CH2CF3


2062
3
naphthylen-2-yl
—CH2CH2CF3


2063
3
naphthylen-2-yl
Cyclopropyl


2064
3
naphthylen-2-yl
Cyclobutyl


2065
3
naphthylen-2-yl
Cyclopentyl


2066
3
naphthylen-2-yl
Cyclohexyl


2067
3
naphthylen-2-yl
3-pyridyl


2068
3
naphthylen-2-yl
1-methyl-1H-pyrazol-4-yl


2069
3
naphthylen-2-yl
1H-imidazol-4-yl


2070
3
naphthylen-2-yl
2-furanyl


2071
4
naphthylen-1-yl
Ethyl


2072
4
naphthylen-1-yl
n-propyl


2073
4
naphthylen-1-yl
Isopropyl


2074
4
naphthylen-1-yl
—CH2CH(CH3)2


2075
4
naphthylen-1-yl
CF3


2076
4
naphthylen-1-yl
—CH2CF3


2077
4
naphthylen-1-yl
—CH2CH2CF3


2078
4
naphthylen-1-yl
Cyclopropyl


2079
4
naphthylen-1-yl
Cyclobutyl


2080
4
naphthylen-1-yl
Cyclopentyl


2081
4
naphthylen-1-yl
Cyclohexyl


2082
4
naphthylen-1-yl
3-pyridyl


2083
4
naphthylen-1-yl
1-methyl-1H-pyrazol-4-yl


2084
4
naphthylen-1-yl
1H-imidazol-4-yl


2085
4
naphthylen-1-yl
2-furanyl


2086
4
naphthylen-2-yl
Ethyl


2087
4
naphthylen-2-yl
n-propyl


2088
4
naphthylen-2-yl
Isopropyl


2089
4
naphthylen-2-yl
—CH2CH(CH3)2


2090
4
naphthylen-2-yl
CF3


2091
4
naphthylen-2-yl
—CH2CF3


2092
4
naphthylen-2-yl
—CH2CH2CF3


2093
4
naphthylen-2-yl
Cyclopropyl


2094
4
naphthylen-2-yl
Cyclobutyl


2095
4
naphthylen-2-yl
Cyclopentyl


2096
4
naphthylen-2-yl
Cyclohexyl


2097
4
naphthylen-2-yl
3-pyridyl


2098
4
naphthylen-2-yl
1-methyl-1H-pyrazol-4-yl


2099
4
naphthylen-2-yl
1H-imidazol-4-yl


2100
4
naphthylen-2-yl
2-furanyl









Exemplary embodiments include compounds having the formula (XXXIX)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 32.












