| abstract |
The present invention provides methods of making and using a compound of formula (I) or a pharmaceutically acceptable salt thereof; wherein n is an integer between 1 and 2, inclusive; m is between 0 and 2 is an integer, including 0 and 2; X is selected from the group consisting of CH or N; R 1 is selected from the group consisting of -CH 2 NH 2 and (chemical formula (II)); R 2 is selected from the group consisting of The term consists of: -H, -OH, -NH2 and acetyl; R3 is selected from the group consisting of -H, benzyloxycarbonyl and benzylsulfonyl; and R4 is selected from the following The group consisting of: -OH, (chemical formula (III), (IV), (V), (VI)), where p is an integer between 0 and 2, inclusive, 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 -H or simple (C 1 -C 3 )alkyl and R 6 is selected from the group consisting of -H, simple (C 1 -C 3 )alkyl or simple (C 1 -C 3 )acyl. These compounds are useful as anticoagulants due to their selective dual inhibition of thrombin and prothrombinase. |