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Last Updated: September 19, 2021

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Claims for Patent: 8,691,847


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Summary for Patent: 8,691,847
Title:Benzamides and related inhibitors of factor Xa
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.
Inventor(s): Zhu; Bing-Yan (Palo Alto, CA), Zhang; Penglie (Foster City, CA), Wang; Lingyan (East Brunswick, NJ), Huang; Wenrong (Cupertino, CA), Goldman; Erick A. (Concord, CA), Li; Wenhao (Union City, CA), Zuckett; Jingmei (Bellevue, WA), Song; Yonghong (Foster City, CA), Scarborough; Robert M. (Half Moon Bay, CA)
Assignee: Millennium Pharmaceuticals, Inc. (Cambridge, MA)
Application Number:13/612,597
Patent Claims: 1. A compound of the formula: ##STR00599## wherein: R.sup.1a is H or --F; R.sup.1d1 is H or --OCH.sub.3; R.sup.1d3 is selected from the group consisting of H, --F, --Cl, --Br, --OCH.sub.3 and --OCF.sub.3; R.sup.1e is selected from the group consisting of H, --F, --Cl and --Br; and A-Q is selected from the group consisting of: ##STR00600## ##STR00601## ##STR00602## or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1, wherein A-Q is ##STR00603##

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 ##STR00604## 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: ##STR00605## 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.

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Serving leading biopharmaceutical companies globally:

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Harvard Business School
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Colorcon

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