IP Library Granted Patent US 6,995,163
Granted Patent B2
US 6,995,163 · App. 10/903,059 · Granted Feb 7, 2006

Tricyclic fused heterocyclic compound, process for preparing it and medicament comprising it

Assignee: Eisai Co., Ltd.
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Quick Facts
Patent No.
US 6,995,163
App. No.
10/903,059
Granted
Feb 7, 2006
Kind
B2
Abstract

The present invention provides a novel compound having an excellent corticotrophin-releasing-factor receptor antagonistic activity. That is, it provides a compound represented by the following formula, a pharmacologically acceptable salt thereof or hydrates thereof, wherein R 2 is a hydrogen atom, etc.; R 3 is a hydrogen atom, etc.; M′ represents a hydrogen atom, a halogen atom or a C 1-6 alkyl group; R 7 ′ represents a hydrogen atom or a C 1-6 alkyl group; and W′ represents a phenyl group, pyridyl group, thienyl group, or furyl group, each being optionally substituted; and a pharmacologically acceptable salt thereof or hydrates thereof.

Claims (35)

1. A compound represented by the formula:

wherein

R 2 is a hydrogen atom, a C 1-6 alkyl group, a C 2-6 alkenyl group, a C 2-6 alkynyl group, a C 1-6 alkoxy group, a C 3-8 cycloalkyl group, a C 1-6 alkoxy C 1-6 alkyl group, a C 3-8 cycloalkyl C 1-6 alkyl group or a C 1-6 alkyl-aryl group;

R 3 is

(i) a hydrogen atom;

(ii) formula —COR 4 (wherein R 4 represents a C 1-6 alkyl group, an optionally substituted aryl C 1-4 alkyl group, an optionally substituted aryl group, an optionally substituted heteroaryl C 1-4 alkyl group or an optionally substituted heteroaryl group);

(iii) —S(O) n R 5 (wherein R 5 represents a C 1-6 alkyl group, an optionally substituted aryl C 1-4 alkyl group, an optionally substituted aryl group, an optionally substituted heteroaryl C 1-4 alkyl group or an optionally substituted heteroaryl group; and n is an integer of 0, 1 or 2);

(iv) a C 1-10 alkyl group optionally substituted with any of one or more groups defined in the following A group;

(v) a C 2-10 alkenyl group optionally substituted with any of one or more groups defined in the following A group;

(vi) a C 2-10 alkynyl group optionally substituted with any of one or more groups defined in the following A group;

(vii) an optionally substituted aryl group; or

(viii) a C 3-8 cycloalkyl group optionally fused with optionally substituted benzene ring and optionally substituted with a C 1-4 alkyl group;

the A group defined above is selected from at least one of the group consisting of:

(1) halogen atom,

(2) hydroxy group,

(3) nitro group,

(4) cyano group,

(5) carboxy group,

(6) a C 1-6 alkyloxycarbonyl group, and

(7) a group represented by the formula —S(O) r R 15 (wherein r is an integer of 0, 1 or 2; and R 15 represents:

(i) hydrogen atom;

(ii) a C 1-6 alkyl group;

(iii) a group represented by the formula —NR 16 R 17 (wherein R 16 and R 17 are the same as or different from each other and each represents hydrogen atom, a C 1-6 alkyl group optionally substituted with an optionally substituted aryl group, a C 1-4 alkylacyl group, an optionally substituted aryl C 1-4 alkyl group, an optionally substituted heteroaryl C 1-4 alkyl group, an optionally substituted aryl group or an optionally substituted heteroaryl group);

(iv) an optionally substituted aryl C 1-4 alkyl group;

(v) an optionally substituted aryl group;

(vi) an optionally substituted heteroaryl C 1-4 alkyl group; or

(vii) an optionally substituted heteroaryl group);

M′ represents a hydrogen atom, a halogen atom or a C 1-6 alkyl group;

R 7 ′ represents a hydrogen atom or a C 1-6 alkyl group; and

W′ represents a phenyl group, pyridyl group, thienyl group, or furyl group, each being optionally substituted; and

a pharmacologically acceptable salt thereof or hydrates thereof.

2. The compound of claim 1 , a pharmacologically acceptable salt thereof or hydrates thereof, wherein at least one selected from R 2 and R 3 are the same as or different from each other and each represents hydrogen atom, a C 1-6 alkyl group, a C 2-6 alkynyl group, a C 1-6 alkoxy C 1-6 alkyl group or a C 1-6 alkyl-aryl group.

3. A medicament which comprises the compound of claim 1 , a pharmacologically acceptable salt thereof or hydrates thereof, and a pharmacologically acceptable carrier.

4. A method for treating a disease to which at least one of CRF and CRF receptor relate, by administering a pharmaceutically effective dose of the compound of claim 1 , a pharmacologically acceptable salt thereof or hydrates thereof to a patient.

5. A method for treating a disease against which CRF receptor antagonism is efficacious, by administering a pharmaceutically effective dose of the compound of claim 1 , a pharmacologically acceptable salt thereof or hydrates thereof to a patient.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 29, 2007
From: EISAI CO., LTD.
To: EISAI R&D MANAGEMENT CO., LTD.
Reel/Frame 019501/0049 →
Priority Claims (1)
JP 11-352553 · Dec 13, 1999 · national
Continuity (2)
Division 1014883600
Related Publication 20050004147A1 · Jan 6, 2005