Low molecular weight bicyclic thrombin inhibitors

Details Low molecular weight bicyclic thrombin inhibitors Low molecular weight bicyclic thrombin inhibitors

C - Chemistry, Metallurgy

07

D

C07D 513/04 (2006.01) A61K 31/435 (2006.01) A61K 31/495 (2006.01) A61K 31/53 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) C07D 471/04 (2006.01) C07D 487/04 (2006.01) C07D 498/04 (2006.01) C07K 5/00 (2006.01) C07K 5/02 (2006.01) C07K 5/065 (2006.01) C07K 5/078 (2006.01) C07K 5/087 (2006.01) C07K 5/097 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2208772

This invention relates to the discovery of heterocyclic competitive inhibitors of the enzyme thrombin having formula (I), their preparation, and pharmaceutical compositions thereof. As well, this invention relates to the use of such compounds and compositions in vitro as anticoagulants and in vivo as agents for the treatment and prophylaxis of thrombotic disorders such as venous thrombosis, pulmonary embolism and arterial thrombosis resulting in acute ischemic events such as myocardial infarction or cerebral infarction. Moreover, these compounds and compositions have therapeutic utility for the prevention and treatment of coagulopathies associated with coronary bypass operations as well as restenotic events following transluminal angioplasty.

L'invention a pour objet la découverte d' inhibiteurs compétitifs hétérocycliques de l'enzyme thrombine, ayant la formule (I); leur préparation, et les compositions pharmaceutiques de ces derniers. De même, l'invention traite de l'utilisation de ces composés et de ces compositions in vitro comme anticoagulants et in vivo comme agents pour le traitement et la prophylaxie des troubles thrombotiques tels que la thrombose veineuse, l'embolisme pulmonaire et la thrombose artérielle provenant de cas d'ischémie aigüe tels que l'infarctus du myocarde ou l'infarctus cérébral. De plus, ces composés et ses compositions présentent une utilité thérapeutique pour la prévention et le traitement des coagulopathies associées au pontage coronarien, ainsi qu'aux cas de resténose suivant les actes d'angioplastie transluminale.

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