TABLE 32





Entry
n
R4
R10c


















1
1
4-CH3-phenyl
Ethyl


2
1
4-CH3-phenyl
n-propyl


3
1
4-CH3-phenyl
Isopropyl


4
1
4-CH3-phenyl
—CH2CH(CH3)2


5
1
4-CH3-phenyl
CF3


6
1
4-CH3-phenyl
—CH2CF3


7
1
4-CH3-phenyl
—CH2CH2CF3


8
1
4-CH3-phenyl
Cyclopropyl


9
1
4-CH3-phenyl
Cyclobutyl


10
1
4-CH3-phenyl
Cyclopentyl


11
1
4-CH3-phenyl
cyclohexyl


12
1
4-CH3-phenyl
3-pyridyl


13
1
4-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


14
1
4-CH3-phenyl
1H-imidazol-4-yl


15
1
4-CH3-phenyl
2-furanyl


16
1
3-CH3-phenyl
ethyl


17
1
3-CH3-phenyl
n-propyl


18
1
3-CH3-phenyl
isopropyl


19
1
3-CH3-phenyl
—CH2CH(CH3)2


20
1
3-CH3-phenyl
CF3


21
1
3-CH3-phenyl
—CH2CF3


22
1
3-CH3-phenyl
—CH2CH2CF3


23
1
3-CH3-phenyl
cyclopropyl


24
1
3-CH3-phenyl
Cyclobutyl


25
1
3-CH3-phenyl
cyclopentyl


26
1
3-CH3-phenyl
cyclohexyl


27
1
3-CH3-phenyl
3-pyridyl


28
1
3-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


29
1
3-CH3-phenyl
1H-imidazol-4-yl


30
1
3-CH3-phenyl
2-furanyl


31
1
3-OH-Phenyl
ethyl


32
1
3-OH-Phenyl
n-propyl


33
1
3-OH-Phenyl
isopropyl


34
1
3-OH-Phenyl
—CH2CH(CH3)2


35
1
3-OH-Phenyl
CF3


36
1
3-OH-Phenyl
—CH2CF3


37
1
3-OH-Phenyl
—CH2CH2CF3


38
1
3-OH-Phenyl
cyclopropyl


39
1
3-OH-Phenyl
Cyclobutyl


40
1
3-OH-Phenyl
cyclopentyl


41
1
3-OH-Phenyl
cyclohexyl


42
1
3-OH-Phenyl
3-pyridyl


43
1
3-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


44
1
3-OH-Phenyl
1H-imidazol-4-yl


45
1
3-OH-Phenyl
2-furanyl


46
1
4-OMe-Phenyl
ethyl


47
1
4-OMe-Phenyl
n-propyl


48
1
4-OMe-Phenyl
isopropyl


49
1
4-OMe-Phenyl
—CH2CH(CH3)2


50
1
4-OMe-Phenyl
CF3


51
1
4-OMe-Phenyl
—CH2CF3


52
1
4-OMe-Phenyl
—CH2CH2CF3


53
1
4-OMe-Phenyl
cyclopropyl


54
1
4-OMe-Phenyl
Cyclobutyl


55
1
4-OMe-Phenyl
cyclopentyl


56
1
4-OMe-Phenyl
cyclohexyl


57
1
4-OMe-Phenyl
3-pyridyl


58
1
4-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


59
1
4-OMe-Phenyl
1H-imidazol-4-yl


60
1
4-OMe-Phenyl
2-furanyl


61
1
2-OMe-Phenyl
ethyl


62
1
2-OMe-Phenyl
n-propyl


63
1
2-OMe-Phenyl
isopropyl


64
1
2-OMe-Phenyl
—CH2CH(CH3)2


65
1
2-OMe-Phenyl
CF3


66
1
2-OMe-Phenyl
—CH2CF3


67
1
2-OMe-Phenyl
—CH2CH2CF3


68
1
2-OMe-Phenyl
cyclopropyl


69
1
2-OMe-Phenyl
Cyclobutyl


70
1
2-OMe-Phenyl
cyclopentyl


71
1
2-OMe-Phenyl
cyclohexyl


72
1
2-OMe-Phenyl
3-pyridyl


73
1
2-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


74
1
2-OMe-Phenyl
1H-imidazol-4-yl


75
1
2-OMe-Phenyl
2-furanyl


76
1
3-CN-Phenyl
ethyl


77
1
3-CN-Phenyl
n-propyl


78
1
3-CN-Phenyl
isopropyl


79
1
3-CN-Phenyl
—CH2CH(CH3)2


80
1
3-CN-Phenyl
CF3


81
1
3-CN-Phenyl
—CH2CF3


82
1
3-CN-Phenyl
—CH2CH2CF3


83
1
3-CN-Phenyl
cyclopropyl


84
1
3-CN-Phenyl
Cyclobutyl


85
1
3-CN-Phenyl
cyclopentyl


86
1
3-CN-Phenyl
cyclohexyl


87
1
3-CN-Phenyl
3-pyridyl


88
1
3-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


89
1
3-CN-Phenyl
1H-imidazol-4-yl


90
1
3-CN-Phenyl
2-furanyl


91
1
2-F-Phenyl
ethyl


92
1
2-F-Phenyl
n-propyl


93
1
2-F-Phenyl
isopropyl


94
1
2-F-Phenyl
—CH2CH(CH3)2


95
1
2-F-Phenyl
CF3


96
1
2-F-Phenyl
—CH2CF3


97
1
2-F-Phenyl
—CH2CH2CF3


98
1
2-F-Phenyl
cyclopropyl


99
1
2-F-Phenyl
Cyclobutyl


100
1
2-F-Phenyl
cyclopentyl


101
1
2-F-Phenyl
cyclohexyl


102
1
2-F-Phenyl
3-pyridyl


103
1
2-F-Phenyl
1-methyl-1H-pyrazol-4-yl


104
1
2-F-Phenyl
1H-imidazol-4-yl


105
1
2-F-Phenyl
2-furanyl


106
1
4-F-Phenyl
ethyl


107
1
4-F-Phenyl
n-propyl


108
1
4-F-Phenyl
isopropyl


109
1
4-F-Phenyl
—CH2CH(CH3)2


110
1
4-F-Phenyl
CF3


111
1
4-F-Phenyl
—CH2CF3


112
1
4-F-Phenyl
—CH2CH2CF3


113
1
4-F-Phenyl
cyclopropyl


114
1
4-F-Phenyl
Cyclobutyl


115
1
4-F-Phenyl
cyclopentyl


116
1
4-F-Phenyl
cyclohexyl


117
1
4-F-Phenyl
3-pyridyl


118
1
4-F-Phenyl
1-methyl-1H-pyrazol-4-yl


119
1
4-F-Phenyl
1H-imidazol-4-yl


120
1
4-F-Phenyl
2-furanyl


121
1
3-Cl-Phenyl
ethyl


122
1
3-Cl-Phenyl
n-propyl


123
1
3-Cl-Phenyl
isopropyl


124
1
3-Cl-Phenyl
—CH2CH(CH3)2


125
1
3-Cl-Phenyl
CF3


126
1
3-Cl-Phenyl
—CH2CF3


127
1
3-Cl-Phenyl
—CH2CH2CF3


128
1
3-Cl-Phenyl
cyclopropyl


129
1
3-Cl-Phenyl
Cyclobutyl


130
1
3-Cl-Phenyl
cyclopentyl


131
1
3-Cl-Phenyl
cyclohexyl


132
1
3-Cl-Phenyl
3-pyridyl


133
1
3-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


134
1
3-Cl-Phenyl
1H-imidazol-4-yl


135
1
3-Cl-Phenyl
2-furanyl


136
1
2-Br-Phenyl
ethyl


137
1
2-Br-Phenyl
n-propyl


138
1
2-Br-Phenyl
isopropyl


139
1
2-Br-Phenyl
—CH2CH(CH3)2


140
1
2-Br-Phenyl
CF3


141
1
2-Br-Phenyl
—CH2CF3


142
1
2-Br-Phenyl
—CH2CH2CF3


143
1
2-Br-Phenyl
cyclopropyl


144
1
2-Br-Phenyl
Cyclobutyl


145
1
2-Br-Phenyl
cyclopentyl


146
1
2-Br-Phenyl
cyclohexyl


147
1
2-Br-Phenyl
3-pyridyl


148
1
2-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


149
1
2-Br-Phenyl
1H-imidazol-4-yl


150
1
2-Br-Phenyl
2-furanyl


151
1
4-Br-Phenyl
ethyl


152
1
4-Br-Phenyl
n-propyl


153
1
4-Br-Phenyl
isopropyl


154
1
4-Br-Phenyl
—CH2CH(CH3)2


155
1
4-Br-Phenyl
CF3


156
1
4-Br-Phenyl
—CH2CF3


157
1
4-Br-Phenyl
—CH2CH2CF3


158
1
4-Br-Phenyl
cyclopropyl


159
1
4-Br-Phenyl
Cyclobutyl


160
1
4-Br-Phenyl
cyclopentyl


161
1
4-Br-Phenyl
cyclohexyl


162
1
4-Br-Phenyl
3-pyridyl


163
1
4-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


164
1
4-Br-Phenyl
1H-imidazol-4-yl


165
1
4-Br-Phenyl
2-furanyl


166
1
3-CF3-Phenyl
ethyl


167
1
3-CF3-Phenyl
n-propyl


168
1
3-CF3-Phenyl
isopropyl


169
1
3-CF3-Phenyl
—CH2CH(CH3)2


170
1
3-CF3-Phenyl
CF3


171
1
3-CF3-Phenyl
—CH2CF3


172
1
3-CF3-Phenyl
—CH2CH2CF3


173
1
3-CF3-Phenyl
cyclopropyl


174
1
3-CF3-Phenyl
Cyclobutyl


175
1
3-CF3-Phenyl
cyclopentyl


176
1
3-CF3-Phenyl
cyclohexyl


177
1
3-CF3-Phenyl
3-pyridyl


178
1
3-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


179
1
3-CF3-Phenyl
1H-imidazol-4-yl


180
1
3-CF3-Phenyl
2-furanyl


181
1
2-iPr-Phenyl
ethyl


182
1
2-iPr-Phenyl
n-propyl


183
1
2-iPr-Phenyl
isopropyl


184
1
2-iPr-Phenyl
—CH2CH(CH3)2


185
1
2-iPr-Phenyl
CF3


186
1
2-iPr-Phenyl
—CH2CF3


187
1
2-iPr-Phenyl
—CH2CH2CF3


188
1
2-iPr-Phenyl
cyclopropyl


189
1
2-iPr-Phenyl
Cyclobutyl


190
1
2-iPr-Phenyl
cyclopentyl


191
1
2-iPr-Phenyl
cyclohexyl


192
1
2-iPr-Phenyl
3-pyridyl


193
1
2-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


194
1
2-iPr-Phenyl
1H-imidazol-4-yl


195
1
2-iPr-Phenyl
2-furanyl


196
1
4-iPr-Phenyl
ethyl


197
1
4-iPr-Phenyl
n-propyl


198
1
4-iPr-Phenyl
isopropyl


199
1
4-iPr-Phenyl
—CH2CH(CH3)2


200
1
4-iPr-Phenyl
CF3


201
1
4-iPr-Phenyl
—CH2CF3


202
1
4-iPr-Phenyl
—CH2CH2CF3


203
1
4-iPr-Phenyl
cyclopropyl


204
1
4-iPr-Phenyl
Cyclobutyl


205
1
4-iPr-Phenyl
cyclopentyl


206
1
4-iPr-Phenyl
cyclohexyl


207
1
4-iPr-Phenyl
3-pyridyl


208
1
4-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


209
1
4-iPr-Phenyl
1H-imidazol-4-yl


210
1
4-iPr-Phenyl
2-furanyl


211
1
3-morpholino-phenyl
ethyl


212
1
3-morpholino-phenyl
n-propyl


213
1
3-morpholino-phenyl
isopropyl


214
1
3-morpholino-phenyl
—CH2CH(CH3)2


215
1
3-morpholino-phenyl
CF3


216
1
3-morpholino-phenyl
—CH2CF3


217
1
3-morpholino-phenyl
—CH2CH2CF3


218
1
3-morpholino-phenyl
cyclopropyl


219
1
3-morpholino-phenyl
Cyclobutyl


220
1
3-morpholino-phenyl
cyclopentyl


221
1
3-morpholino-phenyl
cyclohexyl


222
1
3-morpholino-phenyl
3-pyridyl


223
1
3-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


224
1
3-morpholino-phenyl
1H-imidazol-4-yl


225
1
3-morpholino-phenyl
2-furanyl


226
1
4-cyano-2-morpholino-phenyl
ethyl


227
1
4-cyano-2-morpholino-phenyl
n-propyl


228
1
4-cyano-2-morpholino-phenyl
isopropyl


229
1
4-cyano-2-morpholino-phenyl
—CH2CH(CH3)2


230
1
4-cyano-2-morpholino-phenyl
CF3


231
1
4-cyano-2-morpholino-phenyl
—CH2CF3


232
1
4-cyano-2-morpholino-phenyl
—CH2CH2CF3


233
1
4-cyano-2-morpholino-phenyl
cyclopropyl


234
1
4-cyano-2-morpholino-phenyl
Cyclobutyl


235
1
4-cyano-2-morpholino-phenyl
cyclopentyl


236
1
4-cyano-2-morpholino-phenyl
cyclohexyl


237
1
4-cyano-2-morpholino-phenyl
3-pyridyl


238
1
4-cyano-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


239
1
4-cyano-2-morpholino-phenyl
1H-imidazol-4-yl


240
1
4-cyano-2-morpholino-phenyl
2-furanyl


241
1
4-hydroxy-2-morpholino-phenyl
ethyl


242
1
4-hydroxy-2-morpholino-phenyl
n-propyl


243
1
4-hydroxy-2-morpholino-phenyl
isopropyl


244
1
4-hydroxy-2-morpholino-phenyl
—CH2CH(CH3)2


245
1
4-hydroxy-2-morpholino-phenyl
CF3


246
1
4-hydroxy-2-morpholino-phenyl
—CH2CF3


247
1
4-hydroxy-2-morpholino-phenyl
—CH2CH2CF3


248
1
4-hydroxy-2-morpholino-phenyl
cyclopropyl


249
1
4-hydroxy-2-morpholino-phenyl
Cyclobutyl


250
1
4-hydroxy-2-morpholino-phenyl
cyclopentyl


251
1
4-hydroxy-2-morpholino-phenyl
cyclohexyl


252
1
4-hydroxy-2-morpholino-phenyl
3-pyridyl


253
1
4-hydroxy-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


254
1
4-hydroxy-2-morpholino-phenyl
1H-imidazol-4-yl


255
1
4-hydroxy-2-morpholino-phenyl
2-furanyl


256
1
2-CH3-phenyl
Ethyl


257
1
2-CH3-phenyl
n-propyl


258
1
2-CH3-phenyl
Isopropyl


259
1
2-CH3-phenyl
—CH2CH(CH3)2


260
1
2-CH3-phenyl
CF3


261
1
2-CH3-phenyl
—CH2CF3


262
1
2-CH3-phenyl
—CH2CH2CF3


263
1
2-CH3-phenyl
cyclopropyl


264
1
2-CH3-phenyl
Cyclobutyl


265
1
2-CH3-phenyl
cyclopentyl


266
1
2-CH3-phenyl
cyclohexyl


267
1
2-CH3-phenyl
3-pyridyl


268
1
2-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


269
1
2-CH3-phenyl
1H-imidazol-4-yl


270
1
2-CH3-phenyl
2-furanyl


271
1
4-OH-Phenyl
Ethyl


272
1
4-OH-Phenyl
n-propyl


273
1
4-OH-Phenyl
Isopropyl


274
1
4-OH-Phenyl
—CH2CH(CH3)2


275
1
4-OH-Phenyl
CF3


276
1
4-OH-Phenyl
—CH2CF3


277
1
4-OH-Phenyl
—CH2CH2CF3


278
1
4-OH-Phenyl
cyclopropyl


279
1
4-OH-Phenyl
Cyclobutyl


280
1
4-OH-Phenyl
cyclopentyl


281
1
4-OH-Phenyl
cyclohexyl


282
1
4-OH-Phenyl
3-pyridyl


283
1
4-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


284
1
4-OH-Phenyl
1H-imidazol-4-yl


285
1
4-OH-Phenyl
2-furanyl


286
1
2-OH-Phenyl
Ethyl


287
1
2-OH-Phenyl
n-propyl


288
1
2-OH-Phenyl
Isopropyl


289
1
2-OH-Phenyl
—CH2CH(CH3)2


290
1
2-OH-Phenyl
CF3


291
1
2-OH-Phenyl
—CH2CF3


292
1
2-OH-Phenyl
—CH2CH2CF3


293
1
2-OH-Phenyl
cyclopropyl


294
1
2-OH-Phenyl
Cyclobutyl


295
1
2-OH-Phenyl
cyclopentyl


296
1
2-OH-Phenyl
cyclohexyl


297
1
2-OH-Phenyl
3-pyridyl


298
1
2-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


299
1
2-OH-Phenyl
1H-imidazol-4-yl


300
1
2-OH-Phenyl
2-furanyl


301
1
3-OMe-Phenyl
Ethyl


302
1
3-OMe-Phenyl
n-propyl


303
1
3-OMe-Phenyl
Isopropyl


304
1
3-OMe-Phenyl
—CH2CH(CH3)2


305
1
3-OMe-Phenyl
CF3


306
1
3-OMe-Phenyl
—CH2CF3


307
1
3-OMe-Phenyl
—CH2CH2CF3


308
1
3-OMe-Phenyl
cyclopropyl


309
1
3-OMe-Phenyl
Cyclobutyl


310
1
3-OMe-Phenyl
cyclopentyl


311
1
3-OMe-Phenyl
cyclohexyl


312
1
3-OMe-Phenyl
3-pyridyl


313
1
3-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


314
1
3-OMe-Phenyl
1H-imidazol-4-yl


315
1
3-OMe-Phenyl
2-furanyl


316
1
4-CN-Phenyl
Ethyl


317
1
4-CN-Phenyl
n-propyl


318
1
4-CN-Phenyl
Isopropyl


319
1
4-CN-Phenyl
—CH2CH(CH3)2


320
1
4-CN-Phenyl
CF3


321
1
4-CN-Phenyl
—CH2CF3


322
1
4-CN-Phenyl
—CH2CH2CF3


323
1
4-CN-Phenyl
cyclopropyl


324
1
4-CN-Phenyl
Cyclobutyl


325
1
4-CN-Phenyl
cyclopentyl


326
1
4-CN-Phenyl
cyclohexyl


327
1
4-CN-Phenyl
3-pyridyl


328
1
4-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


329
1
4-CN-Phenyl
1H-imidazol-4-yl


330
1
4-CN-Phenyl
2-furanyl


331
1
2-CN-Phenyl
Ethyl


332
1
2-CN-Phenyl
n-propyl


333
1
2-CN-Phenyl
Isopropyl


334
1
2-CN-Phenyl
—CH2CH(CH3)2


335
1
2-CN-Phenyl
CF3


336
1
2-CN-Phenyl
—CH2CF3


337
1
2-CN-Phenyl
—CH2CH2CF3


338
1
2-CN-Phenyl
cyclopropyl


339
1
2-CN-Phenyl
Cyclobutyl


340
1
2-CN-Phenyl
cyclopentyl


341
1
2-CN-Phenyl
cyclohexyl


342
1
2-CN-Phenyl
3-pyridyl


343
1
2-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


344
1
2-CN-Phenyl
1H-imidazol-4-yl


345
1
2-CN-Phenyl
2-furanyl


346
1
3-F-Phenyl
Ethyl


347
1
3-F-Phenyl
n-propyl


348
1
3-F-Phenyl
Isopropyl


349
1
3-F-Phenyl
—CH2CH(CH3)2


350
1
3-F-Phenyl
CF3


351
1
3-F-Phenyl
—CH2CF3


352
1
3-F-Phenyl
—CH2CH2CF3


353
1
3-F-Phenyl
cyclopropyl


354
1
3-F-Phenyl
Cyclobutyl


355
1
3-F-Phenyl
cyclopentyl


356
1
3-F-Phenyl
cyclohexyl


357
1
3-F-Phenyl
3-pyridyl


358
1
3-F-Phenyl
1-methyl-1H-pyrazol-4-yl


359
1
3-F-Phenyl
1H-imidazol-4-yl


360
1
3-F-Phenyl
2-furanyl


361
1
2-Cl-Phenyl
Ethyl


362
1
2-Cl-Phenyl
n-propyl


363
1
2-Cl-Phenyl
Isopropyl


364
1
2-Cl-Phenyl
—CH2CH(CH3)2


365
1
2-Cl-Phenyl
CF3


366
1
2-Cl-Phenyl
—CH2CF3


367
1
2-Cl-Phenyl
—CH2CH2CF3


368
1
2-Cl-Phenyl
cyclopropyl


369
1
2-Cl-Phenyl
Cyclobutyl


370
1
2-Cl-Phenyl
cyclopentyl


371
1
2-Cl-Phenyl
cyclohexyl


372
1
2-Cl-Phenyl
3-pyridyl


373
1
2-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


374
1
2-Cl-Phenyl
1H-imidazol-4-yl


375
1
2-Cl-Phenyl
2-furanyl


376
1
4-Cl-Phenyl
Ethyl


377
1
4-Cl-Phenyl
n-propyl


378
1
4-Cl-Phenyl
Isopropyl


379
1
4-Cl-Phenyl
—CH2CH(CH3)2


380
1
4-Cl-Phenyl
CF3


381
1
4-Cl-Phenyl
—CH2CF3


382
1
4-Cl-Phenyl
—CH2CH2CF3


383
1
4-Cl-Phenyl
cyclopropyl


384
1
4-Cl-Phenyl
Cyclobutyl


385
1
4-Cl-Phenyl
cyclopentyl


386
1
4-Cl-Phenyl
cyclohexyl


387
1
4-Cl-Phenyl
3-pyridyl


388
1
4-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


389
1
4-Cl-Phenyl
1H-imidazol-4-yl


390
1
4-Cl-Phenyl
2-furanyl


391
1
3-Br-Phenyl
Ethyl


392
1
3-Br-Phenyl
n-propyl


393
1
3-Br-Phenyl
Isopropyl


394
1
3-Br-Phenyl
—CH2CH(CH3)2


395
1
3-Br-Phenyl
CF3


396
1
3-Br-Phenyl
—CH2CF3


397
1
3-Br-Phenyl
—CH2CH2CF3


398
1
3-Br-Phenyl
cyclopropyl


399
1
3-Br-Phenyl
Cyclobutyl


400
1
3-Br-Phenyl
cyclopentyl


401
1
3-Br-Phenyl
cyclohexyl


402
1
3-Br-Phenyl
3-pyridyl


403
1
3-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


404
1
3-Br-Phenyl
1H-imidazol-4-yl


405
1
3-Br-Phenyl
2-furanyl


406
1
2-CF3-Phenyl
Ethyl


407
1
2-CF3-Phenyl
n-propyl


408
1
2-CF3-Phenyl
Isopropyl


409
1
2-CF3-Phenyl
—CH2CH(CH3)2


410
1
2-CF3-Phenyl
CF3


411
1
2-CF3-Phenyl
—CH2CF3


412
1
2-CF3-Phenyl
—CH2CH2CF3


413
1
2-CF3-Phenyl
cyclopropyl


414
1
2-CF3-Phenyl
Cyclobutyl


415
1
2-CF3-Phenyl
cyclopentyl


416
1
2-CF3-Phenyl
cyclohexyl


417
1
2-CF3-Phenyl
3-pyridyl


418
1
2-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


419
1
2-CF3-Phenyl
1H-imidazol-4-yl


420
1
2-CF3-Phenyl
2-furanyl


421
1
4-CF3-Phenyl
Ethyl


422
1
4-CF3-Phenyl
n-propyl


423
1
4-CF3-Phenyl
Isopropyl


424
1
4-CF3-Phenyl
—CH2CH(CH3)2


425
1
4-CF3-Phenyl
CF3


426
1
4-CF3-Phenyl
—CH2CF3


427
1
4-CF3-Phenyl
—CH2CH2CF3


428
1
4-CF3-Phenyl
cyclopropyl


429
1
4-CF3-Phenyl
Cyclobutyl


430
1
4-CF3-Phenyl
cyclopentyl


431
1
4-CF3-Phenyl
cyclohexyl


432
1
4-CF3-Phenyl
3-pyridyl


433
1
4-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


434
1
4-CF3-Phenyl
1H-imidazol-4-yl


435
1
4-CF3-Phenyl
2-furanyl


436
1
3-iPr-Phenyl
Ethyl


437
1
3-iPr-Phenyl
n-propyl


438
1
3-iPr-Phenyl
Isopropyl


439
1
3-iPr-Phenyl
—CH2CH(CH3)2


440
1
3-iPr-Phenyl
CF3


441
1
3-iPr-Phenyl
—CH2CF3


442
1
3-iPr-Phenyl
—CH2CH2CF3


443
1
3-iPr-Phenyl
cyclopropyl


444
1
3-iPr-Phenyl
Cyclobutyl


445
1
3-iPr-Phenyl
cyclopentyl


446
1
3-iPr-Phenyl
cyclohexyl


447
1
3-iPr-Phenyl
3-pyridyl


448
1
3-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


449
1
3-iPr-Phenyl
1H-imidazol-4-yl


450
1
3-iPr-Phenyl
2-furanyl


451
1
2-morpholino-phenyl
Ethyl


452
1
2-morpholino-phenyl
n-propyl


453
1
2-morpholino-phenyl
isopropyl


454
1
2-morpholino-phenyl
—CH2CH(CH3)2


455
1
2-morpholino-phenyl
CF3


456
1
2-morpholino-phenyl
—CH2CF3


457
1
2-morpholino-phenyl
—CH2CH2CF3


458
1
2-morpholino-phenyl
cyclopropyl


459
1
2-morpholino-phenyl
Cyclobutyl


460
1
2-morpholino-phenyl
cyclopentyl


461
1
2-morpholino-phenyl
cyclohexyl


462
1
2-morpholino-phenyl
3-pyridyl


463
1
2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


464
1
2-morpholino-phenyl
1H-imidazol-4-yl


465
1
2-morpholino-phenyl
2-furanyl


466
1
4-morpholino-phenyl
ethyl


467
1
4-morpholino-phenyl
n-propyl


468
1
4-morpholino-phenyl
isopropyl


469
1
4-morpholino-phenyl
—CH2CH(CH3)2


470
1
4-morpholino-phenyl
CF3


471
1
4-morpholino-phenyl
—CH2CF3


472
1
4-morpholino-phenyl
—CH2CH2CF3


473
1
4-morpholino-phenyl
cyclopropyl


474
1
4-morpholino-phenyl
Cyclobutyl


475
1
4-morpholino-phenyl
cyclopentyl


476
1
4-morpholino-phenyl
cyclohexyl


477
1
4-morpholino-phenyl
3-pyridyl


478
1
4-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


479
1
4-morpholino-phenyl
1H-imidazol-4-yl


480
1
4-morpholino-phenyl
2-furanyl


481
1
4-methyl-2-morpholino-phenyl
ethyl


482
1
4-methyl-2-morpholino-phenyl
n-propyl


483
1
4-methyl-2-morpholino-phenyl
isopropyl


484
1
4-methyl-2-morpholino-phenyl
—CH2CH(CH3)2


485
1
4-methyl-2-morpholino-phenyl
CF3


486
1
4-methyl-2-morpholino-phenyl
—CH2CF3


487
1
4-methyl-2-morpholino-phenyl
—CH2CH2CF3


488
1
4-methyl-2-morpholino-phenyl
cyclopropyl


489
1
4-methyl-2-morpholino-phenyl
Cyclobutyl


490
1
4-methyl-2-morpholino-phenyl
cyclopentyl


491
1
4-methyl-2-morpholino-phenyl
cyclohexyl


492
1
4-methyl-2-morpholino-phenyl
3-pyridyl


493
1
4-methyl-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


494
1
4-methyl-2-morpholino-phenyl
1H-imidazol-4-yl


495
1
4-methyl-2-morpholino-phenyl
2-furanyl


496
2
4-CH3-phenyl
ethyl


497
2
4-CH3-phenyl
n-propyl


498
2
4-CH3-phenyl
isopropyl


499
2
4-CH3-phenyl
—CH2CH(CH3)2


500
2
4-CH3-phenyl
CF3


501
2
4-CH3-phenyl
—CH2CF3


502
2
4-CH3-phenyl
—CH2CH2CF3


503
2
4-CH3-phenyl
cyclopropyl


504
2
4-CH3-phenyl
Cyclobutyl


505
2
4-CH3-phenyl
cyclopentyl


506
2
4-CH3-phenyl
cyclohexyl


507
2
4-CH3-phenyl
3-pyridyl


508
2
4-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


509
2
4-CH3-phenyl
1H-imidazol-4-yl


510
2
4-CH3-phenyl
2-furanyl


511
2
3-CH3-phenyl
ethyl


512
2
3-CH3-phenyl
n-propyl


513
2
3-CH3-phenyl
isopropyl


514
2
3-CH3-phenyl
—CH2CH(CH3)2


515
2
3-CH3-phenyl
CF3


516
2
3-CH3-phenyl
—CH2CF3


517
2
3-CH3-phenyl
—CH2CH2CF3


518
2
3-CH3-phenyl
cyclopropyl


519
2
3-CH3-phenyl
Cyclobutyl


520
2
3-CH3-phenyl
cyclopentyl


521
2
3-CH3-phenyl
cyclohexyl


522
2
3-CH3-phenyl
3-pyridyl


523
2
3-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


524
2
3-CH3-phenyl
1H-imidazol-4-yl


525
2
3-CH3-phenyl
2-furanyl


526
2
3-OH-Phenyl
ethyl


527
2
3-OH-Phenyl
n-propyl


528
2
3-OH-Phenyl
isopropyl


529
2
3-OH-Phenyl
—CH2CH(CH3)2


530
2
3-OH-Phenyl
CF3


531
2
3-OH-Phenyl
—CH2CF3


532
2
3-OH-Phenyl
—CH2CH2CF3


533
2
3-OH-Phenyl
cyclopropyl


534
2
3-OH-Phenyl
Cyclobutyl


535
2
3-OH-Phenyl
cyclopentyl


536
2
3-OH-Phenyl
cyclohexyl


537
2
3-OH-Phenyl
3-pyridyl


538
2
3-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


539
2
3-OH-Phenyl
1H-imidazol-4-yl


540
2
3-OH-Phenyl
2-furanyl


541
2
4-OMe-Phenyl
ethyl


542
2
4-OMe-Phenyl
n-propyl


543
2
4-OMe-Phenyl
isopropyl


544
2
4-OMe-Phenyl
—CH2CH(CH3)2


545
2
4-OMe-Phenyl
CF3


546
2
4-OMe-Phenyl
—CH2CF3


547
2
4-OMe-Phenyl
—CH2CH2CF3


548
2
4-OMe-Phenyl
cyclopropyl


549
2
4-OMe-Phenyl
Cyclobutyl


550
2
4-OMe-Phenyl
cyclopentyl


551
2
4-OMe-Phenyl
cyclohexyl


552
2
4-OMe-Phenyl
3-pyridyl


553
2
4-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


554
2
4-OMe-Phenyl
1H-imidazol-4-yl


555
2
4-OMe-Phenyl
2-furanyl


556
2
2-OMe-Phenyl
ethyl


557
2
2-OMe-Phenyl
n-propyl


558
2
2-OMe-Phenyl
isopropyl


559
2
2-OMe-Phenyl
—CH2CH(CH3)2


560
2
2-OMe-Phenyl
CF3


561
2
2-OMe-Phenyl
—CH2CF3


562
2
2-OMe-Phenyl
—CH2CH2CF3


563
2
2-OMe-Phenyl
cyclopropyl


564
2
2-OMe-Phenyl
Cyclobutyl


565
2
2-OMe-Phenyl
cyclopentyl


566
2
2-OMe-Phenyl
cyclohexyl


567
2
2-OMe-Phenyl
3-pyridyl


568
2
2-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


569
2
2-OMe-Phenyl
1H-imidazol-4-yl


570
2
2-OMe-Phenyl
2-furanyl


571
2
3-CN-Phenyl
ethyl


572
2
3-CN-Phenyl
n-propyl


573
2
3-CN-Phenyl
isopropyl


574
2
3-CN-Phenyl
—CH2CH(CH3)2


575
2
3-CN-Phenyl
CF3


576
2
3-CN-Phenyl
—CH2CF3


577
2
3-CN-Phenyl
—CH2CH2CF3


578
2
3-CN-Phenyl
cyclopropyl


579
2
3-CN-Phenyl
Cyclobutyl


580
2
3-CN-Phenyl
cyclopentyl


581
2
3-CN-Phenyl
cyclohexyl


582
2
3-CN-Phenyl
3-pyridyl


583
2
3-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


584
2
3-CN-Phenyl
1H-imidazol-4-yl


585
2
3-CN-Phenyl
2-furanyl


586
2
2-F-Phenyl
ethyl


587
2
2-F-Phenyl
n-propyl


588
2
2-F-Phenyl
isopropyl


589
2
2-F-Phenyl
—CH2CH(CH3)2


590
2
2-F-Phenyl
CF3


591
2
2-F-Phenyl
—CH2CF3


592
2
2-F-Phenyl
—CH2CH2CF3


593
2
2-F-Phenyl
cyclopropyl


594
2
2-F-Phenyl
Cyclobutyl


595
2
2-F-Phenyl
cyclopentyl


596
2
2-F-Phenyl
cyclohexyl


597
2
2-F-Phenyl
3-pyridyl


598
2
2-F-Phenyl
1-methyl-1H-pyrazol-4-yl


599
2
2-F-Phenyl
1H-imidazol-4-yl


600
2
2-F-Phenyl
2-furanyl


601
2
4-F-Phenyl
ethyl


602
2
4-F-Phenyl
n-propyl


603
2
4-F-Phenyl
isopropyl


604
2
4-F-Phenyl
—CH2CH(CH3)2


605
2
4-F-Phenyl
CF3


606
2
4-F-Phenyl
—CH2CF3


607
2
4-F-Phenyl
—CH2CH2CF3


608
2
4-F-Phenyl
cyclopropyl


609
2
4-F-Phenyl
Cyclobutyl


610
2
4-F-Phenyl
cyclopentyl


611
2
4-F-Phenyl
cyclohexyl


612
2
4-F-Phenyl
3-pyridyl


613
2
4-F-Phenyl
1-methyl-1H-pyrazol-4-yl


614
2
4-F-Phenyl
1H-imidazol-4-yl


615
2
4-F-Phenyl
2-furanyl


616
2
3-Cl-Phenyl
ethyl


617
2
3-Cl-Phenyl
n-propyl


618
2
3-Cl-Phenyl
isopropyl


619
2
3-Cl-Phenyl
—CH2CH(CH3)2


620
2
3-Cl-Phenyl
CF3


621
2
3-Cl-Phenyl
—CH2CF3


622
2
3-Cl-Phenyl
—CH2CH2CF3


623
2
3-Cl-Phenyl
cyclopropyl


624
2
3-Cl-Phenyl
Cyclobutyl


625
2
3-Cl-Phenyl
cyclopentyl


626
2
3-Cl-Phenyl
cyclohexyl


627
2
3-Cl-Phenyl
3-pyridyl


628
2
3-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


629
2
3-Cl-Phenyl
1H-imidazol-4-yl


630
2
3-Cl-Phenyl
2-furanyl


631
2
2-Br-Phenyl
ethyl


632
2
2-Br-Phenyl
n-propyl


633
2
2-Br-Phenyl
isopropyl


634
2
2-Br-Phenyl
—CH2CH(CH3)2


635
2
2-Br-Phenyl
CF3


636
2
2-Br-Phenyl
—CH2CF3


637
2
2-Br-Phenyl
—CH2CH2CF3


638
2
2-Br-Phenyl
cyclopropyl


639
2
2-Br-Phenyl
Cyclobutyl


640
2
2-Br-Phenyl
cyclopentyl


641
2
2-Br-Phenyl
cyclohexyl


642
2
2-Br-Phenyl
3-pyridyl


643
2
2-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


644
2
2-Br-Phenyl
1H-imidazol-4-yl


645
2
2-Br-Phenyl
2-furanyl


646
2
4-Br-Phenyl
ethyl


647
2
4-Br-Phenyl
n-propyl


648
2
4-Br-Phenyl
isopropyl


649
2
4-Br-Phenyl
—CH2CH(CH3)2


650
2
4-Br-Phenyl
CF3


651
2
4-Br-Phenyl
—CH2CF3


652
2
4-Br-Phenyl
—CH2CH2CF3


653
2
4-Br-Phenyl
cyclopropyl


654
2
4-Br-Phenyl
Cyclobutyl


655
2
4-Br-Phenyl
cyclopentyl


656
2
4-Br-Phenyl
cyclohexyl


657
2
4-Br-Phenyl
3-pyridyl


658
2
4-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


659
2
4-Br-Phenyl
1H-imidazol-4-yl


660
2
4-Br-Phenyl
2-furanyl


661
2
3-CF3-Phenyl
ethyl


662
2
3-CF3-Phenyl
n-propyl


663
2
3-CF3-Phenyl
isopropyl


664
2
3-CF3-Phenyl
—CH2CH(CH3)2


665
2
3-CF3-Phenyl
CF3


666
2
3-CF3-Phenyl
—CH2CF3


667
2
3-CF3-Phenyl
—CH2CH2CF3


668
2
3-CF3-Phenyl
cyclopropyl


669
2
3-CF3-Phenyl
Cyclobutyl


670
2
3-CF3-Phenyl
cyclopentyl


671
2
3-CF3-Phenyl
cyclohexyl


672
2
3-CF3-Phenyl
3-pyridyl


673
2
3-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


674
2
3-CF3-Phenyl
1H-imidazol-4-yl


675
2
3-CF3-Phenyl
2-furanyl


676
2
2-iPr-Phenyl
ethyl


677
2
2-iPr-Phenyl
n-propyl


678
2
2-iPr-Phenyl
isopropyl


679
2
2-iPr-Phenyl
—CH2CH(CH3)2


680
2
2-iPr-Phenyl
CF3


681
2
2-iPr-Phenyl
—CH2CF3


682
2
2-iPr-Phenyl
—CH2CH2CF3


683
2
2-iPr-Phenyl
cyclopropyl


684
2
2-iPr-Phenyl
Cyclobutyl


685
2
2-iPr-Phenyl
cyclopentyl


686
2
2-iPr-Phenyl
cyclohexyl


687
2
2-iPr-Phenyl
3-pyridyl


688
2
2-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


689
2
2-iPr-Phenyl
1H-imidazol-4-yl


690
2
2-iPr-Phenyl
2-furanyl


691
2
4-iPr-Phenyl
ethyl


692
2
4-iPr-Phenyl
n-propyl


693
2
4-iPr-Phenyl
isopropyl


694
2
4-iPr-Phenyl
—CH2CH(CH3)2


695
2
4-iPr-Phenyl
CF3


696
2
4-iPr-Phenyl
—CH2CF3


697
2
4-iPr-Phenyl
—CH2CH2CF3


698
2
4-iPr-Phenyl
cyclopropyl


699
2
4-iPr-Phenyl
Cyclobutyl


700
2
4-iPr-Phenyl
cyclopentyl


701
2
4-iPr-Phenyl
cyclohexyl


702
2
4-iPr-Phenyl
3-pyridyl


703
2
4-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


704
2
4-iPr-Phenyl
1H-imidazol-4-yl


705
2
4-iPr-Phenyl
2-furanyl


706
2
3-morpholino-phenyl
ethyl


707
2
3-morpholino-phenyl
n-propyl


708
2
3-morpholino-phenyl
isopropyl


709
2
3-morpholino-phenyl
—CH2CH(CH3)2


710
2
3-morpholino-phenyl
CF3


711
2
3-morpholino-phenyl
—CH2CF3


712
2
3-morpholino-phenyl
—CH2CH2CF3


713
2
3-morpholino-phenyl
cyclopropyl


714
2
3-morpholino-phenyl
Cyclobutyl


715
2
3-morpholino-phenyl
cyclopentyl


716
2
3-morpholino-phenyl
cyclohexyl


717
2
3-morpholino-phenyl
3-pyridyl


718
2
3-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


719
2
3-morpholino-phenyl
1H-imidazol-4-yl


720
2
3-morpholino-phenyl
2-furanyl


721
2
4-cyano-2-morpholino-phenyl
ethyl


722
2
4-cyano-2-morpholino-phenyl
n-propyl


723
2
4-cyano-2-morpholino-phenyl
isopropyl


724
2
4-cyano-2-morpholino-phenyl
—CH2CH(CH3)2


725
2
4-cyano-2-morpholino-phenyl
CF3


726
2
4-cyano-2-morpholino-phenyl
—CH2CF3


727
2
4-cyano-2-morpholino-phenyl
—CH2CH2CF3


728
2
4-cyano-2-morpholino-phenyl
cyclopropyl


729
2
4-cyano-2-morpholino-phenyl
Cyclobutyl


730
2
4-cyano-2-morpholino-phenyl
cyclopentyl


731
2
4-cyano-2-morpholino-phenyl
cyclohexyl


732
2
4-cyano-2-morpholino-phenyl
3-pyridyl


733
2
4-cyano-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


734
2
4-cyano-2-morpholino-phenyl
1H-imidazol-4-yl


735
2
4-cyano-2-morpholino-phenyl
2-furanyl


736
2
4-hydroxy-2-morpholino-phenyl
ethyl


737
2
4-hydroxy-2-morpholino-phenyl
n-propyl


738
2
4-hydroxy-2-morpholino-phenyl
isopropyl


739
2
4-hydroxy-2-morpholino-phenyl
—CH2CH(CH3)2


740
2
4-hydroxy-2-morpholino-phenyl
CF3


741
2
4-hydroxy-2-morpholino-phenyl
—CH2CF3


742
2
4-hydroxy-2-morpholino-phenyl
—CH2CH2CF3


743
2
4-hydroxy-2-morpholino-phenyl
cyclopropyl


744
2
4-hydroxy-2-morpholino-phenyl
Cyclobutyl


745
2
4-hydroxy-2-morpholino-phenyl
cyclopentyl


746
2
4-hydroxy-2-morpholino-phenyl
cyclohexyl


747
2
4-hydroxy-2-morpholino-phenyl
3-pyridyl


748
2
4-hydroxy-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


749
2
4-hydroxy-2-morpholino-phenyl
1H-imidazol-4-yl


750
2
4-hydroxy-2-morpholino-phenyl
2-furanyl


751
2
2-CH3-phenyl
Ethyl


752
2
2-CH3-phenyl
n-propyl


753
2
2-CH3-phenyl
Isopropyl


754
2
2-CH3-phenyl
—CH2CH(CH3)2


755
2
2-CH3-phenyl
CF3


756
2
2-CH3-phenyl
—CH2CF3


757
2
2-CH3-phenyl
—CH2CH2CF3


758
2
2-CH3-phenyl
cyclopropyl


759
2
2-CH3-phenyl
Cyclobutyl


760
2
2-CH3-phenyl
cyclopentyl


761
2
2-CH3-phenyl
cyclohexyl


762
2
2-CH3-phenyl
3-pyridyl


763
2
2-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


764
2
2-CH3-phenyl
1H-imidazol-4-yl


765
2
2-CH3-phenyl
2-furanyl


766
2
4-OH-Phenyl
Ethyl


767
2
4-OH-Phenyl
n-propyl


768
2
4-OH-Phenyl
Isopropyl


769
2
4-OH-Phenyl
—CH2CH(CH3)2


770
2
4-OH-Phenyl
CF3


771
2
4-OH-Phenyl
—CH2CF3


772
2
4-OH-Phenyl
—CH2CH2CF3


773
2
4-OH-Phenyl
cyclopropyl


774
2
4-OH-Phenyl
Cyclobutyl


775
2
4-OH-Phenyl
cyclopentyl


776
2
4-OH-Phenyl
cyclohexyl


777
2
4-OH-Phenyl
3-pyridyl


778
2
4-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


779
2
4-OH-Phenyl
1H-imidazol-4-yl


780
2
4-OH-Phenyl
2-furanyl


781
2
2-OH-Phenyl
Ethyl


782
2
2-OH-Phenyl
n-propyl


783
2
2-OH-Phenyl
Isopropyl


784
2
2-OH-Phenyl
—CH2CH(CH3)2


785
2
2-OH-Phenyl
CF3


786
2
2-OH-Phenyl
—CH2CF3


787
2
2-OH-Phenyl
—CH2CH2CF3


788
2
2-OH-Phenyl
cyclopropyl


789
2
2-OH-Phenyl
Cyclobutyl


790
2
2-OH-Phenyl
cyclopentyl


791
2
2-OH-Phenyl
cyclohexyl


792
2
2-OH-Phenyl
3-pyridyl


793
2
2-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


794
2
2-OH-Phenyl
1H-imidazol-4-yl


795
2
2-OH-Phenyl
2-furanyl


796
2
3-OMe-Phenyl
Ethyl


797
2
3-OMe-Phenyl
n-propyl


798
2
3-OMe-Phenyl
Isopropyl


799
2
3-OMe-Phenyl
—CH2CH(CH3)2


800
2
3-OMe-Phenyl
CF3


801
2
3-OMe-Phenyl
—CH2CF3


802
2
3-OMe-Phenyl
—CH2CH2CF3


803
2
3-OMe-Phenyl
cyclopropyl


804
2
3-OMe-Phenyl
Cyclobutyl


805
2
3-OMe-Phenyl
cyclopentyl


806
2
3-OMe-Phenyl
cyclohexyl


807
2
3-OMe-Phenyl
3-pyridyl


808
2
3-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


809
2
3-OMe-Phenyl
1H-imidazol-4-yl


810
2
3-OMe-Phenyl
2-furanyl


811
2
4-CN-Phenyl
Ethyl


812
2
4-CN-Phenyl
n-propyl


813
2
4-CN-Phenyl
Isopropyl


814
2
4-CN-Phenyl
—CH2CH(CH3)2


815
2
4-CN-Phenyl
CF3


816
2
4-CN-Phenyl
—CH2CF3


817
2
4-CN-Phenyl
—CH2CH2CF3


818
2
4-CN-Phenyl
cyclopropyl


819
2
4-CN-Phenyl
Cyclobutyl


820
2
4-CN-Phenyl
cyclopentyl


821
2
4-CN-Phenyl
cyclohexyl


822
2
4-CN-Phenyl
3-pyridyl


823
2
4-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


824
2
4-CN-Phenyl
1H-imidazol-4-yl


825
2
4-CN-Phenyl
2-furanyl


826
2
2-CN-Phenyl
Ethyl


827
2
2-CN-Phenyl
n-propyl


828
2
2-CN-Phenyl
Isopropyl


829
2
2-CN-Phenyl
—CH2CH(CH3)2


830
2
2-CN-Phenyl
CF3


831
2
2-CN-Phenyl
—CH2CF3


832
2
2-CN-Phenyl
—CH2CH2CF3


833
2
2-CN-Phenyl
cyclopropyl


834
2
2-CN-Phenyl
Cyclobutyl


835
2
2-CN-Phenyl
cyclopentyl


836
2
2-CN-Phenyl
cyclohexyl


837
2
2-CN-Phenyl
3-pyridyl


838
2
2-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


839
2
2-CN-Phenyl
1H-imidazol-4-yl


840
2
2-CN-Phenyl
2-furanyl


841
2
3-F-Phenyl
Ethyl


842
2
3-F-Phenyl
n-propyl


843
2
3-F-Phenyl
Isopropyl


844
2
3-F-Phenyl
—CH2CH(CH3)2


845
2
3-F-Phenyl
CF3


846
2
3-F-Phenyl
—CH2CF3


847
2
3-F-Phenyl
—CH2CH2CF3


848
2
3-F-Phenyl
cyclopropyl


849
2
3-F-Phenyl
Cyclobutyl


850
2
3-F-Phenyl
cyclopentyl


851
2
3-F-Phenyl
cyclohexyl


852
2
3-F-Phenyl
3-pyridyl


853
2
3-F-Phenyl
1-methyl-1H-pyrazol-4-yl


854
2
3-F-Phenyl
1H-imidazol-4-yl


855
2
3-F-Phenyl
2-furanyl


856
2
2-Cl-Phenyl
Ethyl


857
2
2-Cl-Phenyl
n-propyl


858
2
2-Cl-Phenyl
Isopropyl


859
2
2-Cl-Phenyl
—CH2CH(CH3)2


860
2
2-Cl-Phenyl
CF3


861
2
2-Cl-Phenyl
—CH2CF3


862
2
2-Cl-Phenyl
—CH2CH2CF3


863
2
2-Cl-Phenyl
cyclopropyl


864
2
2-Cl-Phenyl
Cyclobutyl


865
2
2-Cl-Phenyl
cyclopentyl


866
2
2-Cl-Phenyl
cyclohexyl


867
2
2-Cl-Phenyl
3-pyridyl


868
2
2-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


869
2
2-Cl-Phenyl
1H-imidazol-4-yl


870
2
2-Cl-Phenyl
2-furanyl


871
2
4-Cl-Phenyl
Ethyl


872
2
4-Cl-Phenyl
n-propyl


873
2
4-Cl-Phenyl
Isopropyl


874
2
4-Cl-Phenyl
—CH2CH(CH3)2


875
2
4-Cl-Phenyl
CF3


876
2
4-Cl-Phenyl
—CH2CF3


877
2
4-Cl-Phenyl
—CH2CH2CF3


878
2
4-Cl-Phenyl
cyclopropyl


879
2
4-Cl-Phenyl
Cyclobutyl


880
2
4-Cl-Phenyl
cyclopentyl


881
2
4-Cl-Phenyl
cyclohexyl


882
2
4-Cl-Phenyl
3-pyridyl


883
2
4-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


884
2
4-Cl-Phenyl
1H-imidazol-4-yl


885
2
4-Cl-Phenyl
2-furanyl


886
2
3-Br-Phenyl
Ethyl


887
2
3-Br-Phenyl
n-propyl


888
2
3-Br-Phenyl
Isopropyl


889
2
3-Br-Phenyl
—CH2CH(CH3)2


890
2
3-Br-Phenyl
CF3


891
2
3-Br-Phenyl
—CH2CF3


892
2
3-Br-Phenyl
—CH2CH2CF3


893
2
3-Br-Phenyl
cyclopropyl


894
2
3-Br-Phenyl
Cyclobutyl


895
2
3-Br-Phenyl
cyclopentyl


896
2
3-Br-Phenyl
cyclohexyl


897
2
3-Br-Phenyl
3-pyridyl


898
2
3-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


899
2
3-Br-Phenyl
1H-imidazol-4-yl


900
2
3-Br-Phenyl
2-furanyl


901
2
2-CF3-Phenyl
Ethyl


902
2
2-CF3-Phenyl
n-propyl


903
2
2-CF3-Phenyl
Isopropyl


904
2
2-CF3-Phenyl
—CH2CH(CH3)2


905
2
2-CF3-Phenyl
CF3


906
2
2-CF3-Phenyl
—CH2CF3


907
2
2-CF3-Phenyl
—CH2CH2CF3


908
2
2-CF3-Phenyl
cyclopropyl


909
2
2-CF3-Phenyl
Cyclobutyl


910
2
2-CF3-Phenyl
cyclopentyl


911
2
2-CF3-Phenyl
cyclohexyl


912
2
2-CF3-Phenyl
3-pyridyl


913
2
2-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


914
2
2-CF3-Phenyl
1H-imidazol-4-yl


915
2
2-CF3-Phenyl
2-furanyl


916
2
4-CF3-Phenyl
Ethyl


917
2
4-CF3-Phenyl
n-propyl


918
2
4-CF3-Phenyl
Isopropyl


919
2
4-CF3-Phenyl
—CH2CH(CH3)2


920
2
4-CF3-Phenyl
CF3


921
2
4-CF3-Phenyl
—CH2CF3


922
2
4-CF3-Phenyl
—CH2CH2CF3


923
2
4-CF3-Phenyl
cyclopropyl


924
2
4-CF3-Phenyl
Cyclobutyl


925
2
4-CF3-Phenyl
cyclopentyl


926
2
4-CF3-Phenyl
cyclohexyl


927
2
4-CF3-Phenyl
3-pyridyl


928
2
4-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


929
2
4-CF3-Phenyl
1H-imidazol-4-yl


930
2
4-CF3-Phenyl
2-furanyl


931
2
3-iPr-Phenyl
Ethyl


932
2
3-iPr-Phenyl
n-propyl


933
2
3-iPr-Phenyl
Isopropyl


934
2
3-iPr-Phenyl
—CH2CH(CH3)2


935
2
3-iPr-Phenyl
CF3


936
2
3-iPr-Phenyl
—CH2CF3


937
2
3-iPr-Phenyl
—CH2CH2CF3


938
2
3-iPr-Phenyl
cyclopropyl


939
2
3-iPr-Phenyl
Cyclobutyl


940
2
3-iPr-Phenyl
cyclopentyl


941
2
3-iPr-Phenyl
cyclohexyl


942
2
3-iPr-Phenyl
3-pyridyl


943
2
3-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


944
2
3-iPr-Phenyl
1H-imidazol-4-yl


945
2
3-iPr-Phenyl
2-furanyl


946
2
2-morpholino-phenyl
Ethyl


947
2
2-morpholino-phenyl
n-propyl


948
2
2-morpholino-phenyl
isopropyl


949
2
2-morpholino-phenyl
—CH2CH(CH3)2


950
2
2-morpholino-phenyl
CF3


951
2
2-morpholino-phenyl
—CH2CF3


952
2
2-morpholino-phenyl
—CH2CH2CF3


953
2
2-morpholino-phenyl
cyclopropyl


954
2
2-morpholino-phenyl
Cyclobutyl


955
2
2-morpholino-phenyl
cyclopentyl


956
2
2-morpholino-phenyl
cyclohexyl


957
2
2-morpholino-phenyl
3-pyridyl


958
2
2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


959
2
2-morpholino-phenyl
1H-imidazol-4-yl


960
2
2-morpholino-phenyl
2-furanyl


961
2
4-morpholino-phenyl
ethyl


962
2
4-morpholino-phenyl
n-propyl


963
2
4-morpholino-phenyl
isopropyl


964
2
4-morpholino-phenyl
—CH2CH(CH3)2


965
2
4-morpholino-phenyl
CF3


966
2
4-morpholino-phenyl
—CH2CF3


967
2
4-morpholino-phenyl
—CH2CH2CF3


968
2
4-morpholino-phenyl
cyclopropyl


969
2
4-morpholino-phenyl
Cyclobutyl


970
2
4-morpholino-phenyl
cyclopentyl


971
2
4-morpholino-phenyl
cyclohexyl


972
2
4-morpholino-phenyl
3-pyridyl


973
2
4-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


974
2
4-morpholino-phenyl
1H-imidazol-4-yl


975
2
4-morpholino-phenyl
2-furanyl


976
2
4-methyl-2-morpholino-phenyl
ethyl


977
2
4-methyl-2-morpholino-phenyl
n-propyl


978
2
4-methyl-2-morpholino-phenyl
isopropyl


979
2
4-methyl-2-morpholino-phenyl
—CH2CH(CH3)2


980
2
4-methyl-2-morpholino-phenyl
CF3


981
2
4-methyl-2-morpholino-phenyl
—CH2CF3


982
2
4-methyl-2-morpholino-phenyl
—CH2CH2CF3


983
2
4-methyl-2-morpholino-phenyl
cyclopropyl


984
2
4-methyl-2-morpholino-phenyl
Cyclobutyl


985
2
4-methyl-2-morpholino-phenyl
cyclopentyl


986
2
4-methyl-2-morpholino-phenyl
cyclohexyl


987
2
4-methyl-2-morpholino-phenyl
3-pyridyl


988
2
4-methyl-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


989
2
4-methyl-2-morpholino-phenyl
1H-imidazol-4-yl


990
2
4-methyl-2-morpholino-phenyl
2-furanyl


991
3
4-CH3-phenyl
ethyl


992
3
4-CH3-phenyl
n-propyl


993
3
4-CH3-phenyl
isopropyl


994
3
4-CH3-phenyl
—CH2CH(CH3)2


995
3
4-CH3-phenyl
CF3


996
3
4-CH3-phenyl
—CH2CF3


997
3
4-CH3-phenyl
—CH2CH2CF3


998
3
4-CH3-phenyl
cyclopropyl


999
3
4-CH3-phenyl
Cyclobutyl


1000
3
4-CH3-phenyl
cyclopentyl


1001
3
4-CH3-phenyl
cyclohexyl


1002
3
4-CH3-phenyl
3-pyridyl


1003
3
4-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


1004
3
4-CH3-phenyl
1H-imidazol-4-yl


1005
3
4-CH3-phenyl
2-furanyl


1006
3
3-CH3-phenyl
ethyl


1007
3
3-CH3-phenyl
n-propyl


1008
3
3-CH3-phenyl
isopropyl


1009
3
3-CH3-phenyl
—CH2CH(CH3)2


1010
3
3-CH3-phenyl
CF3


1011
3
3-CH3-phenyl
—CH2CF3


1012
3
3-CH3-phenyl
—CH2CH2CF3


1013
3
3-CH3-phenyl
cyclopropyl


1014
3
3-CH3-phenyl
Cyclobutyl


1015
3
3-CH3-phenyl
cyclopentyl


1016
3
3-CH3-phenyl
cyclohexyl


1017
3
3-CH3-phenyl
3-pyridyl


1018
3
3-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


1019
3
3-CH3-phenyl
1H-imidazol-4-yl


1020
3
3-CH3-phenyl
2-furanyl


1021
3
3-OH-Phenyl
ethyl


1022
3
3-OH-Phenyl
n-propyl


1023
3
3-OH-Phenyl
isopropyl


1024
3
3-OH-Phenyl
—CH2CH(CH3)2


1025
3
3-OH-Phenyl
CF3


1026
3
3-OH-Phenyl
—CH2CF3


1027
3
3-OH-Phenyl
—CH2CH2CF3


1028
3
3-OH-Phenyl
cyclopropyl


1029
3
3-OH-Phenyl
Cyclobutyl


1030
3
3-OH-Phenyl
cyclopentyl


1031
3
3-OH-Phenyl
cyclohexyl


1032
3
3-OH-Phenyl
3-pyridyl


1033
3
3-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


1034
3
3-OH-Phenyl
1H-imidazol-4-yl


1035
3
3-OH-Phenyl
2-furanyl


1036
3
4-OMe-Phenyl
ethyl


1037
3
4-OMe-Phenyl
n-propyl


1038
3
4-OMe-Phenyl
isopropyl


1039
3
4-OMe-Phenyl
—CH2CH(CH3)2


1040
3
4-OMe-Phenyl
CF3


1041
3
4-OMe-Phenyl
—CH2CF3


1042
3
4-OMe-Phenyl
—CH2CH2CF3


1043
3
4-OMe-Phenyl
cyclopropyl


1044
3
4-OMe-Phenyl
Cyclobutyl


1045
3
4-OMe-Phenyl
cyclopentyl


1046
3
4-OMe-Phenyl
cyclohexyl


1047
3
4-OMe-Phenyl
3-pyridyl


1048
3
4-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


1049
3
4-OMe-Phenyl
1H-imidazol-4-yl


1050
3
4-OMe-Phenyl
2-furanyl


1051
3
2-OMe-Phenyl
ethyl


1052
3
2-OMe-Phenyl
n-propyl


1053
3
2-OMe-Phenyl
isopropyl


1054
3
2-OMe-Phenyl
—CH2CH(CH3)2


1055
3
2-OMe-Phenyl
CF3


1056
3
2-OMe-Phenyl
—CH2CF3


1057
3
2-OMe-Phenyl
—CH2CH2CF3


1058
3
2-OMe-Phenyl
cyclopropyl


1059
3
2-OMe-Phenyl
Cyclobutyl


1060
3
2-OMe-Phenyl
cyclopentyl


1061
3
2-OMe-Phenyl
cyclohexyl


1062
3
2-OMe-Phenyl
3-pyridyl


1063
3
2-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


1064
3
2-OMe-Phenyl
1H-imidazol-4-yl


1065
3
2-OMe-Phenyl
2-furanyl


1066
3
3-CN-Phenyl
ethyl


1067
3
3-CN-Phenyl
n-propyl


1068
3
3-CN-Phenyl
isopropyl


1069
3
3-CN-Phenyl
—CH2CH(CH3)2


1070
3
3-CN-Phenyl
CF3


1071
3
3-CN-Phenyl
—CH2CF3


1072
3
3-CN-Phenyl
—CH2CH2CF3


1073
