Acylamino-substituted heteroaromatic compounds and their use...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 417/12 (2006.01) A61K 31/4184 (2006.01) A61K 31/422 (2006.01) A61K 31/425 (2006.01) A61K 31/4439 (2006.01) A61K 31/47 (2006.01) A61K 31/497 (2006.01) A61K 31/5377 (2006.01) A61P 9/00 (2006.01) C07D 215/00 (2006.01) C07D 215/38 (2006.01) C07D 235/30 (2006.01) C07D 263/54 (2006.01) C07D 263/58 (2006.01) C07D 277/82 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 403/12 (2006.01) C07D 409/12 (2006.01) C07D 413/12 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2494298

The present invention relates to acylamino-substituted heteroaromatic compounds of the formula (I), in which R1, R2, R3, R4 and R5 and X have the meanings indicated in the claims. The compounds of formula (I) are valuable pharmaceutically active compounds which are useful in the treatment of various disease states including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency. They upregulate the expression of the enzyme endothelial nitric oxide (NO) synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. 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 hétéroaromatiques acylamino-substitutués correspondant à la formule (I), dans laquelle R?1¿, R?2¿, R?3¿, R?4¿ et R?5¿ et X ont la teneur indiquée dans les revendications. Les composés de la formule (I) sont des composés pharmaceutiquement actifs d'une grande utilité, qui servent à traiter divers états pathologiques, y compris des troubles cardio-vasculaires tels que l'athérosclerose, la thrombose, la maladie d'artère coronarienne, l'hypertension et l'insuffisance cardiaque. Ils régulent vers le haut l'expression de l'enzyme de synthase endothéliale d'oxyde nitrique (NO) et peuvent s'utiliser dans des états lorsque l'on veut augmenter l'expression de cette enzyme ou normaliser le taux de NO qui s'était baissé. L'invention concerne en outre des processus de préparation des composés de la formule (I) et leur utilisation, notamment en tant qu'ingrédients actifs dans des préparations pharmaceutiques ainsi que des préparations pharmaceutiques les comprenant.

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