| abstract |
The invention provides methods of making and using compounds of the formula (I) 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 (Formula (II)); R2 is selected from the group consisting of -H, -OH, -NH2 and acetyl; R3 is selected from the group consisting of -H, benzyloxycarbonyl and benzyisulfonyl;and R4 is selected from the group consisting of -OH, (Formulae (III), (IV), (V), (VI)), wherein p is an integer between 0 and 2 inclusively, Y is selected from the group consisting of -0-, -S-, -S(=0)-, -S02-, 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. |