ANTITHROMBOTIC AMIDINOPHENYLALANINE AND AMIDINOPYRIDYLALANINE DERIVATIVES

摘要

Compounds of formula (I), pharmaceutically acceptable salt thereof, and pharmaceutically acceptable solvates of either entity, wherein X is CH or N; Y is optionally monounsaturated C3-C5 alkylene optionally substituted with C1-C4 alkyl or methylene; R<1> is H; C1-C4 alkyl optionally substituted with C1-C4 alkoxy, OH, NR<5>R<6>, CONR<5>R<6>, C3-C6 cycloalkyl or aryl; or C3-C6 alkenyl; R<2> is H; C1-C4 alkyl optionally substituted with C1-C4 alkoxy, OH, NR<5>R<6>, CONR<5>R<6>, C3-C6 cycloalkyl or aryl; or CONR<5>R<6>; R<3> and R<4> are each independently selected from H; C1-C4 alkyl optionally substituted with NR<5>R<6>; C1-C4 alkoxy; halo; CONR<5>R<6> and aryl; R<5> and R<6> are each independently selected from H and C1-C4 alkyl; and m and n are each independently 1, 2 or 3; are potent and selective thrombin inhibitors useful in the treatment of, inter alia, deep vein thrombosis; reocclusion following thrombolytic therapy; chronic arterial obstruction; peripheral vascular disease; acute myocardial infarction; unstable angina; atrial fibrillation; thrombotic stroke; transient ischaemic attacks; restenosis and occlusion following angioplasty; or neurodegenerative disorders.