Protease inhibitors

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C - Chemistry, Metallurgy

07

D

C07D 235/18 (2006.01) A61K 31/40 (2006.01) A61K 31/415 (2006.01) A61K 31/425 (2006.01) A61K 31/44 (2006.01) A61K 31/66 (2006.01) A61P 7/02 (2006.01) C07D 209/12 (2006.01) C07D 209/18 (2006.01) C07D 235/20 (2006.01) C07D 401/10 (2006.01) C07D 401/12 (2006.01) C07D 403/10 (2006.01) C07D 403/12 (2006.01) C07D 405/04 (2006.01) C07D 405/10 (2006.01) C07D 405/12 (2006.01) C07D 407/10 (2006.01) C07D 407/12 (2006.01) C07D 409/10 (2006.01) C07D 409/12 (2006.01) C07D 413/10 (2006.01) C07D 417/10 (2006.01) C07D 417/12

Patent

CA 2355249

The present invention provides novel compounds of the Formula (I): A-B, its prodrug forms, or pharmaceutically acceptable salts thereof, wherein A represents a saturated, unsaturated, or a partially unsaturated bicyclic heterocyclic ring structure, and B represents an aryl or a heteroaryl group. Preferred compounds of the present invention comprise a benzimidazole or indole nucleus. The compounds of this invention are inhibitors of serine proteases, Urokinase (uPA), Factor Xa (FXa), and/or Factor VIIa (FVIIa), and have utility as anti cancer agents and/or as anticoagulants for the treatment or prevention of thromboembolic disorders in mammals.

La présente invention concerne de nouveaux composés de formule (I), A-B, ainsi que leurs promédicaments ou leurs sels pharmaceutiquement acceptables, où A représente une structure à noyau hétérocyclique, bicyclique saturée, non saturée ou partiellement non saturée, et où B représente un groupe aryle ou hétéroaryle. Les composés préférés de l'invention comportent un noyau de benzimidazole ou d'indol. Les composés de cette invention sont des inhibiteurs des sérine protéases, de l'urokinase (uPA), du facteur Xa et/ou du facteur VIIa (FVIIa), et conviennent en tant qu'agents anticancéreux et/ou en tant qu'anticoagulants destinés à la prophylaxie ou à la thérapie d'affections thromboemboliques chez les mammifères.

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