3
3-CN-Phenyl
cyclopropyl


1074
3
3-CN-Phenyl
Cyclobutyl


1075
3
3-CN-Phenyl
cyclopentyl


1076
3
3-CN-Phenyl
cyclohexyl


1077
3
3-CN-Phenyl
3-pyridyl


1078
3
3-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


1079
3
3-CN-Phenyl
1H-imidazol-4-yl


1080
3
3-CN-Phenyl
2-furanyl


1081
3
2-F-Phenyl
ethyl


1082
3
2-F-Phenyl
n-propyl


1083
3
2-F-Phenyl
isopropyl


1084
3
2-F-Phenyl
—CH2CH(CH3)2


1085
3
2-F-Phenyl
CF3


1086
3
2-F-Phenyl
—CH2CF3


1087
3
2-F-Phenyl
—CH2CH2CF3


1088
3
2-F-Phenyl
cyclopropyl


1089
3
2-F-Phenyl
Cyclobutyl


1090
3
2-F-Phenyl
cyclopentyl


1091
3
2-F-Phenyl
cyclohexyl


1092
3
2-F-Phenyl
3-pyridyl


1093
3
2-F-Phenyl
1-methyl-1H-pyrazol-4-yl


1094
3
2-F-Phenyl
1H-imidazol-4-yl


1095
3
2-F-Phenyl
2-furanyl


1096
3
4-F-Phenyl
ethyl


1097
3
4-F-Phenyl
n-propyl


1098
3
4-F-Phenyl
isopropyl


1099
3
4-F-Phenyl
—CH2CH(CH3)2


1100
3
4-F-Phenyl
CF3


1101
3
4-F-Phenyl
—CH2CF3


1102
3
4-F-Phenyl
—CH2CH2CF3


1103
3
4-F-Phenyl
cyclopropyl


1104
3
4-F-Phenyl
Cyclobutyl


1105
3
4-F-Phenyl
cyclopentyl


1106
3
4-F-Phenyl
cyclohexyl


1107
3
4-F-Phenyl
3-pyridyl


1108
3
4-F-Phenyl
1-methyl-1H-pyrazol-4-yl


1109
3
4-F-Phenyl
1H-imidazol-4-yl


1110
3
4-F-Phenyl
2-furanyl


1111
3
3-Cl-Phenyl
ethyl


1112
3
3-Cl-Phenyl
n-propyl


1113
3
3-Cl-Phenyl
isopropyl


1114
3
3-Cl-Phenyl
—CH2CH(CH3)2


1115
3
3-Cl-Phenyl
CF3


1116
3
3-Cl-Phenyl
—CH2CF3


1117
3
3-Cl-Phenyl
—CH2CH2CF3


1118
3
3-Cl-Phenyl
cyclopropyl


1119
3
3-Cl-Phenyl
Cyclobutyl


1120
3
3-Cl-Phenyl
cyclopentyl


1121
3
3-Cl-Phenyl
cyclohexyl


1122
3
3-Cl-Phenyl
3-pyridyl


1123
3
3-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


1124
3
3-Cl-Phenyl
1H-imidazol-4-yl


1125
3
3-Cl-Phenyl
2-furanyl


1126
3
2-Br-Phenyl
ethyl


1127
3
2-Br-Phenyl
n-propyl


1128
3
2-Br-Phenyl
isopropyl


1129
3
2-Br-Phenyl
—CH2CH(CH3)2


1130
3
2-Br-Phenyl
CF3


1131
3
2-Br-Phenyl
—CH2CF3


1132
3
2-Br-Phenyl
—CH2CH2CF3


1133
3
2-Br-Phenyl
cyclopropyl


1134
3
2-Br-Phenyl
Cyclobutyl


1135
3
2-Br-Phenyl
cyclopentyl


1136
3
2-Br-Phenyl
cyclohexyl


1137
3
2-Br-Phenyl
3-pyridyl


1138
3
2-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


1139
3
2-Br-Phenyl
1H-imidazol-4-yl


1140
3
2-Br-Phenyl
2-furanyl


1141
3
4-Br-Phenyl
ethyl


1142
3
4-Br-Phenyl
n-propyl


1143
3
4-Br-Phenyl
isopropyl


1144
3
4-Br-Phenyl
—CH2CH(CH3)2


1145
3
4-Br-Phenyl
CF3


1146
3
4-Br-Phenyl
—CH2CF3


1147
3
4-Br-Phenyl
—CH2CH2CF3


1148
3
4-Br-Phenyl
cyclopropyl


1149
3
4-Br-Phenyl
Cyclobutyl


1150
3
4-Br-Phenyl
cyclopentyl


1151
3
4-Br-Phenyl
cyclohexyl


1152
3
4-Br-Phenyl
3-pyridyl


1153
3
4-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


1154
3
4-Br-Phenyl
1H-imidazol-4-yl


1155
3
4-Br-Phenyl
2-furanyl


1156
3
3-CF3-Phenyl
ethyl


1157
3
3-CF3-Phenyl
n-propyl


1158
3
3-CF3-Phenyl
isopropyl


1159
3
3-CF3-Phenyl
—CH2CH(CH3)2


1160
3
3-CF3-Phenyl
CF3


1161
3
3-CF3-Phenyl
—CH2CF3


1162
3
3-CF3-Phenyl
—CH2CH2CF3


1163
3
3-CF3-Phenyl
cyclopropyl


1164
3
3-CF3-Phenyl
Cyclobutyl


1165
3
3-CF3-Phenyl
cyclopentyl


1166
3
3-CF3-Phenyl
cyclohexyl


1167
3
3-CF3-Phenyl
3-pyridyl


1168
3
3-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


1169
3
3-CF3-Phenyl
1H-imidazol-4-yl


1170
3
3-CF3-Phenyl
2-furanyl


1171
3
2-iPr-Phenyl
ethyl


1172
3
2-iPr-Phenyl
n-propyl


1173
3
2-iPr-Phenyl
isopropyl


1174
3
2-iPr-Phenyl
—CH2CH(CH3)2


1175
3
2-iPr-Phenyl
CF3


1176
3
2-iPr-Phenyl
—CH2CF3


1177
3
2-iPr-Phenyl
—CH2CH2CF3


1178
3
2-iPr-Phenyl
cyclopropyl


1179
3
2-iPr-Phenyl
Cyclobutyl


1180
3
2-iPr-Phenyl
cyclopentyl


1181
3
2-iPr-Phenyl
cyclohexyl


1182
3
2-iPr-Phenyl
3-pyridyl


1183
3
2-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


1184
3
2-iPr-Phenyl
1H-imidazol-4-yl


1185
3
2-iPr-Phenyl
2-furanyl


1186
3
4-iPr-Phenyl
ethyl


1187
3
4-iPr-Phenyl
n-propyl


1188
3
4-iPr-Phenyl
isopropyl


1189
3
4-iPr-Phenyl
—CH2CH(CH3)2


1190
3
4-iPr-Phenyl
CF3


1191
3
4-iPr-Phenyl
—CH2CF3


1192
3
4-iPr-Phenyl
—CH2CH2CF3


1193
3
4-iPr-Phenyl
cyclopropyl


1194
3
4-iPr-Phenyl
Cyclobutyl


1195
3
4-iPr-Phenyl
cyclopentyl


1196
3
4-iPr-Phenyl
cyclohexyl


1197
3
4-iPr-Phenyl
3-pyridyl


1198
3
4-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


1199
3
4-iPr-Phenyl
1H-imidazol-4-yl


1200
3
4-iPr-Phenyl
2-furanyl


1201
3
3-morpholino-phenyl
ethyl


1202
3
3-morpholino-phenyl
n-propyl


1203
3
3-morpholino-phenyl
isopropyl


1204
3
3-morpholino-phenyl
—CH2CH(CH3)2


1205
3
3-morpholino-phenyl
CF3


1206
3
3-morpholino-phenyl
—CH2CF3


1207
3
3-morpholino-phenyl
—CH2CH2CF3


1208
3
3-morpholino-phenyl
cyclopropyl


1209
3
3-morpholino-phenyl
Cyclobutyl


1210
3
3-morpholino-phenyl
cyclopentyl


1211
3
3-morpholino-phenyl
cyclohexyl


1212
3
3-morpholino-phenyl
3-pyridyl


1213
3
3-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1214
3
3-morpholino-phenyl
1H-imidazol-4-yl


1215
3
3-morpholino-phenyl
2-furanyl


1216
3
4-cyano-2-morpholino-phenyl
ethyl


1217
3
4-cyano-2-morpholino-phenyl
n-propyl


1218
3
4-cyano-2-morpholino-phenyl
isopropyl


1219
3
4-cyano-2-morpholino-phenyl
—CH2CH(CH3)2


1220
3
4-cyano-2-morpholino-phenyl
CF3


1221
3
4-cyano-2-morpholino-phenyl
—CH2CF3


1222
3
4-cyano-2-morpholino-phenyl
—CH2CH2CF3


1223
3
4-cyano-2-morpholino-phenyl
cyclopropyl


1224
3
4-cyano-2-morpholino-phenyl
Cyclobutyl


1225
3
4-cyano-2-morpholino-phenyl
cyclopentyl


1226
3
4-cyano-2-morpholino-phenyl
cyclohexyl


1227
3
4-cyano-2-morpholino-phenyl
3-pyridyl


1228
3
4-cyano-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1229
3
4-cyano-2-morpholino-phenyl
1H-imidazol-4-yl


1230
3
4-cyano-2-morpholino-phenyl
2-furanyl


1231
3
4-hydroxy-2-morpholino-phenyl
ethyl


1232
3
4-hydroxy-2-morpholino-phenyl
n-propyl


1233
3
4-hydroxy-2-morpholino-phenyl
isopropyl


1234
3
4-hydroxy-2-morpholino-phenyl
—CH2CH(CH3)2


1235
3
4-hydroxy-2-morpholino-phenyl
CF3


1236
3
4-hydroxy-2-morpholino-phenyl
—CH2CF3


1237
3
4-hydroxy-2-morpholino-phenyl
—CH2CH2CF3


1238
3
4-hydroxy-2-morpholino-phenyl
cyclopropyl


1239
3
4-hydroxy-2-morpholino-phenyl
Cyclobutyl


1240
3
4-hydroxy-2-morpholino-phenyl
cyclopentyl


1241
3
4-hydroxy-2-morpholino-phenyl
cyclohexyl


1242
3
4-hydroxy-2-morpholino-phenyl
3-pyridyl


1243
3
4-hydroxy-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1244
3
4-hydroxy-2-morpholino-phenyl
1H-imidazol-4-yl


1245
3
4-hydroxy-2-morpholino-phenyl
2-furanyl


1246
3
2-CH3-phenyl
Ethyl


1247
3
2-CH3-phenyl
n-propyl


1248
3
2-CH3-phenyl
Isopropyl


1249
3
2-CH3-phenyl
—CH2CH(CH3)2


1250
3
2-CH3-phenyl
CF3


1251
3
2-CH3-phenyl
—CH2CF3


1252
3
2-CH3-phenyl
—CH2CH2CF3


1253
3
2-CH3-phenyl
cyclopropyl


1254
3
2-CH3-phenyl
Cyclobutyl


1255
3
2-CH3-phenyl
cyclopentyl


1256
3
2-CH3-phenyl
cyclohexyl


1257
3
2-CH3-phenyl
3-pyridyl


1258
3
2-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


1259
3
2-CH3-phenyl
1H-imidazol-4-yl


1260
3
2-CH3-phenyl
2-furanyl


1261
3
4-OH-Phenyl
Ethyl


1262
3
4-OH-Phenyl
n-propyl


1263
3
4-OH-Phenyl
Isopropyl


1264
3
4-OH-Phenyl
—CH2CH(CH3)2


1265
3
4-OH-Phenyl
CF3


1266
3
4-OH-Phenyl
—CH2CF3


1267
3
4-OH-Phenyl
—CH2CH2CF3


1268
3
4-OH-Phenyl
cyclopropyl


1269
3
4-OH-Phenyl
Cyclobutyl


1270
3
4-OH-Phenyl
cyclopentyl


1271
3
4-OH-Phenyl
cyclohexyl


1272
3
4-OH-Phenyl
3-pyridyl


1273
3
4-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


1274
3
4-OH-Phenyl
1H-imidazol-4-yl


1275
3
4-OH-Phenyl
2-furanyl


1276
3
2-OH-Phenyl
Ethyl


1277
3
2-OH-Phenyl
n-propyl


1278
3
2-OH-Phenyl
Isopropyl


1279
3
2-OH-Phenyl
—CH2CH(CH3)2


1280
3
2-OH-Phenyl
CF3


1281
3
2-OH-Phenyl
—CH2CF3


1282
3
2-OH-Phenyl
—CH2CH2CF3


1283
3
2-OH-Phenyl
cyclopropyl


1284
3
2-OH-Phenyl
Cyclobutyl


1285
3
2-OH-Phenyl
cyclopentyl


1286
3
2-OH-Phenyl
cyclohexyl


1287
3
2-OH-Phenyl
3-pyridyl


1288
3
2-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


1289
3
2-OH-Phenyl
1H-imidazol-4-yl


1290
3
2-OH-Phenyl
2-furanyl


1291
3
3-OMe-Phenyl
Ethyl


1292
3
3-OMe-Phenyl
n-propyl


1293
3
3-OMe-Phenyl
Isopropyl


1294
3
3-OMe-Phenyl
—CH2CH(CH3)2


1295
3
3-OMe-Phenyl
CF3


1296
3
3-OMe-Phenyl
—CH2CF3


1297
3
3-OMe-Phenyl
—CH2CH2CF3


1298
3
3-OMe-Phenyl
cyclopropyl


1299
3
3-OMe-Phenyl
Cyclobutyl


1300
3
3-OMe-Phenyl
cyclopentyl


1301
3
3-OMe-Phenyl
cyclohexyl


1302
3
3-OMe-Phenyl
3-pyridyl


1303
3
3-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


1304
3
3-OMe-Phenyl
1H-imidazol-4-yl


1305
3
3-OMe-Phenyl
2-furanyl


1306
3
4-CN-Phenyl
Ethyl


1307
3
4-CN-Phenyl
n-propyl


1308
3
4-CN-Phenyl
Isopropyl


1309
3
4-CN-Phenyl
—CH2CH(CH3)2


1310
3
4-CN-Phenyl
CF3


1311
3
4-CN-Phenyl
—CH2CF3


1312
3
4-CN-Phenyl
—CH2CH2CF3


1313
3
4-CN-Phenyl
cyclopropyl


1314
3
4-CN-Phenyl
Cyclobutyl


1315
3
4-CN-Phenyl
cyclopentyl


1316
3
4-CN-Phenyl
cyclohexyl


1317
3
4-CN-Phenyl
3-pyridyl


1318
3
4-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


1319
3
4-CN-Phenyl
1H-imidazol-4-yl


1320
3
4-CN-Phenyl
2-furanyl


1321
3
2-CN-Phenyl
Ethyl


1322
3
2-CN-Phenyl
n-propyl


1323
3
2-CN-Phenyl
Isopropyl


1324
3
2-CN-Phenyl
—CH2CH(CH3)2


1325
3
2-CN-Phenyl
CF3


1326
3
2-CN-Phenyl
—CH2CF3


1327
3
2-CN-Phenyl
—CH2CH2CF3


1328
3
2-CN-Phenyl
cyclopropyl


1329
3
2-CN-Phenyl
Cyclobutyl


1330
3
2-CN-Phenyl
cyclopentyl


1331
3
2-CN-Phenyl
cyclohexyl


1332
3
2-CN-Phenyl
3-pyridyl


1333
3
2-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


1334
3
2-CN-Phenyl
1H-imidazol-4-yl


1335
3
2-CN-Phenyl
2-furanyl


1336
3
3-F-Phenyl
Ethyl


1337
3
3-F-Phenyl
n-propyl


1338
3
3-F-Phenyl
Isopropyl


1339
3
3-F-Phenyl
—CH2CH(CH3)2


1340
3
3-F-Phenyl
CF3


1341
3
3-F-Phenyl
—CH2CF3


1342
3
3-F-Phenyl
—CH2CH2CF3


1343
3
3-F-Phenyl
cyclopropyl


1344
3
3-F-Phenyl
Cyclobutyl


1345
3
3-F-Phenyl
cyclopentyl


1346
3
3-F-Phenyl
cyclohexyl


1347
3
3-F-Phenyl
3-pyridyl


1348
3
3-F-Phenyl
1-methyl-1H-pyrazol-4-yl


1349
3
3-F-Phenyl
1H-imidazol-4-yl


1350
3
3-F-Phenyl
2-furanyl


1351
3
2-Cl-Phenyl
Ethyl


1352
3
2-Cl-Phenyl
n-propyl


1353
3
2-Cl-Phenyl
Isopropyl


1354
3
2-Cl-Phenyl
—CH2CH(CH3)2


1355
3
2-Cl-Phenyl
CF3


1356
3
2-Cl-Phenyl
—CH2CF3


1357
3
2-Cl-Phenyl
—CH2CH2CF3


1358
3
2-Cl-Phenyl
cyclopropyl


1359
3
2-Cl-Phenyl
Cyclobutyl


1360
3
2-Cl-Phenyl
cyclopentyl


1361
3
2-Cl-Phenyl
cyclohexyl


1362
3
2-Cl-Phenyl
3-pyridyl


1363
3
2-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


1364
3
2-Cl-Phenyl
1H-imidazol-4-yl


1365
3
2-Cl-Phenyl
2-furanyl


1366
3
4-Cl-Phenyl
Ethyl


1367
3
4-Cl-Phenyl
n-propyl


1368
3
4-Cl-Phenyl
Isopropyl


1369
3
4-Cl-Phenyl
—CH2CH(CH3)2


1370
3
4-Cl-Phenyl
CF3


1371
3
4-Cl-Phenyl
—CH2CF3


1372
3
4-Cl-Phenyl
—CH2CH2CF3


1373
3
4-Cl-Phenyl
cyclopropyl


1374
3
4-Cl-Phenyl
Cyclobutyl


1375
3
4-Cl-Phenyl
cyclopentyl


1376
3
4-Cl-Phenyl
cyclohexyl


1377
3
4-Cl-Phenyl
3-pyridyl


1378
3
4-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


1379
3
4-Cl-Phenyl
1H-imidazol-4-yl


1380
3
4-Cl-Phenyl
2-furanyl


1381
3
3-Br-Phenyl
Ethyl


1382
3
3-Br-Phenyl
n-propyl


1383
3
3-Br-Phenyl
Isopropyl


1384
3
3-Br-Phenyl
—CH2CH(CH3)2


1385
3
3-Br-Phenyl
CF3


1386
3
3-Br-Phenyl
—CH2CF3


1387
3
3-Br-Phenyl
—CH2CH2CF3


1388
3
3-Br-Phenyl
cyclopropyl


1389
3
3-Br-Phenyl
Cyclobutyl


1390
3
3-Br-Phenyl
cyclopentyl


1391
3
3-Br-Phenyl
cyclohexyl


1392
3
3-Br-Phenyl
3-pyridyl


1393
3
3-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


1394
3
3-Br-Phenyl
1H-imidazol-4-yl


1395
3
3-Br-Phenyl
2-furanyl


1396
3
2-CF3-Phenyl
Ethyl


1397
3
2-CF3-Phenyl
n-propyl


1398
3
2-CF3-Phenyl
Isopropyl


1399
3
2-CF3-Phenyl
—CH2CH(CH3)2


1400
3
2-CF3-Phenyl
CF3


1401
3
2-CF3-Phenyl
—CH2CF3


1402
3
2-CF3-Phenyl
—CH2CH2CF3


1403
3
2-CF3-Phenyl
cyclopropyl


1404
3
2-CF3-Phenyl
Cyclobutyl


1405
3
2-CF3-Phenyl
cyclopentyl


1406
3
2-CF3-Phenyl
cyclohexyl


1407
3
2-CF3-Phenyl
3-pyridyl


1408
3
2-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


1409
3
2-CF3-Phenyl
1H-imidazol-4-yl


1410
3
2-CF3-Phenyl
2-furanyl


1411
3
4-CF3-Phenyl
Ethyl


1412
3
4-CF3-Phenyl
n-propyl


1413
3
4-CF3-Phenyl
Isopropyl


1414
3
4-CF3-Phenyl
—CH2CH(CH3)2


1415
3
4-CF3-Phenyl
CF3


1416
3
4-CF3-Phenyl
—CH2CF3


1417
3
4-CF3-Phenyl
—CH2CH2CF3


1418
3
4-CF3-Phenyl
cyclopropyl


1419
3
4-CF3-Phenyl
Cyclobutyl


1420
3
4-CF3-Phenyl
cyclopentyl


1421
3
4-CF3-Phenyl
cyclohexyl


1422
3
4-CF3-Phenyl
3-pyridyl


1423
3
4-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


1424
3
4-CF3-Phenyl
1H-imidazol-4-yl


1425
3
4-CF3-Phenyl
2-furanyl


1426
3
3-iPr-Phenyl
Ethyl


1427
3
3-iPr-Phenyl
n-propyl


1428
3
3-iPr-Phenyl
Isopropyl


1429
3
3-iPr-Phenyl
—CH2CH(CH3)2


1430
3
3-iPr-Phenyl
CF3


1431
3
3-iPr-Phenyl
—CH2CF3


1432
3
3-iPr-Phenyl
—CH2CH2CF3


1433
3
3-iPr-Phenyl
cyclopropyl


1434
3
3-iPr-Phenyl
Cyclobutyl


1435
3
3-iPr-Phenyl
cyclopentyl


1436
3
3-iPr-Phenyl
cyclohexyl


1437
3
3-iPr-Phenyl
3-pyridyl


1438
3
3-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


1439
3
3-iPr-Phenyl
1H-imidazol-4-yl


1440
3
3-iPr-Phenyl
2-furanyl


1441
3
2-morpholino-phenyl
Ethyl


1442
3
2-morpholino-phenyl
n-propyl


1443
3
2-morpholino-phenyl
isopropyl


1444
3
2-morpholino-phenyl
—CH2CH(CH3)2


1445
3
2-morpholino-phenyl
CF3


1446
3
2-morpholino-phenyl
—CH2CF3


1447
3
2-morpholino-phenyl
—CH2CH2CF3


1448
3
2-morpholino-phenyl
cyclopropyl


1449
3
2-morpholino-phenyl
Cyclobutyl


1450
3
2-morpholino-phenyl
cyclopentyl


1451
3
2-morpholino-phenyl
cyclohexyl


1452
3
2-morpholino-phenyl
3-pyridyl


1453
3
2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1454
3
2-morpholino-phenyl
1H-imidazol-4-yl


1455
3
2-morpholino-phenyl
2-furanyl


1456
3
4-morpholino-phenyl
ethyl


1457
3
4-morpholino-phenyl
n-propyl


1458
3
4-morpholino-phenyl
isopropyl


1459
3
4-morpholino-phenyl
—CH2CH(CH3)2


1460
3
4-morpholino-phenyl
CF3


1461
3
4-morpholino-phenyl
—CH2CF3


1462
3
4-morpholino-phenyl
—CH2CH2CF3


1463
3
4-morpholino-phenyl
cyclopropyl


1464
3
4-morpholino-phenyl
Cyclobutyl


1465
3
4-morpholino-phenyl
cyclopentyl


1466
3
4-morpholino-phenyl
cyclohexyl


1467
3
4-morpholino-phenyl
3-pyridyl


1468
3
4-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1469
3
4-morpholino-phenyl
1H-imidazol-4-yl


1470
3
4-morpholino-phenyl
2-furanyl


1471
3
4-methyl-2-morpholino-phenyl
ethyl


1472
3
4-methyl-2-morpholino-phenyl
n-propyl


1473
3
4-methyl-2-morpholino-phenyl
isopropyl


1474
3
4-methyl-2-morpholino-phenyl
—CH2CH(CH3)2


1475
3
4-methyl-2-morpholino-phenyl
CF3


1476
3
4-methyl-2-morpholino-phenyl
—CH2CF3


1477
3
4-methyl-2-morpholino-phenyl
—CH2CH2CF3


1478
3
4-methyl-2-morpholino-phenyl
cyclopropyl


1479
3
4-methyl-2-morpholino-phenyl
Cyclobutyl


1480
3
4-methyl-2-morpholino-phenyl
cyclopentyl


1481
3
4-methyl-2-morpholino-phenyl
cyclohexyl


1482
3
4-methyl-2-morpholino-phenyl
3-pyridyl


1483
3
4-methyl-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1484
3
4-methyl-2-morpholino-phenyl
1H-imidazol-4-yl


1485
3
4-methyl-2-morpholino-phenyl
2-furanyl


1486
4
4-CH3-phenyl
ethyl


1487
4
4-CH3-phenyl
n-propyl


1488
4
4-CH3-phenyl
isopropyl


1489
4
4-CH3-phenyl
—CH2CH(CH3)2


1490
4
4-CH3-phenyl
CF3


1491
4
4-CH3-phenyl
—CH2CF3


1492
4
4-CH3-phenyl
—CH2CH2CF3


1493
4
4-CH3-phenyl
cyclopropyl


1494
4
4-CH3-phenyl
Cyclobutyl


1495
4
4-CH3-phenyl
cyclopentyl


1496
4
4-CH3-phenyl
cyclohexyl


1497
4
4-CH3-phenyl
3-pyridyl


1498
4
4-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


1499
4
4-CH3-phenyl
1H-imidazol-4-yl


1500
4
4-CH3-phenyl
2-furanyl


1501
4
3-CH3-phenyl
ethyl


1502
4
3-CH3-phenyl
n-propyl


1503
4
3-CH3-phenyl
isopropyl


1504
4
3-CH3-phenyl
—CH2CH(CH3)2


1505
4
3-CH3-phenyl
CF3


1506
4
3-CH3-phenyl
—CH2CF3


1507
4
3-CH3-phenyl
—CH2CH2CF3


1508
4
3-CH3-phenyl
cyclopropyl


1509
4
3-CH3-phenyl
Cyclobutyl


1510
4
3-CH3-phenyl
cyclopentyl


1511
4
3-CH3-phenyl
cyclohexyl


1512
4
3-CH3-phenyl
3-pyridyl


1513
4
3-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


1514
4
3-CH3-phenyl
1H-imidazol-4-yl


1515
4
3-CH3-phenyl
2-furanyl


1516
4
3-OH-Phenyl
ethyl


1517
4
3-OH-Phenyl
n-propyl


1518
4
3-OH-Phenyl
isopropyl


1519
4
3-OH-Phenyl
—CH2CH(CH3)2


1520
4
3-OH-Phenyl
CF3


1521
4
3-OH-Phenyl
—CH2CF3


1522
4
3-OH-Phenyl
—CH2CH2CF3


1523
4
3-OH-Phenyl
cyclopropyl


1524
4
3-OH-Phenyl
Cyclobutyl


1525
4
3-OH-Phenyl
cyclopentyl


1526
4
3-OH-Phenyl
cyclohexyl


1527
4
3-OH-Phenyl
3-pyridyl


1528
4
3-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


1529
4
3-OH-Phenyl
1H-imidazol-4-yl


1530
4
3-OH-Phenyl
2-furanyl


1531
4
4-OMe-Phenyl
ethyl


1532
4
4-OMe-Phenyl
n-propyl


1533
4
4-OMe-Phenyl
isopropyl


1534
4
4-OMe-Phenyl
—CH2CH(CH3)2


1535
4
4-OMe-Phenyl
CF3


1536
4
4-OMe-Phenyl
—CH2CF3


1537
4
4-OMe-Phenyl
—CH2CH2CF3


1538
4
4-OMe-Phenyl
cyclopropyl


1539
4
4-OMe-Phenyl
Cyclobutyl


1540
4
4-OMe-Phenyl
cyclopentyl


1541
4
4-OMe-Phenyl
cyclohexyl


1542
4
4-OMe-Phenyl
3-pyridyl


1543
4
4-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


1544
4
4-OMe-Phenyl
1H-imidazol-4-yl


1545
4
4-OMe-Phenyl
2-furanyl


1546
4
2-OMe-Phenyl
ethyl


1547
4
2-OMe-Phenyl
n-propyl


1548
4
2-OMe-Phenyl
isopropyl


1549
4
2-OMe-Phenyl
—CH2CH(CH3)2


1550
4
2-OMe-Phenyl
CF3


1551
4
2-OMe-Phenyl
—CH2CF3


1552
4
2-OMe-Phenyl
—CH2CH2CF3


1553
4
2-OMe-Phenyl
cyclopropyl


1554
4
2-OMe-Phenyl
Cyclobutyl


1555
4
2-OMe-Phenyl
cyclopentyl


1556
4
2-OMe-Phenyl
cyclohexyl


1557
4
2-OMe-Phenyl
3-pyridyl


1558
4
2-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


1559
4
2-OMe-Phenyl
1H-imidazol-4-yl


1560
4
2-OMe-Phenyl
2-furanyl


1561
4
3-CN-Phenyl
ethyl


1562
4
3-CN-Phenyl
n-propyl


1563
4
3-CN-Phenyl
isopropyl


1564
4
3-CN-Phenyl
—CH2CH(CH3)2


1565
4
3-CN-Phenyl
CF3


1566
4
3-CN-Phenyl
—CH2CF3


1567
4
3-CN-Phenyl
—CH2CH2CF3


1568
4
3-CN-Phenyl
cyclopropyl


1569
4
3-CN-Phenyl
Cyclobutyl


1570
4
3-CN-Phenyl
cyclopentyl


1571
4
3-CN-Phenyl
cyclohexyl


1572
4
3-CN-Phenyl
3-pyridyl


1573
4
3-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


1574
4
3-CN-Phenyl
1H-imidazol-4-yl


1575
4
3-CN-Phenyl
2-furanyl


1576
4
2-F-Phenyl
ethyl


1577
4
2-F-Phenyl
n-propyl


1578
4
2-F-Phenyl
isopropyl


1579
4
2-F-Phenyl
—CH2CH(CH3)2


1580
4
2-F-Phenyl
CF3


1581
4
2-F-Phenyl
—CH2CF3


1582
4
2-F-Phenyl
—CH2CH2CF3


1583
4
2-F-Phenyl
cyclopropyl


1584
4
2-F-Phenyl
Cyclobutyl


1585
4
2-F-Phenyl
cyclopentyl


1586
4
2-F-Phenyl
cyclohexyl


1587
4
2-F-Phenyl
3-pyridyl


1588
4
2-F-Phenyl
1-methyl-1H-pyrazol-4-yl


1589
4
2-F-Phenyl
1H-imidazol-4-yl


1590
4
2-F-Phenyl
2-furanyl


1591
4
4-F-Phenyl
ethyl


1592
4
4-F-Phenyl
n-propyl


1593
4
4-F-Phenyl
isopropyl


1594
4
4-F-Phenyl
—CH2CH(CH3)2


1595
4
4-F-Phenyl
CF3


1596
4
4-F-Phenyl
—CH2CF3


1597
4
4-F-Phenyl
—CH2CH2CF3


1598
4
4-F-Phenyl
cyclopropyl


1599
4
4-F-Phenyl
Cyclobutyl


1600
4
4-F-Phenyl
cyclopentyl


1601
4
4-F-Phenyl
cyclohexyl


1602
4
4-F-Phenyl
3-pyridyl


1603
4
4-F-Phenyl
1-methyl-1H-pyrazol-4-yl


1604
4
4-F-Phenyl
1H-imidazol-4-yl


1605
4
4-F-Phenyl
2-furanyl


1606
4
3-Cl-Phenyl
ethyl


1607
4
3-Cl-Phenyl
n-propyl


1608
4
3-Cl-Phenyl
isopropyl


1609
4
3-Cl-Phenyl
—CH2CH(CH3)2


1610
4
3-Cl-Phenyl
CF3


1611
4
3-Cl-Phenyl
—CH2CF3


1612
4
3-Cl-Phenyl
—CH2CH2CF3


1613
4
3-Cl-Phenyl
cyclopropyl


1614
4
3-Cl-Phenyl
Cyclobutyl


1615
4
3-Cl-Phenyl
cyclopentyl


1616
4
3-Cl-Phenyl
cyclohexyl


1617
4
3-Cl-Phenyl
3-pyridyl


1618
4
3-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


1619
4
3-Cl-Phenyl
1H-imidazol-4-yl


1620
4
3-Cl-Phenyl
2-furanyl


1621
4
2-Br-Phenyl
ethyl


1622
4
2-Br-Phenyl
n-propyl


1623
4
2-Br-Phenyl
isopropyl


1624
4
2-Br-Phenyl
—CH2CH(CH3)2


1625
4
2-Br-Phenyl
CF3


1626
4
2-Br-Phenyl
—CH2CF3


1627
4
2-Br-Phenyl
—CH2CH2CF3


1628
4
2-Br-Phenyl
cyclopropyl


1629
4
2-Br-Phenyl
Cyclobutyl


1630
4
2-Br-Phenyl
cyclopentyl


1631
4
2-Br-Phenyl
cyclohexyl


1632
4
2-Br-Phenyl
3-pyridyl


1633
4
2-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


1634
4
2-Br-Phenyl
1H-imidazol-4-yl


1635
4
2-Br-Phenyl
2-furanyl


1636
4
4-Br-Phenyl
ethyl


1637
4
4-Br-Phenyl
n-propyl


1638
4
4-Br-Phenyl
isopropyl


1639
4
4-Br-Phenyl
—CH2CH(CH3)2


1640
4
4-Br-Phenyl
CF3


1641
4
4-Br-Phenyl
—CH2CF3


1642
4
4-Br-Phenyl
—CH2CH2CF3


1643
4
4-Br-Phenyl
cyclopropyl


1644
4
4-Br-Phenyl
Cyclobutyl


1645
4
4-Br-Phenyl
cyclopentyl


1646
4
4-Br-Phenyl
cyclohexyl


1647
4
4-Br-Phenyl
3-pyridyl


1648
4
4-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


1649
4
4-Br-Phenyl
1H-imidazol-4-yl


1650
4
4-Br-Phenyl
2-furanyl


1651
4
3-CF3-Phenyl
ethyl


1652
4
3-CF3-Phenyl
n-propyl


1653
4
3-CF3-Phenyl
isopropyl


1654
4
3-CF3-Phenyl
—CH2CH(CH3)2


1655
4
3-CF3-Phenyl
CF3


1656
4
3-CF3-Phenyl
—CH2CF3


1657
4
3-CF3-Phenyl
—CH2CH2CF3


1658
4
3-CF3-Phenyl
cyclopropyl


1659
4
3-CF3-Phenyl
Cyclobutyl


1660
4
3-CF3-Phenyl
cyclopentyl


1661
4
3-CF3-Phenyl
cyclohexyl


1662
4
3-CF3-Phenyl
3-pyridyl


1663
4
3-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


1664
4
3-CF3-Phenyl
1H-imidazol-4-yl


1665
4
3-CF3-Phenyl
2-furanyl


1666
4
2-iPr-Phenyl
ethyl


1667
4
2-iPr-Phenyl
n-propyl


1668
4
2-iPr-Phenyl
isopropyl


1669
4
2-iPr-Phenyl
—CH2CH(CH3)2


1670
4
2-iPr-Phenyl
CF3


1671
4
2-iPr-Phenyl
—CH2CF3


1672
4
2-iPr-Phenyl
—CH2CH2CF3


1673
4
2-iPr-Phenyl
cyclopropyl


1674
4
2-iPr-Phenyl
Cyclobutyl


1675
4
2-iPr-Phenyl
cyclopentyl


1676
4
2-iPr-Phenyl
cyclohexyl


1677
4
2-iPr-Phenyl
3-pyridyl


1678
4
2-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


1679
4
2-iPr-Phenyl
1H-imidazol-4-yl


1680
4
2-iPr-Phenyl
2-furanyl


1681
4
4-iPr-Phenyl
ethyl


1682
4
4-iPr-Phenyl
n-propyl


1683
4
4-iPr-Phenyl
isopropyl


1684
4
4-iPr-Phenyl
—CH2CH(CH3)2


1685
4
4-iPr-Phenyl
CF3


1686
4
4-iPr-Phenyl
—CH2CF3


1687
4
4-iPr-Phenyl
—CH2CH2CF3


1688
4
4-iPr-Phenyl
cyclopropyl


1689
4
4-iPr-Phenyl
Cyclobutyl


1690
4
4-iPr-Phenyl
cyclopentyl


1691
4
4-iPr-Phenyl
cyclohexyl


1692
4
4-iPr-Phenyl
3-pyridyl


1693
4
4-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


1694
4
4-iPr-Phenyl
1H-imidazol-4-yl


1695
4
4-iPr-Phenyl
2-furanyl


1696
4
3-morpholino-phenyl
ethyl


1697
4
3-morpholino-phenyl
n-propyl


1698
4
3-morpholino-phenyl
isopropyl


1699
4
3-morpholino-phenyl
—CH2CH(CH3)2


1700
4
3-morpholino-phenyl
CF3


1701
4
3-morpholino-phenyl
—CH2CF3


1702
4
3-morpholino-phenyl
—CH2CH2CF3


1703
4
3-morpholino-phenyl
cyclopropyl


1704
4
3-morpholino-phenyl
Cyclobutyl


1705
4
3-morpholino-phenyl
cyclopentyl


1706
4
3-morpholino-phenyl
cyclohexyl


1707
4
3-morpholino-phenyl
3-pyridyl


1708
4
3-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1709
4
3-morpholino-phenyl
1H-imidazol-4-yl


1710
4
3-morpholino-phenyl
2-furanyl


1711
4
4-cyano-2-morpholino-phenyl
ethyl


1712
4
4-cyano-2-morpholino-phenyl
n-propyl


1713
4
4-cyano-2-morpholino-phenyl
isopropyl


1714
4
4-cyano-2-morpholino-phenyl
—CH2CH(CH3)2


1715
4
4-cyano-2-morpholino-phenyl
CF3


1716
4
4-cyano-2-morpholino-phenyl
—CH2CF3


1717
4
4-cyano-2-morpholino-phenyl
—CH2CH2CF3


1718
4
4-cyano-2-morpholino-phenyl
cyclopropyl


1719
4
4-cyano-2-morpholino-phenyl
Cyclobutyl


1720
4
4-cyano-2-morpholino-phenyl
cyclopentyl


1721
4
4-cyano-2-morpholino-phenyl
cyclohexyl


1722
4
4-cyano-2-morpholino-phenyl
3-pyridyl


1723
4
4-cyano-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1724
4
4-cyano-2-morpholino-phenyl
1H-imidazol-4-yl


1725
4
4-cyano-2-morpholino-phenyl
2-furanyl


1726
4
4-hydroxy-2-morpholino-phenyl
ethyl


1727
4
4-hydroxy-2-morpholino-phenyl
n-propyl


1728
4
4-hydroxy-2-morpholino-phenyl
isopropyl


1729
4
4-hydroxy-2-morpholino-phenyl
—CH2CH(CH3)2


1730
4
4-hydroxy-2-morpholino-phenyl
CF3


1731
4
4-hydroxy-2-morpholino-phenyl
—CH2CF3


1732
4
4-hydroxy-2-morpholino-phenyl
—CH2CH2CF3


1733
4
4-hydroxy-2-morpholino-phenyl
cyclopropyl


1734
4
4-hydroxy-2-morpholino-phenyl
Cyclobutyl


1735
4
4-hydroxy-2-morpholino-phenyl
cyclopentyl


1736
4
4-hydroxy-2-morpholino-phenyl
cyclohexyl


1737
4
4-hydroxy-2-morpholino-phenyl
3-pyridyl


1738
4
4-hydroxy-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1739
4
4-hydroxy-2-morpholino-phenyl
1H-imidazol-4-yl


1740
4
4-hydroxy-2-morpholino-phenyl
2-furanyl


1741
4
2-CH3-phenyl
Ethyl


1742
4
2-CH3-phenyl
n-propyl


1743
4
2-CH3-phenyl
Isopropyl


1744
4
2-CH3-phenyl
—CH2CH(CH3)2


1745
4
2-CH3-phenyl
CF3


1746
4
2-CH3-phenyl
—CH2CF3


1747
4
2-CH3-phenyl
—CH2CH2CF3


1748
4
2-CH3-phenyl
cyclopropyl


1749
4
2-CH3-phenyl
Cyclobutyl


1750
4
2-CH3-phenyl
cyclopentyl


1751
4
2-CH3-phenyl
cyclohexyl


1752
4
2-CH3-phenyl
3-pyridyl


1753
4
2-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


1754
4
2-CH3-phenyl
1H-imidazol-4-yl


1755
4
2-CH3-phenyl
2-furanyl


1756
4
4-OH-Phenyl
Ethyl


1757
4
4-OH-Phenyl
n-propyl


1758
4
4-OH-Phenyl
Isopropyl


1759
4
4-OH-Phenyl
—CH2CH(CH3)2


1760
4
4-OH-Phenyl
CF3


1761
4
4-OH-Phenyl
—CH2CF3


1762
4
4-OH-Phenyl
—CH2CH2CF3


1763
4
4-OH-Phenyl
cyclopropyl


1764
4
4-OH-Phenyl
Cyclobutyl


1765
4
4-OH-Phenyl
cyclopentyl


1766
4
4-OH-Phenyl
cyclohexyl


1767
4
4-OH-Phenyl
3-pyridyl


1768
4
4-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


1769
4
4-OH-Phenyl
1H-imidazol-4-yl


1770
4
4-OH-Phenyl
2-furanyl


1771
4
2-OH-Phenyl
Ethyl


1772
4
2-OH-Phenyl
n-propyl


1773
4
2-OH-Phenyl
Isopropyl


1774
4
2-OH-Phenyl
—CH2CH(CH3)2


1775
4
2-OH-Phenyl
CF3


1776
4
2-OH-Phenyl
—CH2CF3


1777
4
2-OH-Phenyl
—CH2CH2CF3


1778
4
2-OH-Phenyl
cyclopropyl


1779
4
2-OH-Phenyl
Cyclobutyl


1780
4
2-OH-Phenyl
cyclopentyl


1781
4
2-OH-Phenyl
cyclohexyl


1782
4
2-OH-Phenyl
3-pyridyl


1783
4
2-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


1784
4
2-OH-Phenyl
1H-imidazol-4-yl


1785
4
2-OH-Phenyl
2-furanyl


1786
4
3-OMe-Phenyl
Ethyl


1787
4
3-OMe-Phenyl
n-propyl


1788
4
3-OMe-Phenyl
Isopropyl


1789
4
3-OMe-Phenyl
—CH2CH(CH3)2


1790
4
3-OMe-Phenyl
CF3


1791
4
3-OMe-Phenyl
—CH2CF3


1792
4
3-OMe-Phenyl
—CH2CH2CF3


1793
4
3-OMe-Phenyl
cyclopropyl


1794
4
3-OMe-Phenyl
Cyclobutyl


1795
4
3-OMe-Phenyl
cyclopentyl


1796
4
3-OMe-Phenyl
cyclohexyl


1797
4
3-OMe-Phenyl
3-pyridyl


1798
4
3-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


1799
4
3-OMe-Phenyl
1H-imidazol-4-yl


1800
4
3-OMe-Phenyl
2-furanyl


1801
4
4-CN-Phenyl
Ethyl


1802
4
4-CN-Phenyl
n-propyl


1803
4
4-CN-Phenyl
Isopropyl


1804
4
4-CN-Phenyl
—CH2CH(CH3)2


1805
4
4-CN-Phenyl
CF3


1806
4
4-CN-Phenyl
—CH2CF3


1807
4
4-CN-Phenyl
—CH2CH2CF3


1808
4
4-CN-Phenyl
cyclopropyl


1809
4
4-CN-Phenyl
Cyclobutyl


1810
4
4-CN-Phenyl
cyclopentyl


1811
4
4-CN-Phenyl
cyclohexyl


1812
4
4-CN-Phenyl
3-pyridyl


1813
4
4-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


1814
4
4-CN-Phenyl
1H-imidazol-4-yl


1815
4
4-CN-Phenyl
2-furanyl


1816
4
2-CN-Phenyl
Ethyl


1817
4
2-CN-Phenyl
n-propyl


1818
4
2-CN-Phenyl
Isopropyl


1819
4
2-CN-Phenyl
—CH2CH(CH3)2


1820
4
2-CN-Phenyl
CF3


1821
4
2-CN-Phenyl
—CH2CF3


1822
4
2-CN-Phenyl
—CH2CH2CF3


1823
4
2-CN-Phenyl
cyclopropyl


1824
4
2-CN-Phenyl
Cyclobutyl


1825
4
2-CN-Phenyl
cyclopentyl


1826
4
2-CN-Phenyl
cyclohexyl


1827
4
2-CN-Phenyl
3-pyridyl


1828
4
2-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


1829
4
2-CN-Phenyl
1H-imidazol-4-yl


1830
4
2-CN-Phenyl
2-furanyl


1831
4
3-F-Phenyl
Ethyl


1832
4
3-F-Phenyl
n-propyl


1833
4
3-F-Phenyl
Isopropyl


1834
4
3-F-Phenyl
—CH2CH(CH3)2


1835
4
3-F-Phenyl
CF3


1836
4
3-F-Phenyl
—CH2CF3


1837
4
3-F-Phenyl
—CH2CH2CF3


1838
4
3-F-Phenyl
cyclopropyl


1839
4
3-F-Phenyl
Cyclobutyl


1840
4
3-F-Phenyl
cyclopentyl


1841
4
3-F-Phenyl
cyclohexyl


1842
4
3-F-Phenyl
3-pyridyl


1843
4
3-F-Phenyl
1-methyl-1H-pyrazol-4-yl


1844
4
3-F-Phenyl
1H-imidazol-4-yl


1845
4
3-F-Phenyl
2-furanyl


1846
4
2-Cl-Phenyl
Ethyl


1847
4
2-Cl-Phenyl
n-propyl


1848
4
2-Cl-Phenyl
Isopropyl


1849
4
2-Cl-Phenyl
—CH2CH(CH3)2


1850
4
2-Cl-Phenyl
CF3


1851
4
2-Cl-Phenyl
—CH2CF3


1852
4
2-Cl-Phenyl
—CH2CH2CF3


1853
4
2-Cl-Phenyl
cyclopropyl


1854
4
2-Cl-Phenyl
Cyclobutyl


1855
4
2-Cl-Phenyl
cyclopentyl


1856
4
2-Cl-Phenyl
cyclohexyl


1857
4
2-Cl-Phenyl
3-pyridyl


1858
4
2-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


1859
4
2-Cl-Phenyl
1H-imidazol-4-yl


1860
4
2-Cl-Phenyl
2-furanyl


1861
4
4-Cl-Phenyl
Ethyl


1862
4
4-Cl-Phenyl
n-propyl


1863
4
4-Cl-Phenyl
Isopropyl


1864
4
4-Cl-Phenyl
—CH2CH(CH3)2


1865
4
4-Cl-Phenyl
CF3


1866
4
4-Cl-Phenyl
—CH2CF3


1867
4
4-Cl-Phenyl
—CH2CH2CF3


1868
4
4-Cl-Phenyl
cyclopropyl


1869
4
4-Cl-Phenyl
Cyclobutyl


1870
4
4-Cl-Phenyl
cyclopentyl


1871
4
4-Cl-Phenyl
cyclohexyl


1872
4
4-Cl-Phenyl
3-pyridyl


1873
4
4-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


1874
4
4-Cl-Phenyl
1H-imidazol-4-yl


1875
4
4-Cl-Phenyl
2-furanyl


1876
4
3-Br-Phenyl
Ethyl


1877
4
3-Br-Phenyl
n-propyl


1878
4
3-Br-Phenyl
Isopropyl


1879
4
3-Br-Phenyl
—CH2CH(CH3)2


1880
4
3-Br-Phenyl
CF3


1881
4
3-Br-Phenyl
—CH2CF3


1882
4
3-Br-Phenyl
—CH2CH2CF3


1883
4
3-Br-Phenyl
cyclopropyl


1884
4
3-Br-Phenyl
Cyclobutyl


1885
4
3-Br-Phenyl
cyclopentyl


1886
4
3-Br-Phenyl
cyclohexyl


1887
4
3-Br-Phenyl
3-pyridyl


1888
4
3-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


1889
4
3-Br-Phenyl
1H-imidazol-4-yl


1890
4
3-Br-Phenyl
2-furanyl


1891
4
2-CF3-Phenyl
Ethyl


1892
4
2-CF3-Phenyl
n-propyl


1893
4
2-CF3-Phenyl
Isopropyl


1894
4
2-CF3-Phenyl
—CH2CH(CH3)2


1895
4
2-CF3-Phenyl
CF3


1896
4
2-CF3-Phenyl
—CH2CF3


1897
4
2-CF3-Phenyl
—CH2CH2CF3


1898
4
2-CF3-Phenyl
cyclopropyl


1899
4
2-CF3-Phenyl
Cyclobutyl


1900
4
2-CF3-Phenyl
cyclopentyl


1901
4
2-CF3-Phenyl
cyclohexyl


1902
4
2-CF3-Phenyl
3-pyridyl


1903
4
2-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


1904
4
2-CF3-Phenyl
1H-imidazol-4-yl


1905
4
2-CF3-Phenyl
2-furanyl


1906
4
4-CF3-Phenyl
Ethyl


1907
4
4-CF3-Phenyl
n-propyl


1908
4
4-CF3-Phenyl
Isopropyl


1909
4
4-CF3-Phenyl
—CH2CH(CH3)2


1910
4
4-CF3-Phenyl
CF3


1911
4
4-CF3-Phenyl
—CH2CF3


1912
4
4-CF3-Phenyl
—CH2CH2CF3


1913
4
4-CF3-Phenyl
cyclopropyl


1914
4
4-CF3-Phenyl
Cyclobutyl


1915
4
4-CF3-Phenyl
cyclopentyl


1916
4
4-CF3-Phenyl
cyclohexyl


1917
4
4-CF3-Phenyl
3-pyridyl


1918
4
4-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


1919
4
4-CF3-Phenyl
1H-imidazol-4-yl


1920
4
4-CF3-Phenyl
2-furanyl


1921
4
3-iPr-Phenyl
Ethyl


1922
4
3-iPr-Phenyl
n-propyl


1923
4
3-iPr-Phenyl
Isopropyl


1924
4
3-iPr-Phenyl
—CH2CH(CH3)2


1925
4
3-iPr-Phenyl
CF3


1926
4
3-iPr-Phenyl
—CH2CF3


1927
4
3-iPr-Phenyl
—CH2CH2CF3


1928
4
3-iPr-Phenyl
cyclopropyl


1929
4
3-iPr-Phenyl
Cyclobutyl


1930
4
3-iPr-Phenyl
cyclopentyl


1931
4
3-iPr-Phenyl
cyclohexyl


1932
4
3-iPr-Phenyl
3-pyridyl


1933
4
3-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


1934
4
3-iPr-Phenyl
1H-imidazol-4-yl


1935
4
3-iPr-Phenyl
2-furanyl


1936
4
2-morpholino-phenyl
Ethyl


1937
4
2-morpholino-phenyl
n-propyl


1938
4
2-morpholino-phenyl
isopropyl


1939
4
2-morpholino-phenyl
—CH2CH(CH3)2


1940
4
2-morpholino-phenyl
CF3


1941
4
2-morpholino-phenyl
—CH2CF3


1942
4
2-morpholino-phenyl
—CH2CH2CF3


1943
4
2-morpholino-phenyl
cyclopropyl


1944
4
2-morpholino-phenyl
Cyclobutyl


1945
4
2-morpholino-phenyl
cyclopentyl


1946
4
2-morpholino-phenyl
cyclohexyl


1947
4
2-morpholino-phenyl
3-pyridyl


1948
4
2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1949
4
2-morpholino-phenyl
1H-imidazol-4-yl


1950
4
2-morpholino-phenyl
2-furanyl


1951
4
4-morpholino-phenyl
ethyl


1952
4
4-morpholino-phenyl
n-propyl


1953
4
4-morpholino-phenyl
isopropyl


1954
4
4-morpholino-phenyl
—CH2CH(CH3)2


1955
4
4-morpholino-phenyl
CF3


1956
4
4-morpholino-phenyl
—CH2CF3


1957
4
4-morpholino-phenyl
—CH2CH2CF3


1958
4
4-morpholino-phenyl
cyclopropyl


1959
4
4-morpholino-phenyl
Cyclobutyl


1960
4
4-morpholino-phenyl
cyclopentyl


1961
4
4-morpholino-phenyl
cyclohexyl


1962
4
4-morpholino-phenyl
3-pyridyl


1963
4
4-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1964
4
4-morpholino-phenyl
1H-imidazol-4-yl


1965
4
4-morpholino-phenyl
2-furanyl


1966
4
4-methyl-2-morpholino-phenyl
ethyl


1967
4
4-methyl-2-morpholino-phenyl
n-propyl


1968
4
4-methyl-2-morpholino-phenyl
isopropyl


1969
4
4-methyl-2-morpholino-phenyl
—CH2CH(CH3)2


1970
4
4-methyl-2-morpholino-phenyl
CF3


1971
4
4-methyl-2-morpholino-phenyl
—CH2CF3


1972
4
4-methyl-2-morpholino-phenyl
—CH2CH2CF3


1973
4
4-methyl-2-morpholino-phenyl
cyclopropyl


1974
4
4-methyl-2-morpholino-phenyl
Cyclobutyl


1975
4
4-methyl-2-morpholino-phenyl
cyclopentyl


1976
4
4-methyl-2-morpholino-phenyl
cyclohexyl


1977
4
4-methyl-2-morpholino-phenyl
3-pyridyl


1978
4
4-methyl-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1979
4
4-methyl-2-morpholino-phenyl
1H-imidazol-4-yl


1980
4
4-methyl-2-morpholino-phenyl
2-furanyl


1981
1
naphthylen-1-yl
Ethyl


1982
1
naphthylen-1-yl
n-propyl


1983
1
naphthylen-1-yl
Isopropyl


1984
1
naphthylen-1-yl
—CH2CH(CH3)2


1985
1
naphthylen-1-yl
CF3


1986
1
naphthylen-1-yl
—CH2CF3


1987
1
naphthylen-1-yl
—CH2CH2CF3


1988
1
naphthylen-1-yl
Cyclopropyl


1989
1
naphthylen-1-yl
Cyclobutyl


1990
1
naphthylen-1-yl
Cyclopentyl


1991
1
naphthylen-1-yl
Cyclohexyl


1992
1
naphthylen-1-yl
3-pyridyl


1993
1
naphthylen-1-yl
1-methyl-1H-pyrazol-4-yl


1994
1
naphthylen-1-yl
1H-imidazol-4-yl


1995
1
naphthylen-1-yl
2-furanyl


1996
1
naphthylen-2-yl
Ethyl


1997
1
naphthylen-2-yl
n-propyl


1998
1
naphthylen-2-yl
Isopropyl


1999
1
naphthylen-2-yl
—CH2CH(CH3)2


2000
1
naphthylen-2-yl
CF3


2001
1
naphthylen-2-yl
—CH2CF3


2002
1
naphthylen-2-yl
—CH2CH2CF3


2003
1
naphthylen-2-yl
Cyclopropyl


2004
1
naphthylen-2-yl
Cyclobutyl


2005
1
naphthylen-2-yl
Cyclopentyl


2006
1
naphthylen-2-yl
Cyclohexyl


2007
1
naphthylen-2-yl
3-pyridyl


2008
1
naphthylen-2-yl
1-methyl-1H-pyrazol-4-yl


2009
1
naphthylen-2-yl
1H-imidazol-4-yl


2010
1
naphthylen-2-yl
2-furanyl


2011
2
naphthylen-1-yl
Ethyl


2012
2
naphthylen-1-yl
n-propyl


2013
2
naphthylen-1-yl
Isopropyl


2014
2
naphthylen-1-yl
—CH2CH(CH3)2


2015
2
naphthylen-1-yl
CF3


2016
2
naphthylen-1-yl
—CH2CF3


2017
2
naphthylen-1-yl
—CH2CH2CF3


2018
2
naphthylen-1-yl
Cyclopropyl


2019
2
naphthylen-1-yl
Cyclobutyl


2020
2
naphthylen-1-yl
Cyclopentyl


2021
2
naphthylen-1-yl
Cyclohexyl


2022
2
naphthylen-1-yl
3-pyridyl


2023
2
naphthylen-1-yl
1-methyl-1H-pyrazol-4-yl


2024
2
naphthylen-1-yl
1H-imidazol-4-yl


2025
2
naphthylen-1-yl
2-furanyl


2026
2
naphthylen-2-yl
Ethyl


2027
2
naphthylen-2-yl
n-propyl


2028
2
naphthylen-2-yl
Isopropyl


2029
2
naphthylen-2-yl
—CH2CH(CH3)2


2030
2
naphthylen-2-yl
CF3


2031
2
naphthylen-2-yl
—CH2CF3


2032
2
naphthylen-2-yl
—CH2CH2CF3


2033
2
naphthylen-2-yl
Cyclopropyl


2034
2
naphthylen-2-yl
Cyclobutyl


2035
2
naphthylen-2-yl
Cyclopentyl


2036
2
naphthylen-2-yl
Cyclohexyl


2037
2
naphthylen-2-yl
3-pyridyl


2038
2
naphthylen-2-yl
1-methyl-1H-pyrazol-4-yl


2039
2
naphthylen-2-yl
1H-imidazol-4-yl


2040
2
naphthylen-2-yl
2-furanyl


2041
3
naphthylen-1-yl
Ethyl


2042
3
naphthylen-1-yl
n-propyl


2043
3
naphthylen-1-yl
Isopropyl


2044
3
naphthylen-1-yl
—CH2CH(CH3)2


2045
3
naphthylen-1-yl
CF3


2046
3
naphthylen-1-yl
—CH2CF3


2047
3
naphthylen-1-yl
—CH2CH2CF3


2048
3
naphthylen-1-yl
Cyclopropyl


2049
3
naphthylen-1-yl
Cyclobutyl


2050
3
naphthylen-1-yl
Cyclopentyl


2051
3
naphthylen-1-yl
Cyclohexyl


2052
3
naphthylen-1-yl
3-pyridyl


2053
3
naphthylen-1-yl
1-methyl-1H-pyrazol-4-yl


2054
3
naphthylen-1-yl
1H-imidazol-4-yl


2055
3
naphthylen-1-yl
2-furanyl


2056
3
naphthylen-2-yl
Ethyl


2057
3
naphthylen-2-yl
n-propyl


2058
3
naphthylen-2-yl
Isopropyl


2059
3
naphthylen-2-yl
—CH2CH(CH3)2


2060
3
naphthylen-2-yl
CF3


2061
3
naphthylen-2-yl
—CH2CF3


2062
3
naphthylen-2-yl
—CH2CH2CF3


2063
3
naphthylen-2-yl
Cyclopropyl


2064
3
naphthylen-2-yl
Cyclobutyl


2065
3
naphthylen-2-yl
Cyclopentyl


2066
3
naphthylen-2-yl
Cyclohexyl


2067
3
naphthylen-2-yl
3-pyridyl


2068
3
naphthylen-2-yl
1-methyl-1H-pyrazol-4-yl


2069
3
naphthylen-2-yl
1H-imidazol-4-yl


2070
3
naphthylen-2-yl
2-furanyl


2071
4
naphthylen-1-yl
Ethyl


2072
4
naphthylen-1-yl
n-propyl


2073
4
naphthylen-1-yl
Isopropyl


2074
4
naphthylen-1-yl
—CH2CH(CH3)2


2075
4
naphthylen-1-yl
CF3


2076
4
naphthylen-1-yl
—CH2CF3


2077
4
naphthylen-1-yl
—CH2CH2CF3


2078
4
naphthylen-1-yl
Cyclopropyl


2079
4
naphthylen-1-yl
Cyclobutyl


2080
4
naphthylen-1-yl
Cyclopentyl


2081
4
naphthylen-1-yl
Cyclohexyl


2082
4
naphthylen-1-yl
3-pyridyl


2083
4
naphthylen-1-yl
1-methyl-1H-pyrazol-4-yl


2084
4
naphthylen-1-yl
1H-imidazol-4-yl


2085
4
naphthylen-1-yl
2-furanyl


2086
4
naphthylen-2-yl
Ethyl


2087
4
naphthylen-2-yl
n-propyl


2088
4
naphthylen-2-yl
Isopropyl


2089
4
naphthylen-2-yl
—CH2CH(CH3)2


2090
4
naphthylen-2-yl
CF3


2091
4
naphthylen-2-yl
—CH2CF3


2092
4
naphthylen-2-yl
—CH2CH2CF3


2093
4
naphthylen-2-yl
Cyclopropyl


2094
4
naphthylen-2-yl
Cyclobutyl


2095
4
naphthylen-2-yl
Cyclopentyl


2096
4
naphthylen-2-yl
Cyclohexyl


2097
4
naphthylen-2-yl
3-pyridyl


2098
4
naphthylen-2-yl
1-methyl-1H-pyrazol-4-yl


2099
4
naphthylen-2-yl
1H-imidazol-4-yl


2100
4
naphthylen-2-yl
2-furanyl









Exemplary embodiments include compounds having the formula (XXXX)




embedded image


or a pharmaceutically acceptable salt form thereof defined herein below in Table 33.












