IP Library Granted Patent US 8,691,847
Granted Patent B2
US 8,691,847 · App. 13/612,597 · Granted Apr 8, 2014

Benzamides and related inhibitors of factor Xa

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Quick Facts
Patent No.
US 8,691,847
App. No.
13/612,597
Granted
Apr 8, 2014
Kind
B2
Abstract

Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.

Claims (20)

1. A compound of the formula:

wherein:

R 1a is H or —F;

R 1d1 is H or —OCH 3 ;

R 1d3 is selected from the group consisting of H, —F, —Cl, —Br, —OCH 3 and —OCF 3 ;

R 1e is selected from the group consisting of H, —F, —Cl and —Br; and

A-Q is selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 , wherein A-Q is

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

4. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 2 .

5. A method for preventing or treating a condition in a mammal in need thereof characterized by undesired thrombosis comprising administering to said mammal a therapeutically effective amount of a compound of claim 1 .

6. A method for preventing or treating a condition in a mammal in need thereof characterized by undesired thrombosis comprising administering to said mammal a therapeutically effective amount of a compound of claim 2 .

7. A compound of the formula

or a pharmaceutically acceptable salt thereof.

8. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 7 .

9. A method for preventing or treating a condition in a mammal in need thereof characterized by undesired thrombosis comprising administering to said mammal a therapeutically effective amount of a compound of claim 7 .

10. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of the formula:

or a pharmaceutically acceptable salt thereof.

11. A method for preventing or treating a condition in a mammal in need thereof characterized by undesired thrombosis comprising administering to said mammal the pharmaceutical composition of claim 10 .

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 19, 2012
From: ZHU, BING-YAN; ZHANG, PENGLIE; WANG, LINGYAN; HUANG, WENRONG; GOLDMAN, ERICK A.; LI, WENHAO; ZUCKETT, JINGMEI; SONG, YONGHONG; SCARBOROUGH, ROBERT M.
To: COR THERAPEUTICS, INC.
Reel/Frame 029503/0020 →
MERGER Recorded Dec 19, 2012
From: COR THERAPEUTICS, INC.
To: MILLENNIUM PHARMACEUTICALS, INC.
Reel/Frame 029504/0084 →