Coagulation Factor Xa inhibitor, useful for treatment, prophylaxis or diagnosis of thromboembolic disease, comprising acylated 3- or 4-amidino-benzylamine derivative

摘要

A novel coagulation Factor Xa inhibitor comprises an acylated 3- or 4-amidino-benzylamine derivative (I). A novel coagulation Factor Xa inhibitor comprises an acylated 3- or 4-amidino-benzylamine derivative of formula (I). X = CH or N; R1 = H, 1-8C alkyl or -(CH2)nOH; n = 1-5; R2 = H or 1-8C alkyl; R3 = 1-8C alkyl or -(CH2)n-OR6; R4 = SO2R', COR', COOR' or H; R5 = H, OH, COR or COOR; R, R6 = 1-16C alkyl or (all optionally substituted) aryl, heteroaryl, aralkyl or heteroaralkyl; R' = as R; or an adamantyl or camphor residue; the amidino group is in the 3- or 4-position.