TABLE 33





Entry
n
R5
R10C


















1
1
4-CH3-phenyl
Ethyl


2
1
4-CH3-phenyl
n-propyl


3
1
4-CH3-phenyl
Isopropyl


4
1
4-CH3-phenyl
—CH2CH(CH3)2


5
1
4-CH3-phenyl
CF3


6
1
4-CH3-phenyl
—CH2CF3


7
1
4-CH3-phenyl
—CH2CH2CF3


8
1
4-CH3-phenyl
Cyclopropyl


9
1
4-CH3-phenyl
Cyclobutyl


10
1
4-CH3-phenyl
Cyclopentyl


11
1
4-CH3-phenyl
Cyclohexyl


12
1
4-CH3-phenyl
3-pyridyl


13
1
4-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


14
1
4-CH3-phenyl
1H-imidazol-4-yl


15
1
4-CH3-phenyl
2-furanyl


16
1
3-CH3-phenyl
Ethyl


17
1
3-CH3-phenyl
n-propyl


18
1
3-CH3-phenyl
Isopropyl


19
1
3-CH3-phenyl
—CH2CH(CH3)2


20
1
3-CH3-phenyl
CF3


21
1
3-CH3-phenyl
—CH2CF3


22
1
3-CH3-phenyl
—CH2CH2CF3


23
1
3-CH3-phenyl
Cyclopropyl


24
1
3-CH3-phenyl
Cyclobutyl


25
1
3-CH3-phenyl
Cyclopentyl


26
1
3-CH3-phenyl
cyclohexyl


27
1
3-CH3-phenyl
3-pyridyl


28
1
3-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


29
1
3-CH3-phenyl
1H-imidazol-4-yl


30
1
3-CH3-phenyl
2-furanyl


31
1
3-OH-Phenyl
ethyl


32
1
3-OH-Phenyl
n-propyl


33
1
3-OH-Phenyl
isopropyl


34
1
3-OH-Phenyl
—CH2CH(CH3)2


35
1
3-OH-Phenyl
CF3


36
1
3-OH-Phenyl
—CH2CF3


37
1
3-OH-Phenyl
—CH2CH2CF3


38
1
3-OH-Phenyl
cyclopropyl


39
1
3-OH-Phenyl
Cyclobutyl


40
1
3-OH-Phenyl
cyclopentyl


41
1
3-OH-Phenyl
cyclohexyl


42
1
3-OH-Phenyl
3-pyridyl


43
1
3-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


44
1
3-OH-Phenyl
1H-imidazol-4-yl


45
1
3-OH-Phenyl
2-furanyl


46
1
4-OMe-Phenyl
ethyl


47
1
4-OMe-Phenyl
n-propyl


48
1
4-OMe-Phenyl
isopropyl


49
1
4-OMe-Phenyl
—CH2CH(CH3)2


50
1
4-OMe-Phenyl
CF3


51
1
4-OMe-Phenyl
—CH2CF3


52
1
4-OMe-Phenyl
—CH2CH2CF3


53
1
4-OMe-Phenyl
cyclopropyl


54
1
4-OMe-Phenyl
Cyclobutyl


55
1
4-OMe-Phenyl
cyclopentyl


56
1
4-OMe-Phenyl
cyclohexyl


57
1
4-OMe-Phenyl
3-pyridyl


58
1
4-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


59
1
4-OMe-Phenyl
1H-imidazol-4-yl


60
1
4-OMe-Phenyl
2-furanyl


61
1
2-OMe-Phenyl
ethyl


62
1
2-OMe-Phenyl
n-propyl


63
1
2-OMe-Phenyl
isopropyl


64
1
2-OMe-Phenyl
—CH2CH(CH3)2


65
1
2-OMe-Phenyl
CF3


66
1
2-OMe-Phenyl
—CH2CF3


67
1
2-OMe-Phenyl
—CH2CH2CF3


68
1
2-OMe-Phenyl
cyclopropyl


69
1
2-OMe-Phenyl
Cyclobutyl


70
1
2-OMe-Phenyl
cyclopentyl


71
1
2-OMe-Phenyl
cyclohexyl


72
1
2-OMe-Phenyl
3-pyridyl


73
1
2-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


74
1
2-OMe-Phenyl
1H-imidazol-4-yl


75
1
2-OMe-Phenyl
2-furanyl


76
1
3-CN-Phenyl
ethyl


77
1
3-CN-Phenyl
n-propyl


78
1
3-CN-Phenyl
isopropyl


79
1
3-CN-Phenyl
—CH2CH(CH3)2


80
1
3-CN-Phenyl
CF3


81
1
3-CN-Phenyl
—CH2CF3


82
1
3-CN-Phenyl
—CH2CH2CF3


83
1
3-CN-Phenyl
cyclopropyl


84
1
3-CN-Phenyl
Cyclobutyl


85
1
3-CN-Phenyl
cyclopentyl


86
1
3-CN-Phenyl
cyclohexyl


87
1
3-CN-Phenyl
3-pyridyl


88
1
3-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


89
1
3-CN-Phenyl
1H-imidazol-4-yl


90
1
3-CN-Phenyl
2-furanyl


91
1
2-F-Phenyl
ethyl


92
1
2-F-Phenyl
n-propyl


93
1
2-F-Phenyl
isopropyl


94
1
2-F-Phenyl
—CH2CH(CH3)2


95
1
2-F-Phenyl
CF3


96
1
2-F-Phenyl
—CH2CF3


97
1
2-F-Phenyl
—CH2CH2CF3


98
1
2-F-Phenyl
cyclopropyl


99
1
2-F-Phenyl
Cyclobutyl


100
1
2-F-Phenyl
cyclopentyl


101
1
2-F-Phenyl
cyclohexyl


102
1
2-F-Phenyl
3-pyridyl


103
1
2-F-Phenyl
1-methyl-1H-pyrazol-4-yl


104
1
2-F-Phenyl
1H-imidazol-4-yl


105
1
2-F-Phenyl
2-furanyl


106
1
4-F-Phenyl
ethyl


107
1
4-F-Phenyl
n-propyl


108
1
4-F-Phenyl
isopropyl


109
1
4-F-Phenyl
—CH2CH(CH3)2


110
1
4-F-Phenyl
CF3


111
1
4-F-Phenyl
—CH2CF3


112
1
4-F-Phenyl
—CH2CH2CF3


113
1
4-F-Phenyl
cyclopropyl


114
1
4-F-Phenyl
Cyclobutyl


115
1
4-F-Phenyl
cyclopentyl


116
1
4-F-Phenyl
cyclohexyl


117
1
4-F-Phenyl
3-pyridyl


118
1
4-F-Phenyl
1-methyl-1H-pyrazol-4-yl


119
1
4-F-Phenyl
1H-imidazol-4-yl


120
1
4-F-Phenyl
2-furanyl


121
1
3-Cl-Phenyl
ethyl


122
1
3-Cl-Phenyl
n-propyl


123
1
3-Cl-Phenyl
isopropyl


124
1
3-Cl-Phenyl
—CH2CH(CH3)2


125
1
3-Cl-Phenyl
CF3


126
1
3-Cl-Phenyl
—CH2CF3


127
1
3-Cl-Phenyl
—CH2CH2CF3


128
1
3-Cl-Phenyl
cyclopropyl


129
1
3-Cl-Phenyl
Cyclobutyl


130
1
3-Cl-Phenyl
cyclopentyl


131
1
3-Cl-Phenyl
cyclohexyl


132
1
3-Cl-Phenyl
3-pyridyl


133
1
3-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


134
1
3-Cl-Phenyl
1H-imidazol-4-yl


135
1
3-Cl-Phenyl
2-furanyl


136
1
2-Br-Phenyl
ethyl


137
1
2-Br-Phenyl
n-propyl


138
1
2-Br-Phenyl
isopropyl


139
1
2-Br-Phenyl
—CH2CH(CH3)2


140
1
2-Br-Phenyl
CF3


141
1
2-Br-Phenyl
—CH2CF3


142
1
2-Br-Phenyl
—CH2CH2CF3


143
1
2-Br-Phenyl
cyclopropyl


144
1
2-Br-Phenyl
Cyclobutyl


145
1
2-Br-Phenyl
cyclopentyl


146
1
2-Br-Phenyl
cyclohexyl


147
1
2-Br-Phenyl
3-pyridyl


148
1
2-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


149
1
2-Br-Phenyl
1H-imidazol-4-yl


150
1
2-Br-Phenyl
2-furanyl


151
1
4-Br-Phenyl
ethyl


152
1
4-Br-Phenyl
n-propyl


153
1
4-Br-Phenyl
isopropyl


154
1
4-Br-Phenyl
—CH2CH(CH3)2


155
1
4-Br-Phenyl
CF3


156
1
4-Br-Phenyl
—CH2CF3


157
1
4-Br-Phenyl
—CH2CH2CF3


158
1
4-Br-Phenyl
cyclopropyl


159
1
4-Br-Phenyl
Cyclobutyl


160
1
4-Br-Phenyl
cyclopentyl


161
1
4-Br-Phenyl
cyclohexyl


162
1
4-Br-Phenyl
3-pyridyl


163
1
4-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


164
1
4-Br-Phenyl
1H-imidazol-4-yl


165
1
4-Br-Phenyl
2-furanyl


166
1
3-CF3-Phenyl
ethyl


167
1
3-CF3-Phenyl
n-propyl


168
1
3-CF3-Phenyl
isopropyl


169
1
3-CF3-Phenyl
—CH2CH(CH3)2


170
1
3-CF3-Phenyl
CF3


171
1
3-CF3-Phenyl
—CH2CF3


172
1
3-CF3-Phenyl
—CH2CH2CF3


173
1
3-CF3-Phenyl
cyclopropyl


174
1
3-CF3-Phenyl
Cyclobutyl


175
1
3-CF3-Phenyl
cyclopentyl


176
1
3-CF3-Phenyl
cyclohexyl


177
1
3-CF3-Phenyl
3-pyridyl


178
1
3-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


179
1
3-CF3-Phenyl
1H-imidazol-4-yl


180
1
3-CF3-Phenyl
2-furanyl


181
1
2-iPr-Phenyl
ethyl


182
1
2-iPr-Phenyl
n-propyl


183
1
2-iPr-Phenyl
isopropyl


184
1
2-iPr-Phenyl
—CH2CH(CH3)2


185
1
2-iPr-Phenyl
CF3


186
1
2-iPr-Phenyl
—CH2CF3


187
1
2-iPr-Phenyl
—CH2CH2CF3


188
1
2-iPr-Phenyl
cyclopropyl


189
1
2-iPr-Phenyl
Cyclobutyl


190
1
2-iPr-Phenyl
cyclopentyl


191
1
2-iPr-Phenyl
cyclohexyl


192
1
2-iPr-Phenyl
3-pyridyl


193
1
2-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


194
1
2-iPr-Phenyl
1H-imidazol-4-yl


195
1
2-iPr-Phenyl
2-furanyl


196
1
4-iPr-Phenyl
ethyl


197
1
4-iPr-Phenyl
n-propyl


198
1
4-iPr-Phenyl
isopropyl


199
1
4-iPr-Phenyl
—CH2CH(CH3)2


200
1
4-iPr-Phenyl
CF3


201
1
4-iPr-Phenyl
—CH2CF3


202
1
4-iPr-Phenyl
—CH2CH2CF3


203
1
4-iPr-Phenyl
cyclopropyl


204
1
4-iPr-Phenyl
Cyclobutyl


205
1
4-iPr-Phenyl
cyclopentyl


206
1
4-iPr-Phenyl
cyclohexyl


207
1
4-iPr-Phenyl
3-pyridyl


208
1
4-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


209
1
4-iPr-Phenyl
1H-imidazol-4-yl


210
1
4-iPr-Phenyl
2-furanyl


211
1
3-morpholino-phenyl
ethyl


212
1
3-morpholino-phenyl
n-propyl


213
1
3-morpholino-phenyl
isopropyl


214
1
3-morpholino-phenyl
—CH2CH(CH3)2


215
1
3-morpholino-phenyl
CF3


216
1
3-morpholino-phenyl
—CH2CF3


217
1
3-morpholino-phenyl
—CH2CH2CF3


218
1
3-morpholino-phenyl
cyclopropyl


219
1
3-morpholino-phenyl
Cyclobutyl


220
1
3-morpholino-phenyl
cyclopentyl


221
1
3-morpholino-phenyl
cyclohexyl


222
1
3-morpholino-phenyl
3-pyridyl


223
1
3-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


224
1
3-morpholino-phenyl
1H-imidazol-4-yl


225
1
3-morpholino-phenyl
2-furanyl


226
1
4-cyano-2-morpholino-phenyl
ethyl


227
1
4-cyano-2-morpholino-phenyl
n-propyl


228
1
4-cyano-2-morpholino-phenyl
isopropyl


229
1
4-cyano-2-morpholino-phenyl
—CH2CH(CH3)2


230
1
4-cyano-2-morpholino-phenyl
CF3


231
1
4-cyano-2-morpholino-phenyl
—CH2CF3


232
1
4-cyano-2-morpholino-phenyl
—CH2CH2CF3


233
1
4-cyano-2-morpholino-phenyl
cyclopropyl


234
1
4-cyano-2-morpholino-phenyl
Cyclobutyl


235
1
4-cyano-2-morpholino-phenyl
cyclopentyl


236
1
4-cyano-2-morpholino-phenyl
cyclohexyl


237
1
4-cyano-2-morpholino-phenyl
3-pyridyl


238
1
4-cyano-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


239
1
4-cyano-2-morpholino-phenyl
1H-imidazol-4-yl


240
1
4-cyano-2-morpholino-phenyl
2-furanyl


241
1
4-hydroxy-2-morpholino-phenyl
ethyl


242
1
4-hydroxy-2-morpholino-phenyl
n-propyl


243
1
4-hydroxy-2-morpholino-phenyl
isopropyl


244
1
4-hydroxy-2-morpholino-phenyl
—CH2CH(CH3)2


245
1
4-hydroxy-2-morpholino-phenyl
CF3


246
1
4-hydroxy-2-morpholino-phenyl
—CH2CF3


247
1
4-hydroxy-2-morpholino-phenyl
—CH2CH2CF3


248
1
4-hydroxy-2-morpholino-phenyl
cyclopropyl


249
1
4-hydroxy-2-morpholino-phenyl
Cyclobutyl


250
1
4-hydroxy-2-morpholino-phenyl
cyclopentyl


251
1
4-hydroxy-2-morpholino-phenyl
cyclohexyl


252
1
4-hydroxy-2-morpholino-phenyl
3-pyridyl


253
1
4-hydroxy-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


254
1
4-hydroxy-2-morpholino-phenyl
1H-imidazol-4-yl


255
1
4-hydroxy-2-morpholino-phenyl
2-furanyl


256
1
2-CH3-phenyl
Ethyl


257
1
2-CH3-phenyl
n-propyl


258
1
2-CH3-phenyl
Isopropyl


259
1
2-CH3-phenyl
—CH2CH(CH3)2


260
1
2-CH3-phenyl
CF3


261
1
2-CH3-phenyl
—CH2CF3


262
1
2-CH3-phenyl
—CH2CH2CF3


263
1
2-CH3-phenyl
cyclopropyl


264
1
2-CH3-phenyl
Cyclobutyl


265
1
2-CH3-phenyl
cyclopentyl


266
1
2-CH3-phenyl
cyclohexyl


267
1
2-CH3-phenyl
3-pyridyl


268
1
2-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


269
1
2-CH3-phenyl
1H-imidazol-4-yl


270
1
2-CH3-phenyl
2-furanyl


271
1
4-OH-Phenyl
Ethyl


272
1
4-OH-Phenyl
n-propyl


273
1
4-OH-Phenyl
Isopropyl


274
1
4-OH-Phenyl
—CH2CH(CH3)2


275
1
4-OH-Phenyl
CF3


276
1
4-OH-Phenyl
—CH2CF3


277
1
4-OH-Phenyl
—CH2CH2CF3


278
1
4-OH-Phenyl
cyclopropyl


279
1
4-OH-Phenyl
Cyclobutyl


280
1
4-OH-Phenyl
cyclopentyl


281
1
4-OH-Phenyl
cyclohexyl


282
1
4-OH-Phenyl
3-pyridyl


283
1
4-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


284
1
4-OH-Phenyl
1H-imidazol-4-yl


285
1
4-OH-Phenyl
2-furanyl


286
1
2-OH-Phenyl
Ethyl


287
1
2-OH-Phenyl
n-propyl


288
1
2-OH-Phenyl
Isopropyl


289
1
2-OH-Phenyl
—CH2CH(CH3)2


290
1
2-OH-Phenyl
CF3


291
1
2-OH-Phenyl
—CH2CF3


292
1
2-OH-Phenyl
—CH2CH2CF3


293
1
2-OH-Phenyl
cyclopropyl


294
1
2-OH-Phenyl
Cyclobutyl


295
1
2-OH-Phenyl
cyclopentyl


296
1
2-OH-Phenyl
cyclohexyl


297
1
2-OH-Phenyl
3-pyridyl


298
1
2-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


299
1
2-OH-Phenyl
1H-imidazol-4-yl


300
1
2-OH-Phenyl
2-furanyl


301
1
3-OMe-Phenyl
Ethyl


302
1
3-OMe-Phenyl
n-propyl


303
1
3-OMe-Phenyl
Isopropyl


304
1
3-OMe-Phenyl
—CH2CH(CH3)2


305
1
3-OMe-Phenyl
CF3


306
1
3-OMe-Phenyl
—CH2CF3


307
1
3-OMe-Phenyl
—CH2CH2CF3


308
1
3-OMe-Phenyl
cyclopropyl


309
1
3-OMe-Phenyl
Cyclobutyl


310
1
3-OMe-Phenyl
cyclopentyl


311
1
3-OMe-Phenyl
cyclohexyl


312
1
3-OMe-Phenyl
3-pyridyl


313
1
3-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


314
1
3-OMe-Phenyl
1H-imidazol-4-yl


315
1
3-OMe-Phenyl
2-furanyl


316
1
4-CN-Phenyl
Ethyl


317
1
4-CN-Phenyl
n-propyl


318
1
4-CN-Phenyl
Isopropyl


319
1
4-CN-Phenyl
—CH2CH(CH3)2


320
1
4-CN-Phenyl
CF3


321
1
4-CN-Phenyl
—CH2CF3


322
1
4-CN-Phenyl
—CH2CH2CF3


323
1
4-CN-Phenyl
cyclopropyl


324
1
4-CN-Phenyl
Cyclobutyl


325
1
4-CN-Phenyl
cyclopentyl


326
1
4-CN-Phenyl
cyclohexyl


327
1
4-CN-Phenyl
3-pyridyl


328
1
4-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


329
1
4-CN-Phenyl
1H-imidazol-4-yl


330
1
4-CN-Phenyl
2-furanyl


331
1
2-CN-Phenyl
Ethyl


332
1
2-CN-Phenyl
n-propyl


333
1
2-CN-Phenyl
Isopropyl


334
1
2-CN-Phenyl
—CH2CH(CH3)2


335
1
2-CN-Phenyl
CF3


336
1
2-CN-Phenyl
—CH2CF2


337
1
2-CN-Phenyl
—CH2CH2CF2


338
1
2-CN-Phenyl
cyclopropyl


339
1
2-CN-Phenyl
Cyclobutyl


340
1
2-CN-Phenyl
cyclopentyl


341
1
2-CN-Phenyl
cyclohexyl


342
1
2-CN-Phenyl
3-pyridyl


343
1
2-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


344
1
2-CN-Phenyl
1H-imidazol-4-yl


345
1
2-CN-Phenyl
2-furanyl


346
1
3-F-Phenyl
Ethyl


347
1
3-F-Phenyl
n-propyl


348
1
3-F-Phenyl
Isopropyl


349
1
3-F-Phenyl
—CH2CH(CH3)2


350
1
3-F-Phenyl
CF3


351
1
3-F-Phenyl
—CH2CF2


352
1
3-F-Phenyl
—CH2CH2CF2


353
1
3-F-Phenyl
cyclopropyl


354
1
3-F-Phenyl
Cyclobutyl


355
1
3-F-Phenyl
cyclopentyl


356
1
3-F-Phenyl
cyclohexyl


357
1
3-F-Phenyl
3-pyridyl


358
1
3-F-Phenyl
1-methyl-1H-pyrazol-4-yl


359
1
3-F-Phenyl
1H-imidazol-4-yl


360
1
3-F-Phenyl
2-furanyl


361
1
2-Cl-Phenyl
Ethyl


362
1
2-Cl-Phenyl
n-propyl


363
1
2-Cl-Phenyl
Isopropyl


364
1
2-Cl-Phenyl
—CH2CH(CH2)2


365
1
2-Cl-Phenyl
CF3


366
1
2-Cl-Phenyl
—CH2CF3


367
1
2-Cl-Phenyl
—CH2CH2CF3


368
1
2-Cl-Phenyl
cyclopropyl


369
1
2-Cl-Phenyl
Cyclobutyl


370
1
2-Cl-Phenyl
cyclopentyl


371
1
2-Cl-Phenyl
cyclohexyl


372
1
2-Cl-Phenyl
3-pyridyl


373
1
2-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


374
1
2-Cl-Phenyl
1H-imidazol-4-yl


375
1
2-Cl-Phenyl
2-furanyl


376
1
4-Cl-Phenyl
Ethyl


377
1
4-Cl-Phenyl
n-propyl


378
1
4-Cl-Phenyl
Isopropyl


379
1
4-Cl-Phenyl
—CH2CH(CH3)2


380
1
4-Cl-Phenyl
CF3


381
1
4-Cl-Phenyl
—CH2CF3


382
1
4-Cl-Phenyl
—CH2CH2CF33


383
1
4-Cl-Phenyl
cyclopropyl


384
1
4-Cl-Phenyl
Cyclobutyl


385
1
4-Cl-Phenyl
cyclopentyl


386
1
4-Cl-Phenyl
cyclohexyl


387
1
4-Cl-Phenyl
3-pyridyl


388
1
4-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


389
1
4-Cl-Phenyl
1H-imidazol-4-yl


390
1
4-Cl-Phenyl
2-furanyl


391
1
3-Br-Phenyl
Ethyl


392
1
3-Br-Phenyl
n-propyl


393
1
3-Br-Phenyl
Isopropyl


394
1
3-Br-Phenyl
—CH2CH(CH3)2


395
1
3-Br-Phenyl
CF3


396
1
3-Br-Phenyl
—CH2CF3


397
1
3-Br-Phenyl
—CH2CH2CF3


398
1
3-Br-Phenyl
cyclopropyl


399
1
3-Br-Phenyl
Cyclobutyl


400
1
3-Br-Phenyl
cyclopentyl


401
1
3-Br-Phenyl
cyclohexyl


402
1
3-Br-Phenyl
3-pyridyl


403
1
3-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


404
1
3-Br-Phenyl
1H-imidazol-4-yl


405
1
3-BrPhenyl
2-furanyl


406
1
2-CF3-Phenyl
Ethyl


407
1
2-CF3-Phenyl
n-propyl


408
1
2-CF3-Phenyl
Isopropyl


409
1
2-CF3-Phenyl
—CH2CH(CH3)2


410
1
2-CF3-Phenyl
CF3


411
1
2-CF3-Phenyl
—CH2CF3


412
1
2-CF3-Phenyl
—CH2CH2CF3


413
1
2-CF3-Phenyl
cyclopropyl


414
1
2-CF3-Phenyl
Cyclobutyl


415
1
2-CF3-Phenyl
cyclopentyl


416
1
2-CF3-Phenyl
cyclohexyl


417
1
2-CF3-Phenyl
3-pyridyl


418
1
2-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


419
1
2-CF3-Phenyl
1H-imidazol-4-yl


420
1
2-CF3-Phenyl
2-furanyl


421
1
4-CF3-Phenyl
Ethyl


422
1
4-CF3-Phenyl
n-propyl


423
1
4-CF3-Phenyl
Isopropyl


424
1
4-CF3-Phenyl
—CH2CH(CH3)2


425
1
4-CF3-Phenyl
CF3


426
1
4-CF3-Phenyl
—CH2CF3


427
1
4-CF3-Phenyl
—CH2CH2CF3


428
1
4-CF3-Phenyl
cyclopropyl


429
1
4-CF3-Phenyl
Cyclobutyl


430
1
4-CF3-Phenyl
cyclopentyl


431
1
4-CF3-Phenyl
cyclohexyl


432
1
4-CF3-Phenyl
3-pyridyl


433
1
4-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


434
1
4-CF3-Phenyl
1H-imidazol-4-yl


435
1
4-CF3-Phenyl
2-furanyl


436
1
3-iPr-Phenyl
Ethyl


437
1
3-iPr-Phenyl
n-propyl


438
1
3-iPr-Phenyl
Isopropyl


439
1
3-iPr-Phenyl
—CH2CH(CH3)2


440
1
3-iPr-Phenyl
CF3


441
1
3-iPr-Phenyl
—CH2CF3


442
1
3-iPr-Phenyl
—CH2CH2CF3


443
1
3-iPr-Phenyl
cyclopropyl


444
1
3-iPr-Phenyl
Cyclobutyl


445
1
3-iPr-Phenyl
cyclopentyl


446
1
3-iPr-Phenyl
cyclohexyl


447
1
3-iPr-Phenyl
3-pyridyl


448
1
3-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


449
1
3-iPr-Phenyl
1H-imidazol-4-yl


450
1
3-iPr-Phenyl
2-furanyl


451
1
2-morpholino-phenyl
Ethyl


452
1
2-morpholino-phenyl
n-propyl


453
1
2-morpholino-phenyl
isopropyl


454
1
2-morpholino-phenyl
—CH2CH(CH3)2


455
1
2-morpholino-phenyl
CF3


456
1
2-morpholino-phenyl
—CH2CF3


457
1
2-morpholino-phenyl
—CH2CH2CF3


458
1
2-morpholino-phenyl
cyclopropyl


459
1
2-morpholino-phenyl
Cyclobutyl


460
1
2-morpholino-phenyl
cyclopentyl


461
1
2-morpholino-phenyl
cyclohexyl


462
1
2-morpholino-phenyl
3-pyridyl


463
1
2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


464
1
2-morpholino-phenyl
1H-imidazol-4-yl


465
1
2-morpholino-phenyl
2-furanyl


466
1
4-morpholino-phenyl
ethyl


467
1
4-morpholino-phenyl
n-propyl


468
1
4-morpholino-phenyl
isopropyl


469
1
4-morpholino-phenyl
—CH2CH(CH3)2


470
1
4-morpholino-phenyl
CF3


471
1
4-morpholino-phenyl
—CH2CF3


472
1
4-morpholino-phenyl
—CH2CH2CF3


473
1
4-morpholino-phenyl
cyclopropyl


474
1
4-morpholino-phenyl
Cyclobutyl


475
1
4-morpholino-phenyl
cyclopentyl


476
1
4-morpholino-phenyl
cyclohexyl


477
1
4-morpholino-phenyl
3-pyridyl


478
1
4-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


479
1
4-morpholino-phenyl
1H-imidazol-4-yl


480
1
4-morpholino-phenyl
2-furanyl


481
1
4-methyl-2-morpholino-phenyl
ethyl


482
1
4-methyl-2-morpholino-phenyl
n-propyl


483
1
4-methyl-2-morpholino-phenyl
isopropyl


484
1
4-methyl-2-morpholino-phenyl
—CH2CH(CH3)2


485
1
4-methyl-2-morpholino-phenyl
CF3


486
1
4-methyl-2-morpholino-phenyl
—CH2CF3


487
1
4-methyl-2-morpholino-phenyl
—CH2CH2CF3


488
1
4-methyl-2-morpholino-phenyl
cyclopropyl


489
1
4-methyl-2-morpholino-phenyl
Cyclobutyl


490
1
4-methyl-2-morpholino-phenyl
cyclopentyl


491
1
4-methyl-2-morpholino-phenyl
cyclohexyl


492
1
4-methyl-2-morpholino-phenyl
3-pyridyl


493
1
4-methyl-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


494
1
4-methyl-2-morpholino-phenyl
1H-imidazol-4-yl


495
1
4-methyl-2-morpholino-phenyl
2-furanyl


496
2
4-CH3-phenyl
ethyl


497
2
4-CH3-phenyl
n-propyl


498
2
4-CH3-phenyl
isopropyl


499
2
4-CH3-phenyl
—CH2CH(CH3)2


500
2
4-CH3-phenyl
CF3


501
2
4-CH3-phenyl
—CH2CF3


502
2
4-CH3-phenyl
—CH2CH2CF3


503
2
4-CH3-phenyl
cyclopropyl


504
2
4-CH3-phenyl
Cyclobutyl


505
2
4-CH3-phenyl
cyclopentyl


506
2
4-CH3-phenyl
cyclohexyl


507
2
4-CH3-phenyl
3-pyridyl


508
2
4-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


509
2
4-CH3-phenyl
1H-imidazol-4-yl


510
2
4-CH3-phenyl
2-furanyl


511
2
3-CH3-phenyl
ethyl


512
2
3-CH3-phenyl
n-propyl


513
2
3-CH3-phenyl
isopropyl


514
2
3-CH3-phenyl
—CH2CH(CH3)2


515
2
3-CH3-phenyl
CF3


516
2
3-CH3-phenyl
—CH2CF3


517
2
3-CH3-phenyl
—CH2CH2CF3


518
2
3-CH3-phenyl
cyclopropyl


519
2
3-CH3-phenyl
Cyclobutyl


520
2
3-CH3-phenyl
cyclopentyl


521
2
3-CH3-phenyl
cyclohexyl


522
2
3-CH3-phenyl
3-pyridyl


523
2
3-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


524
2
3-CH3-phenyl
1H-imidazol-4-yl


525
2
3-CH3-phenyl
2-furanyl


526
2
3-OH-Phenyl
ethyl


527
2
3-OH-Phenyl
n-propyl


528
2
3-OH-Phenyl
isopropyl


529
2
3-OH-Phenyl
—CH2CH(CH3)2


530
2
3-OH-Phenyl
CF3


531
2
3-OH-Phenyl
—CH2CF3


532
2
3-OH-Phenyl
—CH2CH2CF3


533
2
3-OH-Phenyl
cyclopropyl


534
2
3-OH-Phenyl
Cyclobutyl


535
2
3-OH-Phenyl
cyclopentyl


536
2
3-OH-Phenyl
cyclohexyl


537
2
3-OH-Phenyl
3-pyridyl


538
2
3-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


539
2
3-OH-Phenyl
1H-imidazol-4-yl


540
2
3-OH-Phenyl
2-furanyl


541
2
4-OMe-Phenyl
ethyl


542
2
4-OMe-Phenyl
n-propyl


543
2
4-OMe-Phenyl
isopropyl


544
2
4-OMe-Phenyl
—CH2CH(CH3)2


545
2
4-OMe-Phenyl
CF3


546
2
4-OMe-Phenyl
—CH2CF3


547
2
4-OMe-Phenyl
—CH2CH2CF3


548
2
4-OMe-Phenvl
cyclopropyl


549
2
4-OMe-Phenyl
Cyclobutyl


550
2
4-OMe-Phenyl
cyclopentyl


551
2
4-OMe-Phenyl
cyclohexyl


552
2
4-OMe-Phenyl
3-pyridyl


553
2
4-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


554
2
4-OMe-Phenyl
1H-imidazol-4-yl


555
2
4-OMe-Phenyl
2-furanyl


556
2
2-OMe-Phenyl
ethyl


557
2
2-OMe-Phenyl
n-propyl


558
2
2-OMe-Phenyl
isopropyl


559
2
2-OMe-Phenyl
—CH2CH(CH3)2


560
2
2-OMe-Phenyl
CF3


561
2
2-OMe-Phenyl
—CH2CF3


562
2
2-OMe-Phenyl
—CH2CH2CF3


563
2
2-OMe-Phenyl
cyclopropyl


564
2
2-OMe-Phenyl
Cyclobutyl


565
2
2-OMe-Phenyl
cyclopentyl


566
2
2-OMe-Phenyl
cyclohexyl


567
2
2-OMe-Phenyl
3-pyridyl


568
2
2-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


569
2
2-OMe-Phenyl
1H-imidazol-4-yl


570
2
2-OMe-Phenyl
2-furanyl


571
2
3-CN-Phenyl
ethyl


572
2
3-CN-Phenyl
n-propyl


573
2
3-CN-Phenyl
isopropyl


574
2
3-CN-Phenyl
—CH2CH(CH3)2


575
2
3-CN-Phenyl
CF3


576
2
3-CN-Phenyl
—CH2CF3


577
2
3-CN-Phenyl
—CH2CH2CF3


578
2
3-CN-Phenyl
cyclopropyl


579
2
3-CN-Phenyl
Cyclobutyl


580
2
3-CN-Phenyl
cyclopentyl


581
2
3-CN-Phenyl
cyclohexyl


582
2
3-CN-Phenyl
3-pyridyl


583
2
3-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


584
2
3-CN-Phenyl
1H-imidazol-4-yl


585
2
3-CN-Phenyl
2-furanyl


586
2
2-F-Phenyl
ethyl


587
2
2-F-Phenyl
n-propyl


588
2
2-F-Phenyl
isopropyl


589
2
2-F-Phenyl
—CH2CH(CH3)2


590
2
2-F-Phenyl
CF3


591
2
2-F-Phenyl
—CH2CF3


592
2
2-F-Phenyl
—CH2CH2CF3


593
2
2-F-Phenyl
cyclopropyl


594
2
2-F-Phenyl
Cyclobutyl


595
2
2-F-Phenyl
cyclopentyl


596
2
2-F-Phenyl
cyclohexyl


597
2
2-F-Phenyl
3-pyridyl


598
2
2-F-Phenyl
1-methyl-1H-pyrazol-4-yl


599
2
2-F-Phenyl
1H-imidazol-4-yl


600
2
2-F-Phenyl
2-furanyl


601
2
4-F-Phenyl
ethyl


602
2
4-F-Phenyl
n-propyl


603
2
4-F-Phenyl
isopropyl


604
2
4-F-Phenyl
—CH2CH(CH3)2


605
2
4-F-Phenyl
CF3


606
2
4-F-Phenyl
—CH2CF3


607
2
4-F-Phenyl
—CH2CH2CF3


608
2
4-F-Phenyl
cyclopropyl


609
2
4-F-Phenyl
Cyclobutyl


610
2
4-F-Phenyl
cyclopentyl


611
2
4-F-Phenyl
cyclohexyl


612
2
4-F-Phenyl
3-pyridyl


613
2
4-F-Phenyl
1-methyl-1H-pyrazol-4-yl


614
2
4-F-Phenyl
1H-imidazol-4-yl


615
2
4-F-Phenyl
2-furanyl


616
2
3-Cl-Phenyl
ethyl


617
2
3-Cl-Phenyl
n-propyl


618
2
3-Cl-Phenyl
isopropyl


619
2
3-Cl-Phenyl
—CH2CH(CH3)2


620
2
3-Cl-Phenyl
CF3


621
2
3-Cl-Phenyl
—CH2CF3


622
2
3-Cl-Phenyl
—CH2CH2CF3


623
2
3-Cl-Phenyl
cyclopropyl


624
2
3-Cl-Phenyl
Cyclobutyl


625
2
3-Cl-Phenyl
cyclopentyl


626
2
3-Cl-Phenyl
cyclohexyl


627
2
3-Cl-Phenyl
3-pyridyl


628
2
3-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


629
2
3-Cl-Phenyl
1H-imidazol-4-yl


630
2
3-Cl-Phenyl
2-furanyl


631
2
2-Br-Phenyl
ethyl


632
2
2-Br-Phenyl
n-propyl


633
2
2-Br-Phenyl
isopropyl


634
2
2-Br-Phenyl
—CH2CH(CH3)2


635
2
2-Br-Phenyl
CF3


636
2
2-Br-Phenyl
—CH2CF3


637
2
2-Br-Phenyl
—CH2CH2CF3


638
2
2-Br-Phenyl
cyclopropyl


639
2
2-Br-Phenyl
Cyclobutyl


640
2
2-Br-Phenyl
cyclopentyl


641
2
2-Br-Phenyl
cyclohexyl


642
2
2-Br-Phenyl
3-pyridyl


643
2
2-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


644
2
2-Br-Phenyl
1H-imidazol-4-yl


645
2
2-Br-Phenyl
2-furanyl


646
2
4-Br-Phenyl
ethyl


647
2
4-Br-Phenyl
n-propyl


648
2
4-Br-Phenyl
isopropyl


649
2
4-Br-Phenyl
—CH2CH(CH3)2


650
2
4-Br-Phenyl
CF3


651
2
4-Br-Phenyl
—CH2CF3


652
2
4-Br-Phenyl
—CH2CH2CF3


653
2
4-Br-Phenyl
cyclopropyl


654
2
4-Br-Phenyl
Cyclobutyl


655
2
4-Br-Phenyl
cyclopentyl


656
2
4-Br-Phenyl
cyclohexyl


657
2
4-Br-Phenyl
3-pyridyl


658
2
4-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


659
2
4-Br-Phenyl
1H-imidazol-4-yl


660
2
4-Br-Phenyl
2-furanyl


661
2
3-CF3-Phenyl
ethyl


662
2
3-CF3-Phenyl
n-propyl


663
2
3-CF3-Phenyl
isopropyl


664
2
3-CF3-Phenyl
—CH2CH(CH3)2


665
2
3-CF3-Phenyl
CF3


666
2
3-CF3-Phenyl
—CH2CF3


667
2
3-CF3-Phenyl
—CH2CH2CF3


668
2
3-CF3-Phenyl
cyclopropyl


669
2
3-CF3-Phenyl
Cyclobutyl


670
2
3-CF3-Phenyl
cyclopentyl


671
2
3-CF3-Phenyl
cyclohexyl


672
2
3-CF3-Phenyl
3-pyridyl


673
2
3-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


674
2
3-CF3-Phenyl
1H-imidazol-4-yl


675
2
3-CF3-Phenyl
2-furanyl


676
2
2-iPr-Phenyl
ethyl


677
2
2-iPr-Phenyl
n-propyl


678
2
2-iPr-Phenyl
isopropyl


679
2
2-iPr-Phenyl
—CH2CH(CH3)2


680
2
2-iPr-Phenyl
CF3


681
2
2-iPr-Phenyl
—CH2CF3


682
2
2-iPr-Phenyl
—CH2CH2CF3


683
2
2-iPr-Phenyl
cyclopropyl


684
2
2-iPr-Phenyl
Cyclobutyl


685
2
2-iPr-Phenyl
cyclopentyl


686
2
2-iPr-Phenyl
cyclohexyl


687
2
2-iPr-Phenyl
3-pyridyl


688
2
2-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


689
2
2-iPr-Phenyl
1H-imidazol-4-yl


690
2
2-iPr-Phenyl
2-furanyl


691
2
4-iPr-Phenyl
ethyl


692
2
4-iPr-Phenyl
n-propyl


693
2
4-iPr-Phenyl
isopropyl


694
2
4-iPr-Phenyl
—CH2CH(CH3)2


695
2
4-iPr-Phenyl
CF3


696
2
4-iPr-Phenyl
—CH2CF3


697
2
4-iPr-Phenyl
—CH2CH2CF3


698
2
4-iPr-Phenyl
cyclopropyl


699
2
4-iPr-Phenyl
Cyclobutyl


700
2
4-iPr-Phenyl
cyclopentyl


701
2
4-iPr-Phenyl
cyclohexyl


702
2
4-iPr-Phenyl
3-pyridyl


703
2
4-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


704
2
4-iPr-Phenyl
1H-imidazol-4-yl


705
2
4-iPr-Phenyl
2-furanyl


706
2
3-morpholino-phenyl
ethyl


707
2
3-morpholino-phenyl
n-propyl


708
2
3-morpholino-phenyl
isopropyl


709
2
3-morpholino-phenyl
—CH2CH(CH3)2


710
2
3-morpholino-phenyl
CF3


711
2
3-morpholino-phenyl
—CH2CF3


712
2
3-morpholino-phenyl
—CH2CH2CF3


713
2
3-morpholino-phenyl
cyclopropyl


714
2
3-morpholino-phenyl
Cyclobutyl


715
2
3-morpholino-phenyl
cyclopentyl


716
2
3-morpholino-phenyl
cyclohexyl


717
2
3-morpholino-phenyl
3-pyridyl


718
2
3-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


719
2
3-morpholino-phenyl
1H-imidazol-4-yl


720
2
3-morpholino-phenyl
2-furanyl


721
2
4-cyano-2-morpholino-phenyl
ethyl


722
2
4-cyano-2-morpholino-phenyl
n-propyl


723
2
4-cyano-2-morpholino-phenyl
isopropyl


724
2
4-cyano-2-morpholino-phenyl
—CH2CH(CH3)2


725
2
4-cyano-2-morpholino-phenyl
CF3


726
2
4-cyano-2-morpholino-phenyl
—CH2CF3


727
2
4-cyano-2-morpholino-phenyl
—CH2CH2CF3


728
2
4-cyano-2-morpholino-phenyl
cyclopropyl


729
2
4-cyano-2-morpholino-phenyl
Cyclobutyl


730
2
4-cyano-2-morpholino-phenyl
cyclopentyl


731
2
4-cyano-2-morpholino-phenyl
cyclohexyl


732
2
4-cyano-2-morpholino-phenyl
3-pyridyl


733
2
4-cyano-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


734
2
4-cyano-2-morpholino-phenyl
1H-imidazol-4-yl


735
2
4-cyano-2-morpholino-phenyl
2-furanyl


736
2
4-hydroxy-2-morpholino-phenyl
ethyl


737
2
4-hydroxy-2-morpholino-phenyl
n-propyl


738
2
4-hydroxy-2-morpholino-phenyl
isopropyl


739
2
4-hydroxy-2-morpholino-phenyl
—CH2CH(CH3)2


740
2
4-hydroxy-2-morpholino-phenyl
CF3


741
2
4-hydroxy-2-morpholino-phenyl
—CH2CF3


742
2
4-hydroxy-2-morpholino-phenyl
—CH2CH2CF3


743
2
4-hydroxy-2-morpholino-phenyl
cyclopropyl


744
2
4-hydroxy-2-morpholino-phenyl
Cyclobutyl


745
2
4-hydroxy-2-morpholino-phenyl
cyclopentyl


746
2
4-hydroxy-2-morpholino-phenyl
cyclohexyl


747
2
4-hydroxy-2-morpholino-phenyl
3-pyridyl


748
2
4-hydroxy-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


749
2
4-hydroxy-2-morpholino-phenyl
1H-imidazol-4-yl


750
2
4-hydroxy-2-morpholino-phenyl
2-furanyl


751
2
2-CH3-phenyl
Ethyl


752
2
2-CH3-phenyl
n-propyl


753
2
2-CH3-phenyl
Isopropyl


754
2
2-CH3-phenyl
—CH2CH(CH3)2


755
2
2-CH3-phenyl
CF3


756
2
2-CH3-phenyl
—CH2CF3


757
2
2-CH3-phenyl
—CH2CH2CF3


758
2
2-CH3-phenyl
cyclopropyl


759
2
2-CH3-phenyl
Cyclobutyl


760
2
2-CH3-phenyl
cyclopentyl


761
2
2-CH3-phenyl
cyclohexyl


762
2
2-CH3-phenyl
3-pyridyl


763
2
2-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


764
2
2-CH3-phenyl
1H-imidazol-4-yl


765
2
2-CH3-phenyl
2-furanyl


766
2
4-OH-Phenyl
Ethyl


767
2
4-OH-Phenyl
n-propyl


768
2
4-OH-Phenyl
Isopropyl


769
2
4-OH-Phenyl
—CH2CH(CH3)2


770
2
4-OH-Phenyl
CF3


771
2
4-OH-Phenyl
—CH2CF3


772
2
4-OH-Phenyl
—CH2CH2CF3


773
2
4-OH-Phenyl
cyclopropyl


774
2
4-OH-Phenyl
Cyclobutyl


775
2
4-OH-Phenyl
cyclopentyl


776
2
4-OH-Phenyl
cyclohexyl


777
2
4-OH-Phenyl
3-pyridyl


778
2
4-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


779
2
4-OH-Phenyl
1H-imidazol-4-yl


780
2
4-OH-Phenyl
2-furanyl


781
2
2-OH-Phenyl
Ethyl


782
2
2-OH-Phenyl
n-propyl


783
2
2-OH-Phenyl
Isopropyl


784
2
2-OH-Phenyl
—CH2CH(CH3)2


785
2
2-OH-Phenyl
CF3


786
2
2-OH-Phenyl
—CH2CF3


787
2
2-OH-Phenyl
—CH2CH2CF3


788
2
2-OH-Phenyl
cyclopropyl


789
2
2-OH-Phenyl
Cyclobutyl


790
2
2-OH-Phenyl
cyclopentyl


791
2
2-OH-Phenyl
cyclohexyl


792
2
2-OH-Phenyl
3-pyridyl


793
2
2-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


794
2
2-OH-Phenyl
1H-imidazol-4-yl


795
2
2-OH-Phenyl
2-furanyl


796
2
3-OMe-Phenyl
Ethyl


797
2
3-OMe-Phenyl
n-propyl


798
2
3-OMe-Phenyl
Isopropyl


799
2
3-OMe-Phenyl
—CH2CH(CH3)2


800
2
3-OMe-Phenyl
CF3


801
2
3-OMe-Phenyl
—CH2CF3


802
2
3-OMe-Phenyl
—CH2CH2CF3


803
2
3-OMe-Phenyl
cyclopropyl


804
2
3-OMe-Phenyl
Cyclobutyl


805
2
3-OMe-Phenyl
cyclopentyl


806
2
3-OMe-Phenyl
cyclohexyl


807
2
3-OMe-Phenyl
3-pyridyl


808
2
3-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


809
2
3-OMe-Phenyl
1H-imidazol-4-yl


810
2
3-OMe-Phenyl
2-furanyl


811
2
4-CN-Phenyl
Ethyl


812
2
4-CN-Phenyl
n-propyl


813
2
4-CN-Phenyl
Isopropyl


814
2
4-CN-Phenyl
—CH2CH(CH3)2


815
2
4-CN-Phenyl
CF3


816
2
4-CN-Phenyl
—CH2CF3


817
2
4-CN-Phenyl
—CH2CH2CF3


818
2
4-CN-Phenyl
cyclopropyl


819
2
4-CN-Phenyl
Cyclobutyl


820
2
4-CN-Phenyl
cyclopentyl


821
2
4-CN-Phenyl
cyclohexyl


822
2
4-CN-Phenyl
3-pyridyl


823
2
4-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


824
2
4-CN-Phenyl
1H-imidazol-4-yl


825
2
4-CN-Phenyl
2-furanyl


826
2
2-CN-Phenyl
Ethyl


827
2
2-CN-Phenyl
n-propyl


828
2
2-CN-Phenyl
Isopropyl


829
2
2-CN-Phenyl
—CH2CH(CH3)2


830
2
2-CN-Phenyl
CF3


831
2
2-CN-Phenyl
—CH2CF3


832
2
2-CN-Phenyl
—CH2CH2CF3


833
2
2-CN-Phenyl
cyclopropyl


834
2
2-CN-Phenyl
Cyclobutyl


835
2
2-CN-Phenyl
cyclopentyl


836
2
2-CN-Phenyl
cyclohexyl


837
2
2-CN-Phenyl
3-pyridyl


838
2
2-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


839
2
2-CN-Phenyl
1H-imidazol-4-yl


840
2
2-CN-Phenyl
2-furanyl


841
2
3-F-Phenyl
Ethyl


842
2
3-F-Phenyl
n-propyl


843
2
3-F-Phenyl
Isopropyl


844
2
3-F-Phenyl
—CH2CH(CH3)2


845
2
3-F-Phenyl
CF3


846
2
3-F-Phenyl
—CH2CF3


847
2
3-F-Phenyl
—CH2CH2CF3


848
2
3-F-Phenyl
cyclopropyl


849
2
3-F-Phenyl
Cyclobutyl


850
2
3-F-Phenyl
cyclopentyl


851
2
3-F-Phenyl
cvclohexyl


852
2
3-F-Phenyl
3-pyridyl


853
2
3-F-Phenyl
1-methyl-1H-pyrazol-4-yl


854
2
3-F-Phenyl
1H-imidazol-4-yl


855
2
3-F-Phenyl
2-furanyl


856
2
2-Cl-Phenyl
Ethyl


857
2
2-Cl-Phenyl
n-propyl


858
2
2-Cl-Phenyl
Isopropyl


859
2
2-Cl-Phenyl
—CH2CH(CH3)2


860
2
2-Cl-Phenyl
CF3


861
2
2-Cl-Phenyl
—CH2CF3


862
2
2-Cl-Phenyl
—CH2CH2CF3


863
2
2-Cl-Phenyl
cyclopropyl


864
2
2-Cl-Phenyl
Cyclobutyl


865
2
2-Cl-Phenyl
cyclopentyl


866
2
2-Cl-Phenyl
cyclohexyl


867
2
2-Cl-Phenyl
3-pyridyl


868
2
2-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


869
2
2-Cl-Phenyl
1H-imidazol-4-yl


870
2
2-Cl-Phenyl
2-furanyl


871
2
4-Cl-Phenyl
Ethyl


872
2
4-Cl-Phenyl
n-propyl


873
2
4-Cl-Phenyl
Isopropyl


874
2
4-Cl-Phenyl
—CH2CH(CH3)2


875
2
4-Cl-Phenyl
CF3


876
2
4-Cl-Phenyl
—CH2CF3


877
2
4-Cl-Phenyl
—CH2CH2CF3


878
2
4-Cl-Phenyl
cyclopropyl


879
2
4-Cl-Phenyl
Cyclobutyl


880
2
4-Cl-Phenyl
cyclopentyl


881
2
4-Cl-Phenyl
cyclohexyl


882
2
4-Cl-Phenyl
3-pyridyl


883
2
4-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


884
2
4-Cl-Phenyl
1H-imidazol-4-yl


885
2
4-Cl-Phenyl
2-furanyl


886
2
3-Br-Phenyl
Ethyl


887
2
3-Br-Phenyl
n-propyl


888
2
3-Br-Phenyl
Isopropyl


889
2
3-Br-Phenyl
—CH2CH(CH3)2


890
2
3-Br-Phenyl
CF3


891
2
3-Br-Phenyl
—CH2CF3


892
2
3-Br-Phenyl
—CH2CH2CF3


893
2
3-Br-Phenyl
cyclopropyl


894
2
3-Br-Phenyl
Cyclobutyl


895
2
3-Br-Phenyl
cyclopentyl


896
2
3-Br-Phenyl
cyclohexyl


897
2
3-Br-Phenyl
3-pyridyl


898
2
3-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


899
2
3-Br-Phenyl
1H-imidazol-4-yl


900
2
3-Br-Phenyl
2-furanyl


901
2
2-CF3-Phenyl
Ethyl


902
2
2-CF3-Phenyl
n-propyl


903
2
2-CF3-Phenyl
Isopropyl


904
2
2-CF3-Phenyl
—CH2CH(CH3)2


905
2
2-CF3-Phenyl
CF3


906
2
2-CF3-Phenyl
—CH2CF3


907
2
2-CF3-Phenyl
—CH2CH2CF3


908
2
2-CF3-Phenyl
cyclopropyl


909
2
2-CF3-Phenyl
Cyclobutyl


910
2
2-CF3-Phenyl
cyclopentyl


911
2
2-CF3-Phenyl
cyclohexyl


912
2
2-CF3-Phenyl
3-pyridyl


913
2
2-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


914
2
2-CF3-Phenyl
1H-imidazol-4-yl


915
2
2-CF3-Phenyl
2-furanyl


916
2
4-CF3-Phenyl
Ethyl


917
2
4-CF3-Phenyl
n-propyl


918
2
4-CF3-Phenyl
Isopropyl


919
2
4-CF3-Phenyl
—CH2CH(CH3)2


920
2
4-CF3-Phenyl
CF3


921
2
4-CF3-Phenyl
—CH2CF3


922
2
4-CF3-Phenyl
—CH2CH2CF3


923
2
4-CF3-Phenyl
cyclopropyl


924
2
4-CF3-Phenyl
Cyclobutyl


925
2
4-CF3-Phenyl
cyclopentyl


926
2
4-CF3-Phenyl
cyclohexyl


927
2
4-CF3-Phenyl
3-pyridyl


928
2
4-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


929
2
4-CF3-Phenyl
1H-imidazol-4-yl


930
2
4-CF3-Phenyl
2-furanyl


931
2
3-iPr-Phenyl
Ethyl


932
2
3-iPr-Phenyl
n-propyl


933
2
3-iPr-Phenyl
Isopropyl


934
2
3-iPr-Phenyl
—CH2CH(CH3)2


935
2
3-iPr-Phenyl
CF3


936
2
3-iPr-Phenyl
—CH2CF3


937
2
3-iPr-Phenyl
—CH2CH2CF3


938
2
3-iPr-Phenyl
cyclopropyl


939
2
3-iPr-Phenyl
Cyclobutyl


940
2
3-iPr-Phenyl
cyclopentyl


941
2
3-iPr-Phenyl
cyclohexyl


942
2
3-iPr-Phenyl
3-pyridyl


943
2
3-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


944
2
3-iPr-Phenyl
1H-imidazol-4-yl


945
2
3-iPr-Phenyl
2-furanyl


946
2
2-morpholino-phenyl
Ethyl


947
2
2-morpholino-phenyl
n-propyl


948
2
2-morpholino-phenyl
isopropyl


949
2
2-morpholino-phenyl
—CH2CH(CH3)2


950
2
2-morpholino-phenyl
CF3


951
2
2-morpholino-phenyl
—CH2CF3


952
2
2-morpholino-phenyl
—CH2CH2CF3


953
2
2-morpholino-phenyl
cyclopropyl


954
2
2-morpholino-phenyl
Cyclobutyl


955
2
2-morpholino-phenyl
cyclopentyl


956
2
2-morpholino-phenyl
cyclohexyl


957
2
2-morpholino-phenyl
3-pyridyl


958
2
2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


959
2
2-morpholino-phenyl
1H-imidazol-4-yl


960
2
2-morpholino-phenyl
2-furanyl


961
2
4-morpholino-phenyl
ethyl


962
2
4-morpholino-phenyl
n-propyl


963
2
4-morpholino-phenyl
isopropyl


964
2
4-morpholino-phenyl
—CH2CH(CH3)2


965
2
4-morpholino-phenyl
CF3


966
2
4-morpholino-phenyl
—CH2CF3


967
2
4-morpholino-phenyl
—CH2CH2CF3


968
2
4-morpholino-phenyl
cyclopropyl


969
2
4-morpholino-phenyl
Cyclobutyl


970
2
4-morpholino-phenyl
cyclopentyl


971
2
4-morpholino-phenyl
cyclohexyl


972
2
4-morpholino-phenyl
3-pyridyl


973
2
4-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


974
2
4-morpholino-phenyl
1H-imidazol-4-yl


975
2
4-morpholino-phenyl
2-furanyl


976
2
4-methyl-2-morpholino-phenyl
ethyl


977
2
4-methyl-2-morpholino-phenyl
n-propyl


978
2
4-methyl-2-morpholino-phenyl
isopropyl


979
2
4-methyl-2-morpholino-phenyl
—CH2CH(CH3)2


980
2
4-methyl-2-morpholino-phenyl
CF3


981
2
4-methyl-2-morpholino-phenyl
—CH2CF3


982
2
4-methyl-2-morpholino-phenyl
—CH2CH2CF3


983
2
4-methyl-2-morpholino-phenyl
cyclopropyl


984
2
4-methyl-2-morpholino-phenyl
Cyclobutyl


985
2
4-methyl-2-morpholino-phenyl
cyclopentyl


986
2
4-methyl-2-morpholino-phenyl
cyclohexyl


987
2
4-methyl-2-morpholino-phenyl
3-pyridyl


988
2
4-methyl-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


989
2
4-methyl-2-morpholino-phenyl
1H-imidazol-4-yl


990
2
4-methyl-2-morpholino-phenyl
2-furanyl


991
3
4-CH3-phenyl
ethyl


992
3
4-CH3-phenyl
n-propyl


993
3
4-CH3-phenyl
isopropyl


994
3
4-CH3-phenyl
—CH2CH(CH3)2


995
3
4-CH3-phenyl
CF3


996
3
4-CH3-phenyl
—CH2CF3


997
3
4-CH3-phenyl
—CH2CH2CF3


998
3
4-CH3-phenyl
cyclopropyl


999
3
4-CH3-phenyl
Cyclobutyl


1000
3
4-CH3-phenyl
cyclopentyl


1001
3
4-CH3-phenyl
cyclohexyl


1002
3
4-CH3-phenyl
3-pyridyl


1003
3
4-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


1004
3
4-CH3-phenyl
1H-imidazol-4-yl


1005
3
4-CH3-phenyl
2-furanyl


1006
3
3-CH3-phenyl
ethyl


1007
3
3-CH3-phenyl
n-propyl


1008
3
3-CH3-phenyl
isopropyl


1009
3
3-CH3-phenyl
—CH2CH(CH3)2


1010
3
3-CH3-phenyl
CF3


1011
3
3-CH3-phenyl
—CH2CF3


1012
3
3-CH3-phenyl
—CH2CH2CF3


1013
3
3-CH3-phenyl
cyclopropyl


1014
3
3-CH3-phenyl
Cyclobutyl


1015
3
3-CH3-phenyl
cyclopentyl


1016
3
3-CH3-phenyl
cyclohexyl


1017
3
3-CH3-phenyl
3-pyridyl


1018
3
3-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


1019
3
3-CH3-phenyl
1H-imidazol-4-yl


1020
3
3-CH3-phenyl
2-furanyl


1021
3
3-OH-Phenyl
ethyl


1022
3
3-OH-Phenyl
n-propyl


1023
3
3-OH-Phenyl
isopropyl


1024
3
3-OH-Phenyl
—CH2CH(CH3)2


1025
3
3-OH-Phenyl
CF3


1026
3
3-OH-Phenyl
—CH2CF3


1027
3
3-OH-Phenyl
—CH2CH2CF3


1028
3
3-OH-Phenyl
cyclopropyl


1029
3
3-OH-Phenyl
Cyclobutyl


1030
3
3-OH-Phenyl
cyclopentyl


1031
3
3-OH-Phenyl
cyclohexyl


1032
3
3-OH-Phenyl
3-pyridyl


1033
3
3-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


1034
3
3-OH-Phenyl
1H-imidazol-4-yl


1035
3
3-OH-Phenyl
2-furanyl


1036
3
4-OMe-Phenyl
ethyl


1037
3
4-OMe-Phenyl
n-propyl


1038
3
4-OMe-Phenyl
isopropyl


1039
3
4-OMe-Phenyl
—CH2CH(CH3)2


1040
3
4-OMe-Phenyl
CF3


1041
3
4-OMe-Phenyl
—CH2CF3


1042
3
4-OMe-Phenyl
—CH2CH2CF3


1043
3
4-OMe-Phenyl
cyclopropyl


1044
3
4-OMe-Phenyl
Cyclobutyl


1045
3
4-OMe-Phenyl
cyclopentyl


1046
3
4-OMe-Phenyl
cyclohexyl


1047
3
4-OMe-Phenyl
3-pyridyl


1048
3
4-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


1049
3
4-OMe-Phenyl
1H-imidazol-4-yl


1050
3
4-OMe-Phenyl
2-furanyl


1051
3
2-OMe-Phenyl
ethyl


1052
3
2-OMe-Phenyl
n-propyl


1053
3
2-OMe-Phenyl
isopropyl


1054
3
2-OMe-Phenyl
—CH2CH(CH3)2


1055
3
2-OMe-Phenyl
CF3


1056
3
2-OMe-Phenyl
—CH2CF3


1057
3
2-OMe-Phenyl
—CH2CH2CF3


1058
3
2-OMe-Phenyl
cyclopropyl


1059
3
2-OMe-Phenyl
Cyclobutyl


1060
3
2-OMe-Phenyl
cyclopentyl


1061
3
2-OMe-Phenyl
cyclohexyl


1062
3
2-OMe-Phenyl
3-pyridyl


1063
3
2-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


1064
3
2-OMe-Phenyl
1H-imidazol-4-yl


1065
3
2-OMe-Phenyl
2-furanyl


1066
3
3-CN-Phenyl
ethyl


1067
3
3-CN-Phenyl
n-propyl


1068
3
3-CN-Phenyl
isopropyl


1069
3
3-CN-Phenyl
—CH2CH(CH3)2


1070
3
3-CN-Phenyl
CF3


1071
3
3-CN-Phenyl
—CH2CF3


1072
3
3-CN-Phenyl
—CH2CH2CF3


1073
3
3-CN-Phenyl
cyclopropyl


1074
3
3-CN-Phenyl
Cyclobutyl


1075
3
3-CN-Phenyl
cyclopentyl


1076
3
3-CN-Phenyl
cyclohexyl


1077
3
3-CN-Phenyl
3-pyridyl


1078
3
3-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


1079
3
3-CN-Phenyl
1H-imidazol-4-yl


1080
3
3-CN-Phenyl
2-furanyl


1081
3
2-F-Phenyl
ethyl


1082
3
2-F-Phenyl
n-propyl


1083
3
2-F-Phenyl
isopropyl


1084
3
2-F-Phenyl
—CH2CH(CH3)2


1085
3
2-F-Phenyl
CF3


1086
3
2-F-Phenyl
—CH2CF3


1087
3
2-F-Phenyl
—CH2CH2CF3


1088
3
2-F-Phenyl
cyclopropyl


1089
3
2-F-Phenyl
Cyclobutyl


1090
3
2-F-Phenyl
cyclopentyl


1091
3
2-F-Phenyl
cyclohexyl


1092
3
2-F-Phenyl
3-pyridyl


1093
3
2-F-Phenyl
1-methyl-1H-pyrazol-4-yl


1094
3
2-F-Phenyl
1H-imidazol-4-yl


1095
3
2-F-Phenyl
2-furanyl


1096
3
4-F-Phenyl
ethyl


1097
3
4-F-Phenyl
n-propyl


1098
3
4-F-Phenyl
isopropyl


1099
3
4-F-Phenyl
—CH2CH(CH3)2


1100
3
4-F-Phenyl
CF3


1101
3
4-F-Phenyl
—CH2CF3


1102
3
4-F-Phenyl
—CH2CH2CF3


1103
3
4-F-Phenyl
cyclopropyl


1104
3
4-F-Phenyl
Cyclobutyl


1105
3
4-F-Phenyl
cyclopentyl


1106
3
4-F-Phenyl
cyclohexyl


1107
3
4-F-Phenyl
3-pyridyl


1108
3
4-F-Phenyl
1-methyl-1H-pyrazol-4-yl


1109
3
4-F-Phenyl
1H-imidazol-4-yl


1110
3
4-F-Phenyl
2-furanyl


1111
3
3-Cl-Phenyl
ethyl


1112
3
3-Cl-Phenyl
n-propyl


1113
3
3-Cl-Phenyl
isopropyl


1114
3
3-Cl-Phenyl
—CH2CH(CH3)2


1115
3
3-Cl-Phenyl
CF3


1116
3
3-Cl-Phenyl
—CH2CF3


1117
3
3-Cl-Phenyl
—CH2CH2CF3


1118
3
3-Cl-Phenyl
cyclopropyl


1119
3
3-Cl-Phenyl
Cyclobutyl


1120
3
3-Cl-Phenyl
cyclopentyl


1121
3
3-Cl-Phenyl
cyclohexyl


1122
3
3-Cl-Phenyl
3-pyridyl


1123
3
3-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


1124
3
3-Cl-Phenyl
1H-imidazol-4-yl


1125
3
3-Cl-Phenyl
2-furanyl


1126
3
2-Br-Phenyl
ethyl


1127
3
2-Br-Phenyl
n-propyl


1128
3
2-Br-Phenyl
isopropyl


1129
3
2-Br-Phenyl
—CH2CH(CH3)2


1130
3
2-Br-Phenyl
CF3


1131
3
2-Br-Phenyl
—CH2CF3


1132
3
2-Br-Phenyl
—CH2CH2CF3


1133
3
2-Br-Phenyl
cyclopropyl


1134
3
2-Br-Phenyl
Cyclobutyl


1135
3
2-Br-Phenyl
cyclopentyl


1136
3
2-Br-Phenyl
cyclohexyl


1137
3
2-Br-Phenyl
3-pyridyl


1138
3
2-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


1139
3
2-Br-Phenyl
1H-imidazol-4-yl


1140
3
2-Br-Phenyl
2-furanyl


1141
3
4-Br-Phenyl
ethyl


1142
3
4-Br-Phenyl
n-propyl


1143
3
4-Br-Phenyl
isopropyl


1144
3
4-Br-Phenyl
—CH2CH(CH3)2


1145
3
4-Br-Phenyl
CF3


1146
3
4-Br-Phenyl
—CH2CF3


1147
3
4-Br-Phenyl
—CH2CH2CF3


1148
3
4-Br-Phenyl
cyclopropyl


1149
3
4-Br-Phenyl
Cyclobutyl


1150
3
4-Br-Phenyl
cyclopentyl


1151
3
4-Br-Phenyl
cyclohexyl


1152
3
4-Br-Phenyl
3-pyridyl


1153
3
4-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


1154
3
4-Br-Phenyl
1H-imidazol-4-yl


1155
3
4-Br-Phenyl
2-furanyl


1156
3
3-CF3-Phenyl
ethyl


1157
3
3-CF3-Phenyl
n-propyl


1158
3
3-CF3-Phenyl
isopropyl


1159
3
3-CF3-Phenyl
—CH2CH(CH3)2


1160
3
3-CF3-Phenyl
CF3


1161
3
3-CF3-Phenyl
—CH2CF3


1162
3
3-CF3-Phenyl
—CH2CH2CF3


1163
3
3-CF3-Phenyl
cyclopropyl


1164
3
3-CF3-Phenyl
Cyclobutyl


1165
3
3-CF3-Phenyl
cyclopentyl


1166
3
3-CF3-Phenyl
cyclohexyl


1167
3
3-CF3-Phenyl
3-pyridyl


1168
3
3-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


1169
3
3-CF3-Phenyl
1H-imidazol-4-yl


1170
3
3-CF3-Phenyl
2-furanyl


1171
3
2-iPr-Phenyl
ethyl


1172
3
2-iPr-Phenyl
n-propyl


1173
3
2-iPr-Phenyl
isopropyl


1174
3
2-iPr-Phenyl
—CH2CH(CH3)2


1175
3
2-iPr-Phenyl
CF3


1176
3
2-iPr-Phenyl
—CH2CF3


1177
3
2-iPr-Phenyl
—CH2CH2CF3


1178
3
2-iPr-Phenyl
cyclopropyl


1179
3
2-iPr-Phenyl
Cyclobutyl


1180
3
2-iPr-Phenyl
cyclopentyl


1181
3
2-iPr-Phenyl
cyclohexyl


1182
3
2-iPr-Phenyl
3-pyridyl


1183
3
2-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


1184
3
2-iPr-Phenyl
1H-imidazol-4-yl


1185
3
2-iPr-Phenyl
2-furanyl


1186
3
4-iPr-Phenyl
ethyl


1187
3
4-iPr-Phenyl
n-propyl


1188
3
4-iPr-Phenyl
isopropyl


1189
3
4-iPr-Phenyl
—CH2CH(CH3)2


1190
3
4-iPr-Phenyl
CF3


1191
3
4-iPr-Phenyl
—CH2CF3


1192
3
4-iPr-Phenyl
—CH2CH2CF3


1193
3
4-iPr-Phenyl
cyclopropyl


1194
3
4-iPr-Phenyl
Cyclobutyl


1195
3
4-iPr-Phenyl
cyclopentyl


1196
3
4-iPr-Phenyl
cyclohexyl


1197
3
4-iPr-Phenyl
3-pyridyl


1198
3
4-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


1199
3
4-iPr-Phenyl
1H-imidazol-4-yl


1200
3
4-iPr-Phenyl
2-furanyl


1201
3
3-morpholino-phenyl
ethyl


1202
3
3-morpholino-phenyl
n-propyl


1203
3
3-morpholino-phenyl
isopropyl


1204
3
3-morpholino-phenyl
—CH2CH(CH3)2


1205
3
3-morpholino-phenyl
CF3


1206
3
3-morpholino-phenyl
—CH2CF3


1207
3
3-morpholino-phenyl
—CH2CH2CF3


1208
3
3-morpholino-phenyl
cyclopropyl


1209
3
3-morpholino-phenyl
Cyclobutyl


1210
3
3-morpholino-phenyl
cyclopentyl


1211
3
3-morpholino-phenyl
cyclohexyl


1212
3
3-morpholino-phenyl
3-pyridyl


1213
3
3-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1214
3
3-morpholino-phenyl
1H-imidazol-4-yl


1215
3
3-morpholino-phenyl
2-furanyl


1216
3
4-cyano-2-morpholino-phenyl
ethyl


1217
3
4-cyano-2-morpholino-phenyl
n-propyl


1218
3
4-cyano-2-morpholino-phenyl
isopropyl


1219
3
4-cyano-2-morpholino-phenyl
—CH2CH(CH3)2


1220
3
4-cyano-2-morpholino-phenyl
CF3


1221
3
4-cyano-2-morpholino-phenyl
—CH2CF3


1222
3
4-cyano-2-morpholino-phenyl
—CH2CH2CF3


1223
3
4-cyano-2-morpholino-phenyl
cyclopropyl


1224
3
4-cyano-2-morpholino-phenyl
Cyclobutyl


1225
3
4-cyano-2-morpholino-phenyl
cyclopentyl


1226
3
4-cyano-2-morpholino-phenyl
cyclohexyl


1227
3
4-cyano-2-morpholino-phenyl
3-pyridyl


1228
3
4-cyano-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1229
3
4-cyano-2-morpholino-phenyl
1H-imidazol-4-yl


1230
3
4-cyano-2-morpholino-phenyl
2-furanyl


1231
3
4-hydroxy-2-morpholino-phenyl
ethyl


1232
3
4-hydroxy-2-morpholino-phenyl
n-propyl


1233
3
4-hydroxy-2-morpholino-phenyl
isopropyl


1234
3
4-hydroxy-2-morpholino-phenyl
—CH2CH(CH3)2


1235
3
4-hydroxy-2-morpholino-phenyl
CF3


1236
3
4-hydroxy-2-morpholino-phenyl
—CH2CF3


1237
3
4-hydroxy-2-morpholino-phenyl
—CH2CH2CF3


1238
3
4-hydroxy-2-morpholino-phenyl
cyclopropyl


1239
3
4-hydroxy-2-morpholino-phenyl
Cyclobutyl


1240
3
4-hydroxy-2-morpholino-phenyl
cyclopentyl


1241
3
4-hydroxy-2-morpholino-phenyl
cyclohexyl


1242
3
4-hydroxy-2-morpholino-phenyl
3-pyridyl


1243
3
4-hydroxy-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1244
3
4-hydroxy-2-morpholino-phenyl
1H-imidazol-4-yl


1245
3
4-hydroxy-2-morpholino-phenyl
2-furanyl


1246
3
2-CH3-phenyl
Ethyl


1247
3
2-CH3-phenyl
n-propyl


1248
3
2-CH3-phenyl
Isopropyl


1249
3
2-CH3-phenyl
—CH2CH(CH3)2


1250
3
2-CH3-phenyl
CF3


1251
3
2-CH3-phenyl
—CH2CF3


1252
3
2-CH3-phenyl
—CH2CH2CF3


1253
3
2-CH3-phenyl
cyclopropyl


1254
3
2-CH3-phenyl
Cyclobutyl


1255
3
2-CH3-phenyl
cyclopentyl


1256
3
2-CH3-phenyl
cyclohexyl


1257
3
2-CH3-phenyl
3-pyridyl


1258
3
2-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


1259
3
2-CH3-phenyl
1H-imidazol-4-yl


1260
3
2-CH3-phenyl
2-furanyl


1261
3
4-OH-Phenyl
Ethyl


1262
3
4-OH-Phenyl
n-propyl


1263
3
4-OH-Phenyl
Isopropyl


1264
3
4-OH-Phenyl
—CH2CH(CH3)2


1265
3
4-OH-Phenyl
CF3


1266
3
4-OH-Phenyl
—CH2CF3


1267
3
4-OH-Phenyl
—CH2CH2CF3


1268
3
4-OH-Phenyl
cyclopropyl


1269
3
4-OH-Phenyl
Cyclobutyl


1270
3
4-OH-Phenyl
cyclopentyl


1271
3
4-OH-Phenyl
cyclohexyl


1272
3
4-OH-Phenyl
3-pyridyl


1273
3
4-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


1274
3
4-OH-Phenyl
1H-imidazol-4-yl


1275
3
4-OH-Phenyl
2-furanyl


1276
3
2-OH-Phenyl
Ethyl


1277
3
2-OH-Phenyl
n-propyl


1278
3
2-OH-Phenyl
Isopropyl


1279
3
2-OH-Phenyl
—CH2CH(CH3)2


1280
3
2-OH-Phenyl
CF3


1281
3
2-OH-Phenyl
—CH2CF3


1282
3
2-OH-Phenyl
—CH2CH2CF3


1283
3
2-OH-Phenyl
cyclopropyl


1284
3
2-OH-Phenyl
Cyclobutyl


1285
3
2-OH-Phenyl
cyclopentyl


1286
3
2-OH-Phenyl
cyclohexyl


1287
3
2-OH-Phenyl
3-pyridyl


1288
3
2-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


1289
3
2-OH-Phenyl
1H-imidazol-4-yl


1290
3
2-OH-Phenyl
2-furanyl


1291
3
3-OMe-Phenyl
Ethyl


1292
3
3-OMe-Phenyl
n-propyl


1293
3
3-OMe-Phenyl
Isopropyl


1294
3
3-OMe-Phenyl
—CH2CH(CH3)2


1295
3
3-OMe-Phenyl
CF3


1296
3
3-OMe-Phenyl
—CH2CF3


1297
3
3-OMe-Phenyl
—CH2CH2CF3


1298
3
3-OMe-Phenyl
cyclopropyl


1299
3
3-OMe-Phenyl
Cyclobutyl


1300
3
3-OMe-Phenyl
cyclopentyl


1301
3
3-OMe-Phenyl
cyclohexyl


1302
3
3-OMe-Phenyl
3-pyridyl


1303
3
3-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


1304
3
3-OMe-Phenyl
1H-imidazol-4-yl


1305
3
3-OMe-Phenyl
2-furanyl


1306
3
4-CN-Phenyl
Ethyl


1307
3
4-CN-Phenyl
n-propyl


1308
3
4-CN-Phenyl
Isopropyl


1309
3
4-CN-Phenyl
—CH2CH(CH3)2


1310
3
4-CN-Phenyl
CF3


1311
3
4-CN-Phenyl
—CH2CF3


1312
3
4-CN-Phenyl
—CH2CH2CF3


1313
3
4-CN-Phenyl
cyclopropyl


1314
3
4-CN-Phenyl
Cyclobutyl


1315
3
4-CN-Phenyl
cyclopentyl


1316
3
4-CN-Phenyl
cyclohexyl


1317
3
4-CN-Phenyl
3-pyridyl


1318
3
4-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


1319
3
4-CN-Phenyl
1H-imidazol-4-yl


1320
3
4-CN-Phenyl
2-furanyl


1321
3
2-CN-Phenyl
Ethyl


1322
3
2-CN-Phenyl
n-propyl


1323
3
2-CN-Phenyl
Isopropyl


1324
3
2-CN-Phenyl
—CH2CH(CH3)2


1325
3
2-CN-Phenyl
CF3


1326
3
2-CN-Phenyl
—CH2CF3


1327
3
2-CN-Phenyl
—CH2CH2CF3


1328
3
2-CN-Phenyl
cyclopropyl


1329
3
2-CN-Phenyl
Cyclobutyl


1330
3
2-CN-Phenyl
cyclopentyl


1331
3
2-CN-Phenyl
cyclohexyl


1332
3
2-CN-Phenyl
3-pyridyl


1333
3
2-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


1334
3
2-CN-Phenyl
1H-imidazol-4-yl


1335
3
2-CN-Phenyl
2-furanyl


1336
3
3-F-Phenyl
Ethyl


1337
3
3-F-Phenyl
n-propyl


1338
3
3-F-Phenyl
Isopropyl


1339
3
3-F-Phenyl
—CH2CH(CH3)2


1340
3
3-F-Phenyl
CF3


1341
3
3-F-Phenyl
—CH2CF3


1342
3
3-F-Phenyl
—CH2CH2CF3


1343
3
3-F-Phenyl
cyclopropyl


1344
3
3-F-Phenyl
Cyclobutyl


1345
3
3-F-Phenyl
cyclopentyl


1346
3
3-F-Phenyl
cyclohexyl


1347
3
3-F-Phenyl
3-pyridyl


1348
3
3-F-Phenyl
1-methyl-1H-pyrazol-4-yl


1349
3
3-F-Phenyl
1H-imidazol-4-yl


1350
3
3-F-Phenyl
2-furanyl


1351
3
2-Cl-Phenyl
Ethyl


1352
3
2-Cl-Phenyl
n-propyl


1353
3
2-Cl-Phenyl
Isopropyl


1354
3
2-Cl-Phenyl
—CH2CH(CH3)2


1355
3
2-Cl-Phenyl
CF3


1356
3
2-Cl-Phenyl
—CH2CF3


1357
3
2-Cl-Phenyl
—CH2CH2CF3


1358
3
2-Cl-Phenyl
cyclopropyl


1359
3
2-Cl-Phenyl
Cyclobutyl


1360
3
2-Cl-Phenyl
cyclopentyl


1361
3
2-Cl-Phenyl
cyclohexyl


1362
3
2-Cl-Phenyl
3-pyridyl


1363
3
2-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


1364
3
2-Cl-Phenyl
1H-imidazol-4-yl


1365
3
2-Cl-Phenyl
2-furanyl


1366
3
4-Cl-Phenyl
Ethyl


1367
3
4-Cl-Phenyl
n-propyl


1368
3
4-Cl-Phenyl
Isopropyl


1369
3
4-Cl-Phenyl
—CH2CH(CH3)2


1370
3
4-Cl-Phenyl
CF3


1371
3
4-Cl-Phenyl
—CH2CF3


1372
3
4-Cl-Phenyl
—CH2CH2CF3


1373
3
4-Cl-Phenyl
cyclopropyl


1374
3
4-Cl-Phenyl
Cyclobutyl


1375
3
4-Cl-Phenyl
cyclopentyl


1376
3
4-Cl-Phenyl
cyclohexyl


1377
3
4-Cl-Phenyl
3-pyridyl


1378
3
4-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


1379
3
4-Cl-Phenyl
1H-imidazol-4-yl


1380
3
4-Cl-Phenyl
2-furanyl


1381
3
3-Br-Phenyl
Ethyl


1382
3
3-Br-Phenyl
n-propyl


1383
3
3-Br-Phenyl
Isopropyl


1384
3
3-Br-Phenyl
—CH2CH(CH3)2


1385
3
3-Br-Phenyl
CF3


1386
3
3-Br-Phenyl
—CH2CF3


1387
3
3-Br-Phenyl
—CH2CH2CF3


1388
3
3-Br-Phenyl
cyclopropyl


1389
3
3-Br-Phenyl
Cyclobutyl


1390
3
3-Br-Phenyl
cyclopentyl


1391
3
3-Br-Phenyl
cyclohexyl


1392
3
3-Br-Phenyl
3-pyridyl


1393
3
3-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


1394
3
3-Br-Phenyl
1H-imidazol-4-yl


1395
3
3-Br-Phenyl
2-furanyl


1396
3
2-CF3-Phenyl
Ethyl


1397
3
2-CF3-Phenyl
n-propyl


1398
3
2-CF3-Phenyl
Isopropyl


1399
3
2-CF3-Phenyl
—CH2CH(CH3)2


1400
3
2-CF3-Phenyl
CF3


1401
3
2-CF3-Phenyl
—CH2CF3


1402
3
2-CF3-Phenyl
—CH2CH2CF3


1403
3
2-CF3-Phenyl
cyclopropyl


1404
3
2-CF3-Phenyl
Cyclobutyl


1405
3
2-CF3-Phenyl
cyclopentyl


1406
3
2-CF3-Phenyl
cyclohexyl


1407
3
2-CF3-Phenyl
3-pyridyl


1408
3
2-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


1409
3
2-CF3-Phenyl
1H-imidazol-4-yl


1410
3
2-CF3-Phenyl
2-furanyl


1411
3
4-CF3-Phenyl
Ethyl


1412
3
4-CF3-Phenyl
n-propyl


1413
3
4-CF3-Phenyl
Isopropyl


1414
3
4-CF3-Phenyl
—CH2CH(CH3)2


1415
3
4-CF3-Phenyl
CF3


1416
3
4-CF3-Phenyl
—CH2CF3


1417
3
4-CF3-Phenyl
—CH2CH2CF3


1418
3
4-CF3-Phenyl
cyclopropyl


1419
3
4-CF3-Phenyl
Cyclobutyl


1420
3
4-CF3-Phenyl
cyclopentyl


1421
3
4-CF3-Phenyl
cyclohexyl


1422
3
4-CF3-Phenyl
3-pyridyl


1423
3
4-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


1424
3
4-CF3-Phenyl
1H-imidazol-4-yl


1425
3
4-CF3-Phenyl
2-furanyl


1426
3
3-iPr-Phenyl
Ethyl


1427
3
3-iPr-Phenyl
n-propyl


1428
3
3-iPr-Phenyl
Isopropyl


1429
3
3-iPr-Phenyl
—CH2CH(CH3)2


1430
3
3-iPr-Phenyl
CF3


1431
3
3-iPr-Phenyl
—CH2CF3


1432
3
3-iPr-Phenyl
—CH2CH2CF3


1433
3
3-iPr-Phenyl
cyclopropyl


1434
3
3-iPr-Phenyl
Cyclobutyl


1435
3
3-iPr-Phenyl
cyclopentyl


1436
3
3-iPr-Phenyl
cyclohexyl


1437
3
3-iPr-Phenyl
3-pyridyl


1438
3
3-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


1439
3
3-iPr-Phenyl
1H-imidazol-4-yl


1440
3
3-iPr-Phenyl
2-furanyl


1441
3
2-morpholino-phenyl
Ethyl


1442
3
2-morpholino-phenyl
n-propyl


1443
3
2-morpholino-phenyl
isopropyl


1444
3
2-morpholino-phenyl
—CH2CH(CH3)2


1445
3
2-morpholino-phenyl
CF3


1446
3
2-morpholino-phenyl
—CH2CF3


1447
3
2-morpholino-phenyl
—CH2CH2CF3


1448
3
2-morpholino-phenyl
cyclopropyl


1449
3
2-morpholino-phenyl
Cyclobutyl


1450
3
2-morpholino-phenyl
cyclopentyl


1451
3
2-morpholino-phenyl
cyclohexyl


1452
3
2-morpholino-phenyl
3-pyridyl


1453
3
2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1454
3
2-morpholino-phenyl
1H-imidazol-4-yl


1455
3
2-morpholino-phenyl
2-furanyl


1456
3
4-morpholino-phenyl
ethyl


1457
3
4-morpholino-phenyl
n-propyl


1458
3
4-morpholino-phenyl
isopropyl


1459
3
4-morpholino-phenyl
—CH2CH(CH3)2


1460
3
4-morpholino-phenyl
CF3


1461
3
4-morpholino-phenyl
—CH2CF3


1462
3
4-morpholino-phenyl
—CH2CH2CF3


1463
3
4-morpholino-phenyl
cyclopropyl


1464
3
4-morpholino-phenyl
Cyclobutyl


1465
3
4-morpholino-phenyl
cyclopentyl


1466
3
4-morpholino-phenyl
cyclohexyl


1467
3
4-morpholino-phenyl
3-pyridyl


1468
3
4-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1469
3
4-morpholino-phenyl
1H-imidazol-4-yl


1470
3
4-morpholino-phenyl
2-furanyl


1471
3
4-methyl-2-morpholino-phenyl
ethyl


1472
3
4-methyl-2-morpholino-phenyl
n-propyl


1473
3
4-methyl-2-morpholino-phenyl
isopropyl


1474
3
4-methyl-2-morpholino-phenyl
—CH2CH(CH3)2


1475
3
4-methyl-2-morpholino-phenyl
CF3


1476
3
4-methyl-2-morpholino-phenyl
—CH2CF3


1477
3
4-methyl-2-morpholino-phenyl
—CH2CH2CF3


1478
3
4-methyl-2-morpholino-phenyl
cyclopropyl


1479
3
4-methyl-2-morpholino-phenyl
Cyclobutyl


1480
3
4-methyl-2-morpholino-phenyl
cyclopentyl


1481
3
4-methyl-2-morpholino-phenyl
cyclohexyl


1482
3
4-methyl-2-morpholino-phenyl
3-pyridyl


1483
3
4-methyl-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1484
3
4-methyl-2-morpholino-phenyl
1H-imidazol-4-yl


1485
3
4-methyl-2-morpholino-phenyl
2-furanyl


1486
4
4-CH3-phenyl
ethyl


1487
4
4-CH3-phenyl
n-propyl


1488
4
4-CH3-phenyl
isopropyl


1489
4
4-CH3-phenyl
—CH2CH(CH3)2


1490
4
4-CH3-phenyl
CF3


1491
4
4-CH3-phenyl
—CH2CF3


1492
4
4-CH3-phenyl
—CH2CH2CF3


1493
4
4-CH3-phenyl
cyclopropyl


1494
4
4-CH3-phenyl
Cyclobutyl


1495
4
4-CH3-phenyl
cyclopentyl


1496
4
4-CH3-phenyl
cyclohexyl


1497
4
4-CH3-phenyl
3-pyridyl


1498
4
4-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


1499
4
4-CH3-phenyl
1H-imidazol-4-yl


1500
4
4-CH3-phenyl
2-furanyl


1501
4
3-CH3-phenyl
ethyl


1502
4
3-CH3-phenyl
n-propyl


1503
4
3-CH3-phenyl
isopropyl


1504
4
3-CH3-phenyl
—CH2CH(CH3)2


1505
4
3-CH3-phenyl
CF3


1506
4
3-CH3-phenyl
—CH2CF3


1507
4
3-CH3-phenyl
—CH2CH2CF3


1508
4
3-CH3-phenyl
cyclopropyl


1509
4
3-CH3-phenyl
Cyclobutyl


1510
4
3-CH3-phenyl
cyclopentyl


1511
4
3-CH3-phenyl
cyclohexyl


1512
4
3-CH3-phenyl
3-pyridyl


1513
4
3-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


1514
4
3-CH3-phenyl
1H-imidazol-4-yl


1515
4
3-CH3-phenyl
2-furanyl


1516
4
3-OH-Phenyl
ethyl


1517
4
3-OH-Phenyl
n-propyl


1518
4
3-OH-Phenyl
isopropyl


1519
4
3-OH-Phenyl
—CH2CH(CH3)2


1520
4
3-OH-Phenyl
CF3


1521
4
3-OH-Phenyl
—CH2CF3


1522
4
3-OH-Phenyl
—CH2CH2CF3


1523
4
3-OH-Phenyl
cyclopropyl


1524
4
3-OH-Phenyl
Cyclobutyl


1525
4
3-OH-Phenyl
cyclopentyl


1526
4
3-OH-Phenyl
cyclohexyl


1527
4
3-OH-Phenyl
3-pyridyl


1528
4
3-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


1529
4
3-OH-Phenyl
1H-imidazol-4-yl


1530
4
3-OH-Phenyl
2-furanyl


1531
4
4-OMe-Phenyl
ethyl


1532
4
4-OMe-Phenyl
n-propyl


1533
4
4-OMe-Phenyl
isopropyl


1534
4
4-OMe-Phenyl
—CH2CH(CH3)2


1535
4
4-OMe-Phenyl
CF3


1536
4
4-OMe-Phenyl
—CH2CF3


1537
4
4-OMe-Phenyl
—CH2CH2CF3


1538
4
4-OMe-Phenyl
cyclopropyl


1539
4
4-OMe-Phenyl
Cyclobutyl


1540
4
4-OMe-Phenyl
cyclopentyl


1541
4
4-OMe-Phenyl
cyclohexyl


1542
4
4-OMe-Phenyl
3-pyridyl


1543
4
4-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


1544
4
4-OMe-Phenyl
1H-imidazol-4-yl


1545
4
4-OMe-Phenyl
2-furanyl


1546
4
2-OMe-Phenyl
ethyl


1547
4
2-OMe-Phenyl
n-propyl


1548
4
2-OMe-Phenyl
isopropyl


1549
4
2-OMe-Phenyl
—CH2CH(CH3)2


1550
4
2-OMe-Phenyl
CF3


1551
4
2-OMe-Phenyl
—CH2CF3


1552
4
2-OMe-Phenyl
—CH2CH2CF3


1553
4
2-OMe-Phenyl
cyclopropyl


1554
4
2-OMe-Phenyl
Cyclobutyl


1555
4
2-OMe-Phenyl
cyclopentyl


1556
4
2-OMe-Phenyl
cyclohexyl


1557
4
2-OMe-Phenyl
3-pyridyl


1558
4
2-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


1559
4
2-OMe-Phenyl
1H-imidazol-4-yl


1560
4
2-OMe-Phenyl
2-furanyl


1561
4
3-CN-Phenyl
ethyl


1562
4
3-CN-Phenyl
n-propyl


1563
4
3-CN-Phenyl
isopropyl


1564
4
3-CN-Phenyl
—CH2CH(CH3)2


1565
4
3-CN-Phenyl
CF3


1566
4
3-CN-Phenyl
—CH2CF3


1567
4
3-CN-Phenyl
—CH2CH2CF3


1568
4
3-CN-Phenyl
cyclopropyl


1569
4
3-CN-Phenyl
Cyclobutyl


1570
4
3-CN-Phenyl
cyclopentyl


1571
4
3-CN-Phenyl
cyclohexyl


1572
4
3-CN-Phenyl
3-pyridyl


1573
4
3-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


1574
4
3-CN-Phenyl
1H-imidazol-4-yl


1575
4
3-CN-Phenyl
2-furanyl


1576
4
2-F-Phenyl
ethyl


1577
4
2-F-Phenyl
n-propyl


1578
4
2-F-Phenyl
isopropyl


1579
4
2-F-Phenyl
—CH2CH(CH3)2


1580
4
2-F-Phenyl
CF3


1581
4
2-F-Phenyl
—CH2CF3


1582
4
2-F-Phenyl
—CH2CH2CF3


1583
4
2-F-Phenyl
cyclopropyl


1584
4
2-F-Phenyl
Cyclobutyl


1585
4
2-F-Phenyl
cyclopentyl


1586
4
2-F-Phenyl
cyclohexyl


1587
4
2-F-Phenyl
3-pyridyl


1588
4
2-F-Phenyl
1-methyl-1H-pyrazol-4-yl


1589
4
2-F-Phenyl
1H-imidazol-4-yl


1590
4
2-F-Phenyl
2-furanyl


1591
4
4-F-Phenyl
ethyl


1592
4
4-F-Phenyl
n-propyl


1593
4
4-F-Phenyl
isopropyl


1594
4
4-F-Phenyl
—CH2CH(CH3)2


1595
4
4-F-Phenyl
CF3


1596
4
4-F-Phenyl
—CH2CF3


1597
4
4-F-Phenyl
—CH2CH2CF3


1598
4
4-F-Phenyl
cyclopropyl


1599
4
4-F-Phenyl
Cyclobutyl


1600
4
4-F-Phenyl
cyclopentyl


1601
4
4-F-Phenyl
cyclohexyl


1602
4
4-F-Phenyl
3-pyridyl


1603
4
4-F-Phenyl
1-methyl-1H-pyrazol-4-yl


1604
4
4-F-Phenyl
1H-imidazol-4-yl


1605
4
4-F-Phenyl
2-furanyl


1606
4
3-Cl-Phenyl
ethyl


1607
4
3-Cl-Phenyl
n-propyl


1608
4
3-Cl-Phenyl
isopropyl


1609
4
3-Cl-Phenyl
—CH2CH(CH3)2


1610
4
3-Cl-Phenyl
CF3


1611
4
3-Cl-Phenyl
—CH2CF3


1612
4
3-Cl-Phenyl
—CH2CH2CF3


1613
4
3-Cl-Phenyl
cyclopropyl


1614
4
3-Cl-Phenyl
Cyclobutyl


1615
4
3-Cl-Phenyl
cyclopentyl


1616
4
3-Cl-Phenyl
cyclohexyl


1617
4
3-Cl-Phenyl
3-pyridyl


1618
4
3-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


1619
4
3-Cl-Phenyl
1H-imidazol-4-yl


1620
4
3-Cl-Phenyl
2-furanyl


1621
4
2-Br-Phenyl
ethyl


1622
4
2-Br-Phenyl
n-propyl


1623
4
2-Br-Phenyl
isopropyl


1624
4
2-Br-Phenyl
—CH2CH(CH3)2


1625
4
2-Br-Phenyl
CF3


1626
4
2-Br-Phenyl
—CH2CF3


1627
4
2-Br-Phenyl
—CH2CH2CF3


1628
4
2-Br-Phenyl
cyclopropyl


1629
4
2-Br-Phenyl
Cyclobutyl


1630
4
2-Br-Phenyl
cyclopentyl


1631
4
2-Br-Phenyl
cyclohexyl


1632
4
2-Br-Phenyl
3-pyridyl


1633
4
2-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


1634
4
2-Br-Phenyl
1H-imidazol-4-yl


1635
4
2-Br-Phenyl
2-furanyl


1636
4
4-Br-Phenyl
ethyl


1637
4
4-Br-Phenyl
n-propyl


1638
4
4-Br-Phenyl
isopropyl


1639
4
4-Br-Phenyl
—CH2CH(CH3)2


1640
4
4-Br-Phenyl
CF3


1641
4
4-Br-Phenyl
—CH2CF3


1642
4
4-Br-Phenyl
—CH2CH2CF3


1643
4
4-Br-Phenyl
cyclopropyl


1644
4
4-Br-Phenyl
Cyclobutyl


1645
4
4-Br-Phenyl
cyclopentyl


1646
4
4-Br-Phenyl
cyclohexyl


1647
4
4-Br-Phenyl
3-pyridyl


1648
4
4-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


1649
4
4-Br-Phenyl
1H-imidazol-4-yl


1650
4
4-Br-Phenyl
2-furanyl


1651
4
3-CF3-Phenyl
ethyl


1652
4
3-CF3-Phenyl
n-propyl


1653
4
3-CF3-Phenyl
isopropyl


1654
4
3-CF3-Phenyl
—CH2CH(CH3)2


1655
4
3-CF3-Phenyl
CF3


1656
4
3-CF3-Phenyl
—CH2CF3


1657
4
3-CF3-Phenyl
—CH2CH2CF3


1658
4
3-CF3-Phenyl
cyclopropyl


1659
4
3-CF3-Phenyl
Cyclobutyl


1660
4
3-CF3-Phenyl
cyclopentyl


1661
4
3-CF3-Phenyl
cyclohexyl


1662
4
3-CF3-Phenyl
3-pyridyl


1663
4
3-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


1664
4
3-CF3-Phenyl
1H-imidazol-4-yl


1665
4
3-CF3-Phenyl
2-furanyl


1666
4
2-iPr-Phenyl
ethyl


1667
4
2-iPr-Phenyl
n-propyl


1668
4
2-iPr-Phenyl
isopropyl


1669
4
2-iPr-Phenyl
—CH2CH(CH3)2


1670
4
2-iPr-Phenyl
CF3


1671
4
2-iPr-Phenyl
—CH2CF3


1672
4
2-iPr-Phenyl
—CH2CH2CF3


1673
4
2-iPr-Phenyl
cyclopropyl


1674
4
2-iPr-Phenyl
Cyclobutyl


1675
4
2-iPr-Phenyl
cyclopentyl


1676
4
2-iPr-Phenyl
cyclohexyl


1677
4
2-iPr-Phenyl
3-pyridyl


1678
4
2-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


1679
4
2-iPr-Phenyl
1H-imidazol-4-yl


1680
4
2-iPr-Phenyl
2-furanyl


1681
4
4-iPr-Phenyl
ethyl


1682
4
4-iPr-Phenyl
n-propyl


1683
4
4-iPr-Phenyl
isopropyl


1684
4
4-iPr-Phenyl
—CH2CH(CH3)2


1685
4
4-iPr-Phenyl
CF3


1686
4
4-iPr-Phenyl
—CH2CF3


1687
4
4-iPr-Phenyl
—CH2CH2CF3


1688
4
4-iPr-Phenyl
cyclopropyl


1689
4
4-iPr-Phenyl
Cyclobutyl


1690
4
4-iPr-Phenyl
cyclopentyl


1691
4
4-iPr-Phenyl
cyclohexyl


1692
4
4-iPr-Phenyl
3-pyridyl


1693
4
4-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


1694
4
4-iPr-Phenyl
1H-imidazol-4-yl


1695
4
4-iPr-Phenyl
2-furanyl


1696
4
3-morpholino-phenyl
ethyl


1697
4
3-morpholino-phenyl
n-propyl


1698
4
3-morpholino-phenyl
isopropyl


1699
4
3-morpholino-phenyl
—CH2CH(CH3)2


1700
4
3-morpholino-phenyl
CF3


1701
4
3-morpholino-phenyl
—CH2CF3


1702
4
3-morpholino-phenyl
—CH2CH2CF3


1703
4
3-morpholino-phenyl
cyclopropyl


1704
4
3-morpholino-phenyl
Cyclobutyl


1705
4
3-morpholino-phenyl
cyclopentyl


1706
4
3-morpholino-phenyl
cyclohexyl


1707
4
3-morpholino-phenyl
3-pyridyl


1708
4
3-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1709
4
3-morpholino-phenyl
1H-imidazol-4-yl


1710
4
3-morpholino-phenyl
2-furanyl


1711
4
4-cyano-2-morpholino-phenyl
ethyl


1712
4
4-cyano-2-morpholino-phenyl
n-propyl


1713
4
4-cyano-2-morpholino-phenyl
isopropyl


1714
4
4-cyano-2-morpholino-phenyl
—CH2CH(CH3)2


1715
4
4-cyano-2-morpholino-phenyl
CF3


1716
4
4-cyano-2-morpholino-phenyl
—CH2CF3


1717
4
4-cyano-2-morpholino-phenyl
—CH2CH2CF3


1718
4
4-cyano-2-morpholino-phenyl
cyclopropyl


1719
4
4-cyano-2-morpholino-phenyl
Cyclobutyl


1720
4
4-cyano-2-morpholino-phenyl
cyclopentyl


1721
4
4-cyano-2-morpholino-phenyl
cyclohexyl


1722
4
4-cyano-2-morpholino-phenyl
3-pyridyl


1723
4
4-cyano-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1724
4
4-cyano-2-morpholino-phenyl
1H-imidazol-4-yl


1725
4
4-cyano-2-morpholino-phenyl
2-furanyl


1726
4
4-hydroxy-2-morpholino-phenyl
ethyl


1727
4
4-hydroxy-2-morpholino-phenyl
n-propyl


1728
4
4-hydroxy-2-morpholino-phenyl
isopropyl


1729
4
4-hydroxy-2-morpholino-phenyl
—CH2CH(CH3)2


1730
4
4-hydroxy-2-morpholino-phenyl
CF3


1731
4
4-hydroxy-2-morpholino-phenyl
—CH2CF3


1732
4
4-hydroxy-2-morpholino-phenyl
—CH2CH2CF3


1733
4
4-hydroxy-2-morpholino-phenyl
cyclopropyl


1734
4
4-hydroxy-2-morpholino-phenyl
Cyclobutyl


1735
4
4-hydroxy-2-morpholino-phenyl
cyclopentyl


1736
4
4-hydroxy-2-morpholino-phenyl
cyclohexyl


1737
4
4-hydroxy-2-morpholino-phenyl
3-pyridyl


1738
4
4-hydroxy-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1739
4
4-hydroxy-2-morpholino-phenyl
1H-imidazol-4-yl


1740
4
4-hydroxy-2-morpholino-phenyl
2-furanyl


1741
4
2-CH3-phenyl
Ethyl


1742
4
2-CH3-phenyl
n-propyl


1743
4
2-CH3-phenyl
Isopropyl


1744
4
2-CH3-phenyl
—CH2CH(CH3)2


1745
4
2-CH3-phenyl
CF3


1746
4
2-CH3-phenyl
—CH2CF3


1747
4
2-CH3-phenyl
—CH2CH2CF3


1748
4
2-CH3-phenyl
cyclopropyl


1749
4
2-CH3-phenyl
Cyclobutyl


1750
4
2-CH3-phenyl
cyclopentyl


1751
4
2-CH3-phenyl
cyclohexyl


1752
4
2-CH3-phenyl
3-pyridyl


1753
4
2-CH3-phenyl
1-methyl-1H-pyrazol-4-yl


1754
4
2-CH3-phenyl
1H-imidazol-4-yl


1755
4
2-CH3-phenyl
2-furanyl


1756
4
4-OH-Phenyl
Ethyl


1757
4
4-OH-Phenyl
n-propyl


1758
4
4-OH-Phenyl
Isopropyl


1759
4
4-OH-Phenyl
—CH2CH(CH3)2


1760
4
4-OH-Phenyl
CF3


1761
4
4-OH-Phenyl
—CH2CF3


1762
4
4-OH-Phenyl
—CH2CH2CF3


1763
4
4-OH-Phenyl
cyclopropyl


1764
4
4-OH-Phenyl
Cyclobutyl


1765
4
4-OH-Phenyl
cyclopentyl


1766
4
4-OH-Phenyl
cyclohexyl


1767
4
4-OH-Phenyl
3-pyridyl


1768
4
4-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


1769
4
4-OH-Phenyl
1H-imidazol-4-yl


1770
4
4-OH-Phenyl
2-furanyl


1771
4
2-OH-Phenyl
Ethyl


1772
4
2-OH-Phenyl
n-propyl


1773
4
2-OH-Phenyl
Isopropyl


1774
4
2-OH-Phenyl
—CH2CH(CH3)2


1775
4
2-OH-Phenyl
CF3


1776
4
2-OH-Phenyl
—CH2CF3


1777
4
2-OH-Phenyl
—CH2CH2CF3


1778
4
2-OH-Phenyl
cyclopropyl


1779
4
2-OH-Phenyl
Cyclobutyl


1780
4
2-OH-Phenyl
cyclopentyl


1781
4
2-OH-Phenyl
cyclohexyl


1782
4
2-OH-Phenyl
3-pyridyl


1783
4
2-OH-Phenyl
1-methyl-1H-pyrazol-4-yl


1784
4
2-OH-Phenyl
1H-imidazol-4-yl


1785
4
2-OH-Phenyl
2-furanyl


1786
4
3-OMe-Phenyl
Ethyl


1787
4
3-OMe-Phenyl
n-propyl


1788
4
3-OMe-Phenyl
Isopropyl


1789
4
3-OMe-Phenyl
—CH2CH(CH3)2


1790
4
3-OMe-Phenyl
CF3


1791
4
3-OMe-Phenyl
—CH2CF3


1792
4
3-OMe-Phenyl
—CH2CH2CF3


1793
4
3-OMe-Phenyl
cyclopropyl


1794
4
3-OMe-Phenyl
Cyclobutyl


1795
4
3-OMe-Phenyl
cyclopentyl


1796
4
3-OMe-Phenyl
cyclohexyl


1797
4
3-OMe-Phenyl
3-pyridyl


1798
4
3-OMe-Phenyl
1-methyl-1H-pyrazol-4-yl


1799
4
3-OMe-Phenyl
1H-imidazol-4-yl


1800
4
3-OMe-Phenyl
2-furanyl


1801
4
4-CN-Phenyl
Ethyl


1802
4
4-CN-Phenyl
n-propyl


1803
4
4-CN-Phenyl
Isopropyl


1804
4
4-CN-Phenyl
—CH2CH(CH3)2


1805
4
4-CN-Phenyl
CF3


1806
4
4-CN-Phenyl
—CH2CF3


1807
4
4-CN-Phenyl
—CH2CH2CF3


1808
4
4-CN-Phenyl
cyclopropyl


1809
4
4-CN-Phenyl
Cyclobutyl


1810
4
4-CN-Phenyl
cyclopentyl


1811
4
4-CN-Phenyl
cyclohexyl


1812
4
4-CN-Phenyl
3-pyridyl


1813
4
4-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


1814
4
4-CN-Phenyl
1H-imidazol-4-yl


1815
4
4-CN-Phenyl
2-furanyl


1816
4
2-CN-Phenyl
Ethyl


1817
4
2-CN-Phenyl
n-propyl


1818
4
2-CN-Phenyl
Isopropyl


1819
4
2-CN-Phenyl
—CH2CH(CH3)2


1820
4
2-CN-Phenyl
CF3


1821
4
2-CN-Phenyl
—CH2CF3


1822
4
2-CN-Phenyl
—CH2CH2CF3


1823
4
2-CN-Phenyl
cyclopropyl


1824
4
2-CN-Phenyl
Cyclobutyl


1825
4
2-CN-Phenyl
cyclopentyl


1826
4
2-CN-Phenyl
cyclohexyl


1827
4
2-CN-Phenyl
3-pyridyl


1828
4
2-CN-Phenyl
1-methyl-1H-pyrazol-4-yl


1829
4
2-CN-Phenyl
1H-imidazol-4-yl


1830
4
2-CN-Phenyl
2-furanyl


1831
4
3-F-Phenyl
Ethyl


1832
4
3-F-Phenyl
n-propyl


1833
4
3-F-Phenyl
Isopropyl


1834
4
3-F-Phenyl
—CH2CH(CH3)2


1835
4
3-F-Phenyl
CF3


1836
4
3-F-Phenyl
—CH2CF3


1837
4
3-F-Phenyl
—CH2CH2CF3


1838
4
3-F-Phenyl
cyclopropyl


1839
4
3-F-Phenyl
Cyclobutyl


1840
4
3-F-Phenyl
cyclopentyl


1841
4
3-F-Phenyl
cyclohexyl


1842
4
3-F-Phenyl
3-pyridyl


1843
4
3-F-Phenyl
1-methyl-1H-pyrazol-4-yl


1844
4
3-F-Phenyl
1H-imidazol-4-yl


1845
4
3-F-Phenyl
2-furanyl


1846
4
2-Cl-Phenyl
Ethyl


1847
4
2-Cl-Phenyl
n-propyl


1848
4
2-Cl-Phenyl
Isopropyl


1849
4
2-Cl-Phenyl
—CH2CH(CH3)2


1850
4
2-Cl-Phenyl
CF3


1851
4
2-Cl-Phenyl
—CH2CF3


1852
4
2-Cl-Phenyl
—CH2CH2CF3


1853
4
2-Cl-Phenyl
cyclopropyl


1854
4
2-Cl-Phenyl
Cyclobutyl


1855
4
2-Cl-Phenyl
cyclopentyl


1856
4
2-Cl-Phenyl
cyclohexyl


1857
4
2-Cl-Phenyl
3-pyridyl


1858
4
2-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


1859
4
2-Cl-Phenyl
1H-imidazol-4-yl


1860
4
2-Cl-Phenyl
2-furanyl


1861
4
4-Cl-Phenyl
Ethyl


1862
4
4-Cl-Phenyl
n-propyl


1863
4
4-Cl-Phenyl
Isopropyl


1864
4
4-Cl-Phenyl
—CH2CH(CH3)2


1865
4
4-Cl-Phenyl
CF3


1866
4
4-Cl-Phenyl
—CH2CF3


1867
4
4-Cl-Phenyl
—CH2CH2CF3


1868
4
4-Cl-Phenyl
cyclopropyl


1869
4
4-Cl-Phenyl
Cyclobutyl


1870
4
4-Cl-Phenyl
cyclopentyl


1871
4
4-Cl-Phenyl
cyclohexyl


1872
4
4-Cl-Phenyl
3-pyridyl


1873
4
4-Cl-Phenyl
1-methyl-1H-pyrazol-4-yl


1874
4
4-Cl-Phenyl
1H-imidazol-4-yl


1875
4
4-Cl-Phenyl
2-furanyl


1876
4
3-Br-Phenyl
Ethyl


1877
4
3-Br-Phenyl
n-propyl


1878
4
3-Br-Phenyl
Isopropyl


1879
4
3-Br-Phenyl
—CH2CH(CH3)2


1880
4
3-Br-Phenyl
CF3


1881
4
3-Br-Phenyl
—CH2CF3


1882
4
3-Br-Phenyl
—CH2CH2CF3


1883
4
3-Br-Phenyl
cyclopropyl


1884
4
3-Br-Phenyl
Cyclobutyl


1885
4
3-Br-Phenyl
cyclopentyl


1886
4
3-Br-Phenyl
cyclohexyl


1887
4
3-Br-Phenyl
3-pyridyl


1888
4
3-Br-Phenyl
1-methyl-1H-pyrazol-4-yl


1889
4
3-Br-Phenyl
1H-imidazol-4-yl


1890
4
3-Br-Phenyl
2-furanyl


1891
4
2-CF3-Phenyl
Ethyl


1892
4
2-CF3-Phenyl
n-propyl


1893
4
2-CF3-Phenyl
Isopropyl


1894
4
2-CF3-Phenyl
—CH2CH(CH3)2


1895
4
2-CF3-Phenyl
CF3


1896
4
2-CF3-Phenyl
—CH2CF3


1897
4
2-CF3-Phenyl
—CH2CH2CF3


1898
4
2-CF3-Phenyl
cyclopropyl


1899
4
2-CF3-Phenyl
Cyclobutyl


1900
4
2-CF3-Phenyl
cyclopentyl


1901
4
2-CF3-Phenyl
cyclohexyl


1902
4
2-CF3-Phenyl
3-pyridyl


1903
4
2-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


1904
4
2-CF3-Phenyl
1H-imidazol-4-yl


1905
4
2-CF3-Phenyl
2-furanyl


1906
4
4-CF3-Phenyl
Ethyl


1907
4
4-CF3-Phenyl
n-propyl


1908
4
4-CF3-Phenyl
Isopropyl


1909
4
4-CF3-Phenyl
—CH2CH(CH3)2


1910
4
4-CF3-Phenyl
CF3


1911
4
4-CF3-Phenyl
—CH2CF3


1912
4
4-CF3-Phenyl
—CH2CH2CF3


1913
4
4-CF3-Phenyl
cyclopropyl


1914
4
4-CF3-Phenyl
Cyclobutyl


1915
4
4-CF3-Phenyl
cyclopentyl


1916
4
4-CF3-Phenyl
cyclohexyl


1917
4
4-CF3-Phenyl
3-pyridyl


1918
4
4-CF3-Phenyl
1-methyl-1H-pyrazol-4-yl


1919
4
4-CF3-Phenyl
1H-imidazol-4-yl


1920
4
4-CF3-Phenyl
2-furanyl


1921
4
3-iPr-Phenyl
Ethyl


1922
4
3-iPr-Phenyl
n-propyl


1923
4
3-iPr-Phenyl
Isopropyl


1924
4
3-iPr-Phenyl
—CH2CH(CH3)2


1925
4
3-iPr-Phenyl
CF3


1926
4
3-iPr-Phenyl
—CH2CF3


1927
4
3-iPr-Phenyl
—CH2CH2CF3


1928
4
3-iPr-Phenyl
cyclopropyl


1929
4
3-iPr-Phenyl
Cyclobutyl


1930
4
3-iPr-Phenyl
cyclopentyl


1931
4
3-iPr-Phenyl
cyclohexyl


1932
4
3-iPr-Phenyl
3-pyridyl


1933
4
3-iPr-Phenyl
1-methyl-1H-pyrazol-4-yl


1934
4
3-iPr-Phenyl
1H-imidazol-4-yl


1935
4
3-iPr-Phenyl
2-furanyl


1936
4
2-morpholino-phenyl
Ethyl


1937
4
2-morpholino-phenyl
n-propyl


1938
4
2-morpholino-phenyl
isopropyl


1939
4
2-morpholino-phenyl
—CH2CH(CH3)2


1940
4
2-morpholino-phenyl
CF3


1941
4
2-morpholino-phenyl
—CH2CF3


1942
4
2-morpholino-phenyl
—CH2CH2CF3


1943
4
2-morpholino-phenyl
cyclopropyl


1944
4
2-morpholino-phenyl
Cyclobutyl


1945
4
2-morpholino-phenyl
cyclopentyl


1946
4
2-morpholino-phenyl
cyclohexyl


1947
4
2-morpholino-phenyl
3-pyridyl


1948
4
2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1949
4
2-morpholino-phenyl
1H-imidazol-4-yl


