Trypsin-like serine protease inhibitors, their preparation and use as selective inhibitors of coagulation factors IIa and Xa

摘要

A compound having the following formula ** Formula ** or a pharmaceutically acceptable salt thereof; where: n is an integer from 1 to 2 inclusive; m is an integer from 0 to 2 inclusive; X is selected from the group consisting of CH or N; R1 is selected from the group consisting of -CH2NH2, and R2 is selected from the group consisting of -H, -OH, -NH2, and acetyl; R3 is selected from the group consisting of -H, benzyloxycarbonyl, and benzylsulfonyl; and R4 is selected from the group consisting of -OH, where p is an integer from 0 to 2 inclusive, Y is selected from the group consisting of -O-, -S-, -S ( = O) -, -SO2-, methylene, -CH (OH) -, -CH (NH2) -, -CH (CH2-OH) -, -CH (CH2-NH2) - or -N (R6) -, R5 is selected from the group consisting of -H or a simple (C1-C3) alkyl and R6 is selected from the group consisting of -H; a simple (C1-C3) alkyl or a simple (C1-C3) acyl.