Malonamide and malonamic ester derivatives with...

C - Chemistry – Metallurgy – 07 – C

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C07C 257/18 (2006.01) A61K 31/155 (2006.01) A61K 31/167 (2006.01) A61K 31/225 (2006.01) A61K 31/27 (2006.01) A61P 7/02 (2006.01) C07C 257/20 (2006.01)

Patent

CA 2423857

The present invention relates to compounds of formula (I), in which R1, R2 and B have the meanings indicated in the claims. The compounds of formula (I) are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of thromboembolic diseases and restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of formula (I), their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

L'invention concerne des composés représentés par la formule (I), dans laquelle R<1>, R<2>, A et B ont les notations indiquées dans les revendications. Les composés représentés par la formule (I) constituent des composés pharmacologiquement actifs intéressants. Ils possèdent une forte action antithrombotique et conviennent, par exemple, dans le traitement et la prévention de maladies thrombo-emboliques et de resténoses. Ils constituent des inhibiteurs réversibles du facteur enzymatique VIIa de coagulation sanguine, et peuvent généralement être appliqués en cas d'activité indésirable du facteur VIIa, ou lorsqu'une inhibition du facteur VIIa est requise à des fins de prévention ou de traitement. L'invention se réfère en outre trait à des procédés utiles à la préparation des composés représentés par la formule (I), à l'utilisation de ceux-ci, notamment comme principe actif de produits pharmaceutiques, et à des préparations pharmaceutiques contenant ceux-ci.

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