Novel quinazoline derivatives and methods of treatment related to the use thereof

Abstract

The present invention relates to novel compounds of Formula (1): which act as MCH receptor antagonists. These compositions are useful in pharmaceutical compositions whose use includes prophylaxis or treatment of improving memory function, sleeping and arousal, anxiety, depression, mood disorders, seizure, obesity, diabetes, appetite and eating disorders, cardiovascular disease, hypertension, dyslipidemia, myocardial infarction, binge eating disorders including bulimia, anorexia, mental disorders including manic depression, schizophrenia, delirium, dementia, stress, cognitive disorders, attention deficit disorder, substance abuse disorders and dyskinesias including Parkinson's disease, epilepsy, and addiction.

Description

FIELD OF THE INVENTION

The present invention relates to compounds which act as antagonists for MCH receptors and to the use of these compounds in pharmaceutical compositions.

BACKGROUND OF THE INVENTION

Melanin Concentrating Hormone (MCH), a cyclic peptide, has been identified as the endogenous ligand of the orphan G-protein coupled receptor SLC-1. See, for example, Shimomura et al., Biochem. Biophys. Res. Commun. 261, 622-26 (1999). Studies have indicated that MCH acts as a neurotransmitter/neuromodulator to alter a number of behavioral responses such as feeding habits. For example, injection of MCH into rats has been reported to increase their consumption of food. Reports indicate that genetically engineered mice which lack MCH show lower body weight and increased metabolism. See Saito et al., TEM, vol. 11, 299 (2000). As such, the literature suggests that discovery of MCH antagonists that interact with SCL-1 expressing cells will be useful in developing obesity treatments. See Shimomura et al., Biochem. Biophys. Res. Commun. 261, 622-26 (1999).

G protein-coupled receptors (GPCRs) share a common structural motif. All these receptors have seven sequences of between 22 to 2z4 hydrophobic amino acids that form seven alpha helices, each of which spans the membrane. The fourth and fifth transmembrane helices are joined on the extracellular side of the membrane by a strand of amino acids that forms a relatively large loop. Another larger loop, composed primarily of hydrophilic amino acids, joins transmembrane helices five and six on the intracellular side of the membrane. The carboxy terminus of the receptor lies intracellularly and the amino terminus lies in the extracellular space. It is thought that the loop joining helices five and six, as well as the carboxy terminus, interact with the G protein. Currently, Gq, Gs, Gi, and Go are G proteins that have been identified as possible proteins that interact with the receptor.

Under physiological conditions, GPCRs exist in the cell membrane in equilibrium between two different states or conformations: an “inactive” state and an “active” state. A receptor in an inactive state is unable to link to the intracellular transduction pathway to produce a biological response. Changing the receptor conformation to the active state allows linkage to the transduction pathwvay and produces a biological response.

A receptor may be stabilized in an active state by an endogenous ligand or an exogenous agonist ligand. Recent discoveries, including but not exclusively limited to, modifications to the amino acid sequence of the receptor, provide alternative mechanisms other than ligands to stabilize the active state conformation. These approaches effectively stabilize the receptor in an active state by simulating the effect of a ligand binding to the receptor. Stabilization by such ligand-independent approaches is termed “constitutive receptor activation.” In contrast, antagonists can competitively bind to the receptor at the same site as agonists, but do not activate the intracellular response initiated by the active form of the receptor, and therefore inhibit the intracellular responses by agonists.

Certain 2-aminoquinazoline derivatives have been reported to be NPY antagonists which are said to be effective in the treatment of disorders and diseases associated wvith the NPY receptor subtype Y5. See PCT Patent Application 97/20823. Quinazoline derivatives have also been found to be useful by enhancing antitumor activity. See PCT Patent Application 92/07844. And also the quinoline derivatives which have an antagonist activity for MCH receptor are known in these patents, WO0/070244, WO03/105850, WO03/45313, WO03/045920, and WO04/04726.

Recently, our current knowledge of human obesity has advanced dramatically. Previously, obesity was viewed as an oppugnant behavior of inappropriate eating in the setting of appealing foods. Studies of animal models of obesity, biochemical alterations in both humans and animals, and the complex interactions of psychosocial and cultural factors that create receptiveness to human obesity indicate that this disease in humans is multifaceted and deeply entrenched in biologic systems. Thus, it is almost certain that obesity has multiple causes and that there are different types of obesity. Not only does MCHR1 antagonist have potent and durable anti-obesity effects in rodents, it has surprising antidepressant and anxiolytic properties as well (Borowsky et al., Nature Medicine, 8, 825-830, 2002). MCHR1 antagonists have been reported to show antidepressant and anxiolytic activities in rodent models such as social interaction, forced swimming test and ultrasonic vocalization. These findings indicate that MCHR1 antagonists could be useful for treatment of obesity patients with multiple causes. Moreover, MCHR1 antagonists could be used to treat subjects not only with obesity, but also those with depression and anxiety. These advantages make it different from NPY receptor antagonists, with which anxiogenic-like activity can be expected, as NPY itself has anxiolytic-like effect.

Obesity is also regarded as a chronic disease and the possibly of long-term treatment is a concept that is receiving more attention. In this context, it is noteworthy that the depletion of MCH leads to hypophagia as whell as leanness (Shimada et al., Nature, 396, 670-674, 1998). By contrast, NPY (Erickson et al., Nature, 3 S, 415-418, 1996), as well as the Y1 (Pedrazzini et al., Nature Medicine, 4, 722-726, 1998) and Y5 receptors (Marsh et al., Nature Medicine, 4, 718-721, 1998), disrupted mice maintained a stable body weight or rather became obese. Considering the above reports, MCHR1 antagonists can be more attractive than Y1 or Y5 receptor antagonists in terms of long-term treatment of obese patients.

An increasing number of children and adolescents are overweight. Although not all overweight children will necessarily become overweight adults, the growing occurrence of obesity in childhood is likely to be reflected in increasing obesity in adult years. The high prevalence of obesity in our adult population and the likelihood that the nation of the future will be even more obese demands a re-examination of the health implications of this disease. See, Health Implications of Obesity. NIH Consens. Statement Online 1985 Feb. 11-13; 5(9):1-7.

“Clinical obesity” is a measurement of the excess body fat relative to lean body mass and is defined as a body weight more than 20% above the ideal body weight. Recent estimates suggest that 1 in 2 adults in the United States is clinically obese, an increase of more than 25% over the past decades. Flegal M. D. et al., 22 Int. J. Obes. Relat. Metab. Disor. 39 (1998). Both overweight conditions and clinical obesity are a major health concerns worldwide, in particular because clinical obesity is often accompanied by numerous complications, i.e., hypertension and Type II diabetes, which in turn can cause coronary artery disease, stroke, late-stage complications of diabetes and premature death. (See, e.g., Nishina P. M. et al., 43 Metab. 554 (1994)).

Although the etiologic mechanisms underlying obesity require further clarification, the net effect of such mechanisms leads to an imbalance betwveen energy intake and expenditure. Both genetic and environmental factors are likely to be involved in the pathogenesis of obesity. These include excess caloric intake, decreased physical activity, and metabolic and endocrine abnonnalities.

Treatment of overweight conditions and clinical obesity via pharmaceutical agents are not only of importance with respect to the conditions themselves, but also weith respect to the possibility of preventing other diseases that are associated with, e.g., clinical obesity, as well as enhancement of the positive feeling of “self” that often accompanies those who are overweight or clinically obese and who encounter a significant reduction in body weight. Given the foregoing discussion, it is apparent that compounds which help in the treatment of such disorders would be useful and would provide an advance in both research and clinical medicine. The present invention is directed to these, as well as other, important ends.

SUMMARY OF THE INVENTION

The present invention is drawvn to compounds, which bind to and modulate the activity of a GPCR referred to herein as MCH, and uses thereof. The term MCH, as used herein, includes the human sequences found in GeneBank accession number NM_—005297, naturally-occurring allelic variants, mammalian orthologs, biologically active fragments and recombinant mutants thereof.

One aspect of the present invention relates to certain substituted heterocyclic compounds represented by Formula (I):

• • wherein Q is:

R₁ is selected from the group consisting of:

• • (i) C_1-8 alkyl, and C_1-8 alkyl substituted by substituent(s) independently selected from the group consisting of:
    • oxo,
    • halogen,
    • C_1-5 alkoxy carbonyl,
    • C_1-5 alkoxy,
    • C_1-5 alkoxy substituted by carbocyclic aryl,
    • mono-C_1-5 allkylamino,
    • mono-C_1-5 alkylamino substituted by carbocyclic aryl,
    • di-C_1-5 alkylamino,
    • di-C_1-5 alkylarnino substituted by carbocyclic aryl,
    • C_1-5 alkylthio,
    • C_3-6 cycloalkyl,
    • C_3-6 cycloalkyl substituted by C_1-5 alkyl,
    • C_3-6 cycloalkenyl,
    • carbocyclyl,
    • carbocyclic aryl,
    • carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of:
      • hydroxy,
      • halogen,
      • nitro,
      • amino,
      • C_1-5 alkylcarbonylamino,
      • C_3-6 cycloalkylcarbonylamino,
      • carbocyclic aryl,
      • C_1-5 alkyl,
      • C_1-5 alkyl substituted by halogen,
      • C_1-5 alkylsulfonyl,
      • C_2-6alkenyl,
      • C_1-5 alkoxy, and
      • C_1-5 alkoxy substituted by halogen,
    • mono-carbocyclic arylamino,
    • mono-carbocyclic arylamino substituted by substituent(s) independently selected from the group consisting of:
      • halogen,
      • C_1-5 alkyl,
      • C_1-5 alkyl substituted by halogen,
      • C_1-5 alkoxy, and
      • C_1-5 alkoxy substituted by halogen,
    • di-carbocyclic arylamino,
    • di-carbocyclic arylamino substituted by substituent(s) independently selected from the group consisting of:
      • halogen,
      • C_1-5 alkyl,
      • C_1-5 alkyl substituted by halogen,
      • C_1-5 alkoxy, and
      • C_1-5 alkoxy substituted by halogen,
    • carbocyclic aryloxy,
    • carbocyclic aryloxy substituted by substituieit(s) independently selected from the group consisting of:
      • halogen,
      • C_1-5 alkyl,
      • C_1-5 alkyl substituted by halogen,
      • C_1-5 alkoxy,
      • C_1-5 sustited by halogen, and
      • carbocyclic aryl,
    • hydroxy,
    • heterocyclyl, and
    • heterocyclyl substituted by halogen,
  • (ii) C_2-5 alkenyl, and C_2-5 alkenyl substituted by substituent(s) independently selected from the group consisting of:
    • oxo, and
    • carbocyclic aryl,
  • (iii) C_2-5 alkynyl,
  • (iv) C_3-12 cycloalkyl, and C_3-12 cycloalkyl substituted by carbocyclic aryl,
  • (v) carbocyclyl, and carbocyclyl substituted by substituent(s) independently selected from the group consisting of:
    • hydroxy, and
    • carbocyclic aryl,
  • (vi) carbocyclic aryl, and carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of:
    • halogen,
    • cyano,
    • nitro,
    • amino,
    • C_1-10 alkyl,
    • C_1-10 alkyl substituted by substituent(s) independently selected from the group consisting of:
      • halogen,
      • oxo, and
      • carbocyclic aryl,
    • carboxy,
    • C_1-5 alkoxy carbonyl,
      • C_1-7 alkoxy,
      • C_1-7 alkoxy substituted by substituent(s) independently selected from the group consisting of:
      • halogen, and
      • carbocyclic aryl,
    • C_3-6 cycloalkoxy,
    • carbocyclic aryloxy,
    • carbocyclic aryloxy substituted by substituent(s) independently selected from the group consisting of:
      • halogen,
      • nitro,
      • C_1-5 alkyl,
      • C_1-5 alkyl substituted by halogen,
      • C_1-5 alkoxy, and
      • C_1-5 alkoxy substituted by halogen,
    • heterocyclyloxy,
    • heterocyclyloxy substituted by substituent(s) independently selected from the group consisting of:
      • halogen,
      • nitro,
      • C_1-5 alkyl,
      • C_1-5 alkyl substituted by halogen,
      • C_1-5 alkoxy, and
      • C_1-5 alkoxy substituted by halogen,
    • mono-C_1-5 alkylamino,
    • di-C_1-5 alkylamino,
    • C_1-5 alkylcarbonylamino,
    • C_3-6 cycloalkylcarbonylamino,
    • C_1-5 alkoxy carbonylamino,
    • carbocyclic aryl azo,
    • carbocyclic aryl azo substituted by substituent(s) independently selected from the group consisting of:
      • mono-C_1-5 alkylamino, and
      • di-C_1-5 alkylamino,
    • C_1-5 alkylthio,
    • C_1-5 alkylthio substituted by halogen,
    • carbocyclic arylthio,
    • carbocyclic arylthio substituted by nitro,
    • amino sulfonyl,
    • heterocyclyl sulfonyl,
    • C_3-6 cycloalkyl,
    • C_3-6 cycloalkyl substituted by C_1-5 alkyl,
    • carbocyclic aryl,
    • carbocyclic aryl substituted by C_1-5 alkoxy,
    • hydroxy,
    • heterocyclyl, and
    • heterocyclyl substituted by C_1-5 alkyl,
  • (vii) heterocyclyl, and heterocyclyl substituted by substitiient(s) independently selected from the group consisting of:
    • halogen,
    • C_1-5 alkyl,
    • C_1-5 alkyl substituted by halogen,
    • C_1-5 alkoxy,
    • C_1-5 alkoxy substituted by halogen,
    • C_1-5 alkoxy carbonyl,
    • C_1-5 alkoxy caibon)l substituted by carbocyclic aryl,
    • carbocyclic aryloxy,
    • carbocyclic aryloxy substituted by substituent(s) independently selected from the group consisting of:
      • halogen,
      • nitro,
      • cyano,
      • hydroxy,
      • C_1-5 alkyl,
      • C_1-5 alkyl substituted by halogen,
      • mono-C_1-5 alkylamino,
      • di-C_1-5 alkylamino,
      • C_1-5 alkylcarbonylamino,
      • C_3-6 cycloalkylcarbobylamino,
      • C_1-5 alkoxy,
      • C_1-5 alkoxy substituted by halogen,
      • C_3-6 cycloalkyl,
      • C_2-5 alkenyl,
      • C_2-5 alkynyl,
      • carboxy,
      • C_1-5 alkoxycarbonyl,
      • mono-C_1-5 alkylaminocarbonyl,
      • di-C_1-5 alkylaminocarbonyl,
      • mono-C_3-6 cycloalkylaminocarbonyl,
      • di-C_3-6 cycloalkylaminocarbonyl,
      • mono-C_1-5 alkylaminocarbonylanmino,
      • di-C_1-5 alkylaminocarbonylamino,
      • mono-C_3-6 cycloalkylaminocarbonylamino,
      • di-C_3-6 cycloalkylaminocarbonylamino,
      • C_1-5 alkylthio,
      • C_1-5 alkylthio substituted by halogen,
      • C_1-5 alkylsulfinyl,
      • C_1-5 alkylsulfinyl substituted by halogen,
      • C_1-5 alkylsulfonyl, and
      • C_1-5 alkylsulfonyl substituted by halogen,
    • heterocyclyloxy,
    • heterocyclyloxy substituted by substituent(s) independently selected from the group consisting of:
      • halogen,
      • nitro,
      • C_1-5 alkyl,
      • C_1-5 alkyl substituted by halogen,
      • C_1-5 alkoxy, and
      • C_1-5 alkoxy substituted by halogen,
    • carbocyclic aryl, and
    • heterocyclyl;
  • R₂ is C_1-5 alkyl or —N(R_2a)(R_2b); wherein R_2a and R_2b are independently hydrogen or C_1-5 alkyl,
  • R₃ is C_1-5 alkyl;
  • R₄ is —NHNH₂, —NHNBoc, —N(R_1a)(R_1b), morpholino, 4-acetyl-piperazyl, or 4-phenyl-piperazyl; wherein R_1a is hydrogen or C_1-5 alkyl; R_1b is C_1-5 alkyl, C_1-5 alkyl substituted by substittent(s) independently selected fronm the group consisting of:
    • hydroxy,
    • C_1-5 alkoxy,
    • amino,
    • —NHBoc,
    • C_3-6 cycloalkyl,
    • *arbocyclic aryl,
    • carbocyclic aryl substituted by substitient(s) independently selected from the group consisting of:
      • halogen,
      • C_1-5 alkyl,
      • C_1-5 alkoxy, and
      • —SO₂NH₂, and
    • heterocyclyl,
  • C₃-₆ cycloalkyl, carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of:
    • halogen,
    • C_1-5 alkyl,
    • C_1-5 alkoxy, and
    • a group of Formula (III):
  • wherein Boc is carbamic acid tert-butyl ester and G is C_1-5 alkyl or C_1-5 alkeyl substituted by substituent(s) independently selected from the group consisting of:
    • carbocyclic aryl,
    • halogenated carbocyclic aryl, and
    • carbocyclic aryl substituted by C_1-5 alkoxy;
  • L is selected from the group consisting of Formulae (IV) to (XIX):
  • wherein R₅ and R₆ are independently hydrogen or C_1-5 alkyl; and A and B are independently a single bond, —CH₂—, or —(CH₂)₂—;
  • X₁, X₂, X₃ and X₄ are independently selected from the group consisting of hydrogen, halogen, C_1-4 alkyl, C_1-4 alkyl substituted by halogen, C_1-4 alkylthio, C_1-4 alkylsulfinyl, C₁₄ alkylsulfonyl, C_1-4 alkoxy, C_1-4 alkoxy substituted by halogen, nitro, amino, mono-C_1-4 alkylamino, di-C_1-4 alkylamino, piperidyl, morpholinyl, mono-C-_1-4 alkylaminosulfonyyl di-C_1-4 alkylaminosulfonyl and hydroxy; provided that at least one substituent selected from the group consisting of X₁, X₂, X₃ and X₄ is not hydrogen; and
  • Y is selected from the group consisting of:
  • (i) —C(O)NR₇—, —C(S)NR₇—, or —C(O)O— when L is selected from the group consisting of Formulae (IV) to (XIX); wherein R₇ is hydrogen or C_1-5 alkyl;
  • (ii) —S(O)₂—, —C(O)—, a single bond or —CH₂— when L is selected from the group consisting of Formulae (IV) to (.I), and Q is Formula (IIa) or (IIb);
  • (iii) —S(O)₂—, —C(O)—, a single bond or —CH₂— when L is selected from the group consisting of Formulae (VII) to (XI), and Q is Formula (IIc); and
  • (iv) —OC(O)— when L is selected from the group consisting of Formulae (XII) to (XIX);
    • wherein carbocyclic aryl is phenyl, naphthyl, or biphenyl;
    • carbocyclyl is indanyl, bicyclo[2.2.1]heptyl, bicyclo[2.2.1]heptenyl, adamantly, 9H-fluorenyl, menthyl, 1,2,3,4-tetrahydro-naphthalen-1-yl, or 1H-indolyl;
    • heterocyclyl is 2,3-dihydro-benzo[1,4]dioxinyl, 3,4-dihydro-2H-benzo[b][1,4]dioxepinyl, 4,5,6,7-tetrahydro-benzo[b]thienyl, 4H-benzo[1,3]dioxinyl, benzo[1,3]dioxolyl, benzo[2,1,3]thiadiazolyl, benzothiazolyl, furyl, isoxazolyl, morpholinyl, oxazolyl, piperidyl, pyrazolyl, pyridyl, tetrahydrofuryl, thienyl, dibenzofuranyl, 1H-benzoimidazolyl, or thiazolyl; and
    • halogen is fluoro, chloro, bromo, or iodo;
  • or a pharmaceutically acceptable salt, hydrate or solvate thereof.

One aspect of the present invention pertains to pharmaceutical compositions comprising at least one compound, as described herein, in combination with a pharmaceutically acceptable carrier.

One aspect of the present invention pertains to methods for the prophylaxis or treatment of improving memory function, sleeping and arousal, anxiety, depression, mood disorders, seizure, obesity, diabetes, appetite and eatino disorders. cardiovascular disease. hypertension, dyslipidemia myocardial infarction, binge eating disorders including bulimia, anorexia, mental disorders inc;luding manic depression, schizophrenia, delirium, dementia, stress, cognitive disorders, attention deficit disorder, substance abuse disorders and dyskiiiesias including Parkinison's disease, epilepsy, and addiction comprising administering to an individual suffering from said condition a therapeutically effective amount of a compound, as described herein, or a pharmaceutical composition thereof.

One aspect of the present invention pertains to methods for the prophylaxis or treatment of an eating disorder, obesity or an obesity related disorder comprising administering to an individual suffering from the condition a therapeutically effective amount of a compound, as described herein, or a pharmaceutical composition thereof.

One aspect of the present invention pertains to methods for the prophylaxis or treatment of anxiety, depression, schizophrenia, addiction, or epilepsy comprising administering to an individual suffering from the condition a therapeutically effective amount of a compound, as described herein, or a pharmaceutical composition.

One aspect of the present invention pertains to compounds of the present invention, as described herein, or a phan-naceutical composition thereof, for use in a method of treatment of the human or animal body by therapy.

One aspect of the present invention pertains to compounds of the present invention, as described herein, or a pharmaceutical composition thereof, for use in a method of prophylaxis or treatment of an eating disorder, obesity or an obesity related disorder of the human or animal body by therapy.

One aspect of the present invention pertains to compounds of the present invention. as described herein, or a pharmaceutical composition thereof, for use in a method of prophylaxis or treatment of anxiety, depression, schizophrenia, addiction, or epilepsy of the human or animal body by therapy.

One aspect of the present invention pertains to compounds of the present invention, as described herein, for the manufacture of a medicament for use in the prophylaxis or treatment of an eating disorder, obesity or obesity related disorders.

One aspect of the present invention pertains to compounds of the present invention, as described herein, for the manufacture of a medicament for use in the prophylaxis or treatment of anxiety, depression, schizophrenia, addiction or epilepsy.

One aspect of the present hinvention pertains to methods of decreasing food intake of an individual comprising administering to the individual a therapeutically effective amount of a compound, as described herein, or a pharmaceutical composition thereof.

One aspect of the present invention pertains to methods of inducing satiety in an individual comprising administering to said individual a therapeutically effective amount of a compound, as described herein, or a pharmaceutical composition thereof.

One aspect of the present invention pertains to methods of controlling or reducing weight gain in an individual comprising administering to said individual a therapeutically effective amount of a compound, as described herein, or a pharmaceutical composition thereof.

One aspect of the present invention pertains to methods of modulating a MCH receptor in an individual comprising contacting the receptor with a compound, as described herein. In some embodiments, the compound is an antagonist. In some embodiments, the modulation of the MCH receptor is for the prophylaxis or treatment of an eating disorder, obesity or obesity related disorder. In some embodiments, the modulation of the MCH receptor reduces food intake of the individual. In some embodiments, the modulation of the MCH receptor induces satiety in the individual. In some embodiments, the modulation of the MCH receptor controls or reduces weight gain of the individual. In some embodiments, the modulation of the MCH receptor is for prophylaxis or treatment of anxiety, depression, schizophrenia, addiction, or epilepsy.

In some embodiments, the individual is a mammal.

In sone embodiments, the mammal is a human.

In some embodiments, the human has a body mass index of about 18.5 to about 45. In some embodiments, the human has a body mass index of about 25 to about 45. In some embodiments, the human has a body mass index of about 30 to about 45. In some embodiments, the human has a body mass index of about 35 to about 45.

One aspect of the present invention pertains to methods of producing a pharmaceutical composition comprising admixing a compound as described herein, and a pharmaceul:ic311 acceptable carrier.

This application claims priority to U.S. Provisional Patent Application, Ser. No. 60/458,424, filed March 31, 2003; and is incorporated herein by reference in its entirety.

DETAILED DESCRIPTION OF THE INVENTION

One aspect of the present invention relates to certain substituted heterocyclic compounds represented by Formula (I): or a pharmaceutically acceptable salt, hydrate or solvate thereof, wherein Q, L, Y, and R₁ are as described herein, supra and infra.

It is appreciated that certain features of the invention, which are, for clarity, described in the context of separate embodiments, may also be provided in combination in a single embodiment. Conversely, various features of the invention which are, for brevity, described in the context of a single embodiment, may also be provided separately or in any suitable subcombination.

In some embodiments of the present invention, Q is Formulae (IIa), (IIb), or (IIc);

R₁ is selected from the group consisting of:

• • (i) C_1-8 alkyl, and C_1-8 alkyl substituted by substituent(s) independently selected from the group consisting of:
    • halogen,
    • C_1-5 alkoxy carbonyl,
    • C_1-5 alkoxy,
    • C_1-5 alkoxy substituted by carbocyclic aryl,
    • mono-C_1-5 alkylamino,
    • di-C_1-5 alkylamino,
    • C₃-₆ cycloalkyl,
    • C_3-6 cycloalkenyl,
    • carbocyclyl,
    • carbocyclic aryl,
    • carbocyclic aryl substituted by substitulent(s) independently selected from the group consisting of:
      • hydroxy,
      • halogen,
      • nitro,
      • C_1-5 alkylcarbonylamino,
      • C_3-6 cycloalkylcarbonylaminio,
      • C_1-5 alkyl,
      • C_1-5 alkyl substituted by halogen,
      • C_1-5 alkylsulfonyl,
      • C_2-6 alkenyl,
      • C_1-5 alkoxy,
      • C1-5 alkoxy substituted by halogen, and
      • carbocyclic aryl,
    • heterocyclyl, and
    • heterocyclyl substituted by halogen,
  • (ii) C_2-5 alkenyl, and
  • C_2-5 alkenyl substituted by carbocyclic aryl,
  • (iii) C_2-5 alkyynyl,
  • (iv) C_3-12 cycloalkyl, and
  • C_3-12 cycloalkyl substituted by carbocyclic aryl,
  • (v) carbocyclyl, and carbocyclyl by substituent(s) independently selected from the group consisting of:
    • hydroxy, and
    • carbocyclic aryl
  • (vi) carbocyclic aryl, and carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of:
    • halogen,
    • cyano,
    • nitro,
    • C_1-10 alkyl,
    • C_1-10 alkyl substituted by substituent(s) independently selected from the group consisting of:
      • halogen,
      • oxo, and
      • carbocyclic aryl,
    • carboxy,
    • C_1-5 alkoxy carbonyl,
    • C_1-7 alkoxy,
    • C_1-7 alkoxy substituted by substituent(s) independently selected from the group consisting of:
      • halogen, and
      • carbocyclic aryl,
    • carbocyclic aryloxy,
    • carbocyclic aryloxy substituted by nitro,
    • mono-C_1-5 alkylamino,
    • di-C_1-5 alkylamino,
    • C_1-5 alkoxy carbonylamino,
    • carbocyclic aryl azo,
    • carbocyclic aryl azo substituted by substituent(s) independently selected from the group consisting of:
      • mono-C_1-5 alkylamino, and
      • di-C_1-5 alkylamino,
    • C_1-5 alkylthlio,
    • C_1-5 alkylthio substituted by halogen,
    • carbocyclic arylthio,
    • carbocyclic arylthio substituted by nitro,
    • amino sulfonyl,
    • heterocyclyl sulfonyl,
    • C_3-6 cycloalkyl,
    • C_3-6 cycloalkyl substituted by C_1-5 alkyl,
    • carbocyclic aryl,
    • heterocyclyl, and
    • heterocyclyl substituted by C_1-5 alkyl,
  • (vii) lieterocyclyl, and heterocyclyl substituted by substituent(s) independently selected from the group consisting of:
    • halogen,
    • C_1-5 alkyl,
    • C_1-5 alkyl substituted by hialogen,
    • C_1-5 alkoxy,
    • C_1-5 alkoxy carbonyl,
    • C_1-5 alkoxy carbonyl substituted by carbocyclic aryl,
    • carbocyclic aryloxy,
    • carbocyclic aryl, and
    • heterocyclyl;
  • R₂ is —N(R_2a)(R_2b), wherein R_2a is hydrogen or C_1-5 alkyl; R_2b is C_1-5 alkyl;
  • R₃ is C_1-5 alkyl;
  • R₄ is —N(R_4a)(R_4b) wherein R_4a is hydrogen or C_1-5 alklyl; R_4b is C_1-5 alkyl;
  • L is selected from Formula (V), (VIII), (IX ) (XIII), (XVI), or (XVII);
  • X₁, X₂, X₃ and X₄ are independently selected from the group consisting of hydrogen, halogen, and C_1-4 alkyl; provided that at least one substituent selected from the group consisting of X₁, X₂, X₃ and X₄ is not hydrogen; and
  • Y is selected from the group consisting of:
  • (i) —C(O)NR₇—, —C(S)NR₇—, or —C(O)O— when L is selected from the group consisting of Formula (V), (VIII), (IX), (XIII), (XVI), or (XVII); wherein R₇ is hydrogen or C_1-5 alkyl;
  • (ii) —S(O)₂—, —C(O)—, a single bond or —CH₂— when L is selected from the group consisting of Formula (VIII) or (IX); and
  • (iii) —OC(O)— when L is selected from the group consisting of Formula (XIII), (XVI), or (XVII);
    • wherein carbocyclic aryl is phenyl or naphthyl;
    • carbocyclyl is indanyl, bicyclo[2.2.1]heptyl, bicyclo[2.2.1]heptenyl, adamantly, 9H-flutorenyl, menthyl, 1,2,3,4-tetrahydro-naphthalen-1-yl, or 1H-indolyl,
    • heterocyclyl is 2,3-dihydro-benzo[1,4]dioxinyl, 3,4-dihydro-2H-benzo[b][1,4]dioxepinyl, 4,5,6,7-tetrahydro-benzo[b]thienyl, 4H-benzo[1,3]dioxiiiyl, benzo[1,3]dioxolyl, benzo[2,1,3]thiadiazolyl, benzotiliazolyl, furyl, isoxazolyl. morpliolinyl, oxazolyl, piperidyl, pyrazolyl, pyridyl, tetrahydrofuryl, thienyl, dibenzofuranyl, 1H-benzoimidazolyl, or thiazolyl; and
    • halogen is fluoro, chloro, bromo, or iodo;
  • or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments of the present invention, Q is Formula (IIc) and can be represented by the following formula: or a pharmaceutically acceptable salt, hydrate or solvate thereof, wherein R₄, L, Y, and R₁ are as described herein, supra and infra.

In some embodiments of the present invention, R₁ is selected from the group consisting of:

• • (i) C_1-5 alkyl, and C_1-5 alkyl substituted by substituent(s) independently selected from the group consisting of:
    • C_1-5 alkoxy carbonyl,
    • carbocyclic aryl,
    • carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of:
      • halogen,
      • C_1-5 alkyl,
      • C_2-5 alkenyl, and
      • C_1-5 alkoxy,
    • C_1-5 alkyltlilo, and
    • heterocyclyl,
  • (ii) C_3-6 cycloalkyl, and C_3-6 cycloalkyl substituted by carbocyclic aryl,
  • (iii) carbocyclyl,
  • (iv) carbocyclic aryl, and carbocyclic aryl substituted by substitient(s) independently selected from the group consisting of:
    • halogen,
    • cyano,
    • nitro,
    • C_1-5 alkyl,
    • C_1-5 alkyl substituted by substituent(s) independently selected from the group consisting of:
      • halogen,
      • oxo, and
      • carbocyclic aryl,
    • C_1-5 alkoxy carbonyl,
    • C_1-7 alkoxy,
    • C_1-7 alkoxy substituted by substituent(s) independently selected from the group consisting of:
      • halogen, and
      • carbocyclic aryl,
    • cycloalkoxy,
    • carbocyclic aryloxy,
    • mono-C_1-5 alkylamino,
    • di-C_1-5 alkylainino,
    • C_1-5 alkylthio,
    • C_1-5 alkylthio substituted by halogen,
    • carbocyclic aryl,
    • heterocyclyl, and
    • heterocyclyl substituted by C_1-5 alkyl,
  • (v) heterocyclyl, and heterocyclyl substituted by substituent(s) independently selected from the group consisting of:
    • halogen,
    • C_1-5 alkyl,
    • C_1-5 alkyl substituted by halogen,
    • C_1-5 allkoxy carbonyl
    • C_1-5 alkoxy carbonyl substituted by carbocyclic aryl, and
    • carbocyclic aryl;
  • L is Formula (V); and
  • Y is —C(O)NR₇—; wherein R₇ is hydrogen or C_1-5 alkyl;
    • wherein carbocyclic aryl is phenyl or naphthyl;
    • carbocyclyl is indanyl, adamantly, or 9H-fluorenyl;
    • heterocyclyl is 2,3-dihydro-benzo[1,4]dioxinyl, 3,4-dihydro-2H-benzo[b][1,4]dioxepinyl, 4H-benzo[1,3]dioxinyl, benzo[1,3]dioxolyl, benzothiazolyl, furyl, isoxazolyl, piperidyl, pyridyl, or thienyl; and
    • halogen is fluoro, chloro, broino, or iodo;
  • or a pharmaceutically acceptable salt, hydrate or solvate thereof

In some embodiments of the present invention, R_1a is hydrogen or methyl; R_4b is methyl; R₅ and R₆ are hydrogen; A is a single bond and B is a single bond or —CH₂—; and R₇ is hydrogen; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments of the present invention, R₁ is selected from the group consisting of:

• • (i) C_1-5 alkyl, and C_1-5 alkyl substituted by substituent(s) independently selected from the group consisting of:
    • C_1-5 alkoxy carbonyl,
    • carbocyclic aryl,
    • carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of:
      • halogen,
      • C_1-5 alkyl,
      • C_1-5 alkenyl, and
      • C_1-5 alkoxy,
    • C_1-5 alkythio, and
    • heterocyclyl,
  • (ii) C_3-6 cycloalkyl, and C_3-6 cycloalkyl substituted by carbocyclic aryl,
  • (iii) carbocyclyl,
  • (iv) carbocyclic aryl, and carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of:
    • halogen,
    • cyano,
    • nitro,
    • C_1-5 alkyl,
    • C_1-5 alkyl substituted by halogen
    • C_1-5 alkoxy carbonyl,
    • C_1-5 alkoxy,
    • C_1-5 alkoxy substituted by halogen,
    • cycloalkoxy,
    • carbocyclic aryloxy,
    • C_1-5 alkylthio, and
    • carbocyclic aryl,
  • (v) heterocyclyl, and heterocyclyl substituted by substituent(s) independently selected from the group consisting of:
    • halogen,
    • C_1-5 alkyl,
    • C_1-5 alkyl substituted by halogen, and
    • carbocyclic aryl;
    • wherein carbocyclic aryl is phenyl or naphthyl;
    • carbocyclyl is 9H-fluorenyl;
    • heterocyclyl is 2,3-dihydro-benzo[1,4]dioxinyl, 3,4-dihydro-2H-benzo[b][1,4]dioxepinyl, 4H-benzo[1,3]dioxinyl, benzo[1,3]dioxolyl, furyl, isoxazolyl, or thienyl; and
    • halogen is fluoro, chloro, bromo, or iodo;
  • or a pharmaceutically acceptable salt, hydrate or solvate thereof

In some embodiments of the present invention, R₁ is selected from the group consisting of:

• • (i) C_1-5 alkyl, and C_1-5 alkyl substituted by substituent(s) independently selected from the group consisting of:
    • C_1-5 alkoxy carbonyl,
    • carbocyclic aryl,
    • carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of:
      • halogen,
      • C_1-5 alkyl, and
      • C_2-5 alkenyl,
    • C_1-5 alkylthio,
  • (ii) C_3-6 cycloalkyl, and C₃-6 cycloalkyl substituted by carbocyclic aryl,
  • (iii) carbocyclic aryl, and carbocyclic aryl substituted by substituent(s) independently selected fiom the group consisting of:
    • halogen,
    • cyano,
    • nitro,
    • C_1-5 alkyl,
    • C_1-5 alkyl substitited by halogen,
    • C_1-5 alkoxy carbonyl,
    • C_1-5 alkoxy,
    • cycloalkoxy,
    • carbocyclic aryloxy,
    • C_1-5 alkylthio, and
    • carbocyclic aryl,
  • (iv) heterocyclyl, and heterocyclyl substituted by substituent(s) independently selected from the group consisting of:
    • C_1-5 alkyl,
    • C_1-5 alkyl substituted by halogen, and
    • carbocyclic aryl;
    • wherein carbocyclic aryl is phenyl or naphthyl;
    • heterocyclyl is 2,3-dihydro-benzo[1,4]dioxinyl, 3,4-dihydio-2H-benzo[b][1,4]dioxepinyl, benzo[1,3]dioxolyl, furyl, or isoxazolyl; and
    • halogen is fluoro, chloro, bromo, or iodo;
  • or a pharmaceutically acceptable salt, hydrate or solvate thereof

In some embodiments, compounds of the present invention are of Formula (I) wherein the compound is selected from the group consisting of:

• N-benzyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-(2-bromophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-biphenyl-2-yl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amyino}cyclohexyl)urea;
• N-(4-bromophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-butyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-cyclohexyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-(2-chlorophetyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,6-dimethylphenyl)-urea;
• N-(2,4-difluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-urea;
• N-(2,4-dichlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino)-cyclohlexyl)-urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,3-dimethylphenyl)-urea;
• ethyl 3-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]carbonyl}-amino)benzoate;
• ethyl 4-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]carbonyl}-amino)benzoate;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-ethylphenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethyl-6-methylphenyl)urea;
• ethyl N-{[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]carbonyl}-leucinate;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-fluorophenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino) cyclohexyl)-N′-[1-(3-isopropenylphenyl)-1-methylethyl]urea;
• methyl N-{[(cis-4-{[4-(dimethylamino)quinazolin-2 -yl]amino}cyclohexyl)amino]carbonyl}-methioninate;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-methoxyphenyl)-urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]aminolcyclohexyl)-N′-(2-methoxyphenyl)-urea;
• N-(cis-4-}[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3-nmethoxyphenyl)-urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[4-(methylthio)-phenyl]urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-methoxybenzyl)-urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-1 -naphthylurea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[(2S)-2-phenylcyclopropyl]urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-phenylurea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-phenoxyphenyl)-urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-pentylurea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[2-(trifluoromethyl)-phenyl]urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-methylphenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-mesitylurea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclolhexyl)-N′-(3-methylphenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methylphenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[1-(1-naphthyl)ethyl]-urea;
• methyl N-{[(cis-4-{[4-(dimethylamino)quinazoiin-2-yl]amino}cyclohexyl)amino]carbonyl)-phenylalaninate;
• N-(cis-4-{[4-(dimethy lamino)quinazlin-2-yl]am iiio cyclohexyl)-N′-(2,4,6-trichlorophenyl)urea;
• N-(cis-4-}[4-(dimethylamino)quiniazolin-2-yl]amino}cyclohexyl)-N′-(1-phenyl-ethyl)urea;
• 1-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-3-(1-phenyl-ethyl)-urea;
• 1-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-3-(1-naphthalen-1-yl-ethyl)-urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[2-(methylthio)-phenyl]urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,3,5,6-tetrachlorophenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,3-dimethyl-6-nitrophenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,4,6-tribromophenyl)urea;
• N-(2,4-dibromo-6-fluorophenyl)-N′-(cis-4-([4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea;
• N-(2,4-dibromophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-urea;
• N-(2,4-dichlorobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-yl]amino}cyclohexyl)-urea;
• N-(2,4-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea;
• N-(2,5-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea;
• N-(7,6-diethylphenyl)-N′-(cis-4-{[4-(dimethylamino)qu iiazolin-2-yl]amino}cyclohexyl)-urea;
• N-(2-chloro-5-nitrophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino)-cyclohexyl)urea;
• N-[2-chloro-6-(trifluoromethyl)phenyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-(2-chloro-6-methylphenyl)-N′-(cis-4-([4-(dimethylamino)quinazolin-2-yl)amino}-cyclohexyl)urea;
• N-(2-chlorobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-(cis-4-{(4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethoxyphenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethyl-6-isopropylphenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethylphenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-fluorobenzyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-iodophenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-isopropyl-6-methylphenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-isopropylphenyl)-urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methoxy-4-nitrophenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methoxy-5-methylphenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methyl-3-nitrophenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quiiazolin-2-yl]amino}cyclohexyl)-N′-(2-methyl-4-nitrophenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methyl-5-nitrophenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methylbenzyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclolexyl)-N′-(2-nitrophenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-propylphenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-phenoxyphenyl)-urea;
• N-(2-tert-butyl-6-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-(2-tert-butylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino) cyclohexyl)-N′-[3-(methylthio)-phenyl]urea;
• N-1,3-benzodioxol-5-yl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3,4,5-trimethoxyphenyl)urea;
• N-(3,4-dichlorobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-urea;
• N-(3,4-difluorophenyl)-N′-(cis-4-([4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-urea;
• N-(3,4-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea;
• N-(3,5-difluorophienyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-urea;
• N-(3,5-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl)amino}cyclohexyl)-N′-(3,5-dimethylphenyl)-urea;
• methyl 3-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino) cyclohexyl)amino]carbonyl}-amino)benzoate;
• N-(3-chloro-2-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea;
• N-(3-chloro-4-fluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea;
• N-(3-chloro-4-methoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quiniizolin-2-yl]amino}-cyclolexyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3-ethylphenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amnio )cyclolhexyl)-N′-(3-fluorobenzyl)urea;
• N-[4-bromo-2-(trifluoromethyl)phenyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-(4-bronio-2,6-difluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea;
• N-(4-bromobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-[4-chloro-2-(trifluoromethyl)phenyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-(4-chloro-2-methylphenyl)-N′-(cis-4-{[4-(dimetlhylamino)q uI iazolin-2-yl]amino}-cyclohexyl)urea;
• N-(4-cyanophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-ethoxyphenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-fluoro-2-nitrophenyl)urea;
• N-(cis-4-}[4-(dimethylamino)quinazolin-2-yl]amino}cyclolexyl)-N′-(4-fluorobenzyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-iodophenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-methoxy-2-methylphenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-methylbenzyl)urea;
• N-(5-chloro-2,4-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(5-fluoro-2-methylphenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-9H-fluoren-9-ylurea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-phenylethyl)urea;
• N-cyclopentyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(diphenylmethyl)urea;
• N-[1-(4-bromophenyl)ethyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea;
• N-(4-bromo-2,6-dimethylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea;
• N-(4-bromo-2-methylphetnyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea;
• ethyl N-{[(cis-4-{[4-(dimetylamino)quinazolin-2-yl]amino}cyclohexyl)amino]carbonyl}-phenylalaninate;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclolexyl)-N′-[2-(2-thienyl)ethyl]-urea;
• N-(2,3-dihydro-1,4-benzodioxin-6-yl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-(2,6-dibromo-4-isopropylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-ylamino]-cyclohexyl}urea;
• N-[3-(cyclopentyloxy)-4-methoxyphenyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-(3,4-dihydro-2H-1,5-benzodioxepin-7-yl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-(4-butyl-2-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[5-methyl-2-(trifluoromethyl)-3-furyl]urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino) cyclohexyl)-N′-(6-fluoro-4H-1,3-benzodioxin-8-yl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3,5-dimethylisoxazol-4-yl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cycloiexyl)-N′-(3-methyl-5-phenylisoxazol-4-yl)urea;
• N-(cis-4-((4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(5-methyl-3-phenylisoxazol-4-yl)urea;
• N-(2-bromophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]urea;
• N-biphenyl-2-yl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-urea;
• N-butyl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea;
• N-(3-chlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]urea;
• N-cyclohlexyl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]aminio}cyclohexyl)methyl]-urea;
• N-(3-cyanophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]urea;
• N-(2-chlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,6-dimethylphenyl)urea;
• N-(3,4-dichlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]urea;
• N-(2,4-difluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-mnethyl]urea;
• N-(2,4-dichlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]urea;
• N-(3,5-dichlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]urea;
• N-(2,3-dichlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]urea;
• N-(2,6-difluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)-methyl]urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,3-dimethylphenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4-ethylphenyl)urea;
• N-[(cis-4-{[4-(dimethylanino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-ethyl-6-methylphenyl)urea;
• ethyl N-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]amino)-carbonyl)leucinate;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4-fluorophenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(3-fluorophenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-fluorophenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino₁cyclohexyl)methyl]-N′-[1-(3-isopropenylphenyl)-1-methylethyl]urea;
• methyl N-({[(cis-4-{[4-(dimethylamino)quiniazolin-2-yl]amino}cyclohexyl)methyl]amino}-carbonyl)methioninate;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4-methoxyphenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4-methyl-2-nitrophenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-methoxyphenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(3-methoxyphenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-[4-(methylthio)phenyl]urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-1-naphthylurea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-phenylurea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′pentylurea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-[2-(trifluoromethyl)phenyl]urea;
• N-[(cis-4-}[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4-methylphenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-mesitylurea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(3-methylphenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-methylphenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,4,6-trichlorophenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(1-phenylethyl)urea;
• 1-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexylmethyl]-3-(1-phenyl-ethyl)-urea;
• 1-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexylnethyl]-3-(1-naphthalen-1-yl-ethyl)-urea;
• N-(2,6-diisopropylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl)urea;
• N-[2-(difluoromethoxy)phenyl]-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-2-(methylthio)phenyl]urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl)]-N′-(2,3,5,6-tetrachlorophenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quiniazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,3-dimethyl-6-nitrophenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,4,6-tribromophenyl)urea;
• N-(2,4-dibromo-6-fluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea;
• N-(2,4-dichlorobenzyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]urea;
• N-(2,5-dimethoxyphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea;
• N-(2.6-dibromo-4-fluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea;
• N-(2,6-dichlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]urea;
• N-(2,6-diethylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]urea;
• N-(2-chloro-5-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea;
• N-[2-chloro-6-(trifluoromnethyl)phenyl]-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]-amino}cyclohexyl)methyl]urea;
• N-(2-chloro-6-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea;
• N-(2-chlorobenzyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-ethy)-6-isopropylphenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cycliohexyl)metlyl]-N′-(2-ethylphenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-fluoro-5-nitrophenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-fluorobenzyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-iodophenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)mehhyl]-N′-(2-isopropyl-6-methylphenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-isopropylphenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-methoxy-5-methylphenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-methoxy-5-nitrophenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-methyl-3-nitrophenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-methyl-4-nitrophenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-methyl-5-nitrophenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-methyl-6-nitrophenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-methylbenzyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-nitrophenyl)urea:
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-propylphenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclolexyl)methyl]-N′-(2-phenoxyphenyl)urea;
• N-(2-tert-butyl-6-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea;
• N-(2-tert-butylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-[3-(methylthio)phlenyl]urea;
• N-(3,4-difluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]urea;
• N-(3,5-difluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]urea;
• N-(3,5-dimetlioxyphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea;
• N-(3-chloro-2-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea;
• N-(3-chloro-4-fluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl)-N′-(3-ethylphenyl]urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl)-N′-(3-fluoro-5-(trifluoromethyl)phenyl]urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(3-fluorobenzyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4,5-dimethyl-2)-nitrophenyl)urea;
• N-[4-bromo-2-(trifluoromethyl)phenyl]-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea;
• N-(4-bromno-2,6-difluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea;
• N-[4-chloro-2-(trifluorometlyl)phenyl]-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea;
• N-(4-chloro-2-methlylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea;
• N-(4-cyanophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl)-N′-(4-fluoro-2-nitrophenyl]urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl)-N′-(4-fluorobenzyl]urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4-iodophenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4-methoxy-2-methylphenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4-methyl-3-nitrophenyl)urea;
• N-(5-chloro-2-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(5-fluoro-2-methylphenyl)urea;
• N-cyclopentyl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl)-N′-(diphenlylmethyl)urea;
• N-(4-bromo-2,6-dimethylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea;
• N-(4-bromo-2-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quiniazolin-2-yl]amino}-cyclohexyl)methyl]urea;
• N-(2,6-dibromo-4-isopropylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-3-thienylurea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-[5-methyl-2-(trifluoromethyl)-3-furyl]urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(6-fluoro-4H-1,3-benzodioxin-8-yl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(3,5-dimethylisoxazol-4-yl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(3-methyl-5-phenylisoxazol-4-yl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(5-methyl-3-phenylisoxazol-4-yl)urea; and
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[3-(trifluoromethoxy)-phenyl]urea;

or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments, compounds of the present invention are of Formula (I) wherein the compound is selected from the group consisting of:

• N-(2-bromophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-biphenyl-2-yl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-butyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-(2-chlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,6-dimetlylphenyl)-urea;
• N-(2,4-difluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,3-dimethylphenyl)-urea;
• ethyl 3-{[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]carbonyl}-amino)benzoate;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethyl-6-methylphenyl)urea;
• ethylN-{[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]-amino}cyclohexyl)amino]-carbonyl}leucinate;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-fluorophenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[1-(3-isopropenylphenyl)-1-methylethyl]urea;
• methyl N-{[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]-carbonyl}methioninate;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[4-(methylthio)phenyl]urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-1-naphthylurea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[(2S)-2-phenylcyclopropyl]urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-phenoxyphenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-pentylurea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[2-(trifluoromethyl)-phenyl]urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-mesitylurea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methylphenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohe-:yl)-N′-[1-(1-naphthyl)ethyl]-urea;
• methyl N-{[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]carbonyl}-phenylalaninate;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,4,6-trichlorophenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(1-phenylethyl)urea;
• 1-(4-Dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-3-(1-phenyl-ethyl)-urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,3,5,6-tetrachlorophenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,4,6-tribromophenyl)urea;
• N-(2,4-dibromo-6-fluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea;
• N-(2,4-dibromophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-urea;
• N-(2,4-dichlorobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-urea;
• N-(2,4-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea;
• N-(2,6-diethylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino) cyclohexyl)-urea;
• N-[2-chloro-6-(trifluoromethyl)phenyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]-amino}cyclohexyl)urea;
• N-(2-chloro-6-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea;
• N-(2-chlorobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-(cis4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethoxyphenyl)urea:
• N-(cis-4-{[4-(dimethylamino)quinazolin)-2-yl]amino}cyclohexyl)-N′-(2-ethyl-6-isopropylphenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethylphenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-fluorobenzyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-iodophenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-isopropyl-6-mnethylphenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-isopropylphenyl)-urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclolexyl)-N′-(2-methyl-3-nitrophenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methyl-4-nitrophenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methyl-5-nitrophenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methylbenzyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-nitrophenyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-propylphenyl)urea;
• N-(2-tert-butyl-6-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea;
• N-(2-tert-butylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-urea;
• N-1,3-benzodioxol-5-yl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3,4,5-trimethoxyphenyl)urea;
• N-(3,4-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea;
• N-(3-chloro-2-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea;
• N-(3-chloro-4-methoxyphenyl)-N′-(cis-4-{[4-(dimethlylamino)quinazolin-2-yl]amino}-cyclohexyl)urea;
• N-[4-bromo-2-(trifluoromethyl)phenyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]-amino}cyclohexyl)urea;
• N-(4-bromo-2,6-difluorophenyl)-N′-(cis-4-[4-(dimethylamino)quinzolin-]amino}-cyclohexyl)urea;
• N-(4-bromobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-[4-chloro-2-(trifluoromethyl)phenyl]-N′-(cis-4-{[4-(dinethylamino)quinazolin-2-yl]-amino}cyclohexyl)urea;
• N-(4-chloro-2-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea;
• N-(4-cyanophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-fluorobenzyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-methoxy-2-methylphenyl)urea;
• N-(5-chloro-2,4-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino) cyclohexyl)-N′-(diphenylmethyl)urea;
• N-[1-(4-bromophenyl)ethyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea;
• N-(4-bromo-2,6-dimethylphenyl)-N′-(cis-74-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea;
• N-(4-bromo-2-metylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea;
• ethyl N-{[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]carbonyl}-phenylalaninate;
• N-(2,3-dihydro-1,4-benizodioxin-6-yl)-N′-(cis4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-(2,6-dibromo-4-isopropylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-[3-(cyclopentyloxy)-4-methoxyphenyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-(3,4-dihydro-2H-1,5-benzodioxepin-7-yl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea;
• N-(4-butyl-2-methylphlenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[5-methyl-2-(trifluoromethyl)-3-furyl]urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino) cyclohexyl)-N′-(3-methyl-5-phenylisoxazol-4-yl)urea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino) cyclohexyl)-N′-(5-methyl-3-phenylisoxazol-4-yl)urea;
• N-(2-chlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,6-dimethylphenyl)urea;
• N-(2,4-difluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazoliln-2-yl]amino}cyclohexyl)-methyl]urea;
• N-(3,5-dichlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quiniazolin-2-yl]amino}cyclohexyl)-methyl]urea;
• N-(2,3-dichlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amio}cyclohexyl)-methyl]urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,3-dimethylphenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl)ainiilo cyclohexyl)methyl]-N′-(2-ethyl-6-metlylphenyl]urea;
• ethyl N-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino) cyclohexyl)methyl]amino}-carbonyl)leucinate;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4-fluorophenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-[4-(methylthio)phenyl]urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-phenylurea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-[2-(trifluoromethyl)phenyl]urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4-methylphenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-mesitylurea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-methylphenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,4,6-trichlorophenyl)urea;
• N-(2,6-diisopropylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quiniazolin-2-yl]amino}-cyclohexyl)methyl]urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,3-dimethyl-6-nitrophenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl] amino}cyc liohexyl)methyl]-N′-(2,4,6-tribroinophenyl)urea;
• N-(2,4-dibromo-6-fluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea;
• N-(2,6-dibromo-4-fluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl)urea;
• N-(2,6-dichlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]urea;
• N-(2,6-diethylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl)urea;
• N-[2-chloro-6-(trifluoromethyl)phenyl]-N′-[(cis-4-}[4-(dimethylamino)quinazolin-2-yl]-amino}cyclohexyl)methyl]urea;
• N-(2-chloro-6-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea;
• N-(2-chlorobenzyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-ethyl-6-isopropylphenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-ethylphenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-iodophenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-isopropyl-6-methylphenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-isopropylphenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-ylamino}cyclohexyl)methyl]-N′-(2-methoxy-5-methylphenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino) cyclohexyl)methyl]-N′-(2-methyl-3-nitrophenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-methyl-6-nitrophenyl)urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl)-N′-(2-propylphenyl)urea;
• N-(2-tert-butyl-6-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea;
• N-(2-tert-butylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]urea;
• N-(3,4-difluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl)urea;
• N-(3,5-difluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]urea;
• N-(3-chloro-2-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazoln-2-yl]amino}-cyclohexyl)methyl]urea;
• N-(3-chloro-4-fluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea;
• N-(4-bromo-2,6-difluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea;
• N-[4-chloro-2-(trifluoromethyl)phenyl]-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]-amino}cyclolhexyl)methyl]urea;
• N-(4-cyanophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]urea;
• N-[(cis-4-((4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(diphenylmetlhyl)urea;
• N-(4-bromo-2,6-dimethylphenyl)-N′-[(cis-4-{ (4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-[5-methyl-2-(trifluoromethyl)-3-furyl]urea; and
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino) cyclohexyl)methyl]-N′-(3-methyl-5-phenylisoxazol-4-yl)urea;

or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments of the present invenltion, R₁ is selected fiom the group consisting of:

• • (i) C_1-8 alkyl, and C_1-8 alkyl substituted by substituent(s) independently selected from the group consisting of:
    • mono-C_1-5 alkylamino,
    • di-C_1-5 alkylamino,
    • C_3-6 cycloalkyl,
    • C_3-6 cycloalkenyl
    • carbocyclic aryl,
    • carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of:
      • halogen,
      • C_1-5 alkyl, and
      • C_1-5 alkoxy,
    • heterocyclyl,
  • (ii) C_2-5 alkynyl,
  • (iii) C_2-5 alkenyl, and C_2-5 alkenyl substituted by carbocyclic aryl,
  • (iv) C_3-12 cycloalkyl,
  • (V) carbocyclyl,
  • (vi) carbocyclic aryl, and carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of:
    • halogen,
    • cyano,
    • nitro,
    • C_1-10 alkyl,
    • C_1-10 alkyl substituted by substituent(s) independently selected from the group consisting of:
      • halogen, and
      • oxo,
    • carboxy,
    • C_1-5 alkoxy carbonyl,
    • C_1-5 alkoxy,
    • C_1-5 alkoxy substituted by substituent(s) independently selected from the group consisting of:
      • halogen, and
      • carbocyclic aryl,
    • carbocyclic aryloxy,
    • carbocyclic aryloxy substituted by nitro,
    • mono-C_1-5 alkylamino,
    • di-C_1-5 alkylamino,
    • C_1-5 alkoxy carbonylamino,
    • carbocyclic aryl azo,
    • carbocyclic aryl azo substituted by substituent(s) independently selected from the group consisting of:
      • mono-C_1-5 alkylamino, and
      • di-C_1-5 alkylamino,
    • C_1-5 alkylthio,
    • C_1-5 alkylthio substituted by halogen,
    • carbocyclic arylthio,
    • carbocyclic arylthio substituted by nitro,
    • amino sulfonyl,
    • heterocyclyl sulfonyl,
    • C_3-6 cycloalkyl,
    • C_3-6 cycloalkyl substituted by C_1-5 alkyl,
    • carbocyclic aryl, and
    • heterocyclyl,
  • (vii) heterocyclyl, and heterocyclyl substituted by substituent(s) independently selected from the group consisting of:
    • C_1-5 alkyl,
    • C_1-5 alkoxy carbonyl,
    • carbocyclic aryloxy,
    • carbocyclic aryl, and
    • heterocyclyl;
  • L is Forrnula (V); and
  • Y is —C(S)NR₇—; wherein R₇ is hydrogen or C_1-5 alkyl;
  • wherein carbocyclic aryl is phenyl or naphthyl;
  • carbocyclyl is indanyl, bicyclo[2.2.1]heptyl, bicyclo[2.2.1]heptenyl, or adamantly;
  • heterocyclyl is 2,3-dihydro-benzo[1,4]dioxinyl, 4,5,6,7-tetrahydi-o-benzo[b]thienyl, benzo[ l ,]dioxolyl, benzo[2, 1 ,3]thiadiazolyl, furyl, isoxazolyl, morpliolinyl, oxazolyl. piperidyl, pyrazolyl, pyridyl, tetrahydrofuryl, or thienyl; and
  • halogen is fluoro, chloro, bromo, or iodo;

or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments of the present invention, R_4a is hydrogen or methyl; R_4b is methyl; R₅ and R₆ are hydrogen; A is a single bond; B is a single bond or —CH₂—; and R₇ is hydrogen; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments of the present invention, R₁ is selected from the group consisting of:

• • (i) C_1-6 alk-yl, and C_1-6 alkyl substituted by substituent(s) independently selected from the group consisting of:
    • C_3-6 cycloalkyl,
    • C_3-6 cycloalkenyl,
    • carbocyclic aryl,
    • carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of:
      • halogen,
      • C_1-5 alkyl, and
    • heterocyclyl,
  • (ii) C_3-12 cycloalkyl,
  • (iii) carbocyclyl,
  • (iv) carbocyclic aryl, and carbocyclic aryl substituted by substituent(s) independently selected from the group consistingc of:
    • halogen,
    • cyano,
    • nitro,
    • C_1-5 alkyl,
    • C_1-5 alkyl substituted by halogen,
    • C_1-5 alkoxy carbonyl,
    • C_1-5 alkoxy,
    • C_1-5 alkoxy substituted by halogen,
    • mono-C_1-5 alkylamino,
    • di-C_1-5 alkylamino,
    • C_1-5 alkylthio, and
    • carbocyclic aryl,
  • (v) heterocyclyl, and heterocyclyl substituted by substitlent(s) independently selected from the group consisting of:
    • C_1-5 alkoxy carbonyl, and
    • carbocyclic aryl;
      • wherein carbocyclic aryl is phenyl or naphthyl;
      • carbocyclyl is indanyl, bicyclo[2.2.1]heptyl, or bicyclo[2.2.1]heptenyl;
      • heterocyclyl is 2,3-dihydro-benzo[1,4]dioxinyl, benzo[1,3]dioxolyl, isxoazolyl, tetrahydrofuryl, or thienyl; and
      • halogen is fluoro, chloro, bromno, or iodo;
  • or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments of the present invention, R₁ is selected from the group consisting of:

• • (i) C_1-5 alkyl, and C_1-5 alkyl substituted by substituent(s) independently selected from the group consisting of:
    • carbocyclic aryl,
    • carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of:
      • halogen, and
      • C_1-5 alkoxy;
  • (ii) carbocyclyl,
  • (iii) carbocyclic atyl, and carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of:
    • halogen,
    • cyano,
    • nitro,
    • C_1-5 alkyl,
    • C_1-5 alkyl substituted by halogen,
    • C_1-5 alkoxy carbonyl,
    • C_1-5 allkoxy,
    • C_1-5 alkoxy substituted by halogen,
    • mono-C_1-5 alkylamino,
    • di-C_1-5 alkylamrino, and
    • carbocyclic aryl,
  • (iv) heterocyclyl, and heterocyclyl substituted by substituent(s) independently selected from the group consisting of:
    • C_1-5 alkyl,
    • C_1-5 alkoxy carbonyl, and
    • carbocyclic aryl; wherein carbocyclic aryl is phenyl or naphthyl;
    • carbocyclyl is bicyclo[2.2.1]heptyl;
    • heterocyclyl is 2,3-dihydro-benzo[1,4]dioxinyl, benzo[1,3]dioxolyl, isoxazolyl, or thienyl; and
    • halogen is fluoro, chloro, bromo, or iodo;
  • or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments, compounds of the present invention are of Formula (I) wherein the compound is selected from the group consisting of:

• N-(4-bromophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-thiourea;
• N-(4-cyanophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-thiourea;
• N-cyclohexyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea;
• N-cyclopentyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea;
• N-(4-chlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-thiourea;
• N-(2,4-dichlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-thiourea;
• N-(2,4-dimnethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolinn-yl)]amino}-cyclohexyl)thiourea;
• N-(cis-4-}[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,6-dimethylphenyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethyl-6-isopropylphenyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-fluorophenyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-hexylthiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-isobutylthiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-methoxybiphenyl-3-yl)thiourea;
• N-(1,3-benzodioxol-5-ylmethyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[4-(methylthio)pheny)]-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-methoxyphenyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methoxyphenyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-1-naphthylthiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino) cyclohexyl)-N′-(4-nitrophenyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(pentafluorophenyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino) cyclohexyl)-N′-propylthiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]aminoll cyclohexyl)-N′-(3,4,5-trimethoxyphenyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-methylphenyl)-thiourea;
• N-(3,4-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-ethylphenyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[2-(methylthio)-phenyl]thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[2-(trifluoromethoxy)-phenyl]thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino) cyclohexyl)-N′-(2,3,4-trifltorophenyl)-thiourea;
• N-(2,5-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-(2-chloro-4-nitrophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethylphenyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-iodophenyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methoxy-4-nitrophenyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methoxy-5-methylphenyl)thiourea;
• N-(cis-4-}[4-(dimethylamino)quinazolin-2-yl]amino) cyclohexyl)-N′-(3-iodophenyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino] cyclollexyl)-N′-(3-methoxyphenyl)-thiourea;
• N-[4-(difluoromethoxy)phenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-(cis-4-}[4-(dimethylamino)quinazolin-2-yl]amino) cyclohexyl)-N′-[4-(trifluoromethyl)-phenyl]thiourea;
• N-(4-bromo-2-chlorophenyl)-N′-(cis-4-}[4-(dmethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-iodophenyl)-thiourea;
• N-(5-chloro-2-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-[(1S,4R)-bicyclo[2.2.1]hept-2-yl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-[2-(4-chlorophenyl)ethyl]-N′-(cis-4-{[4-(dimethylanmino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,4,6-tribromophenyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-N′-(2,4,6-trichlorophenyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-mesitylthiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,4-dimethylphenyl)-thiourea;
• N-(2,6-diethylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-thiourea;
• N-(2,6-diisopropylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-(2-bromo-4-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-(2-clorobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethyl-6-methylphenyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclolexyl)-N′-(2-isopropylphenyl)-thiourea;
• N-(3,5-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3,5-dimethylphenyl)-thiourea;
• N-(3-chloro-4-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• methyl 3-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]-carbonothioyl)}amino)benzoate;
• N-(4-bromo-2,6-dimethylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea;
• N-(4-bromo-2-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-[4-bromo-2-(trifluoromethyl)phenyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea;
• N-(4-chloro-2-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[1-(4-fluorophenyl)-ethyl]thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-fluorobenzyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-isopropylphenyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-methoxybenzyl)-thiourea;
• methyl 4-{[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]-carbonothioyl}amino)benzoate;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(1-phenylethyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2yl]amino}cyclohexyl)-N′-(diphenylmethyl)-thiourea;
• N-(cyclohexylmethyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclolhexyl)-thiourea;
• N-cyclooctyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea;
• N-cyclopropyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(1-naphthylmethyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,2-diphenylethyl)-thiourea;
• N-(2,3-dimethoxybenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,4,5-trimethylphenyl)thiourea;
• N-[2-(2,5-dimethoxyphenyl)ethyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-biphenyl-2-yl-N′-(cis4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-fluorobenzyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methyl-4-nitrophenyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methylbenzyl)-thiourea;
• N-(3-chlorobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-thiourea;
• ethyl 3-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]-carbonothioyl)amino)benzoate;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3-ethylpheylyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3-fluorobenzyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3-methoxybenzyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3-methylbenzyl)-thiourea;
• N-[4-chloro-2-(trifluoromethyl)phenyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-fluoro-2-methylphenyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-methoxy-2-methylphenyl)thiourea;
• N-(5-chloro-2,4-dimethoxyphenyl)-N′-(cis-4-}[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-(2,3-dihydro-1H-inden-5-yl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-cycloheptyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[(1R)-1-phenylethyl]-thiourea;
• N-(2-cyclohex-1-en-1-ylethyl)-N′-(cis-4-{[4-(dimetlylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,3-dimethylphenyl)-thiourea;
• N-(2,4-dibromo-6-fluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-(2,4-dichloro-6-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-]amino}cyclohexyl)-N′-(2,5-dimethylphenyl)-thiourea;
• N-(2-bromo-4-isopropylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-(2-bromo-5-fluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino) cyclohexyl)-N′-(2-ethoxyphenyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-isopropyl-6-methylphenyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino) cyclohexyl)-N′-(2-methoxybenzyl)-thiourea;
• N-(2,3-dihydro-1,4-benzodioxin-6-yl)-N′-(cis4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea;
• N-1,3-benzodioxol-5-yl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-thiourea;
• N-(3-chloro-2-methlylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-[4-bromo-2-(trifluoromethoxy)phenyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea;
• N-(4-chloro-2,5-dimethoxyphenyl)-N′-(cis-4-}[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-phenylbutyl)-thiourea;
• N-bicyclo[2.2.1]hept-2-yl-N′-(cis-4-[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• methyl 3-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]-carbonothioyl}amino)-4-methylthiophene-2-carboxylate;
• methyl 3-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]-carbonothioyl}amino)thiophene-2-carboxylate;
• N-(2-bromo-4-fluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-(4-butyl-2-methylphenyl)-N′-(cis-4-{[4-(dimetlhylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-[4-(dimethylamino)-1-naphthyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(5-methyl-3-phenylisoxazol-4-yl)thiourea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,6-dimethylphenyl)thiourea;
• N-(2,6-dichlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]thiourea;
• N-[(cis-4-{[4-(methylamino)quinazolin-2-yl]amino) cyclohexyl)methyl]-N′-(2-ethyl-6-isopropylphenyl)thiourea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino) cyclohexyl)methyl]-N′-isobutylthiourea;
• N-(1,3-benzodioxol-5-ylmethyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4-nitrophenyl)thiourea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl)]-N′-(pentafluorophenyl)thiourea;
• N-[(cis-4-{[4-(dimethylamilo)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(tetrahydrofuran-2-ylmethyl)thiourea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-[2-(trifluoromethoxy)phenyl]thiourea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amine}cyclohexyl)methyl]-N′-(2,3,4-trifluorophenyl)thiourea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-ethylphenyl)thiourea;
• N-(5-chloro-2-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl)thiourea;
• N-[(1S,4R)-bicyclo[2.2.1]hept-2-yl]-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea;
• N-[2-(3,4-methoxyphenyl)ethyl]-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]thiourea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,4,6-tribromophenyl)thiourea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,4,6-trichlorophenyl)thiourea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)metiyl]-N′-mesitylthiourea;
• N-(2,6-diethylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl)thiourea;
• N-(2,6-diisopropylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]thiourea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-ethyl-6-methylphenyl)thiourea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2yl-amino}cyclohexyl)methyl)]-N′-(2-isopropylphenyl)thiourea;
• N-(4-bromo-2,6-dimethylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]thiourea;
• N-[4-bromo-2-(trifluoromethyl)phenyl]-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclobexyl)methyl]thiourea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-[1-(4-fluorophenyl)ethyl]thiourea;
• N-(5-chloro-2-methoxyphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]thiourea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(diphenylmnethyl)thiourea;
• N-cyclododecyl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-thiourea;
• N-(cyclohexylmethyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]thiourea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,3,5,6-tetrachlorophenyl)thiourea;
• N-(2,3-dimethoxybenzyl)-N′-[(cis-4-{[4-(dimethylamino}quinazolin-?-yl]amino}-cyclohexyl)methyl]thiourea;
• N-(2,4-dichlorobenzyl)-N′-[(cis-4-{[4-(dimethylamino}quinazolin-2-yl]amino}cyclohexyl)-methyl]thiourea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-methoxy-5-nitrophenyl)thiourea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4-metl)oxy-2-methylphenyl)thiourea;
• N-(2,4-dibromo-6-fluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]thiourea;
• N-(2,4-dichloro-6-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]thiourea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,5-dimethylphenyl)thiourea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-ethoxyphenyl)thiourea;
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-isopropyl-6-methylphenyl)thiourea;
• N-[4-bromo-2-(trifluoromethoxy)phenyl]-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea;
• N-bicyclo[2.2.1]hept-2-yl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]thiourea;
• N-bicyclo[2.2.1]hept-5-en-2-yl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]thiourea;
• N-(cyclopropylmethyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]thiourea; and
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(5-methyl-3-phenylisoxazol-4-yl)thiourea; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments compounds of the present invention are of Formula (I) wherein the compound is selected from the group consisting of:

