Acylated arylcycloalkylamines and their use as pharmaceuticals

C - Chemistry – Metallurgy – 07 – C

Patent

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Details

C07C 233/58 (2006.01) A61K 31/166 (2006.01) A61P 9/00 (2006.01) C07C 233/65 (2006.01) C07C 237/38 (2006.01) C07C 311/21 (2006.01) C07D 209/08 (2006.01) C07D 213/82 (2006.01) C07D 215/54 (2006.01) C07D 231/14 (2006.01) C07D 235/08 (2006.01) C07D 241/24 (2006.01) C07D 263/34 (2006.01) C07D 277/56 (2006.01) C07D 295/14 (2006.01) C07D 295/155 (2006.01) C07D 333/38 (2006.01) C07D 401/04 (2006.01) C07D 409/04 (2006.01)

Patent

CA 2494628

The present invention relates to acylated arylcycloalkylamines of the formula I, in which R1, R2 and n have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically 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 arylcycloalkylamines acylées de formule I, dans laquelle R?1¿, R?2¿ et n sont tels que décrits dans les revendications. Les composés de formule I constituent des composés actifs pharmacologiquement précieux qui sont utiles dans le traitement de différentes pathologies, notamment, de troubles cardiovasculaires tels que l'athérosclérose, la thrombose, la maladie coronarienne, l'hypertension et l'insuffisance cardiaque. Lesdits composés régulent positivement l'expression de l'enzyme oxyde nitrique (NO) synthase endothéliale et peuvent être utilisés pour des pathologies dans lesquelles une expression accrue de ladite enzyme ou un niveau de NO accru ou la normalisation d'un niveau de NO abaissé est souhaitée. L'invention concerne également des procédés de préparation de composés de formule I, leur utilisation, notamment en tant que principes actifs dans des agents pharmaceutiques, ainsi que des préparations pharmaceutiques les comprenant.

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