Cyclic oxyguanidine pyrazinones as protease inhibitors

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

C - Chemistry, Metallurgy

07

D

C07D 413/12 (2006.01) A61K 31/497 (2006.01) A61P 7/02 (2006.01) C07D 413/14 (2006.01)

Patent

CA 2415932

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 specidification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of protease, especially trypsin-like serine proteases, such as chymotripsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of trombin. Compositions for inhibiting loss of blood platelas, 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 labeled and employed fot in vivo imaging of thrombi.

L'invention concerne des composants de pyrazinones oxyguanidines cycliques comportant des composants de formule (I) : dans laquelle, R?3¿, R?4¿, R?5¿, W, et A sont comme suit dans la spécification, ainsi que des hydrates, des solvats ou encore des sels pharmaceutiquement acceptables de ceux-ci. Les composants de la présente invention sont des inhibiteurs efficaces de protéase, en particulier les protéases de sérine semblables à la trypsine, comme la chymotripsine, la trypsine, la thrombine, la plasmine et le factor Xa. Certains composants présentent une activité antithrombotique par une inhibition de thrombine directe et sélective. L'invention concerne des compositions d'inhibition de la perte de plaquette de sang, d'inhibition de formation d'agrégats de plaquettes de sang, d'inhibition de la formation de fibrine, d'inhibition de formation de thrombose et enfin d'inhibition de la formation d'embolie. L'invention concerne également des utilisations de composants comme anticoagulants, incorporés dans, ou liés physiquement à, des matériaux utilisés dans la fabrication d'instruments utilisés dans la collecte de sang, la circulation de sang, le stockage de sang, comme des cathéters, des machines de dialyse sanguine, des seringues ou des tubes de collecte de sang, des voies et des stents sanguins. De plus, les composants peuvent être étiquetés de manière détectable et utilisés avec cet étiquetage et également utilisés in vivo, afin de produire une image des thrombi.

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