• N-(4-bromopheinyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-thiourea;
• N-(4-cyanophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-thiourea;
• N-(2,4-dichlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-thiourea;
• N-(2,4-dimethoxyphenyl)-N′-(cis-4-{[4-(ditnethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,6-dimethylphenyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethyl-6-isopropylphenyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(-2-methoxyphenyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-1-naphthylthiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3,4,5-trimethoxyphenyl)thiourea;
• N-(3,4-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethylphenyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methoxy-4-nitrophenyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methoxy-5-methylphenyl)thiourea;
• N-(4-bromo-2-chlorophenyl)-N′-(cis-4-{[4-(dimethylaimino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-iodophenyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,4,6-tribromophenyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclolhexyl)-N′-(2,4,6-trichlorophenyl)-thiourea;
• N-(cis-4-{[4-(dimetlylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-mesitylthiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,4-dimethylphenyl)-thiourea;
• N-(2,6-diethylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-thiourea;
• N-(2-bromo-4-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-(2-chlorobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethyl-6-methylphenyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-isopropylphenyl)-thiourea;
• methyl 3-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]-carbonothioyl}amino)benzoate;
• N-(4-bromo-2,6-dimethylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea;
• N-(4-bromo-2-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-[4-bromo-2-(trifluoromethyl)phenyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea;
• N-(4-chioro-2-methylphenyl)-N′-(cis-4-{[4-(dimetlylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(1-naphthylmethyl)-thiourea;
• N-(2,3-dimetihoxybenzyl)-N′-(cis-4-{[4-(dimethylaniiiio)quinazolin-2-yl]amino}cyclohexyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,4,5-trimethylphenyl)thiourea;
• N-biphenyl-2-yl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea;
• N-(cis4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methyl-4-nitrophenyl)thiourea;
• N-(3-chlorobenzyl)-N′-(cis-4-{[4-(dimethylamino)qtuiinazolin-2-yl]amino}cyclohexyl)-thiourea;
• ethyl 3-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]-carbonothioyl)amino)benzoate;
• N-[4-chloro-2-(trifluoromethyl)phenyl)-N′-(cis-4-{[4-(dimetlylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-fluoro-2-methylphenyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino) cyclohexyl)-N′-(4-methoxy-2-methylphenyl)thiourea;
• N-(5-chloro-2,4-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl] amino}-cyclohexyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[(1R)-1-phenylethyl]-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino) cyclohexyl)-N′-(2,3-dimethylphenyl)-thiourea;
• N-(2,4-dibromo-6-fluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-(2,4-dichloro-6-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethoxyphenyl)-thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-isopropyl-6-methylphenyl)thiourea;
• N-(2,3-dihydro-1,4-benzodioxin-6-yl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea;
• N-1,3-benizodioxol-5-yl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclolhexyl)-thiourea;
• N-(3-chloro-2-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-[4-bromo-2-(trifluoromethoxy)phenyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea;
• N-(4-chloro-2,5-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-bicyclo[2.2.1]hept-2-yl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• methyl 3-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]-carbonothioyl}amino)-4-methylthiophene-2-carboxylate;
• methyl 3-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]-carbonothioyl}amino)thiophene-2-carboxylate;
• N-(4-butyl-2-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-[4-(dimethylamino)-1-naphthyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea;
• N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(5-methyl-3-phenylisoxazol-4-yl)thiourea;
• N-(2,6-diethylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]thiourea;
• N-(4-bromo-2,6-dimethylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]thiourea;
• N-[(cis-4-{[4-(dirnetiylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,3,5,6-tetrachlorophenyl)thiourea; and
• N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino) cyclohexyl)methyl]-N′-(2-isopropyl-6-methylphenyl)thiourea;
  • or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments of the present invention, R₁ is selected from the group consistihg of:

• • R₁ is selected from the group consisting of:
  • (i) C_1-8 alkyl, and C_1-8 alkyl substituted by substituent(s) independently selected from the group consisting of:
    • halogen
    • C_1-5 alkoxy,
    • C_1-5 alkoxy substituted by carbocyclic aryl,
    • carbocyclyl,
    • carbocyclic aryl,
    • carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of:
      • halogen,
      • nitro, and
    • C_1-5 alkoxy,
  • (ii) C_2-5 alkenyl,
  • (iii) carbocyclyl,
  • (iv) carbocyclic aryl, and carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of:
    • halogen,
    • C_1-5 alkyl,
    • C_1-5 alkyl substituted by halogen, and
    • C_1-5 alkoxy;
    • L is Formula (V); and
    • Y is —C(O)O—;
    • wherein carbocyclic aryl is phenyl or naphthyl;
    • carbocyclyl is 9H-fluorenyl or menthyl; and
    • halogen is fluoro, chloro, bromo, or iodo;
  • or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments of the present invention, R_4a is hydrogen or methyl; R_4b is methyl; R₅ and R₆ are hydrogen; A is a single bond; and B is a single bond or —CH₂—; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments, compounds of the present invention are of Formula (I) wherein the compound is selected from the group consisting of:

• cis-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-carbamic acid 2-benzyloxy-ethyl ester;
• cis-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-carbamic acid 4,5-dimethoxy-2-nitro-benzyl ester;
• cis-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-carbamic acid 2-chloro-benzyl ester;
• cis-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-carbamic acid 4,5-dimethoxy-2-nitro-benzyl ester;
• cis-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-carbamic acid 4-nitro-benzyl ester;
• cis-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-carbamic acid benzyl ester;
• cis-[4-(4-dimethylamino-quinazolin-2-ylamino)-cylohexylmethyl]-carbamic acid 2-chloro-benzyl ester;
• cis-[4-(4-dimetlylamino-quinazolin-2-ylamino)-cyclohexylmethyl]-carbamic acid 4-nitro-benzyl ester; and
• cis-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexylmethyl]-carbamic acid benzyl ester;
  • or a phannaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments of the present invention, R₁ is C_1-8 alkyl, and

• • C_1-8 alkyl substituted by substituent(s) independently selected from the group consisting of:
    • carbocyclic aryl,
    • carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of:
      • halogen,
      • C_1-5 alkyl,
      • C_1-5alkyl substituted by halogen,
      • C_1-5 alkoxy, and
      • C_1-5 alkoxy substituted by halogen,
  • R₄ is —N(R_4a)(R_4b) wherein R_4a and R_4b are independently C_1-5 alkyl;
  • L is Formula (III) or (IX) wherein R₅ and R₆ are both hydrogen; A and B are each independently a single bond or —CH₂—; and
  • Y is a single bond;
  • wherein carbocyclic aryl is phenyl; and
  • halogen is fluoro or chloro;
  • or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodinments of the present invention, R₁ is C_1-8 alkyl, and

• • C_1-8 alkyl substituted by substituent(s) independently selected from the group consisting of:
    • carbocyclic aryl,
    • carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of:
      • C_1-5 alkoxy, and
      • C_1-5 alkoxy substituted by halogen,
  • wherein carbocyclic aryl is phenyl; and
  • halogen is fluoro or chloro;
  • or a phan-naceutically acceptable salt, hydrate or solvate thereof

In some embodiments of the present invention, R₄ is —N(CH₃)₂; L is Formula (VIII) or (IX) wherein A is a single bond and B is —CH₂—, or A is —CH₂— and B is a single bond; and Y is a single bond; wherein carbocyclic aryl is phenyl; and halogen is fluoro; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments, compounds of the present invention are of Formula (I) wherein the compound is selected from the group consisting of:

• • N²-[(1S,3R)-3-({[4-bromo-2-(trifluoromethoxy)benzyl]amino}-methyl)cyclopentyl]-N¹,N⁴-dimethylquinazoline-2,4-diamine;
  • or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments of the present invention, R₁ is selected from the group consisting of:

• • (i) C_1-8 alkyl, and C_1-8 alkyl substituted by substittlent(s) independently selected from the group consisting of:
    • carbocyclic aryl,
    • carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of:
      • hydroxy,
      • halogen,
      • nitro,
      • C_1-5 alkylcarbonylamino,
      • C_3-6 cycloalkylcarbonylamino,
      • C_1-5 alkyl,
      • C_1-5 alkyl substituted by halogen,
      • C_1-5 alkylsulfonyl,
      • C_1-5 alkoxy,
      • C_1-5 alkoxy substituted by halogen, and carbocyclic aryl,
    • heterocyclyl, and
    • heterocyclyl substituted by halogen,
  • (ii) C_3-12 cycloalkyl, and C_3-12 cycloalkyl substituted by carbocyclic aryl,
  • (iii) carbocyclyl, and carbocyclyl by substittent(s) independently selected from the group consisting of:
    • hydroxy, and
    • carbocyclic aryl,
  • (iv) carbocyclic aryl, and carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of:
    • halogen,
    • C_1-5 alkoxy, and
    • nitro,
  • (v) heterocyclyl, and heterocyclyl substituted by substituent(s) independently selected from the group consisting of:
    • halogen, and
    • C_1-5 alkoxy,
  • R₄ is —N(R_4a)(R_4b) wherein R_4a and R_4b are each independently C_1-5 alkyl;
  • L is Formula (XIII); wherein R₅ and R₆ are both hydrogen; A is a single bond and B is a single bond or —CH₂—; and
  • Y is —C(O)NR₇—, wherein R₇ is hydrogen or C_1-5 alkyl;
    • wherein carbocyclic aryl, is phenyl or naphthyl;
    • carbocyclyl is indanyl, 9H-fluorenyl, 1,2,3,4-tetralhydro-naphthalen-1-yl, or 1H-indolyl;
    • heterocyclyl is benzo[1,3]dioxolyl, pyridyl, dibenzofuranyl, 1H-benzoimidazolyl, or thiazolyl; and
    • halogen is fluoro, chloro, bromo, or iodo;
  • or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments of the present invention, R₁ is selected from the group consisting of:

• • (i) C_1-8 alkyl, and C_1-8 alkyl substituted by substituent(s) independently selected from the group consisting of:
    • carbocyclic aryl,
    • carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of:
      • hydroxy,
      • halogen,
      • nitro,
      • _1-5 alkylcarbonylamino,
      • C_1-5 alkyl,
      • C_1-5 alkyl substituted by halogen,
      • C_1-5 alkylsulfonyl,
      • C_1-5 alkoxy,
      • C_1-5 alkoxy substituted by halogen, and
      • carbocyclic aryl,
    • hleterocyclyl, and
    • heterocyclyl substituted by halogen,
  • (ii) C_3-12 cycloalkyl, and C₃-₁₂ cycloalkyl substituted by carbocyclic aryl,
  • (iii) carbocyclyl,
  • (iv) carbocyclic aryl, and carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of:
    • halogen, and
    • nitro,
  • (v) heterocyclyl, and heterocyclyl substituted by substituent(s) independently selected from the group consisting of:
    • halogen, and
    • C_1-5 alkoxy,
    • wherein carbocyclic aryl is phenyl or naphthyl;
    • carbocyclyl is indanyl, 9H-fluorenyl, or 1,2,3,4-tetrahydro-naphthalen-1-6l;
    • heterocyclyl is benzo[1,3]dioxolyl, or pyridyl; and
    • halogen is fluoro, chloro, bromo, or iodo;
  • or a pharmacetically acceptable salt, hydrate or solvate thereof.

In some embodiments of the present invention, R₄ is —N(CH₃)₂; A and B are both a single bond; and Y is —C(O)NH—; or a pliarmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments, compounds of the present invention are of Formula (I) wherein the compound is selected from the group consisting of:

• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(2,3-dimethylbenzyl)-cyclohexanecarboxamide;
• cis-N-(2-bromobenzyl)-4-((4-(dimethylamino)quinazolin-2-yl]amino3-cyclohexanecarboxamide;
• cis-N-(2-chlorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino)-N-(4-methylbenzyl)-cyclohexanecarboxamide;
• cis-N-[3,5-bis(trifluoromethyl)benzyl]-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-N-(2,4-dimethoxybenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(1,2,3,4-tetrahydronaphthalen-1-yl)cyclohexanecarboxamide;
• cis-N-(2,3-dihydro-1H-inden-2-yl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[(1S)-1-(4-nitrophenyl)ethyl]-cyclohexanecarboxamide;
• cis-N-(3,5-dichlorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cris-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[4-(trifluoromethoxy)benzyl]-cyclohexanecarboxamide;
• cis-N-(4-bromobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(4-methoxybenzyl)-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(2-fluoro-4-nitrophenyl)-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(3-fluoro-4-methylbenzyl)-cyclohexanecarboxamide;
• cis-N-(5-chloro-2-methylbenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; and
• cis-N-(2,4-dichloro-6-methylbenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
  • or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments, compounds of the present invention are of Formula (I) wherein the compound is selected from the group consisting of:

• cis-N-(2,3-dimethoxybenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-N-(2,4-difluorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxaniide;
• cis-N-(2,4-dichlorobenzyl)-4-}[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-N-(2,3-dichlorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-N-(2,5-dichlorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-N-(33-chlorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(3-methoxybenzyl)-cyclohexanecarboxamide;
• cis-N-(3,4-dimethoxybenzyl)-4-}[4-(dimethylamino)quinazolin-2-yl]amino}-cyclolhexanecarboxamide;
• cis-N-(3,5-dimethoxybenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(4-hydroxy-3-methoxybenzyl)-cyclohexanecarboxamide
• cis-N-(1,3-benzodioxol-5-ylmetlhyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[(1R)-1-(4-nitrophenyl)ethyl]-cyclohexanecarboxamide;
• cis-4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexanecarboxylic acid (trans-2-phenylcyclopropyl)-amide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[(1S)-1-(4-methylphenyl)ethyl]-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[(1R)-1-(1-naphthyl)ethyl]-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[3-(trifluoromethyl)benzyl]-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(3-methoxyphenyl)-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(3-iodobenzyl)-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(4-methoxybenzyl)-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(3-iodophenyl)-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[3-(propionylamino)benzyl]-cyclohexanecarboxamide;
• cis-N-benzyl-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide;
• cis-N-[(6-chloropyridin-3-yl)methyl]-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[(1R)-1-(3-mnethoxyphenyl)ethyl]-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[1-(4-fluorophenyl)ethyl]-cyclohexanecarboxamide:
• cis-N-[(1R)-1-(4-chlorophenyl)ethyl]-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-N-[1-(4-bromophenyl)ethyl]-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[(1S)-1-(1-naphthyl)ethyl]-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(3,5-dimethylbenzyl)-cyclohexanecarboxamide:
• cis-N-(3-chloro-2-methylbenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(5-fluoro-2-methylbenzyl)-cyclohexanecarboxamide:
• cis-N-(3-chloro-2,6-difluorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-N-(biphenyl-3-ylmethyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-N-(biphenyl-4-ylmethyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-N-(6-chloro-2-fluoro-3-methylbenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(2-fluorobenzyl)-cyclohexanecarboxamide;
• cis-N-(2,6-difluorobenzyl)-4-{[4-(dimethylamino)quinazoin-2-yl]amino}-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[4-(trifluoromethyl)benzyl]-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(1-naphthylmethyl)-cyclohexanecarboxamide;
• cis-N-(4-chlorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-N-(3,4-dichlorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(3-fluorobenzyl)-cyclohexanecarboxamide;
• cis-N-(2,5-difluorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-N-(2,3-difluorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-N-(3-bromobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-N-(3-bromo-4-fluorobenzyl)-4-}[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-N-(4-bromo-2-fluorobenzyl)4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-N-(5-bromo-2-fluorobenzy)-{[4-(dimethylamino)quinazolin-2-yl]amino)-cyclohexanecarboxamide:
• cis-N-(4-chloro-2-fluorobenzyl)-4-[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-4-{(4-(dimethylamino)quinazolin-2-yl]amino}-N-(3-methylbenzyl)-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(2-methylbenzyl)-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[2-(trifluorometioxy)benzyl]-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(2,3,4-trifluorobenzyl)-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(2,4,5-trifluorobenzyl)-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(3,4,5-tirifluorobenzyl)-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(2,3,6-trifluorobenzyl)-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[3-fluoro-5-(trifluoromethyl)benzyl]-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[4-fluoro-2-(trifluoromethyl)benzyl]-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[2-fluoro-4-(trifluoromethyl)benzyl]-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[4-fluoro-3-(trifluoromethyl)benzyl]-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[2-fluoro-3-(trifluoromethyl)benzyl]-cyclohexanecarboxamide;
• cis-N-[4-chloro-3-(trifluoromethyl)benzyl]-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboamide;
• cis-N-(2-chloro-6-fluorobenzyl)-4-{[4-(dimethylamino)quinazolinl-2-yl]amino}-cyclohexanecarboxamide;
• cis-N-(3-chloro-4-fluorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-N-(2-chloro-4-fluorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino -cyclohexanecarboxamide;
• cis-N-[2-chloro-5-(trifluoromethyl)benzyl]-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-N-[2-(difluoromethoxy)benzyl]-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-N-[3-(difluoromethoxy)benzyl]-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[3-(trifluoromethoxy)benzyl]-cyclohexanecarboxamide;
• cis-N-(2,6-dimethoxybenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[(1R)-1-phenylethyl]-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[(1S)-1-(4-methoxyphenyl)ethyl)-cyclohexanecarboxamide;
• cis-1-[bis(4-methoxyphenyl)methyl]-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[2-(trifluoromethyl)benzyl]-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-1-yl]amino}-N-9H-fluoren-9-ylcyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[4-(methylsulfonyl)benzyl]-cyclohexanecarboxamide; and
• cis-N-(6-chloropyridin-3-yl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}- cyclohexanecarboxamide;
  • or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments of the present invention, R₁ is selected from the group consisting of:

• • (i) C_1-5 alkyl, and
  • C_1-5 alkyl substituted by substituent(s) independently selected from the group consisting of:
    • carbocyclic aryl,
    • carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of:
      • C_1-5 alkoxy, and
      • C_1-5 alkoxy substituted by halogen,
  • (ii) carbocyclic aryl, and carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of:
    • halogen, and
    • C_1-7 alkoxy,
  • R₄ is —N(R_4a)(R_4b) wherein R_4a and R_4b are each independently C_1-5 alkyl;
  • L is Formula (XIII) wherein R₅ is hydrogen; A is a single bond and B is a single bond or —CH₂—; and
  • Y is —C(O)O— or —OC(O)—;
    • wherein carbocyclic aryl is phenyl or naphityl; and
    • halogen is fluoro, chloro, bromo, or iodo;
  • or a phannaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments of the present invention, R₄ is —N(CH₃)₂; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments of the present invention, R₁ is selected from the group consisting of:

• • carbocyclic aryl, and
  • carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of:
    • halogen,
    • C_1-10 alkyl,
  • C_1-10 alkyl substituted by halogen,
    • C_1-7 alkoxy, and
    • C_1-7 alkoxy substituted by halogen,
  • R₄ is —N(R_4a)(R_4b) wherein R_4a and R_4b are each independently C_1-5 alkyl;

L is Formula (VI) or (IX) wherein A and B are each independently a single bond or —CH₂—; and

• • Y is —C(O)—,
    • wherein carbocyclic aryl is phenyl; and
    • halogen is fluoro, chloro, bromo, or iodo;
  • or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments of the present invention, R₄ is —N(CH₃)₂; R₅ and R₆ are both hydrogen; and A is a single bond, and B is —CH₂—; or A is a —CH₂—, and B is a single bond, or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments, compounds of the present invention are of Formula (I) wherein the compound is selected from the group consisting of:

• 3,4-dichloro-N-[((1R,3S)-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclopentyl)-methyl]benzamide;
• N-[(1S,3R)-3-({[4-(dimethylamino)quinazolin-2-yl]amino}methyl)cyclopentyl]-4-fluorobenzamide;
• 4-chloro-N-[((1R,3S)-3-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclopentyl)methlyl]-benzamide; and
• N-[((1R,3 S)-3-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclopentyl)methyl]-3,5-difluorobenzamide;
  • or a pharmaceutically acceptable salt. hy,drate or sol03te thereof

In some embodiments, compounds of the present invention are of Formula (I) wherein the compound is selected from the group consisting of:

• N-[((1R,3S)-3-{(4-(dimethylamino)quinazolin-1-yl]amino}cyclopentyl)methyl]-3,5-dimethoxybenzamide;
• 2,4,6-trichloro-N-[((1R,3S)-3-{(4-(dimethylamino)quinazolin-2-yl]amino}cyclopentyl)-methyl]benzamide;
• N-[((1R,3S)-3-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclopentyl)methyl]-3-fluoro-4-(trifluoromethyl)benzamide;
• N-[((1R,3S)-3-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclopentyl)methyl]-4-(trifluoromethoxy)benzamide; and
• N-[(1S,3R)-3-({[4-(dimethylamino)quinazolin-2-yl]amino}methyl)cyclopentyl]-2,4-difluorobenzamide;
  • or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments of the present invention, Q is Formula (Ila) and can be represented by the following formula: or a pharmaceutically acceptable salt, hydrate or solvate thereof, wherein X₁-X₄, R₂, L, Y, and R₁ are as described herein, supra and infra.

In some embodiments of the present invention, R₁ is selected from the group consisting of:

• • (i) C_1-8 alkyl, and C_1-8 alkyl substituted by carbocyclic aryl,
  • (ii) carbocyclic aryl, and carbocyclic aryl substitited by subttituent(s) independently selected from the group consisting of:
    • halogen,
    • C_1-10 alkyl,
    • C_1-10 alkyl substituted by halogen,
    • C_1-7 alkoxy, and
    • C_1-7 alkoxy substituted by halogen,
  • R₂ is —N(R_2a)(R_2b), wherein R_2a and R_2b are each independently C_1-5 alkyl;
  • L is Formula (V) wherein R₅ and R₆ are both hydrogen; A and B are both a single bond;
  • X₁, X₂, X₃ and X₄ are independently selected from the group consisting of hydrogen, halogen, and C_1-4 alkyl; provided that at least one substituent selected from the group consisting of X₁, X₂, X₃ and X₄ is not hydrogen; and
  • Y is —C(O)—;
    • wherein carbocyclic aryl is phenyl; and
    • halogen is fluoro, chloro, bromo, or iodo;
  • or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments of the present invention, R₂ is —N(CH₃)₂; and X₁, X₂, X₃ and X₄ are independently selected from the group consisting of hydrogen, fluoro, and methyl; provided that at least one substituent selected from the group consisting of X₁, X₂, X₃ and X₄ is not hydrogen; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments, compounds of the present invention are of Formula (I) wherein the compound is selected from the group consisting of:

• N-(cis-4-{[4-(dimethylamino)-6-methylquinazolin-2-yl]amino}cyclohexyl)-2,2-diphenylacetamide;
• N-(cis-4-{[4-(dimethylamino)-6-methylquinazolin-2-yl]amino}cyclohexyl)-4-fluoro-3-(trifluoromethyl)benzamide;
• N-(cis-4-{[4-(dimethylamino)-6-methylquinazolin-2-yl]amino}cyclohexyl)-3,5-bis(trifluoromethyl)benzamide; and
• N-(cis-4-{[4-(dimethylamino)-6-methylquinazolin-2-yl]amino}cyclohexyl)-3,4,5-trimethoxybenzamide;
• or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments, compounds of the present invention are of Formula (I) wherein the compound is selected from the group consisting of:

• 3-chloro-N-(cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexyl)-benzamide;
• 3,4-dichloro-N-(cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexyl)-benzamide;
• N-(cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolini-2-yl]amino}cyclohexyl)-3,5-dimethoxybenzamide;
• N-(cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexyl)benzamide;
• N-(cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexyl)-4-methylbenzamide;
• N-(cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-ylamino}cyclohexyl)-4-fluorobenzamide;
• N-(cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexyl)-3-methoxybenzamide;
• N-(cis4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexyl)-3,4-difluorobenzamide; and
• N-(cis-4-{[4-(dimetilylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexyl)-3-trifluoromethyl)benzamide; or a pliamiacetitically acceptable salt, hydrate or solvate thereof.

In some embodiments of the present invention, R₁ is selected from the grouip consisting of:

• • (i) C_1-8 alkyl, and
  • C_1-8 alkyl substituted by substituent(s) independently selected from the group consisting of:
    • carbocyclic aryl,
    • carbocyclic aryl substituted by substituent(s) independently selected from the group consistinig of:
      • halogen,
      • C_1-5 alkyl,
      • C_1-5 alkyl substituted by halogen,
      • C_1-5 alkoxy, and
      • C_1-5 alkoxy substituted by halogen,
  • (ii) heterocyclyl, and heterocyclyl substituted by halogen,
  • R₂ is —N(R_2a)(R_2b), wherein R_2a and R_2b are each independently C_1-5 alkyl;
  • L is Formula (XIII);
  • X₁, X₂, X₃ and X₄ are independently hydrogen or halogen; provided that at least one substituent selected from the group consisting of X₁, X₂, X₃ and X₄ is not hydrogen; and
  • Y is —C(O)NR₇— wherein R₇ is hydrogen or C_1-5 alkyl;
    • wherein carbocyclic aryl is phenyl;
    • heterocyclyl is pyridyl; and
    • halogen is fluoro, chloro, bromo, or iodo;
  • or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments of the present invention, R₂ is —N(CH₃)₂; L is Formula (XIII) wherein A and B are both a single bond; X₁, X₂, X₃ and X₄ are independently hydrogen or fluoro; provided that at least one stibstittieit selected from the group consisting of X₁, X₂, X₃ and X₄ is not hydrogen; and Y is —C(O)NH—; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments, compounds of the present invention are of Formula (I) wherein the compound is selected from the group consisting of:

• cis-N-benzyl-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-N-(3,5-dimethoxybenzyl)-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl-]amino}-N-(3-methoxybenzyl)-cyclohexanecarboxamide;
• cis-N-[(6-chloropyridin-3-yl)methyl]-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]-amino}cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-N-[3-(trifluoromethyl)-benzyl]cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-N-[4-(trifluoromethyl)-benzyl]cyclohexanecarboxamide;
• cis-N-[3,5-bis(trifluoromethyl)benzyl]-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-N-(3-iodobenzyl)-cyclohexanecarboxamide; and
• cis-N-[1-(4-bromophenyl)ethyl]-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexanecarboxamide;
• or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments, compounds of the present invention are of Formula (I) wherein the compound is selected from the group consisting of:

• cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-N-(4-methylbenzyl)-cyclohexanecarboxamide;
• cis-N-(3-chlorobenzyl)-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-N-[(1R)-1-(3-methoxyphenyl)ethyl]cyclohexanecarboxamide;
• cis-4-({4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-N-(4-methoxybenzyl)-cyclohexanecarboxamide;
• cis-N-(2,4-dichlorobenzyl)-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-N-(3,5-dichlorobenzyl)-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-N-(4-bromobenzyl)-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-N-(2-bromobenzyl)-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-cyclohexanecarboxamide;
• cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-N-(4-(trifluoromethoxy)-benzyl]cyclohexanecarboxamide; and
• cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-N-[(1S)-1-(4-methylphenyl)ethyl]cyclohexanecarboxamide,

or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments of the present invention, Q is Formula (IIb) and can be represented by the following formula: or a pharmaceutically acceptable salt, hydrate or solvate thereof, wherein R₃, L, Y, and R₁ are as described herein, supra and infra.

In some embodiments of the present invention, R₁ is selected from the group consisting of:

• • R₁ is selected from the group consisting of:
  • C_1-8 alkyl, and
  • C_1-8 alkyl substituted by substituent(s) independently selected from the group consisting of:
    • carbocyclic aryl,
    • carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of:
      • halogen,
      • C_1-5 alkyl, and
      • C_1-5 alkoxy,
  • R₃ is C_1-5 alkyl;
  • L is Formula (XIII); whereiii R₅ and R₆ are both hydrogen; A and B are both a single bond;
  • Y is —C(O)NR₇—;
    • wherein carbocyclic aryl is phenyl; and
    • halogen is fluoro, chloro, bromo, or iodo;
  • or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments of the present invention, R₃ is isopropyl; and Y is —C(O)NH—; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments, compounds of the present invention is:

• cis-N-(3-chlorobenzyl-4-[(4-isopropylquinazolin-2-yl]amino]cyclohexanecarboxamide;

or a pharmaceutically acceptable salt, hydrate or solvate thereof.

In some embodiments of the present invention, R₁ is selected from hydrogen, —CO₂tBu, or —CO₂Bn (Bn is a benzyl group);

• • R₂ is —N(R_2a)(R_2b), wherein R_2a is hydrogen or C_1-5 alkyl; R2b is C_1-5 alkyl;
  • R₃ is C_1-5 alkyl;
  • R₄ is —N(R_4a)(R_4b) wherein R_4a is hydrogen or C_1-5 alkyl; R_4b is C_1-5 alkyl;
  • L is selected from Formula (V), (VIII), (IX), (XIII), (XVI), or (XVII);
  • X₁, X₂, X₃ and X₄ are independently selected from the group consisting of hydrogen, halogen, and C_1-4 alkyl; provided that at least one substituent selected from the group consisting of X₁, X₂, X₃ and X₄ is not hydrogen; and
  • Y is a single bond;
  • or a pharmaceutically acceptable salt, hydrate, or solvate thereof.

One aspect of the present invention pertains to pharmaceutical compositions comprising at least one compounds as described herein, in combination with a pharmaceutically acceptable carrier.

One aspect of the present invention pertains to methods for the prophylaxis or treatment of improving memory function, sleeping and arousal, anxiety, depression, mood disorders, seizure, obesity, diabetes, including bulimia, anorexia, mental disorders including manic depression, schizophrenia, delirium, appetite and eating disorders, cardiovascular disease, hypertension, dyslipidemia, myocardialinfarction, binge eating disorders dementia, stress, cognitive disorders, attention deficit disorder, substance abuse disorders and dyskinesias including Parkinson's disease, epilepsy, and addiction comprising administering to an individual suffering from the condition a therapeutically effective amount of a compound, as described herein, or a pharmaceutical composition thereof.

One aspect of the present invention pertains to methods for the prophylaxis or treatment of an eating disorder, obesity or an obesity related disorder comprising administering to an individual suffering from the condition a therapeutically effective amount of a compound, as described herein, or a pharmaceutical composition thereof.

One aspect of the present invention pertains to methods for the prophylaxis or treatment of anxiety, depression, schizophrenia, addiction, or epilepsy comprising administering to an individual suffering from the condition a therapeutically effective amount of a compound, as described herein, or a pharmaceutical composition.

One aspect of the present invention pertains to compounds of the present invention, as described herein, or a pharmaceutical composition thereof, for use in a method of treatment of the human or animal body by therapy.

One aspect of the present invention pertains to compounds of the present invention, as described herein or a pharmaceutical composition thereof, for use in a method of prophylaxis or treatment of an eating disorder, obesity or an obesity related disorder of the human or animal body by therapy.

One aspect of the present invention pertains to compounds of the present invention, as described herein, or a pharmaceutical composition thereof, for use in a method of prophylaxis or treatment of anxiety, depression, schizophrenia, addiction, or epilepsy of the human or animal body by therapy.

One aspect of the present invention pertains to compounds of the present invention, as described herein, for the manufacture of a medicament for use in the prophylaxis or treatment of an eating disorder obesity or obesity related disorders.

One aspect of the present invention pertains to compounds of the present invention, as described herein, for the manufacture of a medicament for use in the prophylaxis or treatment of anxiety, depression, schizophrenia, addiction, or epilepsy.

One aspect of the present invention pertains to methods of decreasing food intake of an individual comprising administering to the individual a therapeutically effective amount of a compound, as described herein, or a pharmaceutical composition thereof.

One aspect of the present invention pertains to methods of inducing satiety in an individual comprising administering to said individual a therapeutically effective amount of a compound, as described herein, or a pharmaceutical composition thereof.

One aspect of the present invention pertains to methods of controlling or reducing weight gain in an individual comprising administering to said individual a therapeutically effective amount of a compound, as described herein, or a pharmaceutical composition thereof.

One aspect of the present invention pertains to methods of modulating a MCH receptor in an individual comprising contacting the receptor with a compound, as described herein. In some embodiments, the compound is an antagonist. In some embodiments, the modulation of the MCH receptor is for the prophylaxis or treatment of an eating disorder, obesity or obesity related disorder. In some embodiments, the modulation of the MCH receptor reduces food intake of the individual. In some embodiments, the modulation of the MCH receptor induces satiety in the individual. In some embodiments, the modulation of the MCH receptor controls or reduces iveight gain of the individual. In some embodiments, the modulation of the MCH receptor is for prophylaxis or treatment of anxiety, depression, schizophrenia, addiction, or epilepsy.

In some embodiments, the individual is a mammal.

In some embodiments, the mammal is a human.

In some embodiments, the human has a body mass index of about 18.5 to about 45. In some embodiments, the human has a body mass index of about 25 to about 45. In some embodiments, the human has a body mass index of about 30 to about 45. In some embodiments, the human has a body mass index of about 35 to about 45.

One aspect of the present invention pertains to methods of producing a pharmaceutical composition comprising admixing a compound, as described herein, and a pharmaceutically acceptable carrier.

One embodiment of the invention includes any compound of the invention which selectively binds an MCH receptor, such selective binding is preferably demonstrated by a Ki for one or more other GPCR(s), preferably NPY, being at least 10-fold greater than the Ki for any particular MCH receptor, preferable MCHR1.

As used herein, the term “alkyl” is intended to denote hydrocarbon compounds including straight chain and branched chain, including for example but not limited to methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, tert-butyl, n-pentyl, isopentyl, tert-pentyl, n-hexyl, and the like.

The term “alkoxy” is intended to denote substituents of the formula —O-alkyl.

At various places in the present specification substituents of compounds of the invention are disclosed in groups. It is specifically intended that the invention include each and every individual subcombination of the members of such groups.

G-protein coupled receptors (GPCRs) represent a major class of cell surface receptors with which many neurotransmitters interact to mediate their effects. GPCRs are predicted to have seven membrane-spanning domains and are coupled to their effectors via G-proteins linking receptor activation with intracellular biochemical sequelae such as stimulation of adenylyl cyclase. Melanin Concentrating Hormone (MCH), a cyclic peptide, has been identified as the endogenous ligand of the orphan G-protein coupled receptor SLC-1. See, for example. Shimomura et al., Biochem. Biophys. Res. Commun. 261, 622-26 (1999). Studies have indicated that MCH acts as a neurotransmitter/modulator/regulator to alter a number of behavioral responses.

Mammalian MCH (19 amino acids) is highly conserved between rat, mouse, and human, exhibiting 100% amino acid identity, but its physiological roles are less clear. MCH has been reported to participate in a variety of processes including feeding, water balance, energy metabolism, general arousal/attention state, memory and cognitive functions, and psychiatric disorders. For reviews, see 1. Baker, Int. Rev. Cytol. 126:1-47 (1991); 2. Baker, TEM 5:120-126 (1994); 3. Nahon, Critical Rev. in Neurobiol 221:21-262, (1994); 4. Knigge et al., Peptides 18(7):1095-1097, (1996). The role of MCH in feeding or body weight regulation is supported by Qu et al., Nature 380:243-247, (1996), demonstrating that MCH is over expressed in the hypothalamus of ob/ob mice compared with ob/+mice, and that fasting further increased MCH mRNA in both obese and normal mice during fasting. MCH also stimulated feeding in normal rats when injected into the lateral ventricles as reported by Rossi et al., Endocrinology 138:351-355, (1997). MCH also has been reported to functionally antagonize the behavioral effects of α-MSH; see: Miller et al., Peptides 14:1-10, (1993); Gonzalez et al, Peptides 17:171-177, (1996); and Sanchez et al., Peptides 18:3933-396, (1997). In addition, stress has been shown to increase POMC mRNA levels while decreasing the MCH precursor preproMCH (ppMCH) mRNA levels; Presse et al., Endocrinology 131:1241-1250, (1992). Thus MCH can serve as an integrative neuropeptide involved in the reaction to stress, as well as in the regulation of feeding and sexual activity; Baker, Int. Rev. Cytol. 126:1-47, (1991): Knigge et al., Peptides 17:1063-1073, (1996).

The localization and biological activities of MCH peptide suggest that the modulation of MCH receptor activity can be useftil in a number of therapeutic applications. MCH is expressed in the lateral hypothalamus, a brain area implicated in the regulation of thirst and hunger: Grillon et al., Neuropeptides 31:131-136, (1997); recently orexins A and B, which are potent orexigenic agents, have been shown to have very similar localization to MCH in the lateral hypothalamus; Sakurai et al., Cell 92:573-585 (1998). MCH mRNA levels in this brain region are increased in rats after 24 hours of food-deprivation; Herve and Fellmann, Neurpeptides3l :237-242 (1997); after insulin injection, a significant increase in the abundance and staining intensity of MCH immunoreactive perikarya and fibres was observed concurrent with a significant increase in the level of MCH mRNA; Bahjaoui-Bouhaddi et al., Neuropeptides 24:251-258(1994). Consistent with the ability of MCH to stimulate feeding in rats; Rossi et al., Endocrinology 138:351-355, (1997); is the observation that MCH mRNA levels are upregulated in the hypothalami of obese ob/ob mice; Qu et al., Nature 380:-743-247, (1996); and decreased in the hypothalami of rats treated with leptin, whose food intake and body weight gains are also decreased; Sahu, Endocrinology 139:795-798, (1998), MCH appears to act as a functional antagonist of the melanocortin system in its effects on food intake and on hormone secretion within the HPA (hypothalamopituitary/adrenal axis); Ludwig et al. Am. J. Physiol. Endocrinol. Metab. 274:E627-E633, (1998). Together these data suggest a role for endogenous MCH in the regulation of energy balance and response to stress, and provide a rationale for the development of specific compounds acting at MCH receptors for use in the treatment of obesity and stress-related disorders.

Accordingly, a MCH receptor antagonist is desirable for the prophylaxis or treatment of obesity or obesity related disorders. An obesity related disorder is a disorder that has been directly or indirectly associated to obesity, such as, type II diabetes, syndrome X, impaired glucose tolerance, dyslipidaemia, hypertension, coronary heart disease and other cardiovascular disorders including atherosclerosis, insulin resistance associated with obesity and psoriasis, for treating diabetic complications and other diseases such as polycystic ovarian syndrome (PCOS), certain renal diseases including diabetic nephropathy, glomerulonepliritis, glomerular sclerosis, neplirotic syndrome, hypertensive nephrosclerosis, end-stage renal diseases and microalbuminuria as Nvell as certain eating disorders.

In species studied to date, a major portion of the neurons of the MCH cell group occupies a rather constant location in those areas of the lateral hypothalamus and subthalamus where they lie and may be a part of some of the so-called “extrapyramidal” motor circuits. These involve substantial striato- and pallidofugal pathways involving the thalamus and cerebral cortex, hypothalamic areas, and reciprocal connections to subthalamic nucleus, substantia nigia, and mid-brain centers. Bittencourt et al., J. Comp. Neurol. 319:218-245, (1992). In their location, the MCH cell group may offer a bridge or mechanism for expressing hypothalamic visceral activity with appropriate and coordinated motor activity. Clinically it can be of some value to consider the involvement of this MCH system in movement disorders, such as Parkinson's disease and Huntingdon's Chorea in which extrapyramidal circuits are known to be involved.

Human genetic linkage studies have located authentic hMCH loci on chromosome 12 (12q23-24) and the variant hMCH loci on chromosome 5 (5q12-13) (Pedeutour et al., 1994). Locus 12q23-24 coincides with a locus to which autosomal dominant cerebellar ataxia type II (SCA2) has been mapped; Auburger et al., Cytogenet. Cell. Genet. 61:252-256 (1992); Twells et al., Cytogenet. Cell. Genet. 61:262-265, (1992). This disease comprises neurodegenerative disorders, including an olivopontocerebellar atrophy. Furthermore, the gene for Darier's disease, has been mapped to locus 12q23-24; Craddock et al., Hum. Mol. Genet. 2:1941-1943, (1993). Dariers' disease is characterized by abnormalities I keratinocyte adhesion and mental illnesses in some families. In view of the functional and neuroanatomical patterns of the MCH neural system in the rat and human brains, the MCH gene can represent a good candidate for SCA2 or Darier's disease. Interestingly, diseases with high social impact have been mapped to this locus. Indeed, the gene responsible for chronic or acute forms of spinal muscular atrophies has been assigned to chromosome 5q12-13 using genetic linkage analysis; Melki et al., Nature (London) 344:767-768, (1990); Westbrook et al., Cytogenet. Cell. Genet. 61:225-231, (1992). Furthermore, independent lines of evidence support the assignment of a major schizophrenia locus to chiomosome 5q11.2-13.3; Sherrington et al., Nature (London) 336:164-167, (1988); Bassett et al., Lancet 1:799-801, (1988); Gilliam et al., Genomics 5:940-944, (1989). The above studies suggest that MCH can play a role in neurodegenerative diseases and disorders of emotion.

Additional therapeutic applications for MCH-related compounds are suggested by the observed effects of MCH in other biological systems. For example, MCH can regulate reproductive functions in male and female rats. MCH transcripts and MCH peptide were found within germ cells in testes of adult rats, suggesting that MCH can participate in stem cell renewal and/or differentiation of early spemlatocytes; Hervieu et al., Biology of Reduction 54:1161-1172, (1996). MCH injected directly into the medial preoptic area (MPOA) or ventromedial nucleus (VMN) stimulated sexual activity in female rats; Gonzalez et al., Peptides 17:171-177, (1996). In ovariectomized rats primed with estradiol, MCH stimulated luteinizing hormone (LH) release while anti-MCH antiserum inhibited LH release; Gonzalez et al., Neuroendocrinology 66:254-262, (1997). The zona incerta, which contains a large population of MCH cell bodies, has previously been identified as a regulatory site for the pre-ovulatory LH surge; MacKenzie et al., Neuroendocrinology 39:289-295, (1984). MCH has been reported to influence release of pituitary hormones including ACTH and oxytocin. MCH analogues can also be useful in treating epilepsy. In the PTZ seizure model, injection of MCH prior to seizure induction prevented seizure activity in both rats and guinea pigs, suggesting that MCH-containing neurons can participate in the neural circuitry underlylng PTZ-induced seizure; Knigge and Wagner, Peptides 18:1095-1097, (1997). MCH has also been observed to affect behavioral correlates of cognitive functions. MCH treatment hastened extinction of the passive avoidance response in rats; McBride et al., Peptides 15:757-759, (1994); raising the possibility that MCH receptor antagonists can be beneficial for memory storage and/or retention. A possible role for MCH in the modulation or perception of pain is supported by the dense innervation of the periaqueductal grey (PAG) by MCH-positive fibers. Finally, MCH can participate in the regulation of fluid intake. ICV infusion of MCH in conscious sheep produced diuretic, natriuretic, and kaliuretic changes in response to increased plasma volume; Parkes, J. Neuroendocrinol. 8:57-63, (1996). Together with anatomical data reporting the presence of MCH in fluid regulatory areas of the brain, the results indicate that MCH can be an important peptide involved in the central control of fluid homeostasis in mammals.

In a recent citation MCHR1 antagonists surprisingly demonstrated their use as an anti-depressants and/or anti-anxiety agents. MCHR1 antagonists have been reported to show antidepressant and anxiolytic activities in rodent models, such as, social interaction, forced swimming test and ultrasonic vocalization. Therefore, MCHR1 antagonists could be useful to independently treat subjects with depression and/or anxiety. Also, MCHR1 antagonists could be useful to treat subjects that suffer from depression and/or anxiety and obesity.

This invention provides a method of treating an abnormality in a subject wherein the abnormality is alleviated by decreasing the activity of a mammalian MCCH1 receptor which comprises administering to the subject an amount of a compound which is a mammalian MCH1 receptor antagonist effective to treat the abnomnality. In separate embodiments, the abnormality is a regulation of a steroid or pituitary hormone disorder, an epinephrine release disorder, an anxiety disorder, genta gastrointestinal disorder, a cardiovascular disorder, an electrolyte balance disorder, hypertension, diabetes, a respiratory disorder, asthma, a reproductive function disorder, an immune disorder, an endocrine disorder, a musculoskeletal disorder, a neutroendocrine disorder, a cognitive disorder, a memory disorder, a sensory modulation and transmission disorder, a motor coordination disorder, a sensory integration disorder, a motor integration disorder, a dopaminergic function disorder, a sensory transmission disorder, an olfaction disorder, a sympathetic innervation disorder, an affective disorder, a stress-related disorder, a fluid-balance disorder, a seizure disorder, pain, psychotic behavior, morphine tolerance, opiate addiction or migraine.

Compositions of the invention can conveniently be administered in unit dosage form and can be prepared by any of the methods well known in the pharmaceutical art, for example, as described in Remington's Pharmaceutical Sciences (Mack Pub. Co., Easton, Pa., 1980).

The compounds of the invention can be employed as the sole active agent in a pharmaceutical or can be used in combination with other active ingredients which could facilitate the therapeutic effect of the compound.

Compounds of the present invention or a solvate or physiologically functional derivative thereof can be used as active ingredients in pharmaceutical compositions, specifically as a MCH receptor antagonists. By the tenn “active ingredient” is defined in the context of a “pharmaceutical composition” and shall mean a component of a pharmaceutical composition tl)at provides the primary phanmaceutical benefit, as opposed to an “inactive ingredient” which would generally be recognized as providing no pharmaceutical benefit. The term “pharmaceutical composition” shall mean a composition comprising at one active ingredient and at least one ingredient that is not an active ingredient (for example and not limitation, a filler, dye, or a mechanism for slow release), whereby the composition is amenable to use for a specified, efficacious outcome in a mammal (for example, and not limitation, a human).

Pharmaceutical compositions, including, but not limited to, pharmaceutical compositions, comprising at least one compound of the present invention and/or an acceptable salt cor solvate thereof (e.g, a pharmaceutically acceptable salt or solvate) as an active ingredient combined with at least one carrier or excipient (e.g., pharmaceutical carrier or excipient) can be used in the treatment of clinical conditions for which a MCH receptor antagonist is indicated. At least one compound of the present invention can be combined with the carrier in either solid or liquid form in a unit dose formulation. The pharmaceutical carrier must be compatible with the other ingredients in the composition and must be tolerated by the individual recipient. Other physiologically active ingredients can be incorporated into the pharmaceutical composition of the invention if desired, and if such ingredients are compatible with the other ingredients in the composition. Formulations can be prepared by any suitable method, typically by uniformly mixing the active compound(s) with liquids or finely divided solid carriers, or both, in the required proportions, and then, if necessary, forming the resulting mixture into a desired shape.

Conventional excipients, such as binding agents, fillers, acceptable wetting agents, tabletting lubricants, and disintegrants can be used in tablets and capsules for oral administration. Liquid preparations for oral administration can be in the form of solutions, emulsions, aqueous or oily suspensions, and syrups. Alternatively, the oral preparations can be in the form of dry powder that can be reconstituted with water or another suitable liquid vehicle before use. Additional additives such as suspending or emulsifying agents, non-aqueous vehicles (including edible oils), preservatives, and flavorings and colorants can be added to the liquid preparations. Parenteral dosage forms can be prepared by dissolving the compound of the invention in a suitable liquid vehicle and filter sterilizing the solution before filling and sealing an appropriate vial or ampoule. These are just a few examples of the many appropriate methods well known in the art for preparing dosage forms.

It is noted that when the MCH receptor antagonists are utilized as active ingredients in a pharmaceutical composition, these are not intended for use only in humans, but in other non-human mammals as well. Indeed, recent advances in the area of animal health-care mandate that consideration be given for the use of MCH receptor antagonists for the treatment of obesity in domestic animals (e.g., cats and dogs), and MCH receptor antagonists in other domestic animals where no disease or disorder is evident (e.g., food-oriented animals such as cows, cihickens, fish, etc.). Those of ordinary skill in the art are readily credited with understanding the utility of such compounds in such settings.

Pharmaceutically acceptable salts of the compounds of the invention can be prepared by reacting the free acid or base forms of these compounds with the appropriate base or acid in water, in an organic solvent, or in a mixture of the two; generally, nonaqueous media like ether, ethyl acetate, ethanol, isopropanol, dioxane, or acetonitrile are preferred. For instance, when the compound (I) possesses an acidic functional group, it can form an inorganic salt such as an alkali metal salt (e.g., sodium salt, potassium salt, etc.), an alkaline earth metal salt (e.g. calcium salt, magnesium salt, barium salt, etc.). and an ammonium salt. When the compound (I) possesses a basic functional group, it can form an inorganic salt (e.g., hydrochloride, sulfate, phosphate, hydrobromate, etc.) or an organic salt (e.g., acetate, maleate, fumarate, succinate, methanesulfonate, p-toluenesulfonate, citrate, tartrate, etc.).

When a compound of the invention contains optical isomers, stereoisomers, regio isomers, rotational isomners, a single substance and a mixture of them are included as a compound of the invention. For example, when a chemical formula is represented as showing no stereochenmical designation(s), such as Formula IV, then all possible stereoisomer, optical isomers and mixtures thereof are considered within the scope of that formula. Accordingly, Formula V, specifically designates the cis relationship between the two amino groups on the coyclohexyl ring and therefore this formula is also fully embraced by Formula IV.

The novel substituted quinazolines of the present invention can be readily prepared according to a variety of synthetic manipulations, all of which would be familiar to one skilled in the art. Preferred methods for the preparation of compounds of the present invention include, but are not limited to, those described in Scheme 1-6.

The common intermediate (F) of the novel substituted quinazolines can be prepared as shown in Scheme 1. Commercially available 1H,3H-quinazoline-2,4-dione (A) is converted to 2,4-dihalo-quinazoline (B) by a halogenating agent with or without a base (wherein X is halogen such as chloro, bromo, or iodo). The halogenating agent includes phosphorous oxychloride (POCl₃), phosphorous oxybromide (POBr₃), or phosphorus pentachloride (PC₃). The base includes a tertiary amine (preferably N,N-diisopropylethylamine etc.) or an aromatic amine (preferably N,N-dimethylaniline, etc.). Reaction temperature ranges from about 100° C. to 200° C., preferably about 140° C. to 180° C.

The halogen of 4-position of 2,4-dihalo-quinazoline (B) is selectively substituted by a primary or secondary amine (HNR_1aR_1b, wherein R_1a and R_1b are as defined above) with or without a base in an inert solvent to provide the corresponding 4-substitued amino adduct (C). The base includes an alkali metal carbonate (preferably sodium carbonate or potassium carbonte, etc.) an alkali metal hydroxide (preferably sodium hydroxide etc.), or a tertiary amine (preferably N,N-diisopropylethylamine, triethylaminem or N-methylmorpholine. etc.). The inert solvent includes lower alkyl alcohol solvents (preferably methanol, ethanol, 2-propanol, or butanol, etc.), ethereal solvents (preferably tetrahydrofuran or dioxane, etc.), or amide solvents (preferably N,N-dimethylformamide or 1-methyl-pyrrolidin-2-one, etc.). Reaction temperature ranges from about 0° C. to 200° C., preferably about 10° C. to 150° C.

In turn, this is substituted by the mono-protected diamine (D), wherein R₅, R₆, A, and B are as defined above and P is a protective group, with or without a base in an inert solvent to provide 2,4-disubstituted amino quinazoline (E). The base includes an alkali metal carbonate (preferably sodium carbonate or potassium carbonate, etc.), an alkali metal hydroxide (preferably sodium hydroxide, etc.), or a tertiary amine (preferably N,N-diisopropylethylamine, triethylamine, or N-methylmorpholine, etc.). The inert solvent includes lower alkyl alcohol solvents (preferably methanol, ethanol, 2-propanol, or butanol, etc.) or amide solvents (preferably N,N-dimethylformamide or 1-methyl-pyrrolidin-2-one, etc.). Reaction temperature ranges from about 50° C. to 200° C. preferably about 80° C. to 150° C. Also this reaction can be carried out under microwvave conditions.

Representative protecting groups suitable for a wide variety of synthetic transformations are disclosed in Greene and Wuts, Protective Groups in Organic Synthesis, second edition, John Wiley & Sons, New York, 1991, the disclosure of which is incorporated herein by reference in its entirety. The deprotection of the protective group leads to the common intermediate (F) of the novel substituted quinazolines.

In another method, compounds of the present invention can be prepared wherein the aromatic ring is further substituted such as when Q is Formula (IIa). This method utilizes the conversion of an appropriately substituted 2-amino benzoic acid to the corresponding substinited 1H,3H-quinazoline-2,4-dione (A′); wherein X₁, X₂, X₃ and X₄ have the same meaning as described herein. Suitable conditions for the conversion to the substituted 1H,3H-quinazoline-2,4-dione (A′) are known in the art, for example, potassium cyanate, sodium cyanate, urea, and the like. In a similar method as described above in Scheme 1, the substituted 1H,3H-quinazoline-2,4-dione (A′) can be converted into useful intermediate (F′) as described generallye in Scheme 1.1

In a similar manner as described herein for intermediate (F), common intermediate (F) can be converted into novel quinazolines of Formula (I), wherein one or more of positions 5, 6, 7 or 8 on the quinazoline ring is/are substituted.

The conversion of the common intermediate (F) to the novel substituted quinazolines (G-1) of the present invention is outlined in Scheme 2.

The novel urea (G) of the present invention can be obtained by urea reaction using an isocyanate (R₁NCO) in an inert solvent with or without a base. The base includes an alkali metal carbonate (preferable sodium carbonate or potassium carbonate, etc.), an alkali metal hydrogencarbonate (preferably sodium hdrogencarbonate or potassium hydrogencarbonate, etc.), an alkali hydroxide (preferably sodium hydroxide or potassium hydroxide, etc.), a tertiary amine (preferably N,N-diisopropylethylamine, triethylamine, or N-methylmorpholine, etc.), or an aromatic amine (preferably pyridine or imidazole, etc.). The inert solvent includes lower halocarbon solvents (preferably dichloromethane, dichloroethane, or chloroform, etc.), ethereal solvents (preferably tetrahydrofuran or dioxane), aromatic solvents (preferably benzene or toluene, etc.), or polar solvents (preferably N,N-dimethylformamide or dimethyl sulfoxide. etc.). Reaction temperature ranges from about −20° C. to 120° C., preferably about 0° C. to 100° C.

The amine (F) is reacted with a isothiocyanate (R₁NCS) in an inert solvent with or without a base to provide the novel thiourea (H) of the present invention. The base includes an alkali metal carbonate (preferably sodium carbonate or potassium carbonate, etc.), an alkali metal hydrogcencarbonate (preferably sodium hydrogencarbonate or potassium hydrogencarbonate, etc.), an alkali hydroxide (preferably sodium hydroxide or potassium hydroxide, etc.), a tertiary amine (preferably N,N-diisopropylethylamine, triethylamine, or N-methylmorpholine, etc.), or an aromatic amine (preferably pyridine or imidazole, etc.). The inert solvent includes lower halocarbon solvents (preferably dichloromethane, dichloroethane, or chlooforn, etc.), ethereal solvents (preferably tetrahydrofuran or dioxane), aromatic solvents (preferably) benzene or toluene, etc.), or amide solvents (preferably N,N-dimethylformamide, etc.). Reaction temperature ranges from about −20° C. to 120° C., preferably about 0° C. to 100° C.

The novel urethane (I) of the present invention can be obtained by urethane reaction using R₁OCOCl, wherein X is halogen such as chloro, bromo, or iodo, in an inert solvent with or without a base. The base includes an alkali metal carbonate (preferably sodium carbonate or potassium carbonate, etc.), an alkali metal hydrogencarbonate (preferably sodium hydrogencarbonate or potassium hydrogencarbonate, etc.), an alkali hydroxide (preferably sodium hydroxide or potassium hydroxide, etc.), a tertiary amine (preferably N,N-diisopropylethylamine, triethylamine, or N-methylmorplioline, etc.), or an aromatic amine (preferably pyridine, imidazole, or poly-(4-vinylpyridine), etc.). The inert solvent includes lower halocarbon solvents (preferably dichloromethane, dichloroethane, or chloroform, etc.), ethereal solvents (preferably tetrahydrofuran or dioxane), aromatic solvents (preferably benzene or toluene, etc.), or polar solvents (preferably N,N-dimethylformamide or dimethyl sulfoxide, etc.). Reaction temperature ranges from about −20° C. to 120° C., preferabIy about 0° C. to 100 C.

Compounds of Formula (K) can be prepared as shown in Scheme 3, [4-(Benzyloxycarbonylamino-methyl)-cyclohexyl]-carbamic acid tert-butyl ester (J) is synthesized by the method which is described in WO 01/72710. The deprotection of Boc-group is achieved by an acid to give the amine. The coupling of the amine with quinazoline core (C), which is synthesized as scheme 1, gives 2,4-disubstituted amino quinazoline. The depiotection of Z-group is achieved by hydrogen reduction to give compounds of Formula (K).

Compounds of Formula (L) can be prepared as shown in Scheme 4. The dicarboxylic acid of commercially available cis-cyclohexane-1,4-dicarboxylic acid is transformed to dibenzyl carbanate by curtius rearrangement. The deprotection of Z-group is achieved by hydrogen reduction to give the diamine. The mono-protection of the diamine can be achieved by the method described in Synthetic communications, 20, 2559-2564 (1990). The coupling of the amine with quinazoline core (C), which is synthesized as scheme 1, gives 2,4disubstituted amino quinazoline. The deprotection of Boc-group is achieved by an acid to give the amine (L).

Compounds of Formula (M) can be prepared as show an in Scheme. This method utilizes 1-protected aminocyclopentane-3-carboxylic acids. The 1-protected aminocyclopentane-3-carboxylic acids that can be used are either commercially available or prepaared using methods known in the art. One particularly useful compound is (1R,3S)-N-Boc-1-aminocyclopentane-3-carboxylic acid. The 1-protected aminocyclopentane-3-carboxylic acid can be converted to the orthogonally protected 1,3-diaminocyclopentane by an arrangement, such as, the Curtius, Hoffman, Lossen, Schmidt, and the like; and subsequently protected. In the Curtius Rearrangement method, the protected amine is generated by subjecting the isocyanate intermediate with an alcohol to give a useful urethane protection group, such as, Boc, Cbz, and the like. In a subsequent step, one protecting group is removed and allowed to react in a similar manner as described herein with intermediate (C) or (C′). depicted as Q-X in Scheme 5. The second protecting group is removed to achieve amine (M).

In a similar manner as described herein for intermediate (F), compound (M) can be converted into novel quinazolines of Formula (I) using methods described herein.

Novel compounds of Formula (N) of the present invention can be prepared as shown in Scheme 6. This method can utilize any of the intemnediate amines, such as amines (F), (F′), (K), (L), and (M). The amine is coupled to a 2-halopyridine carboxylic acid or similar comnpound, such as an acid halide, to give the corresponding 2-halopyridyl product. Suitable coupling methods are known in the art, such as, DCC, EDC, PyBoP, HATU, HBTU, BOP, and the like. In a subsequent step, the 2-halopyridyl product is converted to compounds of Formula (N) by treatment with an appropriate alcohol, under basic conditions such as, NaH, KH, Cs₂CO₃,K₂CO₃, Na₂CO₃ and the like. In some circumstances, a metal alkoxide can be used, such as, sodium alkoxide, potassium alkoxide and the like. The alcohol or metal alkoxide can be either substituted or unsubstituted. In a similar manner, novel compounds of Formula (O) can be prepared using a substituted or unsubstituted phenol, wherein R₈-R₁₂ represent various substitutions on the phenyl ring, including but not limited those substitutions described herein.

EXAMPLES

The compounds of the inventicon and their synthesis are further illustrated by the following examples. The following examples are provided to further define the invention without, howvever, limiting the invention to the particulas of these examples. “Ambient temperature” as referred to in the folloing example is meant to indicate a temperature falling between 0° C. and 40° C. The following compounds are named by Beilstein Auto Nom Version 4.0, CS Chem Draw Ultra Version 6.0, CS compounds are named by Beilstein Auto Nom Version 4.0, CS Chem Drawv Ultra Version 6.0, CS Chein Drawv Ultra version 6.0.2, Chem Draw Ultra Version 7.0.1, or ACD Name Version 7.0.

Abbreviations used in the instant specification particularly the Schemes and Examples, are as follows:

• • ¹H NMR: proton nuclear magnetic resonance spectrum
  • APCI: atmospheric pressure chemical ionization
  • Boc: t-butoxycarbonyl
  • (Boc)₂O: di-tertiary-bytyl dicarbonate
  • BuOH: butanol
  • CDCl₃ deuterated chlorofom
  • CH₂Cl₂: dichloromethane
  • CHCl₃ chloroform
  • Cl: chemical ionization
  • DIEA: diisopropylethlamine
  • DMA: n,N-dimethylacetamide
  • DMSO: dimethylsulfoxide
  • EI: electron ionization
  • ESI: electrospray ionization
  • Et₂O: dietihyl ether
  • EtOAc: acetic acid ethyl ester
  • EtOH: ethanol
  • FAB: fast atom bombardment
  • HATU: O(7-azabenzotriazol-1-yl)-N,N,N′,N′-tetramethyluroniumhexafluorophosphate
  • H₂SO₄: sulfuric acid
  • HCl: hydrogen chloride
  • K₂CO₃ : potassiunm carbonate
  • Me₂NH: dimethylamine
  • MeNH₂: methylamine
  • MeOH: methanol
  • MgSO₄: magnesium sulfate
  • NaH: sodium hydride
  • NaBH(OAc)₃: sodium triacetoxyborohydride
  • NaBH₃CN: sodium cyanoborohydride
  • NaBH₄: sodium borohydride
  • NaHCO₃ : sodium hydrogencarbonate
  • Pd/C: palladium carbon
  • POCl₃ : phosphoryl chloride
  • PVP: poly(4-vinylpyridine)
  • SOCl₂ : thionyl chloride
  • TEA: triethylamine
  • TFA: trifluoroacetic acid
  • THF: tetrahydrofuran
  • ZCl: benzyloxycarbonyl chloride
  • s: singlet
  • d: doublet
  • t: triplet
  • q: qualtet
  • dd: doublet doublet
  • dt: doublet triplet
  • ddd: doublet doublet doublet
  • brs: broad singlel
  • m: multiplet
  • J: coupling constant
  • Hz: Hertz.

Example 1

1-(3,4-Dimethoxy)-phenyl)-3-[cis-4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl -urea hydrochloride

Step A: Synthesis of 2,4-dichloro-quinazoline

To a suspension of 1H-quinazoline-2,4-dione (150 g, 925 mmol) in POCl₃ (549 mL, 5.89 mol) was added dimethyl-phenyl-amine (123 mL, 962 mmol). The mixture was stirred at reflux for 7 hr and concentrated. The solution was poured into ice water, and the aqueous layer was extracted with CHCl₃ (three times). The combined organic layer was dried over MgSO₄, filtrated, concentrated, and purified by flash chromatographv (silica gel, 50% CHCl₃ in hexane to 10%o EtOAc in CHCl₃) to give 2,4-dichloro-quinazoline (159 g, 86%) as a pale yellow solid.

Cl MS m/e 199 M⁺; ¹H NMR (300 MHz, CDCl₃) δ 7.71-7.81 (m, 1 H), 7.95-8.04 (m, 2 H), 8.27 (dt, J=8.3, 1.1 Hz, 1 H).

Step B: Synthesis of (2-chloro-quinazolin-4-yl)-dimethyl-amine

A solution of 2,4-dichloro-quinazoline (102 g, 530 mmol) in THF (1.2 L) was cooled to 4 ° C. and 50% aqueous Me₂NH (139 mL, 1.33 mol) was added. The mixture was stirred at ambient temperature for 80 min. The solution was alkalized with saturated aqueous NaHCO₃ (pH =9), and the aqueous layer was extracted with CHCl₃ (three times). The combined organic layer was dried over MgSO₄, filtrated, and concentrated. The residue was suspended in 50% Et₂O in hexane (250 mL) and the mixture was stirred at ambient temperature for 30 min. The precipitate was collected by filtration, washed with 50% Et₂O in hexane, and dried at 80° C. to give (2-chloro-quinazolin-4-yl)-dimethylamine (104 g 94%) as a pale yellow solid.

ESI MS m/e 207, M⁺; ¹H NMR (300 MHz, CDCl₃) δ 3.41 (s, 6 H), 7.68 (ddd, J=8.4, 6.9, 1.4 Hz, 1 H), 7.73-7.78 ( m, 2 H), 8.00 (d, J=8.4 Hz, 1 H).

Step C: Synthesis of (cis-4-benzyloxycarbonylamino-cyclohexyl)-carbamic acid benzyl ester

To a suspension of cis-N-cyclohexane-1,4-dicarboxylic acid (25.0 g, 145 mmol) in benzene (125 mL) were added phosphorazidic acid diphenyl ester (81.9 g, 298 mmol) and triethylamine (30.1 g, 297 mml). The reaction mixture was stirred at reflux for 2.5 hr. Benzylalcohol (32.2 g, 298 mmol) was added and the mixture was stirred at reflux for 2-4 hr. The reaction mixture was concentrated and the residue was dissolved in EtOAc and H₂O. The organic layer was separated and the aqueous layer was extracted with EtOAc (twice). The combined organic layer was washed with 1M aqueous KHSO₄, saturated aqueous NaHCO₃, and brine. The organic layer as dried over MgSO₄, filtrated, concentrated, and purified by flash chromatography (silica gel, 33% EtOAc in hexane) to give (cis-4-benzylox)carbonylamino-cyclohexyl)-carbanic acid benzyl ester (52.0 g, 94%) as a colorless oil.

