IP Library Granted Patent US 7,105,533
Granted Patent B2
US 7,105,533 · App. 10/527,044 · Granted Sep 12, 2006

Fused heterobicyclo substituted phenyl metabotropic glutamate-5 modulators

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Quick Facts
Patent No.
US 7,105,533
App. No.
10/527,044
Granted
Sep 12, 2006
Kind
B2
Abstract

Phenyl compounds substituted with a fused-heterobicyclo moiety, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, and panic, as well as in the treatment of pain and other diseases.

Claims (14)

1. A compound represented by Formula (I):

or a pharmaceutically acceptable salt thereof, wherein X 1 , X 2 , X 4 , and X 6 are independently C, N, S or O; X 3 is C; and X 5 is N; wherein at most one of X 1 , X 2 , X 4 , and X 6 is S or O; Y is heteroaryl; R 1 and R 2 are independently halogen, C 0-4 alkyl, or pyridyl; and n 1 and n 2 are independently 0 or 1.

2. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein X 1 , X 2 , X 3 , X 4 , and X 6 are C.

3. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein one of X 2 and X 4 is N, the other is C; and X 1 and X 6 are C.

4. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein X 2 and X 4 are N, and X 1 and X 6 are C.

5. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein one of X 2 and X 4 is N, the other is C; X 1 is S; and X 6 is C.

6. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein one of X 2 and X 4 is N, the other is C; X 1 is S; and X 6 is N.

7. A compound represented by

or a pharmaceutically acceptable salt thereof.

8. A pharmaceutical composition comprising: a therapeutically effective amount of the compound according to claim 1 , or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier.

9. A method of treatment of pain comprising the step of administering a therapeutically effective amount of the compound according to claim 1 or a pharmaceutically acceptable salt thereof.

10. A method of treatment of a pain disorder wherein said pain disorder is acute pain, persistent pain, chronic pain, inflammatory pain, or neuropathic pain, comprising the step of administering a therapeutically effective amount of the compound according to claim 1 or a pharmaceutically acceptable salt thereof.

11. A method of treatment of neuropathic pain comprising the step of administering a therapeutically effective amount of the compound according to claim 1 or a pharmaceutically acceptable salt thereof.

12. A method of treatment of inflammatory pain comprising the step of administering a therapeutically effective amount of the compound according to claim 1 or a pharmaceutically acceptable salt thereof.

Assignments (2)
CHANGE OF NAME Recorded Jan 28, 2010
From: MERCK & CO., INC.
To: MERCK SHARP & DOHME CORP.
Reel/Frame 023861/0349 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 8, 2005
From: CAMPBELL, BRIAN THOMAS; GUZNER, JANET LORRAINE; MUNOZ, BENITO; STEARNS, BRIAN ANDREW; VERNIER, JEAN-MICHEL ANDRE; WANG, BOWEI
To: MERCK & CO., INC.
Reel/Frame 016752/0286 →