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 401/08 (2006.01) C07D 401/14 (2006.01) C07D 409/14 (2006.01) C07D 417/06 (2006.01)
Patent
CA 2612601
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 de formule (I), où A, Het, X, R1, R2 et R3 ont les significations indiquées dans les revendications. Ces composés modulent la transcription de l~oxyde citrique (NO) synthase endothéliale et sont des composés pharmacologiquement actifs d~une grande utilité. En particulier, les composés de formule régulent de manière positive l~expression de l~enzyme NO synthase endothéliale et peuvent être appliqués dans des conditions visant une expression accrue de ladite enzyme, un taux accru de NO ou la normalisation d~un taux réduit de NO. Cette invention concerne également des procédés de préparation de composés de formule I, des compositions pharmaceutiques comprenant ces derniers et l~utilisation de composés de formule I pour la fabrication d~un médicament destiné à stimuler l~expression de la NO synthase endothéliale ou à traiter diverses maladies, y compris les affections cardiovasculaires telles 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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