ESI MS m/e 405, M+Na⁺; ¹H NMR (300 MHz, CDCl₃) δ 1.45-1.60 (m, 4 H), 1.60-1.80 (m, 4 H), 3.52-3.80 (m, 2 H). 4.70-5.00 (m, H), 5.07 (s, 4 H), 715-7.40 (m, 10 H)

Step D: Sy nthesis of (cis-4-amino-cyclohex)yl)-carbamic acid fert-butyl ester

To a solution of (cis-4-benzyloxxcarbonylamino-cyclohexyl)-carbaiic acid benzyl ester (91.7 g, 240 mmol) in MeOH (460 mL) was added 5% Pd/C (9.17 g). The reaction mixture was stirred at ambient temperature under hydrogen atmosphere for 2.5 days filtrated through a pad of celite, and concentrated to give a diamine as a colorless oil. To a solution of the diamine in MeOH (550 mL) was added a solution of (Boc)₂O (6.59 g, 30.2 mmol) in MeOH (80 mL) dropwvise over 4 hr. The reaction mixture was stirred at ambient temperature for 1.5 days and concentrated. After dissolution with H₂O, the aqueous layer was extracted wvith CHCl₃ (three times). The combined organic layer was dried over MgSO₄, filtrated, and concentrated to give cis-(4-amino-cyclohexyxl)-carbainic acid tert-butyl ester (7.73 g, 15%, crude) as a colorless oil. The aqueous layer was concentrated and the residue was dissolved in MeOH. The solution was dried over MgSO₄, filtered, and concentrated to give a recovered diamine (32.0 g) as a colorless oil. To a solution of the recovered diamine (32.9 g, 299 mmol) in MeOH (660 mL) was added a solution of (Boc)₂O (6.20 g, 28.8 mmol) in MeOH (80 mL) dropwise over 5 hr. The reaction mixture was stirred at ambient temperature for 9.5 hr and concentrated. After dissolution with H₂O, the aqueous layer was extracted with CHCl₃ (three times). The combined organic layer was dried over MgSO₄, filtrated, and concentrated to give (cis-4-amino-cyclohexyl)-carbamiic acid tert-butyl ester (8.16 g, 16% crude) as a colorless oil. The aqueous layer was concentrated and the residue was dissolved in MeOH. The solution was dried over MgSO₄ filtrated, and concentrated to give a recovered diamine (23.1 g) as a colorless oil. To a solution of the recovered diamine (23.1 g, 202 mmol) in MeOH (462 mL) as added a solution of (Boc)₂O (4.42 g, 20.3 mmol) in MeOH (56 mL) dropwise over 4 hr. The reaction mixture was stirred at ambient temperature for 3.5 days and concentrated. After dissolution with H₂O, the aqueous layer was extracted with CHCl₃ (three times). The combined organic layer was dried over MgSO₄, filtrated, and concentrated to give (cis-4-amino-cyclohexyl)-carbamic acid tert-butyl ester (5.01 g, 10% based on starting material) as a colorless oil. The aqueous layer was concentrated and the residue was dissolved in MeOH. Thle solution was dried over MgSO₄, filtrated, and concentrated to give a recovered diamine (16.0 g) as a colorless oil. To a solution of the recovered diamnine (16.0 g, 140 mmol) in MeOH (3-20 mL) was added a solution of (Boc)₂O (3.06 g, 14.0 mmol) in MeOH (40 mL) diropise over 4 hr. The reaction mixture was stirred at ambient temperature for 17 hr and concentrated. After dissolution with H₂O, the aqueous layer was extracted vith CHCl₃ (three times). The combined organic layer was dried over MgSO₄, filtrated, and concentrated to give (cis-4-amino-cyclohexyl)-carbamic acid tert-butyl ester (3.53 g, 7% based on the starting material) as a colorless oil. The aqueous layer was concentrated and the residue was dissolved in MeOH. The solution was dried over MgSO₄, filtrated, and concentrated to give a recovered diamine (11.1 g) as a colorless oil.

ESI NIS m/e 215, M+H⁺; ¹H NMR (300 MHz. CDCl₃) δ 1.20-1.80 (m, 8 H), 1.44 (s, 9 H), 2.78-2.95 (m, 1 H, 3.50-3.80 (m, 1 H)₅ 4.30-4.82 (m, 1 H)

Step E: Synthesis of N²-(cis-4-amino-cyclohexyl)-N⁴,N⁴-dimethyl-quinazoline-2,4-diamine

A mixture of (2-chloro-quinazolin-4-yl)-dimethyl-amine (3.00 g, 14.4 mmol) and (cis-4-amino-cyclohexyl)-carbamic acid tert-butyl ester (3.72 g, 17.4 mmol) in 2-propanol (10 mL) was stirred at reflux for 5.5 days, poured into saturated aqueous NaHCO₃, and the aqueous layer was extracted vith CHCl₃ (three times). The combined organic layer was dried over MgSO₄, filtrated, concentrated, and purified by flash chromatography (NH-silica, 20% EtOAc in hexane) to give [cis-4-(4-dimnethylamino-quinazolin-)ylamino)-cyclohexyl]-carbamic acid tert-butyl ester including sovent (5.44 g) as a colorless oil. To a solution of the above material (5.44 g) in EtOAc (10 mL) was added 4 M hydrocen clhloride in EtOAc (50 mL). The reaction mixture was stirred at ambient temperature for 2 hr and concentrated. The residue was alkalized with saturated aqueous NaHCO₃, and the precipitate was collected by filtration to give N²-(cis-4-amino-cyclohexyl)-N⁴,N⁴-dimethyl-quinazoline-2,4-diamine (2.26 g, 55%) as a white solid. The aqueous layer was extracted CHCl, (three times). The combined organic layer was dried over MgSO₄, filtrated, and concentrated to give N²-(cis-4-amino-cyclohexyl)-N⁴,N⁴-dimethyl-quinazoline-2,4-diamine (687 mg, 17%) as a white solid.

ESI MS m/e 285, M⁺; ¹H NMR (300 MHz, DMSO-d₆) δ 1.22-1.82 (m, 8 H), 3.20 (s, 6 H). 3.38-3.52 (m, 1 H), 3.83-4.06 (m, 1 H), 6.56 (d, J=7.5 Hz, 1 H), 7.01 (t, J=7.6 Hz. 1 H), 7.29 (d, J=8.3 Hz, 1 H), 7.47 (t, J=8.3 Hz, 1 H), 7.86 (d, J=7.5 Hz, 1 H).

Step F: Synthesis of 1-(3,4-dimethoxy)-phenyl)-3-[cis-4-(4-dimelhylamino-quinazolin-2-ylamino)-cyclohexy]-urea hydrochloride

To a solution of N²-(cis-4-amino-cyclohexyl)-N⁴,N⁴-dimethyl-quinazoline-2,4-diamine (500 mg, 1.75 mmol) in DMSO (5 mL) was added 4-isocyanato-1,2-dimethoxy-benzene (345 mg, 1.93 mmol). The mixture was stinred at ambient temperature for 1 hr and poured into water. The precipitate was filtrated, washed with water, and purified by medium-pressure liquid chromatograph (silica gel, 5% EtOAc in hexane) and flash chromatograph) (NH-silica, EtOAc) to give a pale yellow oil. To a solution of the above material in EtOAc (2 mL) was added 4 M hydrogen chloride in EtOAc (10 mL). The mixture was stirred at ambient temperature for 1 hr and concentrated. A suspension of the residue in Et₂O (10 mnL) was stirred at ambient tempareture for 1 hr. The precipitate was collected ny filtration, washed with Et₂O, and dried at 80° C. under reduced pressure to give 1-(3,4-dimethoxy-phenyl)-3-[cis-4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-urea hydrochloride (757 mg, 86% as a white solid.

ESI MS m/e 487, M (free)+Na⁺; ¹H NMR (300 MHz, CDCl₃) δ 1.68-2.07 (m, 8 H). 3.49 (s, 6 H), 3.79 (s, 6 H), 3.95, (brs, 1 H), 4.09 (brs, 1 H), 6.66 (d, J=8.7 Hz, 1 H), 6.82 (d, J=9.0 Hz, 1 H), 7.17-7.33 (m 2 H), 7.48-7.66 (m, 2 H), 7.S7 (d, J=7.3. Hz. 1 H), 8.37 (brs, 1 H), 12.77 (brs, 1 H).

Example 2

1-(2,3-Dichloro-phenyl)-3-[cis-4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexylmethyl]-urea hydrochloride

Step A: Synthesis of (cis-4-hydroxymethyl-cyclohexyl)-carbamic acid tert-butyl ester

A suspension of cis-4-amino-cyclohexanecarboxylic acid (244 g, 1.71 mol) in MeOH (2.45 L) was cooled to −8° C. Thionyl chloride (440 mL, 6.03 mol) was added dropwise. The resulting solution was stirred at ambient temperature for 4.5 hr and concentrated to give a white solid. To a suspension of the above solid in CHCl₃ (3.00 L) were added triethylamine (261 mL, 1.88 mol) and (Boc)₂O (409 g, 1.88 mol) successively. The reaction mixture was stirred at ambient temperature for 5 hr and poured into water. The aqueous layer was extracted with CHCl₃ (three times). The combined organic layer was dried over MgSO, filtrated, concentrated, and purified by flash chromatography (silica gel, 11% EtOAc in hexane to 10% MeOH in CHCl₃) and flash chromatography (NH-silica, 33% EtOAc in hexane to 9% MeOH in CHCl₃) to give a colorless oil (531 g). To a suspension cooled at −4 ° C. of lithium aluminum hydride (78.3 g, 2.06 mol) in Et₂O (7.9 L) was added a solution of the above oil (530.9 g) in Et₂O (5.3 L) below 0° C. The resulting suspension was stirred at ambient temperature for 2 hr. The reaction mixture was cooled on an ice-bath, quenched with cold water, and filtrated through a pad of celite. The filtrate was dried over MgSO₄, filtrated, and concentrated. The residue was suspended in hexane (300 mL), filtrated, washed with hexane, and dried at 70° C. to give (cis-4-hydroxymethyl-cyclohexyl)-carbamic acid tert-butyl ester (301 g, 77% as a white solid.

ESI MS m/e 252, M+Na⁺; ¹H NMR (300 MHz, CDCl₃) δ 1.61-1.36 (m,2 H), 1.45 (s, 9 H), 1.52-1.77 (m, 7 H), 3.51 (d, J=6.2 Hz, 2 H), 3.75 (brs, 1 H), 4.30-4.82 (m, 1 H).

Step B: Synthesis of [cis-4-(benzyloxycarbonylamino-methyl)-cyclohexyl]-carbamic acid tert-butyl ester

To a solution of (cis-4-hydroxymethyl-cyclolexyl)-carbamic acid tert-butyl ester (17.7 g, 77.2 mmol) in THF (245 mL) were added triphenylphosphine (20.2 g, 77.0 mmol) and phthalimide (11.4 g, 77.5 mmol) successively. The resulting suspension was cooled on in ice-bath and 40% diethylazodicarboxylate in toluene (33.6 mL, 74.1 mmol) as added over 1 hr. The reaction mixture was stirred at ambient temperature for 2.5 days, concentrated, and purified by flash chromatography (silica gel, 33% EtOAc in hexane) to give a white solid. To a suspension of the above solid (27.5 g) in EtOH (275 mL) was added hydrazine hydrate (5.76 g, 115 mmol). The mixture was stirred at reflux for 2.25 hr, cooled, and concentrated. The residue was dissolved in 10% aqueous NaOH (350 mL) and the aqueous layer was extracted with CHCl₃ (three times). The combined organic layer was dried over MgSO₄, filtrated, and concentrated. To a solution of the above residue in CHCl₃ (275 mL) was added triethylamine (8.54 g, 84.4 mmol). The resulting solution was cooled to 0° C. and ZCl (14.4 g, 84.4 mmol) was added below 5° C. The reaction mixture was stirred at ambient temperature for 16 hr and poured into saturated aqueous NaHCO₃. The aqueous layer was extracted with CHCl₃ (three times). The combined organic layer was dried over MgSO₄, filtrated, concentrated, and purified by flash chromatography (silica gel, 2% MeOH in CHCl₃) to give [cis-4-(benzyloxycarbonylaminomethyl)-cyclohexyl]-carbamic acid tert-butyl ester (25.3 g, 91%) as a colorless oil.

ESI NIS m/e 385, M+Na⁺; ¹H NMR (300 MHz, CDCl₃), δ 1.13-1.31 (m, 2-H), 1.44 (s, 9 H), 1.48-1.75 (m, 7 H). 3.10 (t, J=6.4 Hz, 2 H), 3.72 (brs, 1 H), 4.42-4.76 (m, 1 H), 4.76-4.92 (m, 1 H), 5.09 (s, 2 H), 7.27-7.38 (m, 5 H).

Step C: Synthesis of (cis-4-amino-cyclohexylmethyl)-carbamic acid benzyl ester

To a solution of [cis-4-(benzyloxycarbonylamino-methyl)-cyclohexyl]-carbamic acid tert-butyl ester (12.9 g, 35.6 mmol) in EtOAc (129 mL) was added 4 M hydrogen chloride in EtOAc (129 mL). The reaction mixture was stirred at ambient temperature for 3 hr, filtrated, washed with EtOAc, and dried under reduced pressure. The above solid was dissolved in saturated aqueous NaHCO₂ (pH=9). The aqueous layer was extracted with CHCl₃ (five times). The combined organic layer was dried over MgSO₄, filtrated, concentrated, and dried under reduced pressure to give (cis-4-aminocyclohexylmethyl)-carbamic acid benznyl ester (8.88 g, 95%) as a colorless oil.

ESI MS m/e 263, M+H⁺; ¹H NMR (300 MHz, CDCl₃) δ 1.36-1.98 (m, 9 H), 2.96-3.32 (m, 3 H), 5.12 (brs, 3 H), 7.36 (s. 5 H).

Step D: Synthesis of [cis-4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexylmethyl]-carbamic acid benezylester

A mixture of (2-chloro-quinazolin-4-yl)-dimethyl-amine obtained in step B of example 1 (50 g, 258 mmol) and (cis-4-amino-cyclohexlmethyl)-carbamic acid benzy!l ester (81 g, 309 mmol) in 2-propanol (75 mL) was stirred at reflux for 7 days. The reaction mixture was poured into saturated aqueous NaHCO₃ and the aqueous layer was extracted with CHCl₃ (three times). The combined organic layer was dried over MgSO₄, filtrated, concentrated, and purified by flash chromatography (NH-silica gel, 13% to 50% EtOAc in hexane) to give [cis-4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexylmethyl)-carbamic acid benzyl ester (65.7 g, 59%) as a pale brown solid.

ESI MS m/e 434, M+H⁺; ¹H NMR (300 MHz, CDCl₃) δ 1.23-1.40 (m, 2 H), 1.52-1.73 (m, 5 H), 1.80-1.93 (m, 2 H), 3.11 (t, J=6.3 Hz, 2 H), 3.26 (s, 6 H), 4.18 -4.28 (m, 1 H), 4.82)-4.93 (m, 1 H), 4.93-5.06 (m, 1 H), 5.10 (s, 2 H), 7.01 (ddd, J=8.2, 6.5, 1.7 Hz, 1 H). 7.26-7.52 (m, 7 H), 7.81 (d, J=9.0 Hz, 1 H).

Step E: Synthesis of N²-(cis-4-aminomethyl-cyclohexyl)-N⁴,N⁴-dimethyl-quinazoline-2,4-diamine

To a solution of [cis-4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl-methy-]-carbamic acid benzyl ester (12.1 g, 27.9 mmol) in MeOH (120 mL) was added 10% Pd/C (1.21 g). The mixture was stirred at 50° C. under hydrogen atmosphere for 19 hr., filtrated, concentrated, and purified by flash chromatography (NH-silica, 66% EtOAc in hexane to 15%, MeOH in CHCl₃) to give N²-(cis-4-aminomethyl-cyclohexyl)-N⁴,N⁴-dimethlyl-quinazoline-2,4-diamine (6.9 g, 83%) a pale yellow solid.

CI MS m/e 300, M+H⁺: ¹H NMR (300 MHz, CDCl₃) δ 0.90-1.51 (m, 5 H), 1.57-1.76 (m, 4 H), 1.81-1.96 (m, 2 H), 2.60 (d, J=6.4 Hz, 2 H), 3.27 (s, 6 H), 4.24-4.30 (m, 1 H), 5.04 (d, J=7.3 Hz, 1 H), 6.98 -7.04 (m, 1 H), 7.40-7.51 (m, 2 H), 7.81 (d, J=8.4 Hz, 1 H).

Step F: Synthesis of 1-(2,3-dichloro-phenyl)-3-[cis-4-(4-dimethylamino-quinazolin-2-ylamino)cyclohexylmethyl]-urea hydrochloride

Using, the procedure for the step F of examiple 1, the title compound was obtained.

ESI MS m/e 509, M (free)+Na⁺; ¹H NMR (300 MHz, CDCl₃) δ 1.48-2.12 (m, 9 H), 3.37-3.44 (m, 2 H), 3.51 (s, 6 H), 4.3 7-4.49 (m, 1 H 6.91-7.13 (m, 3 H), 7.27 (ddd, J=8.4, 7.2, 1.2 Hz, 1 H), 7.50 (dd, J=8.6, 1.2 Hz, 1 H), 7.67 (ddd, J=8.4 7.2, 1.2 Hz, 1 H), 7.89 (d, J=8.4 Hz, 1 H), 8.17 (dd. J=8.2, 1.7Hz, 1 H), 8.24 (s, 1 H), 8.89 (d, J=8.9 Hz, 1 H), 12.42 (s, 1 H).

Example 3

1-(2,6-Dichloro-phenyl)-3-[cis-4-(4-dimethylamino-quinazolin-2-)ylamino)-cyclohexylmethyl]-urea hydrochloride

Step A: Synthesis of 1-(2,6-dichloro-phenyl)-3-[cis-4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexylmethyl]-urea hydrochloride

Using the procedure for the step F of example 1, the title compound was obtained.

ESI MS m/e 509, M (free)+Na⁺; ¹H NMR (300 MHz, CDCl₃) δ 1.51-2.06 (m, 9 H), 3.37-3.42 (m, 2 H), 3.52 (s, 6 H), 4.37-4.47 (m, 1 H), 6.35-6.45 (m, 1 H), 6.96-7.06 (m, 1 H), 7.23-7.31 (m, 3 H), 7.43-7.49 (m, 1 H), 7.61-7.68 (m, 1 H), 7.91 (d, J=7.9 Hz, 2 H), 8.72 (d, J=8.7 Hz, 1 H), 12.64 (s, 1 H).

Example 4-845

To a solution of amines (30 O μmol) as shown below in DMSO (300 μL) were added isocyanate or isothiocyanate (60 μmol) in DNISO (200 μL) at ambient temperature. The mixture was stirred at the same temperature for 22 hr. To the reaction mixture were added 2 M MeNH, in THF (30 μL, 60 μmol) or D-gulcamine (60 μmol) in DMSO (200 μL) at ambient temperature. After stirring at the same temperature for 20 hr, the reaction mixture was filtrated through a pad of SCX, concentrated by a stream of of N₂, and purified by silica gel chromatography (silica gel, 2% to 7% 2M NH₃/MeOH in CHCl₃) and silica gel chromatography (NH-silica,20% to 50% EtOAc in hexane) to give the desired product. The product was determined by ESI-MS or APCI-MS.

Example 846-885

To a solution of poly(4-vinylpyridine) (75 μL) in CH₂Cl₂ (200 μL) were added the amines (30 μmol) as shown below in CH₂Cl₂ (200 μL) and chloroformate (R₁OCOCl, 60 μmol) in CH₂Cl₂ (200 μL) at ambient temperature. After stirring at the same temperature for 17 hr, the reaction mixture was filtrated and concentrated by a stream of dry N₂. To the residue wvere added CH₂Cl₂ (700 μL) and PSA (300 μL). After the stirring at ambient temperature for 19 hr, the reaction mixture was filtrated and purified by silica gel chromatograph) (NH-silica, 20% EtOAc in hexane) and silica gel chromatography (silica gel, 2% to 7% 2M NH₃/MeOH in CHCl₃) to give the desired product. The product was determined by ESI-MS or APCI-MS.

Wherein the amines are selected from N²-(cis-4-amino-cyclohexyl)-N⁴,N⁴H-dimethyl-quinazoline-2,4-diamine obtained in step E of example 1 or N²-(sis-4-aminomethyl-cyclohexyl)-N⁴,N⁴-dimethyl-quinazoline-2,4-diamine obtained in step E of example 2.

Ex. No.	compound name	MS	class
4	N-(3-acetylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	447 (M + H)	3
	yl]amino}cyclohexyl)urea
5	N-1-adamantyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	463 (M + H)	3
	yl]amino}cyclohexyl)urea
6	N-(4-acetylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	447 (M + H)	3
	yl]amino}cyclohexyl)urea
7	N-{[(cis-4-{[4-(dimethylamino)quinazolin-2-	433 (M + H)	3
	yl]amino}cyclohexyl)amino]carbonyl}benzamide
8	N-[3,5-bis(trifluoromethyl)phenyl]-N′-(cis-4-{[4-	541 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
9	N-benzyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	419 (M + H)	2
	yl]amino}cyclohexyl)urea
10	N-(2-bromophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	483 (M + H)	1
	yl]amino}cyclohexyl)urea
11	N-biphenyl-2-yl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	481 (M + H)	1
	yl]amino}cyclohexyl)urea
12	N-(4-bromophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	483 (M + H)	2
	yl]amino}cyclohexyl)urea
13	N-butyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	385 (M + H)	1
	yl]amino}cyclohexyl)urea
14	N-(3-chlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	439 (M + H)	3
	yl]amino}cyclohexyl)urea
15	N-(4-chlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	439 (M + H)	3
	yl]amino}cyclohexyl)urea
16	N-cyclohexyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	411 (M + H)	2
	yl]amino}cyclohexyl)urea
17	N-(3-cyanophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	430 (M + H)	3
	yl]amino}cyclohexyl)urea
18	N-(2-chlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	439 (M + H)	1
	yl]amino}cyclohexyl)urea
19	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	433 (M + H)	1
	N′-(2,6-dimethylphenyl)urea
20	N-(3,4-dichlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	473 (M + H)	3
	2-yl]amino}cyclohexyl)urea
21	N-(2,4-difluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	441 (M + H)	1
	2-yl]amino}cyclohexyl)urea
22	N-(2,4-dichlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	473 (M + H)	2
	2-yl]amino}cyclohexyl)urea
23	N-(3,5-dichlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	473 (M + H)	3
	2-yl]amino}cyclohexyl)urea
24	N-(2,3-dichlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	473 (M + H)	3
	2-yl]amino}cyclohexyl)urea
25	N-(2,6-difluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	441 (M + H)	3
	2-yl]amino}cyclohexyl)urea
26	N-(2,5-dichlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	473 (M + H)	3
	2-yl]amino}cyclohexyl)urea
27	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	433 (M + H)	1
	N′-(2,3-dimethylphenyl)urea
28	ethyl N-{[(cis-4-{[4-(dimethylamino)quinazolin-2-	415 (M + H)	3
	yl]amino}cyclohexyl)amino]carbonyl}glycinate
29	ethyl 3-({[(cis-4-{[4-(dimethylamino)quinazolin-2-	477 (M + H)	1
	yl]amino}cyclohexyl)amino]carbonyl}amino)benzoate
30	ethyl 4-({[(cis-4-{[4-(dimethylamino)quinazolin-2-	477 (M + H)	2
	yl]amino}cyclohexyl)amino]carbonyl}amino)benzoate
31	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	433 (M + H)	2
	N′-(4-ethylphenyl)urea
32	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	357 (M + H)	3
	N′-ethylurea
33	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	447 (M + H)	1
	N′-(2-ethyl-6-methylphenyl)urea
34	ethyl N-{[(cis-4-{[4-(dimethylamino)quinazolin-2-	471 (M + H)	1
	yl]amino}cyclohexyl)amino]carbonyl}lucinate
35	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	468 (M + H)	3
	N′-(4-fluoro-3-nitrophenyl)urea
36	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	423 (M + H)	1
	N′-(4-fluorophenyl)urea
37	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	423 (M + H)	3
	N′-(3-fluorophenyl)urea
38	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	423 (M + H)	3
	N′-(2-fluorophenyl)urea
39	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	447 (M + H)	3
	N′-(4-isopropylphenyl)urea
40	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	487 (M + H)	1
	N′-[1-(3-isopropenylphenyl)-1-methylethyl]urea
41	methyl N-{[(cis-4-{[4-(dimethylamino)quinazolin-2-	475 (M + H)	1
	yl]amino}cyclohexyl)amino]carbonyl}methioninate
42	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	371 (M + H)	3
	N′-isopropylurea
43	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	435 (M + H)	2
	N′-(4-methoxyphenyl)urea
44	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	464 (M + H)	3
	N′-(4-methyl-2-nitrophenyl)urea
45	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	435 (M + H)	2
	N′-(2-methoxyphenyl)urea
46	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	435 (M + H)	2
	N′-(3-methoxyphenyl)urea
47	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	451 (M + H)	1
	N′-[4-(methylthio)phenyl]urea
48	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	449 (M + H)	2
	N′-(4-methoxybenzyl)urea
49	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	433 (M + H)	3
	N′-(3-methylbenzyl)urea
50	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	455 (M + H)	1
	N′-1-napthylurea
51	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	445 (M + H)	1
	N′-[(2S)-2-phenylcyclopropyl]urea
52	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	405 (M + H)	2
	N′-phenylurea
53	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	497 (M + H)	1
	N′-(4-phenoxyphenyl)urea
54	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	399 (M + H)	1
	N′-pentylurea
55	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	473 (M + H)	1
	N′-[2-(trifluoromethyl)phenyl]urea
56	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	473 (M + H)	3
	N′-[3-(trifluoromethyl)phenyl]urea
57	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	419 (M + H)	2
	N′-(4-methylphenyl)urea
58	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	447 (M + H)	1
	N′-mesitylurea
59	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	419 (M + H)	2
	N′-(3-methylphenyl)urea
60	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	419 (M + H)	1
	N′-(2-methylphenyl)urea
61	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	483 (M + H)	1
	N′-[1-(-napthyl)ethyl]urea
62	methyl N-{[(cis-4-{[4-(dimethylamino)quinazolin-2-	491 (M + H)	1
	yl]amino}cyclohexyl)amino]carbonyl}phenylalaninate
63	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	507 (M + H)	1
	N′-(2,4,6-trichlorophenyl)urea
64	N-(3-chloro-4-methylphenyl)-N′-(cis-4-{[4-	453 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
65	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	433 (M + H)	1
	N′-(1-phenylethyl)urea
66	1-[4-(4-Dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-3-(1-	433 (M + H)	1
	phenyl-ethyl)-urea
67	1-[4-(4-Dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-3-(1-	483 (M + H)	2
	napthalen-1-yl-ethyl)-urea
68	N-(2,6-diisopropylphenyl)-N′-(cis-4-{[4-	489 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
69	N-[2-(difluoromethoxy)phenyl]-N′-(cis-4-{[4-	471 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
70	metyl 2-({[4(cis-4-{[-(dimethylamino)quinazolin-2-	463 (M + H)	3
	yl]amino}cyclohexyl)amino]carbonyl}amino)benzoate
71	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	451 (M + H)	2
	N′-[2-(methylthio)phenyl]urea
72	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	541 (M + H)	1
	N′-(2,3,5,6-tetrachlorophenyl)urea
73	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	478 (M + H)	2
	N′-(2,3-dimethyl-6-nitrophenyl)urea
74	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	507 (M + H)	3
	N′-(2,4,5-trichlorophenyl)urea
75	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	638 (M + H)	1
	N′-(2,4,6-tribromophenyl)urea
76	N-(2,4-dibromo-6-fluorophenyl)-N′-(cis-4-{[4-	579 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
77	N-(2,4-dibromophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	561 (M + H)	1
	2-yl]amino}cyclohexyl)urea
78	N-(2,4-dichlorobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	487 (M + H)	1
	2-yl]amino}cyclohexyl)urea
79	N-(2,4-dimethoxyphenyl)-N′-(cis-4-{[4-	465 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
80	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	433 (M + H)	3
	N′-(2,4-dimethylphenyl)urea
81	N-(2,5-dimethoxyphenyl)-N′-(cis-4-{[4-	465 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
82	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	433 (M + H)	3
	N′-(2,5-dimethylphenyl)urea
83	N-(2,6-dibromo-4-fluorophenyl)-N′-(cis-4-{[4-	579 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
84	N-(2,6-dichlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	473 (M + H)	3
	2-yl]amino}cyclohexyl)urea
85	N-(2,6-diethylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	461 (M + H)	1
	2-yl]amino}cyclohexyl)urea
86	N-(2-benzylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	495 (M + H)	3
	yl]amino}cyclohexyl)urea
87	N-(2-chloro-5-methylphenyl)-N′-(cis-4-{[4-	453 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
88	N-(2-chloro-5-nitrophenyl)-N′-(cis-4-{[4-	484 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
89	N-[2-chloro-6-(trifluoromethyl)phenyl]-N′-(cis-4-{[4-	507 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
90	N-(2-chloro-6-methylphenyl)-N′-(cis-4-{[4-	453 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
91	N-(2-chlorobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	453 (M + H)	1
	yl]amino}cyclohexyl)urea
92	ethyl 2-({[(cis-4-{[4-(dimethylamino)quinazolin-2-	477 (M + H)	3
	yl]amino}cyclohexyl)amino]carbonyl}amino)benzoate
93	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	449 (M + H)	1
	N′-(2-ethoxyphenyl)urea
94	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	475 (M + H)	1
	N′-(2-ethyl-6-isopropylphenyl)urea
95	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	433 (M + H)	1
	N′-(2-ethylphenyl)urea
96	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	491 (M + H)	3
	N′-[2-fluoro-3-(trifluoromethyl)phenyl]urea
97	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	491 (M + H)	3
	N′-[2-fluro-5-(trifluoromethyl)phenyl]urea
98	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	437 (M + H)	3
	N′-(2-fluro-5-methylphenyl)urea
99	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	468 (M + H)	3
	N′-(2-fluoro-5-nitrophenyl)urea
100	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	437 (M + H)	1
	N′-(2-fluorobenzyl)urea
101	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	531 (M + H)	1
	N′-(2-iodophenyl)urea
102	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	461 (M + H)	1
	N′-(2-isopropyl-6-methylphenyl)urea
103	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	447 (M + H)	1
	N′-(2-isopropylphenyl)urea
104	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	480 (M + H)	2
	N′-(2-methoxy-4-nitrophenyl)urea
105	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	449 (M + H)	2
	N′-(2-methoxy-5-methylphenyl)urea
106	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	480 (M + H)	3
	N′-(2-methoxy-5-nitrophenyl)urea
107	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	464 (M + H)	1
	N′-(2-methyl-3-nitrophenyl)urea
108	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	464 (M + H)	1
	N′-(2-methyl-4-nitrophenyl)urea
109	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	464 (M + H)	1
	N′-(2-methyl-5-nitrophenyl)urea
110	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	464 (M + H)	3
	N′-(2-methyl-6-nitrophenyl)urea
111	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	433 (M + H)	1
	N′-(2-methylbenzyl)urea
112	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	455 (M + H)	3
	N′-2-naphthylurea
113	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	450 (M + H)	1
	N′-(2-nitrophenyl)urea
114	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	447 (M + H)	1
	N′-(2-propylphenyl)urea
115	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	497 (M + H)	2
	N′-(2-phenoxyphenyl)urea
116	N-(2-tert-butyl-6-methylphenyl)-N′-(cis-4-{[4-	475 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
117	N-(2-tert-butylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	461 (M + H)	1
	2-yl]amino}cyclohexyl)urea
118	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	451 (M + H)	2
	N′-[3-(methylthio)phenyl]urea
119	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	505 (M + H)	3
	N′-{3-[(trifluoromethyl)thio]phenyl}urea
120	N-1,3-benzodioxol-5-yl-N′-(cis-4-{[4-(dimethylamino)quinazolin-	449 (M + H)	1
	2-yl]amino}cyclohexyl)urea
121	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	495 (M + H)	1
	N′-(3,4,5-trimethoxyphenyl)urea
122	N-(3,4-dichlorobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	487 (M + H)	2
	2-yl]amino}cyclohexyl)urea
123	N-(3,4-difluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	441 (M + H)	2
	2-yl]amino}cyclohexyl)urea
124	N-(3,4-dimethoxyphenyl)-N′-(cis-4-{[4-	465 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
125	N-(3,5-difluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	441 (M + H)	2
	2-yl]amino}cyclohexyl)urea
126	N-(3,5-dimethoxyphenyl)-N′-(cis-4-{[4-	465 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
127	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	433 (M + H)	2
	N′-(3,5-dimethylphenyl)urea
128	methyl 3-({[(cis-4-{[4-(dimethylamino)quinazolin-2-	463 (M + H)	2
	yl]amino}cyclohexyl)amino]carbonyl}amino)benzoate
129	N-(3-chloro-2-methylphenyl)-N′-(cis-4-{[4-	453 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
130	N-(3-chloro-4-fluorophenyl)-N′-(cis-4-{[4-	457 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
131	N-(3-chloro-4-methoxyphenyl)-N′-(cis-4-{[4-	469 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
132	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	433 (M + H)	2
	N′-(3-ethylphenyl)urea
133	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	491 (M + H)	3
	N′-[3-fluoro-5-(trifluoromethyl)phenyl]urea
134	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	437 (M + H)	2
	N′-(3-fluorobenzyl)urea
135	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	448(M−H)	3
	N′-(3-nitrophenyl)urea
136	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	473 (M + H)	3
	N′-[4-(trifluoromethyl)phenyl]urea
137	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	505 (M + H)	3
	N′-{4-[(trifluoromethyl)thio]phenyl}urea
138	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	478 (M + H)	3
	N′-(4,5-dimethyl-2-nitrophenyl)urea
139	N-[4-(benzyloxy)phenyl]-N′-(cis-4-{[4-	511 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
140	N-(4-benzylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	495 (M + H)	3
	yl]amino}cyclohexyl)urea
141	N-[4-bromo-2-(trifluoromethyl)pheny]-N′-(cis-4-{[4-	551 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
142	N-(4-bromo-2,6-difluorophenyl)-N′-(cis-4-{[4-	519 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
143	N-(4-bromo-2-chlorophenyl)-N′-(cis-4-{[4-	517 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
144	N-(4-bromobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	497 (M + H)	1
	yl]amino}cyclohexyl)urea
145	N-[4-chloro-2-(trifluoromethyl)phenyl]-N′-(cis-4-{[4-	507 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
146	N-(4-chloro-2-methylphenyl)-N′-(cis-4-{[4-	453 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
147	N-(4-chloro-2-nitrophenyl)-N′-(cis-4-{[4-	484 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
148	N-[4-chloro-3-(trifluoromethyl)phenyl]-N′-(cis-4-{[4-	507 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
149	N-(4-cyanophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	430 (M + H)	1
	yl]amino}cyclohexyl)urea
150	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	449 (M + H)	2
	N′-(4-ethoxyphenyl)urea
151	N-[1-(4-bromophenyl)ethyl]-N′-(cis-4-{[4-	511 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
152	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	489 (M + H)	3
	N′-[2-(trifluoromethoxy)phenyl]urea
153	N-(3-acetylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	463 (M + H)	3
	yl]amino}cyclohexyl)thiourea
154	N-(4-acetylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	463 (M + H)	3
	yl]amino}cyclohexyl)thiourea
155	N-[3,5-bis(trifluoromethyl)phenyl]-N′-(cis-4-{[4-	557 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
156	N-benzyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	435 (M + H)	3
	yl]amino}cyclohexyl)thiourea
157	N-(3-bromopheny)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	499 (M + H)	3
	yl]amino}cyclohexyl)thiourea
158	N-(4-bromophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	499 (M + H)	1
	yl]amino}cyclohexyl)thiourea
159	N-butyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	401 (M + H)	3
	yl]amino}cyclohexyl)thiourea
160	N-(4-cyanophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	446 (M + H)	1
	yl]amino}cyclohexyl)thiourea
161	N-cyclohexyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	427 (M + H)	2
	yl]amino}cyclohexyl)thiourea
162	N-cyclopentyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	413 (M + H)	2
	yl]amino}cyclohexyl)thiourea
163	N-(3-chlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	455 (M + H)	3
	yl]amino}cyclohexyl)thiourea
164	N-(4-chlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	455 (M + H)	2
	yl]amino}cyclohexyl)thiourea
165	N-(2,4-dichlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	489 (M + H)	1
	2-yl]amino}cyclohexyl)thiourea
166	N-(2,4-dimethoxyphenyl)-N′-(cis-4-{[4-	481 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
167	N-(2,5-difluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	457 (M + H)	3
	2-yl]amino}cyclohexyl)thiourea
168	N-(2,5-dichlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	489 (M + H)	3
	2-yl]amino}cyclohexyl)thiourea
169	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	449 (M + H)	1
	N′-(2,6-dimethylphenyl)thiourea
170	N-(3,4-dichlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	489 (M + H)	3
	2-yl]amino}cyclohexyl)thiourea
171	N-(2,6-dichlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	489 (M + H)	3
	2-yl]amino}cyclohexyl)thiourea
172	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	465 (M + H)	3
	N′-(4-ethoxyphenyl)thiourea
173	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	491 (M + H)	1
	N′-(2-ethyl-6-isoprophylphenyl)thiourea
174	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	425 (M + H)	3
	N′-(2-furylmethyl)thiourea
175	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	439 (M + H)	2
	N′-(4-fluorophenyl)thiourea
176	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	429 (M + H)	2
	N′-hexylthiourea
177	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	545 (M + H)	3
	N′-[4-(trans-4-propylcyclohexyl)phenyl]thiourea
178	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	401 (M + H)	2
	N′-isobutylthiourea
179	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	527 (M + H)	2
	N′-(4-methoxybiphenyl-3-yl)thiourea
180	N-(1,3-benzodioxol-5-ylmethyl)-N′-(cis-4-{[4-	479 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
181	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	435 (M + H)	3
	N′-(3-methylphenyl)thiourea
182	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	467 (M + H)	2
	N′-[4-(methylthio)phenyl]thiourea
183	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	451 (M + H)	2
	N′-(4-methoxyphenyl)thiourea
184	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	399 (M + H)	3
	N′-(2-methylprop-2-en-1-yl)thiourea
185	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	451 (M + H)	1
	N′-(2-methoxyphenyl)thiourea
186	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	359 (M + H)	3
	N′-methylthiourea
187	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	471 (M + H)	1
	N′-1-naphthylthiourea
188	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	466 (M + H)	3
	N′-(3-nitrophenyl)thiourea
189	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	466 (M + H)	2
	N′-(4-nitrophenyl)thiourea
190	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	457 (M + H)	3
	N′-(1,1,3,3-tetramethylbutyl)thiourea
191	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	421 (M + H)	3
	N′-phenylthiourea
192	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	511 (M + H)	2
	N′-(pentafluorophenyl)thiourea
193	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	387 (M + H)	2
	N′-propylthiourea
194	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	489 (M + H)	3
	N′-[3-(trifluoromethyl)phenyl]thiourea
195	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	511 (M + H)	1
	N′-(3,4,5-trimethoxyphenyl)thiourea
196	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	429 (M + H)	3
	N′-(tetrahydrofuran-2-ylmethyl)thiourea
197	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	435 (M + H)	2
	N′-(4-methylphenyl)thiourea
198	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	435 (M + H)	3
	N′-(2-methylphenyl)thiourea
199	N-(tert-butyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	401 (M + H)	3
	yl]amino}cyclohexyl)thiourea
200	N-1-adamantyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	479 (M + H)	3
	yl]amino}cyclohexyl)thiourea
201	N-(2-bromophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	499 (M + H)	3
	yl]amino}cyclohexyl)thiourea
202	N-(2-chlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	455 (M + H)	3
	yl]amino}cyclohexyl)thiourea
203	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	449 (M + H)	3
	N′-(2-phenylethyl)thiourea
204	N-(3,4-dimethoxyphenyl)-N′-(cis-4-{[4-	481 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
205	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	449 (M + H)	2
	N′-(4-ethylphenyl)thiourea
206	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	467 (M + H)	2
	N′-[2-(methylthio)phenyl]thiourea
207	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	505 (M + H)	2
	N′-[2-(trifluoromethoxy)phenyl]thiourea
208	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	489 (M + H)	3
	N′-[2-(trifluoromethyl)phenyl]thiourea
209	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	475 (M + H)	2
	N′-(2,3,4-trifluorophenyl)thiourea
210	N-(2,3-dichlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	489 (M + H)	3
	2-yl]amino}cyclohexyl)thiourea
211	N-(2,4-difluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	457 (M + H)	3
	2-yl]amino}cyclohexyl)thiourea
212	N-(2,5-dimethoxyphenyl)-N′-(cis-4-{[4-	481 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
213	N-(2,6-difluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	457 (M + H)	3
	2-yl]amino}cyclohexyl)thiourea
214	N-(2-chloro-4-nitrophenyl)-N′-(cis-4-{[4-	500 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
215	N-[2-(difluoromethoxy)phenyl]-N′-(cis-4-{[4-	487 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
216	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	449 (M + H)	1
	N′-(2-ethylphenyl)thiourea
217	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	507 (M + H)	3
	N′-[2-fluoro-5-(trifluoromethyl)phenyl]thiourea
218	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	439 (M + H)	3
	N′-(2-fluorophenyl)thiourea
219	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	547 (M + H)	2
	N′-(2-iodophenyl)thiourea
220	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	496 (M + H)	1
	N′-(2-methoxy-4-nitrophenyl)thiourea
221	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	465 (M + H)	1
	N′-(2-methoxy-5-methylphenyl)thiourea
222	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	521 (M + H)	3
	N′-{3-[(trifluoromethyl)thio]phenyl}thiourea
223	N-(3,5-dichlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	489 (M + H)	3
	2-yl]amino}cyclohexyl)thiourea
224	N-(3,5-difluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	457 (M + H)	3
	2-yl]amino}cyclohexyl)thiourea
225	N-(3-cyanophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	446 (M + H)	3
	yl]amino}cyclohexyl)thiourea
226	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	439 (M + H)	3
	N′-(3-fluorophenyl)thiourea
227	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	547 (M + H)	2
	N′-(3-iodophenyl)thiourea
228	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	451 (M + H)	2
	N′-(3-methoxyphenyl)thiourea
229	N-[4-(difluoromethoxy)phenyl]-N′-(cis-4-{[4-	487 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
230	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	505 (M + H)	3
	N′-[4-(trifluoromethoxy)phenyl]thiourea
231	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	489 (M + H)	2
	N′-[4-(trifluoromethyl)phenyl]thiourea
232	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	521 (M + H)	3
	N′-{4-[(trifluoromethyl)thio]phenyl}thiourea
233	N-(4-bromo-2-chlorophenyl)-N′-(cis-4-{[4-	533 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
234	N-(4-bromo-2-fluorophenyl)-N′-(cis-4-{[4-	517 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
235	N-[4-chloro-3-(trifluoromethyl)phenyl]-N′-(cis-4-{[4-	523 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
236	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	507 (M + H)	3
	N′-[4-fluoro-3-(trifluoromethyl)phenyl]thiourea
237	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	547 (M + H)	1
	N′-(4-iodophenyl)thiourea
238	N-(5-chloro-2-methylphenyl)-N′-(cis-4-{[4-	469 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
239	N-[(1S,4R)-bicyclo[2,2,1]hept-2-yl]-N′-(cis-4-{[4-	439 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
240	tert-butyl [4-({[(cis-4-{[4-(dimethylamino)quinazolin-2-	536 (M + H)	3
	yl]amino}cyclohexyl)amino]carbonothioyl}amino)phenyl]-
	carbamate
241	N-[2-(3,4-dimethoxyphenyl)ethyl]-N′-(cis-4-{[4-	509 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
242	N-[2-(4-chlorophenyl)ethyl]-N′-(cis-4-{[4-	483 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
243	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	557 (M + H)	3
	N′-(2,3,4,5-tetrachlorophenyl)thiourea
244	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	523 (M + H)	3
	N′-(2,4,5-trichlorophenyl)thiourea
245	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	654 (M + H)	1
	N′-(2,4,6-tribromophenyl)thiourea
246	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	523 (M + H)	1
	N′-(2,4,6-trichlorophenyl)thiourea
247	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	475 (M + H)	3
	N′-(2,4,6-trifluorophenyl)thiourea
248	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	463 (M + H)	1
	N′-mesitylthiourea
249	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	449 (M + H)	1
	N′-(2,4-dimethylphenyl)thiourea
250	N-(2,6-diethylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	477 (M + H)	1
	2-yl]amino}cyclohexyl)thiourea
251	N-(2,6-diisopropylphenyl)-N′-(cis-4-{[4-	505 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
252	N-(2-bromo-4-methylphenyl)-N′-(cis-4-{[4-	513 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
253	N-[2-chloro-5-(trifluoromethyl)phenyl]-N′-(cis-4-{[4-	523 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
254	N-(2-chlorobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	469 (M + H)	1
	yl]amino}cyclohexyl)thiourea
255	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	463 (M + H)	1
	N′-(2-ethyl-6-methylphenyl)thiourea
256	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	463 (M + H)	1
	N′-(2-isopropylphenyl)thiourea
257	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	467 (M + H)	3
	N′-[3-(methylthio)phenyl]thiourea
258	N-(3,4-dichlorobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	503 (M + H)	3
	2-yl]amino}cyclohexyl)thiourea
259	N-(3,5-dimethoxyphenyl)-N′-(cis-4-{[4-	481 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
260	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	449 (M + H)	2
	N′-(3,5-dimethylphenyl)thiourea
261	N-[3-(benzyloxy)phenyl]-N′-(cis-4-{[4-	527 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-thiourea
262	N-(3-chloro-4-methylphenyl)-N′-(cis-4-{[4-	469 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
263	methyl 3-({[(cis-4-{[4-(dimethylamino)quinazolin-2-	479 (M + H)	1
	yl]amino}cyclohexyl)amino]carbonothioyl}amino)benzoate
264	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	463 (M + H)	3
	N′-(3-phenylpropyl)thiourea
265	N-[4-(benzyloxy)phenyl]-N′-(cis-4-{[4-	527 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
266	N-(4-bromo-2,6-dimethylphenyl)-N′-(cis-4-{[4-	527 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
267	N-(4-bromo-2-methylphenyl)-N′-(cis-4-{[4-	513 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
268	N-[4-bromo-2-(trifluoromethyl)phenyl]-N′-(cis-4-{[4-	567 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
269	N-(4-chloro-2-methylphenyl)-N′-(cis-4-{[4-	469 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
270	N-(4-chloro-3-nitrophenyl)-N′-(cis-4-{[4-	500 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
271	N-(4-chlorobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	469 (M + H)	3
	yl]amino}cyclohexyl)thiourea
272	ethyl 4-({[(cis-4-{[4-(dimethylamino)quinazolin-2-	493 (M + H)	3
	yl]amino}cyclohexyl)amino]carbonothioyl}amino)benzoate
273	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	467 (M + H)	2
	N′-[1-(4-fluorophenyl)ethyl]thiourea
274	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	453 (M + H)	2
	N′-(4-fluorobenzyl)thiourea
275	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	463 (M + H)	2
	N′-(4-isopropylphenyl)thiourea
276	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	496 (M + H)	3
	N′-(4-methoxy-2-nitrophenyl)thiourea
277	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	465 (M + H)	2
	N′-(4-methoxybenzyl)thiourea
278	methyl 4-({[(cis-4-{[4-(dimethylamino)quinazolin-2-	479 (M + H)	2
	yl]amino}cyclohexyl)amino]carbonothioyl}amino)benzoate
279	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	480 (M + H)	3
	N′-(4-methyl-2-nitrophenyl)thiourea
280	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	449 (M + H)	3
	N′-(4-methylbenzyl)thiourea
281	N-(4-butylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	477 (M + H)	3
	yl]amino}cyclohexyl)thiourea
282	N-(5-chloro-2-methoxyphenyl)-N′-(cis-4-{[4-	485 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
283	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	449 (M + H)	2
	N′-(1-phenylethyl)thiourea
284	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	511 (M + H)	2
	N′-(diphenylmethyl)thiourea
285	N-cyclododecyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	511 (M + H)	3
	yl]amino}cyclohexyl)thiourea
286	N-(cyclohexylmethyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	441 (M + H)	2
	2-yl]amino}cyclohexyl)thiourea
287	N-cyclooctyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	455 (M + H)	2
	yl]amino}cyclohexyl)thiourea
288	N-cyclopropyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	385 (M + H)	2
	yl]amino}cyclohexyl)thiourea
289	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	485 (M + H)	1
	N′-(1-naphthylmethyl)thiourea
290	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	525 (M + H)	2
	N′-(2,2-diphenylethyl)thiourea
291	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	557 (M + H)	3
	N′-(2,3,5,6-tetrachlorophenyl)thiourea
292	N-(2,3-dimethoxybenzyl)-N′-(cis-4-{[4-	495 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
293	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	463 (M + H)	1
	N′-(2,4,5-trimethylphenyl)thiourea
294	N-(2,4-dichlorobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	503 (M + H)	3
	2-yl]amino}cyclohexyl)thiourea
295	N-(2,5-dibromophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	577 (M + H)	3
	2-yl]amino}cyclohexyl)thiourea
296	N-[2-(2,5-dimethoxyphenyl)ethyl]-N′-(cis-4-{[4-	509 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
297	N-biphenyl-2-yl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	497 (M + H)	1
	yl]amino}cyclohexyl)thiourea
298	N-(2-chloro-5-nitrophenyl)-N′-(cis-4-{[4-	500 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
299	N-(2-cyanophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	446 (M + H)	3
	yl]amino}cyclohexyl)thiourea
300	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	453 (M + H)	2
	N′-(2-fluorobenzyl)thiourea
301	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	496 (M + H)	3
	N′-(2-methoxy-5-nitrophenyl)thiourea
302	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	480 (M + H)	1
	N′-(2-methyl-4-nitrophenyl)thiourea
303	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	449 (M + H)	2
	N′-(2-methylbenzyl)thiourea
304	N-(3,4-dimethoxybenzyl)-N′-(cis-4-{[4-	495 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
305	N-(3-chlorobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	469 (M + H)	1
	yl]amino}cyclohexyl)thiourea
306	ethyl 3-({[(cis-4-{[4-(dimethylamino)quinazolin-2-	493 (M + H)	1
	yl]amino}cyclohexyl)amino]carbonothioyl}amino)benzoate
307	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	449 (M + H)	2
	N′-(3-ethylphenyl)thiourea
308	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	453 (M + H)	2
	N′-(3-fluorobenzyl)thiourea
309	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	465 (M + H)	2
	N′-(3-methoxybenzyl)thiourea
310	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	449 (M + H)	2
	N′-(3-methylbenzyl)thiourea
311	N-(4-bromo-3-chlorophenyl)-N′-(cis-4-{[4-	533 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
312	N-(4-bromo-3-methylphenyl)-N′-(cis-4-{[4-	513 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
313	4-({[(cis-4-{[4-(dimethylamino)quinazolin-2-	465 (M + H)	3
	yl]amino}cyclohexyl)amino]carbonothioyl}amino)benzoic acid
314	N-[4-chloro-2-(trifluoromethyl)phenyl]-N′-(cis-4-{[4-	523 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
315	N-(4-decylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	561 (M + H)	3
	yl]amino}cyclohexyl)thiourea
316	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	453 (M + H)	1
	N′-(4-fluoro-2-methylphenyl)thiourea
317	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	558 (M + H)	3
	N′-[4-(4-nitrophenoxy)phenyl]thiourea
318	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	574 (M + H)	3
	N′-{4-[(4-nitrophenyl)thio]phenyl}thiourea
319	4-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	500 (M + H)	3
	cyclohexyl)amino]carbonothioyl}amino)benzenesulfonamide
320	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	465 (M + H)	1
	N′-(4-methoxy-2-methylphenyl)thiourea
321	N-{[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	479 (M + H)	3
	cyclohexyl)amino]carbonothioyl}-4-methoxybenzamide
322	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	463 (M + H)	3
	N′-[2-(4-methylphenyl)ethyl]thiourea
323	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	513 (M + H)	3
	N′-(4-phenoxyphenyl)thiourea
324	N-(5-chloro-2,4-dimethoxyphenyl)-N′-(cis-4-{[4-	515 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
325	N-(2,3-dihydro-1H-inden-5-yl)-N′-(cis-4-{[4-	461 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
326	(2E)-N-{[(cis-4-{[4-(dimethylamino)quinazolin-2-	475 (M + H)	3
	yl]amino}cyclohexyl)amino]carbonothioyl}-3-phenylacrylamide
327	N-[(2E)-but-2-en-1-yl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-	399 (M + H)	3
	2-yl]amino}cyclohexyl)thiourea
328	N-cycloheptyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	441 (M + H)	2
	yl]amino}cyclohexyl)thiourea
329	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	449 (M + H)	1
	N′-[(1R)-1-phenylethyl]thiourea
330	butyl 2-({[(cis-4-{[4-(dimethylamino)quinazolin-2-	505 (M + H)	3
	yl]amino}cyclohexyl)amino]carbonyl}amino)benzoate
331	dimethyl 5-({[(cis-4-{[4-(dimethylamino)quinazolin-2-	521 (M + H)	3
	yl]amino}cyclohexyl)amino]carbonyl}amino)isophthalate
332	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	489 (M + H)	3
	N′-[4-(trifluoromethoxy)phenyl]urea
333	N-(4-bromo-2,6-dimethylphenyl)-N′-(cis-4-{[4-	511 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
334	N-(4-bromo-2-methylphenyl)-N′-(cis-4-{[4-	497 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
335	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	535 (M + H)	3
	N′-(2,2,4,4-tetrafluoro-4H-1,3-benzodioxin-6-yl)urea
336	ethyl N-{[(cis-4-{[4-(dimethylamino)quinazolin-2-	505 (M + H)	1
	yl]amino}cyclohexyl)amino]carbonyl}phenylalaninate
337	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	439 (M + H)	2
	N′-[2-(2-thienyl)ethyl]urea
338	N-(2,3-dihydro-1,4-benzodioxin-6-yl)-N′-(cis-4-{[4-	463 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
339	N-(2,6-dibromo-4-isopropylphenyl)-N′-(cis-4-{[4-	603 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
340	N-(2-cyanophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	430 (M + H)	3
	yl]amino}cyclohexyl)urea
341	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	411 (M + H)	3
	N′-2-thienylurea
342	N-[3-(cyclopentyloxy)-4-methoxyphenyl]-N′-(cis-4-{[4-	519 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
343	N-(3,4-dihydro-2H-1,5-benzodioxepin-7-yl)-N′-(cis-4-{[4-	477 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
344	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	411 (M + H)	3
	N′-3-thienylurea
345	N-(4-tert-butylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	461 (M + H)	3
	2-yl]amino}cyclohexyl)urea
346	N-(4-butyl-2-methylphenyl)-N′-(cis-4-{[4-	475 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
347	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	477 (M + H)	1
	N′-[5-methyl-2-(trifluoromethyl)-3-furyl]urea
348	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	487 (M + H)	3
	N′-(5-phenyl-2-thienyl)urea
349	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	481 (M + H)	2
	N′-(6-fluoro-4H-1,3-benzodioxin-8-yl)urea
350	benzyl 4-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	546 (M + H)	3
	cyclohexyl)amino]carbonyl}amino)piperidine-1-carboxylate
351	N-[4-(dimethylamino)phenyl]-N′-(cis-4-{[4-	448 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
352	N-(2,6-dichloropyridin-4-yl)-N′-(cis-4-{[4-	474 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
353	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	424 (M + H)	2
	N′-(3,5-dimethylisoxazol-4-yl)urea
354	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	486 (M + H)	1
	N′-(3-methyl-5-phenylisoxazol-4-yl)urea
355	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	486 (M + H)	1
	N′-(5-methyl-3-phenylisoxazol-4-yl)urea
356	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	383 (M + H)	3
	N′-prop-2-yn-1-ylthiourea
357	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	568 (M + H)	3
	N′-[4-(piperidin-1-ylsulfonyl)phenyl]thiourea
358	N-(2-cyclohex-1-en-1-ylethyl)-N′-(cis-4-{[4-	453 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
359	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	449 (M + H)	1
	N′-(2,3-dimethylphenyl)thiourea
360	N-(2,4-dibromo-6-fluorophenyl)-N′-(cis-4-{[4-	595 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
361	N-(2,4-dichloro-6-methylphenyl)-N′-(cis-4-{[4-	503 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
362	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	449 (M + H)	2
	N′-(2,5-dimethylphenyl)thiourea
363	N-(2-bromo-4-isopropylphenyl)-N′-(cis-4-{[4-	541 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
364	N-(2-bromo-5-fluorophenyl)-N′-(cis-4-{[4-	517 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
365	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	465 (M + H)	1
	N′-(2-ethoxyphenyl)thiourea
366	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	477 (M + H)	1
	N′-(2-isopropyl-6-methylphenyl)thiourea
367	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	465 (M + H)	2
	N′-(2-methoxybenzyl)thiourea
368	N-(2,3-dihydro-1,4-benzodioxin-6-yl)-N′-(cis-4-{[4-	479 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
369	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	449 (M + H)	3
	N′-(3,4-dimethylphenyl)thiourea
370	N-1,3-benzodioxol-5-yl-N′-(cis-4-{[4-(dimethylamino)quinazolin-	465 (M + H)	1
	2-yl]amino}cyclohexyl)thiourea
371	N-(3-chloro-2-methylphenyl)-N′-(cis-4-{[4-	469 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
372	N-[4-bromo-2-(trifluoromethoxy)phenyl]-N′-(cis-4-{[4-	583 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
373	N-(4-chloro-2,5-dimethoxyphenyl)-N′-(cis-4-{[4-	515 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
374	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	477 (M + H)	2
	N′-(4-phenylbutyl)thiourea
375	N-(4-tert-butylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	477 (M + H)	3
	2-yl]amino}cyclohexyl)thiourea
376	N-(5-chloro-2-fluorophenyl)-N′-(cis-4-{[4-	473 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
377	N-bicyclo[2.2.1]hept-2-yl-N′-(cis-4-{[4-	439 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
378	N-bicyclo[2.2.1]hept-5-en-2-yl-N′-(cis-4-{[4-	437 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
379	N-(cyclopropylmethyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	399 (M + H)	3
	2-yl]amino}cyclohexyl)thiourea
380	ethyl 2-({[(cis-4-{[4-(dimethylamino)quinazolin-2-	553 (M + H)	3
	yl]amino}cyclohexyl)amino]carbonothioyl}amino)-4,5,6,7-
	tetrahydro-1-benzothiophene-3-carboxylate
381	methyl 3-({[(cis-4-{[4-(dimethylamino)quinazolin-2-	499 (M + H)	1
	yl]amino}cyclohexyl)amino]carbonothioyl}amino)-4-
	methylthiophene-2-carboxylate
382	methyl 3-({[(cis-4-{[4-(dimethylamino)quinazolin-2-	485 (M + H)	1
	yl]amino}cyclohexyl)amino]carbonothioyl}amino)thiophene-2-
	carboxylate
383	N-(2-bromo-4-fluorophenyl)-N′-(cis-4-{[4-	517 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
384	N-(3-chloro-4-fluorophenyl)-N′-(cis-4-{[4-	473 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
385	N-(4-butyl-2-methylphenyl)-N′-(cis-4-{[4-	491 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
386	N-[4-(dimethylamino)phenyl]-N′-(cis-4-{[4-	464 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
387	N-[3-(diethylamino)propyl]-N′-(cis-4-{[4-	458 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
388	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	458 (M + H)	3
	N′-(2-morpholin-4-ylethyl)thiourea
389	N-[4-(dimethylamino)-1-naphthyl]-N′-(cis-4-{[4-	514 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
390	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	422 (M + H)	3
	N′-pyridin-3-ylthiourea
391	N-(4-{(E)-[4-(dimethylamino)phenyl]diazenyl}phenyl)-N′-(cis-4-	568 (M + H)	3
	{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
392	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	472 (M + H)	3
	N′-(3-morpholin-4-ylpropyl)thiourea
393	N-[4-(diethylamino)phenyl]-N′-(cis-4-{[4-	492 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
394	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	525 (M + H)	3
	N′-{4-[(E)-phenyldiazenyl]phenyl}thiourea
395	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	456 (M + H)	3
	N′-(2-piperidin-1-ylethyl)thiourea
396	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	436 (M + H)	3
	N′-(pyridin-3-ylmethyl)thiourea
397	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	487 (M + H)	3
	N′-[4-(1H-pyrazol-1-yl)phenyl]thiourea
398	N-2,1,3-benzothiadiazol-4-yl-N′-(cis-4-{[4-	479 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
399	N-2,1,3-benzothiadiazol-5-yl-N′-(cis-4-{[4-	479 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea
400	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	440 (M + H)	3
	N′-(3,5-dimethylisoxazol-4-yl)thiourea
401	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	488 (M + H)	3
	N′-[4-(1,3-oxazol-5-yl)phenyl]thiourea
402	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	502 (M + H)	1
	N′-(5-methyl-3-phenylisoxazol-4-yl)thiourea
403	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	507 (M + H)	3
	N′-(6-morpholin-4-ylpyridin-3-yl)thiourea
404	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	514 (M + H)	3
	N′-(6-phenoxypyridin-3-yl)thiourea
405	N-(3-acetylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	461 (M + H)	3
	yl]amino}cyclohexyl)methyl]urea
406	N-1-adamantyl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	477 (M + H)	3
	yl]amino}cyclohexyl)methyl]urea
407	N-(4-acetylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	461 (M + H)	3
	yl]amino}cyclohexyl)methyl]urea
408	N-({[(cis-4-{[4-(dimethylamino)quinazolin-2-	447 (M + H)	3
	yl]amino}cyclohexyl)methyl]amino}carbonyl)benzamide
409	N-[3,5-bis(trifluoromethyl)phenyl]-N′-[(cis-4-{[4-	555 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
410	N-benzyl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	433 (M + H)	3
	yl]amino}cyclohexyl)methyl]urea
411	N-(2-bromophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	497 (M + H)	2
	yl]amino}cyclohexyl)methyl]urea
412	N-biphenyl-2-yl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	495 (M + H)	2
	yl]amino}cyclohexyl)methyl]urea
413	N-(4-bromophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	497 (M + H)	3
	yl]amino}cyclohexyl)methyl]urea
414	N-butyl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	399 (M + H)	2
	yl]amino}cyclohexyl)methyl]urea
415	N-(3-chlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	453 (M + H)	2
	yl]amino}cyclohexyl)methyl]urea
416	N-(4-chlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	453 (M + H)	3
	yl]amino}cyclohexyl)methyl]urea
417	N-cyclohexyl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	425 (M + H)	2
	yl]amino}cyclohexyl)methyl]urea
418	N-(3-cyanophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	444 (M + H)	2
	yl]amino}cyclohexyl)methyl]urea
419	N-(2-chlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	453 (M + H)	1
	yl]amino}cyclohexyl)methyl]urea
420	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	447 (M + H)	1
	yl]amino}cyclohexyl)methyl]-N′-(2,6-dimethylphenyl)urea
421	N-(3,4-dichlorophenyl)-N′-[(cis-4-{[4-	487 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
422	N-(2,4-difluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-	455 (M + H)	1
	2-yl]amino}cyclohexyl)methyl]urea
423	N-(2,4-dichlorophenyl)-N′-[(cis-4-{[4-	487 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
424	N-(3,5-dichlorophenyl)-N′-[(cis-4-{[4-	487 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
425	N-(2,3-dichlorophenyl)-N′-[(cis-4-{[4-	487 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
426	N-(2,6-difluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-	455 (M + H)	2
	2-yl]amino}cyclohexyl)methyl]urea
427	N-(2,5-dichlorophenyl)-N′-[(cis-4-{[4-	487 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
428	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	447 (M + H)	1
	yl]amino}cyclohexyl)methyl]-N′-(2,3-dimethylphenyl)urea
429	ethyl N-({[(cis-4-{[4-(dimethylamino)quinazolin-2-	429 (M + H)	3
	yl]amino}cyclohexyl)methyl]amino}carbonyl)glycinate
430	ethyl 3-[({[(cis-4-{[4-(dimethylamino)quinazolin-2-	491 (M + H)	3
	yl]amino}cyclohexyl)methyl]amino}carbonyl)amino]benzoate
431	ethyl 4-[({[(cis-4-{[4-(dimethylamino)quinazolin-2-	491 (M + H)	3
	yl]amino}cyclohexyl)methyl]amino}carbonyl)amino]benzoate
432	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	447 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(4-ethylphenyl)urea
433	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	371 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-ethylurea
434	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	461 (M + H)	1
	yl]amino}cyclohexyl)methyl]-N′-(2-ethyl-6-methylphenyl)urea
435	ethyl N-({[(cis-4-{[4-(dimethylamino)quinazolin-2-	485 (M + H)	1
	yl]amino}cyclohexyl)methyl]amino}carbonyl)leucinate
436	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	482 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(4-fluoro-3-nitrophenyl)urea
437	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	437 (M + H)	1
	yl]amino}cyclohexyl)methyl]-N′-(4-fluorophenyl)urea
438	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	437 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(3-fluorophenyl)urea
439	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	437 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(2-fluorophenyl)urea
440	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	461 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(4-isopropylphenyl)urea
441	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexylmethyl]-	501 (M + H)	2
	N′-[1-(3-isopropenylphenyl)-1-methylethyl]urea
442	methyl N-({[(cis-4-{[4-(dimethylamino)quinazolin-2-	489 (M + H)	2
	yl]amino}cyclohexyl)methyl]amino}carbonyl)methioninate
443	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	385 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-isopropylurea
444	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	449 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(4-methoxyphenyl)urea
445	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	478 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(4-methyl-2-nitrophenyl)urea
446	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	449 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(2-methoxyphenyl)urea
447	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	449 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(3-methoxyphenyl)urea
448	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	465 (M + H)	1
	yl]amino}cyclohexyl)methyl]-N′-[4-(methylthio)phenyl]urea
449	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	463 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(4-methoxybenzyl)urea
450	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	469 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-1-naphthylurea
451	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	459 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-[(2S)-2-phenylcyclopropyl]urea
452	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	419 (M + H)	1
	yl]amino}cyclohexyl)methyl]-N′-phenylurea
453	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	511 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(4-phenoxyphenyl)urea
454	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	413 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-pentylurea
455	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	487 (M + H)	1
	yl]amino}cyclohexyl)methyl]-N′-[2-(trifluoromethyl)phenyl]urea
456	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	487 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-[3-(trifluoromethyl)phenyl]urea
457	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	433 (M + H)	1
	yl]amino}cyclohexyl)methyl]-N′-(4-methylphenyl)urea
458	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	461 (M + H)	1
	yl]amino}cyclohexyl)methyl]-N′-mesitylurea
459	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	433 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(3-methylphenyl)urea
460	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	433 (M + H)	1
	yl]amino}cyclohexyl)methyl]-N′-(2-methylphenyl)urea
461	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	497 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-[1-(1-naphthyl)ethyl]urea
462	methyl N-({[(cis-4-{[4-(dimethylamino)quinazolin-2-	505 (M + H)	3
	yl]amino}cyclohexyl)methyl]amino}carbonyl)phenylalaninate
463	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	521 (M + H)	1
	yl]amino}cyclohexyl)methyl]-N′-(2,4,6-trichlorophenyl)urea
464	N-(3-chloro-4-methylphenyl)-N′-[(cis-4-{[4-	467 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
465	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	447 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(1-phenylethyl)urea
466	1-[4-(4-Dimethylamino-quinazolin-2-ylamino)-	447 (M + H)	2
	cyclohexylmethyl]-3-(1-phenyl-ethyl)-urea
467	1-[4-(4-Dimethylamino-quinazolin-2-ylamino)-	497 (M + H)	2
	cyclohexylmethyl]-3-(1-naphthalen-1-yl-ethyl)-urea
468	N-(2,6-diisopropylphenyl)-N′-[(cis-4-{[4-	503 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
469	N-[2-(difluoromethoxy)phenyl]-N′-[(cis-4-{[4-	485 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
470	methyl 2-[({[(cis-4-{[4-(dimethylamino)quinazoalin-2-	477 (M + H)	3
	yl]amino}cyclohexyl)methyl]amino}carbonyl)amino]benzoate
471	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	465 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-[2-(methylthio)phenyl]urea
472	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	555 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(2,3,5,6-tetrachlorophenyl)urea
473	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	492 (M + H)	1
	cyclohexyl)-methyl]-N′-(2,3-dimethyl-6-nitrophenyl)urea
474	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	521 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(2,4,5-trichlorophenyl)urea
475	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	652 (M + H)	1
	yl]amino}cyclohexyl)methyl]-N′-(2,4,6-tribromophenyl)urea
476	N-(2,4-dibromo-6-fluorophenyl)-N′-[(cis-4-{[4-	593 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
477	N-(2,4-dibromophenyl)-N′-[(cis-4-{[4-	575 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
478	N-(2,4-dichlorobenzyl)-N′-[(cis-4-{[4-	501 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
479	N-(2,4-dimethoxyphenyl)-N′-[(cis-4-{[4-	479 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
480	N-(2,5-dimethylphenyl)-N′-[(cis-4-{[4-	479 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
481	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	447 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(2,5-dimethylphenyl)urea
482	N-(2,6-dibromo-4-fluorophenyl)-N′-[(cis-4-{[4-	593 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
483	N-(2,6-dichlorophenyl)-N′-[(cis-4-{[4-	487 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
484	N-(2,6-diethylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-	475 (M + H)	1
	2-yl]amino}cyclohexyl)methyl]urea
485	N-(2-benzylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	509 (M + H)	3
	yl]amino}cyclohexyl)methyl]urea
486	N-(2-chloro-5-methylphenyl)-N′-[(cis-4-{[4-	467 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
487	N-(2-chloro-5-nitrophenyl)-N′-[(cis-4-{[4-	498 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
488	N-[2-chloro-6-(trifluoromethyl)phenyl]-N′-[(cis-4-{[4-	521 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
489	N-(2-chloro-6-methylphenyl)-N′-[(cis-4-{[4-	467 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
490	N-(2-chlorobenzyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	467 (M + H)	1
	yl]amino}cyclohexyl)methyl]urea
491	ethyl 2-[({[(cis-4-{[4-(dimethylamino)quinazolin-2-	491 (M + H)	3
	yl]amino}cyclohexyl)methyl]amino}carbonyl)amino]benzoate
492	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	463 (M + H)	?
	yl]amino}cyclohexyl)methyl]-N′-(2-ethoxyphenyl)urea
493	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	489 (M + H)	1
	yl]amino}cyclohexyl)methyl]-N′-(2-ethyl-6-isopropylphenyl)urea
494	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	447 (M + H)	1
	yl]amino}cyclohexyl)methyl]-N′-(2-ethylphenyl)urea
495	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	505 (M + H)	3
	cyclohexyl)methyl]-N′-[2-fluoro-3-(trifluoromethyl)phenyl]urea
496	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	505 (M + H)	3
	cyclohexyl)methyl]-N′-[2-fluoro-5-(trifluoromethyl)phenyl]urea
497	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	451 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(2-fluoro-5-methylphenyl)urea
498	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	482 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(2-fluoro-5-nitrophenyl)urea
499	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	451 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(2-fluorobenzyl)urea
500	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	545 (M + H)	1
	yl]amino}cyclohexyl)methyl]-N′-(2-iodophenyl)urea
501	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	475 (M + H)	1
	cyclohexyl)methyl]-N′-(2-isopropyl-6-methylphenyl)urea
502	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	461 (M + H)	1
	yl]amino}cyclohexyl)methyl]-N′-(2-isopropylphenyl)urea
503	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	494 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(2-methoxy-4-nitrophenyl)urea
504	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	463 (M + H)	1
	cyclohexyl)methyl]-N′-(2-methoxy-5-methylphenyl)urea
505	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	494 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(2-methoxy-5-nitrophenyl)urea
506	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	478 (M + H)	1
	yl]amino}cyclohexyl)methyl]-N′-(2-methyl-3-nitrophenyl)urea
507	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	478 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(2-methoxy-4-nitrophenyl)urea
508	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	478 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(2-methoxy-5-nitrophenyl)urea
509	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	478 (M + H)	1
	yl]amino}cyclohexyl)methyl]-N′-(2-methyl-6-nitrophenyl)urea
510	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	447 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(2-methylbenzyl)urea
511	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	469 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-2-naphthylurea
512	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	464 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(2-nitrophenyl)urea
513	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	461 (M + H)	1
	yl]amino}cyclohexyl)methyl]-N′-(2-propylphenyl)urea
514	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	511 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(2-phenoxyphenyl)urea
515	N-(2-tert-butyl-6-methylphenyl)-N′-[(cis-4-{[4-	489 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
516	N-(2-tert-butylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-	475 (M + H)	1
	2-yl]amino}cyclohexyl)methyl]urea
517	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	465 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-[3-(methylthio)phenyl]urea
518	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	519 (M + H)	3
	cyclohexyl)methyl]-N′-{3-[(trifluoromethyl)thio]phenyl}urea
519	N-1,3-benzodioxol-5-yl-N′-[(cis-4-{[4-	463 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
520	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	509 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(3,4,5-trimethoxyphenyl)urea
521	N-(3,4-dichlorobenzyl)-N′-[(cis-4-{[4-	501 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
522	N-(3,4-difluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-	455 (M + H)	1
	2-yl]amino}cyclohexyl)methyl]urea
523	N-(3,4-dimethoxyphenyl)-N′-[(cis-4-{[4-	479 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
524	N-(3,5-difluorobenzyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-	455 (M + H)	1
	2-yl]amino}cyclohexyl)methyl]urea
525	N-(3,5-dimethoxyphenyl)-N′-[(cis-4-{[4-	479 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
526	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	447 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(3,5-dimethylphenyl)urea
527	methyl 3-[({[(cis-4-{[4-(dimethylamino)quinazolin-2-	477 (M + H)	3
	yl]amino}cyclohexyl)methyl]amino}carbonyl)amino]benzoate
528	N-(3-chloro-2-methylphenyl)-N′-[(cis-4-{[4-	467 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
529	N-(3-chloro-4-fluorophenyl)-N′-[(cis-4-{[4-	471 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
530	N-(3-chloro-4-methoxyphenyl)-N′-[(cis-4-{[4-	483 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
531	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	447 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(3-ethylphenyl)urea
532	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	505 (M + H)	2
	cyclohexyl)methyl]-N′-[3-fluoro-5-(trifluoromethyl)phenyl]urea
533	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	451 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(3-fluorobenzyl)urea
534	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	511 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(3-phenoxyphenyl)urea
535	butyl 4-[({[(cis-4-{[4-(dimethylamino)quinazolin-2-	519 (M + H)	3
	yl]amino}cyclohexyl)methyl]amino}carbonyl)amino]benzoate
536	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	487 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-[4-(trifluoromethyl)phenyl]urea
537	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	519 (M + H)	3
	cyclohexyl)methyl]-N′-{4-[(trifluoromethyl)thio]phenyl}urea
538	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	492 (M + H)	2
	cyclohexyl)methyl]-N′-(4,5-dimethyl-2-nitrophenyl)urea
539	N-[4-(benzyloxy)phenyl]-N′-[(cis-4-{[4-	525 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
540	N-(4-benzylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	509 (M + H)	3
	yl]amino}cyclohexyl)methyl]urea
541	N-[4-bromo-2-(trifluoromethyl)phenyl]-N′-[(cis-4-{[4-	565 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
542	N-(4-bromo-2,6-difluorophenyl)-N′-[(cis-4-{[4-	533 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
543	N-(4-bromo-2-chlorophenyl)-N′-[(cis-4-{[4-	531 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
544	N-(4-bromobenzyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	511 (M + H)	3
	yl]amino}cyclohexyl)methyl]urea
545	N-[4-chloro-2-(trifluoromethyl)phenyl]-N′-[(cis-4-{[4-	521 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
546	N-(4-chloro-2-methylphenyl)-N′-[(cis-4-{[4-	467 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
547	N-(4-chloro-2-nitrophenyl)-N′-[(cis-4-{[4-	498 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
548	N-[4-chloro-3-(trifluoromethyl)phenyl]-N′-[(cis-4-{[4-	521 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
549	N-(4-cyanophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	444 (M + H)	1
	yl]amino}cyclohexyl)methyl]urea
550	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	463 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(4-ethoxyphenyl)urea
551	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	482 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(4-fluoro-2-nitrophenyl)urea
552	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	505 (M + H)	3
	cyclohexyl)methyl]-N′-[4-fluoro-3-(trifluoromethyl)phenyl]urea
553	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	451 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(4-fluorobenzyl)urea
554	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	533 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-[4-(heptyloxy)phenyl]urea
555	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	545 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(4-iodophenyl)urea
556	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	463 (M + H)	2
	cyclohexyl)methyl]-N′-(4-methoxy-2-methylphenyl)urea
557	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	494 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(4-methoxy-2-nitrophenyl)urea
558	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	478 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(4-methyl-3-nitrophenyl)urea
559	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	447 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(4-methylbenzyl)urea
560	N-(4-butoxyphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	491 (M + H)	3
	yl]amino}cyclohexyl)methyl]urea
561	N-(4-butylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	475 (M + H)	3
	yl]amino}cyclohexyl)methyl]urea
562	N-biphenyl-4-yl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	495 (M + H)	3
	yl]amino}cyclohexyl)methyl]urea
563	N-(5-chloro-2,4-dimethoxyphenyl)-N′-[(cis-4-{[4-	513 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
564	N-(5-chloro-2-methoxyphenyl)-N′-[(cis-4-{[4-	483 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
565	N-(5-chloro-2-methylphenyl)-N′-[(cis-4-{[4-	467 (M + H)	2
	(dimethylamino)quinazolin-3-yl]amino}cyclohexyl)methyl]urea
566	N-(5-chloro-2-nitrophenyl)-N′-[(cis-4-{[4-	498 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
567	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	451 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(5-fluoro-2-methylphenyl)urea
568	N-(2,3-dihydro-1H-inden-5-yl)-N′-[(cis-4-{[4-	459 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
569	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	507 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-9H-fluoren-2-ylurea
570	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	507 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-9H-fluoren-9-ylurea
571	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	447 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(2-phenylethyl)urea
572	N-cyclopentyl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	411 (M + H)	2
	yl]amino}cyclohexyl)methyl]urea
573	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	509 (M + H)	1
	yl]amino}cyclohexyl)methyl]-N′-(diphenylmethyl)urea
574	methyl 4-[({[(cis-4-{[4-(dimethylamino)quinazolin-2-	477 (M + H)	3
	yl]amino}cyclohexyl)methyl]amino}carbonyl)amino]benzoate
575	N-[1-(4-bromophenyl)ethyl]-N′-[(cis-4-{[4-	525 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
576	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	503 (M + H)	3
	cyclohexyl)methyl]-N′-[2-(trifluoromethoxy)phenyl]urea
577	N-(3-acetylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	477 (M + H)	3
	yl]amino}cyclohexyl)methyl]thiourea
578	N-(4-acetylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	477 (M + H)	3
	yl]amino}cyclohexyl)methyl]thiourea
579	N-[3,5-bis(trifluoromethyl)phenyl]-N′-[(cis-4-{[4-(dimethylamino)	571 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
580	N-benzyl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	449 (M + H)	3
	yl]amino}cyclohexyl)methyl]thiourea
581	N-(3-bromophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	513 (M + H)	3
	yl]amino}cyclohexyl)methyl]thiourea
582	N-(4-bromophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	513 (M + H)	3
	yl]amino}cyclohexyl)methyl]thiourea
583	N-butyl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	415 (M + H)	3
	yl]amino}cyclohexyl)methyl]thiourea
584	N-(4-cyanophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	460 (M + H)	3
	yl]amino}cyclohexyl)methyl]thiourea
585	N-cyclohexyl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	441 (M + H)	3
	yl]amino}cyclohexyl)methyl]thiourea
586	N-cyclopentyl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	427 (M + H)	3
	yl]amino}cyclohexyl)methyl]thiourea
587	N-(3-chlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	469 (M + H)	3
	yl]amino}cyclohexyl)methyl]thiourea
588	N-(4-chlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	469 (M + H)	3
	yl]amino}cyclohexyl)methyl]thiourea
589	N-(2,4-dichlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)-	503 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
590	N-(2,4-dimethoxyphenyl)-N′-[(cis-4-{[4-(dimethylamino)-	495 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
591	N-(2,5-difluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-	471 (M + H)	3
	2-yl]amino}cyclohexyl)methyl]thiourea
592	N-(2,5-dichlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)-	503 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
593	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	463 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(2,6-dimethylphenyl)thiourea
594	N-(3,4-dichlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)-	503 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
595	N-(2,6-dichlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)-	503 (M + H)	2
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
596	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	479 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(4-ethoxyphenyl)thiourea
597	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	505 (M + H)	2
	cyclohexyl)methyl]-N′-(2-ethyl-6-isopropylphenyl)thiourea
598	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	439 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(2-furylmethyl)thiourea
599	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	453 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(4-fluorophenyl)thiourea
600	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	443 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-hexylthiourea
601	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	559 (M + H)	3
	cyclohexyl)methyl]-N′-[4-(trans-4-propylcyclohexyl)phenyl]-
	thiourea
602	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	415 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-isobutylthiourea
603	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	541 (M + H)	3
	cyclohexyl)methyl]-N′-(4-methoxybiphenyl-3-yl)thiourea
604	N-(1,3-benzodioxol-5-ylmethyl)-N′-[(cis-4-{[4-(dimethylamino)-	493 (M + H)	2
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
605	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	449 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(3-methylphenyl)thiourea
606	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	481 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-[4-(methylthio)phenyl]thiourea
607	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	465 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(4-methoxyphenyl)thiourea
608	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	413 (M + H)	3
	cyclohexyl)methyl]-N′-(2-methylprop-2-en-1-yl)thiourea
609	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	465 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(2-methoxyphenyl)thiourea
610	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	373 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-methylthiourea
611	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	485 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-1-naphthylthiourea
612	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	480 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(3-nitrophenyl)thiourea
613	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	480 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(4-nitrophenyl)thiourea
614	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	471 (M + H)	3
	cyclohexyl)methyl]-N′-(1,1,3,3-tetramethylbutyl)thiourea
615	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	435 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-phenylthiourea
616	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	525 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(pentafluorophenyl)thiourea
617	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	401 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-propylthiourea
618	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	503 (M + H)	3
	cyclohexyl)methyl]-N′-[3-(trifluoromethyl)phenyl]thiourea
619	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	525 (M + H)	3
	cyclohexyl)methyl]-N′-(3,4,5-trimethoxyphenyl)thiourea
620	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	443 (M + H)	2
	cyclohexyl)methyl]-N′-(tetrahydrofuran-2-ylmethyl)thiourea
621	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	449 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(4-methylphenyl)thiourea
622	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	449 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(2-methylphenyl)thiourea
623	N-(tert-butyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	415 (M + H)	3
	yl]amino}cyclohexyl)methyl]thiourea
624	N-1-adamantyl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	493 (M + H)	3
	yl]amino}cyclohexyl)methyl]thiourea
625	N-(2-bromophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	513 (M + H)	3
	yl]amino}cyclohexyl)methyl]thiourea
626	N-(2-chlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	469 (M + H)	3
	yl]amino}cyclohexyl)methyl]thiourea
627	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	463 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(2-phenylethyl)thiourea
628	N-(3,4-dimethoxyphenyl)-N′-[(cis-4-{[4-(dimethylamino)-	495 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
629	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	463 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(4-ethylphenyl)thiourea
630	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	481 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-[2-(methylthio)phenyl]thiourea
631	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	519 (M + H)	2
	cyclohexyl)methyl]-N′-[2-(trifluoromethoxy)phenyl]thiourea
632	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	503 (M + H)	3
	cyclohexyl)methyl]-N′-[2-(trifluoromethyl)phenyl]thiourea
633	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	489 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(2,3,4-trifluorophenyl)thiourea
634	N-(2,3-dichlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)-	503 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
635	N-(2,4-difluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-	471 (M + H)	3
	2-yl]amino}cyclohexyl)methyl]thiourea
636	N-(2,5-dimethoxyphenyl)-N′-[(cis-4-{[4-(dimethylamino)-	495 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
637	N-(2,6-difluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-	471 (M + H)	3
	2-yl]amino}cyclohexyl)methyl]thiourea
638	N-(2-chloro-4-nitrophenyl)-N′-[(cis-4-{[4-(dimethylamino)-	514 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
639	N-[2-(difluoromethoxy)phenyl]-N′-[(cis-4-{[4-(dimethylamino)-	501 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
640	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	463 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(2-ethylphenyl)thiourea
641	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	521 (M + H)	3
	cyclohexyl)methyl]-N′-[2-fluoro-5-(trifluoromethyl)phenyl]-
	thiourea
642	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	453 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(2-fluorophenyl)thiourea
643	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	561 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(2-iodophenyl)thiourea
644	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	510 (M + H)	3
	cyclohexyl)methyl]-N′-(2-methoxy-4-nitrophenyl)thiourea
645	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	479 (M + H)	3
	cyclohexyl)methyl]-N′-(2-methoxy-5-methylphenyl)thiourea
646	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	535 (M + H)	3
	cyclohexyl)methyl]-N′-{3-[(trifluoromethyl)thio]phenyl}thiourea
647	N-(3,5-dichlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)-	503 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
648	N-(3,5-difluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-	471 (M + H)	3
	2-yl]amino}cyclohexyl)methyl]thiourea
649	N-(3-ciyanophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	460 (M + H)	3
	yl]amino}cyclohexyl)methyl]thiourea
650	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	453 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(3-fluorophenyl)thiourea
651	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	561 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(3-iodophenyl)thiourea
652	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	465 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(3-methoxyphenyl)thiourea
653	N-[4-(difluoromethoxy)phenyl]-N′-[(cis-4-{[4-(dimethylamino)-	501 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
654	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	519 (M + H)	3
	cyclohexyl)methyl]-N′-[4-(trifluoromethoxy)phenyl]thiourea
655	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	503 (M + H)	3
	cyclohexyl)methyl]-N′-[4-(trifluoromethyl)phenyl]thiourea
656	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	535 (M + H)	3
	cyclohexyl)methyl]-N′-{4-[(trifluoromethyl)thio]phenyl}thiourea
657	N-(4-bromo-2-chlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)-	547 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
658	N-(4-bromo-2-fluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)-	531 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
659	N-[4-chloro-3-(trifluoromethyl)phenyl]-N′-[(cis-4-{[4-(dimethylamino)	537 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
660	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)	521 (M + H)	3
	methyl]-N′-[4-fluoro-3-(trifluoromethyl)phenyl]thiourea
661	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	561 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(4-iodophenyl)thiourea
662	N-(5-chloro-2-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)-	483 (M + H)	2
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
663	N-[(1S,4R)-bicyclo[2.2.1]hept-2-yl]-N′-[(cis-4-{[4-(dimethylamino)	453 (M + H)	2
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
664	tert-butyl {4-[({[(cis-4-{[4-(dimethylamino)quinazolin-2-	550 (M + H)	3
	yl]amino}cyclohexyl)methyl]amino}carbonothioyl)amino]phenyl}-
	carbamate
665	N-[2-(3,4-dimethoxyphenyl)ethyl]-N′-[(cis-4-{[4-(dimethylamino)	523 (M + H)	2
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
666	N-[2-(4-chlorophenyl)ethyl]-N′-[(cis-4-{[4-(dimethylamino)-	497 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
667	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	571 (M + H)	3
	cyclohexyl)methyl]-N′-(2,3,4,5-tetrachlorophenyl)thiourea
668	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	537 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(2,4,5-trichlorophenyl)thiourea
669	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	668 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(2,4,6-tribromophenyl)thiourea
670	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	537 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(2,4,6-trichlorophenyl)thiourea
671	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	489 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(2,4,6-trifluorophenyl)thiourea
672	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	477 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-mesitylthiourea
673	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	463 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(2,4-dimethylphenyl)thiourea
674	N-(2,6-diethylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-	491 (M + H)	1
	2-yl]amino}cyclohexyl)methyl]thiourea
675	N-(2,6-diisopropylphenyl)-N′-[(cis-4-{[4-(dimethylamino)-	519 (M + H)	2
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
676	N-(2-bromo-4-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)-	527 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
677	N-[2-chloro-5-(trifluoromethyl)phenyl]-N′-[(cis-4-{[4-(dimethylamino)	537 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
678	N-(2-chlorobenzyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	483 (M + H)	3
	yl]amino}cyclohexyl)methyl]thiourea
679	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	477 (M + H)	2
	cyclohexyl)methyl]-N′-(2-ethyl-6-methylphenyl)thiourea
680	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	477 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(2-isopropylphenyl)thiourea
681	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	481 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-[3-(methylthio)phenyl]thiourea
682	N-(3,4-dichlorobenzyl)-N′-[(cis-4-{[4-(dimethylamino)-	517 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
683	N-(3,5-dimethoxyphenyl)-N′-[(cis-4-{[4-(dimethylamino)-	495 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
684	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	463 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(3,5-dimethylphenyl)thiourea
685	N-[3-(benzyloxy)phenyl]-N′-[(cis-4-{[4-(dimethylamino)-	541 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
686	3-[({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	479 (M + H)	3
	cyclohexyl)methyl]amino}carbonothioyl)amino]benzoic acid
687	N-(3-chloro-4-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)-	483 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
688	methyl 3-[({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	493 (M + H)	3
	cyclohexyl)methyl]amino}carbonothioyl)amino]benzoate
689	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	477 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(3-phenylpropyl)thiourea
690	N-[4-(benzyloxy)phenyl]-N′-[(cis-4-{[4-(dimethylamino)-	541 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
691	N-(4-bromo-2,6-dimethylphenyl)-N′-[(cis-4-{[4-(dimethylamino)	541 (M + H)	1
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
692	N-(4-bromo-2-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)-	527 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
693	N-[4-bromo-2-(trifluoromethyl)phenyl]-N′-[(cis-4-{[4-(dimethylamino)	581 (M + H)	2
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
694	N-(4-chloro-2-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)-	483 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
695	N-(4-chlorobenzyl)-N′-[(cis-4-([4-(dimethylamino)quinazolin-2-	483 (M + H)	3
	yl]amino)cyclohexyl)methyl]thiourea
696	ethyl 4-[({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	507 (M + H)	3
	cyclohexyl)methyl]amino}carbonothioyl)amino]benzoate
697	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	481 (M + H)	2
	cyclohexyl)methyl]-N′-[1-(4-fluorophenyl)ethyl]thiourea
698	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	467 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(4-fluorobenzyl)thiourea
699	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	477 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(4-isopropylphenyl)thiourea
700	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	510 (M + H)	3
	cyclohexyl)methyl]-N′-(4-methoxy-2-nitrophenyl)thiourea
701	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	479 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(4-methoxybenzyl)thiourea
702	methyl 4-[({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	493 (M + H)	3
	cyclohexyl)methyl]amino}carbonothioyl)amino]benzoate
703	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	494 (M + H)	3
	cyclohexyl)methyl]-N′-(4-methyl-2-nitrophenyl)thiourea
704	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	463 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(4-methylbenzyl)thiourea
705	N-(4-butylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	491 (M + H)	3
	yl]amino}cyclohexyl)methyl]thiourea
706	N-(5-chloro-2-methoxyphenyl)-N′-[(cis-4-{[4-(dimethylamino)-	499 (M + H)	2
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
707	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	463 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(1-phenylethyl)thiourea
708	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	525 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(diphenylmethyl)thiourea
709	N-cyclododecyl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	525 (M + H)	2
	yl]amino}cyclohexyl)methyl]thiourea
710	N-(cyclohexylmethyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-	455 (M + H)	2
	2-yl]amino}cyclohexyl)methyl]thiourea
711	N-cyclooctyl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	469 (M + H)	3
	yl]amino}cyclohexyl)methyl]thiourea
712	N-cyclopropyl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	399 (M + H)	3
	yl]amino}cyclohexyl)methyl]thiourea
713	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	499 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(1-naphthylmethyl)thiourea
714	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	539 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(2,2-diphenylethyl)thiourea
715	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	571 (M + H)	1
	cyclohexyl)methyl]-N′-(2,3,5,6-tetrachlorophenyl)thiourea
716	N-(2,3-dimethoxybenzyl)-N′-[(cis-4-{[4-(dimethylamino)-	509 (M + H)	2
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
717	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	477 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(2,4,5-trimethylphenyl)thiourea
718	N-(2,4-dichlorobenzyl)-N′-[(cis-4-{[4-(dimethylamino)-	517 (M + H)	2
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
719	N-(2,5-dibromophenyl)-N′-[(cis-4-{[4-(dimethylamino)-	591 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
720	N-[2-(2,5-dimethoxyphenyl)ethyl]-N′-[(cis-4-{[4-(dimethylamino)	523 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
721	N-biphenyl-2-yl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	511 (M + H)	3
	yl]amino}cyclohexyl)methyl]thiourea
722	N-(2-chloro-5-nitrophenyl)-N′-[(cis-4-{[4-(dimethylamino)-	514 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
723	N-(2-cyanophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	460 (M + H)	3
	yl]amino}cyclohexyl)methyl]thiourea
724	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	467 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(2-fluorobenzyl)thiourea
725	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	510 (M + H)	2
	cyclohexyl)methyl]-N′-(2-methoxy-5-nitrophenyl)thiourea
726	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	494 (M + H)	3
	cyclohexyl)methyl]-N′-(2-methyl-4-nitrophenyl)thiourea
727	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	463 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(2-methylbenzyl)thiourea
728	N-(3,4-dimethoxybenzyl)-N′-[(cis-4-{[4-(dimethylamino)-	509 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
729	N-(3-chlorobenzyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	483 (M + H)	3
	yl]amino}cyclohexyl)methyl]thiourea
730	ethyl 3-[({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	507 (M + H)	3
	cyclohexyl)methyl]amino}carbonothioyl)amino]benzoate
731	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	463 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(3-ethylphenyl)thiourea
732	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	467 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(3-fluorobenzyl)thiourea
733	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	479 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(3-methoxybenzyl)thiourea
734	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	463 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(3-methylbenzyl)thiourea
735	N-(4-bromo-3-chlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)-	547 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
736	N-(4-bromo-3-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)-	527 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
737	N-[4-chloro-2-(trifluoromethyl)phenyl]-N′-[(cis-4-{[4-(dimethylamino)	537 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
738	N-(4-decylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	575 (M + H)	3
	yl]amino}cyclohexyl)methyl]thiourea
739	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	467 (M + H)	3
	cyclohexyl)methyl]-N′-(4-fluoro-2-methylphenyl)thiourea
740	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	572 (M + H)	3
	cyclohexyl)methyl]-N′-[4-(4-nitrophenoxy)phenyl]thiourea
741	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	588 (M + H)	3
	cyclohexyl)methyl]-N′-{4-[(4-nitrophenyl)thio]phenyl}thiourea
742	4-[({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	514 (M + H)	3
	cyclohexyl)methyl]amino}carbonothioyl)amino]benzenesulfonamide
743	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	479 (M + H)	2
	cyclohexyl)methyl]-N′-(4-methoxy-2-methylphenyl)thiourea
744	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	477 (M + H)	3
	cyclohexyl)methyl]-N′-[2-(4-methylphenyl)ethyl]thiourea
745	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	527 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(4-phenoxyphenyl)thiourea
746	N-(5-chloro-2,4-dimethoxyphenyl)-N′-[(cis-4-{[4-(dimethylamino)	529 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
747	N-(2,3-dihydro-1H-inden-5-yl)-N′-[(cis-4-{[4-(dimethylamino)	475 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
748	N-cycloheptyl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	455 (M + H)	3
	yl]amino}cyclohexyl)methyl]thiourea
749	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	463 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-[(1R)-1-phenylethyl]thiourea
750	butyl 2-[({[(cis-4-{[4-(dimethylamino)quinazolin-2-	519 (M + H)	3
	yl]amino}cyclohexyl)methyl]amino}carbonyl)amino]benzoate
751	dimethyl 5-[({[(cis-4-{[4-(dimethylamino)quinazolin-2-	535 (M + H)	3
	yl]amino}cyclohexyl)methyl]amino}carbonyl)amino]isophthalate
752	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	503 (M + H)	3
	cyclohexyl)methyl]-N′-[4-(trifluoromethoxy)phenyl]urea
753	N-(4-bromo-2,6-dimethylphenyl)-N′-[(cis-4-{[4-	525 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
754	N-(4-bromo-2-methylphenyl)-N′-[(cis-4-{[4-	511 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
755	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	549 (M + H)	3
	cyclohexyl)methyl]-N′-(2,2,4,4,-tetrafluoro-4H-1,3-benzodioxin-
	6-yl)urea
756	ethyl N-({[(cis-4-{[4-(dimethylamino)quinazolin-2-	519 (M + H)	3
	yl]amino}cyclohexyl)methyl]amino}carbonyl)phenylalaninate
757	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	453 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-[2-(2-thienyl)ethyl]urea
758	N-(2,3-dihydro-1,4-benzodioxin-6-yl)-N′-[(cis-4-{[4-	477 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
759	N-(2,6-dibromo-4-isopropylphenyl)-N′-[(cis-4-{[4-	617 (M + H)	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
760	N-(2-cyanophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	444 (M + H)	3
	yl]amino}cyclohexyl)methyl]urea
761	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	425 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-2-thienylurea
762	N-[3-(cyclopentyloxy)-4-methoxyphenyl]-N′-[(cis-4-{[4-	533 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
763	N-(3,4-dihydro-2H-1,5-benzodioxepin-7-yl)-N′-[(cis-4-{[4-	491 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
764	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	425 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-3-thienylurea
765	N-(4-tert-butylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-	475 (M + H)	3
	2-yl]amino}cyclohexyl)methyl]urea
766	N-(4-butyl-2-methylphenyl)-N′-[(cis-4-{[4-	489 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
767	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)	491 (M + H)	1
	methyl]-N′-[5-methyl-2-(trifluoromethyl)-3-furyl]urea
768	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	501 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(5-phenyl-2-thienyl)urea
769	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)	495 (M + H)	2
	methyl]-N′-(6-fluoro-4H-1,3-benzodioxin-8-yl)urea
770	benzyl 4-[({[(cis-4-{[4-(dimethylamino)quinazolin-2-	560 (M + H)	3
	yl]amino}cyclohexyl)methyl]amino}carbonyl)amino]piperidine-
	1-carboxylate
771	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	566 (M + H)	3
	cyclohexyl)methyl]-N′-[4-(6-methyl-1,3-benzothiazol-2-yl)-
	phenyl]urea
772	N-[4-(dimethylamino)phenyl]-N′-[(cis-4-{[4-	462 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
773	N-(2,6-dichloropyridin-4-yl)-N′-[(cis-4-{[4-	488 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
774	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	438 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(3,5-dimethylisoxazol-4-yl)urea
775	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	500 (M + H)	1
	cyclohexyl)methyl]-N′-(3-methyl-5-phenylisoxazol-4-yl)urea
776	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	500 (M + H)	2
	cyclohexyl)methyl]-N′-(5-methyl-3-phenylisoxazol-4-yl)urea
777	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	397 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-prop-2-yn-1-ylthiourea
778	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	582 (M + H)	3
	cyclohexyl)methyl]-N′-[4-(piperidin-1-ylsulfonyl)phenyl]thiourea
779	N-(2-cyclohex-1-en-1-ylethyl)-N′-[(cis-4-{[4-(dimethylamino)-	467 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
780	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	463 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(2,3-dimethylphenyl)thiourea
781	N-(2,4-dibromo-6-fluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)	609 (M + H)	2
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
782	N-(2,4-dichloro-6-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)	517 (M + H)	2
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
783	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	463 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(2,5-dimethylphenyl)thiourea
784	N-(2-bromo-4-isopropylphenyl)-N′-[(cis-4-{[4-(dimethylamino)	555 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
785	N-(2-bromo-5-fluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)-	531 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
786	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	479 (M + H)	2
	yl]amino}cyclohexyl)methyl]-N′-(2-ethoxyphenyl)thiourea
787	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	491 (M + H)	1
	cyclohexyl)methyl]-N′-(2-isopropyl-6-methylphenyl)thiourea
788	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	479 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(2-methoxybenzyl)thiourea
789	N-(2,3-dihydro-1,4-benzodioxin-6-yl)-N′-[(cis-4-{[4-(dimethylamino)	493 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
790	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	463 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(3,4-dimethylphenyl)thiourea
791	N-1,3-benzodioxol-5-yl-N′-[(cis-4-{[4-(dimethylamino)-	479 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
792	N-(3-chloro-2-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)-	483 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
793	N-[4-bromo-2-(trifluoromethoxy)phenyl]-N′-[(cis-4-{[4-	597 (M + H)	2
	(dimethyl-amino)quinazolin-2-yl]amino}cyclohexyl)methyl]-
	thiourea
794	N-(4-chloro-2,5-dimethoxyphenyl)-N′-[(cis-4-{[4-(dimethylamino)	529 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
795	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	491 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(4-phenylbutyl)thiourea
796	N-(4-tert-butylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-	491 (M + H)	3
	2-yl]amino}cyclohexyl)methyl]thiourea
797	N-(5-choloro-2-fluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)-	487 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
798	N-bicyclo[2.2.1]hept-2-yl-N′-[(cis-4-{[4-(dimethylamino)-	453 (M + H)	2
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
799	N-bicyclo[2.2.1]hept-5-en-2-yl-N′-[(cis-4-{[4-(dimethylamino)	451 (M + H)	2
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
800	N-(cyclopropylmethyl)-N′-[(cis-4-{[4-(dimethylamino)-	413 (M + H)	2
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
801	ethyl 2-[({[(cis-4-{[4-(dimethylamino)quinazolin-2-	567 (M + H)	3
	yl]amino}cyclohexyl)methyl]amino}carbonothioyl)amino]-
	4.5.6.7-tetrahydro-1-benzothiophene-3-carboxylate
802	methyl 3-[({[(cis-4-{[4-(dimethylamino)quinazolin-2-	499 (M + H)	3
	yl]amino}cyclohexyl)methyl]amino}carbonothioyl)amino]-
	thiophene-2-carboxylate
803	N-(2-bromo-4-fluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)-	531 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
804	N-(3-chloro-4-fluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)-	487 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
805	N-(4-butyl-2-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)-	505 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
806	N-[4-(dimethylamino)phenyl]-N′-[(cis-4-{[4-(dimethylamino)-	478 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
807	N-[3-(dimethylamino)propyl]-N′-[(cis-4-{[4-(dimethylamino)-	472 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
808	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	472 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(2-morpholin-4-ylethyl)thiourea
809	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	436 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-pyridin-3-ylthiourea
810	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	486 (M + H)	3
	cyclohexyl)methyl]-N′-(3-morpholin-4-ylpropyl)thiourea
811	N-[4-(diethylamino)phenyl]-N′-[(cis-4-{[4-(dimethylamino)-	506 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
812	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	539 (M + H)	3
	cyclohexyl)methyl]-N′-{4-[(E)-phenyldiazenyl]phenyl}thiourea
813	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	470 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(2-piperidin-1-ylethyl)thiourea
814	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	501 (M + H)	3
	cyclohexyl)methyl]-N′-[4-(1H-pyrazol-1-yl)phenyl]thiourea
815	N-2,1,3-benzothiadiazol-4-yl-N′-[(cis-4-{[4-(dimethylamino)-	493 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
816	N-2,1,3-benzothiadiazol-5-yl-N′-[(cis-4-{[4-(dimethylamino)-	493 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea
817	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	454 (M + H)	3
	cyclohexyl)methyl]-N′-(3,5-dimethylisoxazol-4-yl)thiourea
818	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	502 (M + H)	3
	cyclohexyl)methyl]-N′-[4-(1,3-oxazol-5-yl)phenyl]thiourea
819	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	516 (M + H)	2
	cyclohexyl)methyl]-N′-(5-methyl-3-phenylisoxazol-4-yl)-
	thiourea
820	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	521 (M + H)	3
	cyclohexyl)methyl]-N′-(6-morpholin-4-ylpyridin-3-yl)thiourea
821	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	528 (M + H)	3
	yl]amino}cyclohexyl)methyl]-N′-(6-phenoxypyridin-3-yl)thiourea
822	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	468 (M + H)	2
	N′-(4-fluoro-2-nitrophenyl)urea
823	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	491 (M + H)	3
	N′-[4-fluoro-2-(trifluoromethyl)phenyl]urea
824	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	437 (M + H)	1
	N′-(4-fluorobenzyl)urea
825	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	519 (M + H)	3
	N′-[4-(heptyloxy)phenyl]urea
826	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	531 (M + H)	2
	N′-(4-iodophenyl)urea
827	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	449 (M + H)	1
	N′-(4-methoxy-2-methylphenyl)urea
828	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	480 (M + H)	3
	N′-(4-methoxy-2-nitrophenyl)urea
829	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	464 (M + H)	3
	N′-(4-methyl-3-nitrophenyl)urea
830	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	433 (M + H)	2
	N′-(4-methylbenzyl)urea
831	N-(4-butoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	477 (M + H)	3
	yl]amino}cyclohexyl)urea
832	N-(4-butylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	461 (M + H)	3
	yl]amino}cyclohexyl)urea
833	N-biphenyl-4-yl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	481 (M + H)	3
	yl]amino}cyclohexyl)urea
834	N-(5-chloro-2,4-dimethoxyphenyl)-N′-(cis-4-{[4-	499 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
835	N-(5-chloro-2-methoxyphenyl)-N′-(cis-4-{[4-	469 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
836	N-(5-chloro-2-methylphenyl)-N′-(cis-4-{[4-	453 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
837	N-(5-chloro-2-nitrophenyl)-N′-(cis-4-{[4-	484 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
838	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	437 (M + H)	2
	N′-(5-fluoro-2-methylphenyl)urea
839	N-(2,3-dihydro-1H-inden-5-yl)-N′-(cis-4-{[4-	445 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
840	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	493 (M + H)	3
	N′-9H-fluoren-9-ylurea
841	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclonexyl)-	493 (M + H)	2
	N′-9H-fluoren-9-ylurea
842	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclonexyl)-	433 (M + H)	2
	N′-(2-phenylethyl)urea
843	N-cyclophenyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	397 (M + H)	2
	yl]amino}cyclohexyl)urea
844	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	495 (M + H)	1
	N′-(diphenylmethyl)urea
845	methyl 4-({[(cis-4-{[4-(dimethylamino)quinazolin-2-	463 (M + H)	3
	yl]amino}cyclohexyl)amino]carbonyl}amino)benzoate
846	2-(benzyloxy)ethyl (cis-4-{[4-(dimethylamino)quinazolin-2-	464 (M + H)	2
	yl]amino}cyclohexyl)carbamate
847	2,2-dimethylpropyl (cis-4-{[4-(dimethylamino)quinazolin-2-	400 (M + H)	3
	yl]amino}cyclohexyl)carbamate
848	4,5-dimethoxy-2-nitrobenzyl (cis-4-{[4-	525 (M + H)	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)carbamate
849	3-(trifluoromethyl)phenyl (cis-4-{[4-(dimethylamino)quinazolin-	474 (M + H)	3
	2-yl]amino}cyclohexyl)carbamate
850	4-bromophenyl (cis-4-{[4-(dimethylamino)quinazolin-2-	484 (M + H)	3
	yl]amino}cyclohexyl)carbamate
851	2-methoxyphenyl (cis-4-{[4-(dimethylamino)quinazolin-2-	436 (M + H)	3
	yl]amino}cyclohexyl)carbamate
852	2-methoxyethyl (cis-4-{[4-(dimethylamino)quinazolin-2-	388 (M + H)	3
	yl]amino}cyclohexyl)carbamate
853	octyl (cis-4-{[4-(dimethylamino)quinazolin-2-	442 (M + H)	3
	yl]amino}cyclohexyl)carbamate
854	ethyl (cis-4-{[4-(dimethylamino)quinazolin-2-	358 (M + H)	3
	yl]amino}cyclohexyl)carbamate
855	4-nitrobenzyl (cis-4-{[4-(dimethylamino)quinazolin-2-	465 (M + H)	1
	yl]amino}cyclohexyl)carbamate
856	2-naphthyl (cis-4-{[4-(dimethylamino)quinazolin-2-	456 (M + H)	3
	yl]amino}cyclohexyl)carbamate
857	allyl (cis-4-{[4-(dimethylamino)quinazolin-2-	370 (M + H)	3
	yl]amino}cyclohexyl)carbamate
858	benzyl (cis-4-{[4-(dimethylamino)quinazolin-2-	420 (M + H)	2
	yl]amino}cyclohexyl)carbamate
859	phenyl (cis-4-{[4-(dimethylamino)quinazolin-2-	406 (M + H)	3
	yl]amino}cyclohexyl)carbamate
860	(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl (cis-4-{[4-	468 (M + H)	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)carbamate
861	4-methylphenyl (cis-4-{[4-(dimethylamino)quinazolin-2-	420 (M + H)	3
	yl]amino}cyclohexyl)carbamate
862	methyl (cis-4-{[4-(dimethylamino)quinazolin-2-	344 (M + H)	3
	yl]amino}cyclohexyl)carbamate
863	2-chlorobenzyl (cis-4-{[4-(dimethylamino)quinazolin-2-	454 (M + H)	2
	yl]amino}cyclohexyl)carbamate
864	9H-fluoren-9-ylmethyl (cis-4-{[4-(dimethylamino)quinazolin-2-	508 (M + H)	3
	yl]amino}cyclohexyl)carbamate
865	2,2,2-trichloroethyl (cis-4-{[4-(dimethylamino)quinazolin-2-	460 (M + H)	3
	yl]amino}cyclohexyl)carbamate
866	2-(benzyloxy)ethyl [(cis-4-{[4-(dimethylamino)quinazolin-2-	478 (M + H)	3
	yl]amino}cyclohexyl)methyl]carbamate
867	2,2-dimethylpropyl [(cis-4-{[4-(dimethylamino)quinazolin-2-	414 (M + H)	3
	yl]amino}cyclohexyl)methyl]carbamate
868	4,5-dimethoxy-2-nitrobenzyl [(cis-4-{[4-(dimethylamino)-	539 (M + H)	3
	quinazolin-2-yl]amino}cyclohexyl)methyl]carbamate
869	3-(trifluoromethyl)phenyl [(cis-4-{[4-(dimethylamino)quinazolin-	488 (M + H)	3
	2-yl]amino}cyclohexyl)methyl]carbamate
870	4-bromophenyl [(cis-4-{[4-(dimethylamino)quinazolin-2-	498 (M + H)	3
	yl]amino}cyclohexyl)methyl]carbamate
871	2-methoxyphenyl [(cis-4-{[4-(dimethylamino)quinazolin-2-	450 (M + H)	3
	yl]amino}cyclohexyl)methyl]carbamate
872	2-methoxyethyl [(cis-4-{[4-(dimethylamino)quinazolin-2-	402 (M + H)	3
	yl]amino}cyclohexyl)methyl]carbamate
873	octyl [(cis-4-{[4-(dimethylamino)quinazolin-2-	456 (M + H)	3
	yl]amino}cyclohexyl)methyl]carbamate
874	ethyl [(cis-4-{[4-(dimethylamino)quinazolin-2-	372 (M + H)	3
	yl]amino}cyclohexyl)methyl]carbamate
875	4-nitrobenzyl [(cis-4-{[4-(dimethylamino)quinazolin-2-	479 (M + H)	2
	yl]amino}cyclohexyl)methyl]carbamate
876	2-naphthyl [(cis-4-{[4-(dimethylamino)quinazolin-2-	470 (M + H)	3
	yl]amino}cyclohexyl)methyl]carbamate
877	allyl [(cis-4-{[4-(dimethylamino)quinazolin-2-	384 (M + H)	3
	yl]amino}cyclohexyl)methyl]carbamate
878	benzyl [(cis-4-{[4-(dimethylamino)quinazolin-2-	434 (M + H)	2
	yl]amino}cyclohexyl)methyl]carbamate
879	phenyl [(cis-4-{[4-(dimethylamino)quinazolin-2-	420 (M + H)	3
	yl]amino}cyclohexyl)methyl]carbamate
880	(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl [(cis-4-{[4-	482 (M + H)	3
	(dimethyl-amino)quinazolin-2-yl]amino}cyclohexyl)methyl]
	carbamate
881	4-methylphenyl [(cis-4-{[4-(dimethylamino)quinazolin-2-	434 (M + H)	3
	yl]amino}cyclohexyl)methyl]carbamate
882	methyl [(cis-4-{[4-(dimethylamino)quinazolin-2-	358 (M + H)	3
	yl]amino}cyclohexyl)methyl]carbamate
883	2-chlorobenzyl [(cis-4-{[4-(dimethylamino)quinazolin-2-	468 (M + H)	2
	yl]amino}cyclohexyl)methyl]carbamate
884	9H-fluoren-9-ylmethyl [(cis-4-{[4-(dimethylamino)quinazolin-2-	522 (M + H)	3
	yl]amino}cyclohexyl)methyl]carbamate
885	2,2,2-trichloroethyl [(cis-4-{[4-(dimethylamino)quinazolin-2-	474 (M + H)	3
	yl]amino}cyclohexyl)methyl]carbamate

