Heterocyclic keto arginine peptides as thrombin inhibitors

Details Heterocyclic keto arginine peptides as thrombin inhibitors Heterocyclic keto arginine peptides as thrombin inhibitors

C - Chemistry, Metallurgy

07

K

C07K 5/065 (2006.01) A61K 31/445 (2006.01) A61K 31/55 (2006.01) A61K 38/05 (2006.01) A61K 38/06 (2006.01) A61K 38/58 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 417/12 (2006.01) C07K 5/087 (2006.01) C07K 14/815 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2208773

This invention relates to new and useful inhibitors of the enzyme thrombin of the formula (I): AS - X, and more particularly compound (1) in the preparation, and pharmaceutical compositions. 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 coagulopathis associated with coronary bypass operations as well as restenotic events following transluminal angioplasty.

Cette invention se rapporte à de nouveaux inhibiteurs utiles de l'enzyme thrombine de la formule (I) et plus particulièrement à un composé utilisé dans leur préparation, et à des compositions pharmaceutiques. L'invention se rapporte également à l'utilisation de ces composés et compositions in vitro comme anticoagulants et in vivo comme agents s'appliquant au traitement et à la prophylaxie de troubles thrombotiques, tels que la thrombose veineuse, l'embolie pulmonaire et la thrombose artérielle donnant lieu à des accidents ischémiques aigus, tels que l'infarctus du myocarde ou l'infarctus cérébral. De plus, ces composés et compositions sont thérapeutiquement utiles dans la prévention et le traitement de la coagulopathie associée aux interventions de pontage coronarien ainsi qu'à des incidents relatifs à la resténose après une angioplastie transluminale.

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