IP Library Granted Patent US 7,273,871
Granted Patent B2
US 7,273,871 · App. 10/483,872 · Granted Sep 25, 2007

Phenyl-5,6,6A,7,8,9-hexahydro-4H-1,4,9-triaza-phenalene derivatives as CRF antagonists

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Quick Facts
Patent No.
US 7,273,871
App. No.
10/483,872
Granted
Sep 25, 2007
Kind
B2
Abstract

The present invention relates to tricyclic pyridines compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof:

Claims (14)

1. A compound according to formula (I), and stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof

wherein

R is phenyl which may be substituted by 1 to 4 substituents independently selected from the group consisting of:

halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, C1-C6 mono or dialkylamino, nitro, cyano and a group R 5 ; and

R 5 is C3-C7 cycloalkyl, which may contain one or more double bonds; aryl; or a 5-6 membered heterocycle;

wherein each of the above groups R 5 may be substituted by one or more groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, C1-C6 mono or dialkylamino, nitro, and cyano.

2. A compound, according to claim 1 , wherein

R is selected from: 2,4-dichiorophenyl, 2-chloro-4-methylphenyl, 2-chloro-4-trifluoromethylphenyl, 2-chloro-4-methoxyphenyl, 2,4,5-trimethyiphenyl, 2,4-dimethyl-phenyl, 2-methyl-4-methoxyphenyl, 2-methyl-4-chlorophenyl, 2-methyl-4-trifluoromethyiphenyl, 2,4-dimethoxyphenyl, 2-methoxy-4-trifluoromethylphenyl, 2-methoxy-4-chlorophenyl, 3-methoxy-4-chlorophenyl, 2,5-dimethoxy-4-chlorophenyl, 2-methoxy-4-isopropylphenyl, 2-methoxy-4-trifluoromethylphenyl, 2-methoxy-4-isopropyiphenyl, 2-methoxy-4-methylphenyl, 2-trifluoromethyl-4-chlorophenyl, 2,4-trifluoromethyiphenyl, 2-trifluoromethyl-4-methylphenyl, 2-trifluoromethyl-4-methoxy-phenyl, 2-bromo-4-isopropylphenyl, 2-methyl-4-cyanophenyl, 2-chloro-4-cyanophenyl, 4-methyl-6-dimethylaminopyridin-3-yl, 4-dimethylamino-6-methyl-pyridin-3-yl, 6-dimethylamino-pyridin-3-yl and 4-dimethylamino-pyridin-3-yl.

3. A compound, according to claim 1 , selected from the group consisting of:

9-(2,4-dimethyl-phenyl)-2-methyl-4-(1-propyl-butyl)-5,6,6a,7,8,9-hexahydro-4H-1,4,9-triaza-phenalene; and

9-(4-methoxy-2-methyl-phenyl)-2-methyl-4-(1-propyl-butyl)-5,6,6a,7,8,9-hexahydro-4H-1,4,9-triaza-phenalene.

4. A pharmaceutical composition comprising a compound according to claim 1 in admixture with one or more physiologically acceptable carriers or excipients.

5. A method for the treatment of, comprising administration of an effective amount of a compound according to claim 1 , to a mammal in need of treatment thereof.

6. A method for the treatment of anxiety, comprising administration of an effective amount of a compound according to claim 1 , to a mammal in need of treatment thereof.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 21, 2008
From: SB PHARMCO PUERTO RICO INC.
To: SMITHKLINE BEECHAM (CORK) LIMITED
Reel/Frame 021411/0785 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 29, 2004
From: REGAN, COLLIN; SCHWAEBE, MICHAEL
To: NEUROCRINE BIOSCIENCES INC.
Reel/Frame 014923/0360 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 29, 2004
From: DI FABIO, ROMANO; MICHELI, FABRIZIO; ST-DENIS, YVES
To: SB PHARMCO PUERTO RICO INC.
Reel/Frame 015022/0610 →