Example 886

N-(cis-4-{[4-(dimethylamino)-6-methylquinazolin-2-yl]amino}cyclohexyl)-2,2-diphenylacetam idetrifluoroacetate

S Step A: Synthesis of 6-methyl-1H-quinazoline-2,4-dione

To a suspension of 2-amino-5-methylbenzoic acid (5.27 g, 0.035 mol) in 150 mL H₂O and 2 mL acetic acid was added potassium cyanate (3.67 g, 0.045 mol) predissolved in 30 mL H₂O. The reaction mixture was stirred for 5 hours and then 10 g NaOH pellets were added with continued stirring. The mixture was cooled to 0 ° C. in an ice bath and another 30 g, NaOH pellets were added. During the addition of NaOH a precipitate was formed. This precipitate was filtered and resuspended in 100 mL H₂O and 3M HCl was added by pipette until the aqueous solution was slightly acidic. The precipitate was then filtered and washed with ice cold H₂O to yield 6-methyl-1 H-quinazoluie-2,4-dione (2.2 g, 37%) as an off white solid. ESI-MS m/e 177.1 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 11.18 (s, 1H) 11.02 (s. 1 H), 7.66 (s, 1 H), 7.45 (d, J=8.4 Hz, 1 H), 7.05 (d, J=8.4 Hz, 1 H), 2.31 (s, 3H).

Step B: Synthesis of 2,4-dichloro-6-methyl-quinazoline

To a solution of 6-methyl-1 H-quinazoline-2.4-dione (2.29 g, 0.013 mol) in 20 mL POCl₃ was added N,N-dimethylaniline (1.81 mL, 0.014 mol). The mixture was heated to reflux (125 ° C.) and stirred for 4 hours until the starting material completely dissolved and the solution turned dark purple in color. The solution was then cooled and poured slowyl) on ice (40 g; catition highly exothennic) to quench the reaction. The aqueous layer was then extracted three times with CH₂Cl₂ (40 mL). The organic layer was dried over MgSO₄, concentrated, and subjected to purification b)y chromatography (100% CH₂Cl₂) to yield 2,4-dichloro-6-methyl-quinazolin (2.5 g,90 %) as a slightly yellow, solid. ¹ H NMR (400 MHz, DMSO-d₆) δ 8.05 (s, 1H), 8.01 (d, J=9.2 Hz, 1 H), 7.94 (d, J=8.8 Hz, 1 H), 2.57 (s. 3 H).

Step C: Synthesis of (2-chloro-6-methyl-quinazolin-4-yl)-dimethyl-amine

A solution of 2,4-dichloro-6-methyl-quinazoline (2.5 g, 0.012 mol) in CH₂Cl₂ (100 mL) was cooled on an ice bath with stirring. Dimethylamine (23.6 mL, 0.047 mol) was added slowly to the solution removed from the ice bath. The. mixture stirred for 1 hour and the excess solvents were evaporated. The compound was subject to purification by chromatography (100% CH₂Cl₂) to yield (2-chloro-6-methyl-quinazolin-4-yl)-dimethy-amine (2.4 g, 92%) as a white solid. ESI-MS m/e 222.2 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆), δ 7.06 (s, 1 H), 7.61 (d, J=8 Hz, 1 H). 7.54 (d, J=8.4 Hz, 1 H), 3.34 (brs. 6 H), 2.45 (s, 3 H).

Step D: Synthesis of cis-[4-(4-dimethylamino-6-methyl-quinazolin-2-ylamino)-cyclohexyl]-carbamic acid tert-butyl ester

To a solution of (2-chloro-6-methyl-quinazolin-4-yl)-dimethyl-amine (0.5 g, 0.0023 mol) in 0.5 mL 2-propanol was added of cis-(4-amino-cyclohexyl)-carbamic acid tert-butyl ester (483 mg, 0.0023 mol), and DIEA (786 uL, 0.0045 mol). The reaction mixture was heated in a microwave synthesizer at 170° C for 1 hour. The solvent was evaporated and the material subjected to chromatography (2-4% 2M NH₃ in MeOH/CH₂Cl₂) to yield cis-c4-(4-dimethylamino-6-methyl-quiazolin-2-ylamino)-cyclohexy]-carbamic acid tert-butyl ester (850 mg, 94%) as a white solid.

ESI-MS m/e 400.4 M+H⁺; ¹H NMR (400 MHz, CD₃OD) δ 7.68 (s, 1 H)7.37 (d, J=8.4 Hz, 1 H), 7.28 (d, J=8.4 Hz, 1 H), 4.05 (m, 1 H), 3.54 (brs, 1 H), 3.26 (s, 6 H), 2.38 (s, 3 H), 1.76-1.59 (m, 8 H), 1.44 (s, 9 H).

Step E: Synthesis of cis-N²-(4-amino-cyclohexyl)-6,N⁴,N⁴-trimethyl-quinazoline-2,3-diamine

To a solution of cis-[4-(4-dimethylamino-6-methyl-quinazolin-2-ylaminno)-cyclohexyl]-carbamic acid tert-butyl ester (850 mg, 0.0021 mol) in 30 mL CH₂Cl₂ was added TFA (325 uL, 0.042 mol). The solution was stirred at room temperature for 4 hours. The excess solvent was evaporated offand the resulting oil was dissolved in 30 mL CH₂Cl₂. The organic layer was extracted with 30 mL of a dilute NaOH (aq)/NaHCO₃ (aq) solution. The aqueous layer was back extracted twice with CH₂Cl, and the organic layers combined, dried over MgSO₄, and concentrated to yield cis-N²-(4-amino-cyclohexyl)-6,N⁴,N⁴-trimethyl-quinazoline-2,4-diamine (459 mg, 72%) as a white solid.

ESI-MS m/e 300.2 M+H⁺; ¹H NMR (400 MHz, CD₃OD) δ 7.69 (s, 1 H), 7.38 (d, J=8.4 Hz, 1 H), 7.30 (d, J=8.8 Hz, 1 H), 4.07 (m, 1 H), 3.27 (s, 6 H), 2.S5 (mi, 1 H), 2.39 (s, 3 H), 1.84-1.70 (m, 6 H), 1.57-1.52 (m, 2H).

Step F: Synthesis of N-(cis-4-{[4-(dimethylamino)-6-methylquinazolin-2-6l]amino}-cyclohexyl)-2,2-diphenylacetamide trifluoroacetate

To a solution of cis-N²-(4-amino-cyclohexyl)-6,N⁴,N⁴-trimethyl-quinazoline-2,4-diamine (24.9 mg, 0.083 mmol) in 0.5 mL DMF was added pyridine (16.2 uL, 0.2 mmol) and diphenylacetyl chloride (23.0 mg, 0.1 mmol). The reaction mixture was stirred overnight and then 0.5 mL of DMSO was added to the mixture. The compound was then subject to purification by prep LCMS to yield N-(cis-4-{[4-(dimetylamino)-6-methylquinazolin-2-yl]amino}cyclohexyl)-2,2-diphenylacetamide trifluoroacetate (13.6 mg, 27%) as a white solid.

ESI-MS m/e 494.4 M+H⁺; ¹ H NMR (400 MHz, CD₃OD) δ 7.96 (s, 1 H), 7.63 (d, J=8.4 Hz, 1 H), 7.31-7.23 (m, 11 H), 4.16 (brs, 1 H), 3.89 (brs, 1 H), 3.54 (brs, 6 H), 2.66 (s, 1 H), 2.47 (s, 3 H), 1.86-1.79 (m, 8 H).

Example 887

N-(cis-4-{[4-(Dimethylamino)-6-methylquinazolin-2-6l]amino}cyclohexyl)4-fluoro-3-(trifluoromethyl)benzamide trifluoroacetate

Step A: Synthesis of N-(cis-4-{[4-(dimethylamino)-6-methylquinazolin-2-6l]amino}-cyclohexyl)-4-fluoro-3-(trifluoromethyl)benzamide trifluoroacetate

Using a similar procedure as described in step F of Example 386, the title compound was obtained (12.5 mg, 25%) as a white solid.

ESI-MS m/e 490.2 M+H⁺; ¹H NMR (400 MHz, CD₃OD) δ 8.12-8.15 (m, 2 H), 7.98 (s, 1 H), 7.64 (d, J=8.4 Hz, 1 H), 7.49 (t, J=9.2 Hz, 1 H), 7.44 (brs, 1 H), 4.24 (brs. 1 H), 4.03 (brs, 1 H), 3.56 (s, 6H), 2.47(s, 3H),2.01-1.81 (m, 8H).

Example 888

N-(cis-4-{[4l-(Dimethylamino)-6-methylquinazolin-2-yl]amino}cyclohexyl)3,5-bis(trifluoromethyl)benzamide trifluoroacetate

Step A: Synthesis of N-(cis-4-{[4-(dimethylamino)-6-methylquinazolin-2-yl]amino}-cyclohexyl)-3,5-bis(trifluorometbyl)benzamide trifluoroacetate

Using a similar procedure as described in step F of Example 886, the title compound was obtained (18.4 mg, 0.028 mmol, 34%) as a white solid.

ESI-MS m/e 540.4 M+H⁺; ¹H NMR (400 MHz, CD₃OD) δ 8.53 (s, 2 H), 8.18 (s, 1 H), 7.97 (s, 1 H), 7.64 (d, J:=8.4 Hz, 1 H), 7.37 (brs, 1 H), 4.26 (brs, 1 H), 4.07 (brs, 1 H), 3.56 (brs, 6 H), 2.47 (s, 3 H), 2.07-1.32 (m, 8 H).

Example 889

N-(cis-4-{[4-(Dimethylamino)-6-methylquinazolin-2-yl]amino}cyclohexyl)-3,4,5-trimethoxybenzamide trifluoroacetate

Using a similar procedure as described in step F of Example 886, the title compound was obtained (21.2 mg, 0.035 mmol, 42%) as a white solid.

ESI-MS m/e 494.4 M+H⁺; ¹H NMR (400 MHz, CD₃OD) δ 7.98 (s, 1 H), 7.64 (d, J=8.4 Hz, 1 H), 7.37 (brs, 1 H), 7.17 (s, 2 H), 4.28 (brs, 1 H), 4.02 (brs, 1 H), 3.91 (s, 6 H), 3.82 (s, 3 H) 3. (brs, 6 H), 2.47 (s, 3 H), 2.07-1.81 (m, 8 H).

Example 890

cis-4-{[4-(Dimethylamino)-6,7-difluoroquinazolin-2yl]amino}-[4-(4-methylbenzyl)cyclohexane carboxamide trifluoroacetate

Step A: Synthesis of 6,7-difluoro-1H-quinazoline-2,4-dione

A solution of KOCN (6.1 g, 75 mmol) in H₂O (52 mL.) was added to a solution of 2-amino-4,5-difluoro benzoic acid (10 g, 58 mmol) in H₂O/AcOH (260 mL/3.5 mL). The mixture was stirred overnight at room temperature, and then NaOH (55 g, 1.37 mol) was slowly added in a portion of 3˜4 grams. During the addition of NaOH, the reaction was changed to a clear purple solution, and then formation of precipitates was observed. After stirring about 10 min, the precipitates wvere filtered and resuspended in H₂O. The aqueous suspension was acidified to pH 4 with 4N-HCl and stirred for another 10 more min. The precipitates were filtered and washed with cold water and dried to give 7.0 g (61%) of 6,7-difluoro-1H-quinazoline-2,4-dione.

ESI MS m/e 199 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 11.46 (s, 1 H), 11.26 (s, 1 H), 7.81 (dd, J=10.0, 8.4 Hz 1 H), 7.08 (dd, J=11.2, 6.8 Hz, 1 H).

Step B: Synthesis of 2,4-dichloro-6,7-difluoroquinazoline

To a suspension of 6,7-difluoro-1H-quinazoline-2,4-dione (6.9 g, 5 mmol) in POCl₃ (21 mL) was slowlyl added N,N-dimethylaniline (4.9 mL, 3 mol). The reaction was heated at reflux (120° C. for 7 h until the starting material was completely dissoled and the entire solution turned a dark purple color. The reaction was allowed to cool and poured veiy slowly onto ice (1 L); watch out for heat generation!! The resulting precipitate was filtered and washed with ice water. The crude product was purified from a short column of silica with CH₂Cl₂ as an elutinc solvent. The desired product (7.2 88%) was obtained as a white solid.

ESI MS m/e 236 M+H⁺; ¹H NMR (400 MHz CDCl₃) δ 8.01 (dd, J=9.2, 8.0 Hz, 1 H), 7.76 (dd, J=10.0, 7.2 Hz, 1 H).

Step C: Synthesis of 2-chloro-6,7-difluoro-4-dimethylamminoquinazoline

A solution of 2,4-dichloro-6,7-difluoro quinaoline (6.1 g, 26 mmol) in THF (60 mL) was cooled to 2˜4 ° C. in an ice bath and 2M-Me₂NH in MeOH (2 mL, ˜2 eq.) was slowly added. The reaction was stirred for 70 min. at room temperature, neutralized with saturated aqueous NaHCO₃, and concentrated until the most volatile solvent was removed. Addition of water into the concentrated crude reaction mixture gave solid precipitate, which was filtered and dried. 2-Chloro-6,7-difluoro-4-dimethylaminoquinazoline pure compound (5.6 g, 90%) was isolated as a yellowish white solid from a short column of silica using CH₂Cl₂/MeOH (100/0 to 90/10) as an eluting solvent.

ESI MS m/e 244 M+H⁺; ¹H NMR (400 MHz, CDCl₃) o 7.78 (dd, J=11.2, 8.0 Hz, 1 H), 7.50 (dd, J=11.2, 80 Hz, 1 H), 3.40 (s, 6 H).

Step D: Synthesis of cis-4-(4-dimethylamino-6,7-difuoroquinazolin-2-ylamino)-cyclohexane-carboxylic acid ethyl ester

A suspended solution of 2-chloro-6,7-difluoro-4-dimethylamino quinazoline (0.45 g, 1.85 mmol) and cis-(4-ethoxycarbonyl) aminocyclohexane hydrochloride (0.38 g, 1 eq.) in IPA (2.5 mL) and DIEA (0.5 mL. -2eq.) was reacted for 2 h at 155 ° C. in a Smith microwave synthesizer. The reaction was quenched and purified by column chromatogiaphy (DCM:MeOH=100:0 to 90:10) to give 0.25 g (36%) of cis-4(4-dimethylamino-6,7-difluoroquiazolin-2-ylamino)-cyclohexanecarboxylic acid ethyl ester.

ESI MS m/e 379 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 7.57 (dd, J=11.0, 8.0 Hz, 1 H), 7.17 (dd, J=12.0, 7.0 Hz, 1H), 4.96 (d, J=7.0 Hz, 1 H), 4.15 (q, J=7.0 Hz, 2 H), 4.13 (brs, 1 H), 3.23 (s, 6 H), 2.48 (m, 1 H), 1.94 (m, 2 H), 1.83-1.6S (n, 6 H), 1.25 (t, J=7.0 Hz, 3 H).

Step E: Synthesis of cs-4-(4-dimethylamino-6,7-difluoroquinazolin-2-ylamino)-cyclohexanecarboxylic acid

A suspension of cis-4(4-dimethylamino-6,7-difluoroquinazolin-2-ylamino)-cyclohexane carboxylic acid ethyl ester (0.71 g 1.9 mmol) in 4N-HCl (15 mL) was stirred at 82° C. for 3 h. During the reaction, the heterogenous solution turned to be a clear solution, and then the precipitate was formed. The solid was filtered, washed with cold water several times, and dried to give 0.55 g (85%) of cis-4(4-dimethylamino-6,7-difluoroquinazolin-2-ylamino)-cyclohexane carboxylic acid as a white solid.

ESI MS m/e 351 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 12.15 (brs, 1 H), 8.18 (m, 2 H), 7.47 (m, 1 H), 3.99 (brs, 1 H), 3.38 (s, 6 H), 2.38 (brs, 1 H), 1.75-1.59 (m, 8 H).

Step F: Synthesis of cis-4-{[4-(dimethylamino)-6,7-difuoroquinazolin-2-yl]amino}-N-(4-methylbenzyl)cyclohexane carboxamide trifluoroacetate

cis-4(4-Dimethylamino-6,7-difluoroquinazolin-2-ylamino)-cyclohexane carboxylic acid (21 mg, 0.06 mmol) and 4-methylbenzyl amine (7.5 mg, 0.06 mmol) was stirred overnight in the presence of HATU (25 mg, 1.1 eq.) and Et₃N (5 drops). cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-N-(4-methylbenzyl)cyclohexanecarboxamide trifluoroacetate (13 mg, 39%) was obtained ftom a prep-HPLC.

ESI MS m/e 454 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 11.9 (brs, 1 H), 8.19 (m, 2 H), 8.10 (b, 1 H), 7.49 (m, 1 H), 7.05 (s, 4 H), 4.16 (d, J=6.0 Hz, 2 H), 4.08 (brs, 1 H), 3.39 (s, 6 H), 2.26 (m, 1 H), 2.20 (s, 3 H), 1.71-1.57 (m, 8 H).

Example 891

cis-N-(3-Chlorobenzyl)-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexane carboxamide trifluoroacetate

Step A: Synthesis of cis-N-(3-chlorobenzyl)-4-{[4-dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexane carboxamide trifluoroacetate

Using a similar procedure as described in step F of Example 890, the title compound intas obtained.

ESI MS m/e 474 M+H¹; ¹H NMR (400 1MHz, DMSO-d₆)δ 1.21 (brs, 1 H), 8.31 (t,J=7.6 Hz, 1 H), 8.19 (m, 2 H), 7.49 (t, J=8.0 Hz, 1 H), 7.30-7.21 m, 3 H), 7.13 (d, J=7.6 Hz, 1 H), 4.21 (d, J=6.0 Hz, 2 H), 4.08 (brs, 1 H), 3.44 (s, 6 H), 2.29 (brs, 1 H), 1.85-1.59 (m, 8 H),

Example 892

cis-4-{[4-(Dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-N-[(1R)-1-(3-methoxphenyl)ethyl]cyclohexanecarboxamide trifluoroacetate

Step A: Synthesis of cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-N-](1R)-1-(3-methoxyphenyl)ethyl]cyclohexanecarboxamide trifluoroacetate

Using a similar procedure as described in step F of Example 890, the title compound was obtained.

ESI MS m/e 484 M+H⁺; ¹H NMR (400 MHz, DMSO-₆) δ 11.8 (brs, 1 H), 8.19 (m, 1 H), 8.12 (m, J=8.0 Hz, 1 H), 8.07 (brs, 1 H), 7.49 (t, J=8.0 Hz, 1 H), 7.14 (t, J=8.0 Hz, 1 H), 6.80 (d, J=7.6 Hz, 1 H), 6.79 (s, 1H), 6.70 (d, J=7.6 Hz, 1 H), 4.82 (m, 1 H), 4.03 (brs, 1 H), 3.66 (s, 3 H), 3.37 (s, 6 H), 2.26 (brs, 1 H), 1.69-1.52 (m, 8 H), 1.23 (d, J=7.2 Hz, 3 H).

Example 893

N-(3,4-Dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea trifluoroacetate

Step A: Synthesis of cis-(4-benzylcarbonylamino-cyclohexyl)-carbamic acid tert-butyl ester

To a suspension of cis-4-tert-butoxycarbonylamino-cyclohexane carboxylic acid (50 g, 0.21 mol) in benzene was added triethylamine (37 mL, 0.27 mol) and diphenylphosphoryl azide (48.7 mL, 0.23 mol). The reaction mixture was stirred at 80° C. for 1 hour. Benzyl alcohol (30 mL, 0.29 mol) was added and the reaction mixture was stirred at reflux overnight. The solvent benzene was removed under vacuum and the resulting slurry dissolved in etlhyl acetate. The organic layer was extracted with H₂O and separated. The aqueous layer was extracted twice more with ethyl acetate. The organic layers were combined, dried over MgSO₄, concentrated, and subjected to chromatography (30% ethyl acetate in hexanes) to give cis-(4-benzyloxycarbonylamino-cyclohexyl)-carbamic acid tert-butyl ester (54.1 g, 0.16 mol, 75%) as a colorless oil.

ESI-MS m/e 349.4 M+H⁺; ¹H NMR (400 , MHz, DMSO-d₆) δ 7.34-7.28 (m, 5 H), 7.12 (d. J=5.6 Hz, 1 H), 6.62 (brs, 1 H), 4.98 (s, 2 ), 3.39-3.37 (m, 2 H), 1.60-1.45 (m, 8 H), 1.37 (s, 9 H).

Step B: Synthesis of cis-(4-amino-cyclohexyl)-carbamic acid tert-butyl ester

To a solution of cis-(4-benzyloxycarbonylamino-cyclohexyl)-carbamic acid tert-butyl ester (54.1 g, 0.16 mol) in ethanol was added 10% Pd/C (5.4 g). The reaction mixture was stirred at room temperature under an H₂ atmosplere for 3 hours. The H₂ atmosphere as removed and the solution filtered though celite and concentrated. The resulting precipitate was dissolved in ethyl acetate and extracted with a dilute NaOH (aq) solution. The aqueous layer as extracted twice more with ethyl acetate. The organic layers were combined, dried over MgSO₄, and concentrated. The resulting precipitate was recrystallized in ethyl acetate and hexanes to yield cis-(4-amino-cyclohexyl)-carbamic acid tert-butyl ester (28.9 g, 0.14 mol, 87%) as a white solid.

ESI-MS m/e 215.2 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 6.60 (d, J=6.0 Hz, 1 H)3.30-3.28 (m, 1 H), 2.74 (s, 1 H), 1.59-1.51 (m, 2 H), 1.45-1.37 (m, 15 H).

Step C: Synthesis of cis-[4-(4-dimethlyamino-quinazolin-2-ylamino)-cyclohexyl]-carbamic acid tert-butyl ester

To a solution of cis-(4-amino-cyclohexyl)-carbamic acid tert-butyl ester (0.5 g, 0.0023 mol) in 1 mL 2-propanol was added (2-chloro-quinazolin-4-yl)-dimethyl-amine (0.53, 0.0026 mol) and DIEA (1.22 mL. 0.0070 mol). The mixture was heated in a microwave synthesizer at 170° C. for 1 hour. The reaction was repeated 39 more times (20 g total material) and the reaction mixtures were pooled. The solvent was evaporated and the material subjected to chromatography (2-4% 2M NH₃ in MeOH /CH₂Cl₂) to yield cis-[4-(4-dimethlyamino-quinazolin-2-ylamino)-cyclohexyl]-carbamic acid tert-butyl ester (22.1 , 0.057 mol, 61%) as a colorless oil.

ESI-IS m/e 386.4 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 7.85 (d, J=8.0 Hz, 1 H), 7.47 (t, J=8.4 Hz, 1 H), 7.27 (d, J=3.0 Hz, 1 H), 7.00 (t, J=7.6 Hz, 1 H), 6.60 (brs, 1 H), 6.18 (brs, 1 H), 3.89-3.88 (m, 1 H), 3.39 (brs, 1 H), 3.19 (s, 6 H), 1.77-1.71 (m, 2 H), 1.68-1.52 (m, 6 H), 1.38 (s, 9 H).

Step D: Synthesis of cis-N2-(4-amino-cyclohexyl)-N⁴,N⁴-dimethyl-quinazolin-2,4-diamine

To a solution of cis-(4-(4-dimethlyamino-quinazolin-2-ylamino)-cyclohexyl]-carbamic acid tert-butyl ester (22.1 g, 0.057 mol) in CH₂Cl₂ was added TFA (10 mL, 0.13 mol). The solution was stirred at room temperattire for 4 hours. The excess solvent was evaporated off and the resulting oil was dissolved in CH₂Cl₂. The organic layer was extracted with a dilute NaOH (aq)/NaHCO₃ (aq) solution. The aqueous layer was extracted twice more with CH₂Cl₂ and the organic layers combined, dried over MgSO₄, and concentrated. The resulting precipitate was crystallized in ether and hexanes to yield cis-N²-(4-amino-cyclohexyl)-N⁴,N⁴-dimethyl-quinazolin-2,4-diamine (15.0 g, 0.053 mol, 92%) as a pale yellow solid.

ESI-MS m/e 286.2 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 7.84 (d, J 8.4 Hz, 1 H), 7.45 (t, J=6.8 Hz, 1 H), 7.26 (d, J=8.4 Hz, 1 H), 6.99 (t, J=7.6 Hz, 1 H), 6.20 (brs, 1 H), 3.90-3.89 (m, 1 H), 3.18 (s, 6 H) 2.79 (s, 1 H), 1.74-1.71 (m, 2 H), 1.57-1.41 (m, 8 H).

