Chlorothiophene-amides as inhibitors of coagulation factors...

C - Chemistry – Metallurgy – 07 – D

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C07D 333/38 (2006.01) A61K 31/381 (2006.01) A61P 9/10 (2006.01)

Patent

CA 2714654

The present invention relates to compounds of the formula I wherein R1; R2; R3; R4; R5, R13, R16, X and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and thrombin and can in general be applied in conditions in which an undesired activity of factor Xa and/or thrombin are present or for the cure or prevention of which an inhibition of factor Xa and thrombin are intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

La présente invention concerne des composés de formule (I) dans laquelle R1, R2, R3, R4, R5, R13, R16, X et M ont la signification indiquée dans les revendications. Les composés de formule (I) sont des composés actifs d'une valeur pharmacologique certaine. Ils présentent un puissant effet antithrombotique et conviennent, par exemple, pour le traitement et la prophylaxie de troubles cardiovasculaires tels que les maladies thrombo-emboliques ou les resténoses. Ce sont des inhibiteurs réversibles du facteur Xa (FXa) et de la thrombine, enzymes de la coagulation sanguine, et peuvent être utilisés en général dans des pathologies dans lesquelles une activité indésirable du facteur Xa et/ou de la thrombine est présente ou pour le traitement ou la prévention desquelles une inhibition du facteur Xa et/ou de la thrombine est envisagée. L'invention concerne en outre des méthodes de préparation des composés de formule (I), leur utilisation, en particulier comme constituants actifs de produits pharmaceutiques, et des préparations pharmaceutiques contenant ces composés.

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