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

Inventors: Bing-Yan Zhu (Palo Alto, CA); Penglie Zhang (Foster City, CA); Lingyan Wang (East Brunswick, NJ); Wenrong Huang (Cupertino, CA); Erick A. Goldman (Concord, CA); Wenhao Li (Union City, CA); Jingmei Zuckett (Bellevue, WA); Yonghong Song (Foster City, CA); Robert M. Scarborough (Half Moon Bay, CA)
Assignee: Millennium Pharmaceuticals, Inc.
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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 →
Continuity (11)
Continuation 13247937 · Sep 28, 2011
Continuation 12756037 · Apr 7, 2010
Continuation 11924480 · Oct 25, 2007
Continuation 11442060 · May 26, 2006
Continuation 10942733 · Sep 15, 2004
Continuation 10687334 · Oct 15, 2003
Continuation 10126976 · Apr 22, 2002
Continuation 09794225 · Feb 28, 2001
Continuation In Part 09663420 · Sep 15, 2000
Provisional Application 60185746 · Feb 29, 2000
Related Publication 20130172310A1 · Jul 4, 2013