abstract |
The present invention provides a method for making and using a compound of formula (I) or a pharmaceutically acceptable salt thereof; wherein n is an integer of 1 or more and 2 or less; m is 0 or more and 2 or less. 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 (Formula (II)); R 2 is —H, —OH , -NH 2 and is selected from the group consisting of acetyl; is R 3, -H, is selected from the group consisting of benzyloxycarbonyl and benzyl sulfonyl; R 4 is, -OH, (formula (III), (IV), (V), (VI)), wherein p is an integer of 0 or more and 2 or less, and Y is -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) - from is selected from the group consisting, R 5 is, -H or simple (C 1 -C 3 Is selected from the group consisting of alkyl, R 6 is, -H, a simple (C 1 ~C 3) alkyl or a simple (C 1 ~C 3) is selected from the group consisting of acyl. These compounds selectively inhibit thrombin and prothrombinase selectively and as a result are useful as anticoagulants. |