ANTITHROMBOTIC DERIVATIVES OF AMIDINOPHENYLALANINE AND AMIDINOPYRIDYLALANINE.

摘要

THE COMPOUNDS OF FORMULA (I), THE PHARMACEUTICALLY ACCEPTABLE SALT OF THE SAME AND THE PHARMACEUTICALLY ACCEPTABLE SOLVATES OF EITHER OF THE TWO, WHERE X IS CH O N; AND IT IS ALKYLENE C {SUB, 3} -C {SUB, 5} OPTIONALLY MONOINSATURATED OPTIONALLY SUBSTITUTED FOR ALKYL C {SUB, 1} -C {SUB, 4} OR METHYLENE; R {SUP, 1} ES H; ALKYL C {SUB, 1} -C {SUB, 4} OPTIONALLY REPLACED BY ALCOXY C {SUB, 1} -C {SUB, 4}, OH, NR {SUP, 5} R {SUP, 6}, CONR {SUP , 5} R {SUP, 6}, CYCLLOALKYL C {SUB, 3} -C {SUB, 6} OR ARYL; OR ALKYNYL C {SUB, 3} -C {SUB, 6}; R {SUP, 2} ES H; ALKYL C {SUB, 1} C {SUB, 4} OPTIONALLY REPLACED BY ALCOXI C {SUB, 1} -C {SUB, 4}, OH, NR {SUP, 5} R {SUP, 6}, CONR {SUP, 5} R {SUP, 6}, CYCLLOALKYL C {SUB, 3} -C {SUB, 6} OR ARYL; OR CONR {SUP, 5} R {SUP, 6}; R {SUP, 3} AND R {SUP, 4} ARE SELECTED EACH ONE, INDEPENDENTLY, FROM H; ALKYL C {SUB, 1} -C {SUB, 4} OPTIONALLY REPLACED BY NR {SUP, 5} R {SUP, 6}; ALCOXI C {SUB, 1} -C {SUB, 4}; HALO; CONR {SUP, 5} R {SUP, 6} AND ARILO; R {SUP, 5} AND R {SUP, 6} ARE SELECTED EACH ONE, INDEPENDENTLY, FROM H AND ALKYLOC {SUB, 1} -C {SUB, 4}; AND M AND N ARE EACH ONE, INDEPENDENTLY, 1, 2 OR 3; THEY ARE POWERFUL AND SELECTIVE INHIBITORS OF THROMBINE USEFUL IN THE TREATMENT OF, AMONG OTHERS, DEEP VENOUS THROMBOSIS; REOCLUSION AFTER A THROMBOLYTIC THERAPY; CHRONIC ARTERIAL OBSTRUCTION; PERIPHERAL VASCULAR DISEASE; ACUTE Myocardial infarction; UNSTABLE ANGINA; HEADPHONE FIBRILLATION; THROMBOTIC ATTACK; PASSENGER ISCHEMIC ATTACKS; RESTENOSIS AND OCCLUSION AFTER AN ANGIOPLASTY; OR NEURODEGENERATIVE DISORDERS.