1950
4
2-morpholino-phenyl
2-furanyl


1951
4
4-morpholino-phenyl
ethyl


1952
4
4-morpholino-phenyl
n-propyl


1953
4
4-morpholino-phenyl
isopropyl


1954
4
4-morpholino-phenyl
—CH2CH(CH3)2


1955
4
4-morpholino-phenyl
CF3


1956
4
4-morpholino-phenyl
—CH2CF3


1957
4
4-morpholino-phenyl
—CH2CH2CF3


1958
4
4-morpholino-phenyl
cyclopropyl


1959
4
4-morpholino-phenyl
Cyclobutyl


1960
4
4-morpholino-phenyl
cyclopentyl


1961
4
4-morpholino-phenyl
cyclohexyl


1962
4
4-morpholino-phenyl
3-pyridyl


1963
4
4-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1964
4
4-morpholino-phenyl
1H-imidazol-4-yl


1965
4
4-morpholino-phenyl
2-furanyl


1966
4
4-methyl-2-morpholino-phenyl
ethyl


1967
4
4-methyl-2-morpholino-phenyl
n-propyl


1968
4
4-methyl-2-morpholino-phenyl
isopropyl


1969
4
4-methyl-2-morpholino-phenyl
—CH2CH(CH3)2


1970
4
4-methyl-2-morpholino-phenyl
CF3


1971
4
4-methyl-2-morpholino-phenyl
—CH2CF3


1972
4
4-methyl-2-morpholino-phenyl
—CH2CH2CF3


1973
4
4-methyl-2-morpholino-phenyl
Cyclopropyl


1974
4
4-methyl-2-morpholino-phenyl
Cyclobutyl


1975
4
4-methyl-2-morpholino-phenyl
Cyclopentyl


1976
4
4-methyl-2-morpholino-phenyl
Cyclohexyl


1977
4
4-methyl-2-morpholino-phenyl
3-pyridyl


1978
4
4-methyl-2-morpholino-phenyl
1-methyl-1H-pyrazol-4-yl


1979
4
4-methyl-2-morpholino-phenyl
1H-imidazol-4-yl


1980
4
4-methyl-2-morpholino-phenyl
2-furanyl


1981
1
naphthylen-1-yl
Ethyl


1982
1
naphthylen-1-yl
n-propyl


1983
1
naphthylen-1-yl
Isopropyl


1984
1
naphthylen-1-yl
—CH2CH(CH3)2


1985
1
naphthylen-1-yl
CF3


1986
1
naphthylen-1-yl
—CH2CF3


1987
1
naphthylen-1-yl
—CH2CH2CF3


1988
1
naphthylen-1-yl
Cyclopropyl


1989
1
naphthylen-1-yl
Cyclobutyl


1990
1
naphthylen-1-yl
Cyclopentyl


1991
1
naphthylen-1-yl
Cyclohexyl


1992
1
naphthylen-1-yl
3-pyridyl


1993
1
naphthylen-1-yl
1-methyl-1H-pyrazol-4-yl


1994
1
naphthylen-1-yl
1H-imidazol-4-yl


1995
1
naphthylen-1-yl
2-furanyl


1996
1
naphthylen-2-yl
Ethyl


1997
1
naphthylen-2-yl
n-propyl


1998
1
naphthylen-2-yl
Isopropyl


1999
1
naphthylen-2-yl
—CH2CH(CH3)2


2000
1
naphthylen-2-yl
CF3


2001
1
naphthylen-2-yl
—CH2CF3


2002
1
naphthylen-2-yl
—CH2CH2CF3


2003
1
naphthylen-2-yl
Cyclopropyl


2004
1
naphthylen-2-yl
Cyclobutyl


2005
1
naphthylen-2-yl
Cyclopentyl


2006
1
naphthylen-2-yl
Cyclohexyl


2007
1
naphthylen-2-yl
3-pyridyl


2008
1
naphthylen-2-yl
1-methyl-1H-pyrazol-4-yl


2009
1
naphthylen-2-yl
1H-imidazol-4-yl


2010
1
naphthylen-2-yl
2-furanyl


2011
2
naphthylen-1-yl
Ethyl


2012
2
naphthylen-1-yl
n-propyl


2013
2
naphthylen-1-yl
Isopropyl


2014
2
naphthylen-1-yl
—CH2CH(CH3)2


2015
2
naphthylen-1-yl
CF3


2016
2
naphthylen-1-yl
—CH2CF3


2017
2
naphthylen-1-yl
—CH2CH2CF3


2018
2
naphthylen-1-yl
Cyclopropyl


2019
2
naphthylen-1-yl
Cyclobutyl


2020
2
naphthylen-1-yl
Cyclopentyl


2021
2
naphthylen-1-yl
Cyclohexyl


2022
2
naphthylen-1-yl
3-pyridyl


2023
2
naphthylen-1-yl
1-methyl-1H-pyrazol-4-yl


2024
2
naphthylen-1-yl
1H-imidazol-4-yl


2025
2
naphthylen-1-yl
2-furanyl


2026
2
naphthylen-2-yl
Ethyl


2027
2
naphthylen-2-yl
n-propyl


2028
2
naphthylen-2-yl
Isopropyl


2029
2
naphthylen-2-yl
—CH2CH(CH3)2


2030
2
naphthylen-2-yl
CF3


2031
2
naphthylen-2-yl
—CH2CF3


2032
2
naphthylen-2-yl
—CH2CH2CF3


2033
2
naphthylen-2-yl
Cyclopropyl


2034
2
naphthylen-2-yl
Cyclobutyl


2035
2
naphthylen-2-yl
Cyclopentyl


2036
2
naphthylen-2-yl
Cyclohexyl


2037
2
naphthylen-2-yl
3-pyridyl


2038
2
naphthylen-2-yl
1-methyl-1H-pyrazol-4-yl


2039
2
naphthylen-2-yl
1H-imidazol-4-yl


2040
2
naphthylen-2-yl
2-furanyl


2041
3
naphthylen-1-yl
Ethyl


2042
3
naphthylen-1-yl
n-propyl


2043
3
naphthylen-1-yl
Isopropyl


2044
3
naphthylen-1-yl
—CH2CH(CH3)2


2045
3
naphthylen-1-yl
CF3


2046
3
naphthylen-1-yl
—CH2CF3


2047
3
naphthylen-1-yl
—CH2CH2CF3


2048
3
naphthylen-1-yl
Cyclopropyl


2049
3
naphthylen-1-yl
Cyclobutyl


2050
3
naphthylen-1-yl
Cyclopentyl


2051
3
naphthylen-1-yl
Cyclohexyl


2052
3
naphthylen-1-yl
3-pyridyl


2053
3
naphthylen-1-yl
1-methyl-1H-pyrazol-4-yl


2054
3
naphthylen-1-yl
1H-imidazol-4-yl


2055
3
naphthylen-1-yl
2-furanyl


2056
3
naphthylen-2-yl
Ethyl


2057
3
naphthylen-2-yl
n-propyl


2058
3
naphthylen-2-yl
Isopropyl


2059
3
naphthylen-2-yl
—CH2CH(CH3)2


2060
3
naphthylen-2-yl
CF3


2061
3
naphthylen-2-yl
—CH2CF3


2062
3
naphthylen-2-yl
—CH2CH2CF3


2063
3
naphthylen-2-yl
Cyclopropyl


2064
3
naphthylen-2-yl
Cyclobutyl


2065
3
naphthylen-2-yl
Cyclopentyl


2066
3
naphthylen-2-yl
Cyclohexyl


2067
3
naphthylen-2-yl
3-pyridyl


2068
3
naphthylen-2-yl
1-methyl-1H-pyrazol-4-yl


2069
3
naphthylen-2-yl
1H-imidazol-4-yl


2070
3
naphthylen-2-yl
2-furanyl


2071
4
naphthylen-1-yl
Ethyl


2072
4
naphthylen-1-yl
n-propyl


2073
4
naphthylen-1-yl
Isopropyl


2074
4
naphthylen-1-yl
—CH2CH(CH3)2


2075
4
naphthylen-1-yl
CF3


2076
4
naphthylen-1-yl
—CH2CF3


2077
4
naphthylen-1-yl
—CH2CH2CF3


2078
4
naphthylen-1-yl
Cyclopropyl


2079
4
naphthylen-1-yl
Cyclobutyl


2080
4
naphthylen-1-yl
Cyclopentyl


2081
4
naphthylen-1-yl
Cyclohexyl


2082
4
naphthylen-1-yl
3-pyridyl


2083
4
naphthylen-1-yl
1-methyl-1H-pyrazol-4-yl


2084
4
naphthylen-1-yl
1H-imidazol-4-yl


2085
4
naphthylen-1-yl
2-furanyl


2086
4
naphthylen-2-yl
Ethyl


2087
4
naphthylen-2-yl
n-propyl


2088
4
naphthylen-2-yl
Isopropyl


2089
4
naphthylen-2-yl
—CH2CH(CH3)2


2090
4
naphthylen-2-yl
CF3


2091
4
naphthylen-2-yl
—CH2CF3


2092
4
naphthylen-2-yl
—CH2CH2CF3


2093
4
naphthylen-2-yl
Cyclopropyl


2094
4
naphthylen-2-yl
Cyclobutyl


2095
4
naphthylen-2-yl
Cyclopentyl


2096
4
naphthylen-2-yl
Cyclohexyl


2097
4
naphthylen-2-yl
3-pyridyl


2098
4
naphthylen-2-yl
1-methyl-1H-pyrazol-4-yl


2099
4
naphthylen-2-yl
1H-imidazol-4-yl


2100
4
naphthylen-2-yl
2-furanyl









For the purposes of demonstrating the manner in which the compounds of the present invention are named and referred to herein, the compound having the formula:




embedded image


has the chemical name 8-(methylsulfonyl)-3-(2-(4-phenylpiperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one.


For the purposes of demonstrating the manner in which the compounds of the present invention are named and referred to herein, the compound having the formula:




embedded image


has the chemical name 8-(methylsulfonyl)-3-(2-(5-phenylhexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one.


For the purposes of demonstrating the manner in which the compounds of the present invention are named and referred to herein, the compound having the formula:




embedded image


has the chemical name 8-(methylsulfonyl)-3-(2-(4-phenylpiperidin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one


For the purposes of the present invention, a compound depicted by the racemic formula, for example:




embedded image


will stand equally well for either of the two enantiomers having the formula:




embedded image


or the formula:




embedded image


or mixtures thereof, or in the case where a second chiral center is present, all diastereomers.


In all of the embodiments provided herein, examples of suitable optional substituents are not intended to limit the scope of the claimed invention. The compounds of the invention may contain any of the substituents, or combinations of substituents, provided herein.


Process for preparing the 5-hydroxytryptamine receptor 7 activity modulators of the invention


The present invention further relates to a process for preparing the 5-hydroxytryptamine receptor 7 activity modulators of the present invention.


Compounds of the present teachings can be prepared in accordance with the procedures outlined herein, from commercially available starting materials, compounds known in the literature, or readily prepared intermediates, by employing standard synthetic methods and procedures known to those skilled in the art. Standard synthetic methods and procedures for the preparation of organic molecules and functional group transformations and manipulations can be readily obtained from the relevant scientific literature or from standard textbooks in the field. It will be appreciated that where typical or preferred process conditions (i.e., reaction temperatures, times, mole ratios of reactants, solvents, pressures, etc.) are given, other process conditions can also be used unless otherwise stated. Optimum reaction conditions can vary with the particular reactants or solvent used, but such conditions can be determined by one skilled in the art by routine optimization procedures. Those skilled in the art of organic synthesis will recognize that the nature and order of the synthetic steps presented can be varied for the purpose of optimizing the formation of the compounds described herein.


The processes described herein can be monitored according to any suitable method known in the art. For example, product formation can be monitored by spectroscopic means, such as nuclear magnetic resonance spectroscopy (e.g., 1H or 13C), infrared spectroscopy, spectrophotometry (e.g., UV-visible), mass spectrometry, or by chromatography such as high pressure liquid chromatograpy (HPLC), gas chromatography (GC), gel-permeation chromatography (GPC), or thin layer chromatography (TLC).


Preparation of the compounds can involve protection and deprotection of various chemical groups. The need for protection and deprotection and the selection of appropriate protecting groups can be readily determined by one skilled in the art. The chemistry of protecting groups can be found, for example, in Greene et al., Protective Groups in Organic Synthesis, 2d. Ed. (Wiley & Sons, 1991), the entire disclosure of which is incorporated by reference herein for all purposes.


The reactions or the processes described herein can be carried out in suitable solvents which can be readily selected by one skilled in the art of organic synthesis. Suitable solvents typically are substantially nonreactive with the reactants, intermediates, and/or products at the temperatures at which the reactions are carried out, i.e., temperatures that can range from the solvent's freezing temperature to the solvent's boiling temperature. A given reaction can be carried out in one solvent or a mixture of more than one solvent. Depending on the particular reaction step, suitable solvents for a particular reaction step can be selected.


The compounds of these teachings can be prepared by methods known in the art of organic chemistry. The reagents used in the preparation of the compounds of these teachings can be either commercially obtained or can be prepared by standard procedures described in the literature. For example, compounds of the present invention can be prepared according to the method illustrated in the General Synthetic Schemes:


General Synthetic Schemes for Preparation of Compounds

The reagents used in the preparation of the compounds of this invention can be either commercially obtained or can be prepared by standard procedures described in the literature. In accordance with this invention, compounds in the genus may be produced by one of the following reaction schemes. Accordingly, the invention further features any of the synthetic intermediates or processes as described herein.


Compounds of the disclosure may be prepared according to the process outlined in Scheme 1—




embedded image


A suitably substituted compound of formula (1), a known compound or a compound prepared by known methods wherein PG is a protecting selected from the group consisting of benzyl, tert-butyl carbonate, benzyl carbonate, and tert-butyldimethylsilyl, is reacted with a compound of the formula (2), a known compound or a compound prepared by known methods, in the presence of BnNEt3Cl, in the presence of a base such as potassium carbonate, sodium carbonate, cesium carbonate, lithium carbonate, sodium hydroxide, potassium hydroxide, cesium hydroxide, lithium hydroxide, and the like, in the presence of a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, acetonitrile, methanol, ethanol, isopropanol, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation, to provide a compounds of the formula (3). A compounds of the formula (3) is reacted with a compounds of the formula (4) a known compound or compound prepared by known methods in which Z1 is selected from the group consisting of methyl, trifluoromethyl, para-tolyl, and para-NO2-phenyl, in the presence of a base such as pyridine, 2,6-dimethyl pyridine, 2,6-di-tert-butyl pyridine, triethylamine, diisopropylethyl amine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (5). A compound of the formula (5) is reacted with a base such as potassium carbonate, sodium carbonate, cesium carbonate, lithium carbonate, and the like, in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, acetonitrile, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (6)




embedded image


A compound of formula (6) is reacted with a compound of the formula (7), a known compound or a compound prepared by known methods, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (8). A compound of the formula (8) is reacted with an acid such as hydrochloric acid, hydrobromic acid, sulfuric acid, para-toluenesulfonic acid, acetic acid, trifluoracetic acid, and the like, in a solvent such as benzene, toluene, para-xylene, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, acetonitrile, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (9). A compound of the formula (9) is reacted with a compound of the formula (10), a known compound or a compound prepared by known methods wherein LG is selected from the group consisting of bromine, chlorine, methansulfonate, and para-tolylsufonate, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (11).




embedded image


A compound of formula (11) is reacted with sodium in the presence of naphthalene in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (12). A compound of the formula (12) is reacted with hydrogen gas in the presence of a palladium catalyst such as palladium on carbon, palladium on barium sulfate, palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), and the like, in an organic solvent such as methanol, ethanol, ethyl acetate, tetrahydrofuran, 1,4-dioxane, dichloromethane, chloroform, 1,2-dichloroethane, N,N-dimethylformamide, and the like, optionally with heating, to provide a compound of the formula (13). Alternatively, a compound of the formula (12) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (13). Alternatively, a compound of the formula (12) is reacted with tetrabutyl ammonium fluoride in the presence of a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (13). A compound of the (13) is reacted with carbon tetrabromide in the presence of triphenylphosphine, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (14). A compound of the formula (14) is reacted with a compound of the formula (15), a known compound or a compound prepared by known methods, in the presence of a base such as sodium carbonate, potassium carbonate, lithium carbonate, sodium bicarbonate, potassium bicarbonate, lithium bicarbonate, triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (16).




embedded image


A compound of formula (6) is reacted with a compound of the formula (17), a known compound or a compound prepared by known methods, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (18). A compound of the formula (18) is reacted with an acid such as hydrochloric acid, hydrobromic acid, sulfuric acid, para-toluenesulfonic acid, acetic acid, trifluoracetic acid, and the like, in a solvent such as benzene, toluene, para-xylene, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, acetonitrile, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (19). A compound of the formula (19) is reacted with a compound of the formula (20), a known compound or a compound prepared by known methods wherein LG is selected from the group consisting of bromine, chlorine, methansulfonate, and para-tolylsufonate, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (21). A compound of the formula (21) is reacted with a compound of the formula (22), a known compound or a compound prepared by known methods wherein LG is selected from the group consisting of bromine, chlorine, methansulfonate, and para-tolylsufonate, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (11).




embedded image


A compound of the formula (19) is reacted with a compound of the formula (23), a known compound or a compound prepared by known methods wherein LG is selected from the group consisting of bromine, chlorine, methansulfonate, and para-tolylsufonate and wherein Q1 is selected from the group consisting of 1 and 2, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (24). A compound of the formula (24) is reacted with a compound of the formula (25), a known compound or a compound prepared by known methods wherein LG is selected from the group consisting of bromine, chlorine, methansulfonate, and para-tolylsufonate and wherein Q2 is selected from the group consisting of 1 and 2, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (26). A compound of the formula (26) is reacted with a ruthenium catalyst such as benzylidene-bis(tricyclohexylphosphine)dichlororuthenium, (1,3-Bis(2,4,6-trimethylphenyl)-2-imidazolidinylidene)dichloro(phenylmethylene)(tricyclohexyl phosphine)ruthenium, (1,3-bis-(2,4,6-trime thylphenyl)-2-imidazolidinylidene)dichloro(o-isopropoxy phenylmethylene)ruthenium, dichloro(2-isopropoxyphenylme thylene)(tricyclohexylphosphine) ruthenium(II), [1,3-bis(2-methylphenyl)-2-imidazolidinylidene]dichloro(phenylme thylene) (tricyclohexyl phosphine) ruthenium(II), dichloro[1,3-bis(2,4,6-trimethylphenyl)-2-imidazolidinylidene](benzylidene) bis(3-bromopyridine)ruthenium(II), dichloro[1,3-bis(2,4,6-trimethylphenyl)-2-imidazolidinylidene](3-methyl-2-butenylidene) (tricyclohexylphosphine)ruthenium(II), dichloro[1,3-bis(2-methylphenyl)-2-imidazolidinylidene] (2-isopropoxyphenylmethylene)ruthenium(II), [1,3-dimesityl-2-imidazolidinylidene]dichloro [3-(2-pyridinyl)propylidene]ruthenium(II), dichloro[1,3-bis(2,6-isopropylphenyl)-2-imidazolidinylidene] (2-isopropoxyphenylmethylene)ruthenium(II), dichloro(tricyclohexylphosphine) [(tricyclohexylphosphoranyl)methylidene]ruthenium tetrafluoroborate, dichloro[1,3-bis(2,4,6-trimethyl phenyl)-2-imidazolidinylidene][(tricyclohexylphosphoranyl)methylidene]ruthenium(II) tetrafluoroborate, [2-(1-methylethoxy-O)phenylme thyl-C](nitrato-O,O′){rel-(2R,5R,7R)-adamanlane-2,1-diyl[3-(2,4,6-trimethylphenyl)-1-imidazolidinyl-2-ylidene]}ruthenium, dichloro[1,3-bis(2,6-isopropylphenyl)-2-imidazolidinylidene] (benzylidene)(tricyclohexylphosphine)ruthenium(II), [1,3-bis(2-methylphenyl)-2-imidazolidinylidene]dichloro(phenylmethylene)(tricyclohexylphosphine)ruthenium(II), dichloro[1,3-bis(2,4,6-trimethylphenyl)-2-imidazolidinylidene][3-(2-pyridinyl)propylidene]ruthenium(II), and the like in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (27).




embedded image


A compound of the formula (27) is reacted with hydrogen gas in the presence of a palladium catalyst such as palladium on carbon, palladium on barium sulfate, palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), and the like, in an organic solvent such as methanol, ethanol, ethyl acetate, tetrahydrofuran, 1,4-dioxane, dichloromethane, chloroform, 1,2-dichloroethane, N,N-dimethylformamide, and the like, optionally with heating, to provide a compound of the formula (28). A compound of the formula (28) is reacted with hydrogen gas in the presence of a palladium catalyst such as palladium on carbon, palladium on barium sulfate, palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), and the like, in an organic solvent such as methanol, ethanol, ethyl acetate, tetrahydrofuran, 1,4-dioxane, dichloromethane, chloroform, 1,2-dichloroethane, N,N-dimethylformamide, and the like, optionally with heating, to provide a compound of the formula (29). Alternatively, a compound of the formula (28) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (29). Alternatively, a compound of the formula (28) is reacted with tetrabutyl ammonium fluoride in the presence of a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (29). A compound of formula (29) is reacted with sodium in the presence of naphthalene in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (30).




embedded image


Alternatively, a compound of formula (27) is reacted with sodium in the presence of naphthalene in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (31). A compound of the formula (31) is reacted with hydrogen gas in the presence of a palladium catalyst such as palladium on carbon, palladium on barium sulfate, palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), and the like, in an organic solvent such as methanol, ethanol, ethyl acetate, tetrahydrofuran, 1,4-dioxane, dichloromethane, chloroform, 1,2-dichloroethane, N,N-dimethylformamide, and the like, optionally with heating, to provide a compound of the formula (32). A compound of the formula (32) is reacted with hydrogen gas in the presence of a palladium catalyst such as palladium on carbon, palladium on barium sulfate, palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), and the like, in an organic solvent such as methanol, ethanol, ethyl acetate, tetrahydrofuran, 1,4-dioxane, dichloromethane, chloroform, 1,2-dichloroethane, N,N-dimethylformamide, and the like, optionally with heating, to provide a compound of the formula (30). Alternatively, a compound of the formula (32) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (30). Alternatively, a compound of the formula (32) is reacted with tetrabutyl ammonium fluoride in the presence of a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (30).




embedded image


A compound of the (30) is reacted with carbon tetrabromide in the presence of triphenylphosphine, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (33). A compound of the formula (33) is reacted with a compound of the formula (34), a known compound or a compound prepared by known methods, in the presence of a base such as sodium carbonate, potassium carbonate, lithium carbonate, sodium bicarbonate, potassium bicarbonate, lithium bicarbonate, triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (35).




embedded image


A compound of the formula (31) is reacted with hydrogen gas in the presence of a palladium catalyst such as palladium on carbon, palladium on barium sulfate, palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), and the like, in an organic solvent such as methanol, ethanol, ethyl acetate, tetrahydrofuran, 1,4-dioxane, dichloromethane, chloroform, 1,2-dichloroethane, N,N-dimethylformamide, and the like, optionally with heating, to provide a compound of the formula (36). Alternatively, a compound of the formula (31) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (36). Alternatively, a compound of the formula (31) is reacted with tetrabutyl ammonium fluoride in the presence of a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (36). A compound of the (36) is reacted with carbon tetrabromide in the presence of triphenylphosphine, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (37). A compound of the formula (37) is reacted with a compound of the formula (38), a known compound or a compound prepared by known methods, in the presence of a base such as sodium carbonate, potassium carbonate, lithium carbonate, sodium bicarbonate, potassium bicarbonate, lithium bicarbonate, triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (39).




embedded image


A compound of the formula (26) is reacted with a compound of the formula ozone in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation. The resulting material is then treated with triphenyl phosphine in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation to provide a compound of the formula (40). Alternatively, a compound of the formula (26) is reacted with a compound of the formula ozone in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation. The resulting material is then treated with dimethyl sulfide in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxye thane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation to provide a compound of the formula (40). Alternatively, a compound of the formula (26) is reacted with ruthenium chloride in the presence of sodium periodate in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating optionally with microwave irradiation to provide a compound of the formula (40). Alternatively, a compound of the formula (26) is reacted with potassium osmate dehydrate in the presence of potassium ferricyanide, optionally in the presence of potassium carbonate, optionally in the presence of a base such as potassium hydroxide, sodium hydroxide, lithium hydroxide, and the like, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating optionally with microwave irradiation to provide a compound of the formula (40). Alternatively, a compound of the formula (26) is reacted with osmium tetraoxide in the presence of sodium periodate, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of a base such as pyridine, 2,6-lutidine, 2,6-di-tert-butylpyridine, and the like, optionally in the presence of water, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (40). Alternatively, a compound of the formula (26) is reacted with osmium tetraoxide in the presence of N-methylmorpholine N-oxide, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (40). A compound of the formula (40) is reacted with benzyl amine in the presence of a reducing agent such as sodium borohydride, sodium triacetoxy borohydride, sodium cyanoborohydride, lithium borohydride, lithium triacetoxy borohydride, lithium cyanoborohydride and the like, in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (41). A compound of the formula (41) is reacted with hydrogen gas in the presence of a palladium catalyst such as palladium on carbon, palladium on barium sulfate, palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), and the like, in an organic solvent such as methanol, ethanol, ethyl acetate, tetrahydrofuran, 1,4-dioxane, dichloromethane, chloroform, 1,2-dichloroethane, N,N-dimethylformamide, and the like, to provide a compound of the formula (42).




embedded image


A compound of the formula (42) is reacted with Di-tert-butyl dicarbonate in the presence of a base such as such as pyridine, 2,6-lutidine, triethylamine, diisopropylethylamine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (43). A compound of formula (43) is reacted with sodium in the presence of naphthalene in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (44). A compound of the formula (44) is reacted with hydrogen gas in the presence of a palladium catalyst such as palladium on carbon, palladium on barium sulfate, palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), and the like, in an organic solvent such as methanol, ethanol, ethyl acetate, tetrahydrofuran, 1,4-dioxane, dichloromethane, chloroform, 1,2-dichloroethane, N,N-dimethylformamide, and the like, optionally with heating, to provide a compound of the formula (45). Alternatively, a compound of the formula (44) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (45). Alternatively, a compound of the formula (44) is reacted with tetrabutyl ammonium fluoride in the presence of a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (45).




embedded image


A compound of the (45) is reacted with carbon tetrabromide in the presence of triphenylphosphine, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (46). A compound of the formula (46) is reacted with a compound of the formula (47), a known compound or a compound prepared by known methods, in the presence of a base such as sodium carbonate, potassium carbonate, lithium carbonate, sodium bicarbonate, potassium bicarbonate, lithium bicarbonate, triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (48). A compound of the formula (48) is reacted with an acid such as trifluoroacetic acid, formic acid, acetic acid, hydrochloric acid, sulfuric acid, and the like, optionally in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (49).




embedded image


A compound of the formula (49) is reacted with a compound of the formula (50), a known compound or a compound prepared by known methods, in the presence of a base such as triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dime thoxyethane, N,N-dimethylformamide, N,N-dime thylacetamide, acetonitrile, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (51).




embedded image


A compound of the formula (49) is reacted with a compound of the formula (52), a known compound or a compound prepared by known methods, in the presence of a base such as triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dime thoxyethane, N,N-dimethylformamide, N,N-dime thylacetamide, acetonitrile, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (53).




embedded image


A compound of the formula (49) is reacted with a compound of the formula (54), a known compound or a compound prepared by known methods, in the presence of a base such as triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dime thoxyethane, N,N-dimethylformamide, N,N-dime thylacetamide, acetonitrile, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (55).




embedded image


A compound of the formula (49) is reacted with a compound of the formula (56), a known compound or a compound prepared by known methods, in the presence of a base such as triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dime thoxyethane, N,N-dimethylformamide, N,N-dime thylacetamide, acetonitrile, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (57).




embedded image


A compound of the formula (49) is reacted with a compound of the formula (58), a known compound or a compound prepared by known methods, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dime thoxyethane, N,N-dimethylformamide, N,N-dime thylacetamide, acetonitrile, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (59).




embedded image


A compound of the formula (49) is reacted with a compound of the formula (60), a known compound or a compound prepared by known methods, in the presence of a base such as triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dime thoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (61).




embedded image


A compound of the formula (62) is reacted with a compound of the formula ozone in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation. The resulting material is then treated with triphenyl phosphine in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation to provide a compound of the formula (63). Alternatively, a compound of the formula (62) is reacted with a compound of the formula ozone in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation. The resulting material is then treated with dimethyl sulfide in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation to provide a compound of the formula (63). Alternatively, a compound of the formula (62) is reacted with ruthenium chloride in the presence of sodium periodate in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating optionally with microwave irradiation to provide a compound of the formula (63). Alternatively, a compound of the formula (62) is reacted with potassium osmate dehydrate in the presence of potassium ferricyanide, optionally in the presence of potassium carbonate, optionally in the presence of a base such as potassium hydroxide, sodium hydroxide, lithium hydroxide, and the like, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating optionally with microwave irradiation to provide a compound of the formula (63). Alternatively, a compound of the formula (62) is reacted with osmium tetraoxide in the presence of sodium periodate, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of a base such as pyridine, 2,6-lutidine, 2,6-di-tert-butylpyridine, and the like, optionally in the presence of water, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (63). Alternatively, a compound of the formula (62) is reacted with osmium tetraoxide in the presence of N-methylmorpholine N-oxide, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (63).




embedded image


A compound of the formula (64) is reacted with a compound of the formula ozone in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation. The resulting material is then treated with triphenyl phosphine in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation to provide a compound of the formula (65). Alternatively, a compound of the formula (64) is reacted with a compound of the formula ozone in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation. The resulting material is then treated with dimethyl sulfide in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation to provide a compound of the formula (65). Alternatively, a compound of the formula (64) is reacted with ruthenium chloride in the presence of sodium periodate in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating optionally with microwave irradiation to provide a compound of the formula (65). Alternatively, a compound of the formula (64) is reacted with potassium osmate dehydrate in the presence of potassium ferricyanide, optionally in the presence of potassium carbonate, optionally in the presence of a base such as potassium hydroxide, sodium hydroxide, lithium hydroxide, and the like, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating optionally with microwave irradiation to provide a compound of the formula (65). Alternatively, a compound of the formula (64) is reacted with osmium tetraoxide in the presence of sodium periodate, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of a base such as pyridine, 2,6-lutidine, 2,6-di-tert-butylpyridine, and the like, optionally in the presence of water, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (65). Alternatively, a compound of the formula (64) is reacted with osmium tetraoxide in the presence of N-methylmorpholine N-oxide, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (65). A compound of the formula (65) is reacted with benzyl amine in the presence of a reducing agent such as sodium borohydride, sodium triacetoxy borohydride, sodium cyanoborohydride, lithium borohydride, lithium triacetoxy borohydride, lithium cyanoborohydride and the like, in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (66). A compound of the formula (66) is reacted with hydrogen gas in the presence of a palladium catalyst such as palladium on carbon, palladium on barium sulfate, palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), and the like, in an organic solvent such as methanol, ethanol, ethyl acetate, tetrahydrofuran, 1,4-dioxane, dichloromethane, chloroform, 1,2-dichloroethane, N,N-dimethylformamide, and the like, to provide a compound of the formula (67).




embedded image


A compound of the formula (68) is reacted with a compound of the formula ozone in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation. The resulting material is then treated with a reducing agent such as sodium borohydride, sodium triacetoxy borohydride, sodium cyanoborohydride, lithium borohydride, lithium triacetoxy borohydride, lithium cyanoborohydride and the like, in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (69). Alternatively, a compound of the formula (68) is reacted with a compound of the formula ozone in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation. The resulting material is then treated with dimethyl sulfide in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation to provide a compound of the formula (68a). Alternatively, a compound of the formula (68) is reacted with ruthenium chloride in the presence of sodium periodate in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating optionally with microwave irradiation to provide a compound of the formula (68a). Alternatively, a compound of the formula (68) is reacted with potassium osmate dehydrate in the presence of potassium ferricyanide, optionally in the presence of potassium carbonate, optionally in the presence of a base such as potassium hydroxide, sodium hydroxide, lithium hydroxide, and the like, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating optionally with microwave irradiation to provide a compound of the formula (68a). Alternatively, a compound of the formula (68) is reacted with osmium tetraoxide in the presence of sodium periodate, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of a base such as pyridine, 2,6-lutidine, 2,6-di-tert-butylpyridine, and the like, optionally in the presence of water, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (68a). Alternatively, a compound of the formula (68) is reacted with osmium tetraoxide in the presence of N-methylmorpholine N-oxide, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (68a). A compound of the formula (68a) is reacted with a reducing agent such as sodium borohydride, sodium triacetoxy borohydride, sodium cyanoborohydride, lithium borohydride, lithium triacetoxy borohydride, lithium cyanoborohydride and the like, in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (69). A compound of the (69) is reacted with carbon tetrabromide in the presence of triphenylphosphine, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (70). Alternatively, a compound of the formula (69) is reacted with bromine in the presence of triphenylphosphine, in the presence of a base such as pyridine 2,6-dimethyl pyridine, 2,6-di-tert-butyl pyridine, triethylamine, diisopropylethyl amine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (70). Alternatively, a compound of the formula (69) is reacted with dibromotriphenylphosphorane, optionally in the presence of a base such as pyridine 2,6-dimethyl pyridine, 2,6-di-tert-butyl pyridine, triethylamine, diisopropylethyl amine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (70). A compound of the formula (70) is reacted with sodium sulfide in the presence of a solvent such as ethanol, methanol, isopropanol, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (71).




embedded image


A compound of the formula (71) is reacted with hydrogen gas in the presence of a palladium catalyst such as palladium on carbon, palladium on barium sulfate, palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), and the like, in an organic solvent such as methanol, ethanol, ethyl acetate, tetrahydrofuran, 1,4-dioxane, dichloromethane, chloroform, 1,2-dichloroethane, N,N-dimethylformamide, and the like, optionally with heating, to provide a compound of the formula (72). Alternatively, a compound of the formula (71) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (72). Alternatively, a compound of the formula (71) is reacted with tetrabutyl ammonium fluoride in the presence of a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (72). A compound of the (72) is reacted with carbon tetrabromide in the presence of triphenylphosphine, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (73). A compound of the formula (73) is reacted with a compound of the formula (74), a known compound or a compound prepared by known methods, in the presence of a base such as sodium carbonate, potassium carbonate, lithium carbonate, sodium bicarbonate, potassium bicarbonate, lithium bicarbonate, triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (75).




embedded image


A compound of the formula (75) is reacted with an oxidizing agent such as m-chloroperoxybenzoic acid, monoperphthalic acid, peracetic acid, perpropionic acid, pertrifluoroacetic acid, potassium periodate, sodium metaperiodate, sodium perborate, potassium peroxymonosulfate (Oxon®), potassium peroxydisulfate, dimethyldioxirane, and the like, in the presence of a solvent such as tetrahydrofuran, ether, 1,4-dioxane, acetone, acetonitrile, methanol, ethanol, isopropanol, water, and the like, optionally with heating, optionally with microwave irradiation to provide compounds of the formula (76) and (77). Alternatively, a formula of the compound (75) is reacted with a sulfoxide such as diphenyl sulfoxide, dimethyl sulfoxide, and the like, in the presence of a rhenium catalyst such as ReOCl3(PPh3)2, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, chloroform, tetrahydrofuran, ether, 1,4-dioxane, acetone, acetonitrile, and the like, optionally with heating, optionally with microwave irradiation to provide compounds of the formula (76) and (77). Alternatively, a formula of the compound (75) is reacted with a urea hydrogen peroxide complex in the presence of a rhenium catalyst such as ReOCl3(PPh3)2, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, chloroform, tetrahydrofuran, ether, 1,4-dioxane, acetone, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide compounds of the formula (76) and (77). Alternatively, a compound of the formula (75) is reacted with hydrogen peroxide in the presence titanium (IV) isopropoxide-diethyltartarate, optionally in the presence of an amino alcohol such as 2-amino-3-phenylpropan-1-ol, 2-amino-4-methylpentan-1-ol, 2-amino-4-(methylthio)butan-1-ol, 2-aminopropan-1-ol, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, chloroform, tetrahydrofuran, ether, 1,4-dioxane, acetone, acetonitrile, N,N-dimethylformamide, and the like optionally with heating, optionally with microwave irradiation to provide compounds of the formula (76) and (77). It is understood that one skilled in the art would readily understand that the ratio of products (76) and (77) will be controlled by the amount of oxidant added and would adjust the amount of oxidant accordingly to produce the desired ration of products.




embedded image


A suitably substituted compound of the formula (78), a known compound or a compound prepared by known methods wherein PG is a protecting selected from the group consisting of benzyl, tert-butyl carbonate, benzyl carbonate, and tert-butyldimethylsilyl, is reacted with a compound of the formula (79), a known compound or a compound prepared by known methods in which PG1 is a protecting group selected from the group consisting of benzyl, tert-butyl carbonate, benzyl carbonate, and tert-butyldimethylsilyl, and wherein the LG is selected from the group consisting of bromine, chlorine, methansulfonate, and para-tolylsufonate, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (80). A compound of the formula (80) is reacted with hydrogen gas in the presence of a palladium catalyst such as palladium on carbon, palladium on barium sulfate, palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), and the like, in an organic solvent such as methanol, ethanol, ethyl acetate, tetrahydrofuran, 1,4-dioxane, dichloromethane, chloroform, 1,2-dichloroethane, N,N-dimethylformamide, and the like, optionally with heating, to provide a compound of the formula (81). Alternatively, a compound of the formula (80) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (81). Alternatively, a compound of the formula (80) is reacted with tetrabutyl ammonium fluoride in the presence of a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (81). A compound of the formula (81) is reacted with carbon tetrabromide in the presence of triphenylphosphine, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (82). Alternatively, a compound of the formula (81) is reacted with bromine in the presence of triphenylphosphine, in the presence of a base such as pyridine 2,6-dimethyl pyridine, 2,6-di-tert-butyl pyridine, triethylamine, diisopropylethyl amine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (82). Alternatively, a compound of the formula (81) is reacted with dibromotriphenylphosphorane, optionally in the presence of a base such as pyridine 2,6-dimethyl pyridine, 2,6-di-tert-butyl pyridine, triethylamine, diisopropylethyl amine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (82).




embedded image


A compound of the formula (82), is reacted with a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (83). A compound of formula (83) is reacted with sodium in the presence of naphthalene in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (84). A compound of the formula (84) is reacted with hydrogen gas in the presence of a palladium catalyst such as palladium on carbon, palladium on barium sulfate, palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), and the like, in an organic solvent such as methanol, ethanol, ethyl acetate, tetrahydrofuran, 1,4-dioxane, dichloromethane, chloroform, 1,2-dichloroethane, N,N-dimethylformamide, and the like, optionally with heating, to provide a compound of the formula (85). Alternatively, a compound of the formula (84) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (85). Alternatively, a compound of the formula (84) is reacted with tetrabutyl ammonium fluoride in the presence of a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (85).




embedded image


A compound of the formula (85) is reacted with carbon tetrabromide in the presence of triphenylphosphine, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (86). Alternatively, a compound of the formula (85) is reacted with bromine in the presence of triphenylphosphine, in the presence of a base such as pyridine 2,6-dimethyl pyridine, 2,6-di-tert-butyl pyridine, triethylamine, diisopropylethyl amine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (86). Alternatively, a compound of the formula (85) is reacted with dibromotriphenylphosphorane, optionally in the presence of a base such as pyridine 2,6-dimethyl pyridine, 2,6-di-tert-butyl pyridine, triethylamine, diisopropylethyl amine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (86). A compound of the formula (86) is reacted with a compound of the formula (87), a known compound or a compound prepared by known methods, in the presence of a base such as sodium carbonate, potassium carbonate, lithium carbonate, sodium bicarbonate, potassium bicarbonate, lithium bicarbonate, triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (88).




embedded image


Diethanolamine (89) is reacted with 4-nitrobenzenesulfonyl chloride (NosCl) in the presence of a base such as triethylamine, diisopropylethylamine, pyridine, 2,6-lutidine, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride and the like to provide a compound of the formula (90). A compound of the formula (90) is then reacted with a compound of the formula (91), a known compound or one prepared by known methods, in the presence of a base such as triethylamine, diisopropylethylamine, pyridine, 2,6-lutidine, and the like, in a solvent such as acetonitrile, methanol, ethanol, dimethyl formamide, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (92). A compound of the formula (92) is reacted with a thiophenol in the presence of a base such as sodium bicarbonate, potassium bicarbonate, lithium bicarbonate, sodium carbonate, potassium carbonate, lithium bicarbonate, sodium hydroxide, potassium hydroxide, lithium hydroxide, and the like, in the presence of a solvent such as tetrahydrofuran, ethyl ether, 1,4-dioxane, acetonitrile and the like, optionally in the presence of dimethylsulfoxide, optionally with heating, optionally with microwave irradiation, to provide a compound of the formula (93).




embedded image


A compound of the formula (94), a known compound or a compound prepared by known methods, is reacted with a compound of the formula (95), a known compound or a compound prepared by known methods in which X3 is selected from the group consisting of chlorine, bromine, iodine, and methanetrifluorosulfonate, in the presence of a base such as sodium tert-butoxide, lithium tert-butoxide, potassium tert-butoxide, and the like, optionally in the presence of a base such as triethylamine, diisopropylethyl amine, pyridine, 2,6-lutidine, and the like, in the presence of a palladium catalyst such as palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), tris(dibenzylideneacetone)dipalladium(0), and the like, in the presence of a solvent such as toluene, benzene, methylene chloride, 1,2-dichloroethae, tetrahydrofuran, 1,4-dioxane, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation, to provide a compound of the formula (96). A compound of the formula (96) is reacted with an acid such as trifluoroacetic acid, formic acid, acetic acid, hydrochloric acid, sulfuric acid, and the like, optionally in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (97).




embedded image


A compound of the formula (98), a known compound or a compound prepared by known methods, is reacted with a compound of the formula (99), a known compound or a compound prepared by known methods in which X3 is selected from the group consisting of chlorine, bromine, iodine, and methanetrifluorosulfonate, in the presence of a base such as sodium tert-butoxide, lithium tert-butoxide, potassium tert-butoxide, and the like, optionally in the presence of a base such as triethylamine, diisopropylethyl amine, pyridine, 2,6-lutidine, and the like, in the presence of a palladium catalyst such as palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), tris(dibenzylideneacetone)dipalladium(0), and the like, in the presence of a solvent such as toluene, benzene, methylene chloride, 1,2-dichloroethae, tetrahydrofuran, 1,4-dioxane, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation, to provide a compound of the formula (100). A compound of the formula (100) is reacted with an acid such as trifluoroacetic acid, formic acid, acetic acid, hydrochloric acid, sulfuric acid, and the like, optionally in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (101).




embedded image


A compound of the formula (102), a known compound or a compound prepared by known methods, is reacted with tert-butylchlorodimethylsilane in the presence of a base such as imidazole, 4-dimethylaminopyridine, potassium carbonate, sodium carbonate, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (103). A compound of the formula (103) is reacted with di-tert-butyl dicarbonate in the presence of 4-dimethylaminopyridine, in the presence of a base such as triethylamine, N,N-diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (104). A compound of the formula (104) is reacted with a compound of the formula (105), a known compound or a compound prepared by known methods wherein LG is selected from the group consisting of bromine, chlorine, methansulfonate, and para-tolylsufonate, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (106). A compound of the formula (106) is reacted with a compound of the formula (107), a known compound or a compound prepared by known methods wherein LG is selected from the group consisting of bromine, chlorine, methansulfonate, and para-tolylsufonate, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (108).




embedded image


A compound of the formula (108) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (109). A compound of the formula (109) is reacted with 4-methylbenzenesulfonyl chloride in the presence of 4-dimethylaminopyridine, in the presence of a base such as triethylamine, N,N-diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (110). A compound of the formula (110) is reacted with a compound of the formula (111), a known compound or a compound prepared by known methods, in the presence of a base such as sodium carbonate, potassium carbonate, lithium carbonate, sodium bicarbonate, potassium bicarbonate, lithium bicarbonate, triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (112).




embedded image


A compound of the formula (113), a known compound or a compound prepared by known methods, is reacted with 4-methylbenzenesulfonyl chloride in the presence of 4-dimethylaminopyridine, in the presence of a base such as triethylamine, N,N-diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (114). A compound of the formula (114) is reacted with a source of cyanide such as potassium cyanide, sodium cyanide, lithium cyanide, tetrabutylammonium cyanide, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (115). A compound of the formula (115) is reacted with an acid such as as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (116) where Rz is H. Alternatively, a compound of the formula of the formula (115) can be treated with acid and a suitable alcoholic solvent to provide the compound of the formula (116) that is a carboxylic acid ester (e.g., where Rz is a C1-6 alkyl): suitable conditions include using 6M HCl in methanol to provide ester compounds of the formula (116) where Rz is methyl. A compound of the formula (116) is reacted with a reducing agent such as sodium borohydride, sodium triacetoxy borohydride, sodium cyanoborohydride, lithium borohydride, lithium triacetoxy borohydride, lithium cyanoborohydride and the like, in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (117). A compound of the formula (117) is reacted with tert-butylchlorodimethylsilane in the presence of a base such as imidazole, 4-dimethylaminopyridine, potassium carbonate, sodium carbonate, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (118). A compound of the formula (118) is reacted with di-tert-butyl dicarbonate in the presence of 4-dimethylaminopyridine, in the presence of a base such as triethylamine, N,N-diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (119).




embedded image


A compound of the formula (119) is reacted with a compound of the formula (120), a known compound or a compound prepared by known methods wherein LG is selected from the group consisting of bromine, chlorine, methansulfonate, and para-tolylsufonate and wherein Q1 is selected from the group consisting of 1 and 2, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (121). A compound of the formula (121) is reacted with a compound of the formula (122), a known compound or a compound prepared by known methods wherein LG is selected from the group consisting of bromine, chlorine, methansulfonate, and para-tolylsufonate and wherein Q2 is selected from the group consisting of 1 and 2, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (123). A compound of the formula (123) is reacted with a ruthenium catalyst such as benzylidene-bis(tricyclohexylphosphine)dichlororuthenium, (1,3-Bis(2,4,6-trimethylphenyl)-2-imidazolidinylidene)dichloro(phenylme thylene)(tricyclohexyl phosphine)ruthenium, (1,3-bis-(2,4,6-trime thylphenyl)-2-imidazolidinylidene)dichloro(o-isopropoxy phenylme thylene)ruthenium, dichloro(2-isopropoxyphenylme thylene)(tricyclohexylphosphine) ruthenium(II), [1,3-bis(2-me thylphenyl)-2-imidazolidinylidene] dichloro(phenylme thylene) (tricyclohexyl phosphine) ruthenium(II), dichloro[1,3-bis(2,4,6-trimethylphenyl)-2-imidazolidinylidene](benzylidene) bis(3-bromopyridine)ruthenium(II), dichloro[1,3-bis(2,4,6-trimethylphenyl)-2-imidazolidinylidene](3-methyl-2-butenylidene) (tricyclohexylphosphine)ruthenium(II), dichloro [1,3-bis(2-methylphenyl)-2-imidazolidinylidene](2-isopropoxyphenylmethylene)ruthenium(II), [1,3-dime sityl-2-imidazolidinylidene] dichloro [3-(2-pyridinyl)propylidene]ruthenium(II), dichloro[1,3-bis(2,6-isopropylphenyl)-2-imidazolidinylidene](2-isopropoxyphenylmethylene)ruthenium(II), dichloro(tricyclohexylphosphine) [(tricyclohexylphosphoranyl)methylidene]ruthenium tetrafluoroborate, dichloro[1,3-bis(2,4,6-trimethyl phenyl)-2-imidazolidinylidene][(tricyclohexylphosphoranyl)methylidene]ruthenium(II) tetrafluoroborate, [2-(1-me thylethoxy-O)phenylme thyl-C](nitrato-O,O′){rel-(2R,5 R,7R)-adamanlane -2,1-diyl[3-(2,4,6-trimethylphenyl)-1-imidazolidinyl-2-ylidene]}ruthenium, dichloro[1,3-bis(2,6-isopropylphenyl)-2-imidazolidinylidene](benzylidene)(tricyclohexylphosphine)ruthenium(II), [1,3-bis(2-methylphenyl)-2-imidazolidinylidene]dichloro(phenylmethylene)(tricyclohexylphosphine)ruthenium(II), dichloro[1,3-bis(2,4,6-trimethylphenyl)-2-imidazolidinylidene][3-(2-pyridinyl)propylidene]ruthenium(II), and the like in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, dimethylsulfoxide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (124).




embedded image


A compound of the formula (124) is reacted with ozone in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation. The resulting material is then treated with triphenyl phosphine in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation to provide a compound of the formula (125). Alternatively, a compound of the formula (124) is reacted with a ozone in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation. The resulting material is then treated with dimethyl sulfide in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating optionally with microwave irradiation to provide a compound of the formula (125). Alternatively, a compound of the formula (124) is reacted with ruthenium chloride in the presence of sodium periodate in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating optionally with microwave irradiation to provide a compound of the formula (125). Alternatively, a compound of the formula (124) is reacted with potassium osmate dehydrate in the presence of potassium ferricyanide, optionally in the presence of potassium carbonate, optionally in the presence of a base such as potassium hydroxide, sodium hydroxide, lithium hydroxide, and the like, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating optionally with microwave irradiation to provide a compound of the formula (125). Alternatively, a compound of the formula (124) is reacted with osmium tetraoxide in the presence of sodium periodate, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of a base such as pyridine, 2,6-lutidine, 2,6-di-tert-butylpyridine, and the like, optionally in the presence of water, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (125). Alternatively, a compound of the formula (124) is reacted with osmium tetraoxide in the presence of N-methylmorpholine N-oxide, in the presence of a solvent such as methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, acetone, ethyl acetate, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally in the presence of water, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (125). A compound of the formula (125) is reacted with benzyl amine in the presence of a reducing agent such as sodium borohydride, sodium triacetoxy borohydride, sodium cyanoborohydride, lithium borohydride, lithium triacetoxy borohydride, lithium cyanoborohydride and the like, in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (126). A compound of the formula (126) is reacted with hydrogen gas in the presence of a palladium catalyst such as palladium on carbon, palladium on barium sulfate, palladium (II) acetate, tetrakis(triphenylphosphine)palladium(0), dichlorobis (triphenylphosphine)palladium(II), palladium on carbon, bis(acetonitrile)dichloropalladium(II), and the like, in an organic solvent such as methanol, ethanol, ethyl acetate, tetrahydrofuran, 1,4-dioxane, dichloromethane, chloroform, 1,2-dichloroethane, N,N-dimethylformamide, and the like, to provide a compound of the formula (127).




embedded image


A compound of the formula (127) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (128). A compound of the formula (128) is reacted with di-tert-butyl dicarbonate in the presence of 4-dimethylaminopyridine, in the presence of a base such as triethylamine, N,N-diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (129). A compound of the formula (129) is reacted with 4-methylbenzenesulfonyl chloride in the presence of 4-dimethylaminopyridine, in the presence of a base such as triethylamine, N,N-diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (130).




embedded image


A compound of the formula (130) is reacted with a compound of the formula (131), a known compound or a compound prepared by known methods, in the presence of a base such as sodium carbonate, potassium carbonate, lithium carbonate, sodium bicarbonate, potassium bicarbonate, lithium bicarbonate, triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (132). A compound of the formula (132) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (133).




embedded image


A compound of the formula (134) wherein n is selected from the group consisting 1 and 2, a known compound or a compound prepared by known methods, is reacted with 4-methylbenzenesulfonyl chloride in the presence of 4-dimethylaminopyridine, in the presence of a base such as triethylamine, N,N-diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (135). A compound of the formula (135) is reacted with di-tert-butyl malonate in the presence of a base such as potassium tert-butoxide, sodium tert-butoxide, lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (136). A compound of the formula (136) an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (137). A compound of the formula (137) is reacted with methanol in the presence of an acid such as hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, 1,2-dime thoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (138). Alternatively, a compound of the formula (137) is reacted with methanol in the presence of a coupling agent such as 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride, N,N′-dicyclohexylcarbodiimide, O-benzotriazole-N,N,N ,N′-tetramethyl-uronium-hexafluoro-phosphate, O-(7-azabenzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium hexafluorophosphate, benzotriazole-1-yl-oxy-tris-(dimethylamino)-phosphonium hexafluorophosphate, benzotriazol-1-yl-oxytripyrrolidinophosphonium hexafluorophosphate, and the like, optionally in the presence of a base such as triethylamine, diisopropylethylamine, pyridine, 2,6-lutidine, and the like, optionally in the presence of 4-N,N-dimethylaminopyridine, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (138). Alternatively, a compound of the formula (137) is reacted with (diazomethyl)trimethylsilane in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (138).




embedded image


A compound of the formula (138) is reacted with a reducing agent such as sodium borohydride, sodium triacetoxy borohydride, sodium cyanoborohydride, lithium borohydride, lithium triacetoxy borohydride, lithium cyanoborohydride and the like, in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (139). A compound of the formula (139) is reacted with tert-butylchlorodimethylsilane in the presence of a base such as imidazole, 4-dimethylaminopyridine, potassium carbonate, sodium carbonate, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (140). A compound of the formula (140) is reacted with di-tert-butyl dicarbonate in the presence of 4-dimethylaminopyridine, in the presence of a base such as triethylamine, N,N-diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (141). A compound of the formula (141) is reacted with a compound of the formula (142), a known compound or a compound prepared by known methods wherein LG is selected from the group consisting of bromine, chlorine, methansulfonate, and para-tolylsufonate, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (143). A compound of the formula (143) is reacted with a compound of the formula (144), a known compound or a compound prepared by known methods wherein LG is selected from the group consisting of bromine, chlorine, methansulfonate, and para-tolylsufonate, in the presence of a base such as lithium diisopropylamide, sodium diisopropylamide, potassium diisopropylamide, lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, potassium bis(trimethylsilyl)amide, sodium hydride, potassium hydride, lithium hydride, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, 1,2-diethoxyethane, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (145).




embedded image


A compound of the formula (145) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (146). A compound of the formula (146) is reacted with 4-methylbenzenesulfonyl chloride in the presence of 4-dimethylaminopyridine, in the presence of a base such as triethylamine, N,N-diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (147). A compound of the formula (147) is reacted with a compound of the formula (148), a known compound or a compound prepared by known methods, in the presence of a base such as sodium carbonate, potassium carbonate, lithium carbonate, sodium bicarbonate, potassium bicarbonate, lithium bicarbonate, triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (149).




embedded image


embedded image


Intermediate (130) of Scheme 34 can also be used in methods that allow the further homologation of the alkylene linker group. An exemplary method is shown in Scheme 39.


