Cyclic oxyguanidine pyrazinones as protease inhibitors

Details Cyclic oxyguanidine pyrazinones as protease inhibitors Cyclic oxyguanidine pyrazinones as protease inhibitors

2006-04-18

2006-04-18

Wang, Shengjun (Department: 1617)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

C514S252100, C514S252110, C514S252120, C514S255050, C514S211070, C514S211010, C514S211150, C514S217060, C514S236500, C514S236800, C514S232200, C514S212080, C514S183000

Reexamination Certificate

active

07030110

ABSTRACT:
Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I:wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.

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