Claims
- 1. A compound having the formula (I):
- 2. The compound of claim 1 wherein X1 is —O—.
- 3. The compound of claim 1 wherein Ar1 and Ar2 are each independently
- 4. The compound of claim 3 wherein R8, R9 and R10 are each independently selected from the group consisting of H, —CH3, halogen and —CF3.
- 5. The compound of claim 1 wherein
X1 is —O—; and Ar1 and Ar2 are each independently 130wherein R8, R9 and R10 are each independently selected from the group consisting of H, —CH3, halogen and —CF3.
- 6. The compound of claim 1 wherein
- 7. The compound of claim 6 wherein
X1 is —O—; and R3, R4, R27 and R28 are each H.
- 8. The compound of claim 6 wherein R5 and R6 are H.
- 9. The compound of claim 7 wherein R7 and R11, taken together with the nitrogen to which they are attached, form a 5-7 membered ring having the following formula:
- 10. The compound of claim 1 having the formula
- 11. The compound of claim 1 having the formula:
- 12. The compound of claim 11 or the pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R7, R8 and R11 are selected from the group consisting of
- 13. The compound of claim 12 having the formula:
- 14. The compound of claim 12 having the formula:
- 15. The compound of claim 12 having the formula:
- 16. The compound of claim 12 having the formula:
- 17. The compound of claim 12 having the formula:
- 18. A pharmaceutical composition comprising at least one compound of claim 1, and a pharmaceutically acceptable carrier.
- 19. A pharmaceutical composition comprising a pharmaceutically acceptable carrier, at least one serotonin reuptake inhibitor, and at least one compound of claim 1.
- 20. A method for treating a physiological disorder, symptom or disease in a patient in need of such treatment, comprising administering to said patient an effective amount of at least one compound of claim 1, wherein said physiological disorder, symptom or disease is selected from the group consisting of: respiratory diseases, inflammatory diseases, skin disorders, ophthalmalogical disorders, central nervous system conditions, addictions, epilepsy, nociception, psychosis, schizophrenia, Alzheimer's disease, AIDs related dementia, Towne's disease, stress related disorders, obsessive/compulsive disorders, eating disorders, sleep disorders, mania, premenstrual syndrome, gastrointestinal disorders, atherosclerosis, fibrosing disorders, obesity, Type II diabetes, pain related disorders, bladder and genitourinary disorders, and nausea.
- 21. A method for treating a physiological disorder, symptom or disease in a patient in need of such treatment, comprising administering to said patient an effective amount of at least one compound of claim 1, wherein said physiological disorder, symptom or disease is selected from the group consisting of: a respiratory disease, depression, anxiety, phobia, bipolar disorder, alcohol dependence, psychoactive substance abuse, nociception, psychosis, schizophrenia, stress related disorder, obsessive/compulsive disorder, bulemia, anorexia nervosa, binge eating, sleep disorder, mania, premenstrual syndrome, gastrointestinal disorder, obesity, headache, neuropathic pain, post-operative pain, chronic pain syndrome, bladder disorder, genitourinary disorder, cough, emesis and nausea.
- 22. A method for treating a physiological disorder, symptom or disease in a patient in need of such treatment, comprising administering to said patient an effective amount of at least one compound of claim 1, and an effective amount of at least one active ingredient selected from the group consisting of: other NK1 receptor antagonists, selective serotonin reuptake inhibitors, dopamine receptor agonists, serotonin 5-HT3 receptor antagonists, serotonin 5-HT2c receptor agonists, nociceptin receptor agonists, glucocorticoids and inhibitors of multidrug resistance protein 5, wherein said physiological disorder, symptom or disease is selected from the group consisting of: a respiratory disease, depression, anxiety, phobia, bipolar disorder, alcohol dependence, psychoactive substance abuse, nociception, psychosis, schizophrenia, stress related disorder, obsessive/compulsive disorder, bulemia, anorexia nervosa, binge eating, sleep disorder, mania, premenstrual syndrome, gastrointestinal disorder, obesity, headache, neuropathic pain, post-operative pain, chronic pain syndrome, bladder disorder, genitourinary disorder, cough, emesis and nausea.
- 23. A method of treating emesis and/or nausea in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound having the formula (I) in combination with an effective amount of at least one serotonin 5-HT3 receptor antagonist and/or at least one glucocorticoid.