A compound of the formula (130) is reacted with a source of cyanide such as potassium cyanide, sodium cyanide, lithium cyanide, tetrabutylammonium cyanide, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (150).


A compound of the formula (150) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (151).


A group corresponding to R7 as described herein can be introduced according to methods known in the art (e.g., as described in Scheme 13). For example, a compound of the formula (151) can be reacted with a compound of the formula (50), a known compound or a compound prepared by known methods, in the presence of a base such as triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (152), where R7 is SO2R10c. Alternatively, a compound of the formula (151) can be used as a starting material in the exemplary methods of Schemes 14 and 15 to provide respectively a compound of the formula (152), where R7 is COR8 or CO2R9.


A compound of the formula (152) is reacted with an acid such as trifluoroacetic acid, hydrochloric acid, sulfuric acid, and the like in a solvent such as tetrahydrofuran, 1,4-dioxane, methylene chloride, 1,2-dichloroethane, methanol, ethanol, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (153) where Rz is H. Alternatively, a compound of the formula of the formula (152) can be treated with acid and a suitable alcoholic solvent to provide the compound of the formula (153) that is a carboxylic acid ester (e.g., where Rz is a C1-6 alkyl): suitable conditions include using 6M HCl in methanol to provide ester compounds of the formula (153) where Rz is methyl.


A compound of the formula (153) is reacted with a reducing agent such as sodium borohydride, sodium triacetoxy borohydride, sodium cyanoborohydride, lithium borohydride, lithium triacetoxy borohydride, lithium cyanoborohydride and the like, in the presence of a solvent such as methylene chloride, 1,2-dichloroethane, methanol, ethanol, isopropanol, tert-butanol, 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxtethane, benzene toluene, N,N-dimethylformamide, N,N-dimethylacetamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (154).


A compound of the formula (154) is reacted with 4-methylbenzenesulfonyl chloride in the presence of 4-dimethylaminopyridine, in the presence of a base such as triethylamine, N,N-diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, acetonitrile, N,N-dimethylformamide, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (155).


A compound of the formula (155) is reacted with a compound of the formula (131), a known compound or a compound prepared by known methods, in the presence of a base such as sodium carbonate, potassium carbonate, lithium carbonate, sodium bicarbonate, potassium bicarbonate, lithium bicarbonate, triethylamine, diisopropylethylamine, pyridine, and the like, in a solvent such as methylene chloride, 1,2-dichloroethane, tetrahydrofuran, 1,4-dioxane, 1,2-dimethoxyethane, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, methanol, ethanol, isopropanol, and the like, optionally with heating, optionally with microwave irradiation to provide a compound of the formula (156).


The Examples provided below provide representative methods for preparing exemplary compounds of the present invention. The skilled practitioner will know how to substitute the appropriate reagents, starting materials and purification methods known to those skilled in the art, in order to prepare the compounds of the present invention.


EXAMPLES

The practice of the invention is illustrated by the following non-limiting examples. The Examples provided below provide representative methods for preparing exemplary compounds of the present invention. The skilled practitioner will know how to substitute the appropriate reagents, starting materials and purification methods known to those skilled in the art, in order to prepare the compounds of the present invention.


In the examples that follow, 1H-NMR spectra were obtained on a Varian Mercury 300-MHz NMR. Purity (%) and mass spectral data were determined with a Waters Alliance 2695 HPLC/MS (Waters Symmetry C18, 4.6×75 mm, 3.5 μm) with a 2996 diode array detector from 210-400 nm.


Example 1
Compound Synthesis



embedded image


Preparation of tert-butyl (R)-2-(((tert-butyldimethylsilyl)oxy)methyl)-5-oxopyrrolidine-1-carboxylate: To a stirred solution of (R)-(+5-(hydroxymethyl)-2-pyrrolidinone (1.0 g, 8.68 mmol, 1.0 equiv) and tert-butyldimethylsilyl chloride (1.44 g, 9.54 mmol, 1.1 equiv.) in dichloromethane (17.3 mL) was added imidazole (0.650 g, 9.54 mmol, 1.1 equiv.). The resulting mixture was then allowed to stirred at 23° C. for 2 hours before being diluted with deionized H2O (25 mL) and extracted with diethyl ether (3×25 mL). The combined organic layers were dried over Na2SO4 and concentrated in vacuum to give a crude intermediate which was then dissolved in acetonitrile (43 mL). To the resulting solution was added triethylamine (1.75 g, 17.3 mmol, 2 equiv.), 4-dimethylaminopyridine (0.212 g, 1.73 mmol, 0.2 equiv.) and di-tert-butyl dicarbonate (2.6 g, 16.5 mmol, 1.9 equiv.). The reaction solution was then allowed to stir at 23° C. for 2 hours before being diluted with saturated aqueous NH4Cl (25 mL) and extracted with ethyl acetate (3×25 mL). The combined organic layers were dried over Na2SO4 and concentrated in vacuum to give a crude product which was further purified by column chromatography (Ethyl acetate/Hexanes, 20%-30%). 1H NMR (400 MHz, CDCl3) δ 4.13 (m, 1H), 3.88 (dd, J=4.0, 10.3 Hz, 1H), 3.65 (dd, J=2.2, 10.3 Hz, 1H), 2.66 (m, 1H), 2.33 (m, 1H), 2.13-1.92 (m, 2H), 1.49 (s, 9H), 0.84 (s, 9H), 0.00 (d, J=5.3 Hz, 6H).




embedded image


Preparation of tert-butyl (R)-5-(((tert-butyldimethylsilyl)oxy)methyl)-3,3-diethyl-2-oxopyrrolidine-1-carboxylate: To a dry round bottom flask under N2 atmosphere was added tert-butyl (R)-2-(((tert-butyldimethylsilyl)oxy)methyl)-5-oxopyrrolidine-1-carboxylate (2.63 g, 7.98 mmol, 1.0 equiv.) and then dissolved in dry tetrahydrofuran (11.5 mL). The resulting solution was then cooled to −78° C. and 1 M Lithium bis(trimethylsilyl)amide solution (tetrahydrofuran, 16.8 mL, 16.8 mmol, 2.1 equiv.) was added dropwise. The resulting solution was allowed to gradually warm to −20° C. before being cooled back to −78° C. and followed by dropwise addition of iodoethane (3.12 g, 20 mmol, 2.5 equiv.). The reaction solution was then allowed to gradually warm to 0° C. and stir at that temperature for 2 hours before being warmed to 23° C. and allowed to stir for an additional 2 hours. The resulting solution was diluted with saturated aq. NH4Cl (25 mL) and extracted with ethyl acetate (3×25 mL). The combined organic layers were dried over Na2SO4 and concentrated in vacuum to give a crude product which was further purified by column chromatography (Ethyl acetate/Hexanes, 0%-10%). 1H NMR (400 MHz, CDCl3) δ 3.94 (m, 1H), 3.83 (dd, J=5.2, 10.0 Hz, 1H), 3.67 (dd, J=2.5, 10.0 Hz, 1H), 1.95 (dd, J=6.3, 13.4 Hz, 1H), 1.79 (dd, J=9.0, 13.4 Hz, 1H), 1.65-1.40 (m, 13H), 0.90-0.75 (m, 15H), 0.00 (d, J=3.3 Hz, 6H).




embedded image


Preparation of (R)-3,3-diethyl-5-(hydroxymethyl)pyrrolidin-2-one: A 6M HCl in methanol solution was prepared via the addition of acetyl chloride (4.8 mL) to methanol (12 mL). To a small round bottom flask was added tert-butyl (R)-5-(((tert-butyldimethylsilyl)oxy)methyl)-3,3-diethyl-2-oxopyrrolidine-1-carboxylate (0.875 g, 2.65 mmol, 1.0 equiv.) and 1 mL of methanol. The prepared methanolic HCl solution was then added dropwise (12 mL) and the resulting mixture was allowed to stir at 23° C. for 30 min before being diluted with methanol and concentrated in vacuum to produce a crude product that was used in the next step without further purification. 1H NMR (400 MHz, CDCl3) δ 7.61 (b, 1H), 4.96 (b, 1H), 3.69-3.48 (m, 2H), 3.33 (dd, J=8.1, 11.2 Hz, 1H), 1.84 (dd, J=7.8, 13.3 Hz, 1H), 1.58-1.31 (m, 5H), 0.80 (dt, J=7.5, 21.9 Hz, 6H).




embedded image


Preparation of (R)-(4,4-diethyl-5-oxopyrrolidin-2-yl)methyl 4-methylbenzenesulfonate: To a stirred solution of (R)-3,3-diethyl-5-(hydroxymethyl)pyrrolidin-2-one (0.367 g, 2.14 mmol, 1.0 equiv) and triethylamine (0.240 g, 2.36 mmol, 1.1 equiv) in dichloromethane (3.3 mL), 4-methylbenzenesulfonyl chloride (0.450 g, 2.36 mmol, 1.1 equiv) and 4-dimethylaminopyridine (0.053 g, 0.428 mmol, 0.2 equiv.) were subsequently added at 0° C. The resulting mixture was stirred at 0° C. for 10 minutes and allowed to stir overnight at 23° C. Then, the reaction mixture was diluted with dichloromethane (25 mL), washed with 1N HCl (1×5 mL) and deionized H2O (2×5 mL), dried over Na2SO4 and concentrated in vacuum to give a crude product which was further purified by column chromatography (Ethyl acetate/Hexanes, 0%-100%). 1H NMR (400 MHz, CDCl3) δ 7.71 (d, J=8.3 Hz, 2H), 7.28 (d, J=8.1 Hz, 2H), 6.57 (b, 1H), 3.96 (dd, J=4.0, 9.6 Hz, 1H), 3.82-3.67 (m, 2H), 2.37 (s, 3H), 1.90 (dd, J=7.9, 13.5 Hz, 1H), 1.52 (dd, J=7.1, 13.6 Hz, 1H) 1.49-1.31 (m, 4H), 0.75 (dt, J=7.4, 26.5 Hz, 6H).




embedded image


Preparation of (R)-3,3-diethyl-5-((4-phenylpiperazin-1-yl)methyl)pyrrolidin-2-one formate: To a small vial was added (R)-(4,4-diethyl-5-oxopyrrolidin-2-yl)methyl 4-methylbenzenesulfonate (75 mg, 0.23 mmol, 1 equiv.) and 1-phenylpiperazine (79 mg, 0.48 mmol, 2.1 equiv.) then both were dissolved in acetonitrile (2.3 mL). Then K2CO3 (80 mg, 0.57 mmol, 2.5 equiv.) was added, the reaction mixture was allowed to stir at 80° C. for 3 days, and then cooled to 23° C. The mixture was filtered, washed with acetonitrile, and the filtrate was concentrated in vacuum to give a crude product which was further purified by HPLC (CH3CN/H2O, 0.1% Formic acid), 0%˜100%). 1H NMR (400 MHz, CDCl3) δ 7.19 (m, 2H), 6.85 (d, J=8.3 Hz, 2H), 6.79 (t, J=7.0 Hz, 1H), 6.42 (b, 1H), 3.70 (m, 1H), 3.12 (m, 4H), 2.70 (m, 2H), 2.50 (m, 2H), 2.41 (dd, J=3.6, 12.4 Hz, 1H), 2.29 (dd, J=9.8, 12.4 Hz, 1H), 1.93 (dd, J=7.6, 13.5 Hz, 1H), 1.57-1.37 (m, 5H), 0.84 (dt, J=7.4, 19.6 Hz, 6H). LC/MS [M+H]=m/z 316.2.




embedded image


Preparation of (R)-3,3-diethyl-5-((4-(p-tolyppiperazin-1-yl)methyl)pyrrolidin-2-one formate: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-((4-phenylpiperazin-1-yl)methyl)pyrrolidin-2-one formate, except 1-(4-methylphenyl)piperazine was substituted for 1-phenylpiperazine. 1H NMR (400 MHz, CDCl3) δ 7.09 (d, J=8.2 Hz, 2H), 6.85 (d, J=8.5 Hz, 2H), 6.47 (b, 1H), 3.78 (m, 1H), 3.15 (m, 4H), 2.78 (m, 2H), 2.59 (m, 2H), 2.49 (dd, J=3.6, 12.4 Hz, 1H), 2.38 (dd, J=9.9, 12.4 Hz, 1H), 2.28 (s, 3H), 2.01 (dd, J=7.6, 13.1 Hz, 1H), 1.67-1.45 (m, 5H), 0.93 (dt, J=7.4, 19.6 Hz, 6H). LC/MS [M+H]=m/z 330.2.




embedded image


Preparation of (R)-5-((4-(3-chlorophenyl)piperazin-1-yl)methyl)-3,3-diethylpyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-((4-phenylpiperazin-1-yl)methyl)pyrrolidin-2-one formate, except 1-(3-chlorophenyl)piperazine hydrochloride was substituted for 1-phenylpiperazine and 5 equiv. of K2CO3 used instead of 2.5 equiv. 1H NMR (400 MHz, CDCl3) δ 7.09 (t, J=8.1 Hz, 1H), 6.79 (t, J=2.0 Hz, 1H), 6.74 (dd, J=1.8, 7.7 Hz, 1H), 6.70 (dd, J=2.3, 8.3 Hz, 1H), 6.36 (b, 1H), 3.69 (m, 1H), 3.11 (m, 4H), 2.67 (m, 2H), 2.47 (m, 2H), 2.39 (dd, J=3.5, 12.3 Hz, 1H), 2.28 (dd, J=10.0, 12.4 Hz, 1H), 1.92 (dd, J=7.8, 13.2 Hz, 1H), 1.58-1.38 (m, 5H), 0.84 (dt, J=7.5, 20.2 Hz, 6H). LC/MS [M+H]=m/z 350.2.




embedded image


Preparation of (R)-3,3-diethyl-5-((4-(4-fluorophenyl)piperazin-1-yl)methyl)pyrrolidin-2-one formate: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-((4-phenylpiperazin-1-yl)methyl)pyrrolidin-2-one formate, except 1-(4-fluorophenyl)piperazine was substituted for 1-phenylpiperazine. 1H NMR (400 MHz, CDCl3) δ 6.97 (m, 2H), 6.92-6.77 (m, 3H), 3.81 (m, 1H), 3.15 (m, 4H), 2.82 (m, 2H), 2.65 (m, 2H), 2.53 (dd, J=3.5, 12.4 Hz, 1H), 2.44 (dd, J=9.6, 12.4 Hz, 1H), 2.03 (dd, J=7.6, 13.3 Hz, 1H), 1.68-1.44 (m, 5H), 0.92 (dt, J=7.5, 18.9 Hz, 6H). LC/MS [M+H]=m/z 334.2.




embedded image


Preparation of (R)-3,3-diethyl-5-(pyridin-2-yl)piperazin-1-yl)methyl)pyrrolidin-2-one formate: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-((4-phenylpiperazin-1-yl)methyl)pyrrolidin-2-one formate, except 1-(2-pyridyl)piperazine was substituted for 1-phenylpiperazine. 1H NMR (400 MHz, CDCl3) δ 8.19 (m, 1H), 7.50 (m, 1H), 6.86 (b, 1H) 6.65 (m, 2H), 3.81 (m, 1H), 3.57 (m, 4H), 2.77 (m, 2H), 2.59 (m, 2H), 2.51 (dd, J=3.8, 12.6 Hz, 1H), 2.43 (dd, J=9.4, 12.5 Hz, 1H), 2.02 (dd, J=7.7, 13.2 Hz, 1H), 1.66-1.44 (m, 5H), 0.90 (dt, J=7.4, 20.0 Hz, 6H). LC/MS [M+H]=m/z 317.2.




embedded image


Preparation of (R)-3,3-diethyl-5-((4-(2-isopropylphenyl)piperazin-1-yl)methyl)pyrrolidin-2-one formate: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-((4-phenylpiperazin-1-yl)methyl)pyrrolidin-2-one formate, except 1-(2-isopropylphenyl)piperazine was substituted for 1-phenylpiperazine. 1H NMR (400 MHz, CDCl3) δ 7.18 (m, 1H), 7.12-6.99 (m, 3H), 6.34 (b, 1H), 3.71 (m, 1H), 3.40 (sept, J=6.8 Hz, 1H), 2.83 (m, 4H), 2.71 (b, 2H), 2.60-2.39 (b, 3H), 2.32 (m, 1H), 1.94 (dd, J=7.5, 13.2 Hz, 1H), 1.60-1.36 (m, 5H), 1.12 (d, J=6.9 Hz, 6H), 0.84 (dt, J=7.4, 18.3 Hz, 6H). LC/MS [M+H]=m/z 358.2.




embedded image


Preparation of (R)-3,3-diethyl-5-((4-(4-methyl-2-morpholinophenyl)piperazin-1-yl)methyl)pyrrolidin-2-one formate: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-((4-phenylpiperazin-1-yl)methyl)pyrrolidin-2-one formate, except 1-(4-methyl-2-morpholinophenyl)piperazine was substituted for 1-phenylpiperazine. NMR (400 MHz, CDCl3) δ 6.73 (m, 2H), 6.63 (b, 1H), 6.45 (b, 1H) 3.82-3.64 (m, 5H), 3.31-2.84 (b, 8H), 2.68 (b, 2H), 2.57-2.38 (b, 3H), 2.32 (m, 1H), 2.21 (s, 3H), 1.94 (dd, J=7.4, 13.0 Hz, 1H), 1.59-1.38 (m, 5H), 0.84 (dt, J=7.4, 18.8 Hz, 6H). LC/MS [M+H]=m/z 415.2.




embedded image


Preparation of (S)—N-(4-(benzyloxy)-2-hydroxybutyl)-4-methylbenzenesulfonamide: To a stirred solution of (S)-2-(2-(benzyloxy)ethyl)oxirane (0.5 g, 2.8 mmo, 1.0 equiv.) in 1,4-dioxane (11.25 mL) was added p-toluenesulfonamide (0.96 g, 5.6 mmol, 2.0 equiv.), benzyltriethylammonium chloride (0.064 g, 0.28 mmol, 0.1 equiv.) and Cs2CO3 (0.092 g, 0.28 mmol, 0.1 equiv.). The resulting mixture was then stirred at 90° C. for 48 hours. The reaction was then allowed to cool to 23° C. and concentrated in vacuum to give a crude product which was further purified by HPLC (CH3CN/H2O, 0.1% Formic acid), 0%˜100%). Desired fractions were further purified by column chromatography (Ethyl acetate/Hexanes, 10%˜100%). 1H NMR (400 MHz, CDCl3) δ 7.73 (d, J=8.2 Hz, 2H), 7.44-7.22 (m, 7H), 5.00 (t, J=6.2 Hz, 1H), 4.50 (s, 2H), 3.93 (m, 1H), 3.66 (m, 2H), 3.07 (m, 1H), 2.87 (m, 1H), 2.43 (s, 3H), 1.83 (m, 1H), 1.70 (m, 1H).




embedded image


Preparation of (R)—N-(4-(benzyloxy)-2-hydroxybutyl)-4-methylbenzenesulfonamide: The title compound was prepared according to the procedure for (S)—N-(4-(benzyloxy)-2-hydroxybutyl)-4-methylbenzenesulfonamide, except (R)-2-(2-(benzyloxy)ethyl)oxirane was substituted for (S)-2-(2-(benzyloxy)ethyl)oxirane. 1H NMR (400 MHz, CDCl3) δ 7.64 (d, J=8.2 Hz, 2H), 7.31-7.16 (m, 7H), 4.90 (t, J=6.1 Hz, 1H), 4.41 (s, 2H), 3.84 (m, 1H), 3.57 (m, 2H), 2.98 (m, 1H), 2.78 (m, 1H), 2.34 (s, 3H), 1.74 (m, 1H), 1.60 (m, 1H).




embedded image


Preparation of N-(4-(benzyloxy)-2-hydroxybutyl)-4-methylbenzenesulfonamide: The title compound was prepared according to the procedure for (S)—N-(4-(benzyloxy)-2-hydroxybutyl)-4-methylbenzenesulfonamide, except (rac)-2-(2-(benzyloxy)ethyl)oxirane was substituted for (S)-2-(2-(benzyloxy)ethyl)oxirane. 1H NMR (400 MHz, CDCl3) δ 7.66 (d, J=8.2 Hz, 2H), 7.35-7.18 (m, 7H), 4.92 (t, J=6.1 Hz, 1H), 4.43 (s, 2H), 3.89 (m, 1H), 3.60 (m, 2H), 3.02 (m, 1H), 2.80 (m, 1H), 2.38 (s, 3H), 1.77 (m, 1H), 1.63 (m, 1H).




embedded image


Preparation of (R)-2-(2-(benzyloxy)ethyl)-1-tosylaziridine: This reaction was performed in oven-dried glassware under a nitrogen atmosphere. To a stirred solution of pyridine (1.57 g, 19.9 mmol, 5.0 equiv.) and methanesulfonyl chloride (2.28 g, 19.9 mmol, 5.0 equiv.) in dry dichloromethane (22.5 mL) at 0° C. was added a solution of (S)—N-(4-(benzyloxy)-2-hydroxybutyl)-4-methylbenzenesulfonamide (1.4 g, 3.99 mmol, 1.0 equiv.) in dry dichloromethane (22.5 mL). The resulting solution was stirred at reflux overnight, cooled to 23° C., and washed with brine (50 mL). The organic layer was dried over Na2SO4 and concentrated in vacuo to give crude mesylate which was further purified by column chromatography (Ethyl acetate/Hexanes, 10%˜50%).


The purified mesylate was then dissolved in acetonitrile (45 mL) and K2CO3 (2.22 g, 16.0 mmol, 4.0 equiv.) was added. The resulting mixture was allowed to stir at 45° C. overnight before being cooled to 23° C. and filtered. The filtrate was concentrated in vacuo to give crude product which was purified by column chromatography (Ethyl acetate/Hexanes, 10% 20%). 1H NMR (400 MHz, CDCl3) δ 7.84 (d, J=8.2 Hz, 2H), 7.45-7.19 (m, 7H), 4.39 (s, 2H), 3.46 (dt, J=3.7, 9.2 Hz, 1H), 3.35 (m, 1H), 2.93 (m, 1H), 2.70 (d, J=7.1 Hz, 1H), 2.45 (s, 3H), 2.15 (d, J=4.6 Hz, 1H), 1.94 (m, 1H), 1.58 (m, 1H).




embedded image


Preparation of (S)-2-(2-(benzyloxy)ethyl)-1-tosylaziridine: The title compound was prepared according to the procedure for (R)-2-(2-(benzyloxy)ethyl)-1-tosylaziridine, except (R)—N-(4-(benzyloxy)-2-hydroxybutyl)-4-methylbenzenesulfonamide was substituted for (S)—N-(4-(benzyloxy)-2-hydroxybutyl)-4-methylbenzenesulfonamide. 1H NMR (400 MHz, CDCl3) δ 7.84 (d, J=8.3 Hz, 2H), 7.43-7.23 (m, 7H), 4.39 (s, 2H), 3.46 (dt, J=3.8, 9.3 Hz, 1H), 3.35 (m, 1H), 2.93 (m, 1H), 2.69 (d, J=7.0 Hz, 1H), 2.45 (s, 3H), 2.15 (d, J=4.5 Hz, 1H), 1.94 (m, 1H), 1.59 (m, 1H).




embedded image


Preparation of 2-(2-(benzyloxy)ethyl)-1-tosylaziridine: The title compound was prepared according to the procedure for (R)-2-(2-(benzyloxy)ethyl)-1-tosylaziridine, except (rac)-N-(4-(benzyloxy)-2-hydroxybutyl)-4-methylbenzenesulfonamide was substituted for (S)—N-(4-(benzyloxy)-2-hydroxybutyl)-4-methylbenzenesulfonamide. 1H NMR (400 MHz, CDCl3) δ 7.84 (d, J=8.3 Hz, 2H), 7.41-7.26 (m, 7H), 4.39 (s, 2H), 3.46 (dt, J=3.8, 9.3 Hz, 1H), 3.35 (m, 1H), 2.93 (m, 1H), 2.69 (d, J=7.0 Hz, 1H), 2.45 (s, 3H), 2.15 (d, J=4.6 Hz, 1H), 1.93 (m, 1H), 1.59 (m, 1H).




embedded image


Preparation of (S)-6-(benzyloxy)-N,N-dimethyl-4-((4-methylphenyl)sulfonamido) hexanamide: This reaction was performed in oven-dried glassware under a nitrogen atmosphere. To a cooled solution of dry N,N-dimethylacetamide (0.527 g, 6.05 mmol, 1.1 equiv.) and dry tetrahydrofuran (18 mL) at −78° C. was added dropwise a 1M Lithium diisopropylamide solution (tetrahydrofuran/Hexanes, 7.26 mL, 7.26 mmol, 1.3 equiv.). The resulting solution was then stirred at −78° C. for 30 minutes before being allowed to warm to 0° C. At 0° C., a solution of (R)-2-(2-(benzyloxy)ethyl)-1-tosylaziridine (1.82 g, 5.5 mmol, 1.0 equiv.) in dry tetrahydrofuran (18 mL) was added to the solution. The reaction was stirred at 0° C. for 20 minutes and then allowed to warm to 23° C. and stir overnight. The reaction was quenched with sat. NH4Cl (40 mL) and extracted with ethyl acetate (3×30 mL). The combined organic layers were dried over Na2SO4 and concentrated in vacuum to give a crude product which was further purified by column chromatography (Ethyl acetate/Hexanes, 40%˜100%). 1H NMR (400 MHz, CDCl3) δ 7.72 (d, J=8.2 Hz, 2H), 7.41-7.19 (m, 7H), 5.91 (d, J=7.5 Hz, 1H), 4.40 (q, J=9.3 Hz, 2H), 3.56 (m, 1H), 3.40 (m, 2H), 2.93 (s, 3H), 2.90 (s, 3H), 2.48-2.35 (m, 4H), 2.21 (dt, J=6.6, 16.6 Hz, 1H), 1.88-1.69 (m, 2H), 1.68-1.55 (m, 2H).




embedded image


Preparation of (R)-6-(benzyloxy)-N,N-dimethyl-4-((4-methylphenyl)sulfonamido) hexanamide: The title compound was prepared according to the procedure for (S)-6-(benzyloxy)-N,N-dimethyl-4-((4-methylphenyOsulfonamido)hexanamide, except (S)-2-(2-(benzyloxy)ethyl)-1-tosylaziridine was substituted for (R)-2-(2-(benzyloxy)ethyl)-1-tosylaziridine. 1H NMR (400 MHz, CDCl3) δ 7.71 (d, J=8.2 Hz, 2H), 7.41-7.18 (m, 7H), 5.91 (d, J=7.5 Hz, 1H), 4.40 (q, J=8.9 Hz, 2H), 3.54 (m, 1H), 3.40 (m, 2H), 2.94 (s, 3H), 2.91 (s, 3H), 2.47-2.35 (m, 4H), 2.21 (dt, J=6.6, 16.6 Hz, 1H), 1.87-1.68 (m, 2H), 1.67-1.52 (m, 2H).




embedded image


Preparation of 6-(benzyloxy)-N,N-dimethyl-4-((4-methylphenyl)sulfonamido) hexanamide: The title compound was prepared according to the procedure for (S)-6-(benzyloxy)-N,N-dimethyl-4-((4-methylphenyOsulfonamido)hexanamide, except (rac)-2-(2-(benzyloxy)ethyl)-1-tosylaziridine was substituted for (R)-2-(2-(benzyloxy)ethyl)-1-tosylaziridine. 1H NMR (400 MHz, CDCl3) δ 7.72 (d, J=8.2 Hz, 2H), 7.42-7.21 (m, 7H), 5.90 (d, J=7.5 Hz, 1H), 4.41 (q, J=9.3 Hz, 2H), 3.57 (m, 1H), 3.40 (m, 2H), 2.95 (s, 3H), 2.93 (s, 3H), 2.50-2.36 (m, 4H), 2.23 (dt, J=6.6, 16.6 Hz, 1H), 1.88-1.70 (m, 2H), 1.69-1.57 (m, 2H).




embedded image


Preparation of (S)-5-(2-(benzyloxy)ethyl)-1-tosylpyrrolidin-2-one: (S)-6-(benzyloxy)-N,N-dimethyl-4-((4-methylphenyl)sulfonamido)hexanamide (0.565g, 1.35 mmol, 1.0 equiv.) was mixed with p-toluenesulfonic acid monohydrate (0.282g, 1.48 mmol, 1.1 equiv.) and toluene (5.65 mL) in a microwave vial. The mixture was then heated in a microwave reactor at 190° C. for 2 hours. The mixture was then neutralized with sat. NaHCO3 and extracted with ethyl acetate (3×15 mL). The combined organic phase was dried over Na2SO4 and concentrated in vacuum to give a crude product which was further purified by column chromatography (Ethyl acetate/Hexanes, 0%˜40%). 1H NMR (400 MHz, CDCl3) δ 7.96 (d, J=8.2 Hz, 2H), 7.42-7.26 (m, 7H), 4.59-4.42 (m, 3H), 3.65-3.54 (m, 2H), 2.62-2.50 (m, 1H), 2.45 (s, 3H), 2.42-2.27 (m, 2H), 2.25-2.12 (m, 1H), 2.11-1.89 (m, 2H).




embedded image


Preparation of (R)-5-(2-(benzyloxy)ethyl)-1-tosylpyrrolidin-2-one: The title compound was prepared according to the procedure for (S)-5-(2-(benzyloxy)ethyl)-1-tosylpyrrolidin-2-one, except (R)-6-(benzyloxy)-N,N-dimethyl-4-((4-methylphenyl)sulfonamido)hexanamide was substituted for (S)-6-(benzyloxy)-N,N-dimethyl-4-((4-methylphenyl)sulfonamido)hexanamide. 1H NMR (400 MHz, CDCl3) δ 7.95 (d, J=8.4 Hz, 2H), 7.39-7.25 (m, 7H), 4.59-4.42 (m, 3H), 3.67-3.53 (m, 2H), 2.61-2.47 (m, 1H), 2.42 (s, 3H), 2.40-2.23 (m, 2H), 2.22-2.09 (m, 1H), 2.07-1.89 (m, 2H).




embedded image


Preparation of 5-(2-(benzyloxy)ethyl)-1-tosylpyrrolidin-2-one: The title compound was prepared according to the procedure for (S)-5-(2-(benzyloxy)ethyl)-1-tosylpyrrolidin-2-one, except (rac)-6-(benzyloxy)-N,N-dimethyl-4-((4-methylphenyl)sulfonamido)hexanamide was substituted for (S)-6-(benzyloxy)-N,N-dimethyl-4-((4-methylphenyl)sulfonamido)hexanamide. 1H NMR (400 MHz, CDCl3) δ 7.96 (d, J=8.3 Hz, 2H), 7.41-7.25 (m, 7H), 4.60-4.42 (m, 3H), 3.64-3.54 (m, 2H), 2.62-2.49 (m, 1H), 2.44 (s, 3H), 2.42-2.26 (m, 2H), 2.24-2.11 (m, 1H), 2.10-1.88 (m, 2H).




embedded image


Preparation of (R)-(5-oxopyrrolidin-2-yl)methyl 4-methylbenzenesulfonate: To a cooled mixture of (R)-(−)-5-(hydroxymethyl)-2-pyrrolidinone (10.0 g, 87 mmol, 1.0 equiv.) and triethylamine (9.68 g, 95.7 mmol, 1.1 equiv.) in methylene chloride (134 mL) at 0° C. was added 4-toluenesulfonyl chloride (18.25 g, 95.7 mmol, 1.1 equiv.) followed by 4-dimethylaminopyridine (2.12 g, 17.3 mmol, 0.2 equiv.). The resulting reaction mixture was stirred at 0° C. for 5 minutes before being warmed to 23° C. and allowed to stir overnight. Then, the reaction mixture was diluted with dichloromethane (200 mL), washed with 1N HCl (1×200 mL) and deionized H2O (2×150 mL), dried over Na2SO4 and concentrated in vacuum to give a crude product which used in the next step without further purification. 1H NMR (400 MHz, CDCl3) δ 7.77 (d, J=8.2 Hz, 2H), 7.35 (d, J=8.2 Hz, 2H), 6.76 (b, 1H), 4.01 (dd, J=3.6, 9.7 Hz, 1H), 3.86 (m, 1H), 3.80 (dd, J=7.4, 9.6 Hz, 1H), 2.44 (s, 3H), 2.37-2.12 (m, 3H), 1.77 (m, 1H)




embedded image


Preparation of (S)-(5-oxopyrrolidin-2-yl)methyl 4-methylbenzenesulfonate: The title compound was prepared according to the procedure for (R)-(5-oxopyrrolidin-2-yl)methyl 4-methylbenzenesulfonate, except L-pyroglutaminol was substituted for (R)-(−)-5-(hydroxymethyl)-2-pyrrolidinone. 1HNMR (400 MHz, CDCl3) δ 7.71 (d, J=8.3 Hz, 2H), 7.30 (d, J=8.2 Hz, 2H), 5.77 (b, 1H), 3.99 (dd, J=3.5, 9.7 Hz, 1H), 3.86 (m, 1H), 3.79 (dd, J=7.4, 9.6 Hz, 1H), 2.39 (s, 3H), 2.29-2.11 (m, 3H), 1.69 (m, 1H).




embedded image


Preparation of (R)-2-(5-oxopyrrolidin-2-yl)acetonitrile: To a solution of (R)-(5-oxopyrrolidin-2-yl)methyl 4-methylbenzenesulfonate (21.25 g, 79 mmol, 1.0 equiv.) in acetonitrile (335 mL) was added potassium cyanide (12.86 g, 197 mmol, 2.5 equiv.). The resulting reaction mixture was then heated to reflux and allowed to reflux overnight. After cooling to 23° C., the reaction mixture was filtered thru a plug of Celite and concentrated in vacuum to give a crude product which was further purified by column chromatography (MeOH/Ethyl acetate, 10%). 1H NMR (400 MHz, CDCl3) δ 7.23 (b, 1H), 3.93 (m, 1H), 2.54 (d, J=5.7 Hz, 2H), 2.48-2.24 (m, 3H), 1.88 (m, 1H).




embedded image


Preparation of (S)-2-(5-oxopyrrolidin-2-yl)acetonitrile: The title compound was prepared according to the procedure for (R)-2-(5-oxopyrrolidin-2-yl)acetonitrile, except (S)-(5-oxopyrrolidin-2-yl)methyl 4-methylbenzenesulfonate was substituted for (R)-(5-oxopyrrolidin-2-yl)methyl 4-methylbenzenesulfonate. 1H NMR (400 MHz, CDCl3) δ 7.47 (b, 1H), 3.92 (m, 1H), 2.55 (d, J=5.6 Hz, 2H), 2.47-2.24 (m, 3H), 1.86 (m, 1H).




embedded image


Preparation of methyl (R)-2-(5-oxopyrrolidin-2-yl)acetate: A 6 M HCl in methanol solution was prepared via the addition of acetyl chloride (33 mL) to methanol (77 mL). (R)-2-(5-oxopyrrolidin-2-yl)acetonitrile (4.73 g, 38 mmol, 1.0 equiv.) was dissolved in the prepared 6 M methanolic HCl solution (77 mL) and stirred at 23° C. overnight. The reaction mixture was diluted with deionized H2O (100 mL) and methylene chloride (100 mL) and layers were seperated. The aqueous layer was backwashed with methylene chloride (8×100 mL). The combined organic phase was dried over Na2SO4 and concentrated in vacuum to give a crude product that was used in the next step without further purification. 1H NMR (400 MHz, CDCl3) δ 6.40 (b, 1H), 3.94 (m, 1H), 3.64 (s, 3H), 2.52 (dd, J=4.5, 16.5 Hz, 1H), 2.43 (dd, J=9.0, 16.5 Hz, 1H), 2.35-2.19 (m, 3H), 1.68 (m, 1H).




embedded image


Preparation of methyl (S)-2-(5-oxopyrrolidin-2-yl)acetate: The title compound was prepared according to the procedure for methyl (R)-2-(5-oxopyrrolidin-2-yl)acetate, except (S)-2-(5-oxopyrrolidin-2-yl)acetonitrile was substituted for (R)-2-(5-oxopyrrolidin-2-yl)acetonitrile. 1H NMR (400 MHz, CDCl3) δ 6.25 (b, 1H), 3.94 (m, 1H), 3.64 (s, 3H), 2.52 (dd, J=4.3, 16.4 Hz, 1H), 2.42 (dd, J=9.2, 16.5 Hz, 1H), 2.32-2.23 (m, 3H), 1.68 (m, 1H).




embedded image


Preparation of (R)-5-(2-hydroxyethyl)pyrrolidin-2-one: To a stirred solution of methyl (R)-2-(5-oxopyrrolidin-2-yl)acetate (0.525 g, 3.3 mmol, 1.0 equiv.) in ethanol (13.4 mL) was added NaBH4 (0.380 g, 10 mmol, 3.0 equiv.) and the resulting mixture was stirred at 23° C. for 5 minutes then at reflux for 1 hour. After cooling to 23° C., the reaction mixture was quenched with 1 mL of acetic acid and the filtered while washing with methanol. The filtrate was concentrated in vacuum to give a crude product which was further purified by column chromatography (MeOH/methanol, 10%). 1H NMR (400 MHz, CDCl3) δ 7.36 (b, 1H), 4.86-4.09 (b, 1H), 3.82-3.54 (m, 3H), 2.32-2.14 (m, 3H), 1.74-1.53 (m, 3H).




embedded image


Preparation of (S)-5-(2-hydroxyethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-5-(2-hydroxyethyl)pyrrolidin-2-one, except methyl (S)-2-(5-oxopyrrolidin-2-yl)acetate was substituted for methyl (R)-2-(5-oxopyrrolidin-2-yl)acetate. 1H NMR (400 MHz, CDCl3) δ 7.04 (b, 1H), 3.81-3.59 (m, 3H), 3.35-2.88 (b, 1H), 2.31-2.14 (m, 3H), 1.75-1.57 (m, 3H).




embedded image


Preparation of tert-butyl (R)-2-(2-(ftert-butyldimethylsilyl)oxy)ethyl)-5-oxopyrrolidine-1-carboxylate: To a stirred solution of (R)-5-(2-hydroxyethyl)pyrrolidin-2-one (3.41 g, 26.4 mmol, 1.0 equiv.) in methylene chloride (50 mL) was added tert-butylchlorodimethylsilane (4.37 g, 29 mmol, 1.1 equiv.) followed by imidazole (1.98 g, 29 mmol, 1.1 equiv.). The resulting mixture was then stirred at 23° C. for 2 hr before being diluted with diethyl ether (100 mL) and washed with deionized H2O (50 mL). The aqueous layer was backwashed with diethyl ether (2×20 mL). The combined organic phase was dried over Na2SO4 and concentrated in vacuum to give a crude intermediate that was dissolved in acetonitrile (132 mL). Triethylamine (5.34 g, 52.8 mmol, 2.0 equiv.), di-tert-butyl dicarbonate (10.95 g, 50.2 mmol, 1.9 equiv.) and 4-dimethylaminopyridine (0.645 g, 5.28 mmol, 0.2 equiv.) were then added and the resulting solution was stirred at 23° C. for 2 hrs. The reaction was diluted with ethyl acetate (200 mL) and washed with sat. NH4Cl (100 mL). The aqueous layer was backwashed with ethyl acetate (2×20 mL) and the combined organic phase was dried over Na2SO4 and concentrated in vacuum to give a crude product which was further purified by column chromatography (Ethyl acetate/Hexanes, 20-30%). 1H NMR (400 MHz, CDCl3) δ 4.18 (m, 1H), 3.66 (t, J=6.2 Hz, 2H), 2.54 (ddd, J=9.2, 11.3, 17.6 Hz, 1H), 2.36 (ddd, J=2.4, 9.2, 17.6 Hz, 1H), 2.13-1.82 (m, 3H), 1.66 (m, 1H), 1.47 (s, 9H), 0.83 (s, 9H), 0.00 (s, 6H).




embedded image


Preparation of tert-butyl (S)-2-(2-((tert-butyldimethylsilyl)oxy)ethyl)-5-oxopyrrolidine-1-carboxylate: The title compound was prepared according to the procedure for tert-butyl (R)-2-(2-((tert-butyldimethylsilyl)oxy)ethyl)-5-oxopyrrolidine-1-carboxylate, except (S)-5-(2-hydroxyethyl)pyrrolidin-2-one was substituted for (R)-5-(2-hydroxyethyl)pyrrolidin-2-one. 1H NMR (400 MHz, CDCl3) δ 4.18 (m, 1H), 3.66 (t, J=6.3 Hz, 2H), 2.54 (ddd, J=9.1, 11.3, 17.6 Hz, 1H), 2.36 (ddd, J=2.4, 9.2, 17.6 Hz, 1H), 2.12-1.85 (m, 3H), 1.66 (m, 1H), 1.47 (s, 9H), 0.83 (s, 9H), 0.00 (s, 6H).




embedded image


Preparation of tert-butyl (R)-5-(2-((tert-butyldimethylsilyl)oxy)ethyl)-3,3-diethyl-2-oxopyrrolidine-1-carboxylate: This reaction was performed in oven-dried glassware under a nitrogen atmosphere. A stirred solution of tert-butyl (R)-2-(2-((tert-butyldimethylsilyl)oxy)ethyl)-5-oxopyrrolidine-1-carboxylate (8.0 g, 23.2 mmol, 1.0 equiv.) in dry tetrahydrofuran (35 mL) was cooled to −78° C. and 1M lithium bis(trimethylsilyl)amide solution (tetrahydrofuran, 51 mL, 51 mmol, 2.2 equiv.) was added dropwise while maintaining the reaction temperature below −70° C. The resulting solution was allowed to slowly warm to −30° C. before being cooled back to −78° C. at which iodoethane (8.48 g, 50.5 mmol, 2.15 equiv.) was slowly added dropwise. The resulting solution was slowly warmed to −15° C. and allowed to stir at this temperature for 2 hr before being warmed to 23° C. and allowed to stir for an additional 2.5 hr. The reaction was quenched with sat. NH4Cl (40 mL) and extracted with ethyl acetate (3×50 mL). The combined organic layers were dried over Na2SO4 and concentrated in vacuum to give a crude product which was further purified by column chromatography (Ethyl acetate/Hexanes, 0%˜10%). 1H NMR (400 MHz, CDCl3) δ 3.97 (m, 1H), 3.65 (t, J=5.9 Hz, 2H), 2.23 (m, 1H), 1.95 (dd, J=8.6, 13.5 Hz, 1H), 1.66 (dd, J=6.1, 13.5 Hz, 1H), 1.58-1.39 (m, 14H), 0.90-0.74 (m, 15H), 0.00 (s, 3H).




embedded image


Preparation of (R)-5-(2-(benzyloxy)ethyl)-3,3-diethyl-1-tosylpyrrolidin-2-one: The title compound was prepared according to the procedure for tert-butyl (R)-5-(2-((tert-butyldimethylsilyl)oxy)ethyl)-3,3-diethyl-2-oxopyrrolidine-1-carboxylate, except (R)-5-(2-(benzyloxy)ethyl)-1-tosylpyrrolidin-2-one was substituted for tert-butyl (R)-2-(2-((tert-butyldimethylsilyl)oxy)ethyl)-5-oxopyrrolidine-1-carboxylate. 1H NMR (400 MHz, CDCl3) δ 7.84 (d, J=8.4 Hz, 2H), 7.33-7.16 (m, 7H), 4.44 (dd, J=12.0, 32.0 Hz, 2H), 4.21 (m, 1H), 3.54 (t, J=5.5 Hz, 2H), 2.69 (m, 1H), 2.34 (s, 3H), 1.95 (dd, J=8.1, 13.5 Hz, 1H), 1.81-1.64 (m, 2H), 1.41 (q, J=7.5 Hz, 2H), 1.33-1.13 (m, 2H), 0.71 (t, J=7.5 Hz, 3H), 0.48 (t, J=7.5 Hz, 3H).




embedded image


Preparation of (S)-5-(2-(benzyloxy)ethyl)-3,3-diethyl-1-tosylpyrrolidin-2-one: The title compound was prepared according to the procedure for tert-butyl (R)-5-(2-((tert-butyldimethylsilyl)oxy)ethyl)-3,3-diethyl-2-oxopyrrolidine-1-carboxylate, except (S)-5-(2-(benzyloxy)ethyl)-1-tosylpyrrolidin-2-one was substituted for tert-butyl (R)-2-(2-((tert-butyldimethylsilyl)oxy)ethyl)-5-oxopyrrolidine-1-carboxylate. 1H NMR (400 MHz, CDCl3) δ 7.93 (d, J=8.2 Hz, 2H), 7.40-7.24 (m, 7H), 4.53 (dd, J=11.9, 32.6 Hz, 2H), 4.31 (m, 1H), 3.63 (t, J=5.8 Hz, 2H), 2.78 (m, 1H), 2.42 (s, 3H), 2.04 (dd, J=8.6, 13.5 Hz, 1H), 1.90-1.74 (m, 2H), 1.50 (q, J=7.7 Hz, 2H), 1.44-1.23 (m, 2H), 0.80 (t, J=7.4 Hz, 3H), 0.57 (t, J=7.4 Hz, 3H).




embedded image


Preparation of 5-(2-(benzyloxy)ethyl)-3 ,3-diethyl-1-tosylpyrrolidin-2-one: The title compound was prepared according to the procedure for tert-butyl (R)-5-(2-((tert-butyldimethylsilyl)oxy)ethyl)-3,3-diethyl-2-oxopyrrolidine-1-carboxylate, except (rac)-5-(2-(benzyloxy)ethyl)-1-tosylpyrrolidin-2-one was substituted for tert-butyl (R)-2-(2-((tert-butyldimethylsilyl)oxy)ethyl)-5-oxopyrrolidine-1-carboxylate. 1H NMR (400 MHz, CDCl3) δ 7.93 (d, J=8.3 Hz, 2H), 7.41-7.24 (m, 7H), 4.52 (dd, J=12.0, 32.4 Hz, 2H), 4.30 (m, 1H), 3.62 (t, J=5.7 Hz, 2H), 2.78 (m, 1H), 2.41 (s, 3H), 2.04 (dd, J=8.6, 13.5 Hz, 1H), 1.89-1.72 (m, 2H), 1.49 (q, J=7.6 Hz, 2H), 1.43-1.19 (m, 2H), 0.80 (t, J=7.4 Hz, 3H), 0.56 (t, J=7.4 Hz, 3H).




embedded image


Preparation of (R)-5-(2-(benzyloxy)ethyl)-3,3-diethylpyrrolidin-2-one: This reaction was performed in oven-dried glassware under a nitrogen atmosphere. A mixture of Na metal (800 mg) and dry tetrahydrofuran (100 mL) was stirred at 23° C. for 45 minutes. The reaction mixture was cooled to −78° C. followed by the addition of a solution of (R)-5-(2-(benzyloxy)ethyl)-3,3-diethyl-1-tosylpyrrolidin-2-one (1.48 g, 3.45 mmol, 1.0 equiv.) in dry tetrahydrofuran (51 mL). The resulting mixture was allowed to stir at −78° C. for 1.5 hours before being quenched with sat. NH4Cl (50 mL) and extracted with ethyl acetate (3×40 mL). The combined organic layers were dried over Na2SO4 and concentrated in vacuum to give a crude product which was further purified by column chromatography (Ethyl acetate/Hexanes, 0% 100%). 1H NMR (400 MHz, CDCl3) δ 7.31-7.14 (m, 5H), 6.59 (b, 1H), 4.40 (s, 2H), 3.60-3.37 (m, 3H), 1.93 (dd, J=7.5, 13.3 Hz, 1H), 1.75-1.58 (m, 2H), 1.57-1.32 (m, 5H), 0.80 (dt, J=7.6, 18.3 Hz, 6H).




embedded image


Preparation of (S)-5-(2-(benzyloxy)ethyl)-3,3-diethylpyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-5-(2-(benzyloxy)ethyl)-3,3-diethylpyrrolidin-2-one, except (S)-5-(2-(benzyloxy)ethyl)-3,3-diethyl-1-tosylpyrrolidin-2-one was substituted for (R)-5-(2-(benzyloxy)ethyl)-3,3-diethyl-1-tosylpyrrolidin-2-one. 1H NMR (400 MHz, CDCl3) δ 7.35-7.13 (m, 5H), 6.06 (b, 1H), 4.42 (s, 2H), 3.62-3.36 (m, 3H), 1.95 (dd, J=7.5, 13.3 Hz, 1H), 1.75-1.59 (m, 2H), 1.57-1.36 (m, 5H), 0.80 (dt, J=7.6, 18.3 Hz, 6H)




embedded image


Preparation of 5-(2-(benzyloxy)ethyl)-3,3-diethylpyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-5-(2-(benzyloxy)ethyl)-3,3-diethylpyrrolidin-2-one, except (rac)-5-(2-(benzyloxy)ethyl)-3 ,3-diethyl-1-tosylpyrrolidin-2-one was substituted for (R)-5-(2-(benzyloxy)ethyl)-3,3-diethyl-1-tosylpyrrolidin-2-one. 1H NMR (400 MHz, CDCl3) δ 7.28-7.10 (m, 5H), 6.17 (b, 1H), 4.36 (s, 2H), 3.58-3.32 (m, 3H), 1.89 (dd, J=7.3, 13.3 Hz, 1H), 1.68-1.53 (m, 2H), 1.52-1.28 (m, 5H), 0.76 (dt, J=7.4, 19.8 Hz, 6H)




embedded image


Preparation of (R)-5-(2-bromoethyl)-3,3-diethylpyrrolidin-2-one: To a round bottom flask was added 10% Pd/C (175 mg, 20% wt) followed by a solution of (R)-5-(2-(benzyloxy)ethyl)-3,3-diethylpyrrolidin-2-one (876 mg, 3.19 mmol, 1 equiv.) in ethanol (17 mL). The system was put under H2 (1 atm) using a balloon and allowed to stir at 23° C. under a H2 atmosphere overnight. The reaction was filtered through a plug of Celite and concentrated under reduced pressure. The crude alcohol was dissolved in tetrahydrofuran (12.8 mL) and then triphenylphosphine (1.35 g, 5.13 mmol, 1.6 equiv.) and carbon tetrabromide (1.70 g, 5.13 mmol, 1.6 equiv.) were sequentially added and the reaction was allowed to stir at 23° C. for —3 hours. The resulting mixture was filtered and concentrated in vacuum to give a crude product which was further purified by column chromatography (100% Hexanes then Ethyl acetate/Hexanes, 30%˜50%). 1H NMR (400 MHz, CDCl3) δ 7.31 (b, 1H), 3.65 (p, J=6.8 Hz, 1H), 3.38 (t, J=6.7 Hz, 2H), 2.12-1.85 (m, 3H), 1.62-1.32 (m, 5H), 0.82 (dt, J=7.5, 17.8 Hz, 6H).




embedded image


Preparation of (S)-5-(2-bromoethyl)-3,3-diethylpyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-5-(2-bromoethyl)-3,3-diethylpyrrolidin-2-one, except (S)-5-(2-(benzyloxy)ethyl)-3,3-diethylpyrrolidin-2-one was substituted for (R)-5-(2-(benzyloxy)ethyl)-3,3-diethylpyrrolidin-2-one. 1H NMR (400 MHz, CDCl3) δ 7.16 (b, 1H), 3.66 (p, J=6.8 Hz, 1H), 3.38 (t, J=6.8 Hz, 2H), 2.08-1.88 (m, 3H), 1.59-1.35 (m, 5H), 0.82 (dt, J=7.5, 17.8 Hz, 6H).




embedded image


Preparation of 5-(2-bromoethyl)-3,3-diethylpyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-5-(2-bromoethyl)-3,3-diethylpyrrolidin-2-one, except 5-(2-(benzyloxy)ethyl)-3,3-diethylpyrrolidin-2-one was substituted for (R)-5-(2-(benzyloxy)ethyl)-3,3-diethylpyrrolidin-2-one. 1H NMR (400 MHz, CDCl3) δ 8.06 (b, 1H), 3.64 (p, J=6.5 Hz, 1H), 3.40 (t, J=6.8 Hz, 2H), 2.06-1.86 (m, 3H), 1.58-1.34 (m, 5H), 0.81 (dt, J=7.5 16.8 Hz 6H).




embedded image


Preparation of (R)-3,3-diethyl-5-(2-hydroxyethyl)pyrrolidin-2-one: A 6M HCl in methanol solution was prepared via the addition of acetyl chloride (18 mL) to methanol (45 mL). tert-Butyl (R)-5-(2-((tert-butyldimethylsilyl)oxy)ethyl)-3,3-diethyl-2-oxopyrrolidine-1-carboxylate (3.98 g, 10 mmol, 1.0 equiv.) was dissolved in the prepared 6M methanolic HCl solution (45 mL) and stirred at 23° C. for 30 minutes. The resulting reaction solution was diluted with methanol and then concentrated in vacuo to give a crude product which used in the next step without further purification. 1H NMR (400 MHz, CDCl3) δ 7.28 (b, 1H), 3.82 (m, 2H), 3.68 (m, 1H), 2.07 (dd, J=7.7, 13.4 Hz, 1H), 1.70 (m, 2H), 1.61 (dd, J=7.7, 13.3 Hz, 1H), 1.57-1.39 (m, 4H), 0.84 (dt, J=7.5, 18.0 Hz, 6H).




embedded image


Preparation of (R)-2-(4,4-diethyl-5-oxopyrrolidin-2-yl)ethyl 4-methylbenzenesulfonate: To a cooled solution of (R)-3,3-diethyl-5-(2-hydroxyethyl)pyrrolidin-2-one (1.85 g, 10 mmol, 1.0 equiv.) and triethylamine (2.02 g, 20 mmol, 2.0 equiv.) in tetrahydrofuran/methylene chloride (50 mL:50 mL) at 0° C. was added 4-toluenesulfonyl chloride (2.85 g, 15 mmol, 1.5 equiv.) followed by 4-dimethylaminopyridine (0.122 g, 1 mmol, 0.2 equiv.). The resulting reaction mixture was stirred at 0° C. for 5 minutes before being warmed to 23° C. and allowed to stir for 72 hours. Then, the reaction mixture was diluted with dichloromethane (50 mL), washed with 1N HCl (1×50 mL) and deionized H2O (2×50 mL), dried over Na2SO4 and concentrated in vacuo to give a crude product which was further purified by column chromatography (Ethyl acetate/Hexanes, 20%˜75%). 1H NMR (400 MHz, CDCl3) δ 7.22 (d, J=8.2 Hz, 2H), 7.29 (d, J=7.9 Hz, 2H), 6.05 (b, 1H), 4.04 (t, J=5.8 Hz, 2H), 3.53 (p, J=6.8 Hz, 1H), 2.38 (s, 3H), 1.94 (dd, J=7.6, 13.2 Hz, 1H), 1.75 (q, J=6.0 Hz, 2H), 1.53-1.32 (m, 5H), 0.78 (dt, J=7.5, 21.5 Hz, 6H).




