トリプシン様セリンプロテアーゼ阻害剤、その調製、ならびに凝固因子ＩＩａおよびＸａの選択的阻害剤としての使用

摘要

The invention provides methods of making and using compounds of the formula: or a pharmaceutically acceptable salt thereof; wherein n is an integer between 1 and 2 inclusively; m is an integer between 0 and 2 inclusively; 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, wherein p is an integer between 0 and 2 inclusively, 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. These compounds are useful as anticoagulant agents as a result of their selective dual inhibition of thrombin and prothrombinase.