- 24. The method of claim 23 wherein said serotonin 5-HT3 receptor antagonist is ondansetron and said glucocorticoid is dexamethasone.
- 25. The method of claim 21, wherein the physiological disorder, symptom or disease is emesis, depression, anxiety or cough.
- 26. The method of claim 25 wherein the physiological disorder, symptom or disease is depression or anxiety.
- 27. The method of claim 26, further comprising administering to the patient an effective amount of at least one anti-depressant agent and/or at least one anti-anxiety agent.
- 28. The method of claim 25 wherein depression is being treated and said method further comprises administering to the patient an effective amount of at least one selective serotonin reuptake inhibitor.
- 29. A method for antagonizing an effect of a Substance P at a neurokinin-1 receptor site or for blocking at least one neurokinin-1 receptor, in a patient in need of such treatment, comprising administering to said patient an effective amount of at least one compound of claim 1.
- 30. A kit comprising, in separate containers in a single package, pharmaceutical compositions for use in combination to treat an NK1 receptor mediated disease, wherein one container comprises a pharmaceutical composition comprising an effective amount of a compound of claim 1 in a pharmaceutically acceptable carrier, and wherein, a separate container comprises a pharmaceutical composition comprising another therapeutic agent in a pharmaceutically acceptable carrier, said-therapeutic agent being selected from the group consisting of: SSRIs, other types of NK1 receptor antagonists, prostanoids, H1 receptor antagonists, α-adrenergic receptor agonists, dopamine receptor agonists, melanocortin receptor agonists, endothelin receptor antagonists, endothelin converting enzyme inhibitors, angiotensin II receptor antagonists, angiotensin converting enzyme inhibitors, neutral metalloendopeptidase inhibitors, ETA antagonists, renin inhibitors, serotonin 5-HT3 receptor antagonists, serotonin 5-HT2c receptor agonists, nociceptin receptor agonists, glucocorticoids, rho kinase inhibitors, potassium channel modulators and inhibitors of multi-drug resistance protein 5.
- 31. A kit comprising, in separate containers in a single package, pharmaceutical compositions for use in combination to treat depression and/or anxiety, wherein one container comprises a pharmaceutical composition comprising an effective amount of a compound of claim 1 in a pharmaceutically acceptable carrier, and wherein, a separate container comprises a pharmaceutical composition comprising an antidepressant agent in a pharmaceutically acceptable carrier, and/or wherein a separate container comprises a pharmaceutical composition comprising an antianxiety agent in a pharmaceutically acceptable carrier.
- 32. A kit comprising, in separate containers in a single package, pharmaceutical compositions for use in combination to treat an NK1 receptor mediated disease, wherein one container comprises a pharmaceutical composition comprising an effective amount of a compound of claim 1 in a pharmaceutically acceptable carrier, and wherein, a separate container comprises a pharmaceutical composition comprising an SSRI in a pharmaceutically acceptable carrier.
- 33. A kit comprising, in separate containers in a single package, pharmaceutical compositions for use in combination to treat depression and/or anxiety, wherein one container comprises a pharmaceutical composition comprising an effective amount of a compound of claim 1 in a pharmaceutically acceptable carrier, and wherein, a separate container comprises a pharmaceutical composition comprising an SSRI in a pharmaceutically acceptable carrier.
- 34. A kit comprising, in separate containers in a single package, pharmaceutical compositions for use in combination to treat emesis and/or nausea, wherein one container comprises a pharmaceutical composition comprising an effective amount of a compound of claim 1 in a pharmaceutically acceptable carrier, and wherein, a separate container comprises a pharmaceutical composition comprising a serotonin 5-HT3 receptor antagonist in a pharmaceutically acceptable carrier, and/or wherein a separate container comprises a pharmaceutical composition comprising a glucocorticoid in a pharmaceutically acceptable carrier.
- 35. A kit comprising, in separate containers in a single package, pharmaceutical compositions for use in combination to treat emesis and/or nausea, wherein one container comprises a pharmaceutical composition comprising an effective amount of a compound of claim 1 in a pharmaceutically acceptable carrier, and wherein, a separate container comprises ondansetron, and/or wherein a separate container comprises dexamethasone.
REFERENCE TO RELATED APPLICATION
[0001] This application claims the benefit of U.S. Provisional Application Serial No. 60/393,708 filed Jul. 3, 2002, the disclosure of which is incorporated herein by reference thereto.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60393708 |
Jul 2002 |
US |