embedded image


Preparation of 3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one: To a small vial was added 5-(2-bromoethyl)-3,3-diethylpyrrolidin-2-one (50 mg, 0.201 mmol, 1 equiv.), 1-phenylpiperazine (69 mg, 0.422 mmol, 2.1 eq.) and tetrahydrofuran (3.5 mL). The reaction mixture was allowed to reflux overnight was then cooled to 23° C. The mixture was filtered, washed with tetrahydrofuran, and the filtrate was concentrated in vacuo to give a crude product which was further purified by column chromatography (MeOH/DCM, 0%˜10%). 1H NMR (400 MHz, CDCl3) δ 7.26 (m, 2H), 6.93 (d, J=8.1 Hz, 2H), 6.86 (t, J=7.2 Hz, 1H), 6.76 (b, 1H), 3.58 (m, 1H), 3.22 (t, J=5.0 Hz, 4H), 2.69 (m, 2H), 2.60-2.40 (m, 4H), 2.06 (dd, J=7.2, 13.1 Hz, 1H), 1.78-1.43 (m, 7H), 0.91 (dt, J=7.5, 13.5 Hz, 6H). LC/MS [M+H]=m/z 330.2




embedded image


Preparation of 3,3-diethyl-5-(2-(4-(p-tolyppiperazin-1-yl)ethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for 3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one, except 1-(4-methylphenyl)piperazine was substituted for 1-phenylpiperazine. 1H NMR (400 MHz, CDCl3) δ 7.07 (d, J=8.1 Hz, 2H), 6.84 (d, J=8.6 Hz, 2H), 6.74 (b, 1H), 3.58 (m, 1H), 3.16 (t, J=5.0 Hz, 4H), 2.69 (m, 2H), 2.56-2.40 (m, 4H), 2.27 (s, 3H), 2.05 (dd, J=7.3, 13.3 Hz, 1H), 1.78-1.43 (m, 7H), 0.91 (dt, J=7.4, 13.8 Hz, 6H). LC/MS [M+H]=m/z 344.2




embedded image


Preparation of 3,3-diethyl-5-(2-(4-(4-hydroxyphenyl)piperazin-1-yl)ethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for 3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)e thyl)pyrrolidin-2-one, except 1-(4-hydroxyphenyl)piperazine was substituted for 1-phenylpiperazine. 1H NMR (400 MHz, CDCl3) δ 7.23 (b, 1H), 6.73 (d, J=9.1 Hz, 2H), 6.68 (d, J=9.0 Hz, 2H), 3.59 (m, 1H), 3.04-2.87 (b, 4H), 2.69 (m, 2H), 2.57 (m, 1H), 2.45 (m, 3H), 2.06 (dd, J=7.4, 13.2 Hz, 1H), 1.75-1.43 (m, 7H), 0.91 (dt, J=7.5, 14.3 Hz, 6H). LC/MS [M+H]=m/z 346.2




embedded image


Preparation of 3 ,3-diethyl-5-(2-(4-(2-isopropylphenyl)piperazin-1-yl)ethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for 3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)e thyl)pyrrolidin-2-one, except 1-(2-isopropylphenyl)piperazine was substituted for 1-phenylpiperazine. 1H NMR (400 MHz, CDCl3) δ 7.26 (d, J=7.5 Hz, 1H), 7.20-7.04 (m, 3H), 6.79 (b, 1H), 3.59 (m, 1H), 3.49 (sept. J=6.8 Hz, 1H), 2.93 (t, J=4.6 Hz, 4H), 2.83-2.60 (b, 2H), 2.60-2.42 (m, 4H), 2.07 (dd, J=7.4, 13.1 Hz, 1H), 1.78-1.45 (m, 7H), 1.23 (dd, J=2.4, 6.9 Hz, 6H), 0.92 (dt, J=7.4, 18.3 Hz, 6H). LC/MS [M+H]=m/z 372.2




embedded image


Preparation of 5-(2-(4-(4-chlorophenyl)piperazin-1-yl)ethyl)-3,3-diethylpyrrolidin-2-one: The title compound was prepared according to the procedure for 3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)e thyl)pyrrolidin-2-one, except 1-(4-chlorophenyl)piperazine was substituted for 1-phenylpiperazine. 1HNMR (400 MHz, CDCl3) δ 7.19 (d, J=9.0 Hz, 2H), 6.83 (d, J=9.0 Hz, 2H), 6.73 (b, 1H), 3.57 (m, 1H), 3.17 (t, J=5.0 Hz, 4H), 2.68 (m, 2H), 2.58-2.40 (m, 4H), 2.05 (dd, J=7.4, 13.2 Hz, 1H), 1.76-1.42 (m, 7H), 0.90 (dt, J=7.4, 13.7 Hz, 6H). LC/MS [M+H]=m/z 364.2




embedded image


Preparation of 3,3-diethyl-5-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for 3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one, except 1-(4-fluorophenyl)piperazine was substituted for 1-phenylpiperazine. 1H NMR (400 MHz, CDCl3) δ 6.99-6.90 (m, 2H), 6.89-6.83 (m, 2H), 6.79 (b, 1H), 3.56 (m, 1H), 3.12 (t, J=4.9 Hz, 4H), 2.68 (m, 2H), 2.58-2.39 (m, 4H), 2.04 (dd, J=7.5, 13.2 Hz, 1H), 1.74-1.42 (m, 7H), 0.89 (dt, J=7.4, 13.9 Hz, 6H). LC/MS [M+H]=m/z 348.2




embedded image


Preparation of 3,3-diethyl-5-(2-(4-(2-morpholinophenyl)piperazin-1-yl)ethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for 3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one, except 4-(2-(piperazin-1-yl)phenyl)morpholine was substituted for 1-phenylpiperazine. 1H NMR (400 MHz, CDCl3) δ 6.91-6.84 (m, 2H), 6.84-6.74 (m, 2H), 6.51 (b, 1H), 3.71 (t, J=4.8 Hz, 4H), 3.46 (m, 1H), 3.36-2.77 (b, 8H), 2.74-2.07 (b, 6H), 1.94 (dd, J=7.5, 13.2 Hz, 1H), 1.65-1.31 (m, 7H), 0.79 (dt, J=7.3, 15.9 Hz, 6H). LC/MS [M+H]=m/z 415.2




embedded image


Preparation of 3,3-diethyl-5-(2-(4-(4-methyl-2-morpholinophenyl)piperazin-1-yl)ethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for 3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one, except 4-(5-methyl-2-(piperazin-1-yl)phenyl)morpholine was substituted for 1-phenylpiperazine. 1H NMR (400 MHz, CDCl3) δ 6.88-6.78 (m, 2H), 6.77-6.67 (m, 2H), 3.84 (t, J=4.6 Hz, 4H), 3.59 (m, 1H), 3.42-2.86 (b, 8H), 2.80-2.32 (b, 6H), 2.29 (s, 3H), 2.06 (dd, J=7.5, 13.3 Hz, 1H), 1.78-1.44 (m, 7H), 0.92 (dt, J=7.4, 15.6 Hz, 6H). LC/MS [M+H]=m/z 429.2




embedded image


Preparation of (R)-3 ,3-diethyl-5-(2-(4-(p-tolyl)piperazin-1-yl)ethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for 3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one, except (R)-5-(2-bromoethyl)-3,3-diethylpyrrolidin-2-one was substituted 5-(2-bromoethyl)-3,3-diethylpyrrolidin-2-one and 1-(4-methylphenyl)piperazine was substituted for 1-phenylpiperazine. 1H NMR (400 MHz, CDCl3) δ 7.07 (d, J=8.2 Hz, 2H), 6.84 (d, J=8.5 Hz, 2H), 6.41 (b, 1H), 3.57 (m, 1H), 3.16 (t, J=4.9 Hz, 4H), 2.69 (m, 2H), 2.58-2.40 (m, 4H), 2.27 (s, 3H), 2.05 (dd, J=7.3, 13.1 Hz, 1H), 1.77-1.43 (m, 7H), 0.91 (dt, J=7.4, 13.7 Hz, 6H). LC/MS [M+H]=m/z 344.2




embedded image


Preparation of (S)-3 ,3-diethyl-5-(2-(4-(p-tolyl)piperazin-1-yl)ethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for 3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one, except (S)-5-(2-bromoethyl)-3,3-diethylpyrrolidin-2-one was substituted 5-(2-bromoethyl)-3,3-diethylpyrrolidin-2-one and 1-(4-methylphenyl)piperazine was substituted for 1-phenylpiperazine. 1H NMR (400 MHz, CDCl3) δ 7.00 (d, J=8.5 Hz, 2H), 6.76 (d, J=8.5 Hz, 2H), 6.41 (b, 1H), 3.50 (m, 1H), 3.09 (t, J=5.1 Hz, 4H), 2.64 (m, 2H), 2.54-2.32 (m, 4H), 2.19 (s, 3H), 1.98 (dd, J=7.3, 13.1 Hz, 1H), 1.69-1.69 (m, 7H), 0.83 (dt, J=7.4, 14.5 Hz, 6H). LC/MS [M+H]=m/z 344.2




embedded image


Preparation of (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one: To a small vial was added (R)-2-(4,4-diethyl-5-oxopyrrolidin-2-yl)ethyl 4-methylbenzenesulfonate (75 mg, 0.22 mmol, 1 equiv.) and 1-phenylpiperazine (76 mg, 0.46 mmol, 2.1 equiv.) then both were dissolved in acetonitrile (2.2 mL). Then K2CO3 (77 mg, 0.55 mmol, 2.5 equiv.) was added, the reaction was allowed to stir at 80° C. overnight, and then cooled to 23° C. The mixture was filtered, washed with acetonitrile and the filtrate was concentrated in vacuo to give a crude product which was by further purified by column chromatography (MeOH/DCM, 0%˜10%). 1H NMR (400 MHz, CDCl3) δ 7.27 (m, 2H), 6.94 (d, J=8.1 Hz, 2H), 6.87 (t, J=7.2 Hz, 1H), 6.65 (b, 1H), 3.59 (m, 1H), 3.23 (t, J=5.0 Hz, 4H), 2.71 (m, 2H), 2.61-2.41 (m, 4H), 2.07 (dd, J=7.4, 13.1 Hz, 1H), 1.77-1.45 (m, 7H), 0.92 (dt, J=7.4, 14.0 Hz, 6H). LC/MS [M+H]=m/z 330.2.




embedded image


Preparation of (R)-3,3-diethyl-5-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)e thyl)pyrrolidin-2-one, except 1-(4-fluorophenyl)piperazine was substituted for 1-phenylpiperazine. 1H NMR (400 MHz, CDCl3) δ 7.00-6.91 (m, 2H), 6.91-6.82 (m, 2H), 6.74 (b, 1H), 3.57 (m, 1H), 3.13 (t, J=5.0 Hz, 4H), 2.70 (m, 2H), 2.60-2.41 (m, 4H), 2.05 (dd, J=7.3, 13.1 Hz, 1H), 1.76-1.44 (m, 7H), 0.90 (dt, J=7.5, 14.1 Hz, 6H). LC/MS [M+H]=m/z 348.2




embedded image


Preparation of (R)-5-(2-(4-(3,4-dichlorophenyl)piperazin-1-yl)ethyl)-3,3-diethylpyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)e thyl)pyrrolidin-2-one, except 1-(3,4-dichlorophenyl)piperazine was substituted for 1-phenylpiperazine. 1HNMR (400 MHz, CDCl3) δ 7.26 (d, J=9.0 Hz, 1H), 6.95 (d, J=2.9 Hz, 1H), 6.79-2.67 (b, 2H), 3.58 (m, 1H), 3.18 (t, J=5.0 Hz, 4H), 2.67 (m, 2H), 2.59-2.39 (m, 4H), 2.05 (dd, J=7.4, 13.1 Hz, 1H), 1.75-1.42 (m, 7H), 0.90 (dt, J=7.4, 13.7 Hz, 6H). LC/MS [M+H]=m/z 398.2.




embedded image


Preparation of (R)-5-(2-(4-(3-chloro-4-fluorophenyl)piperazin-1-yl)ethyl)-3,3-diethylpyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)e thyl)pyrrolidin-2-one, except 1-(3-chloro-4-fluorophenyl)piperazine was substituted for 1-phenylpiperazine. 1HNMR (400 MHz, CDCl3) δ 7.01 (t, J=8.8 Hz, 1H), 6.91 (dd, J=2.9, 6.2 Hz, 1H), 6.79-6.66 (b, 2H), 3.57 (m, 1H), 3.14 (t, J=5.0 Hz, 4H), 2.68 (m, 2H), 2.60-2.40 (m, 4H), 2.05 (dd, J=7.5, 13.2 Hz, 1H), 1.75-1.43 (m, 7H), 0.90 (dt, J=7.3, 13.9 Hz, 6H). LC/MS [M+H]=m/z 382.2.




embedded image


Preparation of (R)-5-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-3,3-diethylpyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)e thyl)pyrrolidin-2-one, except 1-(3-chlorophenyl)piperazine was substituted for 1-phenylpiperazine. 1H NMR (400 MHz, CDCl3) δ 7.16 (t, J=8.1 Hz, 1H), 6.87 (t, J=2.1 Hz, 1H), 6.83-6.75 (m, 2H), 6.71 (b, 1H), 3.58 (m, 1H), 3.21 (t, J=5.0 Hz, 4H), 2.68 (m, 2H), 2.60-2.40 (m, 4H), 2.06 (dd, J=7.2, 13.1 Hz, 1H), 1.76-1.44 (m, 7H), 0.91 (dt, J=7.4, 13.8 Hz, 6H). LC/MS [M+H]=m/z 364.2




embedded image


Preparation of (R)-5-(2-(4-(2-chlorophenyl)piperazin-1-yl)ethyl)-3,3-diethylpyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)e thyl)pyrrolidin-2-one, except 1-(2-chlorophenyl)piperazine was substituted for 1-phenylpiperazine. 1H NMR (400 MHz, CDCl3) δ 7.27 (dd, J=1.5, 7.9 Hz, 1H), 7.14 (td, J=1.5, 7.7 Hz, 1H), 6.98 (dd, J=1.5, 8.0 Hz, 1H), 6.89 (td, J=1.5, 7.7 Hz, 1H), 6.63 (b, 1H), 3.50 (m, 1H), 3.18-2.83 (b, 4H), 2.77-2.56 (b, 2H), 2.55-2.31 (m, 4H), 1.98 (dd, J=7.4, 13.1 Hz, 1H), 1.69-1.36 (m, 7H), 0.83 (dt, J=7.4, 16.9 Hz, 6H). LC/MS [M+H]=m/z 364.2




embedded image


Preparation of (R)-5-(2-(4-(3-fluorophenyl)piperazin-1-yl)ethyl)-3,3-diethylpyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)e thyl)pyrrolidin-2-one, except 1-(3-fluorophenyl)piperazine was substituted for 1-phenylpiperazine. 1H NMR (400 MHz, CDCl3) δ 7.10 (m, 1H), 6.64-6.54 (b, 2H), 6.50 (dt, J=2.4, 12.4 Hz, 1H), 6.45 (td, J=2.3, 8.2 Hz, 1H), 3.50 (m, 1H), 3.14 (t, J=5.0 Hz, 4H), 2.60 (m, 2H), 2.51-2.30 (m, 4H), 1.98 (dd, J=7.3, 13.2 Hz, 1H), 1.67-1.36 (m, 7H), 0.83 (dt, J=7.3, 14.0 Hz, 6H). LC/MS [M+H]=m/z 348.2




embedded image


Preparation of (R)-5-(2-(4-(2-methylphenyl)piperazin-1-yl)ethyl)-3,3-diethylpyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)e thyl)pyrrolidin-2-one, except 1-(2-methylphenyl)piperazine was substituted for 1-phenylpiperazine. 1H NMR (400 MHz, CDCl3) δ 7.17 (m, 2H), 7.04 (dd, J=1.2, 8.5 Hz, 1H), 6.99 (td, J=1.2, 7.4 Hz, 1H), 6.73 (b, 1H), 3.59 (m, 1H), 3.03-2.89 (b, 4H), 2.83-2.62 (b, 2H), 2.62-2.38 (m, 4H), 2.31 (s, 3H), 2.07 (dd, J=7.5, 13.1 Hz, 1H), 1.77-1.45 (m, 7H), 0.92 (dt, J=7.5, 17.5 Hz, 6H). LC/MS [M+H]=m/z 344.2




embedded image


Preparation of (R)-5-(2-(4-(3-methylphenyl)piperazin-1-yl)ethyl)-3,3-diethylpyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one, except 1-(3-methylphenyl)piperazine was substituted for 1-phenylpiperazine. 1HNMR (400 MHz, CDCl3) δ 7.16 (t, J=7.8 Hz, 1H), 6.80-6.68 (m, 3H), 6.63 (b, 1H), 3.59 (m, 1H), 3.22 (t, J=5.0 Hz, 4H), 2.71 (m, 2H), 2.61-2.41 (m, 4H), 2.33 (s, 3H), 2.07 (dd, J=7.4, 13.2 Hz, 1H), 1.78-1.45 (m, 7H), 0.92 (dt, J=7.4, 14.0 Hz, 6H). LC/MS [M+H]=m/z 344.2




embedded image


Preparation of tert-butyl (R)-3,3-diallyl-5-(2-((tert-butyldimethylsilyl)oxy)ethyl)-2-oxopyrrolidine-1-carboxylate: This reaction was performed in oven-dried glassware under a nitrogen atmosphere. A stirred solution of tert-butyl (R)-2-(2-((tert-butyldimethylsilyl)oxy)ethyl)-5-oxopyrrolidine-1-carboxylate (10.0 g, 29.0 mmol, 1.0 equiv.) in dry tetrahydrofuran (43 mL) was cooled to −78° C. and 1M lithium bis(trimethylsilyl)amide solution (tetrahydrofuran, 63.8 mL, 63.8 mmol, 2.2 equiv.) was added dropwise while maintaining the reaction temperature below −70° C. The resulting solution was allowed to slowly warm to −30° C. before being cooled back to −78° C. at which time allyl iodide (10.71 g, 63.8 mmol, 2.2 equiv.) was slowly added dropwise. The resulting solution was slowly warmed to −20° C. and then quenched with sat. NH4Cl (75 mL) and extracted with ethyl acetate (3×75 mL). The combined organic layers were dried over Na2SO4 and concentrated in vacuo to give a crude product which was further purified by column chromatography (Ethyl acetate/Hexanes, 0% 10%). 1H NMR (400 MHz, CDCl3) δ 5.77-5.58 (m, 2H), 5.12-4.99 (m, 4H), 3.96 (m, 1H), 3.63 (t, J=6.2 Hz, 2H), 2.40-2.09 (m, 5H), 2.01 (dd, J=8.6, 13.6 Hz, 1H), 1.70 (dd, J=6.4, 13.6 Hz, 1H), 1.57-1.42 (m, 10H), 0.84 (s, 9H), 0.00 (s, 6H).




embedded image


Preparation of tert-butyl (S)-3,3-diallyl-5-(2-((tert-butyldimethylsilyl)oxy)ethyl)-2-oxopyrrolidine-1-carboxylate: The title compound was prepared according to the procedure for tert-butyl (R)-3,3-diallyl-5-(2-((tert-butyldimethylsilyl)oxy)ethyl)-2-oxopyrrolidine-1-carboxylate, except tert-butyl (S)-2-(2-((tert-butyldimethylsilyl)oxy)ethyl)-5-oxopyrrolidine-1-carboxylate was substituted for tert-butyl (R)-2-(2-((tert-butyldimethylsilyl)oxy)ethyl)-5-oxopyrrolidine-1-carboxylate. 1H NMR (400 MHz, CDCl3) δ 5.79-5.60 (m, 2H), 5.13-4.98 (m, 4H), 3.96 (m, 1H), 3.62 (t, J=6.2 Hz, 2H), 2.40-2.10 (m, 5H), 2.00 (dd, J=8.6, 13.6 Hz, 1H), 1.69 (dd, J=6.3, 13.6 Hz, 1H), 1.58-1.42 (m, 10H), 0.83 (s, 9H), 0.00 (s, 6H).




embedded image


Preparation of tert-butyl (R)-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2-azaspiro[4.4]non-7-ene-2-carboxylate: To a stirred solution of tert-butyl (R)-3,3-diallyl-5-(2-((tert-butyldimethylsilyl)oxy)ethyl)-2-oxopyrrolidine-1-carboxylate (10.03 g, 23.6 mmol, 1.0 equiv.) in methylene chloride (200 mL) was added benzylidene-bis(tricyclohexyl(phophine) dichlororuthenium (0.388 g, 0.472 mmol, 2 mol %). The resulting solution was allowed to stir at 23° C. for 4 hours before being concentrated in vacuo to give a crude product which was further purified by column chromatography (Ethyl acetate/Hexanes, 0%˜20%). 1H NMR (400 MHz, CDCl3) δ 5.56 (m, 2H), 4.08 (m, 1H), 3.66 (t, J=6.1 Hz, 2H), 2.86 (m, 2H), 2.36 (m, 1H), 2.29-2.14 (m, 2H), 2.09 (dd, J=8.0, 13.0 Hz, 1H), 1.98 (dd, J=3.9, 13.0 Hz, 1H), 1.60 (m, 1H), 1.48 (s, 9H), 0.83 (s, 9H), 0.00 (s, 6H).




embedded image


Preparation of tert-butyl (S)-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2-azaspiro[4.4]non-7-ene-2-carboxylate: The title compound was prepared according to the procedure for tert-butyl (R)-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2-azaspiro[4.4]non-7-ene-2-carboxylate, except tert-butyl (S)-3,3-diallyl-5-(2-((tert-butyldimethylsilyl)oxy)ethyl)-2-oxopyrrolidine-1-carboxylate was substituted for tert-butyl (R)-3,3-diallyl-5-(2-((tert-butyldimethylsilyl)oxy)ethyl)-2-oxopyrrolidine-1-carboxylate. 1H NMR (400 MHz, CDCl3) δ 5.56 (m, 2H), 4.08 (m, 1H), 3.66 (t, J=6.1 Hz, 2H), 2.87 (m, 2H), 2.36 (m, 1H), 2.30-2.14 (m, 2H), 2.09 (dd, J=8.0, 13.1 Hz, 1H), 1.98 (dd, J=3.9, 13.1 Hz, 1H), 1.60 (m, 1H), 1.48 (s, 9H), 0.83 (s, 9H), 0.00 (s, 6H).




embedded image


Preparation of tert-butyl (R)-8-benzyl-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2,8-diazaspiro[4.5]decane-2-carboxylate: A stirred solution of tert-butyl (R)-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2-azaspirop.41non-7-ene-2-carboxylate (9.04 g, 22.8 mmol, 1.0 equiv.) in methylene chloride (235 mL) and methanol (7.7 mL) was cooled to −78° C. and a gaseous stream of O3/O2 was bubbled through the solution until the color developed a purple tint (45 minutes). Residual O3 was removed by bubbling O2 through the solution for 10 minutes. At −78° C., NaBH(OAc)3 (4.93 g, 23.2 mmol, 1.02 equiv.) was added and the reaction mixture was allowed to warm to 23° C. and stir for 45 minutes. Next, BnNH2 (2.70 g, 25.2 mmol, 1.1 equiv.) and NaBH(OAc)3 (9.72 g, 45.8 mmol, 2.0 equiv.) were sequentially added and the reaction was stirred at 23° C. overnight. The resulting mixture was filtered and concentrated in vacuo to give a crude product which was further purified by column chromatography (2M Ammonia in MeOH/methylene chloride, 0%˜2%). 1H NMR (400 MHz, CDCl3) δ 7.34-7.19 (m, 5H), 4.03 (m, 1H), 3.65 (t, J=5.9 Hz, 2H) 3.54 (b, 2H), 2.94 (b, 2H), 2.41 (b, 2H), 2.19 (m, 1H), 2.08-1.86 (m, 3H), 1.79 (dd, J=4.7, 13.5 Hz, 1H), 1.60-1.40 (m, 12H), 0.84 (s, 9H), 0.00 (s, 6H).




embedded image


Preparation of tert-butyl (S)-8-benzyl-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2,8-diazaspiro[4.5]decane-2-carboxylate: The title compound was prepared according to the procedure for tert-butyl (R)-8-benzyl-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2,8-diazaspiro[4.5]decane-2-carboxylate, except tert-butyl (S)-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2-azaspirop.41non-7-ene-2-carboxylate was substituted for tert-butyl (R)-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2-azaspiro[4.4]non-7-ene-2-carboxylate. 1H NMR (400 MHz, CDCl3) δ 7.32-7.14 (m, 5H), 4.02 (m, 1H), 3.65 (t, J=5.9 Hz, 2H) 3.54 (b, 2H), 2.84 (b, 2H), 2.41 (b, 2H), 2.19 (m, 1H), 2.05-1.86 (m, 3H), 1.80 (dd, J=4.7, 13.3 Hz, 1H), 1.60-1.39 (m, 12H), 0.84 (s, 9H), 0.00 (s, 6H).




embedded image


Preparation of (R)-3-(2-hydroxyethyl)-2,8-diazaspiro[4.5]decan-1-one: To a round bottom flask was added 10% Pd/C (1.27 g, 20% by weight) followed by a solution of tert-butyl (R)-8-benzyl-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2,8-diazaspiro [4 .5]decane-2-carboxylate (6.32 g, 12.5 mmol, 1 equiv.) in methanol (83 mL). The reaction was put under H2 (1 atm) using a balloon and stirred at 23° C. overnight. The reaction was filtered through a plug of Celite and concentrated filtrate under reduced pressure to give a crude intermediate.


A 6M HCl in methanol solution was prepared via the addition of acetyl chloride (60 mL) to methanol (160 mL). The crude intermediate was dissolved in the prepared 6M methanolic HCl solution (160 mL) and stirred at 23° C. for 30 minutes before being diluted with methanol and concentrated in vacuo to produce a crude product as an HCl salt. The product was free based by stirring with Amberlite IRN-78 base resin in methanol (˜150 mL) for 15 minutes followed by filtration and concentrated in vacuo to produce a crude product that was used in the next step without further purification. 1H NMR (400 MHz, MeOD) δ 3.82-3.61 (m, 3H), 3.02 (m, 2H), 2.76 (td, J=2.9, 12.9 Hz, 1H), 2.64 (td, J=2.9, 12.9 Hz, 1H), 2.46 (dd, J=7.0, 13.0 Hz, 1H), 1.93 (td, J=4.4, 12.7 Hz, 1H), 1.86-1.74 (m, 1H), 1.74-1.64 (m, 2H), 1.60 (dd, J=8.2, 12.9 Hz, 1H), 1.49 (d, J=13.2 Hz, 1H), 1.36 (d, J=13.6 Hz, 1H).




embedded image


Preparation of (S)-3-(2-hydroxyethyl)-2,8-diazaspiro[4.5]decan-1-one: The title compound was prepared according to the procedure for (R)-3-(2-hydroxyethyl)-2,8-diazaspiro[4 .5]decan-1-one, except tert-butyl (R)-8-benzyl-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2,8-diazaspiro [4 .5] decane-2-carboxylate was substituted for tert-butyl (S)-8-benzyl-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2,8-diazaspiro[4.5]decane-2-carboxylate 1H NMR (400 MHz, MeOD) δ 3.82-3.60 (m, 3H), 3.02 (m, 2H), 2.76 (td, J=2.9, 12.9 Hz, 1H), 2.64 (td, J=2.9, 12.9 Hz, 1H), 2.46 (dd, J=7.1, 13.2 Hz, 1H), 1.93 (td, J=3.7, 12.3 Hz, 1H), 1.86-1.75 (m, 1H), 1.75-1.64 (m, 2H), 1.60 (dd, J=8.0, 12.7 Hz, 1H), 1.49 (d, J=13.1 Hz, 1H), 1.37 (d, J=13.0 Hz, 1H).




embedded image


Preparation of tert-butyl (R)-3-(2-hydroxyethyl)-1-oxo-2,8-diazaspiro [4.5]decane-8-carboxylate: To a solution of (R)-3-(2-hydroxyethyl)-2,8-diazaspiro[4.5]decan-1-one (2.2 g, 11.0 mmol, 1.0 equiv.) and triethylamine (1.12 g, 11.0 mmol, 1.0 equiv.) in methylene chloride (113 mL) and methanol (3 mL) was added di-tert-butyl dicarbonate (2.4 g, 11.0 mmol, 1.0 equiv.). The resulting solution was allowed to stir at 23° C. overnight before being concentrated in vacuo to produce a crude product that was used in the next step without further purification. 1H NMR (400 MHz, CDCl3) δ 6.93 (b, 1H), 4.15-3.55 (b, 6H), 3.15-2.74 (m, 2H), 2.29 (dd, J=6.7, 12.5 H, 1H), 2.00-1.82 (m, 1H), 1.80-1.60 (m, 3H), 1.58-1.29 (m, 12).




embedded image


Preparation of tert-butyl (S)-3-(2-hydroxyethyl)-1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate: The title compound was prepared according to the procedure for (tert-butyl (R)-3-(2-hydroxyethyl)-1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate, except (S)-3-(2-hydroxyethyl)-2,8-diazaspiro[4 .5]decan-1-one was substituted for (R)-3-(2-hydroxyethyl)-2,8-diazaspiro[4.5]decan-1-one. 1H NMR (400 MHz, CDCl3) δ 6.53 (b, 1H), 4.06-3.56 (b, 6H), 3.05-2.77 (m, 2H), 2.25 (dd, J=6.7, 12.9 H, 1H), 1.93-1.80 (m, 1H), 1.74-1.56 (m, 3H), 1.52-1.24 (m, 12).




embedded image


Preparation of (S)-3-(2-hydroxyethyl)-2-azaspiro[4.4]nonan-1-one: To a round bottom flask was added 10% Pd/C (0.60 g, 20% by wieght) followed by a solution of tert-butyl (S)-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2-azaspiro[4.4]non-7-ene-2-carboxylate (0.30 g, 0.758 mmol, 1 equiv.) in methanol (7.5 mL). The reaction was put under H2 (1 atm) using a balloon and stirred at 23° C. for 4 hrs. The reaction was filtered through a plug of Celite and concentrated filtrate under reduced pressure to give a crude intermediate.


A 6M HCl in methanol solution was prepared via the addition of acetyl chloride (3 mL) to methanol (7.5 mL). The crude intermediate was dissolved in the prepared 6M methanolic HCl solution (7.5 mL) and stirred at 23° C. for 30 minutes before being diluted with methanol and concentrated in vacuo to produce a crude product was used in the next step without further purification. 1H NMR (400 MHz, CDCl3) δ 6.95 (b, 1H), 3.99 (b, 1H), 3.76 (m, 1H), 3.64 (m, 2H), 2.09 (dd, J=6.6, 12.6 Hz, 1H), 2.01 (m, 1H), 1.81-1.45 (m, 9H), 1.37 (m, 1H).




embedded image


Preparation of (S)-3-(2-hydroxyethyl)-2-azaspiro[4.4]non-7-en-1-one: A 6M HCl in methanol solution was prepared via the addition of acetyl chloride (3 mL) to methanol (7.5 mL). tert-Butyl (S)-3-(2-((tert-butyldimethylsilyl)oxy)ethyl)-1-oxo-2-azaspiro[4.4]non-7-ene-2-carboxylate (0.30 g, 0.758 mmol, 1 equiv.) was dissolved in the prepared 6M methanolic HCl solution (7.5 mL) and stirred at 23° C. for —30 minutes before being diluted with methanol and concentrated in vacuo to produce a crude product was used in the next step without further purification. 1H NMR (400 MHz, CDCl3) δ 7.04 (b, 1H), 5.62 (m, 1H), 5.52 (m, 1H), 3.83-3.71 (m, 2H), 3.70-3.57 (m, 2H), 2.90 (dp, J=2.4, 16.6 Hz, 1H), 2.58 (dp, J=2.4, 16.3 Hz, 1H), 2.33 (d, J=16.4 Hz, 1H), 2.22 (dd, J=6.2, 12.4 Hz, 1H), 2.14 (d, J=16.2 Hz, 1H), 1.71-1.54 (m, 3H).




embedded image


Preparation of tert-butyl (R)-1-oxo-3-(2-(tosyloxy)ethyl)-2,8-diazaspiro[4.5]decane-8-carboxylate: To a cooled solution of tert-butyl (R)-3-(2-hydroxyethyl)-1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate (3.2 g, 10.7 mmol, 1.0 equiv.) and triethylamine (2.16 g, 21.4 mmol, 2.0 equiv.) in tetrahydrofuran/methylene chloride (46 mL:46 mL) at 0° C. was added 4-toluenesulfonyl chloride (3.06 g, 16 mmol, 1.5 equiv.) followed by 4-dimethylaminopyridine (0.131 g, 1.07 mmol, 0.2 equiv.). The resulting reaction mixture was stirred at 0° C. for 5 minutes before being warmed to 23° C. and allowed to stir overnight. Then, the reaction mixture was diluted with dichloromethane (50 mL) and washed with deionized H2O (1×50 mL). The aqueous layer was backwashed with methylene chloride (2×50 mL). The combined organic phase was dried over Na2SO4 and concentrated in vacuo to give a crude product which was further purified by HPLC (CH3CN/H2O, 0.1% Formic acid), 0%˜100%). 1H NMR (400 MHz, CDCl3) δ 7.81 (d, J=8.3 Hz, 2H), 7.38 (d, J=8.2 Hz, 2H), 6.11 (b, 1H), 4.14 (m, 2H), 4.07-3.89 (b, 2H), 3.72 (p, J=6.8 Hz, 1H), 2.97 (m, 2H), 2.48 (s, 3H), 2.28 (dd, J=6.9, 12.8 Hz, 1H), 1.97-1.83 (m, 3H), 1.75 (m, 1H), 1.56-1.30 (m, 12H).




embedded image


Preparation of tert-butyl (S)-1-oxo-3-(2-(tosyloxy)ethyl)-2,8-diazaspiro[4.5]decane-8-carboxylate: The title compound was prepared according to the procedure for tert-butyl (R)-1-oxo-3-(2-(tosyloxy)ethyl)-2,8-diazaspiro[4.5]decane-8-carboxylate, except tert-butyl (S)-3-(2-hydroxyethyl)-1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate was substituted for tert-butyl (R)-3-(2-hydroxyethyl)-1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate. 1H NMR (400 MHz, CDCl3) δ 7.77 (d, J=8.3 Hz, 2H), 7.34 (d, J=8.2 Hz, 2H), 7.05 (b, 1H), 4.11 (m, 2H), 4.05-3.78 (b, 2H), 3.68 (p, J=6.8 Hz, 1H), 2.92 (m, 2H), 2.43 (s, 3H), 2.22 (dd, J=6.8, 12.9 Hz, 1H), 1.93-1.76 (m, 3H), 1.68 (m, 1H), 1.53-1.24 (m 12H).




embedded image


Preparation of (S)-2-(1-oxo-2-azaspiro[4.4]non-7-en-3-yl)ethyl 4-methylbenzenesulfonate: To a cooled solution of (S)-3-(2-hydroxyethyl)-2-azaspiro[4.4]non-7-en-1-one (0.140 g, 0.758 mmol, 1.0 equiv.) and N-methylimidazole (0.312 g, 3.8 mmol, 5.0 equiv.) in methylene chloride (2.5 mL) at 0° C. was added a solution of 4-toluenesulfonyl chloride (0.217 g, 1.14 mmol, 1.5 equiv.) in methylene chloride (3.5 mL). The resulting reaction mixture was stirred at 0° C. for 5 min utesbefore being warmed to 23° C. and allowed to stir overnight. Then, the reaction mixture was quenched with 1N HCl (1×5 mL) and extracted with methylene chloride (3×15 mL). The combined organic phase was dried over Na2SO4 and concentrated in vacuo to give a crude product which was further by column chromatography (Ethyl acetate/Hexanes, 40%˜100%). 1H NMR (400 MHz, CDCl3) δ 7.71 (d, J=8.3 Hz, 2H), 7.27 (d, J=8.1 Hz, 2H), 6.97 (b, 1H), 5.58 (m, 1H), 5.51 (m, 1H), 4.04 (m, 2H), 3.58 (p, J=6.8 Hz, 1H), 2.86 (dp, J=2.3, 16.5 Hz, 1H), 2.58 (dp, J=2.3, 16.3 Hz, 1H), 2.37 (s, 3H), 2.25 (d, J=16.1 Hz, 1H), 2.19-2.04 (m, 2H), 1.86-1.67 (m, 2H), 1.54 (dd, J=7.7, 12.5 Hz, 1H).




embedded image


Preparation of (S)-2-(1-oxo-2-azaspiro[4.4]nonan-3-yl)ethyl 4-methylbenzenesulfonate: The title compound was prepared according to the procedure for (S)-2-(1-oxo-2-azaspiro[4.4]non-7-en-3-yl)ethyl 4-methylbenzenesulfonate, except (S)-3-(2-hydroxyethyl)-2-azaspiro[4.4]nonan-1-one was substituted for (S)-3-(2-hydroxyethyl)-2-azaspiro[4.4]non-7-en-1-one. 1H NMR (400 MHz, CDCl3) δ 7.78 (d, J=8.2 Hz, 2H), 7.34 (d, J=8.1 Hz, 2H), 6.87 (b, 1H), 4.10 (m, 2H), 3.60 (p, J=6.7 Hz, 1H), 2.44 (s, 3H), 2.12-1.97 (m, 2H), 1.94-1.68 (m, 5H), 1.66-1.45 (m, 4H), 1.40 (m, 1H).




embedded image


Preparation of (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl ethyl)-2-azaspiro[4.4]non-7-en-1-one: To a small vial was added (S)-2-(1-oxo-2-azaspiro[4.4]non-7-en-3-yl)ethyl 4-methylbenzenesulfonate (50 mg, 0.15 mmol, 1 equiv.) and 1-(4-fluorophenyl)piperazine (57 mg, 0.31 mmol, 2.1 equiv.) then both were dissolved in acetonitrile (1.5 mL). Then K2CO3 (52 mg, 0.37 mmol, 2.5 equiv.) was added, the reaction was allowed to stir at 80° C. overnight, and then cooled to 23° C. The mixture was filtered, washed with acetonitrile and filtrate was concentrated in vacuo to give a crude product which was by further purified by column chromatography (MeOH/methylene chloride, 0%˜10%). 1H NMR (400 MHz, CDCl3) δ 7.00-6.82 (m, 5H), 5.70 (m, 1H), 5.59 (m, 1H), 3.63 (m, 1H), 3.13 (t, J=4.9 Hz, 4H), 3.02 (dp, J=2.5, 16.5 Hz, 1H), 2.76-2.62 (m, 3H), 2.61-2.43 (m, 4H), 2.39 (d, J=16.6 Hz, 1H), 2.29 (dd, J=6.1, 12.4 Hz, 1H), 2.20 (d, J=16.4 Hz, 1H), 1.80-1.57 (m, 3H). LC/MS [M+H]=m/z 344.2




embedded image


Preparation of (S)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl ethyl)-2-azaspiro[4.4]non-7-en-1-one: The title compound was prepared according to the procedure for (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2-azaspiro[4 .4]non-7-en-1-one, except 1-(3-chlorophenyl)piperazine was substituted for 1-(4-fluorophenyl)piperazine. 1H NMR (400 MHz, CDCl3) δ 7.08 (t, J=8.0 Hz, 1H), 6.79 (t, J=2.1 Hz, 1H), 6.77-6.65 (m, 3H). 5.60 (m, 1H), 5.51 (m, 1H), 3.56 (m, 1H), 3.13 (t, J=5.1 Hz, 4H), 2.95 (dp, J=2.4, 16.6 Hz, 1H), 2.68-2.54 (m, 3H), 2.54-2.35 (m, 4H), 2.31 (d, J=16.0 Hz, 1H), 2.22 (dd, J=6.1, 12.3 Hz, 1H), 2.13 (d, J=16.5 Hz, 1H), 1.72-1.49 (m, 3H). LC/MS [M+H]=m/z 360.2.




embedded image


Preparation of (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl ethyl)-2-azaspiro[4.4]nonan-1-one: The title compound was prepared according to the procedure for (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2-azaspiro[4.4]non-7-en-1-one, except (S)-2-(1-oxo-2-azaspiro[4.4]nonan-3-yl)ethyl 4-methylbenzenesulfonate was substituted for (S)-2-(1-oxo-2-azaspiro[4.4]non-7-en-3-yl)ethyl 4-methylbenzenesulfonate. 1H NMR (400 MHz, CDCl3) δ 7.00-6.91 (m, 2H), 6.90-6.74 (m, 3H), 3.59 (m, 1H), 3.12 (t, J=4.9 Hz, 4H), 2.69 (m, 2H), 2.60-2.44 (m, 4H), 2.19-2.06 (m, 2H), 1.86-1.51 (m, 9H), 1.44 (m, 1H). LC/MS [M+H]=m/z 346.2.




embedded image


Preparation of (S)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl ethyl)-2-azaspiro[4.4]nonan-1-one: The title compound was prepared according to the procedure for (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2-azaspiro[4.4]non-7-en-1-one, except (S)-2-(1-oxo-2-azaspiro[4.4]nonan-3-yl)ethyl 4-methylbenzenesulfonate was substituted for (S)-2-(1-oxo-2-azaspiro[4.4]non-7-en-3-yl)ethyl 4-methylbenzenesulfonate and 1-(3-chlorophenyl)piperazine was substituted for 1-(4-fluorophenyl)piperazine. 1H NMR (400 MHz, CDCl3) δ 7.16 (t, J=8.0 Hz, 1H), 6.88 (t, J=2.1 Hz, 1H), 6.81 (dd, J=1.7, 7.8 Hz, 1H), 6.78 (dd, J=2.3, 8.3 Hz, 1H), 6.69 (b, 1H), 3.60 (m, 1H), 3.22 (t, J=5.0 Hz, 4H), 2.69 (m, 2H), 2.61-2.39 (m, 4H), 2.23-2.08 (m, 2H), 1.87-1.55 (m, 9H), 1.46 (m, 1H). LC/MS [M+H]=m/z 362.2.




embedded image


Preparation of tert-butyl (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-1-oxo-2,8-diazaspirop.51decane-8-carboxylate: The title compound was prepared according to the procedure for (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2-azaspiro[4.4]non-7-en-1-one, except tert-butyl (R)-1-oxo-3-(2-(tosyloxy)ethyl)-2,8-diazaspiro[4.5]decane-8-carboxylate was substituted for (S)-2-(1-oxo-2-azaspiro[4.4]non-7-en-3-yl)ethyl 4-methylbenzenesulfonate and 1-(3-chlorophenyl)piperazine was substituted for 1-(4-fluorophenyl)piperazine. 1H NMR (400 MHz, CDCl3) δ 7.15 (t, J=7.9 Hz, 1H), 7.06 (b, 1H), 6.84 (t, J=2.0 Hz, 1H), 6.79 (dd, J=1.6, 7.6 Hz, 1H), 6.74 (dd, J=2.1, 8.3 Hz, 1H), 4.13-3.82 (b, 2H), 3.63 (p, J=7.0 Hz, 1H), 3.20 (t, J=4.8 Hz, 4H), 3.10-2.83 (m, 2H), 2.67 (m, 2H), 2.60-2.40 (m, 4H), 2.29 (dd, J=6.7, 12.8 Hz, 1H), 1.96 (m, 1H), 1.80-1.62 (m, 3H), 1.58-1.30 (m, 12H). LC/MS [M+H]=m/z 478.2.




embedded image


Preparation of tert-butyl (R)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-1-oxo-2,8-diazaspirop.51decane-8-carboxylate: The title compound was prepared according to the procedure for (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2-azaspirop.41non-7-en-1-one, except tert-butyl (R)-1-oxo-3-(2-(tosyloxy)ethyl)-2,8-diazaspiro[4.5]decane-8-carboxylate was substituted for (S)-2-(1-oxo-2-azaspiro[4.4]non-7-en-3-yl)ethyl 4-methylbenzenesulfonate. 1H NMR (400 MHz, CDCl3) δ 7.02 (b, 1H), 6.97-6.90 (m, 2H), 6.90-6.80 (m, 2H), 4.23-3.78 (b, 2H), 3.63 (p, J=6.5 Hz, 1H), 3.12 (t, J=4.7 Hz, 4H), 3.07-2.82 (m, 2H), 2.68 (m, 2H), 2.60-2.40 (m, 4H), 2.28 (dd, J=6.7, 12.7 Hz, 1H), 1.95 (m, 1H), 1.80-1.61 (m, 3H), 1.58-1.29 (m, 12H). LC/MS [M+H]=m/z 461.2.




embedded image


Preparation of tert-butyl (S)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-1-oxo-2,8-diazaspirop.51decane-8-carboxylate: The title compound was prepared according to the procedure for (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2-azaspirop.41non-7-en-1-one, except tert-butyl (S)-1-oxo-3-(2-(tosyloxy)ethyl)-2,8-diazaspiro[4.5]decane-8-carboxylate was substituted for (S)-2-(1-oxo-2-azaspiro[4.4]non-7-en-3-yl)ethyl 4-methylbenzenesulfonate and 1-(3-chlorophenyl)piperazine was substituted for 1-(4-fluorophenyl)piperazine. 1H NMR (400 MHz, CDCl3) δ 7.14 (t, J=8.0 Hz, 1H), 7.04 (b, 1H), 6.85 (t, J=2.0 Hz, 1H), 6.79 (dd, J=1.6, 7.7 Hz, 1H), 6.76 (dd, J=2.1, 8.3 Hz, 1H), 4.13-3.83 (b, 2H), 3.63 (p, J=7.0 Hz, 1H), 3.19 (t, J=4.8 Hz, 4H), 3.09-2.80 (m, 2H), 2.67 (m, 2H), 2.60-2.39 (m, 4H), 2.29 (dd, J=6.6, 12.8 Hz, 1H), 1.95 (m, 1H), 1.80-1.63 (m, 3H), 1.57-1.30 (m, 12H). LC/MS [M+H]=m/z 478.2




embedded image


Preparation of tert-butyl (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-1-oxo-2,8-diazaspirop.51decane-8-carboxylate: The title compound was prepared according to the procedure for (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2-azaspiro[4.4]non-7-en-1-one, except tert-butyl (S)-1-oxo-3-(2-(tosyloxy)ethyl)-2,8-diazaspiro[4.5]decane-8-carboxylate was substituted for (S)-2-(1-oxo-2-azaspiro[4.4]non-7-en-3-yl)ethyl 4-methylbenzenesulfonate. NMR (400 MHz, CDCl3) δ 7.01 (b, 1H), 6.97-6.89 (m, 2H), 6.89-6.80 (m, 2H), 4.21-3.76 (b, 2H), 3.63 (p, J=6.5 Hz, 1H), 3.11 (t, J=4.7 Hz, 4H), 3.06-2.82 (m, 2H), 2.69 (m, 2H), 2.61-2.41 (m, 4H), 2.29 (dd, J=6.7, 12.8 Hz, 1H), 1.94 (m, 1H), 1.80-1.60 (m, 3H), 1.57-1.28 (m, 12H). LC/MS [M+H]=m/z 461.




embedded image


Preparation of (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one: A 6M HCl in methanol solution was prepared via the addition of acetyl chloride (1.2 mL) to methanol (3 mL). tert-Butyl (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate (0.127 g, 0.266 mmol, 1.0 equiv.) was dissolved in the prepared 6M methanolic HCl solution (3 mL) and let stir at 23° C. for 30 minutes before being diluted with methanol and concentrated in vacuo to produce a crude product as an HCl salt. The product was free based by stirring with Amberlite IRN-78 base resin in methanol (˜10 mL) for 15 minutes followed by filtration and concentrated in vacuo to produce a crude product that was used in the next step without further purification. 1H NMR (400 MHz, MeOD) δ 7.21 (t, J=8.3 Hz, 1H), 6.95 (s, 1H), 6.88 (d, J=8.5 Hz, 1H), 6.81 (d, J=7.7 Hz, 1H), 3.68 (m, 1H), 3.29-3.13 (m, 4H), 3.01 (m, 2H), 2.81-2.38 (m, 9H), 1.93 (m, 1H), 1.86-1.64 (m, 3H), 1.60 (dd, J=7.6, 12.7 Hz, 1H), 1.49 (d, J=13.2 Hz, 1H), 1.38 (d, J=12.8 Hz, 1H). LC/MS [M+H]=m/z 377.




embedded image


Preparation of (R)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one: The title compound was prepared according to the procedure for (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one, except tert-butyl (R)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-1-oxo-2,8-diazaspiro [4.5]decane-8-carboxylate was substituted for tert-butyl (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate. 1H NMR (400 MHz, MeOD) δ 7.08-6.92 (m, 4H), 3.68 (m, 1H), 3.23-3.09 (m, 4H), 3.01 (m, 2H), 2.81-2.38 (m, 9H), 1.93 (m, 1H), 1.86-1.62 (m, 3H), 1.60 (dd, J=7.6, 12.5 Hz, 1H), 1.48 (d, J=13.5 Hz, 1H), 1.37 (d, J=13.5 Hz, 1H). LC/MS [M+H]=m/z 361.




embedded image


Preparation of (S)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one: The title compound was prepared according to the procedure for (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one, except tert-butyl (S)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2, 8-diazaspiro[4.5]decan-1-one was substituted for tert-butyl (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate 1H NMR (400 MHz, MeOD) δ 7.20 (t, J=8.2 Hz, 1H), 6.94 (s, 1H), 6.88 (d, J=8.5 Hz, 1H), 6.80 (d, J=7.7 Hz, 1H), 3.68 (m, 1H), 3.28-3.13 (m, 4H), 3.02 (m, 2H), 2.80-2.36 (m, 9H), 1.93 (m, 1H), 1.85-1.64 (m, 3H), 1.59 (dd, J=7.6, 12.7 Hz, 1H), 1.48 (d, J=13.2 Hz, 1H), 1.37 (d, J=12.8 Hz, 1H). LC/MS [M+H]=m/z 377.




embedded image


Preparation of (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one: The title compound was prepared according to the procedure for (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one, except tert-butyl (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate was substituted for tert-butyl (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate. 1H NMR (400 MHz, MeOD) δ 7.07-6.91 (m, 4H), 3.68 (m, 1H), 3.22-3.09 (m, 4H), 3.02 (m, 2H), 2.81-2.37 (m, 9H), 1.93 (m, 1H), 1.86-1.63 (m, 3H), 1.59 (dd, J=7.6, 12.5 Hz, 1H), 1.48 (d, J=13.5 Hz, 1H), 1.38 (d, J=13.5 Hz, 1H). LC/MS [M+H]=m/z 361.2.




embedded image


Preparation of (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-8-(methylsulfonyl)-2,8-diazaspirop.51decan-1-one: A solution of (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspirop.51decan-1-one (28 mg, 0.074 mmol, 1 equiv.), dichloromethane (0.85 mL) and triethylamine (15.7 mg, 0.155 mmol, 2.1 eq.) was cooled to 0° C. before methanesulfonyl chloride (12.7 mg. 0.111 mmol, 1.5 equiv.) was added to the solution. The reaction solution was allowed to warm to 23° C. and stir for 15 minutes. The reaction was diluted with methanol (˜2 mL), concentrated in vacuo and further purified by flash column chromatography (methanol/dichloromethane, 0%˜10%). 1H NMR (400 MHz, CDCl3) δ 7.17 (t, J=8.2 Hz, 1H), 6.88 (t, J=2.1 Hz, 1H), 6.83 (dd, J=1.7, 7.8 Hz, 1H), 6.81-6.72 (m, 2H), 3.81-3.61 (m, 2H), 3.50 (m, 1H), 3.32-3.11 (m, 6H), 2.82 (s, 3H), 2.73 (m, 2H), 2.66-2.42 (m, 4H), 2.20 (dd, J=6.5, 12.7 Hz, 1H), 2.04 (m, 1H), 1.96 (m, 1H), 1.79-1.50 (m, 5H); MS (LC/MS, M+H+): 456.2.




embedded image


Preparation of (R)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-8-(methylsulfonyl)-2,8-diazaspirop.51decan-1-one: The title compound was prepared according to the procedure for (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-8-(methylsulfonyl)-2,8-diazaspiro[4.5]decan-1-one, except (R)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one was substituted for (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one. 1H NMR (400 MHz, CDCl3) δ 7.07-6.93 (m, 2H), 6.92-6.84 (m, 2H), 6.80 (b, 1H), 3.80-3.62 (m, 2H), 3.49 (m, 1H), 3.27 (m, 1H), 3.22-3.08 (m, 5H), 2.82 (s, 3H), 2.75 (m, 2H), 2.66-2.43 (m, 4H), 2.20 (dd, J=6.4, 12.7 Hz, 1H), 2.04 (m, 1H), 1.96 (m, 1H), 1.79-1.48 (m, 5H); MS (LC/MS, M+H+): 439.2.




embedded image


Preparation of (S)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-8-(methylsulfonyl)-2,8-diazaspiro[4.5]decan-1-one: The title compound was prepared according to the procedure for (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-8-(methylsulfonyl)-2,8-diazaspiro[4.5]decan-1-one, except (S)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one was substituted for (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one. 1H NMR (400 MHz, CDCl3) δ 7.09 (t, J=8.1 Hz, 1H), 6.79 (t, J=2.1 Hz, 1H), 6.74 (dd, J=1.7, 7.7 Hz, 1H), 6.72-6.65 (m, 2H), 3.72-3.53 (m, 2H), 3.41 (m, 1H), 3.23-3.04 (m, 6H), 2.73 (s, 3H), 2.64 (m, 2H), 2.57-2.33 (m, 4H), 2.12 (dd, J=6.4, 12.8 Hz, 1H), 1.95 (m, 1H), 1.88 (m, 1H), 1.70-1.42 (m, 5H); MS (LC/MS, M+H+): 456.2.