Step E: Synthesis of N-(3,4-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea trifluoroacetate

To a solution of cis-N²(4-aminp-cyclohexyl)-N⁴,N⁴-dimethyl-quinazolin-2,4-diamine (28.5 mg, 0.10 mmol) in 0.5 mL of DMSO was added 3,4-dimethoxyphenylisocyanate (14.9 uL, 0.10 mmol). Note that for this reaction it was necessary to slightly heat the starting material to dissolve it in the DMSO before adding the isocyanate. The reaction mixture was stirred for 1 hour and then 0.5 mL of 50% DMSO in H₂O was added. The compound was subjected to purification by prep LCMS to yield N-(3,4-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea trifluoroacerate (37 mg, 0.064 mmol, 64%) as a white solid.

ESI-MS m/e 465.2 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 12.10 (s, 1 H), 8.21 (s, 1 H), 8.16 (d, J=8.0 Hz, 1 H), 8.08 (brs, 1 H), 7.78 (t, J=7.6 Hz, 1 H), 7.45 (brs, 1 H), 7.37 (t, J=7.6 Hz, 1 H), 7.15 (s, 1 H), 6.83-6.72 (m, 2 H), 6.15 (d, J=6.8 Hz, 1 H), 4.00 (brs, 1 H), 3.72 (s,3 H), 3.69 (s, 3 H), 3.47 (brs, 6 H), 1.80-1.78 (m, 2 H), 1.68 (m, 6 H).

Example 894

N-[(cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}i ) cyclohexyl)methyl]-N′-[2-(trifluoromethoxy)phenyl]urea trifluoroacetate

Step A: Synthesis of cis-4-tert-butoxycarbonylamino-cyclohexanecarboxylic acid

To a solution of cis-4-amino-cyclohexanecarboxylic acid (50 g, 350 mmol) in 200 mL of THF and 38 0mL of 1M NaOH (380 mmol), Boc₂O (83.5 g, 360 mmol) was added. The mixture was stirred at room temperature for 2 hr and evaporated until only water was remained. The reaction mixture was cooled to 0° C. and acidified with 1M HCl until pH about 3. The white solid formed was filtered, washed with water and hexanes to give cis-4-tert-butoxycarbonylamino-cyclohexanecarboxylic acid (71 g, 83%) as a white solid.

ESI-IS m/e 244 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 12.00 (b, 1 H), 6.74 (d, J=4.25, 1 H), 3.30 (brs, 1 H), 2.35 (m, 1 H), 1.87 (m, 2 H), 1.55-1.37 (m 15 H).

Step B: Synthesis of cis (4-carbamoyl-cyclohexyl)-carbamic acid tert-butyl ester

The cis-4-tert-butoxycarbonylamino-cyclohexanecarboxylic acid (68 g, 280 mmol) and triethylamine (42.35 mL, 308 mmol) were dissolved in 300 mL of THF and the mixture was cooled to 0° C. Ethyl chloroformate (29.3 mL, 308 mmol) was added dropwise. After stirring at 0° C. for 30 min, 168 mL of aqueous ammonia was added dropwise. The mixture was allowed to stir at room temperature for 2 hr. The solvent was evaporated until only water was remained. To this mixture was added EtOAc. The organic layer was washed with sat. NaHCO₃, 1M HCl, brine, water, dried over Na₂SO₄ and filtered. The solvent was evaporated to give cis (4-carbamoyl-cycloeexyl)-carbamic acid tert-butyfl ester (62 g, 88%) as a white solid.

ESI-MS m/e 243 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 7.10 (brs, 1 H), 6.69 (bis, 2 H), 3.41 (brs, 1 H), 2.14 (m, 1 H), 1.79 (m, 2 H), 1.59 (m, 2 H), 1.45-1.37 (m, 13 H).

Step C: Synthesis of cis-4-amino-cyclohexanecarboxylic acid amide hydrochloride

The cis-(4-carbamoyl-cyclohexyl)-carbamic acid tert-butyl ester (62 g, 256 mmol) in 250 mL of DMC was added 250 mL of TFA. The mixture was stirred for 1 hr. The solvents wvere evaporated. To the residue was added 150 mL of 2M HCl in ether to give white solid. The solvent was evaporated to give cis-4-amino-cyclohexanecarboxylic acid amide hydrochloride (45 g, 98%) of white solid as the product.

ESI-MS m/e 143 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 8.08 (brs, 3 H), 7.28 (s, 1 H), 6.78 (s, 1 H), 3.10(m, 1 H), 2.24 (m 1 H), 1.90 (m, 2 H), 1.66 (m, 4 H), 1.50 (m, 2 H).

Step D: Synthesis of cis-4-)4-dimethylamino-quinazolin-2-ylamino)-cyclohexanecarboxylic acid amide

(2-Chloro-quinazoline-4-yl)-dimethylamine (31.05 g, 150 mmol) and cis-4-amino-cyclohexanecarboxylic acid amide hydrochloride (26.7 g, 150 mmol) in 150 mL of pyridine was refluxed overnight. The solvent was evaporated. DCM was added to the residue. The organic layer was washed with sat. NaHCO₃. The aqueous layer was backed extracted with DCM. The combined organic layers were dried over Na₂SO₄, filtered and evaporated. The residue w!as purified on silica gel column twice to give a slightly brown solid which was recrystalized from DCM to gixve cis-4 (4-dimethylamino-quinazolin-2-ylamino)-cyclohexanecarboxylic acid amide (20.6 g, 44%) as yellow crystals.

ESI-MS m/e 314 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 8.19 (b, 1 H), 8.15 (d, J=8.4 Hz, 1 H), 7.77 (t, J=8 Hz, 1 H), 7.42 (d, J=7.2 Hz, 1H), 7.35 (t, J=8.4 Hz, 1 H), 7.21 (s, 1 H), 6.74 (s, 1 H), 4.12 (m, H), 3.46 (b, 6 H), 2.24 (m, 1 H), 1.79-1.61 (m, 8 H).

Step E: Synthesis of cis-N²-(4-aminomethyl-cyclohexyl)-N⁴,N⁴-dimethyl-quinazoline-2,4-diamine

To a stirred solution of cis-4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexane carboxylic acid amide (18.78 g, 60 mmol) in 200 mL of THF was added a solution of 1M BH₃ in THF (300 mL, 300 mmol). The mixture was refluxed for 2 hr. After cooling the reaction mixture to 0° C., 100 mL of 4 M HCl and 200 mL of methanol were added. The solvents were removed under reduced pressure. The mixture was treated with 1M NaOH and the aqueous phase was extracted with dichloromethane. The organic layers were combined, dried ovir sodium sulfate, concentrated under reduced pressure, and purified on silica gel column to give cis-N⁷-(4-aminomethyl-cyclohexyl)-N′, N′-dimethyl-quinazoline-2,4-diamine as a white solid (10.6 g, 59%).

ESI-MS m/e 300 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 7.84 (d, J=8.4 Hz, 1 H), 7.46 (t, J=6.8 Hz, 1 H), 7.26 (d, J=8.4 Hz, 1 H), 6.99 (t, J=6.8 Hz, 1 H), 6.28 (brs, 1 H), 4.02 (m, 1 H), 3.19 (brs, 6 H), 2.47 (d, J=6.8 Hz, 2 H), 2.73 (m, 2 H), 1.68-1.33 (m, 9 H).

Step F: Synthesis of N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]-N′-[2(trifluoromethoxy)phenyl]urea trifluoroacetate

A solution of cis-N²-(4-aminomethyl-cyclohexyl)-N⁴,N⁴-dimethyl-quinazoline-2,4-diamine (30 mg, 0.1 mmol) and 2-trifluoromethoxy phenylisocyanate (20 mg, 0.1 mmol) in 0.5 mL of DMSO was stirred at room temperature overnight. DMSO (0.5 mL) was added and the reaction mixture was purified by prep LCMS. The fractions contained the product were combined and lyophilized to give N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-[2-(rrifluoromethox-)phenyl]urea trifluoroacetate (21 mg, 3.4%) as a white solid.

ESI MS m/e. 503 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 12.10 (brs, 1 H), 8.23 (d, J=8.0 Hz, 1, H), 8.15 (d, J=8.0 Hz 1 H), 8.14 (s, 1 H), 8.09 (brs, 1 H), 7.75 (m, 1 H), 7.43-7 24 m, 4 H), 6.98 (m, 2 H), 4.15 (m, 1H), 3.46 (brs, 6 H), 3.05 (m, 2 H), 1.77-1.35 (m, 9 H).

Example 895

2-(4-Chlorophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-nicotinamide trifluoroacetate

Step A: Synthesis of cis-[4-(4-dimethlyamino-quinazolin-2-ylamino)-cyclohexyl]-carbamic acid tert-butyl ester

To a solution of cis-(4-amino-cyclohexyl)-carbamic acid tert-butyl ester (0.5 g, 0.0023 mol) in 1 mL 2-propanol was added (2-chloro-quinazolin-4-yl)-dimethyl-amine (0.53, 0.0026 mol) and DIEA (1.22 mL, 0.0070 mol). The mixture was heated in a microwave synthesizer at 170° C. for 1 hour. The reaction was repeated 39 more times (20 g total material) and the reaction mixtures were pooled. The solvent was evaporated and the material subjected to chromatography (2-4% 2M NH₃ in MeOH/CH₂Cl₂) to yield cis-[4-(4-dimethlylamino-quinazolin-2-ylamino)-cyclohexyl-carbamic acid tert-butly ester (22.1 g 0.057 mol, 61 %) as a colorless oil.

ESI MS m/e 386.4 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 7.85 (d, J=8.0 Hz, 1 H), 7.47 (t, J=8.4 Hz, 1 H), 7.27 (d, J=8.0 Hz, 1 H), 7.00 (t, J=7.6 Hz, 1 H)j 6.60 (brs, 1 H), 6.18 (brs, 1 H), 3.9S-3.SS (m, 1 H), 3.39 (brs, 1 H), 3.19 (s, 6 H), 1.77-1.71 (m, 2 H), 1.68-1.52 (m, 6 H), 1.38 (s, 9 H).

Step B: Synthesis of cis-N²(4-amino-cyclohexyl)-N⁴,N⁴-dimethyl-quinazolin-2,4-diamine

To a solution of cis-(4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-carbamic acid tert-butyl ester (22.1 g, 0.057 mol) in CH₂Cl₂ was added TFA (10 mL, 0.13 mol). The solution was stirred at room temperature for 4 hours. The excess solvent was evaporated off and the resulting oil was dissolved in CH₂Cl₂. The organic later was extracted with a dilute-NaOH (aq) solution. The aqueous layer was extracted twice more with CH₂Cl₂ and the organic layers combined, dried over MgSO₄, and concentrated. The resulting precipitate was crystallized in ether and hexanes to yield cis-N²-(4-amino-cyclohexyl)-N⁴,N⁴-dimethyl-quinazolin-2,4-diamine (15.0 g, 0.053 mol, 92%) as a pale yellow solid.

ESI MS m/e 286.2 M+H⁺; ¹H N-NMR (400 MHz, DMSO-d₆) δ 7.84 (d, J=8.4 Hz, 1 H), 7.45 (t, J=6.8 Hz, 1 H), 7.26 (d, J 8.4 Hz, 1 H), 6.99 (t, J=7.6 Hz, 1 H), 6.20 (brs, 1 H), 3.90-3.89 (m, 1 H), 3.18 (s, 6 H), 2.79 (s, 1 H), 1.74-1.71 (m, 2 H), 1.57-1.41 (m, 8 H).

Step C: Synthesis of 2-(4-chlorophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)nicotinamide trifluoroacetate

To a solution of cis-N²-(4-amino-cyclohexyl-N⁴,N⁴-dimethyl-quinazolin-2,4-diamine (28.5 mg, 0.1 mmol) in 0.5 mL DMF was added 2-(4-chlorophenoxy)nicotinic acid (24.9 mg, 0.1 mmol), HATU (45.6 mg, 0.12 mmol), and DIEA (34.8 L, 0.2 mmol). The reaction mixture was stirred for a couple of hours, and the compound was then subjected to purification by prep LCMS to yield 2-(4-chlorophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}, cyclohexyl)nicotimide trifluoroacetate (15 mg, 0.029 mmol, 29%) as a white solid.

ESI-MS m/e 517.4 M+H⁺; ¹HMR (400 MHz, DMSO-d₆) δ 12.2 (s, 1 H), 8.58 (d, J=8.0 Hz 1 H), 8.48-8.39 (m, 2 H), 8.29 (d, J=8.0 Hz, 1 H), 8.13 (brs, 1 H), 8.02 (t, J=4.0 Hz, 1 H), 7.75 (m, 3 H), 7.61 (t, J=8.0 Hz, 1 H), 7.50 (m, 3 H), 4.25 (brs, 1 H), 4.21 (brs, 1 H), 3.69 (brs, 6 H), 2.00-1.80 (m, 8 H).

Example 8961

N-(cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-2-(4-fluorophenoxy)-nicotinamide trifluoroacetate

Step A: Synthesis of cis-2-chloro-N-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-nicotinamide

To a solution of cis-N²-(4-amino-cyclohexyl)-N⁴,N⁴-dimethyl-quinazolin-2,4-diamine (1.0 g, 3.5 mmol) in 18 mL CH₂Cl₂ was added 2-chloronicotinyl chloride (616.7 mg, 3.5 mmol), DIEA (1.2 mL, 7.0 mmol). The reaction mixture was stirred for 30 minutes at room temperature, the solvent was removed under vacuum, and the residue was purified by column chromatography on silca gel (2-4% 2M NH₃ in CH₃OH/CH₂Cl₂) to yield cis-2-chloro-N-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-nicotinamide (0.71 g, 47%). ESI-MS m/e 425.2 M+H⁺; ¹ NMR (400 MHz, DMSO-d₆) δ 8.59 (brs, 1 H), 8.46 (d, J=4.0 Hz, 1 H), 8.30 (brs, 1 H) 8.18 (d, J=8.0 Hz, 1 H), 7.87 (d, J=8.0 Hz, 1 H), 7.79 (t J=8.0 Hz, 1 H), 7.53-7.43 (m, 2 H), 7.37 (t, J=8.0 Hz, 1 H), 4.09 (brs, 1 H), 3.93 (brs, 1 H), 3.57 (brs, 6 H), 1.90-1.62 (m, 8 H).

Step B:. Synthesis of N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-2-(4-fluorophenoxy)nicotinamide trifluoroacetate

cis-2-Chloro-N-[4-(4-dimethlamino-quinazolin-2-ylamino)-cyclohexyl]-nicotinamide (30 mg, 0.07 mmol) was added into a stirred solution of 4-fluorophenol (7.93mgn. 0.07 mmol) and 60% NaH in mineral oil (5.6 mg, 0.14 mmol) in 0.5 mL DMA. The mixture was heated in a microwave synthesizer at 250° C. for 1 hour. The compound was then subjected to purification by prep LCMS to yield N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-2-(4-fluorophenoxy) nicotinamide trifluoroacetate (10.3 mg, 0.021 mmol 30%) as a white solid.

ESI-MS 501.3 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 12.2 (s, 1 H), 8.51 (brs, 1 H), 8.38-8.34 (m, 2 H), 8.26 (d, J=8.0 Hz, 1 H), 8.17 (brs, 1 H), 7.98 (t. J=8.0 Hz, 1 H), 7.63 (brs, 1 H), 7.57 (t, J=8.0 Hz, 1 H), 7.47-7.40 (m, 5 H), 4.20 (brs, 1 H), 4.17 (brs, 1 H), 3.66 (brs, 6 H), 2.00-1.94 (m, 8 H).

Example 897

N-(cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-2-(4-methoxyphenoxy)-nicotinamide trifluoroacetate

Step A: Synthesis of N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-2-(4-methoxyphenoxy)nicotinamide trifluoroacetate

Using a similar procedure as described in step B of Example 896, the title compound was obtained.

ESI-MS m/e 513.4 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 11.8 (s, 1 H) 8.14 (brs, 1 H) 8.00(m, 2 H), 7.91 (brs, 1 H), 7.80 (brs, 1 H), 7.62 (t, J=8.0 Hz, 1 H), 7.27 (brs, 1 H), 7.21 (t, J=8.0 Hz, 1 H), 7.04 (q, J=4.0 Hz, 1 H), 6.99 (d, J=12.0 Hz, 2 H), 6.80 (d, J=12.0 Hz, 2 H), 3.82-3.76, (brs, 2 H), 3.40-3.30 (m, 6 H), 1.61-1.50 (m, 8 H).

Example 898

N-(cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-2-(3-methylphenoxy)-nicotinamide trifluoroacetate

Step A: Synthesis of N-(cis-4-{[4-(dimethylamino)quinazolin-2-)yl]amino}cyclohexyl)-2-(3-methylphenoxy)nicotinamide trifluoroacetate

Using a similar procedure as described in step B of Example 896, the title compound was obtained.

ESI-MS m/e 497.4 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 12.0 (brs, 1 H), 8.26 (d, J=4.8 Hz, 1 H), 8.18 (m, 2 H), 8.07 (d, J=6.8 Hz, 1 H), 7.88 (brs, 1 H), 7.77 ( t, J=8.0 Hz, 1 H), 7.43 (brs, 1 H), 7.36 (t, J=8.0 Hz, 1 H), 7.27 (t, J=8.0 Hz, 1 H), 7.20 (q, J=8.0 Hz, 1H), 7.02-6.96 (m, 3 H), 4.10-3.90 (m, 2 H), 3.80-3.20 (m, 6 H), 2.30 (s, 3 H), 1.78-1.50 (m, 8 H).

Example 899

N(cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-2-(2-methoxyphenoxy)-nicotinamide trifluoroacetate

Step A: Synthesis of N(cir-4-{[4(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-2-(2-methoxyphenoxy)nicotinamide trifluoroacetate

Using a similar procedure as described in step B of Example 896, the title compounds was obtained.

ESI-MS m/e 513.2 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 11.9 (s, 1 H), 8.15-8.12 (m, 4 H), 7.88 (brs, 1 H), 7.78 (t, J=8.0 Hz, 1 H), 7.42 (brs, 1 H), 7.30-7.10 (m, 4 H), 7.14 ( d, J=8.0 Hz, 1 H), 7.00 (t, J=8.0 Hz, 1 H), 4.15 (brs, 2 H), 3.69 (s, 3 H), 3.39 (brs, 6 H), 1.80-1.50 (m, 8 H).

Example 900

2-(4-Bromophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-nicotinamide trifluoroacetate

Step A: Synthesis of 2-(4-bromophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)nicotinamide trifluoroacetate

Using a similar procedure as described in step B of Example 896, the title compounds was obtained.

ESI-MS m/e 563.2 M+H⁺; ¹H NMR (400 MHz, DPSO-d₆) δ 11.9 (s, 1 H), 8.16 (d, J==8.0 Hz, 1 H), 8.02-7.98 (m, 2 H), 7.88 (d, J=8.0 Hz, 1 H), 7.83 (brs, 1 H), 7.62 (t, J=8.0 Hz, 1 H), 7.42 (d, J=8.0 Hz, 2 H), 7.27 (brs, 1 H), 7.20 (t, J=8.0 Hz, 1 H), 7.03-7.05 (q, J=4.0 Hz, 1 H), 7.03 (d, J=12.0 Hz, 2 H), 3.83 (brs, 2 H), 3.29 (brs, 5 H), 1.59-1.50 (m, 8 H).

Example 901

N-(cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-2,6-dimethoxynicotinamide trifluoroacetate

Step A: Synthesis of N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-2,6-dimethoxynicotinamide trifluoroacetate

To a solution of cis-N²-(4-amino-cyclohexyl)-N⁴,N⁴-dimethyl-quinazolin-2,4-diainine (28.5 mg, 0.1 mmol) in 0.5 mL DMF was added 2,6-dimethoynicotinic acid (18.3 mg, 0.1 mmol, HATU (45.6 mg, 0.12 mmol), and DIEA (34.8 L, 0.2 mmol). The reaction mixture was stirred for a couple of hours, and the compound was then subjected to purification by prep LCMS to yield N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-2,6-dimethoxynicotinamide tritluoroacetate (9.9 mg, 0.022 mmol, 22%) as a white solid.

ESI-MS m/e 451.2 M+H⁺; ¹H NMR (400 Nz, DMSO-d₆) δ 12.5 (s, 1 H), 8.42 (brs, 1 H), 8.13 (dd, J=4.0, 4.0 Hz, 2 H), 7.86 (brs, 1 H), 7.74 (t, J=8.0 Hz, 1 H), 7.39 (brs, 1 H), 7.32 (t, J=8.0 Hz, 1 H), 6.47 (d, J=8.0 Hz, 1 H), 4.02 (s, 3 H), 3.95 (brs, 1 H), 3.85 (s, 3 H), 3.68 (brs, 1 H), 3.42 (brs, 6 H), 1.80-1.68 (m, 8 H).

Example 902

N²-{(1S,3R)-3-[(3,5-Dichlorobenzyl)amino]cyclopentyl}-N⁴,N⁴-dimethylquinazoline-2,4-diamine bistrifluoroacetate

Step A: Synthesis of (1S,3R)-cis-(3-tert-butoxycarbonylamino-cyclopentyl)-carbamic acid benzyl ester

(1R,3 S)-N-Boc-1-aminocyclopentane-3-carboxylic acid (5.00 g, 21.8 mmol), diphenylphosphoryl azide (4.69 mL, 21.8 mmol), and triethylamine (3.04 mL. 21.8 mmol) were combined in benzene (30 mL) at room temperarture. The mixture was heated to 80° C. and stirred 1 hr. Benzylalcohol (2.26 mL, 21.8 mmol) was added and the mixture was heated to 110° C. for 1 hr. The mixture was concentrated and ethyl acetate was added. The organic phase was washed with water, saturated aqueous NaHCO₂, and brine, dried over Na₂SO₄, filtered, and concentrated. The crude product was purified by flash chromatography (silica gel 20% ethyl acetate in hexanes) to give (1S,3R)-cis-(3-tert-butoxycarbonylamino-cyclopentyl)-carbamic acid benzyl ester (5.00 g, 69%) as a white solid.

ESI-MS m/e 335 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 7.25 (m, 5 H), 6.83 (m, 2 H), 4.98 (s, 2 H), 3.77 (brs, 1 H), 2.13 (dt, J=12.8, 7.6 Hz, 1 H), 1.75 (d, J=7.2 Hz, 2 H), 1.43 (m, 2 H), 1.38), (s, 9 H), 1.22 (m, 2 H).

Step B: Synthesis of (1R,3S)-cis-(3-amino-cyclopentyl)-carbamic acid tert-butyl ester

(1S,3R)-(3-tert-Butoxycarbonylamino-cyclopent)-carbamic acid benzyl ester (4.73 g, 14.2 mmol) and 10% Pd/C (0.24 g) were combined in methanol (27 mL) at room temperature. The mixture stirred for 4 days under a hydrogen gas atmosphere, was filtered through celite and concentrated to give (1R,3S)-cis-(3-amino-cyclopentyl)-carbamic acid tert-butyl ester as a yellow oil (2.84 g) (crude).

ESI-MS m/e 201 (M+H)⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 6.8 (brs, 1 H), 3.70 (m, 1 H), 2.10 (brs, 2 H), 1.97 (dt, J=12.8, 6.8 Hz, 1 H), 1.70 (m, 2 H), 1.43 (m, 2 H), 1.38 (s, 9 H), 1.18 (m, 2 H).

Step C: Synthesis of (1S,3R)-cis-N-(3-amino-cyclopent)-N⁴,N⁴-dimethyl-quinazoline-2,4-diamine

(2-Chloro-quinazolin-4-yl)-dimethyl-amine (0.100 g, 0.48 mmol), (1R,3S)-(3-amino-cyclopentyl)-carbamic acid tert-butl ester (0.096 g, 0.48 mmol), and diisopropylethylamine (0.126 mL. 0.72 mmol) were combined in isopropanol (1 mL) at room temperature. The mixture was heated to 160° C. for 40 min. utilizing a Smith synthesizer microwave apparatus. Trifluoroacetic acid (1 mL, neat) was added and the mixture was heated to 100° C. for 30 min. Then it was concentrated, neutralized with saturated aqueous NaHCO₃, concentrated, extracted with methanol, and concentrated again to give (1S,3R)-cis-N²-(3-amino-cyclopentyl)-N⁴,N⁴-dimethyl-quinazoline-2,4-diamine as a yellow gum (0.130 g) (crude).

ESI-MS m/e 272 M+H⁺; ¹H NMR (400 MHz, DMSC-d₆) δ 8.76 (brs, 1 H), 8.17 (d, J=7.6 Hz 1 H), 7.77 (d J=7.2 Hz, 1 H), 7.40 (brs, 1 H), 7.35 (d, J=7.6 Hz, 1 H), 3.80 (m, 1 H), 3.40 (s, 6 H), 2.20 (m, 1 H), 1.98 (brs, 2 H) 1.70 (m, 2 H), 1.43 (m, 2 H), 1.18 (m, 2 H).

Step D: Synthesis of N²-{(1S,3R)-3-[(3,5-dichlorobenzylamino]cyclopentyl}-N⁴,N⁴-dimethyl quinazoline-2,4-diamine bistrifluoroacelate

(1S,3R)-N²-(3-Amino-cyclopentyl)-N⁴,N⁴-dimethly-quinazoline-2,4-diamine (0.065 g, 0.24 mmol) and 2,4-dimethoxybenzaldehyde (0.040 g, 0.24 mmol) were combined in methanol (1 mL) at room temperature. After stirring for 1 hr, sodium triacetoxyborohydride (0.204 g, 0.96 mmol) was added and the mixture as heated to 150° C. for 40 min. utilizing a Smith Synthesizer microwave apparatus. Water (1 mL) was added and the product was purified to give N²-{(1S,3R)-3-[(3,5-dichlorobenzyl)amino]cyclopentl}-N⁴,N⁴-dimethyl quinazoline-2,4-diamine bistrifluoroacetate as a white solid (0.070 g, 45%).

ESI-MS m/e 422 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 9.32 (brs, 1 H), 8.17 (d, J=7.6 Hz, 1 H), 7.77 (t, J=7.2 Hz, 1 H), 7.69 (s, 1 H), 7.61 (s, 1 H), 7.60 (s, 1 H), 7.40 (brs, 1 H), 7.35 (t, J=7.6 Hz, 1 H), 4.33 (brs, 1 H), 3.58 (m, 2 H), 3.40 (s, 6 H), 2.20 (m, 1 H), 2.06 (brs, 1 H), 1.70 (m, 2 H), 1.43 (m, 2 H), 1.18 (m, 2 H).

Example 903

6-(3-Chlorophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl) nicotinamide trifluoroacetate

Step A: Synthesis of cis-6-chloro-N-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-nicotinamide

To a solution of cis-N′-(4-amino-cyclohexyl)-N⁴,N⁴-dimethyl-quinazolin-2,4-diamine (1.8 g, 6.3-mmol) in 3 mL CH₂Cl₂ was added 6-chloronicotinyl choride (1.1 g, 6.3 mmol), DIEA (2.19 mL, 12.6 mmol). The reaction mixture was stirred for 30 minutes at room temperature, the solvent was removed under vacuum, and the residue was purified by column chromatography on silica gel (2-4% 2M, NH₃ in CH₃OH/CH₂Cl₂=5:10) to yield cis-6-chloro-N-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-nicotinamide (1.07 g, 40%).

ESI-MS m/e 425.0 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 8.76 (brs, 1 H), 8.46 (brs, 1 H) 8.37 (brs, 1 H), 8.19 (dd, J=8.0, 4.0 Hz, 1 H), 8.12 (d, J=8.0 Hz, 1 H), 7.74 (t, J=8.0 Hz, 1 H), 7.59 (d, J=8.0 Hz, 1 H), 7.40 (brs, 1 H), 7.32 (t, J=8.0 Hz, 1 H), 3.99 (brs, 1 H), 3.86 (brs, 1 H), 3.30 (brs, 6 H), 1.85-1.62 (m, 8 H).

Step B: Synthesis of 6-(3-cblorophenoxy)-N-(cis-4-{[4-(dimethylamino)q uinazolin-2-yl]amino}-cyclohexyl)nicotinamide trifluoroacetate

cis-6-Chloro-N-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-nicotinamide (30 mg, 0.07 mmol) was added into a stirred solution of 3-chlorophenol (17.9 mg, 0.14 mmol) and 60% NaH in mineral oil (5.6 mg, 0.14 mmol) in 0.5 mL DMA. The mixture was heated in a microwave synthesizer at 250° C. for 1 hour. The compound was then subjected to purification by prep LCMS to yield 6-(3-chlorophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)nicotinamide trifluoroacetate (8.2 mg, 0.016 mmol, 23 %) as a white solid.

ESI-MS m/e 517.02 M+H⁺; ¹H NMR(400 MHz, DMSO-d₆) δ 12.5 (s, 1 H), 8.63 (s, 1 H), 8.37 (brs, 1 H), 8.31 (dd, J=8.0, 4.0 Hz, 1 H), 8.21 (d, J=8.0 Hz, 1 H), 7.83 (t, J=8.0 Hz, 1 H), 7.56 (m, 2 H), 7.41 (m, 3 H), 7.22 (d, J=8.0 Hz, 2 H), 4.08 (brs; 1 H), 3.90 (brs, 1 H), 3.80-3.40 (brs, 6 H), 2.00-1.51 (m, 8 H).

Example 904

N-(cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-6-(3-fluorophenoxy)-nicotinamide trifluoroacetate

Step A: Synthesis of N-(cis-4-{[4(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-6-(3-fluorophenoxy)nicotinamide trifluoroacetate

Using a similar procedure as described in step B of Example 903, the title compounds was obtained.

ESI-MS m/e 501.2 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 1.20 (s, 1 H), 8.40 (brs, 1 H), 8.11 (brs, 1 H), 8.07-8.04 (m, 1 H), 7.97 (d, J=8.0 Hz, 1 H), 7.80 (brs, 1 H), 7.59 (t, J=8.0 Hz, 1 H), 7.29 (m, 2 H), 7.17 (t, J=8.0 Hz, 1 H), 6.97-6.86 (m, 3 H), 6.82 (d, J=8.0 Hz, 1 H), 3.85 (brs, 1 H), 3.77 (brs, 1 H), 3.40-3.20 (m, 6 H), 1.87-1.49 (m, 8 H).

Example 905

N-(cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-2-(3-fluorophenoxy)isonicotinamide trifluoroacetate

Step A: Synthesis of cis-2-chloro-N-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-isonicotinamide

To a solution of cis-N²-(4-amino-cyclolexyl)-N⁴,N⁴-dimethyl-quinazolin-2,4-diamine (1.0 g, 3.5 mmol) in 18 mL CH₂Cl₂ was added 2-chlorophvridine-4-carbonyl chloride (616.7 mg, 3.5 mmol). The reaction mixture was stirred for 30 minutes at room temperature, the solvent was removed under vacuum, and the residue was purified by column chromatography on silica gel (2-4% 2M HN₃ in CH₃OH/CH₂Cl₂=5:0) to yield cis-2-chloro-N-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-isonicotinamide (0.79 g, 54%) as a white solid.

ESI-MS m/e 425.0 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 8.58 (brs, 1 H), 8.50 (d, J=8.0 Hz, 1 H), 8.27 (brs, 1 H), 8.13 (d, J=8.0 Hz, 1 H), 7.81 (s, 1 H), 7.74-7.69 (m, 2 H), 7.40 (brs, 1 H), 7.32 (t, J=8.0 Hz, 1 H), 3.99 (brs, 1 H), 3.85 (brs, 1 H), 3.42 (brs, 6 H), 1.84-1.69 (m, 8 H).

Step B: Synthesis of N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-2-(3-fluorophenoxy)isonicotinamide trifluoroacetate

cis-2-Chloro-N-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-isonicotinamide (30 mg, 0.07 mmol) was added into a stirred solution of 3-fluorophenol (6.34 μl, 0.07 mmol) and 60% NaH in mineral oil (5.6 mg, 0.14 mmol) in 0.5 mL DMA. The mixture was heated in a microwave synthesizer at 250° C. for 1 hour. The compound was then subjected to purification by prep LCMS to yield N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-2-(3-fluorophenoxy)isonicotinamide trifluoroacetate (7.3 mg, 0.0146 mmol, 21%) as a white solid.

ESI-MS m/e 501.4 M+H³⁰ ; ¹H NMR (400 MHz, DMSO-d₆) δ 12.1 (s, 1 H), 8.58 (brs, 1 H), 8.28 (d, J=4.0 Hz, 1 H), 8.18 (d, J=8.0 Hz, 1 H), 7.98 (brs, 1 H), 7.79 (t, J=8.0Hz, 1 H), 7.52 (d, J=4.0 Hz, 1 H), 7.43. (m, 3 H), 7.34 (t, J=8.0 Hz, 1 H), 7.10-7.06 (m, 2 H), 7.00 (d, J=4.0 Hz, 1 H), 4.07 (brs, 1 H), 3.97 (brs, 1 H), 3.50 (brs, 6 H),1.89-1.75 (m, 8 H).

Example 906

N-(cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-2-(4-fluorophenoxy)isonicotinamide trifluoroacetate

Step A: Synthesis of N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-2-(4-fluorophenoxy)isonicotinamide trifluoroacetate

Using a similar procedure as described in step B of Example 905, the title compound was obtained.

ESI-MS m/e 501.3 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 12.5 (s, 1H), 8.58 (brs, 1 H), 8.23 (brs, 1 H),8.22 (d, J=4.0 Hz, 1 H) 8.18(d, J=8.0 H), 7.8 (t, J=8.0 Hz, 1 H) 7.47-7.30 (m,4 H), 7.28-7.14 (m, 4 H) 4.10 (brs, 1 H), 3.95 (brs, H), 3.47 (brs, 6 H), 2.00-1.50(m, 8 H).

Example 907

2-(2,3-Dichlorophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)acetamide trifluoroacetate

Step A: Synthesis of 2-(2,3-dichlorophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)acetamide trifluoroacetate.

To a solution of cis-N²-(4-amino-cyclohexyl)-N⁴,N⁴-dimethyl-quinazolin-2,4-diamine (28.5 mg, 0.1 mmol) in 0.5 mL DMF was added 2,3-dichlorophenoxyacetic acid (18.2 mg, 0.1 mmol), HATU (45.6 mg, 0.12 mmol), and DIEA (34.8 μL, 0.2 mmol). The reaction mixture was stirred for a couple of hours, and the compound was then subjected to purification by prep LCMS to yield 2-(2,3-dichlorophenoxy)-N-(cis-4-{[4-(dimethlamino)quinazolin-2-yl]amino}cyclohexyl)acetamide trifluoroacetate (12. 3 mg, 27%) as a white solid.

ESI-MS m/e 488.2 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 12.3 (s, 1 H), 8.16 (brs, 1 H), 8.12 (d, J=8.0 Hz 1 H), 7.81 (brs, 1 H), 7.74 (t, J=8.0 Hz, 1 H), 7.40 (brs, 1 H), 7.32 (t, J=8.0 Hz, 1 H), 7.27 (t, J=8.0 Hz, 1 H), 7.18 (d, J=8.0 Hz, 1 H), 6.99 (d, J=8.0 Hz, 1 H), 4.65 (s, 2 H), 3.95 (brs, 1 H). 3.76 (brs, 1 H), 3.41 (brs, 6 H), 1.72-1.62 (m 8 H).

Example 908

N-(cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}cyclohexyl-2-(2-naphthyloxy)acetamide trifluoroacetate

Step A: Synthesis of N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-2-(2-naphthyloxy)acetamide trifluoroacetate

To a solution of cis-N²-(4-amino-cyclohexy)-N⁴,N⁴-dimethyl-quinazolin-2,4-diamine (28.5 mg, 0.1 mmol) in 0.5 mL DMF was added 2-naphthoxyacetic acid (20 mg, 0.1 mmol), HATU (45.6 mg, 0.12 mmol), and DIEA (34.8 μL, 0.2 mmol). The reaction mixture was stirred for a couple of hours, and the compound was then subjected to purification by prep LCMS to N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-2-(2-naphthyloxy)acetamide trifluoroacetate (10.0 mg, 0.021 mmol, 21%) as a white solid.

ESI-MS m/e 470.4 M+H⁺; ¹H-NMR (400 MHz, DMSO-d₆) δ 12.1 (s, 1 H), 8.13 (d, J=12.0 Hz, 1 H), 8.02 (brs, 1 H), 7.93 (brs, 1 H), 7.80 (t, J=8.0 Hz, 2 H), 7.74-7.70 (m, 7 H), 7.41 (t, J=8.0 Hz, 2 H), 7.33 (m, ¹H), 7.20-7.17 (m, 1 H), 4.57 (s, 2H), 4.05 (brs, 1H), 3.76 (brs, 1H), 3.41 (brs, 6H), 1.71-1.62 (m, 8H).

Example 909

2-(3,4-Difluorophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-acetamide trifluoroacetate

Step A: Synthesis of cis-2-bromo-N-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-acetamide

To a solution of cis-N²-(4-amino-cyclohexyl)-N⁴,N⁴-dimethyl-quinazolin-2,4-diamine (1.0 g, 3.5 mmol) in 18 mL CH₂Cl₂ was added bromoacetyl bromide (305 μL, 3.5 mmol) at 0° C. The reaction mixture was stirred for 2 hours, the solvent was removed under vacuum, and the residue was purified by column chromatography on silica gel (2-4% 2M NH₃ in CH₂OH/CH₂Cl₂ to yield cis-2-bromo-N-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-acetamide (0.95 g, 2.35 mmol, 67%), as a yellowish solid

ESI-MS m/e 406.2 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 8.63 (brs, 1 H), 8.43 (brs, 1 H), 8.35 (d, J=8.0 Hz 1 H), 7.97 (t, J=8.0 Hz,1 H), 7.62 (brs, 1 H), 7.55 (t J=8.0 Hz, 1 H), 4.23 (brs, 1 H), 4.05 (s, 2 H), 3.89 (brs, 1 H), 3.70-3.60 (brs, 6 H), 2.00-1.75 (m, 8 H).

Step B: Synthesis of 2-(3,4-difluorophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-6l]-amino}cyclohexyl)acetamide trifluoroacetate

cis-2-Bromo-N-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]acetamide (60 mg, 0.15 mmol) was added into a stirred solution of 3,4-difluorophenol (19.3 mg, 0.15 mmol) and 60% NaH in mineral oil (11.8 mg, 0.30 mmol) in 1 mL DMA. The mixture was heated in a microwvave synthesizer at 250° C. for 1 hour. The compound was then subjected to purification by prep LCMS to yield 2-(3,4-difluorophenoxy)-N-(cis-4-{[4-(dimethylamino) quinazolin-2-yl]amino}-cyclohexyl)acetamide trifluoroacetate (32 mg, 0.07 mmol, 47%) as a white solid. ESI-MS m/e 456.2 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 12.4 (s, 1 H), 8.25 (brs, 1 H), 8.2 (d, J=8.0 Hz, 1 H), 7.99 (brs, 1 H), 7.83 (t, J=S.0 Hz, 1 H), 7.49 (brs, 1 H), 7.43-7.36 (m, 2 H), 7.13-7.08 (m, 1 H), 6.82 (brs, 1 H), 4.55 (s, 2 H), 4.06 (brs, 1 H), 3.81 (brs, 1 H), 3.5 (brs, 6 H), 1.89-1.75 (m, 8 H).

Example 910

2-(3,4-Difluorophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-propanamide trifluoroacetate

Step A: Synthesis of cis-2-bromo-N-[4-(4-dimethylamino-quinazolin-2-ylamine)-cyclohexyl]-propionamide

To a solution of cis-N-(4-anino-cyclohexyl)-N⁴,N⁴-dimethyl-quinazolin-2,4-diamine (1.0 g, 3.5 nmmol) in 18 mL CH₂Cl₂ was added 2-bromopropionyl bromide (189 μL, 1.75 mmol) at 0° C. The reaction mixture was stirred for 2 hours, the solvent was removed under vacuum, and the residue was purified by column chromatography on silica gel (2-4% 2M NH₃ in CH₃OH/CH₂Cl₂) to yield cis-2-bromo-N-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-propionamide (0.66 g, 45%) as a white solid.

ESI-MS m/e 410.2 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 8.17 (m, 3 H), 7.76 (t, J=8.0 Hz, 1 H), 7.40 (brs, 1 H), 7.32 (t, J=8.0 Hz, 1 H), 7.55 (q, J=4.0 Hz, 1 H), 3.99 (brs, 1 H), 3.57 (brs, 1 H), 3.41 (brs, 6 H), 1.69-1.50 (m, 11 H).

Step B: Synthesis of 2-(3,4-difluorophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]-amino}cyclohexyl)propanamide trifluoroacetate

cis-2-Bromo-N-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-propionamide (60 mg, 0.14 mmol) was added into a stirred solution of 3,4-difluorophenol (18.6 mg, 0.14 mmol) and 60% NaH in mineral oil ( 1.4 mg, 0.29 mmol) in 1 mL DMA. The mixture was heated in a microwave synthesizer at 250° C. for 1 hour. The compound was then subjected to purification by prep LCMS to yield 2-(3,4-difluorophenoxy)-N-(cis-4-{8 4-(dimethyl]amino)quinazolin-2-yl]amino}cyclohexyl)propanamide trifluoroacetate (6.7 mg, 0.01 4 mmol, 10%) as a white solid.

ESI-MS m/e 470.4 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 12.2 (s, 1 H), 8.19 (d, J=8.0 Hz, 1 H), 7.99 (brs, 1 H), 7.81 (t, J=8.0 Hz, 1 H), 7.46 (brs, 1 H), 7.39-7.31 (m, 2 H), 7.05-6.97 (m, 1 H), 6.75 (brs: 1 H), 4.80-4.73 (m, 1 H), 4.01(brs, 1 H), 3.71 (brs, 1 H), 3.47 (brs, 6 H), 1.62-1.47 (m, 8 H), 1.43 (d, J=4.0 Hz, 3 H).

Example 911

2-(3,4-Difluorophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-butanamide trifluoroacetate

Step A: Synthesis of cis -2-bromo-N-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-butyramide

To a solution of cis-N²-(4-amino-cyclohexyl)-N⁴,N⁴-dimethyl-quinazolin-2,4-diamine (1.0 g, 3.5 mmol in 18 mL CH₂Cl₂ was added 2-bromobutyryl bromide (213 μL, 1.75 mmol) at 0° C. The reaction mixtuire was stirred for 2 hours, the solvent was removed under v acuum, and the residue was purified by column chromatography on silica gel (2-4% 2M NH₃ in CH₃OH/CH₂Cl₂) to yield cis-2-bromo-N-[4-(4-dimethylamino-quinazolin-2-ylamino-cyclohexyl]-butyramide (0.53 g,35 %) as a white solid.

ESI-MS m/e 434.2 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 8.15 (brs,, 1 H), 8.12 (d, J=8.0 Hz, 2 H), 7.74 (t, J=8.0 Hz, 1 H), 7.40 (brs, 1 H), 7.32 (t, J=8.0 Hz, 1 H), 4.3.3 (t, J=8.0 Hz, 1 H), 3.93. (brs, 1 H). 3.66 (brs, 1 H), 3.41 (brs, 6 H), 2.01-1.87 (m, 1 H), 1.85-1.76 (m, 1 H), 1.70-1.59 (m, 8 H), 0.84 (t, J=8.0 Hz, 3 H).

Step B: Synthesis of 2-(3,4-difluorophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)butanamide trifluoroacetate

cis-2-Bromo-N-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-butyramide (60 mg, 0.14 mmol) was added into a stirred solution of 3,4-difluorophenol (18.6 mg, 0.14 mmol) and 60% NaH in mineral oil (10.8 mg, 0.27 mmol) in 1 mL DMA. The mixture was heated in a microwave synthesizer at 250° C. for 1 hour. The compound was then subjected to purification by prep LCMS to yield 2-(3,4-difluorophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)butanamide trifluoroacetate (6.3 mg, 93%) as a white solid.

ESI-MS m/e 484.2 M+H⁺; ¹H NMR (400 MHz DMSO-d₆) δ 12.2 (s, 1 H), 8.12 (d, J=8.0 Hz, 2 H), 8.09 (brs, 1 H), 7.93 (brs, 1 H), 7.74 (t, J=8.0 Hz, 1 H), 7.40 (brs, 1 H), 7.32-7.24 (m, 2 H), 6.97-6.91 (m, 1 H), 6.70-6.67 (m, 1 H), 4.56 (t, J=4.0 Hz, 1 H), 3.95 (brs, 1 H), 3.67 (brs, 2 H), 3.41 (brs, 6 H), 1.84-1.77 (m, 2 H), 1.75-1.56 (m: 8 H), 0.90-0.81 (t, J=16.0 Hz 3 H).

Example 912

N²-(3-Chlorophenyl)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-6l]amino}cyclohexyl)glycinamide bistrifluoroacetate

Step A: Synthesis of N²-(3-chlorophenyl)-N-(cis-4-{[4-(dimethlamino)quinazolin-2-yl]-amino}cyclohexyl)glycinamide bistrifluoroacetate

To a solution of cis-2-bromo-N-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-acetamide (40 mg, 0.1 mmol) in 0.5 mL DFF was added 3-chloroaniline (11.6 μL, 0.11 mmol). The reaction mixture was stirred at 100° C., and another 0.5 mL of DMSO was added. The compound was then subjected to purification by prep LCMS to yield N²-(3-chlorophenyl)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)glycinamide bistrifluoroacetate (6.0 mg, 8.3 %) as a white solid.

ESI-MlS m/e 453.2 M+H⁺; ¹H NMR (400 MHz, CD₃OD) δ 8.18 (d, J=8.4 Hz, 1 H), 7.77 (t, J=8.0 Hz, 1 H) 7.41 (m, 2 H), 7.11 (t, J=8.0 Hz, 1H), 6.66-6.51 (m, 3 H), 4.20 (brs, 1 H), 3.93 (brs, 1 H), 3.76 (s, 2 H), 3.54 (brs, 6 H), 1.87-1.17 (m, 8 H).

Example 913

2-(3,5-Difluorophenyl)-N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-methyl]-2-hydroxyacetamide trifluoroacetate

Step A: Synthesis of cis-(4-amino-cyclohexylmethyl)-carbamic acid benzyl ester

To a solution of (4-aminomethyl-cyclohexl!)-carbamic acid tert-butyl ester (21.9 g, 96.0 mmol) in 400 mL CH₂-Cl₂ was added DIEA (16.6 mL, 96 mmol), CbzCl (11.4 mL, 79.7 mmol). The reaction mixture was stirred at room temperature for 3 hours, and the solvent was then removed under vacuum, and the residue was purified by column chromatography on silica gel (Hexane/EtOAc=1:1). The purified compound in 100 mL CH₂Cl₂ was added TFA (60 mL). The solution was stirred at room temperature for 2 hours. The excess solvent was evaporated off and the resulting oil was dissolved in CH₂Cl₂. The organic layer was extracted with a dilute NaCH (aq) solution. The aqueous layer was extracted twice more with CH₂Cl₂ and the organic layers combined, dried over MgSO₄, and concentrated to yield cis(4-amino-cyclohexylmethyl)-carbamic acid benzyl ester (20 g, 79%) as a yellow solid.

ESI-MS m/e 263.2 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 7.82 (brs, 2 H), 7.39-7.29 (m, 6 H), 5.06 (s, 2 H), 3.15 (brs, 1 H), 2.98 (m, 1 H), ?,51(m, 1 H), 1.60-1.2-4 (m, 8 H).

Step B: Synthesis of cis-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexylmethyl]-carbamic acid benzyl ester

To a solution of cis-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexylmethly]-carbamic acid benzyl ester (0.5 g, 1.9 mmol) in 1 mL 2-propanol was added (2-chloro-quinazolin-4-yl)-dimethyl-amine (0.33 g, 1.58 mmol) and DIEA (661 μL, 3.8 mmol). The mixture was heated in a microwave synthesizer at 150° C. for 1 hour. The reaction was repeated 39 more times (20 g total material) and the reaction mixtures were pooled. The solvent was evaporated and the material subjected to chromatography (2-4% 2M NH₃ in MeOH/CH₂Cl₂) to yield cis-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexylmethyl]-carbamic acid benzyl ester (16 g, 49%) as a yellowish oil.

ESI-MS m/e 434.2 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 8.59 (brs, 1 H), 8.14 (d, J=8.0 Hz, 1 H), 7.76 (t, J=8.0 Hz, 1 H), 7.34 (d J=8.0 Hz, 1 H), 7.35 (m, 7 H), 5.06 (s, 2 H), 4.24 (brs, 1 H), 3.59 (brs, 6 H), 2.85 (brs, 2 H), 1.66-1.35 (m, 9 H).

Step C: Synthesis of cis-N²-(4-aminomethyl-cyclohexyl)-N⁴,N⁴-dimethyl-quinazoline-2,4-diamine

To cis-[4-(4-dimetylamino-quinazolin-2-ylamino)-cyclohexylmethyl]-carbamic acid benzyl ester (16.0 g 37 mmol) in ethanol was added 10% Pd/C (1.6 g). The reaction mixture was stirred at room temperature under an H₂ atmosphere for 3 hours. The H₂ atmosphere was removed and the solution filtered though celite and concentrated to yield cis-N²-(4-aminomethyl-cyclohexyl)-N⁴,N⁴-dimethyl-quinazoline-2,4-diamine (11.2 g, 99%) as a yellowish solid.

ESI-MS m/e 300.2 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 8.50 (brs, 1 H), 8/10 (d, J=127.0 Hz, 1 H), 7.71-7.61 (m, 3 H), 7.34 (d, J=8.0 Hz, 1 H), 7.27 (t, J=8.0 Hz, 1 H), 4.11 (brs, 1 H), 3.30 (brs, 6 H), 2.65 (brs, 2 H), 1.67-1.19 (m, 9 H).

Step D: Synthesis of 2-(3,5-difluorophenyl)-N-[(cis-4-{[4-dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-2-hydroxyacetamide trifluoroacetate

To a solution of cis-N²(4-aminonethyl-cyclohexyl)-N⁴,N⁴-dimethyl-quinazoline-2,4-diamine (29.9 mg, 0.1 mmol) in 0.5 mL DMF was added 3,5-difluoromandelic acid (18.8 mg, 0.1 mmol), HATU (45.6 mg, 0.12 mmol), and DIEA (34.8 μL, 0.2 mmol). The reaction mixture was stirred for a couple of hours, and the compound was then subjected to purification by prep LCMS to 2-(3,5-difluorophenyl)-N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl) methyl]-2-hydroxyacetamide trifluoroacetate (29.5 mg, 51%) as a white solid. ESI-MS m/e 470.4 M+H⁺; ¹H NMR (400 MHz, CD₃OD) δ 8.16 (d, J=8.0 Hz, 1 H), 7.76 (t, J=8.4 Hz, 1 H), 7.39 (m, 2 H), 7.12 (m, 2 H), 6.86 (m, 1 H), 5.04 (s, 1 H), 4.21 (brs, 1 H), 3.53 (brs, 6 H), 3.21 (m, 2 H), 1.86-1.39 (m, 9 H).

Example 914

2-(3,5-Difluorophenyl)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-2-hydroxyacetamide trifluoroacetate

Step A: Synthesis of 2-(3,5-difluorophenyl)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl-2-hydroxyacetamide trifluoroacetate

To a solution of cis-N²-(4-amino-cyclohexyl)-N⁴,N⁴-dimethyl-quinazolin-2,4-diamine (28.5 mg, 0.1 mmol) in 0.5 mL DMF was added 3,5-difluoromandelic acid (18.8 mg, 0.1 mmol), HATU (45.6 mg, 0.12 mmol), and DIEA (34.8 μL, 0.2 mmol). The reaction mixture was stirred for a couple of hours, and the compound was then subjected to purification by prep LCMS to yield 2-(3,5-difluorophenyl)-N-(cis-4-{[4-(dimethylamino)quiazolin-2yl]amino}cyclolexyl)-2-hydroxy acetamide trifluoroacetate (20.5 mg, 0.045 mmol, 45%) as a white solid.

ESI-MS m/e 456.2 M+H¹; ¹H NMR (400 MHz, DMSO-d₆) δ 12.3 (s, 1 H), 8.29 (d, J=8.0Hz, 1 H), 8.18 (brs, 1 H), 7.91 (m, 2 )H, 7.58 (brs, 1 H), 7.49 (t, J=8.0 Hz, 1 H), 7.25-7.22 (m, 3 H), 6.55 (brs, 1 H), 5.13 (s, 1 H), 4.15 (brs, 1 H), 3.82 (brs, 1 H), 3.58 (brs, 6 H), 1.85-1.73 (m 8 H).

Example 915

cis-N-Benzyl-4-[(4-isopropylquinazolin-2-yl)amino]clcylhexanecarboxamide trifluoroacetate

Step A: Synthesis of 2-chloro-4-isopropylquinazoline

2,4-Dichloroquinazoline (0.5 g, 2.5 mmol) and 1,2-bis(diphenylphosphino) ethane nickel (II) chloride (15 mg) were mixed with THF (10 mL), and the reaction was kept under an inert atmosphere. The reaction flask was cooled in a cold bath (˜20° C.), and isopropyl magnesium chloride (1.25 mL of 2M solution, 2.5 mmol) introduced into the reaction through a syringe. The reaction was slowly allowed to room temperature, and stirred ovennight. The reaction was quenched with addition of 1N-HCl (˜5 mL), diluted with water, and extracted with DCM (3×10 mL). Te organic layer was washed with aqueous NaHCO₃ (1×10 nmL) and wiater (1×10 mL), dried with MgSO₄, and concentrated. The crude was purified by column chromatography, (silica gel, hexanes: DCM=90:10 to 70:30) to give 0.11 g (20%) of 2-chloro-4-isopropylquinazoline as a white solid.

ESI MS m/e 207 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 8.16 (d, J=8.0 Hz, 1 H), 7.97 (d, J=8.0 Hz, 1 H), 7.89 (t, J=8.0 Hz, 1 H), 7.63 (t, J=S.0 Hz, 1 H), 3.90 (m, 1 H), 1.44 (d, J=7.0 Hz, 6 H).

Step B: Synthesis of cis-4-amino-cyclohexanecarboxylic acid ethyl ester hydrochloride

To a suspension of cis-aminocyclohexane-4-carboxylic acid (1.5 g, 10 mmol) in EtOH (15 mL) was added concentrated HCl (1.5 mL). The reaction was stirred for 2 h at 72° C. Removal of the volatile solvent under a vacuum gave cis-4-amino-cyclohexanecarboxylic acid ethyl ester hydrochloride (1.7 g, 96) as a white power, which was used directly to the next reaction without further purification.

ESI MS m/e 172 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 4.43 (brs, 2 H), 4.05 (q, J=7.2 Hz, 2 H), 3.02 (brs, 1 H), 2.48 (m, 1 H), 1.93 (m, 2 H), 1.76 (m, 2 H) 1.43-1.57 (m, 4 H), 1.17 (t, J=7.2 Hz, 3 H).

Step C: Synthesis of cis-4-(4-isopropyl-quinazolin-2-ylamino)-cyclohexane carboxylic acid ethyl ester

A solution of 2-chloro-4-isopropylquinazoline (0.26 g, 1.26 mmol) and cis-(4-ethoxycarbonyl)aminocyclohexane hydrochloride (0.26 g, 1 eq.) in IPA (2 mL) and DIEA (0.4 mL, 2 eq.) was reacted for 4 h at 160° C. in a Smith synthesizer. The reaction was purified from column chromatography (silica gel, DCM/MeOH=100:0 to 90:10) to give 0.25 g (58%) of cis-4-(4-isopropyl-quinazolin-2-yalamino)-cyclohexanecarboxylic acid ethyl ester.

ESI MS m/e 342 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 7.90 (d, J=8.0 Hz, 1 H), 7.60 (m, 1 H), 7.55 (d, J=8.0 Hz, 1 H), 7.17 (t, J=8.0Hz, 1 H), 5.22 (d, J=7.0 Hz, 1 H), 4.21(brs, 1 H), 4.16 (q, J=7.0 Hz, 2 H), 3.74 (m, 1 H), 2.50 (m, 1 H) 1.96 (m, 2 H), 1.86-1.77 (m, 6 H), 1.36 (d, J=7.0 Hz, 6 H), 1.27 (t, J=7.0 Hz, 3 H).

Step B: Synthesis of cis-4-(4-isopropl-quinazolin-2-ylamino)-cyclohexane carboxylic acid

A suspension of cis-4-(4-isopropyl-quinazolin-2-ylamino)-cyclohexane carboxylic acid ethyl ester (0.25 g, 0.7 mmol) in 4N-HCl (8 mL) was stirred for 3 h at 85° C. During the reaction, the heterovenous solution turned to be a clear solution, and then the precipitate was formed. The solid was filtered, washed with cold water several times, and dried to give 0.13 g, (58%) of cis-4)4-isopropyl-quinazolin-2-ylamino)-cyclohexane caboxylic acid as a white solid. ESI MS m/e 314 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 12.25 (brs, 1 H), 9.56 (brs, 1 H), 8.40-8.26 (m, 2 H), 8.01 (m, 1 H), 7.59 (m, 1H), 4.31 (brs, 1 H), 4.03 (m, 1 H), 2.62 (brs, 1 H), 2.14 (m, 2 H), 1.93-1.66 (m, 6 H), 1.37 (d, J=6.4 Hz, 6 H).

Step E: Synthesis of cis-N-benzyl-4-[(4-isopropylquinazolin-2-yl)amino]cyclohexanecarboxamide trifluoroacetate

cis-4-(4-Isoprop)l-quinazolin-2-ylamino)-cyclohexane carboxylic acid (20 mg, 0.06 mmol) and benzyl amine (7 mg, 0.06 mmol) was reacted in the presence of HATU (25 mg, 0.066 mmol and Et₃N (4 drops) at room temnperature for 16 hr. cis-N-benzyl-4-[(4-isopropylquiazolin-2-yl) amino]cyclohexanecarboxamide trifluoroacetate (13 mg, 40%) was obtained from a prep-HPLC.

ESI MS m/e 403 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 9.06 (brs, 1 H), 8.24 (m, 2 H), 7.88 (brs, 1 H), 7.75-7.59 (m, 1 H), 7.45 (brs, 1 H), 7.17 (m, 2 H), 7.17 (m, 3 H), 4.24 (brs, 1 H), 4.23 (d, J=6.0 Hz, 2 H), 3.92 (m, 1 H), 2.33 (brs, 1 H), 1.95-1.58 (m, 8 H), 1.26 (d. J=6.4 Hz, 6 H).

Example 916

cis-N-(3-Chlorobenzyl)-4-[(4-isopropylquinazolin-2-yl)amino]cyclohexanecarboxamide trifluoroacetate

Step A: Synthesis of cis-N-(3-chlorobenzyl)-4-[(4-isopropylquinazolin-2-yl)amino]-cyclohexancarboxamide triluoroacetate

Using a similar procedure as described in step E of Example 915, the title compound was obtained.

ESI MS m/e 437 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 9.04 (brs, 1 H), 8.30 (t, J=5.4 Hz, 1 H), 8.20 (brs, 1 H), 7.86 (brs, 1 H), 7.71-7.57 (m, 1 H), 7.45 (brs, 1 H), 7.30-7.22 (m, 3 H), 7.15 (d, J=8.0 Hz, 1 H), 4.24 (brs, 1 H), 4.23 (d, J=6.0 Hz, 2 H), 3.92 (m, 1 H) 2.33 (brs, 1 H), 1.95-1.58 (m, 8H), 1.26 (d, J=6.6 Hz, 6 H).

Example 917

3,4-Dichloro-N-[((1R,3S)-3-({[4-(dimethylamino)quinazolin-2yl]amino}cyclopentyl)methyl]-bemzamide trifluoroacetate

Step A: Synthesis of cis-(1R,3S)-3-tert-butoxycarbonylamino-cyclopentanecarboxylic acid ethylformate ester

(1S,3R)-N-Boc-1-aminocyclopentane-3-carboxylic acid (10.00 g, 43.6 mmol) was dissolved in dichloromethane (100 mL) and cooled to −65° C. Triethylamine (9.19 mL, 65.9 mmol) and a solution of ethyl chloroformate (4.24 mL, 44.4 mmol) in dichloromethane (14 mL) were added and the mixture stirred at 0° C. for 1 hr. The mixture was acidified to pH ˜6 with 1N HCl (aq) and extracted with dichloromethane. The organic phase was washed with saturated aqueous NaHCO₃, water, and brine, dried over Na₂SO₄, filtered, and concentrated to give cis-(1R,3S)-3-tert-butoxycarbonnylamino-cyclopentanecarboxylic acid ethylformate ester as a clear oil.

ESI MS m/e 302, M+H⁺; ¹H N MNR (400 MHz, DMSO-d₆) δ 6.92 (brs, 1 H), 4.25 (q, J=7.2 Hz, 2 H), 3.78 (m, 1 H), 2.98 (m, 1 H), 2.16 (m, 2 H), 1.84 (m, 2 H), 1.80 (m, 2 H), 1.38 (s, 9 H), 1.25 (t, J=7.2 Hz, 3 H).

Step B: Synthesis of cis-(1S,3R)-(3-hydroxymethyl-cyclopentyl)-carbamic acid tert-butyl ester

The 3-tert-butoxycarbonylamino-cyclopentanecarboxylic acid ethylformate ester was then dissolved in tetrahydroforan (106 mL) and cooled to −65° C. Sodium borohydride (1.91 g, 50.5 mmol) and methanol (3.39 mL) were added and the mixture stirred at −40° C. for 30 min., then at 0° C. for 3 hr. 10% HCl (aq) was added to pH 3 and the mixture was concentrated to half volume. Then it was extracted with ethyl acetate, washed with water, brine, dried over Na₂SO₄, filtered, and concentrated to give (1S,3R)-(3-hydroxymethyl-cyclopentyl)-carbamic acid tert-butyl ester as a white solid (8.65 g, 92%).

ESI MS m/e 216, M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 6.74 (d, J=6.8 Hz, 1 H), 4.46 (bt, J=4.8 Hz, 1 H), 3.70 (m, 1 H), 3.25 (t, J=5.6 Hz, 2 H), 1.92 (m, 2 H), 1.73 (m, 2 H), 1.55 (m, 2 H), 1.38 (s 9 H) 1.05 (m, 1 H).

Step C: Synthesis of cis-(1S,3R)-[3-(1,3-dioxo-1,3-dihydro-isoindol-2-ylmethyl)-cyclopentyl]-carbamic acid tert-butyl ester

cis-(1S,3R)-(3-Hydroxymethyl-cyclopentyl)-cabamic acid tert-butyl ester (8.65 g, 40.2 mmol), triphenylphosphine (10.54 g, 40.2 mmol), and phthalimide (5.91 g, 40.2 mmol) were dissolved in tetrahydrofuran (128 mL). The mixture was cooled to 0° C. and a solution of diethylazodicarboxylate (6.96 mL, 44.22 mmol) in tetrahydrofuran (30 mL) was added over a period of 1 hr. The mixture stirred at room temperature for 18 hr, concentrated, and purified by silica get chromatography (30% ethyl acetate in hexanes) to give cis-(1S,3R)-[3-(1,3-dioxo-1,3-dihydro-isoindol-2-ylmethyl-cyclopentyl]-carbamic acid tert-butyl ester (9.52 g, 69%) as a solid.

ESI MS m/e 345 M+H⁺; ¹H NMR (400MHz, DMSO-d₆) δ 7.83 (mn, 4 H), 6.84 (dd, J=11.2, 7.6 Hz, 1 H, 3.70 (m, 1 H), 3.54 (m, 2 H), 1.92 (m, 2 H), 1.73 (m, 2 H), 0.55 (m, 2 H), 1.38 (s, 9 H), 1.10 (m, 1 H).

Step D: Synthesis of cis-(1S,3R)-(3-aminonethyl-cyclopentyl)-carbamic acid tert-butyl ester

The cis-(1S,3R)-[3-(1,3-dioxo-1,3-dihidro-isoindol-2-yl methyl)-cyclopentyl]-carbamic acid tert-butyl ester was suspended in 95% ethanol (143 mL), hydrazine (1.89 mL, 60.3 mmol) was added, and the mixture was heated to reflux temperature (120° C.) for 2.5 hr, then stirred at room temperature for 18 hr. The suspension was concentrated, suspended in 10% NaOH (aq) (182 mL), extracted with dichloromethane, dried over Na₂SO₄, filtered, and concentrated to give cis-(1S,3R)-(3-aminomethyl-cyclopentyl)-carbamic acid tert-butyl ester as a white solid (6.25 g, ˜73%) (crude).

ESI MS m/e 215, M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 6.82 (d, J=6.3 Hz, 1 H), 3.70 (m, 1 H), 1.92 (m, 2 H), 1.75 (m, 2H), 1.73 (m, 2 H), 1.58 (m, 2 H), 1.38 (s, 9 H), 1.30 (m, 2 H), 1.00 (m, 1 H).

Step E: Synthesis of cis-(1S,3R)-N-(3-amino-cyclopentylmethyl)-3,4-dichlorobenzamide

(cis-(1S,3R)-(3-Aminomethyl-cyclopentyl)-carbamic acid tert-butyl ester (0.050 g, 0.230 mmol), 3,4-dicllorobenzoyl chloride (0.049 g, 0.230 mmol), and diisopropylethylamine (0.10 mL, 0.57 mmol) were combined in dichloromethane (2 mL) and stirred for 18 hr at room temperature. The mixture was concentrated, neutralized with saturated aqueous NaHCO₃, and extracted with dichloromethane. The organic phase was then concentrated to give cis-(1S,3R)-N-(3-amino-cyclopentylmethyl)-3,4-dichloro-benzamide as the crude product.

ES MS m/e 287, M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 8.72 (t, J=5.6 Hz, 1 H), 8.04 (d, J=2.0 Hz, 1 H), 7.78 (d, J=2.0 Hz, 1 H), 7.74 (s, 1 H), 3.40 (m, 2 H), 2.80 (brs, 2 H), 2.15 (m, 1 H), 1.88 (m, 2 H), 1.70 (m, 1 H), 1.58 (m, 2 H), 1.48 (m, 2 H).

Step F: Synthesis of 3,4-dichloro-N-[(1R,3S)-3-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclopentyl)methyl]benzamide trifluoroncetate

cis-(1S,3R)-(2-Chloro-quinazolin-4-yl)-dimethyl-amine (0.048 g, 0.23 mmol), N-(3-amino-cyclopentylmethyl)-3,4-dichloro-benzamide (0.23 mmol), diisopropylethylamine (0.061 mL, 0.34 mmol), and isopropanol (1.50 mL) were combined and heated to 160° C. for 40 min. utilizing a Smith synthesizer microwave apparatus. The mixture was then purified by HPLC to give 3,4-dichloro-N-[((1R,3S)-3-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclopentyl)methyl]benzamide trifluoroacelate as a white solid (0.035 g, 26.% over four steps).

ESI MS m/e 458, M+H⁺; ¹H NIR (400 MHz, DMSO-d₆) δ 8.70 (t, J=5.2 Hz, 1 H), 8.20 (brs, 1 H), 8.14 (d, J=8.0 Hz, 1 H), 8.04 (d, J=1.6 Hz, 1 H), 7.80 (d, J=2.0 Hz, 1 H), 7.78 (d, J=2.0 Hz, 1 H), 7.74 (s, 1 H), 7.44 (brs, 1 H), 7.34 (t, J=7.6 Hz, 1 H), 3.29 (t, J=5.2 Hz, 2 H), 2.50 (s, 6 H), 2.24 (m, 1 H), 2.00 (m, 2 H), 1.76 (m, 1 H), 1.65 (m, 2 H), 1.50 (m, 2 H).

Example 918

N²-[(1S,3R)-3-({[4-Bromo-2-(trifluoromethoxy)benzyl]amino}methyl)cyclopentyl]-N⁴,N⁴-dimethylquinazoline-2,4-diamine bistrifluoroacetate

Step A: Synthesis of cis-(1S,3R)-3-[(4-bromo-2-trifluoromethoxy-benzylamino)-methyl]-cyclopentylamine

(3-Aminomethyl)-cyclopentyl)-carbamic acid tert-butyl ester (0.050 g, 0.23 mmol), 4-bromo-2-trifluoromethoxybenzaldehyde (0.063 g, 0.23 mmol), and sodium cyanoborohydride (0.022 g, 0.34 mmol) were combined in methanol (1.00 mL) and stirred at room temperature for 18 hrs. The mixture was concentrated, water (1.00 mL) was added, and it was extracted with dichloromethane. To the organic phase was added trifluoroacetic acid (1.00 mL) and the mixture stirred at room temperature for 18 hrs. The mixture was concentrated, neutralized with saturated aqueous NaHCO₃, extracted with dichloromethane, and concentrated to give (1S,3R)-3-[(4-bromo-2-trifluoromethoxy-benzylamino)-methyl]-cyclopentlamine as the crude product.

