Pyrazinone protease inhibitors

Details Pyrazinone protease inhibitors Pyrazinone protease inhibitors

C - Chemistry, Metallurgy

07

K

C07K 5/078 (2006.01) A61K 38/05 (2006.01) G01N 33/68 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2334679

Pyrazinone compounds are described, including compounds of Formula (I), wherein X is O, NR11 or CH=N, R3-R11, Ra, Rb, Rc, W, m and n are 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.

La présente invention concerne des composés de pyrazinone, y compris des composés de formule (I), et leurs hydrates, solvates ou sels, acceptables sur le plan pharmaceutique. Dans cette formule, X est un O, un NR?11¿ ou un CH=N, et les R?3¿-R?11¿, R?a¿, R?b¿, R?c¿, W, m et n sont décrits dans les spécifications. Les composés de l'invention sont de puissants inhibiteurs de protéases, plus spécialement de sérine protéases de type trypsine, telles que la chymotrypsine, la trypsine, la thrombine, la plasmine et le facteur Xa. Certains de ces composés montrent une activité antithrombique via une inhibition directe et sélective de la thrombine. La présente invention concerne aussi des compositions destinées à inhiber la perte de plaquettes sanguines, la formation d'agrégats de plaquettes sanguines, la formation de fibrine, la formation de thrombus et d'embolus. On peut aussi utiliser les composés de l'invention comme anticoagulants, insérés dans, ou physiquement liés à, des dispositifs de prise de sang, pour la circulation sanguine et le stockage du sang, tel que des cathéters, des machines à dialyser le sang, des seringues et tubes à prise de sang, des extenseurs et des sondes. De plus, les composés peuvent être marqués de manière détectable et employés pour l'imagerie de thrombi in vivo.

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