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):	Zhu; Bing-Yan (Belmont, CA), Zhang; Penglie (Foster City, CA), Wang; Lingyan (East Brunswick, NJ), Huang; Wenrong (Cupertino, CA), Goldman; Erick A. (Berkeley, CA), Li; Wenhao (South San Francisco, 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:	10/687,334
Patent Claims:	1. A compound having the formula: ##STR607## wherein: A-Q is a member selected from the group consisting of: ##STR608## R.sup.1a is a member selected from the group of H, F, Cl and Br; R.sup.1e is a member selected from the group consisting of --H, --F, --Cl, --Br, --OMe, --OH, --Me, --CF.sub.3 and --CH.sub.2 NH.sub.2 ; R.sup.1d1, R.sup.1d2 and R.sup.1d4 are each H; R.sup.1d3 is selected from the group consisting of: H, --Me, --F, --Cl, --Br, aryl, heteroaryl, --NH.sub.2, --NMe.sub.2, --NHMe, --NHSO.sub.2 NMe, --NHCOMe, --CF.sub.3, --OH, --OCH.sub.3, --SCH.sub.3, --OCF.sub.3, --OCH.sub.2 F, --OCHF.sub.2,--OCH.sub.2 CF.sub.3, --OCF.sub.2 CF.sub.3, --NO.sub.2, --CN, --CO.sub.2 H, --CO.sub.2 Me, --CO.sub.2 Et, --CONH.sub.2, --CONHMe, --CONMe.sub.2, --SO.sub.2 NH.sub.2, --SO.sub.2 CH.sub.3, --SO.sub.2 NMe.sub.2, --CH.sub.2 OH, --CH.sub.2 NH.sub.2, --CH.sub.2 NHMe, --CH.sub.2 NMe.sub.2, --OCH.sub.2 CO.sub.2 H, --OCH.sub.2 CO.sub.2 Me, --OCH.sub.2 CO.sub.2 Et, --OCH.sub.2 CONH.sub.2, --OCH.sub.2 CONMe.sub.2, --OCH.sub.2 CONHMe, --OCH.sub.2 CH.sub.2 OMe, --OCH.sub.2 CH.sub.2 OEt, --OCH.sub.2 CH.sub.2 NH.sub.2, --OCH.sub.2 CH.sub.2 NHMe, --OCH.sub.2 CH.sub.2 NMe.sub.2, --NHCH.sub.2 CH.sub.2 OMe, --SCH.sub.2 CH.sub.2 OMe, --SO.sub.2 CH.sub.2 CH.sub.2 OMe, --OCH.sub.2 CH.sub.2 SO.sub.2 Me, --NHCH.sub.2 CH.sub.2 NHMe, --NHCH.sub.2 CH.sub.2 NMe.sub.2, --N(CH.sub.2 CH.sub.2 OH).sub.2, --N(CH.sub.2 CH.sub.2 OMe).sub.2, --NHCH.sub.2 CO.sub.2 H, --NHCH.sub.2 CO.sub.2 Et, --NHCH.sub.2 CO.sub.2 Et, --NHCH.sub.2 CONH.sub.2, --NHCH.sub.2 CONMe.sub.2, --NHCH.sub.2 CONHMe, --N(CH.sub.3)CH.sub.2 CO.sub.2 H, --N(CH.sub.3)CH.sub.2 CO.sub.2 Et, --(NMe)CH.sub.2 COOH, --N(Me)CH.sub.2 CONH.sub.2, --N(Me)CH.sub.2 CH.sub.2 NMe2, --N(Me)CH.sub.2 CH.sub.2 OMe, --NHCH.sub.2 CH.sub.2 OMe, ##STR609## ##STR610## ##STR611## 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: ##STR612## ##STR613## 3. A compound of claim 1 having a structure selected from the group consisting of: ##STR614## ##STR615## 4. A compound claim 1 having a structure selected from the group consisting of: ##STR616## 5. A compound of claim 1 having the formula: ##STR617## wherein: R.sup.1a is a member selected from the group of H, F, Cl and Br; R.sup.1d1, R.sup.1d2, R.sup.1d3 and R.sup.1d4 are each H; R.sup.1e 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: ##STR618## 7. A compound of claim 1: wherein: A-Q is a member selected from the group of: ##STR619## R.sup.1a is a member selected from the group of H, F, Cl and Br; R.sup.1d1, R.sup.1d2, R.sup.1d3, and R.sup.1d4 are each H; R.sup.1e 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: ##STR620## 9. A compound of claim 8 having a structure selected from the group consisting of: ##STR621## 10. A compound of claim 7 having a structure selected from the group consisting of: ##STR622## ##STR623## 11. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 1.