| abstract |
The invention provides methods of making and using compounds of the formula: n nor 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; R 1 is selected from the group consisting of —CH 2 NH 2 , andn n nR 2 is selected from the group consisting of —H, —OH, —NH 2 and acetyl; R 3 is selected from the group consisting of —H, benzyloxycarbonyl and benzylsulfonyl; and R 4 is selected from the group consisting of —OH,n n nwherein p is an integer between 0 and 2 inclusively, Y is selected from the group consisting of —O—, —S—, —S(═O)—, —SO 2 —, methylene, —CH(OH)—, —CH(NH 2 )—, —CH(CH 2 —OH)—, —CH(CH 2 —NH 2 )— or —N(R 6 )—, R 5 is selected from the group consisting of —H or a simple (C 1 -C 3 ) alkyl and R 6 is selected from the group consisting of —H, a simple (C 1 -C 3 ) alkyl or a simple (C 1 -C 3 ) acyl. These compounds are useful as anticoagulant agents as a result of their selective dual inhibition of thrombin and prothrombinase. |