ESI MS m/e 367, M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 7.75-7.62 (m, 3 H), 4.58 (s 1 H), 3.77 (s, 2 H), 3.35 (brs, 2 H), 2.48 (m, 2 H), 2.04 (m, 1 H), 1.74 (m, 2 H), 1.38 (m, 2 H), 1.30 (m, 2 H) 0.98 (m, 1 H).

Step B: Synthesis of N-[(1S,3R)-3-({[4-bromo-2-(trifluoromethoxy)benzyl]amino}methyl)-cyclopentyl]-N⁴,N⁴-dimethylquinazoline-2,4-diamine bistrifluoroacetate

(2-Chloro-quinazolin-4-yl)-dimethyl-amine (0.048 g, 0.23 mmol), (1S,3R)-3-[(4-bromo-2-trifluoromethoxy-benzylamino)-methyl]-cyclopentylamine (0.23 mmol), diisopropylethylamine (0.061 mL. 0.34 mmol), and isopropanol (1.50 mL) were combined and heated to 160° C. for 40 min. utilizing a Smith Synthesizer microwave apparatus. The mixture was then purified by HPLC to give N²-[(1S,3R)-3-({[4-bromo-2-(trifluoronmethoxy)benzyl]amino}methyl)cyclopentyl]-N⁴,N⁴-dimethylquinazoline-2,4-diamine bistrifluoroacetate as a white solid (0.011 g, 62% over four steps).

ESI MS m/e 538 , M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 8.45 (brs, 1 H), 8.14 (d, J 12.0 Hz, 1 H), 7.72 (d, J=2.0 Hz, 1 H), 7.68 (d, J=2.0 Hz, 1 H), 7.63 (s, 1 H), 7.58 (d, J=2.0 Hz, 1 H), 7.44 (brs, 1 H), 7.29 (bt, J=7.6 Hz, 1 H), 4.18 (s, 2 H), 3.40 (s, 2 H), 3.40 (s, 6H) 2.25 (m, 2 H), 1.98 (m, 1 H), 1.82 (m, 2 H), 1.60 (m, 2 H), 1.40 (m, 2 H), 1.22 (m, 1 H).

Example 919

N-[(1S,3R)-3-({[4-(Dimethylamino)quinazolin-2-yl]amino}methyl)cyclopentyl]-4-fluorobenzamide trifluoroacetate

Step A: Synthesis of (1R,3S)-N²-(3-amino-cyclopentylmethyl)-N⁴,N⁴-dimethyl-quinazoline-2,4-diamine

(2-Chloro-quinazolin-4-yl)-dimethyl-amine (0.048 g, 0.23 mmol), (1S,3R)-(3-aminomethyl-cyclopentyl)-carbarnic acid tert-butyl ester (0.050 g, 0.23 mmmol), diisopropylethylamiiie (0.061 mL, 0.34 mmol), and isopropanol (1.50 mL) were combined and heated to 160° C. for 40 min. utilizing a Smith synthesizer microwave apparatus. The mixture was concentrated, dichloromethane (2.00 mL) and trifluoroacetic acid (1.00 mL) wvere added, and the mixture stirred at room temperature for 18 hr. Then it was concentrated, neutralized with saturated aqueous NaHCO₃, extracted with dichloromethane, and concentrated to give (1R,3S)-N²-(3-amino-cyclopentylmethyl)-N′,N′-dmethyl-quinazoline-2,4-diamine as the crude product.

ES MS m/e 286, M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 7.92 (d, J=8.0 Hz, 1 H), 7.53 (t. J=6.0 Hz, 1 H), 7.34 (d, J=7.06 Hz, 1 H), 7.06 (t, J=6.0 Hz, 1 H), 6.78 (brs, 1 H), 3.25 (s, 6 H), 2.28 (m, 2 H), 2.10 (m, 2 H), 1.86 (m, 1 H), 1.75 (m, 2 H), 1.52 (m, 2 H), 1.30 (brs, 2 H), 1.17 (1 H).

Step B: Synthesis of N-[(1S,3R)-3-({[4-(dimethylamino)quinazolin-2-yl]amino}methyl)-cyclopentyl]-4-fluorobtenzamide trifluoroacetate

cis-(1R,3S)-N²-(3-Amino-cyclopenylmethyl)-N⁴,N⁴-dimethyl-quinazoline-2,4-diamine (0.23 mmol), 4-fluorobenzoyl chloride (0.028 mL, 0.23 mmol), and diisopropylethylamine (0.10 mL, 0.57 mmol) were combined in dichloromethane (2.00 mL) at room temperature and stirred for 18 hrs. The mixture was concentrated, dissolved in methanol, and purified by prep-LCMS to give N-[(1S,3R)-3-({[4-(dimethylamitio)quinazolin-2-yl]amino}methyl)cyclopentyl]-4-fluorobenzamide trifluoroacetate as a white solid (5 mg, 4.1 % over four steps).

ESI MS m/e 408, M+H⁺; ¹H NMR (400 MHz, CD₃OD) ε 8.09 (d, J=8.0 Hz, 1 H), 7.76 (d, J=5.3 Hz, 2 H), 7.74(d, J=5.3Hz,2H),7.66(t,J=8.3Hz,1H),7.) 7.30 (bm,2H),7.07 (t, J=4.9 Hz,1 H), 4.25 (m, 1 H), 3.45 (brs, 6 H), 2.2-5 (m?, 2 H), 2.00 (m, 1 H), 1.70 (m, 2 H), 1.62 (m, 2 H), 1.52 (m, 2 H), 1.26 (m, 1 H).

Example 920

N²-({(1R,3S)-3-[(3,4-Difluorobenzyl)amino]cyclopentyl}methyl)-N⁴,N⁴-dimethylquinazoline-2,4-diamine bistrifuoroacetate

Step A: Synthesis of N²({(1R,3S)-3-[(3,4-difluorobenzyl)amino]cyclopentyl}methyl)-N⁴,N⁴-dimethylquinazoline-2,4-diamine bistrifluoroacetate

(1R,3 S)-N²-(3-Amino-cyclopentylmethyl)-N⁴, N⁴-dimethyl-quinazoline-2,4-diamine (0.23 mmol), 3,4-difluorobenzaldehyde (0.026 mL, 0.23 mmol), and sodium cyanoborohydride (0.022 g, 0.34 mmol) were combined in methanol (1.00 mL) and stirred at room temperature for 18 hr. Water (0.50 mL) was added and the mixture was then purified by prep-LCMS to give N²-({(1R,3S)-3[(3,4-difluorobenzyl)amino]cyclopentyl}methyl)-N⁴,N⁴-dimethylquinazoline-2,4-diamine bistrifluoroacetate as a white solid (0.011 g, 7.4% over four steps). ESI MS m/e 412, M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 8.83 (brs, 1 H), 8.12 (d, J=7.7 Hz, 1 H), 7.73 (t, J=4.9 Hz, 1 H), 7.55 (t, J=9.7 Hz, 1 H), 7.50 (q, J=8.9 Hz, 1 H), 7.31 (m, 2 H), 4.09 (brs, 1 H), 3.42 (brs, 6 H), 3.36 (brs, 1 H), 2.18 (m, 2 H), 1.95 (m, 1 H), 1.69 (m, 2 H), 1.42 (m, 2 H), 1.26 (m, 2 H), 1.18 (brs, 2 H) 0.81 (m, 1 H).

Example 921

cis-N-(1,3-Dimethoxybenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide

Step A: Synthesis of cis-4-amino-cyclohexanecarboxylic acid ethyl ester hydrochloride

To a suspension of cis-aminocyclohexane-4-carboxylic acid (1.5 g, 10 mmol) in EtOH (15 mL) was added concentrated HCl (1.5 mL). The reaction was stirred for 2 hr at 72° C. Removal of the volatile solvent under a vacuum gave cis-4-amino-cyclohexanecarboxylic acid ethyl ester hydrochloride (1.7 g, 96%) as a white power, which was used directly to the next reaction without a further purification.

ESI IS m/e 172 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 4.43 (brs, 2 H), 4.05 (q, J=7.2 Hz, 2 H), 3.02 (brs, 1 H), 2.48 (m, 1 H), 1.943 (m, 2 H), 1.76 (m, 2 H), 1.43-1.57 (m, 4 H), 1.17 (t, J=7.2 Hz, 3 H).

Step B: Synthesis of cis-4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexane carboxylic acid ethyl ester

The reaction was done in seven vials. Each vial contains 2-chloro-4-N,N-dimethylamino quinazoline (0.26 g, 1.25 nimol), cis-(4-ethoxycai-bonyl)aminocyclohexane hydrochloride (0.25 g, 1 eq.), DIEA (0.45 mL, 2 eq.), and IPA (2 mL). The vials were heated at 155° C. for 1 hr using a Smith microwave synthesizer. The vial contents were combined and concentrated. The residue was purified on silica gel column using CH₂Cl₂/MeOH (100:0 to 85:15) to give cis-4(4-dimethylamino-quinazolin-2-ylamino)-cyclohexane carboxylic acid ethyl ester (2.2 g, 76%) as pale yellow oil.

ESI MS m/e 343 M+H⁺; ¹H NMR (400 MHz, MeOD) δ 8.17 (d, J=8.0 Hz, 1 H), 7.76 (t,J=8.0 Hz, 1 H), 7.40 (brs, 1 H), 7.40 (t, J=8.0 Hz, 1H), 4.660 (brs, 1 H), 4.16 (q, J=6.8 Hz, 2 H), 3.53 (s, 6 H), 2.59 (m, 1 H), 1.97-1.63 (m, 8 H), 1.27 (t, J=6.8 Hz, 3 H), the

Step C: Syntlieis of cis-4-(4-dimethylamino-quinaolin-2-ylamino)-cyclohexane carboxylic acid

A suspension of cis-4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexane carboxylic acid ethyl ester (0.35 g, 1 mmol) in 4N-HCl (10 mL) was stirred at 82° C. for 2 h. During the reaction, the heterogenous solution turned to be a clear solution, and then the precipitate was formed. The solid was filtered, washed with cold water several times, and dried to give 0.29 g (90 %) of cis-4(4-dimethylamino-quinazolin-2-ylamino)-cyclohexane carboxylic acid as a white solid.

ESI MS m/e 315 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 12.3 (brs, 1 H), 8.13 (d, J=7.6 Hz, 2 H), 7.74 (t, J=7.6 Hz, 1 H), 7.37 (brs, 1 H), 7.36 (t, J=7.6 Hz, 1 H), 4.05 (brs, 1 H), 3.32 (s, 6 H), 2.42 (brs, 1 H), 1.82-1.68 (m, 8 H).

Step D: Synthesis of cis-N-(2,3-dimethoxybenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]-amino}cyclohexanecarboxamide

To a suspension of the acid (25 mg, 0.08 mol) and the 2,3 dimethoxy benzyl amine (13 mg, 0.08 mmol) in DCM (3 mL) was added HATU (33 mg, 0.088 mmol), and followed Et₃N (4 drops). The reaction was stirred overnight at room temperature under an inert atmosphere. After removal of the volatile solvent, the crude product was purified by column chromatography (silica gel, DCM/MeOH=100:0 to 90:10) to give cis-N-(2,3-dimethoxybenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide (8 mg, 21%).

ESI MS m/e 464 M+H+; ¹H NMR (400 MHz, CDCl₃) δ 8.34 (brs, 1 H), 7.89 (d, J=8.4 Hz, 1 H), 7.57 (t, J=6.8 Hz, 1 H), 7.33 (d, J=8.0 Hz, 1 H), 7.23 (t, J=7.6 Hz, 1 H), 7.07 (brs, 1 H), 6.95 (t, J=7.6 Hz, 1 H), 6.89 (d, J=8.0 Hz, 1 H), 6.76 (d, J=8.0Hz, 1 H), 4.56 (d, J=5.6Hz, 2 H), 4.30 (m, 1 H), 3.33 (s, 3 H), 3.80 (s, 3 H), 3.48 (s, 6 H), 2.35 (m, 1 H), 2.05-1.82 (m, 6 H), 1.66 (mn, 2 H),

Example 92

cis-N-(2,4-Difluorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarbozamide

Step A: Synthesis of cis-N-(2,4-difluorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide

Using a similar procedure as described in step D of Example 921, the title compound was obtained.

ESI MS m/e 440 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 7.92 (d. J=8.0 Hz, 1 H), 7.61 (t, J=8.0 Hz, 1 H), 7.28 (m, 3 H), 7.17 (brs, 1 H), 6.82 (brs, 1 H), 6.76 (t, J=8.0 Hz, 1 H), 6.67 (t, J=8.0 Hz, 1 H), 4.41 (d, J=6.0 Hz, 2 H), 4.31 (brs, 1 H), 3.51 (s, 6 H), 2.39 (m, 1 H), 1.96-1.66 (m, 8 H),

Example 923

cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}-N-(2,3-dimethylbenzyl)cyclohexane carboxamide

Step A: Synthesis of cis-4-({[4-(dimethylamino)quinazolin-2-yl] amino}-N-(2,3-dimethylbenzyl)-cyclohexanecarbosamide

Using a similar procedure as described in step D of Example 921 , the title compound ,was obtained.

ESI MS m/e 432 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 7.91 (d, J=8.4 Hz, 1 H), 7.58 (t, J=7.6 Hz, 1 H), 7.27 (t, J=7.6 Hz, 1 H), 7.13 (d, J=7.6 Hz, 1 H), 7.06 (m, 1 H), 6.99 (d, J=4.4 Hz, 2 H), 6.90 (brs, 1 H), 6.45 (brs, 1 H), 4.41 (d, J=6.0 Hz, 2 H), 4.25 (brs, 1 H), 3.50 (s, 6 H), 2.41 (m, 1 H), 2.21 (s, 3 H), 2.14 (s, 3H), 1.96-1.72 (m, 8 H).

Example 924

cis-N-(2-Bromobenzyl)-4-{[4-(dimethylaminoquinazolin-2-yl]amino}cyclohexane-carboxamide

Step A: Synthesis of cis-N-(2-bromobenzyl)-4-{[4-(dimethlamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide

Using a similar procedure as described in step D of Example 921, the title compound was obtained.

ESI MS m/e 482 M+H⁺; ¹H NMR (400 MHz, CDCl₃) S 7.91 (d, J=8,4 Hz, 1 H), 7.62 (t, J=8.0 Hz, 1 H), 7.43 (d, J=7.6 Hz, 1 H), 7.31-7.21 (m, 4 H), 7.05 (t, J=7.2 Hz, 1 H), 6.82 (brs, 1 H), 6.59 (brs, 1 H), 4.48 (d, J=6.0 Hz, 2 H), 4.30 (brs, 1 H), 3.52 (s, 6 H), 2.41 (m, 1 H), 1.97-1.64 (m, 8 H).

Example 925

cis-N-(2,4-Dichlorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide

Step A: Synthesis of cis-N-(2,4-dichlorobenzyl)-4-{[4-(dimethylaminoquinazolin-2-yl]amino}-cyclohexanecarboxamide

Using a similar procedure as described in step D of Example 921, the title compound was obtained.

ESI MS m/e 472 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 7.91 (d, J=S.0 Hz, 1 H), 7.61 (t, J=8.0 Hz, 1 H), 7.28 (t, J=7.6 Hz, 1 H), 7.25-7.19 (m, 3 H), 7.12 (d, J=8.0 Hz, 1 H), 6.98 (brs, 1 H), 6.83 (brs, 1 H), 4.43 (d, J=6.0 Hz, 2 H), 4.31 (brs, 1 H), 3.S2 (s, 6 H), 2.42 (m, 1 H), 1.96-1.67 (m, S H).

Example 926

cis-N-(2.3-Dichlorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide

Step A: -Synthesis of cis-N-(2,3-dichlorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide

Using a similar procedure as described in step D of Eample 921, the title compound was obtained.

ESI MS m/e 472 M+H⁺; ¹NMR (400 MHz, CDCl₃) δ 8.17 (d, J=8.4 Hz, 1 H), 7.75 (t. J=7.6 Hz, 1 H), 7.45-7.37 (m, 3 H), 7.30-7.24 (m, 2 H), 4.4S (s, 2 H), 4.26 (brs, 1 H), 3.54 (s, 6 H), 2.49 (m, 1 H), 1.99-1.77 (m, 8 H).

Example 927

cis-N-(2,5-Dichlorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide

Step A: Synthesis of cis-N-(2,5-dichlorobenzyl)-4-{[4-(dmethylamino)quinizolin-2-ylamino}-cyclohexanecarboxamide

Using a similar procedure as described in step D of Example 921, the title compound was obtained.

ESI MS m/e 472 M+H⁺; ¹H NMR (400 MHz, CDCl₃) 5 7.90 (d, J=8.4 Hz, 1 H), 7.66 (t, J=7.6 Hz, 1 H), 7.58 (brs, 1 H), 7.39 (d, J=8.0 Hz, 1 H), 7.31-7.19 (n, 3 H), 7.10 (d, J=8.4 Hz, 1 H), 7.01 (brs, 1 H), 4.48 (d, J=6.0 Hz, 2 H), 4.30 (brs, 1 H), 3.53 (s, 6 H), 2.42 (m, 1 H), 1.98-1.90 (m, 6 H). 1.63 (m, 2 H).

Example 928

cis-N-(2-Chlorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclolhexanecarboxamide

Step A: Synthesis of cis-N-(2-chlorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide

Using a similar procedure as described in step D of Example 921, the title compound was obtained.

ESI MS m/e 438 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 7.90 (d, J=8.4 Hz, 1 H), 7.60 (t, J=8.0 Hz, 1 4), 7.31-7.09 (m, 6 H), 6.77 (d, J=6.8 Hz, 1 H), 6.66 (brs, 1 H), 4.49 (d, J=6.0 Hz, 2 H), 4.27 (brs, 1 H), 3.51 (s, 6 H), 2.43 (m, 1 H), 1.95-1.68 (m, 8 H).

Example 929

cis-N-(3-Chlorobenzyl)-4-{14-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide

Step A: Synthesis of cis-N-(3-chlorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide

Using a similar procedure as descnbed in step D of Example 921, the title compound was obtained.

ESI MS m/e 438 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 8.13 (d, J=8.0 Hz, 1 H), 7.72 (t, J=7.6 Hz, 1 H), 7.49-7.19 (m, 6 H), 4.35 (s, 2 H), 4.23 (brs, 1 H), 3.51 (s, 6 H), 2.44 (m, 1 H), 2.01-1.74 (m, 8 H).

Example 930

cis-4-{[4-(Dimetlylamino)quinazolin-2-yl]amino}-N-(3-methoxybenzyl)cyclohexanecarboxamide

Step A: Synthesis of cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(3-methoxybenzyl)-cyclohexanecarboxamide

Using a similar procedure as described in step D of Example 921, the title compound was obtained.

ESI MS m/e 434M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 7.90 (d, J=8.4 Hz, 1 H), 7.62 (t, J=8.0 Hz, 1 H), 7.29 (t, J=8.0 Hz, 1 H), 7.22 (m, 1 H), 7.14 (t, J=8.0 Hz, 1 H), 6.85-6.78 (m, 3 H), 6.71 (d, J=8.0 Hz, 1 H), 6.63 (brs, 1 H), 4.38 (d, J=6.0 Hz, 2 H), 4.29 (brs, 1 H), 3.51 (s, 6 H), 2.40 (m, 1 H), 1.95-1.66 (m, 8 H).

Example 931

cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}-N-(4-methylbenzyl)cyclohexanecarboxamide

Step A: Synthesis of cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(4-methylbenzyl)-cyclohexanecarboxamide

Using a similar procedure as described in step D of Example 921, the title compound was obtained.

ESI MS m/e 418 M+H⁻; ¹H NMR (400 MHz, CDCl₃) 6 9.80 (brs, 1 H), 7.90 (d, J=8.4 Hz, 1 H), 7.63 (t, J=8.0Hz, 1 H), 7.29 (t, J=8.0 Hz, 1 H), 7.16 (d, J=8.0 Hz, 2 H), 7.06 (d, J=8.0Hz, 2 H), 6.77 (d, J=7.2 Hz, 1 H), 6.48 (brs, 1 H), 4.37 (d, J=5.6 Hz, 2 H), 4.29 (brs, 1 H), 3.52 (s, 6 H), 2.37 (m, 1 H), 2.27 (s, 3 H), 1.96-1.62 (m, 8 H).

Example 932

cis-N-[3,5-Bis(trifluoromethyl)benzyl]-4-{[4-(dimethylaminoquinazolin-2-yl]amino}cyclohexanecarboxamide

Step A: Synthesis of cis-N-[3,5-bis(trifluoromethyl)benzyl]-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide

Using a similar procedure as described in step D of Example 921, the title compound was obtained.

ESI MS m/e 540 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 8.91 (brs, 1 H), 8.22 (brs, 1 H), 7.SS (d, J=7.6 Hz, 1 H), 7.78 (s, 2 H), 7.68 (s, 1 H), 7.62 (t, J=8.0 Hz, 1 H), 7.40 (d, J=8.0 Hz, 1 H), 7.24 (t, J=7.6Hz, H), 4.55 (d, J=5.6Hz, 2 H), 4:8 (S(m, 1 H), 3.49 (s, 6 H), 2.44 (m, 1 H), 2.19 (m, 2H), 1.95 (m, 4 H), 1.62 (m, 2 H).

Example 933

cis-N-(2,4-Dimethoxybenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide

Step A: Synthesis of cis-N-(2,4-dimethoxybenzyl)-4-{[4-(dimethylaminoquinazolin-2-yl]amino}cyclohexanecarboxamide

Using a similar procedure as described in step D of Example 921, the title compound was obtained.

ESI MS m/e 464 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 8.53 (brs, 1 H), 7.88 (d, J=7.6 Hz, 1 H), 7.60 (t, J=8.0 Hz, 1 H), 7.40 (d, J=7.6 Hz, 1 H), 7.23 (t, J=7.6 Hz, 1 H), 7.16 (d, J=8.4 Hz, 1 H), 6.83 (brs, 1 H), 6.3S (m, 2 H)4.37 (d, J=6.0 Hz, 2 H), 4.2O ((m, 1 H),3.82 (s, 3 H),3.75(s. 3 H),3.48 (s, 6 H), 2.32 (m, 1 H), 2.09-1.2 (m, 6 H), 1.66 (m, 2 H).

Example 934

cis-N-(3,4-Dimethoxybenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide

Step A: Synthesis of cis-N-(3,4-dimethoxybenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]-amino}cyclohexanecarboxamide

Using a similar procedure as described in step D of Example 921, the title compound was obtained.

ESI MS m/e 464 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 8.74 (brs, 1 H, 7.87 (d, J=8.0 Hz, 1 H), 7.61 (t, J=7.6 Hz, 1 H), 7.41 (d, J=8.0 Hz, 2 H), 7.23 (t, J=7.2 Hz, 1 H), 6.91 (m, 2 H), 6.76 (d, J=8.0Hz, 1 H), 4.37 (d, J=6.0 Hz, 2H), 4.36 (m, 1 H), 3.87 (s, 3 H), 3.81 (s, 3 H), 3.48 (s, 6 H), 2.37 (m, 1 H), 2.09 (m, 2 H), 1.83 (m, 4 H), 1.63 (m, 2 H).

Example 935

cis-N-(3,5-Dimethoxybenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide

Step A: Synthesis of cis-N-(3,5-dimethoxybenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]-amino}cyclohexanecarboxanide

Using a similar procedure as described in step D of Example 921, the title compound was obtained.

ESI MS m/e 464 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 8.32 (brs, 1 H), 7.88 (d, J=7.6 Hz, 1 H), 7.59 (t, J=7.6 Hz, 1 H), 7.34 (d, J=8.0 Hz, 1 H), 7.23 (t, J=7.6 Hz, 2 H), 6.46 (d, J=2.0 Hz, 2 H), 6.25 (t, J=2.0 Hz, 1 H), 4.36 (d, J=6.0 Hz, 2 H), 4.34 (bm,1 H), 3.73 (s, 6 H), 3.48 (s, 6 H), 2.39 (m, 1 H), 2.06-1.83 (m, 6 H), 1.65 (m, 2 H).

Example 936

cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino})-N-(4-hydroxy-3-methoxybenzyl)-cyclohexanecarboxamide

Step A: Synthesis of cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(4-hydroxy-3-methoxybenzyl)cyclohexanecarboxamide

Using a similar procedure as described in step D of Example 921, the title compound was obtained.

ESI MS m/e 450 M+H⁺; ¹H NMR (400 MHz, CDCl₃) 8 8.02 (brs, 1 H), 7.88 (d, J=7.6 Hz, 1 H), 7.63 (t, J=8.0 Hz, 1 H), 7.36 (d, J=8.0 Hz, 1 H), 7.26 (t, J=8.0 Hz, 1 H), 7.04 (brs, 1 H), 6.90 (d, J=1.2 Hz, 1 H), 6.79 (m, 2 H), 4.33 (d, J=6.0 Hz, 3 H), 3.87 (s, 3 H), 3.55 (s, 1 H), 3.50 (s, 6 H), 2.37 (m, 1 H), 1.93-1.83 (m, 6 H), 1.65 (m, 2 H).

Example 937

cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}-N-(3,4,5-trimethoxybenzyl)cyclohexanecarboxamide

Step A: Synthesis of cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(3,4,5-trimethoxybenzyl)cyclohexanecarboxamide

Using a similar procedure as described in step D of Example 921, the title compound was obtained.

ESI MS m/e 494 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 7.90 (d, J=8.4 Hz, 1 H), 7.66 (t, J=8.0 Hz, 1 H), 7.30 (m, 2 H), 6.78 (d, J=7.2 Hz, 1 H), 6.56 (s, 3H), 4.34 (d, J=6.0 Hz, 3 H), 3.82 (s, 6 H), 3.78 (s, 3 H), 3.52 (s, 6 H), 2.38 (m, 1 H), 1.97-1.62 (m, 8 H).

Example 938

cis-4-{[4-(Dimetlylamino)quinazolin-2-yl]amino}-N-(2,4,6-trimethoxybenzyl)cyclohexanecarboxamide

Step A; Synthesis of cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(2,4,6-trimethoxybenzyl)cyclohexanecarboxamide

Using a similar procedure as described in step D of Example 921, the title compound was obtained.

ESI MS m/e 494 M+H⁺; ¹H NMR (400 MHz, CDCl₃) 8 8.48 (brs, 1 H), 7.87 (d, J=8.4Hz, 1 H), 7.60 (t, J=8.0 Hz, 1 H), 7.44 (d, J=6.8 Hz, 1 H), 7.22 (t, J=8.0 Hz, 1 H), 6.28 (brs, 1 H), 6.09 (s, 2 H), 4.45 (d, J=5.2 Hz, 2 H), 4.20 (brs, 1 H), 3.83 (s, 6 H), 3.78 (s, 3 H), 3.48 (s, 6 H), 2.26 (m, 1 H), 1.97-1.65 (m, 8 H).

Example 939

cis-N-(1 ,3-Benzodioxol-5-ylmethyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide

Step A: Synthesis of cis-N-(1,3-benzodioxol-5-ylmethyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide

Using a similar procedure as described in step D of Example 921, the title compound was obtained.

ESI MS m/e 448 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 8.52 (brs, 1 H), 7.89 (d, J=7.6 Hz, 1 H), 7.59 (t, J=8.0 Hz, 1 H), 7.39 (brs, 1 H), 7.44 (d, J=8.0 Hz, 1 H), 7.23 (t, J=7.6 Hz, 1 H), 6.79 (s, 1 H), 6.75 (d, J=8.0 Hz, 1 H), 6.66 (d, J=8.0 Hz, 1 H), 5.84 (s, 2 H), 4.35 (m, 1 H), 4.32 (d, J=6.0 Hz, 2 H), 3.48 (s, 6 H), 2.37 (m, 1 H), 2.05 (m, 2 H), 1.87 (m, 4 H), 1.63 (m, 2 H).

Example 940

cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}-N-(2,2-diphenylethyl)cyclohexanecarboxamide

Step A: Syuthesis of cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(2,2-diphenylethyl)-cyclohexanecarboxamide

Using a similar procedure as described in step D of Example 921, the title compound was obtained.

ESI MS m/e 494 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 7.84 (d, J=8.4 Hz, 1 H), 7.56 (t, J=7.6 Hz, 1 H), 7.46 (d, J=8.4 Hz, 1 H), 7.27-7.15 (m, 13 H), 4.38 (brs, 1 H), 4.27 (brs, 1 H), 3.91 (dd, J=8.0, 6.0 Hz, 2 H), 3.39 (s, 6 H), 2.16 (m, 1 H), 1.79 (m, 4 H), 1.60 (m, 4 H).

Example 941

cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}-N-(1,2,3,4-tetrahydronaphthalen-1-yl)cyclohexanecarboxamide

Step A: Synthesis of cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(1,2,3,4-tetrahydronaphthalen-1-yl)cyclohexanecarboxamide

Using a similar procedure as described in step D of Example 921, the title compound was obtained.

ESI MS mi/e 444 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 7.89 (d, J=7.6 Hz, 1 H), 7.63 (t, J=7.6 Hz, 1 H), 7.34-7.03 (m, 6 H), 6.80 (brs, 1 H), 6.09 (d, J=8.4 Hz, 1 H), 5.15 (q, J=6.8 Hz, 1 H), 4.27 (brs, 1 H), 3.52 (s, 6 H), 2.83 (m, 1 H), 2.70 (m, 1 H), 2.36 (m, 1 H), 2.04-1.72 (m, 12 H).

Example 942

cis-N-(2,3-Dihydro-1H-inden-2-yl)-4-({[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide

Step A: Synthesis of cis-N-(2,3-dihydro-1H-inden-2-yl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide

Using a similar procedure as described in step D of Example 921, the title compound was obtained.

ESI MS ni/e 430 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 7.91 (d, J=8.4 Hz, 1 H), 7.63 (t, J=8.0 Hz, 1 H), 7.28 (m, 2 H), 7.15 (m, 2 H). 7.09 (m, 2 H), 6.83 (d, J=6.83 Hz, 1 H), 6.34 (d, J=6.8 Hz, 1 H), 4.63 (m, 1 H), 4.29 (brs, 1 H), 3.51 (s, 6 H), 3.24 (m, 2 H), 2.97 (m, ¹H), 2.33 (m, 1 H), 1.97-1.68 (m, 8 H).

Example 943

cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}-N-[2-(5-methoxy-1H-indol-3-yl)ethyl]cyclohexanecarboxamide

Step A: Synthesis of cis-4-{[4-(dimethylaminoquinazolin-2-yl]amino}-N-[2-(5-methoxy-1H-indol-3-yl)ethyl]cyclohexanecarboxamid

Using a similar procedure as described in step D of Example 921, the title compound was obtained.

ESI MS m/e 487 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 8.32 (brs, 1 H), 7.89 (d, J=8.4 Hz 1 H), 7.53 (t, J=8.0 Hz, 1 H), 7.40 (d, J=8.4 Hz, 1 H), 7.22 (d, J=S.4 Hz, 1 H), 7.10 (t, J=7.6 Hz, 1 H), 7.02 (s, 2 H), 6.81 (dd, J=8.8, 2.0 Hz, 1 H), 5.80 (brs, 1 H), 4.21 (brs, 1 H), 3.84 (s, 3 H), 3.59 (q, J=6.0 Hz, 2 H), 3.34 (s, 6 H), 2.95 (t, J=6.4 Hz, H), 2.19 (m, 1 H), 1.85 (m, 2 H), 1.72-1.63 (m, 6 H).

Example 944

cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}-N-[(1R)-1-(4-nitrophenyl)ethyl]-cyclohexanecarboxamide

Step A: Synthesis of cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[(1R)-1-(4-nitrophenyl)ethyl]cyclohexanecarboxamide

Using a similar procedure as described in step D of Example 921, the title compound was obtained.

ESI MS m/e 463 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 8.13 (d, J=8.8 Hz, 2 H), 7.88 (d, J=7.6 Hz, 2 H), 7.63 (m, 3 H), 7.43 (d, J=7.6 Hz, 1 H), 7.24 (t, J=7.6 Hz, 1 H), 5.13 (m, 1 H), 4.44 (m, 1 H), 3.48 (s, 6 H), 2.35 (m, 1 H), 2.16 (m, 2 H), 1.88 (m, 4 H), 1.76 (m, 1 H), 1.63 (m, 1 H), 1.61 (d, J=7.2 Hz, 3 H).

Example 945

cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}-N-[(1S)-1-(4-nitrophenylethyl)-cyclohexanecarboxamide

Step A: Synthesis of cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[(1S)-1-(4-nitrophenyl)ethyl]cyclohexanecarboxamide

Using a similar procedure as described in step D of Example 921, the title compound was obtained.

ESI MS m/e 463 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 8.13 (d, J=8.8 Hz, 2 H), 7.88 (d, J=7.6 Hz, 2 H), 7.63 (m, H), 7.43 (d, J=7.6 Hz, 1 H), 7.24 (t, J=7.6 Hz, 1 H). 5.13 (m, 1 H), 4.45 (m, J=7.2Hz,3 H).

Example 946

cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}-N-[(1R,2S)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]cyclohexanecarboxamide

Step A: Synthesis of cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[(1R,2S)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]cyclohexanecarboxamide

Using a similar procedure as described in step D of Example 921, the title compound was obtained.

ESI MS m/e 446 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 7.85 (d, J=8.0 Hz, 1 H), 7.59 (t, J=7.6 Hz, 1 H), 7.39 (d, J=8.0 Hz, 1 H), 7.29-7.15 (m, 6 H), 7.12 (brs, 1 H), 5.39 (m, 1 H), 4.69 (brs, 1 H), 4.39 (m, 1 H), 4.23 (brs, 1 H), 3.47 (s, 6 H), 3.12 (m, 2 H), 2.47 (m, 1 H), 2.16-1.88 (m, 6 H), 1.67 (m, 2 H).

Example 947

cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]cyclohexanecarboxamide

Step A: Synthesis of cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-ylcyclohexanecarboxamide

Using a similar procedure as described in step D of Example 921, the title compound was obtained.

ESI MS m/e 446 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 8.73 (brs, 1 H), 7.86 (d, J=8.0 Hz, 1 H), 7.59 (t, J=8.0 Hz: 1 H), 7.38 (d, J=8.4 Hz, 1 H), 7.28-7.15 (m, 5 H), 7.11 (brs, 1 H), 5.38 (m, 1 H), 4.69(m, 1 H),4.39 (m, 1 H), 4.28 (brs, 1 H),3.48(s,6H), 3.12 (m, 2H), 2.47 (m, 1 H), 2.16-1.88 (m, 6 H), 1.67 (m, 2 H).

Example 948

cis-4-(4-Dimethylamino-quinazolin-2-ylamino)-cyclohexanecrboxylic acid (trans 2-phenylcyclopropyl)-amide

Step A: Synthesis of cis-4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexanecarboxylic acid (2-phenylcyclopropyl)-amide

Using a similar procedure as described in step D of Example 921, the title compound was obtained.

ESI MS m/e 430 M+H⁺; ¹HMR (400 MHz, CDCl₃) δ 7.89 (d, J=7.6 Hz, 1 H), 7.64 (t, J=7.6 Hz, 1 H), 7.28 (t, J=8.0 Hz, 2 H), 7.09-7.01 (m, 6 H), 6.65 (brs, 1 H), 4.28 (brs, 1 H), 3.50 (s, 6 H), 2.92 (brs, 1 H), 2.40 (brs, 1 H), 2.13 (m, 1 H), 1.95-1.68 (m, 8 H), 1.31 (m, 1 H), 1.17 (m, 1 H).

Example 949

cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}-N-[(1S)-1-(4-methylphenyl)ethyl]-cyclohexanecarboxamide trifluoroacetate

Step A: Synthesis of cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[(1S)-1-(4-nethylphenyl)ethyl]cyclohexanecarboxantide trifluoroacetate

Using a similar procedure as described in step D of Example 921, the product was purified by prep HPLC to give the title compound.

ESI IMS m/e 432 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 11.72 (brs, 1 H), 8.10 (d, J=8.0 Hz, 1 H), 8.08 (brs, 1 H), 7.90 (brs, 1 H), 7.71 (t, J=8.0 Hz, 1 H), 7.37 (brs, 1 H), 7.30 (t, J=8.0 Hz, 1 H), 7.11 (d, J=8.0 Hz, 2 H), 7.04 (d, J=8.0 Hz, 2 H), 4.81 (m, 1 H), 4.10 (brs, 1 H), 3.36 (s, 6 H), 2.26 (brs, 1 H), 2.19 (s, 3 H), 1.80-1.51 (m, 8 H), 1.24 (d, J=7.2 Hz, 3 H).

Example 950

cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}-N-(1R)-1-(1-naphthyl)ethyl]cyclohexanecarboxamide trifluoroacetate

Step A: Synthesis of cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[(1R)-1-(1-naphthyl) ethyl]cyclohexanecarboxamide trifluoroacetate.

Using a similar procedure as described in step D of Example 921, the product was purified by prep HPLC to give the title compound.

ESI MS m/e 468 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 11.8 (brs, 1 H), 8.30 (d, J=7.6 Hz, 1 H), 8.10 (d, J=8.0 Hz, 1 H), 8.03 (d, J=8.0 Hz, 1 H), 7.94 (brs, 1 H), 7.87 (d, J=8.4 Hz, 1 H), 7.75 (d, J=8.0 Hz, 1 H), 7.70 (t, J=7.6 Hz, 1 H), 7.4.-7.40 (m, 4 H), 7.36 (brs, 1 H), 7.29 (t, J=7.6 Hz, 1 H), 5.64 (m, 1 H), 4.09 (brs, 1 H), 3.40 (s, 6 H), 2.28 (brs, 1 H), 1.84-1.50 (m, 8 H), 1.42 (d, J=7.0 Hz, 3 H).

Example 951

(-cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}-N-[3-(trifluoromethyl)benzyl]cyclohexanecarboxamide

Step A: Synthesis of cis-4-(4-dimethylamino-quinazolin-2-ylanmino)-cyclohexane carbonyl chloride

To a suspension of cis-4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexane carboxylic acid (0.34 g, 1.0 mmol) in CH₂Cl₂ (20 mL) was added 2M-oxalyl chloride (7.4 mL, 1.3 eq.) in CH₂Cl₂ under an inert atmosphere. The reaction was stirred for 18 hr at room temperature. The reaction changed to a clear solution. Removal of the volatile solvent gave the crude cis-4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexane carbonyl chloride (0.35 g, 97%), which was directly used to the next reaction without a further purification (When the acid chloride reacted with EtOH, the formation of 343 M+H⁺ of the ethyl ester) was observed by LC-MS).

Step B: Synthesis of cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[3-(trifluoromethyl)-benzyl]cyclohexanecarboxamide

To a solution of the acid chloride (24 mg, 0.07 mmol), obtained from Step A, in DCM (3 mL) was added the 3-trifluoromethylbenzyl amine (13 mg, 0.07 mmol) and followed DIEA (3 drops). After stirring overnight at room temperature, the reaction was quenched and purified using column chromatography (silica gel, DCM/MeOH=100:0 to 90:10) to give cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[3-(trifluoromethyl)benzyl]cyclohexanecarboxamide (18 mg, 53 %).

ESI MS m/e 472 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 7.84 (d, J=8.4 Hz, 1 H), 7.57-7.3S (m, 7 H), 7.12 (t, J=7.2 Hz, 1 H), 4.50 (d, J=6.0 Hz, 2 H), 4.35 (brs, 1 H), 3.37 (s, 6 H), 2.36 (m, 1 H), 2.06-1.82 (m, 6 H), 1.66 (m, 2 H).

Example 952

cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}-N-(3-methoxyphenyl)cyclohexanecarboxamide

Step A: Synthesis of cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(3-methoxyphenyl)-cyclohexanecarboxamide

Using a similar procedure as described in step B of Example 951, the title compound was obtained.

ESI MS m/e 420 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 7.35 (d, J=7.6 Hz, 1H), 7.56 (m, 2 H), 7.45 (d, J=7.6 Hz, 1 H), 7.37 (brs, 1 H), 7.17 (m, 2 H), 6.59 (d, J=8.0 Hz, 1 H) 4.42 (brs, 1 H), 3.81 (s, 3 H), 3.44 (s, 6 H), 2.45 (m, 1 H), 2.18 (m, 2 H), 1.94 (m, 4 H), 1.67 (m, 2 H).

Example 953

cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}-N-(2-methoxybenzyl)cyclohexanecarboxamide

Step A: Synthesis of cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(2-methoxybenzyl)-cyclohexanecarboxamide

Using a similar procedure as described in step B of Example 951, the title compound was obtained.

ESI MS m/e 434 M+H⁺; ¹HMR (400 MHz, CDCl₃) δ 7.83 (d, J=8.0 Hz, 1 H), 7.56 (t, J=7.2 Hz, 1 H), 7.45 (d, J=8.0 Hz, 1 H), 7.27-7.14 (m, 4 H), 6.88 (t, J=7.6 Hz, 1 H), 6.83 (d, J=8.0 Hz, 1 H), 4.45 (d, J=5.6 Hz, 2 H), 4.31 (brs, 1 H), 3.86 (s, 3 H), 3.40 (s, 6 H), 2.31 (m, 1 H), 2.02-1.82 (m, 6 H), 1.66 (m, 2 H).

Example 954

cis-4-{[4-(Dinetlylamino)quinazolin-2-yl]amino)-N-(3-iodobenzyl)cyclohexanecarboxamide cyclohexanecarboxamide

Using a similar procedure as described in step B of Example 951, the title compound was obtained.

ESI MS m/e 530 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 7.86 (d, J=8.4 Hz, 1 H), 7.66 (s, 1 H), 7.65 (d, J=7.6 Hz, 1 H), 7.54 (m H), 7.44 (d, J=8.0 Hz, 1 H, 7.32 (d, J=8.0 Hz, 1 H), 7.25 (d, J=S.0 Hz, 1 H), 7.19 (t, J=7.6 Hz, 1 H), 7.03 (m, H), 4.40 (d, =6.0 Hz, 3 H), 3.44 (s, 6H), 2.38 (m, 1 H), 2.06 (m, 2 H), 1.89 (m, 4 H), 1.63 (m, 2 H).

Example 955

cis-N-(3,5-Dichlorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide

Step A: Synthesis of cis-N-(3,5-dichlorobenzyl)-4-{[4-(dimethylamino)q uinazolin-2-yl]amino}cyclohexanecarboxamide

Using a similar procedure as described in step B of Example 951, the title compound was obtained.

ESI MS m/e 472 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 7.84 (d, J=8.0 Hz, 1 H), 7.57 (t, J=7.6 Hz, 1 H), 7.44 (d, J=8.0 Hz, 1 H), 7.19 (bm, 4 H), 4.40 (d, J=6.0 Hz, 3 H) 3.42 (s, 6 H), 2.3S (m, 1 H), ) 2.05 (m, 2 H), 1.89 (m, 4 H), 1.65 (m, 2 H).

Example 956

cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}-N-[4-(trifluoromethoxy)benzyl]-cyclohexane carboxamide

Step A: Synthesis of cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[4-(trifluoromethoxy)benzyl]cyclohexanecarboxamide

Using a similar procedure as described in step B of Example 951, the title compound was obtained.

ESI MS m/e 488 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 7.84 (d, J=8.4 Hz, 1 H), 7.58 (t, J=8.0 Hz, 1 H), 7.43 (d, J=8.0 Hz, 1 H), 7.37-7.31 (m, 3 H), 7.19-7.11 (m, 4 H), 4.44 (d, =6.0 Hz, 2 H), 4.48 (brs, 1 H), 3.42 (s, 6 H), 2.36 (m, 1 H), 2.05 (m, 2 H), 1.89 (m, 4 H), 1.64 (m, 2 H).

Example 957

cis-N-(4-Bromobenzyl)-4-{14-(dimethylamino)quinazolin-1-yl]amino}cyclohexanecarboxamide

Step A: Synthesis of cis-N-(4-bronobenl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide

Using a similar procedure as described in step B of Example 951, the title compound was obtained.

ESI MS m/e 488 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 7.87 (d, J=8.4 Hz, 1 H), 7.75 (brs, 1 H), 7.62 (t, J=7.6 Hz, 1 H), 7.44 (brs, 1 H), 7.42 (d, J=8.0 Hz, 2 H), 7.38 (d, J=8.4 Hz, 1 H), 7.24 (m, 1 H),7.17(d, J=8.0 Hz, 2H),4.40(d,J=6.0Hz,3H),3.47(s,6H),2.38 (m, 1 H),2.10(m,2H), 1.87 (m,4 H), 1.61 (m,2 H).

Example 958

cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}-N-(4-methoxybenzyl)cyclohexanecarboxamide

Step A: Synthesis of cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(4-methoxybenzly)-cyclohexanecarboxamide

Using a similar procedure as described in step B of Example 951, the title compound was obtained.

ESI MS m/e 434 M+H⁺; ¹H NMR (4.00 MHz, CDCl₃) δ 7.85 (d, J=8.4 Hz, 1 H), 7.60 (t, J=7.6 Hz, 1 H), 7.45 (d, J=8.4 Hz, 1 H), 7.28 (d, J=8.8 Hz, 2 H), 7.19 (t, J=7.6 Hz, 1 H). 6.82 (d, J=8.4 Hz, 2 H), 4.39 (d, J=6.0 Hz, 2H), 3.45 (s, 6 H) 2.35 (m, 1 H), 2.05 (m, 2 H), 1.87 (m, 4 H) 1.62 (m, 2 H).

Example 959

cis-N-(2,4-Dimethoxyphenyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide

Step A: Synthesis of cis-N-(2,4-dimethoxyphenyl)-4-{[4-(dmethylamino)quinazolin-2-yl]amino}cyclohexaaecarboxamide

Using a similar procedure as described in step B of Example 951, the title compound was obtained.

ESI MS m/e 450 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 8.16 (d, J=8.8 Hz, 1 H), 7.83 (d, J=8.0 Hz, 2 H), 7.55 (m, 1 H), 7.49 (m, 1 H), 7.13 (brs, 1 H), 6.45 (s, 1 H), 6.43 (m, 1 H), 4.27 (brs, 1 H), 3.89 (s, 3 H), 3.77 (s, 3 H), 3.39 (s, 6 H), 2.42 (m, 1 H), 2.04-1.96 (m, 6 H), 1.75 (m, 2 H).

Example 960

cis-N-(3,5-Dichlorophenyl)-4-{[4-(dixethylamino)quinizolin-2-yl]amino}cyclohexanecarboxamide

Step A: Synthesis of cis-N-(3,5-dichlorophenyl)-4-{[4-(dimethylamino)quinazolin-2-yl]-amino}cyclohexanecarboxamide

Using a similar procedure as described in step B of Example 951, the title compound was obtained.

ESI MS m/e 458 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 7.86 (m, 3 H), 7.60 (t, J=7.6 Hz, 1 H), 7.45 (d J=8.4 Hz, 1 H), 7.20 (t, J=7.6 Hz, 1 H), 7.01 (s, 1 H), 4.44 (brs, 1 H), 3.45 (s, 6 H) 2.47 (m, 1 H), 2.18 (m, 2 H), 1.96 (m, 4 H), 1.66 (m, 2 H).

Example 961

cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}-N-(3-iodophenyl)cyclohexanecarboxamide

Step A: Synthesis of cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(3-iodophenyl)-cyclohexanecarboxamide

Using a sinuilar procedure as described in step B of Example 951, the title compound was obtained.

ESI MS m/e 516 M+H⁺; ¹H NMR(400 MHz, CDCl₃) δ 8.15(s, 1 H), 7.83 (d,J=8.0 Hz, 1 H), 7.63 (d, J=7.2 Hz, 1 H), 7.54 (t, J=7.6 Hz, 1 H), 7.44 (d, J=8.0Hz, 1 H), 7.38 (d, J=7.6 Hz, 1 H), 7.11 (t, J=7.6 Hz, 1 H), 7.00 (t, J=7.6 Hz, 1 H), 4.37 (brs, 1 H), 3.36 (s, 6 H), 2.42 (m, 1 H), 2.09-1.66 (m, 8 H).

Example 962

cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}-N-(2-fuoro-4-nitrophenyt)cyclohexanecarboxamide

Step A: Synthesis of cis-4-{[4-(dimethylaminoquinazolin-2-yl[amino}-N-(2-fluoro-4-nitrophenyl)cyclohexanecarboxamide

Using a similar procedure as described in step B of Example 951, the title compound was obtained.

ESI MS m/e 453 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 8.08 (brs, 1H) 7.96 (m, 1 H) 7.83 (d, J=8.0 Hz, 1 H), 7.56 (t J=7.6 Hz, 1 H), 7.44 (d, J=8.0 Hz, 1 H), 7.20 (m, 1 H), 7.14 (t, J=7.6 Hz, 1 H), 4.38 (brs, 1 H), 3.40 (s, 6 H), 2.54 (m, 1 H), 2.17 (m, 2 H), 1.97 (m, 4 H), 1.74 (m, 2 H).

Example 963

cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}-N-(2-methoxydibenzo[b,d]furan-3-yl)cyclohexanecarboxamide trifluoroacetate

Step A: Synthesis of cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(2-methoxydibenzo[b,d]furan-3-yl)cyclohexanecarboxamide trifluoroacetate

Using a similar procedure as described in step B of Example 951, the product was purified by prep HPLC to give the the compound.

ESI MS m/e 510 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 11.8 (brs, 1 H), 9.19 (s, 1 H), 8.38 (s, 1 H), 8.12 (d, J=7.6 Hz, 1 H), 8.01 (d, J=8.0 Hz, 1 H), 8.00 (brs, 1 H), 7.74 (s, 1 H), 7.72 (m, 1 H), 7.57 (d, J=8.0Hz, 1 H), 7.38 (t, J=8.4 Hz, 2 H), 7.29 (m, 2 H), 4.17 (brs, 1 H), 3.92 (s, 3 H), 3.39 (s, 6 H), 2.73 (brs, 1 H), 1.88-1.64 (m, 8 H).

Example 964

(cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl 3,5-dichlorobenzoate

Step A: Synthesis of cis-(4-hydroxymethyl-cyclohexyl)-carbamic acid tert-butyl ester

To a suspension of cis-4-(tert-butoxycarbonylamino)-cyclohexanecarboxlic acid (15.0 g, 61.7 mmol) in CH₂Cl₂ (140 mL) at −65° C. was added trietlhylamine (13 mL, 2.7 eq.) and a solution of ethyl chloroformate (6 mL) in CH₂Cl₂ (20 mL). The reaction was stirred for 60 min. at 0° C., and acidified (pH =˜3) with IN-HCl. The mixture was extracted with CH₂Cl, (2×70 mL), and the combined organic layers wvere washed with sat. aqueous Na₂CO₃ (1×60 mL), water (2×80 mL), and brine (1×80 mL) and dried over MgSO₄ filtered, and concentrated to give cis-(4-hydroxymethyl-cyclohexyl)-carbamic acid tert-butyl ester as a colorless oil. To a solution of the crude oil in THF (150 mL) at −65° C. were added NaBH₄ (2.7 g, 73 mmol) and MeOH (4.8 mL). The reaction was stirred for 3o min. at -40° C., and stirred for an additional 3 hr at 0° C. The reaction was acidified with 1N-HCl, removed a half volume of solvent, and extracted with EtOAc (3×100 mL). The combined organic layer was washed with water (3×80 mL) and brine (1×100 mL), dried with MgSO₄, filtered, and concentrated to give the product (11.5 g, 82 %) as a white solid. ESI MS m/e 230 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 4.69 (brs, 1 H), 3.78 (brs, 1 H), 3.50 (d, J=6.4 Hz, 2 H), 2.19 (brs, 1 H), 1.10-1.55 (m, 7 H), 1.44 (s, 9 H), 1.25 (m, 2 H).

Step B: Synthesis of cis-(4-amino-cyclohexyl)-methanol hydrochloride

To a solution of cis-(4-hydroxymethyl-cyclohexyl)-carbamic acid tert-butyl ester (0.5g, 2.1 mmol) in EtOAc (15 mL) was added 4NI-HCl (10 mL) at room temperature, The reaction was stirred for 1.5 h at room temperature and concentrated to give a crude compound, which was washed with CH₂Cl₂ (the product was not soluble in CH₂Cl₂) to remove organic impurities to give 0.25 g (89 %) of cis-(4-amino-cyclohexyl)-methanol hydrochloride as a white solid.

ESI MS m/e 130 M+H⁺; ¹H NMR (400 MHz, CD₃OD) δ 3.51 (d, J=7.2 Hz, 2 H), 3.31 (brs, 1 H), 1.81-1.57 (m, 9 H).

Step C: Synthesis of cis-[4-(4-dmethylamino-quinazolin-2-ylamino)-cyclohexyl]-methanol

A vial contains 2-chloro-4-N,N-dimethylamino quinazoline (0.31 g, 1.5 mmol), cis-(4-amino-cyclolhexyl)-methaiiol hydrochloride (0.25 g, 1 eq.), DIEA (0.55 mL), and IPA (2 mL). The vial was heated at 155° C. for 1 h using a Smith itmicrowave synthesizer. The vial contents was diluted with DCM, washed with diluted HCl and water, and concentrated. The residue was purified on silica gel column using CH₂Cl₂ and MeOH (100:0 to 80:20) to give cis-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl)-methanol (0.16 g, 28 %) as a pale yellow solid.

ES1 MS m/e 301 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 8.69 (brs, 1 H), 7.86 (d, J=8.8 Hz. 1H), 7.59 (t, J=8.4 Hz, 1 H), 7.51 (d, J=8.4 Hz, 1 H), 7.21 (t, J=8.0 Hz, 1 H). 4.26 (brs, 1 H), 3.57 (s, 2 H), 3.49 (s, 6 H), 1.92 (m, 3 H), 1.65 (m, 6 H).

Step D: Synthesis of (cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl 3,5-dichloroobenzoate

To a solution of cis-[4-(4-dimethylamino-quinazolin-2-yl]amino}-cyclohexyl]-methanol (25 mg, 0.08 mmol) in DCM (3 mL) was added 3,5-dichlorobenzoyl chloride (17 mg, 0.08 mmol) and followed DIEA (3 drops). The reaction was stirred overnight at room temperature under an inert atmosphere. The reaction was diluted with DCM, washed with 1N-HCl and water, and concentrated. The product was purified by coluinn chromatography (DCM/MeOH=100:0 to 90:10) to give (cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl 3,5-dichlorobenzoate (15 mg, 38%).

ESI MS m/e 473 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 7.88 (s, 2 H), 7.80 (d, J=8.4 Hz, 1 H), 7.51 (m, 2 H), 7.46 (t, J=8.0 Hz, 1 H), 7.06 (t, J=7.6 Hz, 1 H), 4.27 (m, 1 H), 4.22 (d, J=7.2 Hz, 2 H), 3.32 (s, 6 H), 1.92 (m, 3 H), 1.72 (m, 4 H), 1.54 (m, 2 H).

Example 965

(cis-4-{[-(Dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl 3-methoxybenzoate

Step A: Synthesis of (cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methtl 3-methozybenzoate

Using a similar procedure as described in step D of Example 964, the title compound was obtained.

ESI MS m/e 435 M+H⁺; ¹HNMR (400 MHz, CDCl₃) δ 7.81 (d, J=8.4 Hz, 1 H), 7.64-7.53 (m, 4 H), 7.30 (t, J=7.6 Hz, 1 H), 7.11 (t, J=7.6 Hz, 1 H), 7.06 (d, J=8.4 Hz, 1 H), 4.26 (brs, 1 H), 4.25 (d, J=6.8 Hz, 2 H), 3.84 (s, 3 H), 3.39 (s, 6 H), 1.97 (m, 3 H), 1.72 (m, 6 H).

Example 966

(cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl 3-bromobenzoate

Step A: Synthesis of (cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl 3-bromobenzoate.

Using a similar procedure as described in step D of Example 964, the title compound was obtained.

ESI MS m/e 483 M+H⁻; ¹H NMR (400 MHz, CDCl₃) δ 8.15 (s, 1 H), 7.96 (d, J=7.2 Hz, 1 H), 7.80 (d, J=8.0 Hz, 1 H), 7.65 (d, J=7.6 Hz, 1 H), 7.50 (s, 2 H), 7.29 (t, J=7.6 Hz, 1 H), 7.04 (m, 1 H), 4.27 (brs, 1 H), 4.23 (d, J=6.8Hz, 2 H), 3.31 (s, 6 H), 1.93 (m, 3 H), 1.72 (m, 4 H, 1.56 (m, 2 H).

Example 967

(cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl 3,4-difuorobenzoate

Step A: Synthesis of (cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl 3,4-difluorobenzoate

Using a similar procedure as described in step D of Example 964, the title compound was obtained.

ESI MS m/e 441 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 7.81 (m, 3 H), 7.48 (m, 2 H), 7.22 (m, 1 H), 7.04 (t, J=7.6 Hz, 1 H), 4.27 (brs, 1 H). 4.21 (d, J=7.2 Hz, 2 H), 3.31 (s, 6 H), 1.92 (m, 3 H), 1.72 (m, 4 H), 1.55 (m, 2 H).

Example 968

3,4-Dimethoxybenzyl cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxylate

Step A: Synthesis of 3,4-dimethoxybenzyl cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxylate

To a solution of the acid chloride (24 mg, 0.07 mmol) in DCM (3 mL) was added 3,4-dimethoxybenzyl alcohol (12 mg, 0.07 mmol) and followed DIEA (3 drops). After stirring overnight at room temperature, the reaction was quenched and purified using column chromatography (silica gel, DCM/MeOH=100:0 to 90:10) to give 3,4-dimethoxybenzyl cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxylate (12 mg, 36%).

ESI MS m/e 465 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 7.79 (d, J=8.0 Hz, 1 H), 7.49 (t, J=7.6 Hz, 1 H), 7.44 (d, J=7.6 Hz, 1 H), 7.04 (t, J=7.2 Hz, 1 H), 6.91 (d, J=8.0 Hz, 1 H), 6.86 (s, 1 H), 6.84 (t, J=8.0 Hz, 1 H), 5.05 (s, 2 H), 4.11 (brs, 1 H), 3.88 (s, 3 H), 3.87 (s, 3 H), 3.30 (s, 6 H), 2.51 (m, 1 H), 1.97 (m, 2 H), 1.78 (m, 6 H).

Example 969

4-(Trifluoromethoxy)benzyl cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxylate

Step A: Synthesis of 4-(trifluoromethoxy)benzyl cis-4-(14-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxylate

Using a similar procedure as described in step A of Example 968 , the title compound was obtained.

ESI MS m/e 489 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 7.84 (d, J=8.0 Hz, 1 H), 7.57 (t, J=7.6 Hz, 1 H), 7.49 (d, J=8.0 Hz, 1 H), 7.39 (d, J=8.4 Hz, 2 H), 7.20 (d, J=8.4 Hz, 2 H), 7.16 (brs, 1 H), 5.12 (s, 2 H), 4.08 (brs, 1 H), 3.42 (s, 6 H), 2.52 (m, 1 H), 2.05 (m, 2 H), 1.79 (m, 6 H).

Example 970

3,5-Dimethoxybenzyl cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxylate

Step A: Synthesis of 3,5-dimethoxybenzyl cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclobexanecarboxylate

Using a similar procedure as described in step A of Example 968, the title compound was obtained.

ESI MS m/e 465 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 7.81 (d, J=8.4 Hz, 1 H), 7.51 (t, J=7.6 Hz, 1 H), 7.43 (d, J=8.0 Hz, 1 H), 7.08 (t, J=7.6Hz, 1 H), 6.47 (d, J=2.4 Hz,2H), 6.38 (t, J=2/4 Hz, 1 H), 5.05 (s, 2 H), 4.11 (brs, 1 H), 3.77 (s, 6 H), 3.36 (s, 6 H), 2.54 (m 1 H), 2.02 (m, 2 H), 1.79 (m, 6 H).

Example 971

3,4,5-Trimethoxybenzyl cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxylate

Step A: Synthesis of 3,4,5-trimethoxybenzyl cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxylate

Usinig a similar procedure as described in step A of Example 968, the title compound was obtained.

ESI MS m/e 495 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 7.79 (d, J=8.0 Hz, 1 H), 7.49 (t, J=7.2 Hz, 1 H). 7.43 (d, J=7.6 Hz, 1 H), 7.04 (t, J=7.6 Hz, 1 H), 6.56 (s, 2 H), 5.05 (s, 2 H), 4.11 (brs, 1 H), 3.85 (s, 6 H), 3.83 (s,3 H), 3.29 (s, 6 H), 2.53 (m, 1 H), 2.00 (m, 2 H), 1.79 (m, 6 H).

Example 972

2,3,4-Trimethoxybenzyl cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxylate

Step A: Synthesis of 2,3,4-trimethoxybenzyl cis-4-{[4-(dimetlylamino)quinazolin-2-yl]amino}cyclohexanecarboxylate

Using a similar procedure as described in step A of Example 968, the title compound was obtained.

ESI MS m/e 495 M+H⁺; ¹H NNR (400 MHz, CDCl₃) δ 7.79 (d, J=8.0 Hz, 1 H), 7.49 (t, J=7.6 Hz, 1 I), 7.44 (d, J=7.6 Hz, 1 H), 7.05 (m, 1 H), 7.02 (d, J=8.4 Hz, 1 H), 6.45 (d, J=8.4 Hz, 1 H), 5.09 (s, 2 H), 4.10 (brs, 1 H), 3.90 (s, 3 H), 3.86 (s, 3 H), 3.85 (s, 3 H), 3.30 (s, 6 H), 2.49 (m 1 H), 2.00 (m, 2 H), 1.77 (m, 6 H).

Example 973

1-(2-Naphthyl)ethyl cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxylate

Step A: Synthesis of 1-(2-naphthy)ethyl cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxylate

Using a similar procedure as described in step A of Example 968, the title compound was obtained.

ESI MS m/e 469 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 7.85 (m, 5 H), 7.45 (m, 5 H), 7.04 (d, J=7.6 Hz, 1 H), 6.05 (q, J=6.4 Hz, 1 H), 4.11 (brs, 1 H), 3.28 (s, 6 H), 2.52 (m, 1 H), 2.01 (m, 2 H), 1.78 (m, 6 H), 1.62 (d, J=6.4 Hz, 3 H).

Example 974

3-[(Cyclopropylcarbonyl)amino]-N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)benzamide

Step A: Synthesis of cis-N-(4-amino-cyclobenzyl)-3-nitrobenzamide trifluoroacetate

To a suspension of cis-(4-amino-cyclohexyl)-carbamic acid tert-butyl ester (1.1 g, 5.2 mmol) in DCM (20 mL) was added 3-nitrobenzoyl chloride (0.96 g, 5.2 mmol) and followed catalytic amount of DIEA (0.1 mL). The reaction was stirred overnight at room temperature, diluted with DCM, washed with 1N-HCl and water, and concentrated. The crude product was preliminary purified by a short pad of silica gel with DCMI/MeOH (100:0 to 90:10). The product was contaminated with impurity having a very close rf value with the product. A solution of this crude compound (1.2 g, 3.2 mmol) in DCM/TFA (16 mL=10/6) was stirred for 2 hr at room temperature. After removal of the volatile solvent, the solid residue was suspended in hexane, filtered, and dried to give 1.0 g (83%) of cis-N-(4-amino-cyclohexyl)-3-nitrobenzamide trifluoroacetate.

ESI MS m/e 264 M+H⁺¹H NMR (400 MHz, DMSO-d₆) δ 8.64 (t, J=2.0 Hz, 1 H), 8.49 (d, J=4.8 Hz, 1 H), S.37 (ddd, J=8.0, 2.0, 0.8 Hz, 1 H), S.27 (d, J=8.0 Hz, 1 H), 7.81 (brs, 2 H), 7.75 (t, J=8.0 Hz, 1 H), 3.90 (m, 1 H), 3.15 (brs, 1 H), 2.51 (m, 1 H), 1.91 (m, 2 H), 1.76-1.64 (m, 6 H).

Step B: Synthesis of cis-N-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-3-nitrobenzanlide

A suspension of 2-chloro-4-N,N-ditnethylamino quinazoline (0.3 g, 1.4 mmol) and cis-N-(4-amino-cyclohexyl)-3-nitrobenzamide trifluoroacetate (0.5 g, 1.35 mmol) in IPA (2.5 mL) and DIEA (0.7 mL) was reacted for 2 hr at 160° C. in a Smith synthesizer. Over 90% conversion was observed by LC-MS. The reaction was quenched and purified by column chromatography (silica gel, DCM/MeOH=100:0 to 85:15) to give 0.45 g (80% of cis-N-[4-(4-dimethylamio-quinazolin-2-ylamino)-cyclohexyl]-3-nitrobenzamide.

ESI MS m/e 435 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 9.04 (d, J=7.6 Hz, 1 H). 8.73 (t, J=2 Hz, 1 H) 8.28 (d, J=8.4 Hz, 1 H) 8.18 (d, J=8.0 Hz, 1 H), 7.88 (d, J=7.2 Hz, 1 H), 7.62 (m, 2 H), 7.49 (d, J=7.6 Hz, 1 H), 7.25 (m, 1 H), 7.16 (d, J=8.4 Hz, 1 H), 4.38 (m, 1 H), 4.18 (m, 1 H), 3.51 (s, 6 H), 1.99-1.93 (m, 6 H), 1.78 (m, 2 H).

Step C: Synthesis of 3-amino-cis-N-[4-(4-dimethylamine-quinazolin-2-ylamino)-cyclohexyl]-benzamide

A heterogenous solution of cis-N-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-3-nitrobenzamide (0.85 g, 1.9 mmol) and 10% Pd/C (100 mg) in EtOH (20 mL) was stirred overnight under H. at room temperature. LC-MS confirmed 100% conversion of the stating material. The reaction was filtered throughi a pad of celite. After removal of the volatile solvent, the residue was purified from a short pad of silica gel (DCM/MeOH=100:0 to 80:20) to give 0.48 g (62%) of 3-amino-cis-N-[4-(4-diethylamino-quinazolin-2-ylamino)-cyclohexyl]-benzamide as the desired product.

ESI MS m/e 405 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 9.42 (brs, 1 H), 7.89 (d, J=8.0 Hz, 1 H), 7.62 (m, 2 H), 7.26-7.1 7 (m, 4 H), 6.79 (m, 1 H), 6.72 (d, J=8.4 Hz, 1 H), 4.36 (brs, 1 H), 4.18 (m, 1 H), 3.51 (s, 6 H), 1.94-1.78 (m, 8 H).

Step D: Synthesis of 3-[(cyclopropylcarbonyl)amino]-N-(cis-4-{[4-(dimethylamino)-quinazolin-2-yl]amino}cyclohexyl)benzamide

To a solution of 3-amino-cis-N-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-benzamide (25 mg, 0.06mmol) in DCM (3 mL) was added cyclopropanecarbonyl chloride (6 mg, 0.06 mmol) and followed DIEA (catalytic, 3 drops). After stirring overnight at room temperature, the reaction was quenched and purified from prep-HPLC [15 to 95% of CH₃CN (5%TFA)/H₂O (5% TFA)] to give 12 mg (33%) of 3-[(cyclopropylcarbonyl)amino]-N-(cis4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)benzaniide.

ESI MS m/e 473 M+H⁺; ¹H NMR (400 MHz, DMSD-d₆) δ 12.1 (brs, 1 H), 10.2 (s, 1 H), 8.2 (d, J=8.0 Hz, 2 H), 7.94 (brs, 1 H), 7.93 (s, 1 H), 7.74-7.67 (m, 2 H), 7.42 (d, J=7.8 Hz, 2 H), 7.31 (m, 2 H), 4.01 (brs, 1 H), 3.83 (brs, 1 H), 3.42 (s, 6 H), 1.83-1.68 (m, 8 H), 1.00 (m, 2 H), 0.93 (m, 2 H).

