Amidine inhibitors of serine proteases

Details Amidine inhibitors of serine proteases Amidine inhibitors of serine proteases

C - Chemistry, Metallurgy

07

D

C07D 207/16 (2006.01) A61K 31/40 (2006.01) A61K 31/401 (2006.01) A61K 31/4025 (2006.01) A61P 7/02 (2006.01) C07D 207/48 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01)

Patent

CA 2421548

Inhibitors of serine proteases are provided having formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein. In particular, the compounds bind to factor VIIa, tissue factor/factor Xa complex, thrombin, trypsin, plasmin and kallikrein and have anticoagulant activity. Pharmaceutical compositions comprising the compounds are useful for inhibiting the formation of veinous and/or arterial thrombi in vivo.

L'invention concerne des inhibiteurs des sérines protéases, correspondant à la formule (I) dans laquelle X, R¿1?, R¿2?, R¿3?, R¿4? et R¿5? possèdent les notations données dans la description. Ces composés se lient notamment au complexe facteur VIIA, facteur tissulaire/facteur Xa, à la thrombine, à la trypsine, à la plasmine et à la kallikréine, et ils possèdent une activité anticoagulante. L'invention concerne également des compositions pharmaceutiques qui comprennent ces composés et sont utiles pour inhiber la formation in vivo de thrombus veineux et/ou artériels.

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