C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 401/06 (2006.01) A61K 31/4439 (2006.01) A61K 31/444 (2006.01) A61P 9/08 (2006.01) C07D 213/36 (2006.01) C07D 213/63 (2006.01) C07D 277/42 (2006.01) C07D 401/12 (2006.01) C07D 417/06 (2006.01)
Patent
CA 2611953
The present invention relates to N-alkylamides of the formula (I), in which A, Het, X, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial 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 further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.
La présente invention concerne des N-alkylamides provenant de la formule (I), dans laquelle A, Het, X, R1, R2 et R3 ont les significations indiquées dans les revendications, qui modulent la transcription de la synthase endothéliale d~oxyde nitrique (NO) et représentent des composés de valeur pharmacologiquement actifs. Plus spécifiquement, les composés de la formule (I) régulent à la hausse l~expression de l~enzyme de la synthase endothéliale d~oxyde nitrique et peuvent être appliqués lorsque l~on souhaite augmenter l~expression dudit enzyme, augmenter le niveau d~oxyde nitrique, ou normaliser le niveau décroissant d~oxyde nitrique. L~invention porte également sur les procédés de préparation de composés de la formule (I), sur les compositions pharmaceutiques les renfermant, et l~utilisation des composés de la formule (I) lors de la fabrication d~un médicament visant à stimuler l~expression de la synthase endothéliale d~oxyde nitrique ou lors du traitement de diverses maladies dont les troubles cardiovasculaires tels que l~athérosclérose, la thrombose, les maladies coronariennes, l~hypertension et l~insuffisance cardiaque, par exemple.
Strobel Hartmut
Will David William
Wohlfart Paulus
Zoller Gerhard
Bereskin & Parr Llp/s.e.n.c.r.l.,s.r.l.
Sanofi-Aventis
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