embedded image


Preparation of (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)e thyl)-8-(methylsulfonyl)-2,8-diazaspiro[4.5]decan-1-one: The title compound was prepared according to the procedure for (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-8-(methylsulfonyl)-2,8-diazaspiro[4.5]decan-1-one, except (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one was substituted for (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one. 1H NMR (400 MHz, CDCl3) δ 6.94-6.84 (m, 2H), 6.83-6.76 (m, 2H), 6.74 (b, 1H), 3.71-3.54 (m, 2H), 3.41 (m, 1H), 3.17 (m, 1H), 3.13-2.99 (m, 5H), 2.73 (s, 3H), 2.65 (m, 2H), 2.57-2.34 (m, 4H), 2.11 (dd, J=6.4, 12.7 Hz, 1H), 1.95 (m, 1H), 1.87 (m, 1H), 1.70-1.39 (m, 5H); MS (LC/MS, M+H+): 439.2




embedded image


Preparation of (R)-8-acetyl-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one: A solution of (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one (21 mg, 0.056 mmol, 1 equiv.), dichloromethane (0.725 mL) and triethylamine (12 mg, 0.118 mmol, 2.1 eq.) was cooled to 0° C. before acetyl chloride (12.7 mg. 0.057 mmol, 1.01 equiv.) was added to the solution. The reaction solution was allowed to warm to 23° C. and stir for 15 minutes. The reaction was diluted with methanol (˜2 mL), concentrated in vacuo and further purified by flash column chromatography (methanol/methylene chloride, 0%˜10%). 1H NMR (400 MHz, CDCl3) δ 7.09 (t, J=8.1 Hz, 1H), 6.80 (t, J=2.2 Hz, 1H), 6.77-6.65 (m, 3H), 4.26 (dt, J=4.8, 13.4 Hz, 0.5H), 4.12 (dt, J=5.0, 13.8 Hz, 0.5H), 3.82 (dt, J=4.5, 13.5 Hz, 0.5H), 3.69 (dt, J=4.9, 13.8 Hz, 0.5H), 3.60 (m, 1H), 3.27-3.03 (m, 5.5H), 2.97 (m, 0.5H), 2.63 (m, 2H), 2.57-2.31 (m, 4H), 2.23 (m, 1H), 2.02 (s, 3H), 1.98-1.80 (m, 1H), 1.80-1.56 (m, 3H), 1.55-1.29 (m, 3H); MS (LC/MS, M+H+): 419.2




embedded image


Preparation of (R)-8-acetyl-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one: The title compound was prepared according to the procedure for (R)-8-acetyl-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one, except (R)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4 .5]decan-1-one was substituted for (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one. 1H NMR (400 MHz, CDCl3) δ 6.93-6.84 (m, 2H), 6.83-6.70 (m, 3H), 4.26 (dt, J=5.2, 13.5 Hz, 0.5H), 4.12 (dt, J=5.0, 13.5 Hz, 0.5H), 3.82 (dt, J=5.0, 13.7 Hz, 0.5H), 3.69 (dt, J=5.0, 13.7 Hz, 0.5H), 3.59 (m, 1H), 3.27-2.91 (m, 6H), 2.65 (m, 2H), 2.58-2.33 (m, 4H), 2.23 (m, 1H), 2.02 (s, 3H), 1.99-1.82 (m, 1H), 1.80-1.55 (m, 3H), 1.54-1.30 (m, 3H); MS (LC/MS, M+H+): 403.2




embedded image


Preparation of (S)-8-acetyl-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one: The title compound was prepared according to the procedure for (R)-8-acetyl-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one, except (S)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one was substituted for (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one. 1H NMR (400 MHz, CDCl3) δ 7.09 (t, J=8.1 Hz, 1H), 6.80 (t, J=2.2 Hz, 1H), 6.77-6.66 (m, 3H), 4.26 (dt, J=4.8, 13.4 Hz, 0.5H), 4.12 (dt, J=5.0, 13.8 Hz, 0.5H), 3.82 (dt, J=4.5, 13.5 Hz, 0.5H), 3.69 (dt, J=4.9, 13.8 Hz, 0.5H), 3.60 (m, 1H), 3.25-3.08 (m, 5.5H), 2.98 (m, 0.5H), 2.63 (m, 2H), 2.56-2.34 (m, 4H), 2.23 (m, 1H), 2.02 (s, 3H), 1.98-1.83 (m, 1H), 1.81-1.56 (m, 3H), 1.54-1.30 (m, 3H); MS (LC/MS, M+H+): 419.2




embedded image


Preparation of (S)-8-acetyl-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one: The title compound was prepared according to the procedure for (R)-8-acetyl-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one, except (S)-3-(2-(4-(4-fluorophenyl)piperazin-1-yl)ethyl)-2,8-diazaspiro[4.5]decan-1-one was substituted for (R)-3-(2-(4-(3-chlorophenyl)piperazin-1-yl)e thyl)-2, 8-diazaspiro[4.5]decan-1-one. 1H NMR (400 MHz, CDCl3) δ 6.93-6.84 (m, 2H), 6.83-6.73 (m, 3H), 4.26 (dt, J=5.2, 13.5 Hz, 0.5H), 4.12 (dt, J=5.0, 13.5 Hz, 0.5H), 3.82 (dt, J=5.0, 13.7 Hz, 0.5H), 3.69 (dt, J=5.0, 13.7 Hz, 0.5H), 3.59 (m, 1H), 3.26-2.91 (m, 6H), 2.65 (m, 2H), 2.57-2.32 (m, 4H), 2.23 (m, 1H), 2.02 (s, 3H), 1.98-1.82 (m, 1H), 1.81-1.55 (m, 3H), 1.54-1.30 (m, 3H); MS (LC/MS, M+H+): 403.2




embedded image


Preparation of (R)-3,3-diethyl-5-(2-(4-(pyridin-2-yl)piperazin-1-yl)ethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one, except 1-(2-pyridyl)piperazine was substituted for 1-phenylpiperazine. 1H NMR (400 MHz, CDCl3) δ 8.18 (dd, J=2.1, 4.8 Hz, 1H), 7.47 (m, 1H), 6.73 (b, 1H), 6.66-6.57 (m, 2H), 3.64-3.47 (m, 5H), 2.63 (m, 2H), 2.58-2.36 (m, 4H), 2.05 (dd, J=7.4, 13.0 Hz, 1H), 1.76-1.43 (m, 7H), 0.90 (dt, J=7.4, 14.5 Hz, 6H). LC/MS [M+H]=m/z 331.2




embedded image


Preparation of (R)-3,3-diethyl-5-(2-(4-(2-me thoxyphenyl)piperazin-1-yl)ethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one, except 1-(2-methoxyphenyl)piperazine was substituted for 1-phenylpiperazine. 1H NMR (400 MHz, CDCl3) δ 7.04-6.88 (m, 3H), 6.85 (dd, J=1.1, 8.0 Hz, 1H), 6.72 (b, 1H), 3.86 (s, 3H), 3.58 (m, 1H), 3.28-2.90 (b, 4H), 2.84-2.65 (b, 2H), 2.64-2.41 (m, 4H), 2.05 (dd, J=7.3, 13.1 Hz, 1H), 1.76-1.43 (m, 7H), 0.91 (dt, J=7.5, 16.1 Hz, 6H). LC/MS [M+H]=m/z 360.2




embedded image


Preparation of (R)-4-(4-(2-(4,4-diethyl-5-oxopyrrolidin-2-yl)ethyl)piperazin-1-yl)benzonitrile: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one, except 1-(4-cyanophenyl)piperazine was substituted for 1-phenylpiperazine. 1H NMR (400 MHz, CDCl3) δ 7.48 (d, J=9.0 Hz, 2H), 6.85 (d, J=9.0 Hz, 2H), 6.73 (b, 1H), 3.58 (m, 1H), 3.34 (t, J=5.1 Hz, 4H), 2.67 (m, 2H), 2.60-2.38 (m, 4H), 2.06 (dd, J=7.6, 13.2 Hz, 1H), 1.75-1.42 (m, 7H), 0.90 (dt, J=7.4, 14.0 Hz, 6H). LC/MS [M+H]=m/z 355.2




embedded image


Preparation of (R)-3,3-diethyl-5-(2-(4-(4-(trifluoromethyl)phenyl)piperazin-1-yl)ethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one, except 1-(4-(trifluoromethyl)phenyl)piperazine was substituted for 1-phenylpiperazine. 1H NMR (400 MHz, CDCl3) δ 7.36 (d, J=8.6 Hz, 2H), 6.80 (d, J=8.6 Hz, 2H), 6.58 (b, 1H), 3.47 (m, 1H), 3.18 (t, J=5.0 Hz, 4H), 2.57 (m, 2H), 2.49-2.28 (m, 4H), 1.95 (dd, J=7.4, 13.1 Hz, 1H), 1.64-1.32 (m, 7H), 0.79 (dt, J=7.3, 13.8 Hz, 6H). LC/MS [M+H]=m/z 398.2




embedded image


Preparation of (5R)-3,3-diethyl-5-(2-(5-phenylhexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)ethyl)pyrrolidin-2-one: The title compound was prepared according to the procedure for (R)-3,3-diethyl-5-(2-(4-phenylpiperazin-1-yl)ethyl)pyrrolidin-2-one, except 2-phenyloctahydropyrrolo[3,4-c]pyrrole was substituted for 1-phenylpiperazine. 1H NMR (400 MHz, CDCl3) δ 7.11 (m, 2H), 6.61 (t, J=7.4 Hz, 1H), 6.56 (d, J=8.6 Hz, 2H), 6.44 (b, 1H), 3.42 (m, 1H), 3.20-3.05 (m, 4H), 2.91 (m, 1H), 2.87-2.70 (m, 3H), 2.51 (m, 1H), 2.34-2.15 (m, 2H), 2.07 (dd, J=4.7, 8.5 Hz, 1H), 1.91 (dd, J=7.4, 13.1 Hz, 1H), 1.58-1.28 (m, 7H), 0.77 (m, 6H). LC/MS [M+H]=m/z 356.2




embedded image


Preparation of tert-butyl (S)-3-(2-cyanoethyl)-1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate: To a solution of tert-butyl (R)-1-oxo-3-(2-(tosyloxy)ethyl)-2,8-diazaspiro[4.5]decane-8-carboxylate (0.2 g, 0.44 mmol, 1.0 equiv.) in acetonitrile (1.9 mL) was added potassium cyanide (0.72 g, 1.1 mmol, 2.5 equiv.). The resulting reaction mixture was then allowed to reflux for 16 hours. After cooling to 23° C., the reaction mixture was filtered thru a plug of Celite and concentrated in vacuo to give a crude product which was further purified by column chromatography (MeOH/dichloromethane, 0%˜10%). iH NMR (400 MHz, CDCl3) δ 8.08 (b, 1H), 4.11-3.79 (b, 2H), 3.72 (p, J=6.6 Hz, 1H), 3.00 (t, J=11.3 Hz, 1H), 2.91 (t, J=11.3 Hz, 1H), 2.49 (td, J=1.2, 7.4 Hz, 2H), 2.32 (dd, J=7.0, 13.0 Hz, 1H), 1.97-1.78 (m, 3H), 1.72 (m, 1H), 1.52 (dd, J=7.8, 12.9 Hz, 1H), 1.48-1.29 (m, 11H).




embedded image


Preparation of (S)-3-(8-(methylsulfonyl)-1-oxo-2,8-diazaspiro[4.5]decan-3-yl)propanenitrile: To a solution of tert-butyl (S)-3-(2-cyanoethyl)-1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate (0.1 g, 0.35 mmol, 1.0 equiv.) in dichloromethane (2.75 mL) was added trifluoroacetic acid (0.5 mL). The resulting solution was allowed to stir at 23° C. for 45 minutes before being concentrated in vacuo. The residue was dissolved in MeOH (5 mL) followed by the addition of Amberlite IRN-78 base resin (0.5 g). This mixture was stirred vigorously for 15 minutes, filtered and the filtrate was concentrated in vacuo to give a crude intermediate that was then dissolved in dichloromethane (3.75 mL). The resulting solution was then cooled to 0° C. before the sequential addition of triethylamine (0.72 g, 0.70 mmol, 2.0 eq.) and methanesulfonyl chloride (0.6 g. 0.53 mmol, 1.5 equiv.). The reaction solution was allowed to warm to 23° C. and stir for 15 minutes. The reaction was diluted with MeOH (2 mL), concentrated in vacuo and further purified by flash column chromatography (MeOH w/2M ammonia/dichloromethane, 0% -10%). 1H NMR (400 MHz, CDCl3) δ 6.56 (b, 1H), 3.81 (p, J=6.8 Hz, 1H), 3.72 (m, 1H), 3.53 (m, 1H), 3.32-3.15 (m, 2H), 2.83 (s, 3H), 2.49 (t, J=6.8 Hz, 2H), 2.29 (dd, J=6.9, 12.9 Hz, 1H), 2.09-1.82 (m, 4H), 1.75-1.59 (m, 3H).




embedded image


Preparation of methyl (S)-3-(8-(methylsulfonyl)-1-oxo-2,8-diazaspiro[4.5]decan-3-yl)propanoate: A 6M HCl in methanol solution was prepared via the addition of acetyl chloride (0.48 mL) to MeOH (1 mL). (S)-3-(8-(methylsulfonyl)-1-oxo-2,8-diazaspiro[4.5]decan-3-yl)propanenitrile (91 mg, 0.32 mmol, 1.0 equiv.) was dissolved in the prepared 6M methanolic HCl solution (0.64 mL) and stirred at 23° C. overnight. The reaction mixture was diluted with MeOH (1 mL) and concentrated in vacuo. The resulting residue was suspended in sat. aqueous NaHCO3 and extracted with dichloromethane (4×15 mL). The combined organic phase was dried over Na2SO4 and concentrated in vacuo to give a crude product that was used in the next step without further purification. 1H NMR (400 MHz, CDCl3) δ 7.13 (b, 1H), 3.75-3.57 (m, 5H), 3.50 (m, 1H), 3.23-3.02 (m, 2H), 2.79 (s, 3H), 2.40 (td, J=1.7, 7.2 Hz, 2H), 2.18 (dd, J=6.8, 13.0 Hz, 1H), 2.01 (m, 1H), 1.92 (m, 1H), 1.83 (q, J=6.9 Hz, 2H), 1.68-1.45 (m, 3H).




embedded image


Preparation of (S)-3-(3-hydroxypropyl)-8-(methylsulfonyl)-2,8-diazaspiro[4.5]decan-1-one: This reaction was performed in oven-dried glassware under a nitrogen atmosphere. To a stirred solution of methyl (S)-3-(8-(methylsulfonyl)-1-oxo-2,8-diazaspiro[4.5]decan-3-yl)propanoate (80 mg, 0.25 mmol, 1.0 equiv.) in dry tetrahydrofuran (1.2 mL) at 0° C. was added LiBH4 (2M in tetrahydrofuran, 0.25 mL, 0.5 mmol, 2.0 equiv.) and the resulting solution was stirred at 23° C. for 6 hours. The reaction was then quenched with 0.5 mL of acetic acid and then filtered while washing with MeOH. The filtrate was concentrated in vacuo to give a crude product which was further purified by column chromatography (MeOH/dichloromethane, 10%). 1H NMR (400 MHz, MeOD) δ 3.74-3.55 (m, 5H), 3.02 (td, J=3.0, 11.2 Hz, 1H), 2.92 (td, J=2.9, 11.5 Hz, 1H), 2.86 (s, 3H), 2.39 (dd, J=7.0, 13.1 Hz, 1H), 2.08-1.97 (m, 1H), 1.89-1.78 (m, 1H), 1.71-1.50 (m, 7H).




embedded image


Preparation of (S)-3-(8-(methylsulfonyl)-1-oxo-2,8-diazaspiro[4.5]decan-3-yl)propyl 4-methylbenzenesulfonate: To a cooled mixture of (S)-3-(3-hydroxypropyl)-8-(methylsulfonyl)-2,8-diazaspiro[4.5]decan-1-one (55 mg, 0.19 mmol, 1.0 equiv.) and triethylamine (40 mg, 0.38 mmol, 2.0 equiv.) in dichloromethane:dimethylformamide (2.0 mL:0.2 mL) at 0° C. was added 4-toluenesulfonyl chloride (55 mg, 0.28 mmol, 1.5 equiv.) followed by 4-dimethylaminopyridine (3 mg, 0.02 mmol, 0.1 equiv.). The resulting reaction mixture was stirred at 0° C. for 5 minutes before being warmed to 23° C. and allowed to stir for 24 hours. Then, the reaction mixture was diluted with dichloromethane (5 mL), washed with 1N HCl (1×5 mL). The aqueous layer was backwashed with dichloromethane (2×5 mL). The combined organic layers were dried over Na2SO4 and concentrated in vacuo to give a crude product which was further purified by HPLC (CH3CN/H2O, 0.1% Formic acid), 0%˜100%). 1H NMR (400 MHz, CDCl3) δ 7.78 (d, J=8.2 Hz, 2H), 7.37 (d, J=8.0 Hz, 2H), 6.84 (b, 1H), 4.04 (t, J=5.9 Hz, 2H), 3.70 (m, 1H), 3.64-3.44 (m, 2H), 3.21-3.00 (m, 2H), 2.80 (s, 3H), 2.46 (s, 3H), 2.17 (dd, J=6.8, 12.8 Hz, 1H), 2.01 (m, 1H), 1.91 (m, 1H), 1.81-1.66 (m, 2H), 1.66-1.44 (m, 5H).




embedded image


Preparation of (S)-3-(3-(4-(4-fluorophenyl)piperazin-1-yl)propyl)-8-(methylsulfonyl)-2,8-diazaspiro[4.5]decan-1-one: To a small vial was added (S)-3-(8-(methylsulfonyl)-1-oxo-2,8-diazaspiro[4.5]decan-3-yl)propyl 4-methylbenzenesulfonate (16 mg, 0.036 mmol, 1 equiv.) and 1-(4-fluorophenyl)piperazine (13.5 mg, 0.75 mmol, 2.1 equiv.) then both were dissolved in acetonitrile (0.4 mL). Then K2CO3 (13 mg, 0.089 mmol, 2.5 equiv.) was added and the reaction mixture was stirred at 80° C. overnight and then cooled to 23° C. The mixture was filtered, washed with acetonitrile and filtrate was concentrated in vacuo to give a crude product which was by further purified by column chromatography (MeOH/dichloromethane, 0%˜10%). 1H NMR (400 MHz, CDCl3) δ 7.02-6.92 (m, 3H), 6.92-6.84 (m, 2H), 3.72 (m, 1H), 3.59 (m, 1H), 3.50 (m, 1H), 3.31-3.09 (m, 6H), 2.81 (s, 3H), 2.74-2.56 (m, 4H), 2.46 (t, J=6.2 Hz, 2H), 2.18 (dd, J=6.6, 12.8 Hz, 1H), 2.09-1.90 (m, 2H), 1.74-1.43 (m, 7H). LC/MS [M+H]=m/z 453.2




embedded image


Preparation of (S)-3-(3-(4-(3-chlorophenyl)piperazin-1-yl)propyl)-8-(methylsulfonyl)-2,8-diazaspiro[4.5]decan-1-one: The title compound was prepared according to the procedure for (S)-3-(3-(4-(4-fluorophenyl)piperazin-1-yl)propyl)-8-(methylsulfonyl)-2,8-diazaspiro[4.5]decan-1-one, except 1-(3-chlorophenyl)piperazine was substituted for 1-(4-fluorophenyl)piperazine. 1H NMR (400 MHz, CDCl3) δ 7.17 (t, J=8.2 Hz, 1H), 6.92-6.85 (m, 2H), 6.84-6.76 (m, 2H), 3.72 (m, 1H), 3.60 (m, 1H), 3.50 (m, 1H), 3.32-3.13 (m, 6H), 2.81 (s, 3H), 2.71-2.55 (m, 4H), 2.45 (t, J=6.3 Hz, 2H), 2.19 (dd, J=6.7, 12.8 Hz, 1H), 2.09-1.90 (m, 2H), 1.73-1.44 (m, 7H). LC/MS [M+H]=m/z 469.2


Example 2
Exemplary Formulations

The present invention also relates to compositions or formulations which comprise the 5-hydroxytryptamine receptor 7 activity modulators according to the present invention. In general, the compositions of the present invention comprise an effective amount of one or more compounds of the disclosure and salts thereof according to the present invention which are effective for providing modulation of 5-hydroxytryptamine receptor 7 activity; and one or more excipients.


For the purposes of the present invention the term “excipient” and “carrier” are used interchangeably throughout the description of the present invention and said terms are defined herein as, “ingredients which are used in the practice of formulating a safe and effective pharmaceutical composition.”


The formulator will understand that excipients are used primarily to serve in delivering a safe, stable, and functional pharmaceutical, serving not only as part of the overall vehicle for delivery but also as a means for achieving effective absorption by the recipient of the active ingredient. An excipient may fill a role as simple and direct as being an inert filler, or an excipient as used herein may be part of a pH stabilizing system or coating to insure delivery of the ingredients safely to the stomach. The formulator can also take advantage of the fact the compounds of the present invention have improved cellular potency, pharmacokinetic properties, as well as improved oral bioavailability.


The present teachings also provide pharmaceutical compositions that include at least one compound described herein and one or more pharmaceutically acceptable carriers, excipients, or diluents. Examples of such carriers are well known to those skilled in the art and can be prepared in accordance with acceptable pharmaceutical procedures, such as, for example, those described in Remington's Pharmaceutical Sciences, 17th edition, ed. Alfonoso R. Gennaro, Mack Publishing Company, Easton, Pa. (1985), the entire disclosure of which is incorporated by reference herein for all purposes. As used herein, “pharmaceutically acceptable” refers to a substance that is acceptable for use in pharmaceutical applications from a toxicological perspective and does not adversely interact with the active ingredient. Accordingly, pharmaceutically acceptable carriers are those that are compatible with the other ingredients in the formulation and are biologically acceptable. Supplementary active ingredients can also be incorporated into the pharmaceutical compositions.


Compounds of the present teachings can be administered orally or parenterally, neat or in combination with conventional pharmaceutical carriers. Applicable solid carriers can include one or more substances which can also act as flavoring agents, lubricants, solubilizers, suspending agents, fillers, glidants, compression aids, binders or tablet-disintegrating agents, or encapsulating materials. The compounds can be formulated in conventional manner, for example, in a manner similar to that used for known 5-hydroxytryptamine receptor 7 activity modulators. Oral formulations containing a compound disclosed herein can comprise any conventionally used oral form, including tablets, capsules, buccal forms, troches, lozenges and oral liquids, suspensions or solutions. In powders, the carrier can be a finely divided solid, which is an admixture with a finely divided compound. In tablets, a compound disclosed herein can be mixed with a carrier having the necessary compression properties in suitable proportions and compacted in the shape and size desired. The powders and tablets can contain up to 99% of the compound.


Capsules can contain mixtures of one or more compound(s) disclosed herein with inert filler(s) and/or diluent(s) such as pharmaceutically acceptable starches (e.g., corn, potato or tapioca starch), sugars, artificial sweetening agents, powdered celluloses (e.g., crystalline and microcrystalline celluloses), flours, gelatins, gums, and the like.


Useful tablet formulations can be made by conventional compression, wet granulation or dry granulation methods and utilize pharmaceutically acceptable diluents, binding agents, lubricants, disintegrants, surface modifying agents (including surfactants), suspending or stabilizing agents, including, but not limited to, magnesium stearate, stearic acid, sodium lauryl sulfate, talc, sugars, lactose, dextrin, starch, gelatin, cellulose, methyl cellulose, microcrystalline cellulose, sodium carboxymethyl cellulose, carboxymethylcellulose calcium, polyvinylpyrrolidine, alginic acid, acacia gum, xanthan gum, sodium citrate, complex silicates, calcium carbonate, glycine, sucrose, sorbitol, dicalcium phosphate, calcium sulfate, lactose, kaolin, mannitol, sodium chloride, low melting waxes, and ion exchange resins. Surface modifying agents include nonionic and anionic surface modifying agents. Representative examples of surface modifying agents include, but are not limited to, poloxamer 188, benzalkonium chloride, calcium stearate, cetostearl alcohol, cetomacrogol emulsifying wax, sorbitan esters, colloidal silicon dioxide, phosphates, sodium dodecylsulfate, magnesium aluminum silicate, and triethanolamine. Oral formulations herein can utilize standard delay or time-release formulations to alter the absorption of the compound(s). The oral formulation can also consist of administering a compound disclosed herein in water or fruit juice, containing appropriate solubilizers or emulsifiers as needed.


Liquid carriers can be used in preparing solutions, suspensions, emulsions, syrups, elixirs, and for inhaled delivery. A compound of the present teachings can be dissolved or suspended in a pharmaceutically acceptable liquid carrier such as water, an organic solvent, or a mixture of both, or a pharmaceutically acceptable oils or fats. The liquid carrier can contain other suitable pharmaceutical additives such as solubilizers, emulsifiers, buffers, preservatives, sweeteners, flavoring agents, suspending agents, thickening agents, colors, viscosity regulators, stabilizers, and osmo-regulators. Examples of liquid carriers for oral and parenteral administration include, but are not limited to, water (particularly containing additives as described herein, e.g., cellulose derivatives such as a sodium carboxymethyl cellulose solution), alcohols (including monohydric alcohols and polyhydric alcohols, e.g., glycols) and their derivatives, and oils (e.g., fractionated coconut oil and arachis oil). For parenteral administration, the carrier can be an oily ester such as ethyl oleate and isopropyl myristate. Sterile liquid carriers are used in sterile liquid form compositions for parenteral administration. The liquid carrier for pressurized compositions can be halogenated hydrocarbon or other pharmaceutically acceptable propellants.


Liquid pharmaceutical compositions, which are sterile solutions or suspensions, can be utilized by, for example, intramuscular, intraperitoneal or subcutaneous injection. Sterile solutions can also be administered intravenously. Compositions for oral administration can be in either liquid or solid form.


Preferably the pharmaceutical composition is in unit dosage form, for example, as tablets, capsules, powders, solutions, suspensions, emulsions, granules, or suppositories. In such form, the pharmaceutical composition can be sub-divided in unit dose(s) containing appropriate quantities of the compound. The unit dosage forms can be packaged compositions, for example, packeted powders, vials, ampoules, prefilled syringes or sachets containing liquids. Alternatively, the unit dosage form can be a capsule or tablet itself, or it can be the appropriate number of any such compositions in package form. Such unit dosage form can contain from about 1 mg/kg of compound to about 500 mg/kg of compound, and can be given in a single dose or in two or more doses. Such doses can be administered in any manner useful in directing the compound(s) to the recipient' s bloodstream, including orally, via implants, parenterally (including intravenous, intraperitoneal and subcutaneous injections), rectally, vaginally, and transdermally.


When administered for the treatment or inhibition of a particular disease state or disorder, it is understood that an effective dosage can vary depending upon the particular compound utilized, the mode of administration, and severity of the condition being treated, as well as the various physical factors related to the individual being treated. In therapeutic applications, a compound of the present teachings can be provided to a patient already suffering from a disease in an amount sufficient to cure or at least partially ameliorate the symptoms of the disease and its complications. The dosage to be used in the treatment of a specific individual typically must be subjectively determined by the attending physician. The variables involved include the specific condition and its state as well as the size, age and response pattern of the patient.


In some cases it may be desirable to administer a compound directly to the airways of the patient, using devices such as, but not limited to, metered dose inhalers, breath-operated inhalers, multidose dry-powder inhalers, pumps, squeeze-actuated nebulized spray dispensers, aerosol dispensers, and aerosol nebulizers. For administration by intranasal or intrabronchial inhalation, the compounds of the present teachings can be formulated into a liquid composition, a solid composition, or an aerosol composition. The liquid composition can include, by way of illustration, one or more compounds of the present teachings dissolved, partially dissolved, or suspended in one or more pharmaceutically acceptable solvents and can be administered by, for example, a pump or a squeeze-actuated nebulized spray dispenser. The solvents can be, for example, isotonic saline or bacteriostatic water. The solid composition can be, by way of illustration, a powder preparation including one or more compounds of the present teachings intermixed with lactose or other inert powders that are acceptable for intrabronchial use, and can be administered by, for example, an aerosol dispenser or a device that breaks or punctures a capsule encasing the solid composition and delivers the solid composition for inhalation. The aerosol composition can include, by way of illustration, one or more compounds of the present teachings, propellants, surfactants, and co-solvents, and can be administered by, for example, a metered device. The propellants can be a chlorofluorocarbon (CFC), a hydrofluoroalkane (HFA), or other propellants that are physiologically and environmentally acceptable.]


Compounds described herein can be administered parenterally or intraperitoneally. Solutions or suspensions of these compounds or a pharmaceutically acceptable salts, hydrates, or esters thereof can be prepared in water suitably mixed with a surfactant such as hydroxyl-propylcellulose. Dispersions can also be prepared in glycerol, liquid polyethylene glycols, and mixtures thereof in oils. Under ordinary conditions of storage and use, these preparations typically contain a preservative to inhibit the growth of microorganisms.


The pharmaceutical forms suitable for injection can include sterile aqueous solutions or dispersions and sterile powders for the extemporaneous preparation of sterile injectable solutions or dispersions. In some embodiments, the form can sterile and its viscosity permits it to flow through a syringe. The form preferably is stable under the conditions of manufacture and storage and can be preserved against the contaminating action of microorganisms such as bacteria and fungi. The carrier can be a solvent or dispersion medium containing, for example, water, ethanol, polyol (e.g., glycerol, propylene glycol and liquid polyethylene glycol), suitable mixtures thereof, and vegetable oils.


Compounds described herein can be administered transdermally, i.e., administered across the surface of the body and the inner linings of bodily passages including epithelial and mucosal tissues. Such administration can be carried out using the compounds of the present teachings including pharmaceutically acceptable salts, hydrates, or esters thereof, in lotions, creams, foams, patches, suspensions, solutions, and suppositories (rectal and vaginal).


Transdermal administration can be accomplished through the use of a transdermal patch containing a compound, such as a compound disclosed herein, and a carrier that can be inert to the compound, can be non-toxic to the skin, and can allow delivery of the compound for systemic absorption into the blood stream via the skin. The carrier can take any number of forms such as creams and ointments, pastes, gels, and occlusive devices. The creams and ointments can be viscous liquid or semisolid emulsions of either the oil-in-water or water-in-oil type. Pastes comprised of absorptive powders dispersed in petroleum or hydrophilic petroleum containing the compound can also be suitable. A variety of occlusive devices can be used to release the compound into the blood stream, such as a semi-permeable membrane covering a reservoir containing the compound with or without a carrier, or a matrix containing the compound. Other occlusive devices are known in the literature.


Compounds described herein can be administered rectally or vaginally in the form of a conventional suppository. Suppository formulations can be made from traditional materials, including cocoa butter, with or without the addition of waxes to alter the suppository' s melting point, and glycerin. Water-soluble suppository bases, such as polyethylene glycols of various molecular weights, can also be used.


Lipid formulations or nanocapsules can be used to introduce compounds of the present teachings into host cells either in vitro or in vivo. Lipid formulations and nanocapsules can be prepared by methods known in the art.


To increase the effectiveness of compounds of the present teachings, it can be desirable to combine a compound with other agents effective in the treatment of the target disease. For example, other active compounds (i.e., other active ingredients or agents) effective in treating the target disease can be administered with compounds of the present teachings. The other agents can be administered at the same time or at different times than the compounds disclosed herein.


Compounds of the present teachings can be useful for the treatment or inhibition of a pathological condition or disorder in a mammal, for example, a human subject. The present teachings accordingly provide methods of treating or inhibiting a pathological condition or disorder by providing to a mammal a compound of the present teachings including its pharmaceutically acceptable salt) or a pharmaceutical composition that includes one or more compounds of the present teachings in combination or association with pharmaceutically acceptable carriers. Compounds of the present teachings can be administered alone or in combination with other therapeutically effective compounds or therapies for the treatment or inhibition of the pathological condition or disorder.


Non-limiting examples of compositions according to the present invention include from about 0.001 mg to about 1000 mg of one or more compounds of the disclosure according to the present invention and one or more excipients; from about 0.01 mg to about 100 mg of one or more compounds of the disclosure according to the present invention and one or more excipients; and from about 0.1 mg to about 10 mg of one or more compounds of the disclosure according to the present invention; and one or more excipients.


Example 3
General Biochemical Procedures

The following procedures can be utilized in evaluating and selecting compounds as 5-hydroxytryptamine receptor 7 activity modulators.


Radiolabel Binding Studies for Serotonin 5HT7 receptors, method 1:


A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer or DMSO according to its solubility. A similar stock of the reference compound chlorpromazine is also prepared as a positive control. Eleven dilutions (5× assay concentration) of the compound of the disclosure and chlorpromazine are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 pM to 10 μM.


A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in 50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4 (Assay Buffer). Aliquots (50 μl) of radioligand are dispensed into the wells of a 96-well plate containing 100 μl of Assay Buffer. Duplicate 50-μl aliquots of the compound of the disclosure test and chlorpromazine positive control reference compound serial dilutions are added.


Membrane fractions of cells expressing recombinant 5HT7 receptors (50 μL) are dispensed into each well. The membranes are prepared from stably transfected cell lines expressing 5HT7 receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000×g, decanting the supernatant and storing at −80° C.; the membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before using in the assay.


The 250-μl reactions are incubated at room temperature for 1.5 hours, then harvested by rapid filtration onto 0.3% polyethyleneimine-treated, 96-well filter mats using a 96-well Filtermate harvester. Four rapid 500-μl washes are performed with chilled Assay Buffer to reduce non-specific binding The filter mats are dried, then scintillant is added to the filters and the radioactivity retained on the filters is counted in a Microbeta scintillation counter.


Raw data (dpm) representing total radioligand binding (i.e., specific+non-specific binding) are plotted as a function of the logarithm of the molar concentration of the competitor (i.e., test or reference compound). Non-linear regression of the normalized (i.e., percent radioligand binding compared to that observed in the absence of test or reference compound) raw data is performed in Prism 4.0 (GraphPad Software) using the built-in three parameter logistic model describing ligand competition binding to radioligand-labeled sites:






y=bottom+[(top-bottom)/(1+10×-log IC50)]


where bottom equals the residual radioligand binding measured in the presence of 10 μM reference compound (i.e., non-specific binding) and top equals the total radioligand binding observed in the absence of competitor. The log IC50 (i.e., the log of the ligand concentration that reduces radioligand binding by 50%) is thus estimated from the data and used to obtain the Ki by applying the Cheng-Prusoff approximation:






Ki=IC50/(1+[ligand]/KD)


where [ligand] equals the assay radioligand concentration and KD equals the affinity constant of the radioligand for the target receptor.


Compounds of the disclosure are also screened at a single concentration of 10 μM using the same method described for the Radiolabel Binding Studies for Serotonin 5HT7 receptors to determine the percent inhibition of [3H]LSD binding.


Radiolabel Binding Studies for Serotonin 5-HT7 Receptors, Method 2:


A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer or DMSO according to its solubility. A similar stock of the reference compound chlorpromazine is also prepared as a positive control. Eleven dilutions (5× assay concentration) of the compound of the disclosure and chlorpromazine are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 μM to 10 μM.


A stock concentration of 5 nM [3H]-5-Hydroxytryptamine ([3H]-5HT) is prepared in 50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4 (Assay Buffer). Aliquots (50 μl) of radioligand are dispensed into the wells of a 96-well plate containing 100 μl of Assay Buffer. Duplicate 50-μl aliquots of the compound of the disclosure test and chlorpromazine positive control reference compound serial dilutions are added.


Membrane fractions of cells expressing recombinant 5HT7 receptors (50 μL) are dispensed into each well. The membranes are prepared from stably transfected cell lines expressing 5HT7 receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000× g, decanting the supernatant and storing at −80° C.; the membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before using in the assay.


The 250 μl reactions are incubated at room temperature for 1.5 hours, then harvested by rapid filtration onto 0.3% polyethyleneimine-treated, 96-well filter mats using a 96-well Filtermate harvester. Four rapid 500-μl washes are performed with chilled Assay Buffer to reduce non-specific binding The filter mats are dried, then scintillant is added to the filters and the radioactivity retained on the filters is counted in a Microbeta scintillation counter.


Raw data (dpm) representing total radioligand binding (i.e., specific+non-specific binding) are plotted as a function of the logarithm of the molar concentration of the competitor (i.e., test or reference compound). Non-linear regression of the normalized (i.e., percent radioligand binding compared to that observed in the absence of test or reference compound) raw data is performed in Prism 4.0 (GraphPad Software) using the built-in three parameter logistic model describing ligand competition binding to radioligand-labeled sites:






y=bottom+[(top-bottom)/(1+10×-log IC50)]


where bottom equals the residual radioligand binding measured in the presence of 10 μM reference compound (i.e., non-specific binding) and top equals the total radioligand binding observed in the absence of competitor. The log IC50 (i.e., the log of the ligand concentration that reduces radioligand binding by 50%) is thus estimated from the data and used to obtain the Ki by applying the Cheng-Prusoff approximation:






Ki=IC50/(1+[ligand]/KD)


where [ligand] equals the assay radioligand concentration and KD equals the affinity constant of the radioligand for the target receptor.


Compounds of the disclosure are also screened at a single concentration of 10 μM using the same method described for the Radiolabel Binding Studies for Serotonin 5HT7 receptors to determine the percent inhibition of [3H]-5HT binding.


Functional Serotonin 5HT7 Assay, Method 1:


Cell lines stably expressing human 5HT7 receptors are seeded in 96-well, poly-L-lysine-coated plates 48 hours prior to the assay (40,000 cells per well) in Dulbecco's Modified Eagle Medium (DMEM) containing 5% dialyzed serum. Twenty hours prior to the assay, the medium is changed to serum-free DMEM. On the day of the assay, the DMEM is washed and replaced with 30 μl of assay buffer (1× Krebs-Ringer bicarbonate glucose buffer, 0.75 mM IBMX, pH 7.4). A 10-min pre-incubation is performed in a 37-degree centigrade, humidified incubator. Then, the cells are stimulated by addition of 30 μl of 2× dilutions of compounds of the disclosure or chlorpromazine (final concentrations ranging from 0.1 nM to 10 μM, each concentration assayed in triplicate). A positive control (100 μM forskolin) is also included. Accumulation of cAMP is allowed to continue for 15 min, after which the buffer is removed and the cells are lysed with Cell Lysis Buffer (CatchPoint cAMP Assay Kit, Molecular Devices). Next, the lysates are transferred to 96-well, glass-bottom plates coated with goat anti-rabbit IgG and adsorbed with rabbit anti-cAMP (Molecular Devices). Following a 5 minute incubation, horseradish peroxidase-cAMP conjugate is added (Molecular Devices) and a 2-hour incubation is performed at room temperature. Then, after three washes with Wash Buffer (Molecular Devices), Stoplight Red substrate (Molecular Devices), reconstituted in Substrate Buffer (Molecular Devices) containing freshly-added 1 mM H2O2, is added and, after a 15-min incubation at room temperature, fluorescence is measured (excitation 510-545 nm, emission 565-625 nm). For each assay, a cAMP calibration curve is generated and controls without lysate and without antibody are included.


For agonist tests, raw data (maximum fluorescence, fluorescence units) for each concentration of the compounds of the disclosure or chlorpromazine are normalized to the basal (vehicle-stimulated) fluorescence (reported as fold increase over basal) and plotted as a function of the logarithm of the molar concentration of the drug (i.e., test or reference compound). Non-linear regression of the normalized data is performed in Prism 4.0 (GraphPad Software) using the built-in three parameter logistic model (i.e., sigmoidal concentration-response) describing agonist-stimulated activation of one receptor population:






y=bottom+[(top-bottom)/(1+10×-log EC50)]


where bottom equals the best-fit basal fluorescence and top equals the best-fit maximal fluorescence stimulated by the compound of the disclosure or chlorpromazine. The log EC50 (i.e., the log of the drug concentration that increases fluorescence by 50% of the maximum fluorescence observed for the compound of the disclosure or chlorpromazine is thus estimated from the data, and the EC50 (agonist potency) is obtained. To obtain an estimate of the relative efficacy of the test compound (Rel. Emax), its best-fit top is compared to and expressed as a ratio of that for the chlorpromazine (Rel. Emax of the reference agonist is 1.00).


To ascertain whether compounds of the disclosure are antagonists, a double-addition paradigm is employed. First, 30 μl of a compound of the disclosure (20 μM) is added (10 μM final concentration) and a 15 minute incubation is performed. Then, 30 μl of chlorpromazine (3×; EC90) is added (final concentration of agonist is EC30) and cAMP accumulation is allowed to proceed for 15 minutes. The samples are then processed for cAMP measurements as detailed above. Measurements of chlorpromazine-induced cAMP accumulation are compared to the signals elicited by the chlorpromazine following addition of vehicle instead of test compound and expressed as a ratio. ‘Hits’ (compounds that antagonize chlorpromazine -stimulated increases in baseline-normalized fluorescence by at least 50%) are then characterized by a modified Schild analysis.


For modified Schild analysis, a family of chlorpromazine concentration-response isotherms is generated in the absence and presence of graded concentrations of test compound (added 15 min prior to reference agonist). Theoretically, compounds that are competitive antagonists cause a dextral shift of agonist concentration-response isotherms without reducing the maximum response to agonist (i.e., surmountable antagonism). However, on occasion, factors such as non-competitive antagonism, hemiequilibria, and/or receptor reserve cause apparent insurmountable antagonism. To account for such deviations, we apply the modified Lew-Angus method to ascertain antagonist potency (Christopoulos et al., 1999). Briefly, equieffective concentrations of agonist (concentrations of agonist that elicit a response equal to the EC25% of the agonist control curve) are plotted as a function of the compound of the disclosure concentration present in the wells in which they were measured. Non-linear regression of the baseline-normalized data is performed in Prism 4.0 using the following equation:






pEC25%=−log([B]+10−pK)−log c


where EC25% equals the concentration of agonist that elicits a response equal to 25% of the maximum agonist control curve response and [B] equals the antagonist concentration; K, c, and s are fit parameters. The parameter s is equal to the Schild slope factor. If s is not significantly different from unity, pK equals pKB; otherwise, pA2 is calculated (pA2=pK/s). The parameter c equals the ratio EC25%/[B].


Functional Efficacy Assay for 5-HT7 Receptors Method 2:


Functional efficacy of the compounds of the disclosure on 5-HT7 serotonin receptors were measured in a cell based cAMP enzyme fragment complementation assay using the HitHunter cAMP assay (DiscoveRx). Cells stably expressing human 5HT7 receptors were plated in 96-well plates at 4000 cells/well, 16-20 hours prior to assay in growth media (Ultraculture medium, 2 mM GlutaMax and G418 1 mg/mL. Serial dilutions of the agonist, 5-Carboxamidotryptamine (5-CT), were prepared in a final concentration range of 10 μM to 10 nM. Compounds of the disclosure were prepared in 3-fold serial dilutions to obtain a final concentration range of 10 μM to 0.1 nM. Compounds of the disclosure are tested for agonist activity in the absence of 5-CT and antagonist activity in the presence of 5-CT. For the cAMP assay, the protocol was followed according to the instructions provided by the supplier. Briefly, cells were incubated with a compound of the disclosure for 30 minutes at 37° C. prior to addition of EC7o concentration of 5-CT. After an additional 30 minutes, cAMP antibody/cell lysis solution was added (20 μL/well) and incubated for 60 minutes at room temperature. cAMP XS+EA reagent is added (20 μL/well) and incubated for 2 hours at room temperature. Luminescence was read on the Envision Multilabel plate reader.


The disclosures of each and every patent, patent application, and publication cited herein are hereby incorporated herein by reference in their entirety.


While this invention has been disclosed with reference to specific embodiments, it is apparent that other embodiments and variations of this invention may be devised by others skilled in the art without departing from the true spirit and scope of the invention. The appended claims are intended to be construed to include all such embodiments and equivalent variations.


Example 4
Biochemical Experiments
Methods:


1Radiolabeled Binding (IC50 and K1)


A solution of the compound of the disclosure to be tested was prepared as a 1-mg/ml stock in Assay Buffer or DMSO according to its solubility. A similar stock of the reference compound chlorpromazine was also prepared as a positive control. Eleven dilutions (5 x assay concentration) of the compound of the disclosure and chlorpromazine were prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 pM to 10 μM.


A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) was prepared in 50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4 (Assay Buffer). Aliquots (50 μl) of radioligand were dispensed into the wells of a 96-well plate containing 100 μl of Assay Buffer. Duplicate 50 μl aliquots of the compound of the disclosure test and chlorpromazine positive control reference compound serial dilutions were added.


Membrane fractions of cells expressing recombinant 5HT7 receptors (50 μL) were dispensed into each well. The membranes were prepared from stably transfected cell lines expressing 5HT7 receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000×g, decanting the supernatant and storing at −80° C.; the membrane preparations were resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before using in the assay.


The 250 μl reactions were incubated at room temperature for 1.5 hours, then harvested by rapid filtration onto 0.3% polyethyleneimine-treated, 96-well filter mats using a 96-well Filtermate harvester. Four rapid 500-μl washes were performed with chilled Assay Buffer to reduce non-specific binding The filter mats were dried, then scintillant is added to the filters and the radioactivity retained on the filters was counted in a Microbeta scintillation counter.


Raw data (dpm) representing total radioligand binding (i.e., specific+non-specific binding) was plotted as a function of the logarithm of the molar concentration of the competitor (i.e., test or reference compound). Non-linear regression of the normalized (i.e., percent radioligand binding compared to that observed in the absence of test or reference compound) raw data was performed in Prism 4.0 (GraphPad Software) using the built-in three parameter logistic model describing ligand competition binding to radioligand-labeled sites:






y=bottom+[(top-bottom)/(1+10×-logIC50)]


where bottom equals the residual radioligand binding measured in the presence of 10 μM reference compound (i.e., non-specific binding) and top equals the total radioligand binding observed in the absence of competitor. The log IC50 (i.e., the log of the ligand concentration that reduces radioligand binding by 50%) was thus estimated from the data and used to obtain the Ki by applying the Cheng-Prusoff approximation:






Ki =IC
50/(1+[ligand]/KD)


where [ligand] equals the assay radioligand concentration and KD equals the affinity constant of the radioligand for the target receptor.


Functional Data (Kb)

Functional efficacy of the compounds of the disclosure on 5-HT7 serotonin receptors were measured in a cell based cAMP enzyme fragment complementation assay using the HitHunter cAMP assay (DiscoveRx). Cells stably expressing human 5HT7 receptors were plated in 96-well plates at 4000 cells/well, 16-20 hours prior to assay in growth media (Ultraculture medium, 2 mM GlutaMax and G418 1 mg/mL. Serial dilutions of the agonist, 5-hydroxytryptamine (5-HT), were prepared in a final concentration range of 10 μM to 10 nM. Compounds of the disclosure were prepared in 3-fold serial dilutions to obtain a final concentration range of 10 μM to 0.1 nM. Compounds of the disclosure are tested for agonist activity in the absence of 5-HT and antagonist activity in the presence of 5-HT. For the cAMP assay, the protocol was followed according to the instructions provided by the supplier. Briefly, cells were incubated with a compound of the disclosure for 30 minutes at 37° C. prior to addition of EC70 concentration of 5-HT. After an additional 30 minutes, cAMP antibody/cell lysis solution was added (20 μL/well) and incubated for 60 minutes at room temperature. cAMP XS+EA reagent is added (20 μL/well) and incubated for 2 hours at room temperature. Luminescence was read on the Envision Multilabel plate reader.


Results



embedded image
















TABLE 34









IC50
Ki
Kb



n
R1
R2
R3
(nM)1
(nM)1
(nM)2
TPSA





















2
Ethyl
Ethyl
4-F-Phenyl
8.5
8.98
35.6


2
Ethyl
Ethyl
4-Cl-Phenyl
13
54.6
35.6


2
Ethyl
Ethyl
2-iPr-phenyl
23
163
35.6


2
Ethyl
Ethyl
2-morpholino-
24
32.3
48.1





phenyl


2
Ethyl
Ethyl
4-Me-Phenyl
28
24.1
35.6


2
Ethyl
Ethyl
4-OH-Phenyl
34
50
55.8


2
Ethyl
Ethyl
Phenyl
68
17.8
35.6


2
Ethyl
Ethyl
4-Me-2-
74
59.3
48.1





morpholino-phenyl











embedded image
















TABLE 35









IC50
Ki
Kb



n
R1
R2
R3
(nM)1
(nM)1
(nM)2
TPSA






















1
Ethyl
Ethyl
2-iPr-phenyl

121

35.6


1
Ethyl
Ethyl
4-Me-2-

132
43.8
48.1





morpholino-phenyl


1
Ethyl
Ethyl
4-F-Phenyl

243

35.6


1
Ethyl
Ethyl
4-Me-Phenyl

249

35.6


1
Ethyl
Ethyl
2-pyridyl

669

48.5


1
Ethyl
Ethyl
Phenyl

819

35.6


1
Ethyl
Ethyl
3-Cl-Phenyl

1087

35.6


2
Ethyl
Ethyl
4-Me-Phenyl

11
8.43
35.6


2
Ethyl
Ethyl
4-F-Phenyl
12.34

0.81
35.6


2
Ethyl
Ethyl
3,4-di-Cl-Phenyl
82.8

6.19
35.6


2
Ethyl
Ethyl
4-F-3-Cl-Phenyl
8.7

1.92
35.6


2
Ethyl
Ethyl
3-Cl-Phenyl
9.9

1.38
35.6


2
Ethyl
Ethyl
Phenyl


6.59
35.6


2
Ethyl
Ethyl
2-Cl-Phenyl


109
35.6


2
Ethyl
Ethyl
3-F-Phenyl


9.89
35.6


2
Ethyl
Ethyl
2-Me-Phenyl


127
35.6


2
Ethyl
Ethyl
3-Me-Phenyl


1.65
35.6


2
Ethyl
Ethyl
2-pyridyl


4.91
48.5


2
Ethyl
Ethyl
2-OMe-Phenyl


230
44.8


2
Ethyl
Ethyl
4-CN-Phenyl


544
59.4


2
Ethyl
Ethyl
4-CF3-Phenyl


137
35.6











embedded image
















TABLE 36









IC50
Ki
Kb



n
R1
R2
R3
(nM)1
(nM)1
(nM)2
TPSA





















2
Ethyl
Ethyl
4-Me-Phenyl
79
58.1
35.6













2
—CH2CH═CHCH2—
4-F-Phenyl


46.2
35.6


2
—CH2CH═CHCH2—
3-Cl-Phenyl


36.3
35.6


2
—CH2CH2CH2CH2—
4-F-Phenyl


52.6
35.6


2
—CH2CH2CH2CH2—
3-Cl-Phenyl


48.4
35.6











embedded image















TABLE 37








IC50
Ki
Kb



n
R3
R7
(nM)1
(nM)1
(nM)2
TPSA




















2
3-Cl-Phenyl
Acetyl
63
5.04
55.9


2
4-F-Phenyl
Acetyl
76
14.4
55.9


2
4-F-Phenyl
MeSO2
89
30.7
81.3


2
3-Cl-Phenyl
MeSO2
107
13.5
81.3


3
3-Cl-Phenyl
MeSO2

321
81.3


3
4-F-Phenyl
MeSO2

526
81.3











embedded image















TABLE 38








IC50
Ki
Kb



n
R3
R7
(nM)1
(nM)1
(nM)2
TPSA




















2
3-Cl-Phenyl
MeSO2
117

81.3


2
4-F-Phenyl
MeSO2
167
74.2
81.3


2
3-Cl-Phenyl
Acetyl
214

55.9


2
4-F-Phenyl
Acetyl
325

55.9











embedded image
















TABLE 39









IC50
Ki
Kb



n
R1
R2
R3
(nM)1
(nM)1
(nM)2
TPSA




















2
Ethyl
Ethyl
Phenyl
144
35.6









From the foregoing description, one skilled in the art can easily ascertain the essential characteristics of this invention, and without departing from the spirit and scope thereof, can make various changes and modifications of the invention to adapt it to various usages and conditions.


All references, patents or applications, U.S. or foreign, cited in the application are hereby incorporated by reference as if written herein in their entireties. Where any inconsistencies arise, material literally disclosed herein controls.

Claims
  • 1. A compound having formula (I):
  • 2. The compound of claim 1, wherein: A is
  • 3. The compound of claim 1 or 2, wherein n is 1, 2 ,or 3.
  • 4. The compound of any one of claims 1-3, having the formula (II):
  • 5. The compound of claim 4, having the formula (XXXXII):
  • 6. The compound of claim 4, having the formula (XXXXIII):
  • 7. The compound of claim 1, having the formula (IIa):
  • 8. The compound of claim 1, having the formula (IIe):
  • 9. The compound of claim 1, having the formula (III):
  • 10. The compound of claim 1, having the formula (IIm):
  • 11. The compound of claim 1, having the formula (IIq):
  • 12. The compound of claim 1, having the formula (Hu):
  • 13. The compound of claim 1, having the formula (III):
  • 14. The compound of claim 1, having the formula (IIIa):
  • 15. The compound of claim 1, having the formula (IIIe):
  • 16. The compound of claim 1, having the formula (IIIi):
  • 17. The compound of claim 1, having the formula (IIIm):
  • 18. The compound of claim 1, having the formula (IIIg):
  • 19. The compound of claim 1, having the formula (IIIu):
  • 20. The compound of claim 1, having the formula (IV):
  • 21. The compound of claim 20, having the following formula,
  • 22. The compound of claim 20, having the following formula,
  • 23. The compound of claim 1, having the formula (IVa):
  • 24. The compound of claim 1, having the formula (IVe):
  • 25. The compound of claim 1, having the formula (IVi):
  • 26. The compound of claim 1, having the formula (IVm):
  • 27. The compound of claim 1, having the formula (IVq):
  • 28. The compound of claim 1, having the formula (IVu):
  • 29. The compound of claim 1, having the formula (V):
  • 30. The compound of claim 1, having the formula (Va):
  • 31. The compound of claim 1, having the formula (Vb):
  • 32. The compound of claim 1, having the formula (Ve):
  • 33. The compound of claim 1, having the formula (Vi):
  • 34. The compound of claim 1, having the formula (Vm):
  • 35. The compound of claim 1, having the formula (Vq):
  • 36. The compound of claim 1, having the formula (Vu):
  • 37. The compound of claim 1, having the formula (VI):
  • 38. The compound of claim 37, having the formula (XXXXVI):
  • 39. The compound of claim 37, having the formula:
  • 40. The compound of claim 1, having the formula (VIa):
  • 41. The compound of claim 1, having the formula (VIe):
  • 42. The compound of claim 1, having the formula (VIi):
  • 43. The compound of claim 1, having the formula (VIm):
  • 44. The compound of claim 1, having the formula (VIq):
  • 45. The compound of claim 1, having the formula (VIu):
  • 46. The compound of claim 1, having the formula (VII):
  • 47. The compound of claim 1, having the formula (VIIa):
  • 48. The compound of claim 1, having the formula (VIIe):
  • 49. The compound of claim 1, having the formula (VIII):
  • 50. The compound of claim 1, having the formula (VIIm):
  • 51. The compound of claim 1, having the formula (VIIq):
  • 52. The compound of claim 1, having the formula (VIIu):
  • 53. The compound of any one of claims 1-52, wherein R1 and R2 are each independently C1-6 linear alkyl or C3-7 branched alkyl.
  • 54. The compound of claim 53, wherein each of R1 and R2 is ethyl.
  • 55. The compound of any one of claims 1-52, wherein R1 and R2 are taken together with the atoms to which they are bound to form a 5- to 8-membered ring, optionally containing one carbon-carbon double bonds and/or a ring atom selected from the group consisting of O, S, SO, SO2, and NR7.
  • 56. The compound of claim 55, wherein R1 and R2 are taken together with the atoms to which they are bound to form a C3-C8 cycloalkyl or a C5-C8 cycloalkenyl.
  • 57. The compound of claim 56 wherein R1 and R2 are taken together with the atoms to which they are bound to form a cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cycloheptenyl, cyclooctyl, or cyclooctenyl.
  • 58. The compound of any one of claims 55-57, having the formula (XLIIIa):
  • 59. The compound of claim 58, wherein represents a single bond.
  • 60. The compound of claim 58, wherein represents a double bond.
  • 61. The compound of claim 55, wherein R1 and R2 are taken together with the atoms to which they are bound to form a 5- to 8-membered ring containing a ring atom that is NR7.
  • 62. The compound of claim 61, wherein R1 and R2 are taken together to form a pyrrolidinyl or piperidinyl group where the nitrogen atom is NR7.
  • 63. The compound of claim 61 or 62, wherein R7 is COR8, and R8 is C1-6 linear alkyl.
  • 64. The compound of claim 63, wherein R7 is acetyl.
  • 65. The compound of claim 61 or 62, wherein R7 is SO2R10c, and R10c is C1-6 linear alkyl.
  • 66. The compound of claim 65, wherein R10c is methyl.
  • 67. The compound of any one of claims 61-66, having the formula (XLIIIb):
  • 68. The compound of claim 67, having the formula (XLIV):
  • 69. The compound of claim 67, having the formula (XLV):
  • 70. The compound of any one of claims 53-69, wherein R3 is unsubstituted phenyl.
  • 71. The compound of any one of claims 53-69, wherein R3 is substituted phenyl, wherein the substitutents are selected from the group consisting of hydroxyl, halo, cyano, C1-6 alkoxy, C1-6 linear alkyl, C3-7 branched alkyl, C1-6 haloalkyl, and heterocylyl.
  • 72. The compound of claim 71, wherein R3 is selected from the group consisting of 4-hydroxyphenyl, 3-fluorophenyl, 4-fluorophenyl, 3-chlorophenyl, 4-chlorophenyl, 3,4-dichlorophenyl, 4-fluoro-3-chlorophenyl, 4-cyanophenyl, 2-methoxyphenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, 2-isopropylphenyl, 4-trifluoromethylphenyl, 2-morpholinophenyl, and 4-methyl-2-morpholinophenyl.
  • 73. The compound of any one of claims 53-69, wherein R3 is 2-pyridyl.
  • 74. The compound of any one of claims 53-56 and 61-62, wherein A is
  • 75. The compound of claim 74, having the formula (XLVI),
  • 76. The compound of claim 74, having the formula (XLVIa),
  • 77. The compound of claim 74, wherein R5 is unsubstituted phenyl.
  • 78. The compound of claim 74, wherein R5 is selected from the group consisting of 4-hydroxyphenyl, 3-fluorophenyl, 4-fluorophenyl, 3-chlorophenyl, 4-chlorophenyl, 3,4-dichlorophenyl, 4-fluoro-3-chlorophenyl, 4-cyanophenyl, 2-methoxyphenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, 2-isopropylphenyl, 4-trifluoromethylphenyl, 2-morpholinophenyl, and 4-methyl-2-morpholinophenyl.
  • 79. The compound of any one of claims 1-78, or a pharmaceutically acceptable salt thereof.
  • 80. The compound of claim 79, wherein the compound is a compound described in any one of Tables 1-39, or a pharmaceutically acceptable salt thereof.
  • 81. The compound of claim 80, wherein the compound is a compound described in any one of Tables 34-39, or a pharmaceutically acceptable salt thereof.
  • 82. A composition comprising an effective amount of at least one compound according to any one of claims 1-81, or a pharmaceutically acceptable salt thereof.
  • 83. A composition according to claim 82, further comprising at least one excipient.
  • 84. A method of treating a disease associated with dysregulation of 5-hydroxytryptamine receptor 7 activity, said method comprising administering to a subject an effective amount of at least one compound according to any one of claims 1-81, or a pharmaceutically acceptable salt thereof.
  • 85. The method of claim 84, wherein the at least one compound, or a pharmaceutically acceptable salt thereof, is administered in a composition further comprising at least one excipient.
  • 86. The method of claim 84 or 85, wherein the disease associated with dysregulation of 5-hydroxytryptamine receptor 7 activity is selected from the group consisting of circadian rhythm disorder, depression, schizophrenia, neurogenic inflammation, hypertension, peripheral, vascular diseases, migraine, neuropathic pain, peripheral pain, allodynia, thermoregulation disorder, learning disorder, memory disorder, hippocampal signaling disorder, sleep disorder, attention deficit/hyperactivity disorder, anxiety, avoidant personality disorder, premature ejaculation, eating disorder, premenstrual syndrome, premenstrual dysphonic disorder, seasonal affective disorder, bipolar disorder, inflammatory bowel disease (IBD), intestinal inflammation, epilepsy, seizure disorders, drug addiction, alcohol addiction, breast cancer, liver fibrosis, chronic liver injury, hepatocellular carcinoma, small intestine neuroendocrine tumors, and lung injury.
  • 87. The method of claim 84 or 85, wherein the disease associated with dysregulation of 5-hydroxytryptamine receptor 7 activity is inflammatory bowel disease (IBD) or intestinal inflammation.
CROSS REFERENCE TO RELATED APPLICATIONS

This application claims the benefit of U.S. Provisional Application No. 62/670,116, filed May 11, 2018, which is herein incorporated by reference in its entirety.

STATEMENT OF FEDERALLY FUNDED RESEARCH

The U.S. Government has a paid-up license in this invention and the right in limited circumstances to require the patent owner to license others on reasonable terms as provided for by the terms of grant number 143DK115254-01 awarded by the National Institute of Diabetes and Digestive and Kidney Disease and grant number HHSN-271-2008-00025-C awarded by the National Institute of Mental Health.

PCT Information
Filing Document Filing Date Country Kind
PCT/US2019/031824 5/10/2019 WO
Provisional Applications (1)
Number Date Country
62670116 May 2018 US