MX9708278A - Antithrombotic amidinotetrahydropyridylalanine derivatives. - Google Patents

Abstract

Compounds of formula (I), pharmaceutically acceptable salts thereof, and pharmaceutically acceptable solvates of either entity, wherein Y is optionally monounsaturated C3-C5 alkylene optionally substituted with C1-C4 alkyl or methylene; R1 is H; C1-C4 alkyl optionally substituded with C1-C4 alkoxy, OH, NR5R6, CONR5R6, C3-C6 cycloalkyl or aryl; or C3-C6 alkenyl; R2 is H; C1-C4 alkyl optionally substituted with C1-C4 alkoxy, OH, NR5R6, CONR5R6, C3-C6 cycloalkyl or aryl; or CONR5R6; R3 and R4 are each independently selected from H; C1-C4 alkyl optionally substituded with NR5R6; C1-C4 alkoxy; halo; CONR5R6 and aryl; aryl is phenyl optionally substituted with one, two or three substituents independently selected from C1-C4 alkyl, C1-C4 alkoxy, OH, halo and CF3; R5 and R6 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.