Novel carboxamides for use as xa inhibitors

摘要

N-substituted 4-heterocyclyl-benzamide derivatives (I), their tautomers, enantiomers, diastereomers (and mixtures) and salts are new. N-substituted 4-heterocyclyl-benzamide derivatives of formula (I), their tautomers, enantiomers, diastereomers (and mixtures) and salts are new. A= heterocyclic group; R 1>= hydrogen, fluoro, chloro, bromo, 1-3C alkyl (optionally (per)fluorinated), 2-3C alkenyl or alkynyl, nitro, amino, 1-3C alkoxy or mono-, di- or tri-fluoromethoxy; R 2>= hydrogen, chloro, bromo or 1-3C alkyl; R 3>= hydrogen or a substituent; R 4>= hydrogen or 1-3C alkyl, or R 3> and R 4> together complete 3-7C cycloalkyl in which one methylene may be replaced by imino, 1-3C alkylimino, acylimino or sulfonylimino; R 5>= hydrogen or 1-3C alkyl; B'= fused heterocyclic group of formulae (Bi), (Bii) and (Biii); n= 1 or 2; R 7>= hydrogen, 1-3C alkyl (optionally substituted by carboxy or 1-3C alkoxycarbonyl), hydroxy, 1-5C alkoxycarbonyl, amino or 1-3C alkylamino; R 8>= hydrogen, fluoro, chloro, bromo, iodo, 1-3C alkyl (optionally (per)fluorinated), 2-3C alkenyl or alkynyl, hydroxy, 1-3C alkoxy, trifluoromethoxy, amino, nitro or cyano. The full definitions are given in the DEFINITIONS (Full Definitions) Field. [Image] [Image] ACTIVITY : Thrombolytic; Anticoagulant; Antiulcer; Cerebroprotective; Cardiant; Cytostatic; Antiarthritic; Antirheumatic. No biological data is given. MECHANISM OF ACTION : (I) are inhibitors of factor Xa and/or related serine proteases (e.g. thrombin, urokinase, factors VIIa, IXa, XIa and XIIa).