Example 975

N-[cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-3-[(2,2-dimethylpropanoyl)amino]bezamide

Step A: Synthesis of {cis-4-[(3-nitro-benzoylamino)-methyl]-cyclohexyl}-carbamic acid tert-butyl ester

cis-(4-Aminomethyl-cyclohexyl)-carbamic acid tert-butyl ester (1.55 g, 6.8 mmol) and 3-nitrobenzoyl chloride (1.25 g, 6.8 mmol, 1 eq.) was reacted using the procedure of step A of Example 974 to give 1.5 g (75%) of {cis-4-[(3-nitro-benzoylamino)-methyl)-cyclohexyl}-carbamic acid tert-butyl ester.

ESI MS m/e 378 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 8.54 (t, J=2.0 Hz, 1 H), 8.33 (d, J=8.0 Hz, 1 H), 8.14 (d, J=8.0 Hz, 1 H), 7.63 (t, J=7.6 Hz, 1 H), 6.31 (brs, 1 H), 4.62 (brs, 1 H), 3.73 (brs, 1 H), 3.41 (t, J=6.4 Hz, 2 H), 1.72-1.57 (m, 7 H), 1.44 (s, 9 H), 1.32 (m, 2 H).

Step B: Synthesis of cis-N-(4-amino-cyclohexylmethyl)-3-nitro-benzamide hydrochloride

{cis-4-[(3-Nitro-benzoylamino)-methyl]-cyclohexyl}-carbamic acid tert-butyl ester (1.4 g, 3.7 mmol) in DCM/TFA (1:1=13 mL) was stirred for 2 hr at room temperature. After removal of the volatile solvent, the residue was dissolved in DCM (10 mL), and 2M-HCl in ether (˜4 mL, 2 eq.) was added. Afer stirring for 20 min at room temperature, removal of the volatile solvent gave 1.2 g (82%) of cis-N-(4-amino-cyclohexylmethyl)-3-nitro-benzamide hydrochloride as the desired product.

ESI MS m/e 278 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 8.91 (t. J=5.6 Hz, 1 H), S.65 (m, 1 H), 8.36 (d, J=2.0 Hz, 1 H). 8.29 (d, J=8.0 Hz, 1 H), 7.97 (brs, 2 H), 7.74 (t, J=8.0 Hz, 1 H), 3.25 (t, J=6.8 Hz, 2 H), 3.13 (brs, 1 H), 1.77 (m, 1 H), 1.65-1.61 (m, 4 H) 1.51 (m, 4 H).

Step C: Synthesis of cis-N-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexylmethyl]-3-nitro-benzamide

A heterogeneous solution of 2-chloro-4-N,N-dimethylamino quinazoline (0.38 g, 1.45 mmol) and cis-N-(4-amino-cyclohexylmethyl)-3-nitro-benzamide hydrochloride (0.45 g, 1 eq.) in IPA (2 mL) and DIEA (0.46 mL, 2 eq.) was irradiated for 1 h 10 min. at 155° C. with a Smith microwave reactor. The reaction was quenched and purified by column chromatography (silica gel. DCM/MeOH=100:0 to 85:15). 0.57 g (87%) of the product was obtained.

ESI MS m/e 449 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 8.91 (brs, 1 H), 8.76 (s, 1 H), 8.45 (d, J=7.6 Hz, 1 H), 8.25 (d: J=8.4 Hz, 1 H), 7.60 (d, J=8.4 Hz, 1 H), 7.60 (m, 2 H), 7.51 (brs, 1 H), 7.42 (d, J=8.4 Hz, 1 H), 7.21 (t, J=8.0 Hz, 1 H), 4.35 (brs, 1 H), 3.51 (brs, 2 H), 3.49 (s, 6 H), 1.94-1.80 (m, 5 H), 1.67-1.62 (m, 4 H).

Step D: Synthesis of N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-3-[(2,2-dimethylprop anoyl)amino]benzamide

A heterogenous solution of cis-N-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexylmethyl]-3-nitro-benzamide (0.57 g, 1.27 mmol) and 10%-Pd/C (100 mg) in EtOH (25 mL) was stirred overnight under H₂. The reaction was filtered through a pad of celite. After removal of the volatile solvent, the residue was purified from a short pad of silica gel (DCM/MeOH=100:0 to 80:20) to give 3-amino-cis-N-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexylmethyl]-benzamide (0.45 g, 83%, ESI MS m/e 419 M+H⁺). 3-Amino-cis-N-[4-(4-diiethylamilo-quinazolin-2-ylamino)-cyclohexylmethyl]-benzamide(30 mg, 0.07 mmol) and 2,2-dimethylpropionyl chloride (9 mmol, 0.07 mmol) was reacted in the presence of catalytic DIEA (4 drops). The product was purified from column chromatogiaplhy (silica gel, DCM/MeOH=100:0 to 90:10) to give N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl) methyl]-3-[(2,2-dimethylpropanoyl)amino]benzamide (12 mg, 33%).

ESI MS m/e 503 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 8.92 (brs, 1 H), 8.86 (s, 1 H), 8.35 (s, 1 H) 8.33 (brs, 1 H), 7.87 (d, J=8.4 Hz, 1 H), 7.61 (m, 2 H), 7.32 (t, J=8.0 Hz, 2 H), 7.22 (t, J=7.2 Hz, 1 H), 6.74 (t, J=4.8 Hz, 1 H), 4.34 (m, 1 H), 3.51 (m, 2 H), 3.48 (s, 6 H), 1.97 (m, 2 H), 1.86-1.78 (m, 3 H), 1.69-1.59 (m, 4. H), 1.44 (s, 9 H).

Example 976

N-[(cis-4-{[4-(Dimetlylamino)quinazolin-2-yl]amino}cyclohexyyl)methyl]-3-propionylamino)benzamide

Step A: Synthesis of N-cis-4-{14-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-3-(propionylamino)benzamide

Using a similar procedure as described in step D of Example 975, the title compound was obtained.

ESI MS m/e 475 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 9.59 (brs, 1 H), 3.53 (brs, 1 H), 8.39 (brs, 1 H), 8.05 (s, 1 H), 7.87 (d, J=8.4 Hz, 1 H), 7.63 (t, J=7.6 Hz, 1 H), 7.58 (d, J=7.6 Hz, 1 H), 7.37 (m, 2 H), 7.23 (m, 1 H), 6.44 (brs, 1 H), 4.33 (m, 1 H), 3.54 (d, J=5.2 Hz, 2 H), 3.48 (s, 6 H), 2.59 (q, J=7.6 Hz, 2 H), 2.05 (m, 2 H), 1.76-1.61 (m, 7 H), 1.31 (t, J=7.6 Hz, 3 H).

Example 977

N-[(cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl)-3-(isobutyrylamino)benzamide

Step A: Synthesis of N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)nethyl]-3-(isobutyrylamino)benzamide

Using a similar procedure as described in step D of Example 975, the title compound was obtained.

ESI MS m/e 489 M+H⁺; ¹H NMR (400 1MHz, CDCl₃) δ 9.59 (brs, 1 H), 8.50 (brs, 1 H), 8.40 (brs, 1 H), 8.17 (s, 1 H), 7.87 (d, J=8.4 Hz, 1 H), 7.62 (t, J 7.6 Hz, 1 H), 7.56 (d, J=7.6 Hz, 1 H), 7.35 (m, 2 H), 7.23 (m, 1 H), 6.54 (brs, 1 H), 4.3) (m, 1 H), 3.51 (d, J=5.6 Hz, 2 H), 3.48 (s, 6 H), 2.88 (m, 1 H), 2.03 (m, 2 H), 1.76-1.62 (m, 7 H), 1.32 (d, J=7.6 Hz, 6 H).

Example 978

N-[(cis-4-{[4-(Dimethylamino)quioazolin-2-yl]amino}cyclohexyl)methyl]-3-[(3-methylbutanoyl)amino]benzamide

Step A: Synthesis of N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyll-3-[(3-methylbutanoyl)amino]benzamide

Using a similar procedure as described in step D of Example 975, the title compound was obtained.

ESI MS m/e 503 M+H⁺; ¹H MNR (400 MHz, CDCl₃) δ 9.71 (brs, 1 H), 8.60 (d, J=7.2 Hz, 1 H), 8.43 (d, J=8.4 Hz, 1 H), 8.15 (s, 1 H), 7.88 (d, J=8.4 Hz, 1 H), 7.62 (t, J=7.6 Hz, 1 H), 7.56 (d, J=7.6 Hz, 1 H), 7.35 (m, 2 H), 7.23 (m, 1 H), 6.57 (brs, 1 H), 4.32 (m, 1 H), 3.49 (s, 8 H), 2.44 (d, J=7.2 Hz, 2 H), 2.33 (m, 1 H), 2.02 (m, 2 H), 1.77-1.62 (m, 7 H), 1.07 (d, J=7.6 Hz, 6 H).

Example 979

3-[(Cyclopropylcarbonyl)amino]-N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]benzamide

Step A: Synthesis of 3-[(cyclopropylcarbonyl)amino]-N-[(cis-4-{[4-(dimethylamino)-quinazolin-2-yl]amino}cyclohexyl)methyl]benzamide

Using a similar procedure as described in step D of Example 975, the title compound was obtained.

ESI MS m/e 487 M+H⁺; ¹H NNR (400 MHz, CDCl₃) δ 10.1 (brs, 1 H), 8.60 (brs, 1 H), 8.34 (d, J=8.4 Hz, 1 H), 8.09 (s, 1 H), 7.86 (d, J=8.4 Hz, 1 H), 7.60 (t, J=7.6 Hz, 1 H), 7.54 (d, J=8.0 Hz, 1 H), 7.41 (d, J=8.4 Hz, 1 H), 7.29 (t, J=8.0 Hz, 1 H), 7.23 (m, 1 H), 6.61 (brs, 1 H), 4.28 (m, 1 H), 3.51 (d, J=6.0 Hz, 2 H), 3.48 (s, 6 H), 2.08 (m, 3 H), 1.78-1.61 (m, 7 H), 1.09 (m, 2 H), 0.87 (m, 2 H).

Example 980

3-[(Cyclobutylcarbonyl)amino]-N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]benzamide

Step A: Synthesis of 3-[(cyclobutylcarbonyl)aminol-N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]benzamide

Using a similar procedure as described in step D of Example 975, the title compound was obtained.

ESI MS m/e 501 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 9.45 (brs, 1 H), 8.68 (brs, 1 H), 8.41 (d, J=7.2 Hz, 1 H), 8.13 (s, 1 H), 7.87 (d, J=8.4 Hz, 1 H), 7.63 (t, J=7.6 Hz, 1 H), 7.56 (d, J=7.6 Hz, 1 H), 7.40 (d, J=7.6 Hz, 1 H), 7.32 (t, J=7.6 Hz, 1 H), 7.23 (m, 1 H), 6.50 (brs, 1 H), 4.32 (m, 1 H), 3.51 (d, J=5.6 Hz, 2 H), 3.49 (s, 6 H), 2.48 (m, 2 H), 2.31 (m, 2 H), 2.06-1.59 (m, 12 H).

Example 981

3-1(Cyclopentylcabonyl)amino]-N-[(cis-4-{[4-(dmethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]benzamide

Step A: Synthesis of 3-[(cyclopentylcarbonyl)amino]-N-[(cis-4-{[4-(dimethylamino)-quinazolin-2-yl]amino}cyclohexyl)methyl]benzamide

Using a similar procedure as described in step D of Example 975, the title compound was obtained.

ESI MS m/e 515 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 9.60 (brs, 1 H), 8.56 (brs, 1 H), 8.40 (d, J=5.6 Hz, 1 H), 8.17 (s, 1 H), 7.87 (d, J=8.4 Hz, 1 H), 7.61 (t, J=7.6 Hz, 1 H), 7.56 (d, J=7.6 Hz, 1 H), 7.37 (d, J=7.6 Hz, 1 H), 7.33 (t, J=7.6 Hz, 1 H), 7.23 (m, 1 H), 6.50 (brs, 1 H), 4.32 (m, 1 H) 3.52 (d, J=5.2 Hz, 2 H), 3.48 (s, 6 H), 3.05 (m, 1 H), 2.06-1.60 (m, 17 H).

Example 982

3-[(Cyclohexylcarbonyl)amino]-N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]benzamide

Step A: Synthesis of 3-[(cyclohexlcarbonyl)amino]-N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)nethyl]benzamide

Using a similar procedure as described in step D of Example 975, the title compound was obtained.

ESI MS m/e 529 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 9.53 (brs, 1 H), 8.61 (brs, 1 H), 8.40 (d, J=6.8Hz, 1 H), 8.20 (s, 1 H), 7.87 (d, J=7.6 Hz, 1 H), 7.60 (t, J=7.6 Hz, 1 H), 7.56 (d, J=7.6 Hz, 1 H), 7.34 (m, 2 H), 7.23 (m, 1 H), 6.49 (brs, 1 H), 4.33 (m, 1 H), 3.53 (d, J=4.0 Hz, 2 H), 3.49 (s, 6 H), 2.59 (m, 1 H), 2.06-1.60 (m, 19 H).

Example 983

cis-4-{[4-(Dimethylamino)quinazolin-2-yl]amino}-N-{3-[(2,2-dimethylpropanoyl)amino]-benzyl}cyclohexanecarboxamide

Step A: Synthesis of cis-[-4-(3-nitrogencyclocarbamoyl)-cyclobenzyl]-carbamic acid tert-butyl ester

cis-4-(tert-Butoxycarbonylamino)-cyclohexanecarboxylic acid (2.0 g, 8/2 mmol) and 3-nitrobenzyl amine hydrochloride (1.54 g, 8.2 mmol, 1 eq) in DCM (30 mL was reacted in the presence of HATU (3.5 g, 9.02 mmol, 1.1 eq.) and Et₃N (˜4 mL). The reaction was diluted with DCM, washed with 1N-HCl and water, dried over MgSO₄, and concentrated. From column chromatography (silica gel, DCM/MeOH =100:0 to 95 to 5), 2.7 g (90%) of cis-[-4-(3-nitrobenzylcarbamoyl)-cyclohexyl]-carbamic acid tert-butyl ester was isolated.

ESI MS m/e 378 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 8.11 (brs, 1 H), 8.09 (s, 1 H), 7.60 (d, J=8.0 Hz, 1 H), 7.48 (t, J=7.6 Hz, 1 H), 6.17 (brs, 1 H), 4.72 (bis, 1 H), 4.53 (d, J=6.0 Hz, 2 H), 3.74 (brs, 1 H), 2.27 (m, 1 H), 1.80-1.71 (m, 6 H), 1.65-1.59 (m, 2 H), 1.45 (s, 9 H).

Step B: Synthesis of cis-4-amino-cyclohexanecarboxylic acid 3-nitro-benzamide hydrochloride

cis-[4-(3-Nitrobenzylcarbamoyl)-cyclohexyl]-carbamic acid tert-butyl ester (2.5 g, 6.6 mmol) was reacted in TFA/DCM. (1:2=23 mL) for 2 hr at room temperature. After removal of the solvents, the residue was dissolved in DCM (15 mL), and added 2M-HCl in ethyl ether (2 eq.). After stirring for 20 min at room temperature, the volatile solvent was removed to give cis-4-amino-cyclohexanecarboxylic acid 3-nitro-benzamide hydrochloride (2.0 g, 95%) as a yellowish white solid.

ESI MS m/e 278 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 8.53 (t, J=6.0 Hz, 1 H), 8.07 (d, J=7.6 Hz, 1 H), 8.06 (s, 1 H), 7.84 (brs, 2 H), 7.68 (d, J=7.6 Hz, 1 H), 7.59 (t, J=7.6 Hz, 1 H), 4.37 (d, J=6.4 Hz, 2 H), 3.13 (m, 1 H), 2.40 (m, 1 H), 1.89 (m, 2 H), 1.68 (m, 4 H), 1.57 (m, 2 H).

Step C: Synthesis of cis-4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexanecarboxylic acid 3-nitro-benzamide

A solution of 2-chloro-4-N,N-dimethylamino quinazoline (0.35 g, 1.7 mmol) and cis-4-amino-cyclohexanecarboxylic acid 3-nitro-benzamide hydrochloride (0.5 g, 1 eq.) in IPA (2.5 mL) and DIEA (0.7 mL) Harrs reacted for 1 h 10 min. at 155° C. in a Smith synthesizer. The reaction was quenicihed and purified by column chromatography (silica gel, DCM/MeOH=100:0 to 85:15). 0.56 g (75%) of cis-4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexanecarboxylic acid 3-nitro-benzamide was isolated.

ESI MS m/e 449 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 9.12 (brs, 1 H), 8.24 (brs, 1 H), 8.15 (s, 1 H), 8.03 (d, J=8.0 Hz, 1 H), 7.88 (d, J=8.0 Hz, 1 H), 7.69 (d, J=8.0 Hz, 1 H), 7.62 (t, J=8.0 Hz, 1 H), 7.44 (m, 2 H), 7.24 (t, J=7.6 Hz, 1 H), 4.54 (d, J=6.4 Hz, 2 H), 4.48 (m, 1H)3.50 (s, 6 H), 2.43 (tt, J=12.4, 4.0 Hz, 1 H), 2.16 (m, 2 H), 1.90 (m, 4 H), 1.63 (m, 2 H).

Step D: Synthesis of cis-4(4-dimethylamino-quinazolin-2-ylamino)-cyclohexanecarboxylic acid 3-aminobenzyl amide

A heterogenous solution of cis-4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexanecarboxylic acid 3-nitro-benzamide (0.55 g, 1.2 mmol) and 10% Pd/C (100 mg) in EtOH (15 mL) was stirred overnight under H₂ atmosphere at room temperatutre. The reaction was filtered through a pad of celite. After removal of the volatile solvent, the residue was purified from a short pad of silica gel (DCM/MeOH=100:0 to 80:20) to give 0.46 g (91%) of cis-4(4-dimethylamino-quinazolin-2-ylamino)-cyclohexane carboxylic acid 3-aminobenzyl amide.

ESI MS m/e 419 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 9.00 (brs, 1 H), 7.86 (d, J=8.4 Hz, 1 H), 7.59 (t, J=8.0 Hz, 1 H), 7.45 (d, J=8.4 Hz, 1 H), 7.37 (brs, 1 H), 7.22 (t, J=7.6 Hz, 1 H), 7.01 (t, J=7.6 Hz, 1 H), 6.73 (s, 1 H), 6.66 (d, J=7.6 Hz, 1 H), 6.49 (d, J=7.6 Hz, 1 H), 4.39 (m, 1 H), 4.35 (d, J=6.0 Hz, 2 H), 3.80 (brs, 2 H), 3.47 (s, 6 H), 2.36 (m, 1 H), 2.05 (m, 4 H), 1.88 (m, 4 H), 1.63 (m, 2 H).

Step E: Synthesis of cis-4-{[4-(dimethylaminio)quinazolin-2-yl]amino}-N-{3-[(2,2-dimethyl-propanoyl)amino]benzyl}cyclohexanecarboxamide

Using a similar procedure as described in step D of Example 975, the title compound was obtained.

ESI MS m/e 503 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 9.05 (brs, 1 H), 8.13 (brs, 1 H), 7.89 (brs, 1 H), 7.87 (d, J=8.0 Hz, 1 H), 7.62 (t, J=7.6 Hz, 1 H), 7.49 (s, 1 H), 7.38 (d J=8.4 Hz, 1 H), 7.22 (t, J=8.0 Hz, 2 H), 7.01 (brs, 1 H), 7.00 (d, J=7.2 Hz, 1 H), 4.43 (d, J=5.6 Hz, 2 H), 4.39 (m, 1 H), 3.48 (s, 6 H), 2.37 (tt, J=120 , 3.6 Hz, 1 H), 2.07 (m, 2 H), 1.97 (m, 4 H), 1.63 (m, 2 H), 1.36(s,9 H).

Example 984

cis-4-{[4-(Dmethylamino)quinazolin-2-yl]amino}-N-[3-(propionylamino)benzyl]cyclobexanecarboxamide

Step A: Synthesis of cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(3-(propionylamino)benzyl]cyclohexanecarboxamide

Using a similar procedure as described in step D of Example 975, the title compound was obtained.

ESI MS m/e 475 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 8.96 (m, 2 H), 8.04 (d, J=8.4 Hz, 1 H), 7.88 (d, J=8.0 Hz, 1 H), 7.64 (t, J=7.6 Hz, 1 H), 7.41 (d, J=8.4 Hz, 1 H), 7.37 (s, 1 H), 7.27-7.18 (m, 2 H), 6.91 (d, J=7.6 Hz, 1 H), 6.70 (brs, 1 H), 4.45 (d, J=5.6 Hz, 2 H), 4.39 (m, 1 H), 3.50 (s, 6 H), 2.53 (q, J=7.6 Hz, 2 H), 2.37 (m, 1 H), 2.04-.94 (m, 6 H), 1.66 (m, 2 H), 1.25 (t, J=7.6 Hz, 3 H).

Example 985

cis-4-{[4-Dimethylamino)quinazolin-2-yl]amino}-N-[3-isobutyrylamino)benzyl]cyclohexanecarboxamide

Step A: Synthesis of cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[3-(isobutyrlamino) benzyl]cyclohexanecarboxamide

Using a similar procedure as described in step D of Example 975, the title compound was obtained.

ESI MS m/e 489 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 8.91 (brs, 2 H), 8.04 (d, J=7.2 Hz, 1 H), 7.88 (d, J=7.6 Hz, 1 H), 7.64 (t, J=7.6 Hz, 1 H), 7.42 (s, 1 H), 7.40 (d, J=8.0 Hz 1 H), 7.27-7.18 (m, 2 H), 6.92 (d, J=8.0 Hz, 1 H), 6.70 (brs, 1 H), 4.44 (d, J=5.6 Hz, 2 H), 4.39 (m, 1 H), 3.49 (s, 6H), 2.80 (m, 1 H), 2.37 (m, 1 H), 2.05-1.94 (m,6 H), 1.66 (m, 1 H), 1.26 (d,J=6.4 Hz,6H).

Example 986

cis-N-{3-[(Cyclopropylcarbonyl)amino]benzyl}-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide

Step A: Synthesis of cis-N-{3-[(cyclopropylcarbonyl)amino]benzyl}-4-{[4-(dimethylamino)-quinazolin-2-yl]amino}cyclohexanecarboxamide

Using a similar procedure as described in step D of Example 975, the title compound was obtained.

ESI MS mn/e 487 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 9.24 (brs, 1 H), 9.00 (brs, 1 H), 7.99 (d, J=8.0 Hz, 1 H), 7.99 (d, J=8.0 Hz, 1 H), 7.62 (t, J=7.6 Hz, 1 H), 7.40 (d, J=8.0 Hz, 1 H), 7.36 (s, 1 H), 7.27-7.15 (m, 2 H), 6.90 (d, J=6.8 Hz, 1 H), 6.81 (brs, 1 H), 4.45 (d, J=5.6 Hz, 2 H), 4.40 (m, 1 H), 3.49 (s, 6 H), 2.37 (m, 1 H), 2.08-1.94 (m, 7 H), 1.66 (m, 2 H), 1.03 (m, 2 H), 0.80 (m, 2 H).

Example 987

cis-N-{3-[(Cyclopentylcarbonyl)amino]benzyl}-1-({[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide

Step A: Synthesis of cis-N-{3-[(cyclopentylcarbonyl)amino]benzyl}-4-{[4-(dimethylamino)-quinazolin-2-yl]amino}cyclohexanecarboxamide

Using a similar procedure as described in step D of Example 975, the title compound was obtained.

ESI MS m/e 515 M+H⁺; ¹H NMR (400 1MHz, CDCl₃) δ 8.88 (brs, 1 H), 8.87 (brs, 1 H), 8.02 (d, J=7.2 Hz, 1 H), 7.88 (d, J=8.4 Hz, 1 H), 7.63 (t, J=7.6 Hz, 1 H), 7.40 (s, 1 H), 7.39 (d, J=8.0 Hz, 1 H), 7.27-7.17 (m, 2 H), 6.92 (d, J=7.6 Hz, 1 H), 6.74 (brs, 1 H), 4.44 (d, J=6.0 Hz, 2 H), 4.40 (m, 1 H), 3.49 (s, 6 H), 2.95 (m, 1 H), 2.37 (m, 1 H), 2.04-1.65 (m, 16 H).

Example 988

cis-N-{3-[(Cyclohexylcarbonyl)amino]benzyl}-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide

Step A: Synthesis of cis-N-{3-[(cyclobexylcarbonyl)amino]benzyl}-4-{[4-(dimethylamino)-quinazolin-2-yl]amino}cyclohexanecarboxamide

Using a similar procedure as descnbed in step D of Example 975, the title compound was obtained.

ESI MS mte 515 M+H⁺; ¹H NMR (400 MHz, CDCl₃) δ 9.06 (brs, 1 H), 8.66 (brs, 1 H), 8.02 (d, J=6.8 Hz, 1 H), 7.88 (d, J=8.0 Hz, 1 H), 7.62 (t, J=7.6 Hz, 1 H), 7.41 (d, J=8.4 Hz, 1 H), 7.40 (s, 1 H), 7.26-7.1 8 (m, 2 H), 6.93 (d, J=8.0 Hz, 1 H), 6.81 (brs, 1 H), 4.45 (d, J=5.6 Hz, 2 H), 4.41 (brs, 1 H), 3.49 (s, 6 H), 2.4S (m, 1 H), 2.37 (m, 1 H), 2.09-1.25 (m, 18 H).

Example 989

3-Chloro-N-(cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexyl)-benzamide

Step A: Synthesis of [cis-4-(4-dimethylamino-6,7-difluoro-quinazolin-2-yamino)-cyclohexyl) carbamic acid tert-butyl ester

A suspended solution of 2-chloro-6,7-difluoro-4-dimethylamino quinazolinie (0.52 g: 2.1 mmol) and cis-(4-amino-cyclohexyl)-carbamic acid tert-butyl ester (0.45 g, 1 eq.) in IPA (2.5 mL) and DIEA (1 mL. ˜2 eq.) was reacted for 2 h 30 min at 155° C. in a Smith microwave synthesizer. The reaction was quenched and purified by column chromatography (DCM:MeOH=100:0 to 90:10) to give 0.28 g (33%) of [cis-4-(4-dimethylamino-6,7-difluoro-quinazolin-2-yamino)-cyclohexyl]carbamic acid tert-butyl ester.

ESI MS m/e 422 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 8.10 (brs, 1 H), 7.40 (brs, 1 H), 6.80 (brs, 1 H), 4.02 (q, J=7.0 Hz, 1 H), 3.82 (brs, 1 H), 3.30 (s, 6 H), 1.65-1.50 (m, 8 H), 1.30 (s, 9 H).

Step B: Synthesis of cis-4-(4-dimethylamino-6,7-difluoro-quinazolin-2-yamino)-4-aminocyclohexane trifluoroacetate

A solution of [cis-4-(4-dimethylamino-6,7-difluoro-quinazolin-2-yamino)-cyclohexyl]carbamic acid tert-butyl ester (0.28 g, 0.66 mmol) in TFA/DCM (1:2=16 mL) was stirred at room temperature for 1.5 hr. After removal of the volatile solvent, the crude product (0.27 g, 95%) was directly used to next reaction without a further purification.

ESI MS m/e 322 M+H⁺.

Step C: Synthesis of 3-chloro-N-(cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclobexyl)benzanide

cis-4-(4-Dimethylamino-6,7-difluoro-quinazolin-2-yamino)-4-amino cyclohexane trifluoroacetate (25 mg, 0.06 mmol) and 3-chlorobenzoyl chloride (10 mg, 0.06 mmol) was stirred overnight at room temperature in the presence of a catalytic amount of DIEA (3 drops). The compounds vere purified from prep-HPLC to give 3-chloro-N-(cis-4-{[4-(drimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexyl)benzamide (9 mg, 27%).

ESI MS m/e 460 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 12.06 (brs, 1 H), 8.29 (brs, 1 H), 8.23 (m, 1 H), 8.04 (brs, 1 H), 7.83 (s, 1 H), 7.74 (d, J=8.0 Hz, 1 H), 7.54 (d, J=8.0 Hz, 1 H), 7.20 (brs, 1 H), 7.44 (t, J=8.0 Hz, 1 H), 3.98 (brs, 1 H), 3.36 (brs, 1 H), 3.36 (s, 6 H), 1.82 (brs, 2 H), 1.68 (brs, 6 H).

Example 990

3,4-Dichloro-N-(cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexyl)-benzamide

Step A: Synthesis of 3,4-dicloro-N-(cis-4-{[4-(dmethylamino)-6,7-difluoroquinazolin-2-yl]-amino}cyclobexyl)benzamide

Using a similar procedure as described in step C of Example 989, the title compound was obtained.

ESI MS m/e 496 M+H⁺; ¹H NMR (400 MHz, DMSO-d₆) δ 12.6 (brs, 1 H), 8.36 (brs, 1 H), 8.28 (brs, 1 H), 8.20 (m, 1 H), 8.03 (d, J=2.0 Hz, 1 H), 7.77 (dd, J=8.0, 2.0 Hz, 1 H), 7.69 (d, J=8.0 Hz, 1 H), 7.45 (brs, 1 H), 3.98 (brs, 1 H), 3.83 (brs, 1 H), 3.41 (s, 6 H), 1.83 (brs, 2 H), 1.68 (brs, 6 H).

Example 991

N-(cis-4-{[4-(Dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexyl)-3,5-dimethoxybenzamide trifluoroacetate

Step A: Synthesis of N-(cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-cyclohexyl)-3,5-dimethoxybenzamide trifluoroacetate

Using a similar procedure as described in step C of Example 989, the title compound was obtained.

ESI MS m/e 486 M+H^{+; 1}H NMR (400 MHz, DMSO-d₆) δ 12.1 (brs, 1 H), 8.20 (m, 1 H), 8.09 (brs, 2H), 7.50 (m, 1 H), 6.92 (d, J=2.0 Hz, 2 H), 6.58 (t, J=2.0 Hz, 1 H), 4.00 (brs, 1 H), 3.80 (brs, 1 H), 3.72 (s, 6 H), 3.37 (s, 6 H), 1.82 (brs, 2 H), 1.67 (brs, 6 H).

Examples 992-1008

Compounds 992 to 1008 were prepared in a similar manner as described in Example 890 using the appropriate benzylamine and the carboxylic acid intermediate from Step E.

Examples 1009-1014

Compounds 1009 to 1014 were prepared in a similar manner as described in Example 893 using the appropriate isocyanate (i.e., Compound 1009 to 1013) or thioisocyanate (i.e., Compound 1014) and the amine intermediate from Step D.

Examples 1015-1029

Compounds 1015 to 1029 were prepared in a similar manner as described in Example 894 using the appropriate isocyanate and the amine intermediate from Step E.

Examples 1030-1043

Compounds 1030 to 1043 were prepared in a similar manner as described in Example 896 using the appropriate phenol and the nicotinamide intermediate from Step A.

Examples 1044-1049

Compounds 1044 to 1049 were prepared in a similar manner as described in Example 902 using the appropriate benzaldehyde and the amine intermediate from Step C.

Examples 1050-1072

Compounds 1050 to 1072 were prepared in a similar manner as described in Example 903 using the appropriate phenol and the nicotinamide intermediate from Step A.

Examples 1073 and 1074

Compounds 1073 and 1074 inwere prepared in a similar manner as described in Example 905 using the appropriate phenol and the nicotinamide intermediate from Step A.

Examples 1075-1034

Compounds 1075 to 1084 were prepared in a similar manner as described in Example 907 using the appropriate phenoxyacetic acid and the amine intermediate from the Example in 895 Step B.

Examples 1085-1091

Compounds 1085 to 1091 were prepared in a similar manner as described in Example 912 using the appropriate aniline and the bromoacetamide.

Examples 1092-1104

Compounds 1092 to 1104 were prepared in a similar manner as described in Example 913 using the appropriate carboxylic acid and the amine intermediate from Step C.

Examples 1105-1115

Compounds 1105 to 1115 were prepared in a simnilar manner as described in Example 914 using the appropriate carboxylic acid and the amine intermediate from the Example in 895 Step B.

Examples 1116-1119

Compounds 1116 to 1119 wvere prepared in a similar manner as described in Example 915 using the appropriate benzylamine and the carboxylic acid intermediate from Step D.

Examples 1120-1130

Compounds 1120 to 1130 were prepared in a similar manner as described in Example 917 using the appropriate acid chloride and the amine intermediate from Step D.

Example 1131

Compound 1131 was prepared in a similar manner as described in Example 1 using 3,5-dichlorobenzaldehyde.

Examples 1132 and 1133

Compounds 1132 and 1133 were prepared in a similar manner as described in Example 919 using the appropriate acid chloride and the amine intermediate from Step A.

Example 1134

Compound 1134 was prepared in a similar manner as described in Example 920 using the appropriate benzaldehyde and the amine intermediate from Example 919 Step A.

Examples 1135-1195

Compounds 1135 to 1195 were prepared in a similar manner as described in Example 921 using the appropriate arylamine and the carboxylic acid intermediate from Step C.

Examples 1196-1199

Compounds 1 196 to 1199 were prepared in a similar manner as described in Example 951 using the appropriate arylamine and the acid chloride intermediate from Step A.

Examples 1200-1204

Compounds 1200 to 1204 were prepared in a similar manner as described in Example 974 using the appropriate acid chloride and aniline intermediate from Step C.

Examples 1205-1211

Compounds 1205 to 1211 were prepared in a similar manner as described in Example 989 using the appropriate acid chloride and amine intermediate from Step B.

Ex. No.	compound name	MS	class
992	cis-N-benzyl-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-	440.5	2
	yl]amino}cyclohexanecarboxamide
993	cis-N-(3,5-dimethoxybenzyl)-4-{[4-(dimethylamino)-6,7-	500.4	2
	difluoroquinazolin-2-yl]amino}cyclohexanecarboxamide
994	cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-N-	470.4	1
	(4-methoxybenzyl)cyclohexanecarboxamide
995	cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-N-	470.3	2
	(3-methoxybenzyl)cyclohexanecarboxamide
996	cis-N-[(6-chloropyridin-3-yl)methyl]-4-{[4-(dimethylamino)-6,7-	475.3	2
	difluoroquinazolin-2-yl]amino}cyclohexanecarboxamide
997	cis-N-(2,4-difluorobenzyl)-4-{[4-(dimethylamino)-6,7-	476.3	3
	difluoroquinazolin-2-yl]amino}cyclohexanecarboxamide
998	cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-N-	508.5	1
	[3-(trifluoromethyl)benzyl]cyclohexanecarboxamide
999	cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-N-	508.4	2
	[4-(trifluoromethyl)benzyl]cyclohexanecarboxamide
1000	cis-N-(2,4-dichlorobenzyl)-4-{[4-(dimethylamino)-6,7-	508	1
	difluoroquinazolin-2-yl]amino}cyclohexanecarboxamide
1001	cis-N-(3,5-dichlorobenzyl)-4-{[4-(dimethylamino)-6,7-	508	1
	difluoroquinazolin-2-yl]amino}cyclohexanecarboxamide
1002	cis-N-(4-bromobenzyl)-4-{[4-(dimethylamino)-6,7-	518.2	1
	difluoroquinazolin-2-yl]amino}cyclohexanecarboxamide
1003	cis-N-(2-bromobenzyl)-4-{[4-(dimethylamino)-6,7-	518.2	1
	difluoroquinazolin-2-yl]amino}cyclohexanecarboxamide
1004	cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-N-	524.6	1
	[4-(trifluoromethoxy)benzyl]cyclohexanecarboxamide
1005	cis-N-[3,5-bis(trifluoromethyl)benzyl]-4-{[4-(dimethylamino)-	576.2	3
	6,7-difluoroquinazolin-2-yl]amino}cyclohexanecarboxamide
1006	cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-N-	566.2	2
	(3-iodobenzyl)cyclohexanecarboxamide
1007	cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-N-	468.4	1
	[(1S)-1-(4-methylphenyl)ethyl]cyclohexanecarboxamide
1008	cis-N-[1-(4-bromophenyl)ethyl]-4-{[4-(dimethylamino)-6,7-	532.2	2
	difluoroquinazolin-2-yl]amino}cyclohexanecarboxamide
1009	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	489.4	1
	N′-[3-(trifluoromethoxy)phenyl]urea
1010	N-(3,4-dimethoxyphenyl)-N′-(cis-4-{[4-	465.2	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea
1011	N-(2-chlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	439.4	2
	yl]amino}cyclohexyl)urea
1012	N-(2,6-dichlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	473.4	3
	2-yl]amino}cyclohexyl)urea
1013	N-(2,3-dichlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-	473.4	3
	2-yl]amino}cyclohexyl)urea
1014	N-(2-bromophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-	499.4	2
	yl]amino}cyclohexyl)thiourea
1015	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	449.4	2
	yl]amino}cyclohexyl)methyl]-N′-(2-methoxyphenyl)urea
1016	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	463.4	2
	yl]amino}cyclohexyl)methyl]-N′-(2-ethoxyphenyl)urea
1017	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	449.4	2
	yl]amino}cyclohexyl)methyl]-N′-(3-methoxyphenyl)urea
1018	N-(3,4-dimethoxyphenyl)-N′-[(cis-4-{[4-	479.4	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
1019	N-(2,4-dimethoxyphenyl)-N′-[(cis-4-{[4-	479.4	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
1020	N-(2,5-dimethoxyphenyl)-N′-[(cis-4-{[4-	479.4	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
1021	N-(2-chlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	453.4	2
	yl]amino}cyclohexyl)methyl]urea
1022	N-(3-chlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	453.4	2
	yl]amino}cyclohexyl)methyl]urea
1023	N-(4-chlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-	453.4	2
	yl]amino}cyclohexyl)methyl]urea
1024	N-(3,5-dichlorophenyl)-N′-[(cis-4-{[4-	487.4	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
1025	N-(2,6-dichlorophenyl)-N′-[(cis-4-{[4-	487.4	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
1026	N-(3,4-dichlorophenyl)-N′-[(cis-4-{[4-	487.4	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
1027	N-(2,5-dichlorophenyl)-N′-[(cis-4-{[4-	487.4	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
1028	N-(2,3-dichlorophenyl)-N′-[(cis-4-{[4-	487.4	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
1029	N-(2,4-dichlorophenyl)-N′-[(cis-4-{[4-	487.4	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea
1030	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	501.30	1
	2-(2-fluorophenoxy)nicotinamide
1031	2-(2-chlorophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-	517.40	1
	yl]amino}cyclohexyl)nicotinamide
1032	2-(2-bromophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-	561.30	1
	yl]amino}cyclohexyl)nicotinamide
1033	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	567.40	1
	2-[2-(trifluoromethoxy)phenoxy]nicotinamide
1034	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	501.50	1
	2-(3-fluorophenoxy)nicotinamide
1035	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	513.40	1
	2-(3-methoxyphenoxy)nicotinamide
1036	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	567.50	1
	2-[3-(trifluoromethoxy)phenoxy]nicotinamide
1037	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	567.40	1
	2-[4-(trifluoromethoxy)phenoxy]nicotinamide
1038	2-(3,4-difluorophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-	519.60	1
	2-yl]amino}cyclohexyl)nicotinamide
1039	2-(3,5-dimethoxyphenoxy)-N-(cis-4-{[4-	543.20	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)nicotinamide
1040	2-(2,3-dimethoxyphenoxy)-N-(cis-4-{[4-	543.20	1
	(dimethylamino)quinazolin-2-yl]-amino}cyclohexyl)nicotinamide
1041	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	573.50	1
	2-(3,4,5-trimethoxyphenoxy)nicotinamide
1042	2-(4-chloro-3-fluorophenoxy)-N-(cis-4-{[4-	535.10	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)nicotinamide
1043	2-(3-chloro-4-fluorophenoxy)-N-(cis-4-{[4-	535.40	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)nicotinamide
1044	N2-{(1S,3R)-3-[(2,4-dimethoxybenzyl)amino]cyclopentyl}-	422	3
	N4,N4-dimethylquinazoline-2,4-diamine
1045	N4,N4-dimethyl-N2-((1S,3R)-3-{[3-(trifluoromethyl)benzyl]-	430
	amino}cyclopentyl)quinazoline-2,4-diamine
1046	N2-((1S,3R)-3-{[2-fluoro-5-(trifluoromethyl)benzyl]amino}-	448
	cyclopentyl)-N4,N4-dimethylquinazoline-2,4-diamine
1047	N4,N4-dimethyl-N2-((1S,3R)-3-{[4-(trifluoromethoxy)benzyl]-	446	3
	amino}cyclopentyl)quinazoline-2,4-diamine
1048	N2-((1S,3R)-3-{[4-bromo-2-(trifluoromethoxy)benzyl]-	524	3
	amino}cyclopentyl)-N4,N4-dimethylquinazoline-2,4-diamine
1049	N2-{(1S,3R)-3-[(3,4-difluorobenzyl)amino]cyclopentyl}-N4,N4-	398	3
	dimethylquinazoline-2,4-diamine
1050	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	501	1
	6-(2-fluorophenoxy)nicotinamide
1051	6-(2-chlorophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-	517	3
	yl]amino}cyclohexyl)nicotinamide
1052	6-(2-bromophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-	561	3
	yl]amino}cyclohexyl)nicotinamide
1053	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	498
	6-(2-methylphenoxy)nicotinamide
1054	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	513	1
	6-(2-methoxyphenoxy)nicotinamide
1055	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	498	1
	6-(3-methylphenoxy)nicotinamide
1056	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	513	1
	6-(3-methoxyphenoxy)nicotinamide
1057	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	551	1
	6-[3-(trifluoromethyl)phenoxy]nicotinamide
1058	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	568
	6-[3-(trifluoromethoxy)phenoxy]nicotinamide
1059	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	501	3
	6-(4-fluorophenoxy)nicotinamide
1060	6-(4-chlorophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-	518	1
	yl]amino}cyclohexyl)nicotinamide
1061	6-(4-bromophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-	561	3
	yl]amino}cyclohexyl)nicotinamide
1062	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	567	3
	6-[4-(trifluoromethoxy)phenoxy]nicotinamide
1063	6-(3,5-difluorophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-	519	3
	2-yl]amino}cyclohexyl)nicotinamide
1064	6-(2,3-difluorophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-	519	1
	2-yl]amino}cyclohexyl)nicotinamide
1065	6-(3,4-difluorophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-	519	1
	2-yl]amino}cyclohexyl)nicotinamide
1066	6-(2,3-dimethoxyphenoxy)-N-(cis-4-{[4-	543	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)nicotinamide
1067	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	574	2
	6-(3,4,5-trimethoxyphenoxy)nicotinamide
1068	6-(4-chloro-2-methoxyphenoxy)-N-(cis-4-{[4-	548	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)nicotinamide
1069	6-(4-chloro-3-fluorophenoxy)-N-(cis-4-{[4-	535	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)nicotinamide
1070	6-(3-chloro-4-fluorophenoxy)-N-(cis-4-{[4-	535	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)nicotinamide
1071	6-(3,5-dimethoxyphenoxy)-N-(cis-4-{[4-	543	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)nicotinamide
1072	6-(3-bromophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-	561	3
	yl]amino}cyclohexyl)nicotinamide
1073	2-(3-chlorophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-	517	2
	yl]amino}cyclohexyl)isonicotinamide
1074	2-(4-chlorophenoxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-	517	1
	yl]amino}cyclohexyl)isonicotinamide
1075	2-(3,4-dichlorophenoxy)-N-(cis-4-{[4-	488.2	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)acetamide
1076	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	448.4	3
	2-(3,4-dimethylphenoxy)acetamide
1077	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	524.2	2
	2-(2,4,5-trichlorophenoxy)acetamide
1078	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	438.2	1
	2-(4-fluorophenoxy)acetamide
1079	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	434.2	1
	2-(3-methylphenoxy)acetamide
1080	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	450.2	1
	2-(4-methoxyphenoxy)acetamide
1081	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	450.2	1
	2-(3-methoxyphenoxy)acetamide
1082	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	450.2	2
	2-(2-methoxyphenoxy)acetamide
1083	2-(2,4-dichlorophenoxy)-N-(cis-4-{[4-	488.2	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)acetamide
1084	4-(benzyloxy)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-	496.5	3
	yl]amino}cyclohexyl)benzamide
1085	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	419.4	1
	N2-phenylglycinamide
1086	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	433.4	1
	N2-(3-methylphenyl)glycinamide
1087	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	437.4	1
	N2-(3-fluorophenyl)glycinamide
1088	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	433.4	1
	N2-methyl-N2-phenylglycinamide
1089	N2-(4-chlorophenyl)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-	453.2	1
	yl]amino}cyclohexyl)glycinamide
1090	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	449.2	1
	N2-(3-methoxyphenyl)glycinamide
1091	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	437.2	1
	N2-(4-fluorophenyl)glycinamide
1092	2-(2,6-difluorophenyl)-N-[(cis-4-{[4-(dimethylamino)quinazolin-	470	3
	2-yl]amino}cyclohexyl)methyl]-2-hydroxyacetamide
1093	2-(2,3-difluorophenyl)-N-[(cis-4-{[4-(dimethylamino)quinazolin-	470	3
	2-yl]amino}cyclohexyl)methyl]-2-hydroxyacetamide
1094	2-(2,5-difluorophenyl)-N-[(cis-4-{[4-(dimethylamino)quinazolin-	470	3
	2-yl]amino}cyclohexyl)methyl]-2-hydroxyacetamide
1095	2-(3,4-difluorophenyl)-N-[(cis-4-{[4-(dimethylamino)quinazolin-	470	3
	2-yl]amino}cyclohexyl)methyl]-2-hydroxyacetamide
1096	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	464	2
	cyclohexyl)-methyl]-2-hydroxy-2-(4-methoxyphenyl)acetamide
1097	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	464
	cyclohexyl)-methyl]-2-hydroxy-2-(3-methoxyphenyl)acetamide
1098	2-(4-bromophenyl)-N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	512	3
	yl]amino}cyclohexyl)methyl]-2-hydroxyacetamide
1099	2-(4-chlorophenyl)-N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	468	3
	yl]amino}cyclohexyl)methyl]-2-hydroxyacetamide
1100	(2S)-2-(3-chlorophenyl)-N-[(cis-4-{[4-(dimethylamino)-	468	2
	quinazolin-2-yl]amino}cyclohexyl)methyl]-2-hydroxyacetamide
1101	(2R)-2-(2-chlorophenyl)-N-[(cis-4-{[4-(dimethylamino)-	468	2
	quinazolin-2-yl]amino}cyclohexyl)methyl]-2-hydroxyacetamide
1102	(2R)-N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	434	3
	yl]amino}cyclohexyl)methyl]-2-hydroxy-2-phenylacetamide
1103	(2S)-N-[(cis-4-{[4-(dimethylamino)quinazolin-2-	434	3
	yl]amino}cyclohexyl)methyl]-2-hydroxy-2-phenylacetamide
1104	N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-	502	2
	cyclohexyl)-methyl]-2-hydroxy-2-[3-(trifluoromethyl)phenyl]-
	acetamide
1105	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	450.00	1
	2-hydroxy-2-(4-methoxyphenyl)acetamide
1106	2-(4-chlorophenyl)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-	454.20	2
	yl]amino}cyclohexyl)-2-hydroxyacetamide
1107	2-(4-bromophenyl)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-	498.40	2
	yl]amino}cyclohexyl)-2-hydroxyacetamide
1108	2-(3,4-difluorophenyl)-N-(cis-4-{[4-(dimethylamino)quinazolin-	456.20	2
	2-yl]amino}cyclohexyl)-2-hydroxyacetamide
1109	2-(2,3-difluorophenyl)-N-(cis-4-{[4-(dimethylamino)quinazolin-	456.20	3
	2-yl]amino}cyclohexyl)-2-hydroxyacetamide
1110	2-(2,6-difluorophenyl)-N-(cis-4-{[4-(dimethylamino)quinazolin-	456.20	3
	2-yl]amino}cyclohexyl)-2-hydroxyacetamide
1111	(2R)-2-(3-chlorophenyl)-N-(cis-4-{[4-(dimethylamino)-	454.20	1
	quinazolin-2-yl]amino}cyclohexyl)-2-hydroxyacetamide
1112	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	488.20	1
	2-hydroxy-2-[3-(trifluoromethyl)phenyl]acetamide
1113	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	450.20	1
	2-hydroxy-2-(3-methoxyphenyl)acetamide
1114	(2S)-2-(2-chlorophenyl)-N-(cis-4-{[4-(dimethylamino)quinazolin-	454.50	1
	2-yl]amino}cyclohexyl)-2-hydroxyacetamide
1115	2-(2,5-difluorophenyl)-N-(cis-4-{[4-(dimethylamino)quinazolin-	456.30	2
	2-yl]amino}cyclohexyl)-2-hydroxyacetamide
1116	cis-4-[(4-isopropylquinazolin-2-yl)amino]-N-(3-	433.3
	methoxybenzyl)cyclohexanecarboxamide
1117	cis-4-[(4-isopropylquinazolin-2-yl)amino]-N-(4-	417.3
	methylbenzyl)cyclohexanecarboxamide
1118	cis-N-(3-fluoro-4-methylbenzyl)-4-[(4-isopropylquinazolin-2-	435.2
	yl)amino]cyclohexanecarboxamide
1119	cis-N-(2,5-dichlorobenzyl)-4-[(4-isopropylquinazolin-2-	471.3
	yl)amino]cyclohexanecarboxamide
1120	N-[((1R,3S)-3-{[4-(dimethylamino)quinazolin-2-	450.4	1
	yl]amino}cyclopentyl)methyl]-3,5-dimethoxybenzamide
1121	4-chloro-N-[((1R,3S)-3-{[4-(dimethylamino)quinazolin-2-	424.2	2
	yl]amino}cyclopentyl)methyl]benzamide
1122	3-chloro-N-[((1R,3S)-3-{[4-(dimethylamino)quinazolin-2-	424.2	1
	yl]amino}cyclopentyl)methyl]benzamide
1123	2,4,6-trichloro-N-[((1R,3S)-3-{[4-(dimethylamino)quinazolin-2-	492	1
	yl]amino}cyclopentyl)methyl]benzamide
1124	N-[((1R,3S)-3-{[4-(dimethylamino)quinazolin-2-yl]amino}-	476.2	3
	cyclopentyl)methyl]-3-fluoro-4-(trifluoromethyl)benzamide
1125	N-[((1R,3S)-3-{[4-(dimethylamino)quinazolin-2-yl]amino}-	476.2	3
	cyclopentyl)methyl]-2-fluoro-4-(trifluoromethyl)benzamide
1126	N-[((1R,3S)-3-{[4-(dimethylamino)quinazolin-2-	526.4	3
	yl]amino}cyclopentyl)methyl]-2,5-bis(trifluoromethyl)benzamide
1127	N-[((1R,3S)-3-{[4-(dimethylamino)quinazolin-2-	458.2	1
	yl]amino}cyclopentyl)methyl]-3-(trifluoromethyl)benzamide
1128	N-[((1R,3S)-3-{[4-(dimethylamino)quinazolin-2-	474.4	3
	yl]amino}cyclopentyl)methyl]-4-(trifluoromethoxy)benzamide
1129	N-[((1R,3S)-3-{[4-(dimethylamino)quinazolin-2-	426.2	2
	yl]amino}cyclopentyl)methyl]-2,5-difluorobenzamide
1130	N-[((1R,3S)-3-{[4-(dimethylamino)quinazolin-2-	426.2	1
	yl]amino}cyclopentyl)methyl]-3,5-difluorobenzamide
1131	N2-((1S,3R)-3-{[(3,5-dichlorobenzyl)amino]methyl}-	444
	cyclopentyl)-N4,N4-dimethylquinazoline-2,4-diamine
1132	N-[(1S,3R)-3-({[4-(dimethylamino)quinazolin-2-	408.2	3
	yl]amino}methyl)cyclopentyl]-3-fluorobenzamide
1133	N-[(1S,3R)-3-({[4-(dimethylamino)quinazolin-2-	426.2	3
	yl]amino}methyl)cyclopentyl]-2,4-difluorobenzamide
1134	N4,N4-dimethyl-N2-[((1R,3S)-3-{[3-(trifluoromethyl)benzyl]-	444
	amino}cyclopentyl)methyl]quinazoline-2,4-diamine
1135	cis-N-benzyl-4-{[4-(dimethylamino)quinazolin-2-	404.3	1
	yl]amino}cyclohexanecarboxamide
1136	cis-N-[(6-chloropyridin-3-yl)methyl]-4-{[4-	439.3	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide
1137	cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[(1R)-1-(3-	448.3	1
	methoxyphenyl)ethyl]cyclohexanecarboxamide
1138	cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[1-(4-	436.3	1
	fluorophenyl)ethyl]cyclohexanecarboxamide
1139	cis-N-[(1R)-1-(4-chlorophenyl)ethyl)-4-{[4-	452.3	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide
1140	cis-N-[1-(4-bromophenyl)ethyl]-4-{[4-	496.4	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide
1141	cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[(1S)-1-(1-	468.7	1
	naphthyl)ethyl]cyclohexanecarboxamide
1142	cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(3,5-	432.4	1
	dimethylbenzyl)cyclohexanecarboxamide
1143	cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(3-fluoro-4-	436.4	2
	methylbenzyl)cyclohexanecarboxamide
1144	cis-N-(3-chloro-2-methylbenzyl)-4-{[4-	452.2	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide
1145	cis-N-(5-chloro-2-methylbenzyl)-4-{[4-	452.2	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide
1146	cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(5-fluoro-2-	436.4	1
	methylbenzyl)cyclohexanecarboxamide
1147	cis-N-(3-chloro-2,6-difluorobenzyl)-4-{[4-	474.4	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide
1148	cis-N-(biphenyl-3-ylmethyl)-4-{[4-(dimethylamino)quinazolin-2-	480.2	1
	yl]amino}cyclohexanecarboxamide
1149	cis-N-(biphenyl-4-ylmethyl)-4-{[4-(dimethylamino)quinazolin-2-	480.2
	yl]amino}cyclohexanecarboxamide
1150	cis-N-(6-chloro-2-fluoro-3-methylbenzyl)-4-{[4-	470.4	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide
1151	cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(2-	422.2	1
	fluorobenzyl)cyclohexanecarboxamide
1152	cis-N-(2,6-difluorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-	440.4	1
	yl]amino}cyclohexanecarboxamide
1153	cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[4-	472.4	1
	(trifluoromethyl)benzyl]cyclohexanecarboxamide
1154	cis-4-{[4-dimethylamino)quinazolin-2-yl]amino}-N-(1-	454.4	1
	naphthylmethyl)cyclohexanecarboxamide
1155	cis-N-(4-chlorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-	438.2	1
	yl]amino}cyclohexanecarboxamide
1156	cis-N-(3,4-dichlorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-	472.4	1
	yl]amino}cyclohexanecarboxamide
1157	cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(3-	422.2	1
	fluorobenzyl)cyclohexanecarboxamide
1158	cis-N-(2,5-difluorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-	440.4	1
	yl]amino}cyclohexanecarboxamide
1159	cis-N-(2,3-difluorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-	440.4	1
	yl]amino}cyclohexanecarboxamide
1160	cis-N-(3-bromobenzyl)-4-{[4-(dimethylamino)quinazolin-2-	482.4	1
	yl]amino}cyclohexanecarboxamide
1161	cis-N-(3-bromo-4-fluorobenzyl)-4-{[4-	501.2	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide
1162	cis-N-(4-bromo-2-fluorobenzyl)-4-{[4-	501.2	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide
1163	cis-N-(5-bromo-2-fluorobenzyl)-4-{[4-	501.2	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide
1164	cis-N-(4-chloro-2-fluorobenzyl)-4-{[4-	456.4	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide
1165	cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(3-	418.2	1
	methylbenzyl)cyclohexanecarboxamide
1166	cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(2-	418.2	1
	methylbenzyl)cyclohexanecarboxamide
1167	cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[2-	488.4	1
	(trifluoromethoxy)benzyl]cyclohexanecarboxamide
1168	cis-N-(2,5-difluorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-	440.4	1
	yl]amino}cyclohexanecarboxamide
1169	cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(2,3,4-	458.2	1
	trifluorobenzyl)cyclohexanecarboxamide
1170	cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(2,4,5-	458.2	1
	trifluorobenzyl)cyclohexanecarboxamide
1171	cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(3,4,5-	458.2	1
	trifluorobenzyl)cyclohexanecarboxamide
1172	cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(2,3,6-	458.2	1
	trifluorobenzy)cyclohexanecarboxamide
1173	cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[3-fluoro-5-	490.4	1
	(trifluoromethyl)benzyl]cyclohexanecarboxamide
1174	cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[4-fluoro-2-	490.4	1
	(trifluoromethyl)benzyl]cyclohexanecarboxamide
1175	cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[2-fluoro-4-	490.4	1
	(trifluoromethyl)benzyl]cyclohexanecarboxamide
1176	cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[4-fluoro-3-	490.4	1
	(trifluoromethyl)benzyl]cyclohexanecarboxamide
1177	cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[2-fluoro-3-	490.4	1
	(trifluoromethyl)benzyl]cyclohexanecarboxamide
1178	cis-N-[4-chloro-3-(trifluoromethyl)benzyl]-4-{[4-	506.2	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide
1179	cis-N-(2-chloro-6-fluorobenzyl)-4-{[4-	456.2	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide
1180	cis-N-(4-chloro-2-fluorobenzyl)-4-{[4-	456.2	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide
1181	cis-N-(3-chloro-4-fluorobenzyl)-4-{[4-	456.2	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide
1182	cis-N-(2-chloro-4-fluorobenzyl)-4-{[4-	456.2	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide
1183	cis-N-[2-chloro-5-(trifluoromethyl)benzyl]-4-{[4-	506.2	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide
1184	cis-N-[2-(difluoromethoxy)benzyl]-4-{[4-	470.4	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide
1185	cis-N-[3-(difluoromethoxy)benzyl]-4-{[4-	470.4	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide
1186	cis-4-{[4-(dimethylamino)quinazolin-2-yl)amino}-N-[3-	488.4	1
	(trifluoromethoxy)benzyl]cyclohexanecarboxamide
1187	cis-N-(2,4-dichloro-6-methylbenzyl)-4-{[4-	486.2	2
	(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide
1188	cis-N-(2,6-dimethoxybenzyl)-4-{[4-(dimethylamino)quinazolin-2-	464.2	1
	yl]amino}cyclohexanecarboxamide
1189	cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[(1R)-1-	418.4	1
	phenylethyl]cyclohexanecarboxamide
1190	cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[(1S)-1-(4-	448.4	1
	methoxyphenyl)ethyl]cyclohexanecarboxamide
1191	cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[(1R)-1-(3-	448.4	1
	methoxyphenyl)ethyl]cyclohexanecarboxamide
1192	cis-N-[bis(4-methoxyphenyl)methyl]-4-{[4-	540.4	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide
1193	cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[2-	472.4	1
	(trifluoromethyl)benzyl]cyclohexanecarboxamide
1194	cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-9H-fluoren-	478.2	1
	9-ylcyclohexanecarboxamide
1195	cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[4-	482.2	1
	(methylsulfonyl)benzyl]cyclohexanecarboxamide
1196	cis-N-(6-chloropyridin-3-yl)-4-{[4-(dimethylamino)quinazolin-2-	425.1	1
	yl]amino}cyclohexanecarboxamide
1197	cis-N-(2-chloropyridin-3-yl)-4-{[4-(dimethylamino)quinazolin-2-	425.1	3
	yl]amino}cyclohexanecarboxamide
1198	cis-N-1H-benzimidazol-2-yl-4-{[4-(dimethylamino)quinazolin-2-	430.3	3
	yl]amino}cyclohexanecarboxamide
1199	cis-N-(5-bromo-4-tert-butyl-1,3-thiazol-2-yl)-4-{[4	531.1	3
	(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide
1200	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	461.4	1
	3-(propionylamino)benzamide
1201	N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	489.4	2
	3-[(3-methylbutanoyl)amino]benzamide
1202	N-(cis-4-{(4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-	489.5	2
	3-[(2,2-dimethylpropanoyl)amino]benzamide
1203	3-[(cyclopentylcarbonyl)amino]-N-(cis-4-{[4-	501.4	1
	(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)benzamide
1204	3-(acetylamino)-N-(cis-4-{[4-(dimethylamino)quinazolin-2-	447.4	1
	yl]amino}cyclohexyl)benzamide
1205	N-(cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-	426	1
	yl]amino}cyclohexyl)benzamide
1206	N-(cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-	440	1
	yl]amino}cyclohexyl)-4-methylbenzamide
1207	N-(cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-	444	1
	yl]amino}cyclohexyl)-4-fluorobenzamide
1208	N-(cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-	456	1
	yl]amino}cyclohexyl)-3-methoxybenzamide
1209	N-(cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-	462	1
	yl]amino}cyclohexyl)-3,4-difluorobenzamide
1210	N-(cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-	494	1
	yl]amino}cyclohexyl)-3-(trifluoromethyl)benzamide
1211	N-(cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-	510	3
	yl]amino}cyclohexyl)-4-(trifluoromethoxy)benzamide

Example 1212

[cis-4-(4-Dimethylaamio-quinazolin-2-ylamino)-cyclohexyl]-carbamic acid isobutyl ester

Step A: Synthesis of [cis-4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-carbamic acid isobutyl ester

To a solution of N²-(cis-4-amino-cyclohexyl)-N¹,N¹-dimethyl-quinazoline-2,4-diamine obtained in step E of example 1 (300 mg) in CHCl₃ (3 mL) were added Et₃N (307 μL) and isobutyl chloroformate (158 mg). The mixture was stirred at ambient temperature for 16 hr. To the reaction was added saturated aqueous NaHCO₃ and the aqueous layer was extracted with CHCl₃ (three times). The combined organic layer was dried over McgSO₄, filtered, concentrated, and purified by flash chromatography (N-silica gel, 25% to 66% EtOAc in hexane) to give [cis-4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-carbamic-acid isobutyl ester (195 mg) as a pale yellow oil.

ESI MS m/e 386, M+H⁺; ¹H NMR (300 MHz, CDCl₃) δ 0.93 (d, J=6.84 Hz, 6 H), 1.51-1.98 (m, 9 H), 3.27 (s, 6 H), 3.69 (brs, 1 H), 3.84 (d, J=6.84 Hz, 2 H), 4.04-4.20 (m, 1 H), 4.69 (brs, 1 H), 4.86-4.98 (m, 1 H), 6.98-7.08 (m, 1 H), 7.40-7.54 (m, 2 H), 7.82 (d, J=-7.93 Hz, 1 H).

Example 1213

1-[cis-4-(4-Dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-3-ethyl-thiourea hydrochloride

Step A: Synthesis of 1-[cis-4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-3-ethyl-thiourea hydrochloride

To a solution of N²-(cis-4-amino-cyclohexyl)-N¹,N¹-dimethyl-quinazoline-2,4-diamine obtained in step E of example 1 (300 ing) in DMSO (3 mL) was added ethyl isothiocyanate (100 mg). The mixture was stirred at ambient temperature for 20 hr. To the reaction mixtuer was added H₂O (20 ml) and the aqueous layer was extracted with CHCl₃ (three times). The combined organic; layer was dried over MgSO₄, filtered, concentrated, and purified by flash chromatography (NH-silica gel, 50% EtOAc in hexane) to give a colorless amorphous. To a solution of the above material in EtOAc (2 mL) was added 4 M hydrogen chloride in EtOAc (10 mL). The mixture was stirred at ambient temperature for 1 hr and concentrated. A suspension of the residue in Et₂O (20 mL) was stirred at ambient temperature for 1 hr. The precipitate was collected by filtration, washed with Et₂O, and dried at 80° C. under reduced pressure to give 1-[cis-4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-3-ethyl-thiourea hydrochloride (296 mg) as a white solid. ESI MS m/e 373, M (free)+H⁺; ¹H NMR (300 MHz, DMSO-d₆) δ 1.07 (t, J=7.23 Hz, 3 H), 1.54-1.93 (m, 8 H), 3.30-3.63 (m, 8 H), 3.95-4.23 (m, 2 H), 7.28-7.57 (m, 3 H), 7.70-7.86 (m, 1 H), 8.03-8.26 (m, 2 H), 12.52 (brs 1 H).

Example 1214

1-[cis-4-(4-Dimethylmamino-quinazolin-2-ylamino)-cyclohexyl]-3-(1,1-dimethyl-propyl)-thiourea hydrochloride

Step A: Synthesis of 1-[cis-4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-3-(1,1-dimethyl-propyl)-thiourea hydrochloride

Using the procedure for the step A of example 1213, the title compound was obtained.

ES MS m/e 415, M (free)+H⁺; ¹H NMR (300 MHz, DMSO-d₆) δ 0.77 (t, J=7.5 Hz, 3 H), 1.16(s, 3 H), 1.36 (s, 3 H), 1.41-1.99 (m, 10 H), 3.4S (s, 6 H), 3.90-4.3 (m, 2 H), 7.13-7.54 (m, 3 H), 7.78 (t, J=7.5 Hz, 1 H), 8.17 (d, J=9.0 Hz, 1 H), 8.28 (brs, 1 H), 12.87 (brs, 1 H).

Assay Procedures

Example 1215

Assay for Determination of Constitutive Activity of Non-Endogenous GPCPs

A. Intracellular IP₃ Accumulation Assay

On day 1, cells to be tranfected can be plated onto 24 well plates. usually 1×10⁵ cells/well (although his umber can be optimized. On day 2 cells can be transfected by firstly mixing 0.25 ug DNA (e.g,, pCMV vector or pCM4V vector comprising polynucleotide enocoding receptor) in 50 ul serum free DMEM/well and 2 ul lipofectainine in 50 ul serum-free DEl,fED,l/well. The solutions are gently mined and incubated for 15-30 min at room temperature. Cells are washed with 0.5 ml PBS and 400 μl of serum free media is mixed with the transfection media and added to thie cells. The cells are then incubated for 3-4 hrs at 37° C./5%CO₂ and then the transfection media is removed and replaced with 1 ml/well of regular growth media. On day 3 the cells are labeled with ³H-myo-inositol. Briefly, the media is removed and the cells are washed with 0.5 ml PBS. Then 0.5 ml inositol-free/serum free media (GIBCO BRL) is added/well with 0.25 μCi of ³H-myo-inositol/well and the cells are incubated for 16-18 hrs o/n at 37° C./5%CO₂ On Day 4 the cells are washed with 0.5 ml PBS and 0.45 ml of assay medium is added containing inositol-free/serum free media 10μM pargyline 10 mM lithium chloride or 0.4 ml of assay medium and 50 ul of 10× ketanserin (ket) to final concentration of 10 μM. The cells are then incubated for 30 min at 37° C. The cells are then washed with 0.5 ml PBS and 200 ul of fresh/ice cold stop solution (1M KOH; 18 mM Na-borate; 3.8 mM EDTA) is added/well. The solution is kept on ice for 5-10 min or until cells were lysed and then neutralized by 200 μl of fresh/ice cold neutralization sol. (7.5% HCL). The lysate is then transferred into 1.5 ml eppendorf tubes and 1 ml of chloroform/methanol (1:2) is added/tube. The solution is vortexed for 15 sec and the upper phase is applied to a Biorad AG1-X8™ anion exchange resin (100-200 mesh). Firstly, the resin is washed with water at 1:1.25 W/V and 0.9 ml of upper phase is loaded onto the column. The column is washed with 10 mls of 5 mM myo-inositol and 10 ml of 5 mM Na-borate/60 mM Na-formate. The inositol tris phosphates are eluted into scintillation vials containing 10 ml of scintillation cocktail with 2 ml of 0.1 M formic acid/1 M ammonium formate. The columns are regenerated by washing with 10 ml of 0.1 M formic acid/3M ammonium formate and rinsed twice with H₂O and stored at 40° C. in water.

Example 1216

High Throughput Functional Screening: FLIPR™

Subsequently, a functional based assay was used to confirm the lead hits, referred to as FLIPR™ (the Fluorometric Imaging Plate Reader) and FDSS6000™ (Functional Drug Screening System). This assay utilized 3 non-endozenous, constitutively active version of the MCH receptor.

