IP Library Granted Patent US 8,003,803
Granted Patent B2
US 8,003,803 · App. 11/734,057 · Granted Aug 23, 2011

Fused ring thrombin receptor antagonists

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Quick Facts
Patent No.
US 8,003,803
App. No.
11/734,057
Granted
Aug 23, 2011
Kind
B2
Abstract

Fused-ring, heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein   represents an optional double bond, and wherein A n , E n , M n , G n , J n , R 3 , n 7 , R 8 , R 9 , R 10 , R 11 , R 32 , R 33 , X, Y, B and Het are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.

Claims (13)

1. A compound represented by structural formula:

or a pharmaceutically acceptable salt of said compound, wherein

B is —CR 12 ═CR 12a —, and R 12 and R 12a are independently selected from the group consisting of hydrogen, alkyl and halogen;

Het is a pyridyl group which is substituted by 1 to 4 moieties, W, wherein each W is independently selected from the group consisting of hydrogen; alkyl and R 21 -aryl;

R 1 and R 2 are independently selected from the group consisting of hydrogen, alkyl, fluoroalkyl, difluoroalkyl and trifluoroalkyl;

R 8 is H or alkyl;

R 10 and R 11 are independently selected from the group consisting of H and alkyl;

R 17 is H and alkyl; and

R 21 is 1 to 3 moieties and each R 21 is independently selected from the group consisting of hydrogen, —CN, —CF 3 , —OCF 3 , halogen, —NO 2 , alkyl, —OH, alkoxy, alkylamino-, di-(alkyl)amino- and C(O)(OR 17 )—.

2. A compound of claim 1 having the formula

or a pharmaceutically acceptable salt thereof.

3. A pharmaceutical composition comprising an effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier.

4. A compound of claim 1 wherein W is aryl or aryl substituted by halogen or —CN.

Assignments (3)
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →
CHANGE OF NAME Recorded Aug 30, 2012
From: SCHERING CORPORATION
To: MERCK SHARP & DOHME CORP.
Reel/Frame 028884/0151 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 10, 2007
From: XIA, YAN; CHELLIAH, MARIAPPAN V.; CHACKALAMANNIL, SAMUEL
To: SCHERING CORPORATION
Reel/Frame 019276/0136 →