abstract |
(57) Abstract: Compounds of formula (VII) and hydrates, solvates or pharmaceutically acceptable salts thereof have been described wherein Het, R 1 , R 7 and A are As described herein, they inhibit proteolytic enzymes (eg, thrombin). Methods for preparing such compounds have also been described. The compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases such as chymotrypsin, trypsin, thrombin, plastin and factor Xa. Some of these compounds show potent antithrombotic activity by direct selective thrombin inhibition. The present invention includes a composition that inhibits blood platelet loss, inhibits blood platelet clump formation, inhibits fibrin formation, inhibits thrombus formation, and inhibits emboli formation, It contains a compound of the present invention in a pharmaceutically acceptable carrier. |