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US 2002/0058813 A1Published application
Spiro-indolines as Y5 receptor antagonists
AssigneesMerck & Co., Inc., Banyu Pharmaceutical Co., Ltd.
InventorsYing-Duo Gao, Douglas J. Macneil, Lihu Yang, Nancy R. Morin, Takehiro Fukami, Akio Kanatani, Takahiro Fukuroda, Yasuyuki Ishii, Masaki Ihara
Life of this patent
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Abstract
Compounds of general structural formula I such as that shown in structural formula II 1 are selective NPY Y5 receptor antagonists, useful in the treatment of obesity and the complications associated therewith.
Claims25
A compound of structural formula I:
- 153
- or a pharmaceutically acceptable salt thereof, wherein;
- V, W, X and Z are independently selected from CH and N;
- R1 is H, C1-3 alkyl, C1-3 alkoxy, F, or Cl;
- R2 is S(O)n R6, COR6 or CHO, wherein
- n is 0, 1 or 2;
- and
- R6 is N(R3)2 or C1-3 alkyl;
- R3 is independently H or C1-3 alkyl;
- Ar is aryl or heteroaryl;
- R4 and R5 are independently selected from:
- (1) hydrogen,
- (2) aryl, either unsubstituted or substituted with
- (a) halo
- (b) C1-3 alkoxy,
- (c) —N(C1-3 alkyl)2,
- (d) C2-4 alkanoyl, or
- (e) aryl;
- (3) nitro,
- (4) C1-5 alkyl,
- (5) C1-5 alkoxy,
- (6) hydroxy-C1-3 alkyl,
- (7) carboxy,
- (8) halo,
- (9) C1-5 alkylthio,
- (10) C1-5 alkoxycarbonyl,
- (11) pyridylcarbonyl,
- (12) benzoyl,
- (13) phenyl-C1-3alkoxy,
- (14) pyridyl, either unsubstituted or substituted with
- C1-3 alkyl or C1-3 alkoxy,
- (15) C3-6 cycloalkyl,
- (16) oxazolyl,
- (17) thiazolyl,
- (18) triazolyl,
- (19) phenoxy or
- (20) C2-6 alkanoyl.
34 more elements
A pharmaceutical composition which comprises a pharmaceutically acceptable carrier and an effective amount of a selective Y5 antagonist.
Dependencies are inferred from the claim text.