Claims for Patent: 6,835,739

Summary for Patent: 6,835,739

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):	Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
Assignee:	Millennium Pharmaceuticals Inc
Application Number:	US10/687,334
Patent Claims:	1. A compound having the formula: wherein: A-Q is a member selected from the group consisting of: R1a is a member selected from the group of H, F, Cl and Br; R1e is a member selected from the group consisting of —H, —F, —Cl, —Br, —OMe, —OH, —Me, —CF3 and —CH2NH2; R1d1, R1d2 and R1d4 are each H; R1d3 is selected from the group consisting of: H, —Me, —F, —Cl, —Br, aryl, heteroaryl, —NH2, —NMe2, —NHMe, —NHSO2NMe, —NHCOMe, —CF3, —OH, —OCH3, —SCH3, —OCF3, —OCH2F, —OCHF2,—OCH2CF3, —OCF2CF3, —NO2, —CN, —CO2H, —CO2Me, —CO2Et, —CONH2, —CONHMe, —CONMe2, —SO2NH2, —SO2CH3, —SO2NMe2, —CH2OH, —CH2NH2, —CH2NHMe, —CH2NMe2, —OCH2CO2H, —OCH2CO2Me, —OCH2CO2Et, —OCH2CONH2, —OCH2CONMe2, —OCH2CONHMe, —OCH2CH2OMe, —OCH2CH2OEt, —OCH2CH2NH2, —OCH2CH2NHMe, —OCH2CH2NMe2, —NHCH2CH2OMe, —SCH2CH2OMe, —SO2CH2CH2OMe, —OCH2CH2SO2Me, —NHCH2CH2NHMe, —NHCH2CH2NMe2, —N(CH2CH2OH)2, —N(CH2CH2OMe)2, —NHCH2CO2H, —NHCH2CO2Et, —NHCH2CO2Et, —NHCH2CONH2, —NHCH2CONMe2, —NHCH2CONHMe, —N(CH3)CH2CO2H, —N(CH3)CH2CO2Et, —(NMe)CH2COOH, —N(Me)CH2CONH2, —N(Me)CH2CH2NMe2, —N(Me)CH2CH2OMe, —NHCH2CH2OMe, and all pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives thereof. 2. A compound of claim 1 structure selected from the group consisting of: 3. A compound of claim 1 having a structure selected from the group consisting of: 4. A compound claim 1 having a structure selected from the group consisting of: 5. A compound of claim 1 having the formula: wherein: R1a is a member selected from the group of H, F, Cl and Br; R1d1, R1d2, R1d3 and R1d4 are each H; R1e is a member selected from the group of F, Cl, Br, OH, Me and OMe; and all pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives thereof. 6. A compound of claim 5 having a structure selected from the group consisting of: 7. A compound of claim 1: wherein: A-Q is a member selected from the group of: R1a is a member selected from the group of H, F, Cl and Br; R1d1, R1d2, R1d3, and R1d4 are each H; R1e is a member selected from the group of F, Cl, Br, OH, Me and OMe; and all pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives thereof. 8. A compound of claim 7, wherein A-Q is: 9. A compound of claim 8 having a structure selected from the group consisting of: 10. A compound of claim 7 having a structure selected from the group consisting of: 11. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 1.