Patent
Lactam tachykinin receptor antagonists
| العنوان: | Lactam tachykinin receptor antagonists |
|---|---|
| Patent Number: | 7,196,113 |
| تاريخ النشر: | March 27, 2007 |
| Appl. No: | 11/135240 |
| Application Filed: | May 23, 2005 |
| مستخلص: | The present invention is directed to certain lactam compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety. |
| Inventors: | Finke, Paul E. (Miltown, NJ, US); Meurer, Laura C. (Scotch Plains, NJ, US); Mills, Sander G. (Scotch Plains, NJ, US) |
| Assignees: | Merck & Co., Inc. (Rahway, NJ, US) |
| Claim: | 1. A compound of the formula I: [chemical expression included] wherein: R 1 is selected from the group consisting of: (1) hydrogen, and (2) C 1-6 alkyl; R 2 is selected from the group consisting of: (1) hydrogen, (2) —OH, (3) —NH 2 , (4) —NH(C 1-6 alkyl), and (5) —N(C 1-6 alkyl)(C 1-6 alkyl); R 3 is selected from the group consisting of: (1) hydrogen, and (2) C 1-6 alkyl; R 4 is selected from the group consisting of: (1) hydrogen, and (2) C 1-6 alkyl; and pharmaceutically acceptable salts thereof and individual enantiomers and diastereomers thereof. |
| Claim: | 2. The compound of claim 1 of the formula Ia: [chemical expression included] and pharmaceutically acceptable salts thereof and individual enantiomers and diastereomers thereof. |
| Claim: | 3. The compound of claim 1 wherein R 1 is selected from the group consisting of: (1) hydrogen, and (2) methyl. |
| Claim: | 4. The compound of claim 1 wherein R 2 is selected from the group consisting of: (1) hydrogen, (2) —OH, and (3) —NH 2 . |
| Claim: | 5. The compound of claim 1 wherein R 3 is selected from the group consisting of: (1) hydrogen, and (2) methyl. |
| Claim: | 6. The compound of claim 1 wherein: R 1 is hydrogen; R 2 is selected from the group consisting of: (1) hydrogen, (2) —OH, and (3) —NH 2 ; R 3 is selected from the group consisting of: (1) hydrogen, and (2) methyl; and R 4 is hydrogen. |
| Claim: | 7. A compound which is selected from the group consisting of: [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] or a pharmaceutically acceptable salts thereof. |
| Claim: | 8. A pharmaceutical composition which comprises an inert carrier and a compound of claim 1 or a pharmaceutically acceptable salt thereof. |
| Claim: | 9. A compound which is [chemical expression included] |
| Claim: | 10. A method for the treatment of emesis in a mammal in need thereof which comprises the administration of a therapeutically effective amount of a compound according to claim 1 . |
| Claim: | 11. A method for the treatment of urinary incontinence in a mammal in need thereof which comprises the administration of a therapeutically effective amount of a compound according to claim 1 . |
| Claim: | 12. A method for the treatment of depression in a mammal in need thereof which comprises the administration of a therapeutically effective amount of a compound according to claim 1 . |
| Claim: | 13. A method for the treatment of anxiety in a mammal in need thereof which comprises the administration of a therapeutically effective amount of a compound according to claim 1 . |
| Claim: | 14. A method for the treatment of emesis in a mammal in need thereof which comprises the administration of a therapeutically effective amount of a compound according to claim 9 . |
| Claim: | 15. A method for the treatment of urinary incontinence in a mammal in need thereof which comprises the administration of a therapeutically effective amount of a compound according to claim 9 . |
| Claim: | 16. A method for the treatment of depression in a mammal in need thereof which comprises the administration of a therapeutically effective amount of a compound according to claim 9 . |
| Claim: | 17. A method for the treatment of anxiety in a mammal in need thereof which comprises the administration of a therapeutically effective amount of a compound according to claim 9 . |
| Claim: | 18. A pharmaceutical composition which comprises an inert carrier and a compound of claim 9 or a pharmaceutically acceptable salt thereof. |
| Current U.S. Class: | 514/424 |
| Patent References Cited: | 5387595 February 1995 Mills et al. 5750549 May 1998 Caldwell et al. 5877191 March 1999 Caldwell et al. 2002/0042431 April 2002 Finke et al. WO 97/14671 April 1997 |
| Assistant Examiner: | Nolan, Jason M. |
| Primary Examiner: | McKane, Joseph K. |
| Attorney, Agent or Firm: | Yuro, Raynard Rose, David L. Thies, J. Eric |
| رقم الانضمام: | edspgr.07196113 |
| قاعدة البيانات: | USPTO Patent Grants |
| الوصف غير متاح. |