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US 6,835,739 B2Granted
Benzamides and related inhibitors of factor Xa
AssigneeMillennium Pharmaceuticals, Inc.
InventorsBing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
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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.
Claims11
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.
5 more elements
Dependencies are inferred from the claim text.