The FLIPR and FDSS assays are able to detect intracellular Ca²⁺ concentration in cells, which can be utilized to assess receptor activation and determine whether a candidate compound is an, for example, antagonist, inverse agonist or agonist to a Gq-coupled receptor. The concentration of free Ca²⁺ in the cytosol of any cell is extremely low, whereas its concentration in the extracellular fluid and endoplasmic reticulum (ER) is very high. Thus, there is a large gradient tending to drive Ca²⁺ into the cytosol across both the plasma membrane and ER. The FLIPR™ and FDSS6000™ systems (Molecular Devices Corporation, HAMAMATSU Photonics K.K.) are designed to perform functional cell-based assays, such as the measurement of intracellular calcium for high-throughput screening, The measurement of fluorescent is associated with calcium release upon activation of the Gq-coupled receptors. Gi or Go coupled receptors are not as easily monitored through the FLIPR™ and FDSS6000™ systems because these G proteins do not couple with calcium siginal pathways.

Fluorometric Imaging Plate Reader system was used to allow for rapid, kinetic measurements of intracellular fluorescence in 96 well microplates (or 384 well microplates). Simultaneous measurements of fluorescence in all wells can be made by FLIPR or FDSS6000™ every second with high sensitivity and precision. These systems are ideal for measuring cell-based functional assays such as monitoring the intracellular calcium fluxes that occur within seconds after activation of the Gq coupled receptor.

Briefly, the cells are seeded into 96 well at 5.5×10⁴ cells/well with complete culture media (Dulbecco's Modified Eagle Medium with 10% fetal bovine serum, 2 mMi L-glutamine, 1 mM sodium pyruvate and 0.5 mg/ml G418, pH 7.4) for the assay next day. On the day of assay, the media is removed and the cells are incubated with 100 μl of loading buffer (4 μM Fluo4-AM in complete culture media containing 2.5 mM Probenicid, 0.5 mg/ml and 0.2% bovine serum albumin) in 5% CO₂ incubator at 37° C. for 1 hr. The loading buffer is removed, and the cells are washed with wash buffer (Hank's Balanced Salt Solution containing 2.5 mM Probenicid, 20 mM HEPES, 0.5 mg/ml and 0.2% bovine serum albumm, pH 7.4)). One hundred fifty μl of wash buffer containing various concentrations of test compound is added to the cells, and the cells are incubated in 5% CO₂ incubator at 37° C. for 3 min. Fifty μl of wash buffer containing various concentration of MCH are added to each well, and transient changes in [Ca²⁺]i evokled bee MCH are monoitored using the FLIPR, or FDSS in 96 shell plates at Ex. 488 nm and Em. 530 nm for 290 second. When antagonist activity of compound is tested, 50 nM of MCH is used.

Use of FLIPR™ and FDSS6000™ can be accomplished by following manufacturer's instruction (Molecular Device Corporation and HAMAMATSU Photonics K.K.).

Representative examples are shown below.

Compound No. IC50 (nM)
Example 1    13
Example 2    13
Example 3    4.9
Example 898  3.3
Example 909  0.97

The results shown in the previous tables are in accordance with the classification as defined below.

• • Class 1: The value of percent of control at 10⁻⁷ M was less than 40% or the value of IC₅₀ was less than 50 nM.
  • Class 2: The value of percent of control at 10⁻⁷ M was from 40% to 60% or the value of IC₅₀ was from 50 nM to 200 nM.
  • Class 3: The value of percent of control at 10⁻⁷ M was more than 60% or the value of IC₅₀ was more than 200 nM.

The compounds in Examples 886 to 991 were tested and they showed IC₅₀ activities less than about 50 μM.

Example 1217

Peceptor Binding Assay

In addition to the methods described herein, another means for evaluating a test compound is by determining binding affinities to the MCH receptor. This type of assay generally requires a radiolabelled ligand to the MCH receptor. Absent the use of known ligands for the MCH receptor and radiolabels thereof, compounds of Formula (I) can be labelled with a radioisotope and used in an assay for evaluating the affinity of a test compound to the MCH receptor.

A radiolabelled MCH compound of Formula (I) can be used in a screening assay to identify/evaluate compounds. In general termns, a newly synthesized or identified compound (i.e., test compound) can be evaluated for its ability to reduce binding of the “radiolabelled compound of Formula (I)” to the MCH receptor. Accordingly, the ability to compete with the “radio-labelled compound of Formula (I)” or Radiolabelled MCH Ligand for the binding to the MCH receptor directly correlates to its binding affinity of the test compound to the MCH receptor.

Assay Protocol for Determiing Receptor Binding for MCH

A. MCH Receptor Preparation

293 cells (human kidney, ATCC), transiently transfected with 10 ug human MCH receptor and 60 ul Lipofectamine (per 15-cm dish), are grown in the dish for 24 hours (75% confluency) with a media change and removed with I 0 ml/dishi of Hepes-EDTA buffer ( 20 mM Hepes+10 mM EDTA, pH 7.4). The cells are then centrifuged in a Beckman Coulter centrifuge for 20 minutes, 17,000 rpm (JA-25.50 rotor). Subsequently, the pellet is resuspended in 20 mM Hepes+1 mM EDTA, pH 7.4 and homogenized with a 50-ml Dounce homogenizer and again centrifuged. After removing the supernatant, the pellets can be stored at −80° C., until used in binding assay. When used in the assay, membranes are thawed on ice for 20 minutes and then 10 mL of incubation buffer (20 mM Hepes. 1 mM MgCl₂, 100 mM NaCl, pH 7.4) added. The membranes are then vortexed to resuspend the crude membrane pellet and homogenized with a Brinkmann PT-3100 Polytron homogenizer for 15 seconds at setting 6. The concentration of membrane protein is determined using the BRL Bradford protein assay.

B. Building Assay

For total binding, a total volume of 50 ul of appropriately diluted membranes (diluted in assay buffer containing 50 mM Tris HCl (pH 7.4), 10 mM MgCl₂, and 1 mM EDTA; 5-50 ug protein) is added to 96-well polyproylene microtiter plates followed by addition of 100 ul of assay buffer and 50 ul of Radiolabelled MCH Ligand. For nonspecific binding, 50 ul of assay buffer is added instead of 100 ul and an additional 50 ul of 10 mM cold MCH is added before 50 ul of Radiolabelled MCH Ligand is added. Plates are then incubated at room temperature for 60-]20 minutes. The binding reaction is terminated by filtering assay plates through a Microplate Devices GF/C Unifilter filtration plate with a Brandell 96-well plate harvestor followed by washing with cold 50 mM Tris HCl, pH 7.4 containing 0.9% NaCl. Then, the bottom of the filtration plate are sealed, 50 μl of Optiphase Supermix is added to each well, the top of the plates are sealed, and plates are counted in a Trilux MicroBeta scintillation counter. For compound competition studies, instead of adding 100 μl of assay buffer, 100 μl of appropriately diluted test compound is added to appropriate wells followed by addition of 50 μl of Radiolabelled MCH Ligand.

C. Calculations

The test compounds are initially assayed at 1 and 0.1 μM and then at a range of concentrations chosen such that the middle dose would cause about 50% inhibition of a Radio-MCH Ligand binding (i.e., IC₅₀). Specific binding in the absence of test compound (B_O) is the difference of total binding (B_T) minus non-specific binding (NSB) and similarly specific binding (in the presence of test compound) (B) is the difference of displacement binding (B_D) minus non-specific binding (NSB). IC₅₀ is determined from an inhibition response curve, logit-log plot of % B/B_O vs concentration of test compound.

K_i is calculated by the Cheng and Prustoff transformation:K_i=IC₅₀/(1+[L]/K_D)

wherein [L] is the concentration of a Radio-MCH Ligand used in the assay and K_D is the dissociation constant of a Radio-MCH Ligand determined independently under the same binding conditions.

It is intended that each of the patents, applications, printed publications, and other published documents mentioned or referred to in this specification be herein incorporated by reference in their entirety.

Those skilled in the art wvill appreciate that numerous changes and modifications may be made to the preferred embodiments of the invention and that such changes and modifications may be made without departing from the spirit of the invention. It is therefore intended that the appended claims cover all such equivalent variations as fall within the true spirit and scope of the invention.

Claims

1. A compound of Formula (I):

2. The compound according to claim 1 wherein Q is Formulae (IIa), (IIb), or (IIc); R1 is selected from the group consisting of: (i) C1-8 alkyl, and C1-8 alkyl substituted by substituent(s) independently selected from the group consisting of: halogen, C1-5 alkoxy carbonyl, C1-5 alkoxy, C1-5 alkoxy substituted by carbocyclic aryl, mono-C1-5 alkylamino, di-C1-5 alkylamino, C3-6 cycloalkyl, C3-6 cycloalkenyl, carbocyclyl, carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: hydroxy, halogen, nitro, C1-5 alkylcarbonylamino, C3-6 cycloalkylcarbonylamino, C1-5 alkyl, C1-5 alkyl substituted by halogen, C1-5 alkylsulfonyl, C2-6 alkenyl, C1-5 alkoxy, C1-5 alkoxy substituted by halogen, and carbocyclic aryl, heterocyclyl, and heterocyclyl substituted by halogen, (ii) C2-5 alkenyl, and C2-s alkenyl substituted by carbocyclic aryl, (iii) C2-5 alkynyl, (iv) C3-12 cycloalkyl, and C3-12 cycloalkyl substituted by carbocyclic aryl, (v) carbocyclyl, and carbocyclyl by substituent(s) independently selected from the group consisting of: hydroxy, and carbocyclic aryl, (vi) carbocyclic aryl, and carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: halogen, cyano, nitro, C1-10 alkyl, C1-10 alkyl substituted by substituent(s) independently selected from the group consisting of halogen, oxo, and carbocyclic aryl, carboxy, C1-5 alkoxy carbonyl, C1-7 alkoxy, C1-7 alkoxy substituted by substituent(s) independently selected from the group consisting of: halogen, and carbocyclic aryl, carbocyclic aryloxy, carbocyclic aryloxy substituted by nitro, mono-C1-5 alkylamino, di-C1-5 alkylamino, C1-5 alkoxy carbonylamino, carbocyclic aryl azo, carbocyclic aryl azo substituted by substituent(s) independently selected from the group consisting of: mono-C1-5 alkylamino, and di-C1-5 alkylamino, C1-5 alkylthio, C1-5 alkylthio substituted by halogen, carbocyclic arylthio, carbocyclic arylthio substituted by nitro, amino sulfonyl, heterocyclyl sulfonyl, C3-6 cycloalkyl, C3-6 cycloalkyl substituted by C1-5 alkyl, carbocyclic aryl, heterocyclyl, and heterocyclyl substituted by C1-5 alkyl, (vii) heterocyclyl, and heterocyclyl substituted by substituent(s) independently selected from the group consisting of: halogen, C1-5 alkyl, C1-5 alkyl substituted by halogen, C1-5 alkoxy, C1-5 alkoxy carbonyl, C1-5 alkoxy carbonyl substituted by carbocyclic aryl, carbocyclic aryloxy, carbocyclic aryl, and heterocyclyl; R2 is —N(R2a)(R2b), wherein R2a is hydrogen or C1-5 alkyl; R2b is C1-5 alkyl; R3 is C1-5 alkyl; R4 is —N(R4a)(R4b) wherein R4a is hydrogen or C1-5 alkyl; R4b is C1-5 alkyl; L is selected from Formula (V), (VIII), (IX), (XIII), (XVI), or (XVII); X1, X2, X3 and X4 are independently selected from the group consisting of hydrogen, halogen, and C1-4 alkyl; provided that at least one substituent selected from the group consisting of X1, X2, X3 and X4 is not hydrogen; and Y is selected from the group consisting of: (i) —C(O)NR7—, —C(S)NR7—, or —C(O)O— when L is selected from the group consisting of Formula (V), (VIII), (IX), (XIII), (XVI), or (XVII); wherein R7 is hydrogen or C1-5 alkyl; (ii) —S(O)2—, —C(O)—, a single bond or —CH2— when L is selected from the group consisting of Formula (VIII) or (IX); and (iii) —OC(O)— when L is selected from the group consisting of Formula (XIII), (XVI), or (XVII); wherein carbocyclic aryl is phenyl or naphthyl; carbocyclyl is indanyl, bicyclo[2.2.1]heptyl, bicyclo[2.2.1]heptenyl, adamantyl, 9H-fluorenyl, menthyl, 1,2,3,4-tetrahydro-naphthalen-1-yl, or 1H-indolyl; heterocyclyl is 2,3-dihydro-benzo[1,4]dioxinyl, 3,4-dihydro-2H-benzo[b][1,4]dioxepinyl, 4,5,6,7-tetrahydro-benzo[b]thienyl, 4H-benzo[1,3]dioxinyl, benzo[1,3]dioxolyl, benzo[2,1,3]thiadiazolyl, benzothiazolyl, furyl, isoxazolyl, morpholinyl, oxazolyl, piperidyl, pyrazolyl, pyridyl, tetrahydrofuryl, thienyl, dibenzofuranyl, 1H-benzoimidazolyl, or thiazolyl; and halogen is fluoro, chloro, bromo, or iodo; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

3. The compound according to claim 2 wherein Q is Formula (IIc); or a pharmaceutically acceptable salt, hydrate or solvate thereof.

4. The compound according to claim 3 wherein R1 is selected from the group consisting of: C1-5 alkyl, and C1-5 alkyl substituted by substituent(s) independently selected from the group consisting of: C1-5 alkoxy carbonyl, carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: halogen, C1-5 alkyl, C2-5 alkenyl, and C1-5 alkoxy, C1-5 alkylthio, and heterocyclyl, (ii) C3-6 cycloalkyl, and C3-6 cycloalkyl substituted by carbocyclic aryl, (iii) carbocyclyl, (iv) carbocyclic aryl, and carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: halogen, cyano, nitro, C1-5 alkyl, C1-5 alkyl substituted by substituent(s) independently selected from the group consisting of: halogen, oxo, and carbocyclic aryl, C1-5 alkoxy carbonyl, C1-7 alkoxy, C1-7 alkoxy substituted by substituent(s) independently selected from the group consisting of: halogen, and carbocyclic aryl, cycloalkoxy, carbocyclic aryloxy, mono-C1-5 alkylamino, di-C1-5 alkylamino, C1-5 alkylthio, C1-5 alkylthio substituted by halogen, carbocyclic aryl, heterocyclyl, and heterocyclyl substituted by C1-5 alkyl, (v) heterocyclyl, and heterocyclyl substituted by substituent(s) independently selected from the group consisting of: halogen, C1-5 alkyl, C1-5 alkyl substituted by halogen, C1-5 alkoxy carbonyl C1-5 alkoxy carbonyl substituted by carbocyclic aryl, and carbocyclic aryl; L is Formula (V); and Y is —C(O)NR7—; wherein R7 is hydrogen or C1-5 alkyl; wherein carbocyclic aryl is phenyl or naphthyl; carbocyclyl is indanyl, adamantyl, or 9H-fluorenyl; heterocyclyl is 2,3-dihydro-benzo[1,4]dioxinyl, 3,4-dihydro-2H-benzo[b][1,4]dioxepinyl, 4H-benzo[1,3]dioxinyl, benzo[1,3]dioxolyl, benzothiazolyl, furyl, isoxazolyl, piperidyl, pyridyl, or thienyl; and halogen is fluoro, chloro, bromo, or iodo; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

5. The compound according to claim 4 wherein R4a is hydrogen or methyl; R4b is methyl; R5 and R6 are hydrogen; A is a single bond and B is a single bond or —CH2—; and R7 is hydrogen; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

6. The compound according to claim 5 wherein R1 is selected from the group consisting of: (i) C1-5 alkyl, and C1-5 alkyl substituted by substituent(s) independently selected from the group consisting of: C1-5 alkoxy carbonyl, carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: halogen, C1-5 alkyl, C2-5 alkenyl, and C1-5 alkoxy, C1-5 alkylthio, and heterocyclyl, (ii) C3-6 cycloalkyl, and C3-6 cycloalkyl substituted by carbocyclic aryl, (iii) carbocyclyl, (iv) carbocyclic aryl, and carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: halogen, cyano, nitro, C1-5 alkyl, C1-5 alkyl substituted by halogen, C1-5 alkoxy carbonyl, C1-5 alkoxy, C1-5 alkoxy substituted by halogen, cycloalkoxy, carbocyclic aryloxy, C1-5 alkylthio, and carbocyclic aryl, (v) heterocyclyl, and heterocyclyl substituted by substituent(s) independently selected from the group consisting of: halogen, C1-5 alkyl, C1-5 alkyl substituted by halogen, and carbocyclic aryl; wherein carbocyclic aryl is phenyl or naphthyl; carbocyclyl is 9H-fluorenyl; heterocyclyl is 2,3-dihydro-benzo[1,4]dioxinyl, 3,4-dihydro-2H-benzo[b][1,4]dioxepinyl, 4H-benzo[1,3]dioxinyl, benzo[1,3]dioxolyl, furyl, isoxazolyl, or thienyl; and halogen is fluoro, chloro, bromo, or iodo; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

7. The compound according to claim 6 wherein R1 is selected from the group consisting of: (i) C1-5 alkyl, and C1-5 alkyl substituted by substituent(s) independently selected from the group consisting of: C1-5 alkoxy carbonyl, carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: halogen, C1-5 alkyl, and C2-5 alkenyl, C1-5 alkylthio, (ii) C3-6 cycloalkyl, and C3-6 cycloalkyl substituted by carbocyclic aryl, (iii) carbocyclic aryl, and carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: halogen, cyano, nitro, C1-5 alkyl, C1-5 alkyl substituted by halogen, C1-5 alkoxy carbonyl, C1-5 alkoxy, cycloalkoxy, carbocyclic aryloxy, C1-5 alkylthio, and carbocyclic aryl, (iv) heterocyclyl, and heterocyclyl substituted by substituent(s) independently selected from the group consisting of: C1-5 alkyl, C1-5 alkyl substituted by halogen, and carbocyclic aryl; wherein carbocyclic aryl is phenyl or naphthyl; heterocyclyl is 2,3-dihydro-benzo[1,4]dioxinyl, 3,4-dihydro-2H-benzo[b][1,4]dioxepinyl, benzo[1,3]dioxolyl, furyl, or isoxazolyl; and halogen is fluoro, chloro, bromo, or iodo; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

8. The compound according to claim 1 selected from the group consisting of: N-benzyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl] amino}cyclohexyl)urea; N-(2-bromophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-biphenyl-2-yl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(4-bromophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-butyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl] amino}cyclohexyl)urea; N-cyclohexyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl] amino}cyclohexyl)urea; N-(2-chlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,6-dimethylphenyl)urea; N-(2,4-difluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(2,4-dichlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,3-dimethylphenyl)urea; ethyl 3-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]carbonyl}amino)benzoate; ethyl 4-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]carbonyl}amino)benzoate; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-ethylphenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethyl-6-methylphenyl)urea; ethyl N-{[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]carbonyl}leucinate; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-fluorophenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[1-(3-isopropenylphenyl)-1-methylethyl]urea; methyl N-{[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]carbonyl}methioninate; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-methoxyphenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methoxyphenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3-methoxyphenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[4-(methylthio)-phenyl]urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-methoxybenzyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-1-naphthylurea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[(2S)-2-phenylcyclopropyl]urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-phenylurea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-phenoxyphenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-pentylurea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[2-(trifluoromethyl)phenyl]urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-methylphenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-mesitylurea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3-methylphenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methylphenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[1-(1-naphthyl)ethyl]urea; methyl N-{[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]carbonyl}phenylalaninate; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,4,6-trichlorophenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(1-phenylethyl)urea; 1-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-3-(1-phenyl-ethyl)urea; 1-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-3-(1-naphthalen-1-yl-ethyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[2-(methylthio)-phenyl]urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,3,5,6-tetrachlorophenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,3-dimethyl-6-nitrophenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,4,6-tribromophenyl)urea; N-(2,4-dibromo-6-fluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(2,4-dibromophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(2,4-dichlorobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(2,4-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea; N-(2,5-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea; N-(2,6-diethylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(2-chloro-5-nitrophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea; N-[2-chloro-6-(trifluoromethyl)phenyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]-amino}cyclohexyl)urea; N-(2-chloro-6-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea; N-(2-chlorobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethoxyphenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethyl-6-isopropylphenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethylphenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-fluorobenzyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-iodophenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-isopropyl-6-methylphenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-isopropylphenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methoxy-4-nitrophenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methoxy-5-methylphenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methyl-3-nitrophenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methyl-4-nitrophenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methyl-5-nitrophenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methylbenzyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-nitrophenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-propylphenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-phenoxyphenyl)urea; N-(2-tert-butyl-6-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(2-tert-butylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[3-(methylthio)-phenyl]urea; N-1,3-benzodioxol-5-yl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3,4,5-trimethoxyphenyl)urea; N-(3,4-dichlorobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(3,4-difluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(3,4-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea; N-(3,5-difluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(3,5-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3,5-dimethylphenyl)urea; methyl 3-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]carbonyl}amino)benzoate; N-(3-chloro-2-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea; N-(3-chloro-4-fluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea; N-(3-chloro-4-methoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3-ethylphenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3-fluorobenzyl)urea; N-[4-bromo-2-(trifluoromethyl)phenyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(4-bromo-2,6-difluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(4-bromobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-[4-chloro-2-(trifluoromethyl)phenyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(4-chloro-2-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea; N-(4-cyanophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-ethoxyphenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-fluoro-2-nitrophenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-fluorobenzyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-iodophenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-methoxy-2-methylphenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-methylbenzyl)urea; N-(5-chloro-2,4-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(5-fluoro-2-methylphenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-9H-fluoren-9-ylurea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-phenylethyl)urea; N-cyclopentyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(diphenylmethyl)urea; N-[I -(4-bromophenyl)ethyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea; N-(4-bromo-2,6-dimethylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(4-bromo-2-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea; ethyl N-{[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]carbonyl}phenylalaninate; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[2-(2-thienyl)ethyl]urea; N-(2,3-dihydro-1,4-benzodioxin-6-yl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(2,6-dibromo-4-isopropylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-[3-(cyclopentyloxy)-4-methoxyphenyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(3,4-dihydro-2H-1,5-benzodioxepin-7-yl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(4-butyl-2-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[5-methyl-2-(trifluoromethyl)-3-furyl]urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(6-fluoro-4H-1,3-benzodioxin-8-yl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3,5-dimethylisoxazol-4-yl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3-methyl-5-phenylisoxazol-4-yl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(5-methyl-3-phenylisoxazol-4-yl)urea; N-(2-bromophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-biphenyl-2-yl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-butyl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(3-chlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-cyclohexyl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(3-cyanophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(2-chlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,6-dimethylphenyl)urea; N-(3,4-dichlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(2,4-difluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(2,4-dichlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(3,5-dichlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(2,3-dichlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(2,6-difluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,3-dimethylphenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4-ethylphenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-ethyl-6-methylphenyl)urea; ethyl N-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]amino}carbonyl)leucinate; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4-fluorophenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(3-fluorophenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-fluorophenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-[1-(3-isopropenylphenyl)-1-methylethyl]urea; methyl N-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]amino}carbonyl)methioninate; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4-methoxyphenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4-methyl-2-nitrophenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-methoxyphenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(3-methoxyphenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-[4-(methylthio)phenyl]urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-1-naphthylurea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-phenylurea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-pentylurea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-[2-(trifluoromethyl)phenyl]urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4-methylphenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-mesitylurea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(3-methylphenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-methylphenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,4,6-trichlorophenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(1-phenylethyl)urea; 1-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexylmethyl]-3-(1-phenyl-ethyl)-urea; 1-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexylmethyl]-3-(1-naphthalen-1-yl-ethyl)urea; N-(2,6-diisopropylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea; N-[2-(difluoromethoxy)phenyl]-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-[2-(methylthio)phenyl]urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,3,5,6-tetrachlorophenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,3-dimethyl-6-nitrophenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,4,6-tribromophenyl)urea; N-(2,4-dibromo-6-fluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(2,4-dichlorobenzyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(2,5-dimethoxyphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea; N-(2,6-dibromo-4-fluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(2,6-dichlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(2,6-diethylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(2-chloro-5-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea; N-[2-chloro-6-(trifluoromethyl)phenyl]-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]-amino}cyclohexyl)methyl]urea; N-(2-chloro-6-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea; N-(2-chlorobenzyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-ethyl-6-isopropylphenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-ethylphenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-fluoro-5-nitrophenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-fluorobenzyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-iodophenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-isopropyl-6-methylphenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-isopropylphenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-methoxy-5-methylphenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-methoxy-5-nitrophenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-methyl-3-nitrophenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-methyl-4-nitrophenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-methyl-5-nitrophenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-methyl-6-nitrophenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-methylbenzyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-nitrophenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-propylphenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-phenoxyphenyl)urea; N-(2-tert-butyl-6-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(2-tert-butylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-[3-(methylthio)phenyl]urea; N-(3,4-difluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(3,5-difluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(3,5-dimethoxyphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea; N-(3-chloro-2-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea; N-(3-chloro-4-fluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(3-ethylphenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-[3-fluoro-5-(trifluoromethyl)phenyl]urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(3-fluorobenzyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4,5-dimethyl-2-nitrophenyl)urea; N-[4-bromo-2-(trifluoromethyl)phenyl]-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(4-bromo-2,6-difluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-[4-chloro-2-(trifluoromethyl)phenyl]-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(4-chloro-2-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea; N-(4-cyanophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4-fluoro-2-nitrophenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4-fluorobenzyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4-iodophenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4-methoxy-2-methylphenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4-methyl-3-nitrophenyl)urea; N-(5-chloro-2-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(5-fluoro-2-methylphenyl)urea; N-cyclopentyl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(diphenylmethyl)urea; N-(4-bromo-2,6-dimethylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(4-bromo-2-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea; N-(2,6-dibromo-4-isopropylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-3-thienylurea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-[5-methyl-2-(trifluoromethyl)-3-furyl]urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(6-fluoro-4H-1,3-benzodioxin-8-yl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(3,5-dimethylisoxazol-4-yl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(3-methyl-5-phenylisoxazol-4-yl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(5-methyl-3-phenylisoxazol-4-yl)urea; and N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[3-(trifluoromethoxy)phenyl]urea; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

9. The compound according to claim 1 selected from the group consisting of: N-(2-bromophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-biphenyl-2-yl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-butyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(2-chlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,6-dimethylphenyl)urea; N-(2,4-difluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,3-dimethylphenyl)urea; ethyl 3-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]carbonyl}amino)benzoate; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethyl-6-methylphenyl)urea; ethyl N-{[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]-carbonyl}leucinate; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-fluorophenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[1-(3-isopropenylphenyl)-1-methyl ethyl]urea; methyl N-{[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]-carbonyl}methioninate; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[4-(methylthio)phenyl]urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-1-naphthylurea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[(2S)-2-phenylcyclopropyl]urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-phenoxyphenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-pentylurea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[2-(trifluoromethyl)phenyl]urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-mesitylurea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methylphenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[1-(1-naphthyl)ethyl]urea; methyl N-{[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]carbonyl}phenylalaninate; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,4,6-trichlorophenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(1-phenylethyl)urea; -[4-(4-Dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-3-(1-phenyl-ethyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,3,5,6-tetrachlorophenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,4,6-tribromophenyl)urea; N-(2,4-dibromo-6-fluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(2,4-dibromophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(2,4-dichlorobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(2,4-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea; N-(2,6-diethylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-[2-chloro-6-(trifluoromethyl)phenyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]-amino}cyclohexyl)urea; N-(2-chloro-6-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea; N-(2-chlorobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethoxyphenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethyl-6-isopropylphenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethylphenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-fluorobenzyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-iodophenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-isopropyl-6-methylphenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-isopropylphenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methyl-3-nitrophenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methyl-4-nitrophenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methyl-5-nitrophenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methylbenzyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-nitrophenyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-propylphenyl)urea; N-(2-tert-butyl-6-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(2-tert-butylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-1,3-benzodioxol-5-yl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3,4,5-trimethoxyphenyl)urea; N-(3,4-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea; N-(3-chloro-2-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea; N-(3-chloro-4-methoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-[4-bromo-2-(trifluoromethyl)phenyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]-amino}cyclohexyl)urea; N-(4-bromo-2,6-difluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(4-bromobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-[4-chloro-2-(trifluoromethyl)phenyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]-amino}cyclohexyl)urea; N-(4-chloro-2-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea; N-(4-cyanophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-fluorobenzyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-methoxy-2-methylphenyl)urea; N-(5-chloro-2,4-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(diphenylmethyl)urea; N-[1-(4-bromophenyl)ethyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea; N-(4-bromo-2,6-dimethylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea; N-(4-bromo-2-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea; ethyl N-{[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]carbonyl}phenylalaninate; N-(2,3-dihydro-1,4-benzodioxin-6-yl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(2,6-dibromo-4-isopropylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-[3-(cyclopentyloxy)-4-methoxyphenyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(3,4-dihydro-2H-1,5-benzodioxepin-7-yl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)urea; N-(4-butyl-2-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[5-methyl-2-(trifluoromethyl)-3-furyl]urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3-methyl-5-phenylisoxazol-4-yl)urea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(5-methyl-3-phenylisoxazol-4-yl)urea; N-(2-chlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,6-dimethylphenyl)urea; N-(2,4-difluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(3,5-dichlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(2,3-dichlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,3-dimethylphenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-ethyl-6-methylphenyl)urea; ethyl N-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]amino}carbonyl)leucinate; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4-fluorophenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-[4-(methylthio)phenyl]urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-phenylurea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-[2-(trifluoromethyl)phenyl]urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4-methylphenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-mesitylurea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-methylphenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,4,6-trichlorophenyl)urea; N-(2,6-diisopropylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,3-dimethyl-6-nitrophenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,4,6-tribromophenyl)urea; N-(2,4-dibromo-6-fluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(2,6-dibromo-4-fluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(2,6-dichlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(2,6-diethylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-[2-chloro-6-(trifluoromethyl)phenyl]-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]-amino}cyclohexyl)methyl]urea; N-(2-chloro-6-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea; N-(2-chlorobenzyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-ethyl-6-isopropylphenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-ethylphenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-iodophenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-isopropyl-6-methylphenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclobexyl)methyl]-N′-(2-isopropylphenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-methoxy-5-methylphenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-methyl-3-nitrophenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-methyl-6-nitrophenyl)urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-propylphenyl)urea; N-(2-tert-butyl-6-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(2-tert-butylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(3,4-difluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(3,5-difluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-(3-chloro-2-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea; N-(3-chloro-4-fluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]urea; N-(4-bromo-2,6-difluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-[4-chloro-2-(trifluoromethyl)phenyl]-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]-amino}cyclohexyl)methyl]urea; N-(4-cyanophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(diphenylmethyl)urea; N-(4-bromo-2,6-dimethylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]urea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-[5-methyl-2-(trifluoromethyl)-3-furyl]urea; and N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(3-methyl-5-phenylisoxazol-4-yl)urea; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

10. The compound according to claim 3 wherein R1 is selected from the group consisting of: (i) C1-8 alkyl, and C1-8 alkyl substituted by substituent(s) independently selected from the group consisting of: mono-C1-5 alkylamino, di-C1-5 alkylamino, C3-6 cycloalkyl, C3-6 cycloalkenyl, carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: halogen, C1-5 alkyl, and C1-5 alkoxy, heterocyclyl, (ii) C2-5 alkynyl, (iii) C2-5 alkenyl, and C2-5 alkenyl substituted by carbocyclic aryl, (iv) C3-12 cycloalkyl, (v) carbocyclyl, (vi) carbocyclic aryl, and carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: halogen, cyano, nitro, C1-10 alkyl, C1-10 alkyl substituted by substituent(s) independently selected from the group consisting of: halogen, and oxo, carboxy, C1-5 alkoxy carbonyl, C1-5 alkoxy, C1-5 alkoxy substituted by substituent(s) independently selected from the group consisting of: halogen, and carbocyclic aryl, carbocyclic aryloxy, carbocyclic aryloxy substituted by nitro, mono-C1-5 alkylamino, di-C1-5 alkylamino, C1-5 alkoxy carbonylamino, carbocyclic aryl azo, carbocyclic aryl azo substituted by substituent(s) independently selected from the group consisting of: -mono-C1-5 alkylamino, and di-C1-5 alkylamino, C1-5 alkylthio, C1-5 alkylthio substituted by halogen, carbocyclic arylthio, carbocyclic arylthio substituted by nitro, amino sulfonyl, heterocyclyl sulfonyl, C3-6 cycloalkyl, C3-6 cycloalkyl substituted by C1-5 alkyl, carbocyclic aryl, and heterocyclyl, (vii) heterocyclyl, and heterocyclyl substituted by substituent(s) independently selected from the group consisting of: C1-5 alkyl, C1-5 alkoxy carbonyl, carbocyclic aryloxy, carbocyclic aryl, and heterocyclyl; L is Formula (V); and Y is —C(S)NR7—; wherein R7 is hydrogen or C1-5 alkyl; wherein carbocyclic aryl is phenyl or naphthyl; carbocyclyl is indanyl, bicyclo[2.2.1]heptyl, bicyclo[2.2.1]heptenyl, or adamantyl; heterocyclyl is 2,3-dihydro-benzo[1,4]dioxinyl, 4,5,6,7-tetrahydro-benzo[b]thienyl, benzo[1,3]dioxolyl, benzo[2,1,3]thiadiazolyl, furyl, isoxazolyl, morpholinyl, oxazolyl, piperidyl, pyrazolyl, pyridyl, tetrahydrofuryl, or thienyl; and halogen is fluoro, chloro, bromo, or iodo; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

11. The compound according to claim 10 wherein R4a is hydrogen or methyl; R4b is methyl; R5 and R6 are hydrogen; A is a single bond; B is a single bond or —CH2—; and R7 is hydrogen; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

12. The compound according to claim 11 wherein R1 is selected from the group consisting of: (i) C1-6 alkyl, and C1-6 alkyl substituted by substituent(s) independently selected from the group consisting of: C3-6 cycloalkyl, C3-6 cycloalkenyl, carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: halogen, C1-5 alkyl, and C1-5 alkoxy, heterocyclyl, (ii) C3-12 cycloalkyl, (iii) carbocyclyl, (iv) carbocyclic aryl, and carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: halogen, cyano, nitro, C1-5 alkyl, C1-5 alkyl substituted by halogen, C1-5 alkoxy carbonyl, C1-5 alkoxy, C1-5 alkoxy substituted by halogen, mono-C1-5 alkylamino, di-C1-5 alkylamino, C1-5 alkylthio, and carbocyclic aryl, (v) heterocyclyl, and heterocyclyl substituted by substituent(s) independently selected from the group consisting of: C1-5 alkyl, C1-5 alkoxy carbonyl, and carbocyclic aryl; wherein carbocyclic aryl is phenyl or naphthyl; carbocyclyl is indanyl, bicyclo[2.2.1]heptyl, or bicyclo[2.2.1]heptenyl; heterocyclyl is 2,3-dihydro-benzo[1,4]dioxinyl, benzo[1,3]dioxolyl, isoxazolyl, tetrahydrofuryl, or thienyl; and halogen is fluoro, chloro, bromo, or iodo; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

13. The compound according to claim 12 wherein R1 is selected from the group consisting of: (i) C1-5 alkyl, and C1-5 alkyl substituted by substituent(s) independently selected from the group consisting of: carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: halogen, and C1-5 alkoxy, (ii) carbocyclyl, (iii) carbocyclic aryl, and carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: halogen, cyano, nitro, C1-5 alkyl, C1-5 alkyl substituted by halogen, C1-5 alkoxy carbonyl, C1-5 alkoxy, C1-5 alkoxy substituted by halogen, mono-C1-5 alkylamino, di-C1-5 alkylamino, and carbocyclic aryl, (iv) heterocyclyl, and heterocyclyl substituted by substituent(s) independently selected from the group consisting of: C1-5 alkyl, C1-5 alkoxy carbonyl, and carbocyclic aryl; wherein carbocyclic aryl is phenyl or naphthyl; carbocyclyl is bicyclo[2.2.1]heptyl; heterocyclyl is 2,3-dihydro-benzo[1,4]dioxinyl, benzo[1,3]dioxolyl, isoxazolyl, or thienyl; and halogen is fluoro, chloro, bromo, or iodo; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

14. The compound according to claim 1 selected from the group consisting of: N-(4-bromophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(4-cyanophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-cyclohexyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-cyclopentyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(4-chlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-thiourea; N-(2,4-dichlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(2,4-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,6-dimethylphenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yla amino}cyclohexyl)-N′-(2-ethyl-6-isopropylphenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-fluorophenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-hexylthiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-isobutylthiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-methoxybiphenyl-3-yl)thiourea; N-(1,3-benzodioxol-5-ylmethyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[4-(methylthio)phenyl]thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-methoxyphenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methoxyphenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-1-naphthylthiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-nitrophenyl)-thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(pentafluorophenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-propylthiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3,4,5-trimethoxyphenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-methylphenyl)thiourea; N-(3,4-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-ethylphenyl)-thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[2-(methylthio)-phenyl]thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[2-(trifluoromethoxy)phenyl]thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,3,4-trifluorophenyl)thiourea; N-(2,5-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea; N-(2-chloro-4-nitrophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethylphenyl)-thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-iodophenyl)-thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methoxy-4-nitrophenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methoxy-5-methylphenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3-iodophenyl)-thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3-methoxyphenyl)thiourea; N-[4-(difluoromethoxy)phenyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[4-(trifluoromethyl)phenyl]thiourea; N-(4-bromo-2-chlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-iodophenyl)-thiourea; N-(5-chloro-2-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea; N-[(1S,4R)-bicyclo[2.2.1]hept-2-yl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-[2-(4-chlorophenyl)ethyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,4,6-tribromophenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,4,6-trichlorophenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-mesitylthiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,4-dimethylphenyl)thiourea; N-(2,6-diethylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(2,6-diisopropylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea; N-(2-bromo-4-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea; N-(2-chlorobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethyl-6-methylphenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-isopropylphenyl)thiourea; N-(3,5-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3,5-dimethylphenyl)thiourea; N-(3-chloro-4-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea; methyl 3-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]-carbonothioyl}amino)benzoate; N-(4-bromo-2,6-dimethylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(4-bromo-2-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea; N-[4-bromo-2-(trifluoromethyl)phenyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(4-chloro-2-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[1-(4-fluorophenyl)ethyl]thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-fluorobenzyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-isopropylphenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-methoxybenzyl)thiourea; methyl 4-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]-carbonothioyl}amino)benzoate; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(1-phenylethyl)-thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(diphenylmethyl)thiourea; N-(cyclohexylmethyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-cyclooctyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-cyclopropyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(1-naphthylmethyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,2-diphenylethyl)thiourea; N-(2,3-dimethoxybenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,4,5-trimethylphenyl)thiourea; N-[2-(2,5-dimethoxyphenyl)ethyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-biphenyl-2-yl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino})cyclohexyl)-N′-(2-fluorobenzyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methyl-4-nitrophenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methylbenzyl)thiourea; N-(3-chlorobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; ethyl 3-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]-carbonothioyl}amino)benzoate; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3-ethylphenyl)-thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3-fluorobenzyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3-methoxybenzyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3-methylbenzyl)thiourea; N-[4-chloro-2-(trifluoromethyl)phenyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-fluoro-2-methylphenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-methoxy-2-methylphenyl)thiourea; N-(5-chloro-2,4-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(2,3-dihydro-1 H-inden-5-yl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-cycloheptyl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[(1 R)-1-phenylethyl]thiourea; N-(2-cyclohex-1-en-I -ylethyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,3-dimethylphenyl)thiourea; N-(2,4-dibromo-6-fluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(2,4-dichloro-6-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,5-dimethylphenyl)thiourea; N-(2-bromo-4-isopropylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(2-bromo-5-fluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethoxyphenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-isopropyl-6-methylphenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methoxybenzyl)thiourea; N-(2,3-dihydro-1,4-benzodioxin-6-yl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-1,3-benzodioxol-5-yl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(3-chloro-2-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea; N-[4-bromo-2-(trifluoromethoxy)phenyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(4-chloro-2,5-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-phenylbutyl)-thiourea; N-bicyclo[2.2.1 ]hept-2-yl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea; methyl 3-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]-carbonothioyl}amino)-4-methylthiophene-2-carboxylate; methyl 3-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]-carbonothioyl}amino)thiophene-2-carboxylate; N-(2-bromo-4-fluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea; N-(4-butyl-2-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea; N-[4-(dimethylamino)-1-naphthyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(5-methyl-3-phenylisoxazol-4-yl)thiourea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,6-dimethylphenyl)thiourea; N-(2,6-dichlorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-ethyl-6-isopropylphenyl)thiourea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-isobutylthiourea; N-(1,3-benzodioxol-5-ylmethyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4-nitrophenyl)thiourea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(pentafluorophenyl)thiourea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(tetrahydrofuran-2-ylmethyl)thiourea; N-[(cis-4-{8 4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-[2-(trifluoromethoxy)phenyl]thiourea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,3,4-trifluorophenyl)thiourea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-ethylphenyl)thiourea; N-(5-chloro-2-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]thiourea; N-[(1 S,4R)-bicyclo[2.2.1 ]hept-2-yl]-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea; N-[2-(3,4-dimethoxyphenyl)ethyl]-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,4,6-tribromophenyl)thiourea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,4,6-trichlorophenyl)thiourea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-mesitylthiourea; N-(2,6-diethylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea; N-(2,6-diisopropylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]thiourea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-ethyl-6-methylphenyl)thiourea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-isopropylphenyl)thiourea; N-(4-bromo-2,6-dimethylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea; N-[4-bromo-2-(trifluoromethyl)phenyl]-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-[1-(4-fluorophenyl)ethyl]thiourea; N-(5-chloro-2-methoxyphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(diphenylmethyl)thiourea; N-cyclododecyl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea; N-(cyclohexylmethyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,3,5,6-tetrachlorophenyl)thiourea; N-(2,3-dimethoxybenzyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]thiourea; N-(2,4-dichlorobenzyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-methoxy-5-nitrophenyl)thiourea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(4-methoxy-2-methylphenyl)thiourea; N-(2,4-dibromo-6-fluorophenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea; N-(2,4-dichloro-6-methylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,5-dimethylphenyl)thiourea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-ethoxyphenyl)thiourea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-isopropyl-6-methylphenyl)thiourea; N-[4-bromo-2-(trifluoromethoxy)phenyl]-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea; N-bicyclo[2.2.1 ]hept-2-yl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)methyl]thiourea; N-bicyclo[2.2.1 ]hept-5-en-2-yl-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea; N-(cyclopropylmethyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea; and N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(5-methyl-3-phenylisoxazol-4-yl)thiourea; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

15. The compound according to claim 1 selected from the group consisting of: N-(4-bromophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(4-cyanophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(2,4-dichlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(2,4-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,6-dimethylphenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethyl-6-isopropylphenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methoxyphenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-1-naphthylthiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(3,4,5-trimethoxyphenyl)thiourea; N-(3,4-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethylphenyl)-thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methoxy-4-nitrophenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-methoxy-5-methylphenyl)thiourea; N-(4-bromo-2-chlorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-iodophenyl)-thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,4,6-tribromophenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,4,6-trichlorophenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-mesitylthiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,4-dimethylphenyl)thiourea; N-(2,6-diethylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(2-bromo-4-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea; N-(2-chlorobenzyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethyl-6-methylphenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-isopropylphenyl)thiourea; methyl 3-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]-carbonothioyl}amino)benzoate; N-(4-bromo-2,6-dimethylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-fluoro-2-methylphenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-methoxy-2-methylphenyl)thiourea; N-(5-chloro-2,4-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[(1R)-1-phenylethyl]thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,3-dimethylphenyl)thiourea; N-(2,4-dibromo-6-fluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(2,4-dichloro-6-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethoxyphenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-isopropyl-6-methylphenyl)thiourea; N-(2,3-dihydro-1,4-benzodioxin-6-yl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-1,3-benzodioxol-5-yl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-fluoro-2-methylphenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(4-methoxy-2-methylphenyl)thiourea; N-(5-chloro-2,4-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-[(1R)-1-phenylethyl]thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2,3-dimethylphenyl)thiourea; N-(2,4-dibromo-6-fluorophenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(2,4-dichloro-6-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-ethoxyphenyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(2-isopropyl-6-methylphenyl)thiourea; N-(2,3-dihydro-1,4-benzodioxin-6-yl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-1,3-benzodioxol-5-yl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(3-chloro-2-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea; N-[4-bromo-2-(trifluoromethoxy)phenyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(4-chloro-2,5-dimethoxyphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-bicyclo[2.2.1 ]hept-2-yl-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea; methyl 3-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]-carbonothioyl}amino)-4-methylthiophene-2-carboxylate; methyl 3-({[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)amino]-carbonothioyl}amino)thiophene-2-carboxylate; N-(4-butyl-2-methylphenyl)-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexyl)thiourea; N-[4-(dimethylamino)-1-naphthyl]-N′-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)thiourea; N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)-N′-(5-methyl-3-phenylisoxazol-4-yl)thiourea; N-(2,6-diethylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea; N-(4-bromo-2,6-dimethylphenyl)-N′-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]thiourea; N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2,3,5,6-tetrachlorophenyl)thiourea; and N-[(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexyl)methyl]-N′-(2-isopropyl-6-methylphenyl)thiourea; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

16. The compound according to claim 3 wherein: R1 is selected from the group consisting of (i) C1-8 alkyl, and C1-8 alkyl substituted by substituent(s) independently selected from the group consisting of: halogen, C1-5 alkoxy, C1-5 alkoxy substituted by carbocyclic aryl, carbocyclyl, carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: halogen, nitro, and C1-5 alkoxy, (ii) C2-5 alkenyl, (iii) carbocyclyl, (iv) carbocyclic aryl, and carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: halogen, C1-5 alkyl, C1-5 alkyl substituted by halogen, and C1-5 alkoxy; L is Formula (V); and Y is —C(O)O—; wherein carbocyclic aryl is phenyl or naphthyl; carbocyclyl is 9H-fluorenyl or menthyl; and halogen is fluoro, chloro, bromo, or iodo; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

17. The compound according to claim 16 wherein R4a is hydrogen or methyl; R4b is methyl; R5 and R6 are hydrogen; A is a single bond; and B is a single bond or —CH2—; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

18. The compound according to claim 1 selected from the group consisting of: cis-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-carbamic acid 2-benzyloxy-ethyl ester; cis-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-carbamic acid 4,5-dimethoxy-2-nitro-benzyl ester; cis-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-carbamic acid 2-chloro-benzyl ester; cis-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-carbamic acid 4,5-dimethoxy-2-nitro-benzyl ester; cis-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-carbamic acid 4-nitro-benzyl ester; cis-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexyl]-carbamic acid benzyl ester; cis-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexylmethyl]-carbamic acid 2-chloro-benzyl ester; cis-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexylmethyl]-carbamic acid 4-nitro-benzyl ester; and cis-[4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexylmethyl]-carbamic acid benzyl ester; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

19. The compound according to claim 3 wherein: R1 is Cl-8 alkyl, and C1-8 alkyl substituted by substituent(s) independently selected from the group consisting of: carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: halogen, C1-5 alkyl, C1-5 alkyl substituted by halogen, C1-5 alkoxy, and C1-5 alkoxy substituted by halogen, R4 is —N(R4a)(R4b) wherein R4a and R4b are independently C1-5 alkyl; L is Formula (VIII) or (IX) wherein R5 and R6 are both hydrogen; A and B are each independently a single bond or —CH2—; and Y is a single bond; wherein carbocyclic aryl is phenyl; and halogen is fluoro or chloro; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

20. The compound according to claim 19 wherein: R1 is C1-8 alkyl, and C1-8 alkyl substituted by substituent(s) independently selected from the group consisting of: carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: C1-5 alkoxy, and C1-5 alkoxy substituted by halogen, wherein carbocyclic aryl is phenyl; and halogen is fluoro or chloro; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

21. The compound according to claim 20 wherein: R4 is —N(CH3)2; L is Formula (VIII) or (IX) wherein A is a single bond and B is —CH2—, or A is —CH2— and B is a single bond; and Y is a single bond; wherein carbocyclic aryl is phenyl; and halogen is fluoro; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

22. The compound according to claim 1 is: N2-[(1S,3R)-3-({[4-bromo-2-(trifluoromethoxy)benzyl]amino}-methyl)cyclopentyl]-N4,N4-dimethylquinazoline-2,4-diamine; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

23. The compound according to claim 3 wherein: R1 is selected from the group consisting of: (i) C1-8 alkyl, and C1-8 alkyl substituted by substituent(s) independently selected from the group consisting of: carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: hydroxy, halogen, nitro, C1-5 alkylcarbonylamino, C3-6 cycloalkylcarbonylamino, C1-5 alkyl, C1-5 alkyl substituted by halogen, C1-5 alkylsulfonyl, C1-5 alkoxy, C1-5 alkoxy substituted by halogen, and carbocyclic aryl, heterocyclyl, and heterocyclyl substituted by halogen, (ii) C3-12 cycloalkyl, and C3-12 cycloalkyl substituted by carbocyclic aryl, (iii) carbocyclyl, and carbocyclyl by substituent(s) independently selected from the group consisting of: hydroxy, and carbocyclic aryl, (iv) carbocyclic aryl, and carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: halogen, C1-5 alkoxy, and nitro, (v) heterocyclyl, and heterocyclyl substituted by substituent(s) independently selected from the group consisting of: halogen, and C1-5 alkoxy, R4 is —N(R4a)(R4b) wherein R4a and R4b are each independently C1-5 alkyl; L is Formula (XIII); wherein R5 and R6 are both hydrogen; A is a single bond and B is a single bond or —CH2—; and Y is —C(O)NR7—, wherein R7 is hydrogen or C1-5 alkyl; wherein carbocyclic aryl is phenyl or naphthyl; carbocyclyl is indanyl, 9H-fluorenyl, 1,2,3,4-tetrahydro-naphthalen-1-yl, or 1H-indolyl; heterocyclyl is benzo[1,3]dioxolyl, pyridyl, dibenzofuranyl, 1H-benzoimidazolyl, or thiazolyl; and halogen is fluoro, chloro, bromo, or iodo; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

24. The compound according to claim 23 wherein: R1 is selected from the group consisting of: (i) C1-8 alkyl, and C1-8 alkyl substituted by substituent(s) independently selected from the group consisting of: carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: hydroxy, halogen, nitro, C1-5 alkylcarbonylamino, C1-5 alkyl, C1-5 alkyl substituted by halogen, C1-5 alkylsulfonyl, C1-5 alkoxy, 1-5 alkoxy substituted by halogen, and carbocyclic aryl, heterocyclyl, and heterocyclyl substituted by halogen, (ii) C3-12 cycloalkyl, and C3-12 cycloalkyl substituted by carbocyclic aryl, (iii) carbocyclyl, (iv) carbocyclic aryl, and carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: halogen, and nitro, (v) heterocyclyl, and heterocyclyl substituted by substituent(s) independently selected from the group consisting of: halogen, and C1-5 alkoxy, wherein carbocyclic aryl is phenyl or naphthyl; carbocyclyl is indanyl, 9H-fluorenyl, or 1,2,3,4-tetrahydro-naphthalen-1-yl; heterocyclyl is benzo[1,3]dioxolyl, or pyridyl; and halogen is fluoro, chloro, bromo, or iodo; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

25. The compound according to claim 24 wherein R4 is —N(CH3)2; A and B are both a single bond; and Y is —C(O)NH—; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

26. The compound according to claim 1 selected from the group consisting of: cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(2,3-dimethylbenzyl)-cyclohexanecarboxamide; cis-N-(2-bromobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-N-(2-chlorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(4-methylbenzyl)-cyclohexanecarboxamide; cis-N-(3,5-bis(trifluoromethyl)benzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide; cis-N-(2,4-dimethoxybenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(1,2,3,4-tetrahydronaphthalen-1-yl)cyclohexanecarboxamide; cis-N-(2,3-dihydro-1H-inden-2-yl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[(1S)-i -(4-nitrophenyl)ethyl]-cyclohexanecarboxamide; cis-N-(3,5-dichlorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[4-(trifluoromethoxy)benzyl]-cyclohexanecarboxamide; cis-N-(4-bromobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(4-methoxybenzyl)-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(2-fluoro-4-nitrophenyl)-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(3-fluoro-4-methylbenzyl)-cyclohexanecarboxamide; cis-N-(5-chloro-2-methylbenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; and cis-N-(2,4-dichloro-6-methylbenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

27. The compound according to claim 1 selected form the group consisting of: cis-N-(2,3-dimethoxybenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-N-(2,4-difluorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-N-(2,4-dichlorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-N-(2,3-dichlorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-N-(2,5-dichlorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-N-(3-chlorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(3-methoxybenzyl)-cyclohexanecarboxamide; cis-N-(3,4-dimethoxybenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-N-(3,5-dimethoxybenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(4-hydroxy-3-methoxybenzyl)-cyclohexanecarboxamide; cis-N-(1,3-benzodioxol-5-ylmethyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[(1R)-1-(4-nitrophenyl)ethyl]-cyclohexanecarboxamide; cis-4-(4-dimethylamino-quinazolin-2-ylamino)-cyclohexanecarboxylic acid (trans-2-phenylcyclopropyl)amide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[(l S)-1-(4-methylphenyl)ethyl]-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[(l R)-1-(1-naphthyl)ethyl]-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[3-(trifluoromethyl)benzyl]-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(3-methoxyphenyl)-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(3-iodobenzyl)-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(4-methoxybenzyl)-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(3-iodophenyl)-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[3-(propionylamino)benzyl]-cyclohexanecarboxamide; cis-N-benzyl-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-N-[(6-chloropyridin-3-yl)methyl]-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[(1R)-1-(3-methoxyphenyl)ethyl]cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[1-(4-fluorophenyl)ethyl]-cyclohexanecarboxamide; cis-N-[(1R)-1-(4-chlorophenyl)ethyl]-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-N-[1-(4-bromophenyl)ethyl]-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[(1 S)-I -(1-naphthyl)ethyl]-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(3,5-dimethylbenzyl)-cyclohexanecarboxamide; cis-N-(3-chloro-2-methylbenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(5-fluoro-2-methylbenzyl)-cyclohexanecarboxamide; cis-N-(3-chloro-2,6-difluorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-N-(biphenyl-3-ylmethyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-N-(biphenyl-4-ylmethyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-N-(6-chloro-2-fluoro-3-methylbenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(2-fluorobenzyl)-cyclohexanecarboxamide; cis-N-(2,6-difluorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[4-(trifluoromethyl)benzyl]-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(1-naphthylmethyl)-cyclohexanecarboxamide; cis-N-(4-chlorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-N-(3,4-dichlorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(3-fluorobenzyl)-cyclohexanecarboxamide; cis-N-(2,5-difluorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-N-(2,3-difluorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-N-(3-bromobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-N-(3-bromo-4-fluorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-N-(4-bromo-2-fluorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-N-(5-bromo-2-fluorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-N-(4-chloro-2-fluorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(3-methylbenzyl)-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(2-methylbenzyl)-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[2-(trifluoromethoxy)benzyl]-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(2,3,4-trifluorobenzyl)-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(2,4,5-trifluorobenzyl)-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(3,4,5-trifluorobenzyl)-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-(2,3,6-trifluorobenzyl)-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[3-fluoro-5-(trifluoromethyl)benzyl]cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[4-fluoro-2-(trifluoromethyl)benzyl]cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[2-fluoro-4-(trifluoromethyl)benzyl]cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[4-fluoro-3-(trifluoromethyl)benzyl]cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[2-fluoro-3-(trifluoromethyl)benzyl]cyclohexanecarboxamide; cis-N-[4-chloro-3-(trifluoromethyl)benzyl]-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide; cis-N-(2-chloro-6-fluorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-N-(3-chloro-4-fluorobenzyl)-4-{[4-(dim ethyl amino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-N-(2-chloro-4-fluorobenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-N-[2-chloro-5-(trifluoromethyl)benzyl]-4-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclohexanecarboxamide; cis-N-[2-(difluoromethoxy)benzyl]-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-N-[3-(difluoromethoxy)benzyl]-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[3-(trifluoromethoxy)benzyl]-cyclohexanecarboxamide; cis-N-(2,6-dimethoxybenzyl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[(1R)-1-phenylethyl]-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[(1S)-1-(4-methoxyphenyl)ethyl]cyclohexanecarboxamide; cis-N-[bis(4-methoxyphenyl)methyl]-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[2-(trifluoromethyl)benzyl]-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-9H-fluoren-9-ylcyclohexanecarboxamide; cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino}-N-[4-(methylsulfonyl)benzyl]-cyclohexanecarboxamide; and cis-N-(6-chloropyridin-3-yl)-4-{[4-(dimethylamino)quinazolin-2-yl]amino}- cyclohexanecarboxamide; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

28. The compound according to claim 3 wherein: R1 is selected from the group consisting of: (i) C1-8 alkyl, and C1-8 alkyl substituted by substituent(s) independently selected from the group consisting of: carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: C1-5 alkoxy, and C1-5 alkoxy substituted by halogen, (ii) carbocyclic aryl, and carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: halogen, and C1-7 alkoxy, R4 is —N(R4a)(R4b) wherein R4a and R4b are each independently C1-5 alkyl; L is Formula (XIII) wherein R5 is hydrogen; A is a single bond and B is a single bond or —CH2—; and Y is —C(O)O— or —OC(O)—; wherein carbocyclic aryl is phenyl or naphthyl; and halogen is fluoro, chloro, bromo, or iodo; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

29. The compound according to claim 28 wherein R4 is —N(CH3)2; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

30. The compound according to claim 3 wherein: R1 is selected from the group consisting of: carbocyclic aryl, and carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: halogen, C1-10 alkyl, C1-10 alkyl substituted by halogen, C1-7 alkoxy, and C1-7 alkoxy substituted by halogen, R4 is —N(R4a)(R4b) wherein R4a and R4b are each independently C1-5 alkyl; L is Formula (VIII) or (IX) wherein A and B are each independently a single bond or —CH2—; and Y is —C(O)—, wherein carbocyclic aryl is phenyl; and halogen is fluoro, chloro, bromo, or iodo; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

31. The compound according to claim 30 wherein R4 is —N(CH3)2; R5 and R6 are both hydrogen; and A is a single bond, and B is —CH2—; or A is a —CH2—, and B is a single bond, or a pharmaceutically acceptable salt, hydrate or solvate thereof.

32. The compound according to claim 1 selected from the group consisting of: p1 3,4-dichloro-N-[((1R,3S)-3-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclopentyl)-methyl]benzamide; N-[(1 S,3R)-3-({[4-(dimethylamino)quinazolin-2-yl]amino}methyl)cyclopentyl]-4-fluorobenzamide; 4-chloro-N-[((1R,3S)-3-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclopentyl)methyl]benzamide; and N-[((1 R,3 S)-3-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclopentyl)methyl]-3,5-difluorobenzamide; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

33. The compound according to claim 1 selected from the group consisting of: N-[((1R,3S)-3-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclopentyl)methyl]-3,5-dimethoxybenzamide; 2,4,6-trichloro-N-[((1R,3S)-3-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclopentyl)methyl]benzamide; N-[((1R,3S)-3-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclopentyl)methyl]-3-fluoro-4-(trifluoromethyl)benzamide; N-[((1R,3S)-3-{[4-(dimethylamino)quinazolin-2-yl]amino}cyclopentyl)methyl]-4-(trifluoromethoxy)benzamide; and N-[(1S,3R)-3-({[4-(dimethylamino)quinazolin-2-yl]amino}methyl)cyclopentyl]-2,4-difluorobenzamide; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

34. The compound according to claim 2 wherein Q is Formula (IIa).

35. The compound according to claim 34 wherein: R1 is selected from the group consisting of: (i) C1-8 alkyl, and C1-8 alkyl substituted by carbocyclic aryl, (ii) carbocyclic aryl, and carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: halogen, C1-10 alkyl, C1-10 alkyl substituted by halogen, C1-7 alkoxy, and C1-7 alkoxy substituted by halogen, R2 is —N(R2a)(R2b), wherein R2a and R2b are each independently C1-5 alkyl; L is Formula (V) wherein R5 and R6 are both hydrogen; A and B are both a single bond; X1, X2, X3 and X4 are independently selected from the group consisting of hydrogen, halogen, and C1-4 alkyl; provided that at least one substituent selected from the group consisting of X1, X2, X3 and X4 is not hydrogen; and Y is —C(O)—; wherein carbocyclic aryl is phenyl; and halogen is fluoro, chloro, bromo, or iodo; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

36. The compound according to claim 35 wherein R2 is —N(CH3)2; and X1, X2, X3 and X4 are independently selected from the group consisting of hydrogen, fluoro, and methyl; provided that at least one substituent selected from the group consisting of X1, X2, X3 and X4 is not hydrogen; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

37. The compound according to claim 1 selected from the group consisting of: N-(cis-4-{[4-(dimethylamino)-6-methylquinazolin-2-yl]amino}cyclohexyl)-2,2-diphenylacetamide; N-(cis-4-{[4-(dimethylamino)-6-methylquinazolin-2-yl]amino}cyclohexyl)-4-fluoro-3-(trifluoromethyl)benzamide; N-(cis-4-{[4-(dimethylamino)-6-methylquinazolin-2-yl]amino}cyclohexyl)-3,5-bis(trifluoromethyl)benzamide; and N-(cis-4-{[4-(dimethylamino)-6-methylquinazolin-2-yl]amino}cyclohexyl)-3,4,5-trimethoxybenzamide; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

38. The compound according to claim 1 selected from the group consisting of: 3-chloro-N-(cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexyl)benzamide; 3,4-dichloro-N-(cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexyl)benzamide; N-(cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexyl)-3,5-dimethoxybenzamide; N-(cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexyl)benzamide; N-(cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexyl)-4-methylbenzamide; N-(cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexyl)-4-fluorobenzamide; N-(cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexyl)-3-methoxybenzamide; N-(cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexyl)-3,4-difluorobenzamide; and N-(cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexyl)-3-(trifluoromethyl)benzamide; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

39. The compound according to claim 34 wherein: R1 is selected from the group consisting of: (i) C1-8 alkyl, and C1-8 alkyl substituted by substituent(s) independently selected from the group consisting of: carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: halogen, C1-5 alkyl, C1-5 alkyl substituted by halogen, C1-5 alkoxy, and C1-5 alkoxy substituted by halogen, (ii) heterocyclyl, and heterocyclyl substituted by halogen, R2 is —N(R2a)(R2b), wherein R2a and R2b are each independently C1-5 alkyl; L is Formula (XIII); X1, X2, X3 and X4 are independently hydrogen or halogen; provided that at least one substituent selected from the group consisting of X1, X2, X3 and X4 is not hydrogen; and Y is —C(O)NR7— wherein R7 is hydrogen or C1-5 alkyl; wherein carbocyclic aryl is phenyl; heterocyclyl is pyridyl; and halogen is fluoro, chloro, bromo, or iodo; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

40. The compound according to claim 39 wherein R2 is —N(CH3)2; L is Formula (XIII) wherein A and B are both a single bond; X1, X2, X3 and X4 are independently hydrogen or fluoro; provided that at least one substituent selected from the group consisting of X1, X2, X3 and X4 is not hydrogen; and Y is —C(O)NH—; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

41. The compound according to claim 1 selected from the group consisting of: cis-N-benzyl-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-N-(3,5-dimethoxybenzyl)-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-N-(3-methoxybenzyl)cyclohexanecarboxamide; cis-N-[(6-chloropyridin-3-yl)methyl]-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-N-[3-(trifluoromethyl)benzyl]cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-N-[4-(trifluoromethyl)benzyl]cyclohexanecarboxamide; cis-N-[3,5-bis(trifluoromethyl)benzyl]-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-N-(3-iodobenzyl)-cyclohexanecarboxamide; and cis-N-[1-(4-bromophenyl)ethyl]-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexanecarboxamide; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

42. The compound according to claim 1 selected from the group consisting of: cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-N-(4-methylbenzyl)-cyclohexanecarboxamide; cis-N-(3-chlorobenzyl)-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-N-[(1R)-1-(3-methoxyphenyl)ethyl]cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-N-(4-methoxybenzyl)cyclohexanecarboxamide; cis-N-(2,4-dichlorobenzyl)-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexanecarboxamide; cis-N-(3,5-dichlorobenzyl)-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}cyclohexanecarboxamide; cis-N-(4-bromobenzyl)-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-N-(2-bromobenzyl)-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-cyclohexanecarboxamide; cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-N-[4-(trifluoromethoxy)benzyl]cyclohexanecarboxamide; and cis-4-{[4-(dimethylamino)-6,7-difluoroquinazolin-2-yl]amino}-N-[(1S)-1-(4-methylphenyl)ethyl]cyclohexanecarboxamide; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

43. The compound according to claim 2 wherein Q is Formula (IIb).

44. The compound according to claim 43 wherein: R1 is selected from the group consisting of: C1-8 alkyl, and C1-8 alkyl substituted by substituent(s) independently selected from the group consisting of: carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from the group consisting of: halogen, C1-5 alkyl, and C1-5 alkoxy, R3 is C1-5 alkyl; L is Formula (XIII); wherein R5 and R6 are both hydrogen; A and B are both a single bond; Y is —C(O)NR7—; wherein carbocyclic aryl is phenyl; and halogen is fluoro, chloro, bromo, or iodo; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

45. The compound according to claim 44 wherein R3 is isopropyl; and Y is —C(O)NH—: or a pharmaceutically acceptable salt, hydrate or solvate thereof.

46. The compound according to claim 1 is: cis-N-(3-chlorobenzyl)-4-[(4-isopropylquinazolin-2-yl)amino]cyclohexanecarboxamide; or a pharmaceutically acceptable salt, hydrate or solvate thereof.

47. The compound according to claim 1 wherein R1 is selected from hydrogen, —CO2tBu, or —CO2Bn (Bn is a benzyl group); R2 is —N(R2a)(R2b), wherein R2a is hydrogen or C1-5 alkyl; R2b is C1-5 alkyl; R3 is C1-5 alkyl; R4 is —N(R4a )(R4b) wherein R4a is hydrogen or C1-5 alkyl; R4b is C1-5 alkyl; L is selected from Formula (V), (VIII), (IX), (XIII), (XVI), or (XVII); X1, X2, X3 and X4 are independently selected from the group consisting of hydrogen, halogen, and C1-4 alkyl; provided that at least one substituent selected from the group consisting of X1, X2, X3 and X4 is not hydrogen; and Y is a single bond; or a pharmaceutically acceptable salt, hydrate, or solvate thereof.

48. A pharmaceutical composition comprising a therapeutically effective amount of a compound according to claim 1 in combination with a pharmaceutically acceptable carrier.

49. A method for the prophylaxis or treatment of improving memory function, sleeping and arousal, anxiety, depression, mood disorders, seizure, obesity, diabetes, appetite and eating disorders, cardiovascular disease, hypertension, dyslipidemia, myocardial infarction, binge eating disorders including bulimia, anorexia, mental disorders including manic depression, schizophrenia, delirium, dementia, stress, cognitive disorders, attention deficit disorder, substance abuse disorders and dyskinesias including Parkinson's disease, epilepsy, and addiction comprising administering to an individual suffering from said condition a therapeutically effective amount of a compound according to claim 1 or a pharmaceutical composition according to claim 48.

50. A method for the prophylaxis or treatment of an eating disorder, obesity or an obesity related disorder comprising administering to an individual suffering from said condition a therapeutically effective amount of a compound according to claim 1 or a pharmaceutical composition according to claim 48.

51. A method for the prophylaxis or treatment of anxiety, depression, schizophrenia, addiction, or epilepsy comprising administering to an individual suffering from said condition a therapeutically effective amount of a compound according to claim 1 or a pharmaceutical composition according to claim 48.

52. A compound according to claim 1 for use in a method of treatment of the human or animal body by therapy.

53. A compound according to claim 1 for use in a method of prophylaxis or treatment of an eating disorder, obesity or an obesity related disorder of the human or animal body by therapy.

54. A compound according to claim 1 for use in a method of prophylaxis or treatment of anxiety, depression, schizophrenia, addiction, or epilepsy of the human or animal body by therapy.

55. A compound according to claim 1 for the manufacture of a medicament for use in the prophylaxis or treatment of an eating disorder, obesity or obesity related disorders.

56. A compound according to claim 1 for the manufacture of a medicament for use in the prophylaxis or treatment of anxiety, depression, schizophrenia, addiction, or epilepsy.

57. A method of producing a pharmaceutical composition comprising admixing a compound according claim 1 and a pharmaceutically acceptable carrier.