Claims
- 1. A compound having the formula (I)
- 2. The compound or salt according to claim 1, where X1 is —O—.
- 3. The compound or salt according to claim 1, where Ar1 and Ar2 are each
- 4. The compound or salt according to claim 3, where for Ar2, at least two of R8, R9 and R10 are each —CF3.
- 5. The compound or salt according to claim 3, where for Ar1 , R8, R9 and R10 are each independently selected from the group consisting of H, —OH and halogen.
- 6. The compound or salt according to claim 1, where X2 is —C— and Y is O.
- 7. The compound or salt according to claim 1, where one of R4 and R5 is H, and the other one of R4 and R5 is —C(R28R29)n1-G, where n, is 0 or 1, and R28, R29 and G are each defined in claim 1.
- 8. The compound or salt according to claim 7, where one of R4 and R5 is H, and the other one of R4 and R5 is H, —CH3, —NHCOR12 or
- 9. The compound or salt according to claim 1, where R4 and R5, together with one another and the carbon to which they are both attached, form a 4- to 7-membered ring containing from 0 to 3 heteroatoms that are each independently selected from the group consisting of —O—, —S—, —S(O)—, —SO2— and —NR18—, the ring being optionally substituted with from 1 to 2 substituents that are each independently selected from the group consisting of R30 and R3′, where R18, R30 and R31 are each defined in claim 1.
- 10. The compound or salt according to claim 9, where R4 and R5, together with one another and the carbon to which they are both attached, form a chemically feasible 4- to 7-membered ring selected from the group consisting of:
- 11. The compound or salt according to claim 1, where:
R1 and R2 are each independently defined in claim 1;X1 is defined in claim 1;R3 is H; Ar1 and Ar2, independently of one another, are each 118where R8, R9 and R10, independently of one another, are each H, —OH, —CF3 or halogen; R1 and R7 are each H; R4 and R5, independently of one another, are each defined in claim 1;X2 is —C—; Y is O; and R18 is H or —P(O)(OH)2.
- 12. The compound according to claim 11, where X1 is —O— or —NR18a —, n2 is 1 or 2, and R4 and R5 are each independently —C(R28R29)n1-G, where n1, R28, R29 and G are each defined in claim 1.
- 13. The compound according to claim 11, where X1 is —O— or —NR18a—, n2 is 1 or 2, and R4 and R5, together with one another and the carbon to which they are both attached, form a 4- to 7-membered ring selected from the group consisting of:
- 14. The compound or salt according to claim 1, wherein the compound is selected from the group consisting of:
- 15. A pharmaceutical composition comprising at least one compound or salt according to claim 1 and a pharmaceutical carrier or excipient therefor.
- 16. The pharmaceutical composition according to claim 15, further comprising at least one selective serotonin reuptake inhibitor.
- 17. The pharmaceutical composition according to claim 15, further comprising at least one serotonin 5-HT3 receptor antagonist.
- 18. A method of treating emesis, nausea, depression, anxiety or cough comprising administering an effective amount of at least one compound of claim 1 to a patient in need of such treatment.
- 19. The method according to claim 18 for treating depression or anxiety, further comprising administering to the patient an effective amount of at least one selective serotonin reuptake inhibitor.
- 20. The method according to claim 19, where the selective serotonin reuptake inhibitor is fluoxetine, fluvoxamine, paroxetine, sertaline, or a pharmaceutically-acceptable salt thereof.
- 21. The method according to claim 18 for treating emesis, further comprising administering to the patient an effective amount of at least one serotonin 5-HT3 receptor antagonist.
- 22. The method according to claim 21, where the serotonin 5-HT3 receptor antagonist is palonsetron, ondansetron, granisetron or a pharmaceutically-acceptable salt thereof.
- 23. 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 mammal in need of such treatment, comprising administering to the mammal an effective amount of at least one compound or salt according to claim 1, or a pharmaceutical composition thereof.
- 24. A method of treating a respiratory disease, inflammatory disease, skin disorder, ophthalmalogical disorder, phobia, bipolar disorder, alcohol dependence, psychoactive substance abuse, epilepsy, nociception, psychosis, schizophrenia, Alzheimer's disease, AIDs related dementia, Towne's disease, stress related disorder, obsessive/compulsive disorder, bulemia, anorexia nervosa, binge eating, mania, premenstrual syndrome, gastrointestinal disorder, atherosclerosis, fibrosing disorder, obesity, Type II diabetes, headache, neuropathic pain, post-operative pain, chronic pain syndrome, bladder disorder or genitourinary disorder comprising administering to the mammal an effective amount of at least one compound or salt according to claim 1, or a pharmaceutical composition thereof.
CROSS REFERENCE TO RELATED APPLICATIONS
[0001] This application claims the benefit of U.S. Provisional Application No. 60/337,652, filed Nov. 13, 2001.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60337652 |
Nov 2001 |
US |