C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 417/12 (2006.01) A61K 31/381 (2006.01) A61K 31/4178 (2006.01) A61K 31/4184 (2006.01) A61K 31/427 (2006.01) A61K 31/435 (2006.01) A61K 31/4436 (2006.01) A61K 31/4439 (2006.01) A61K 31/444 (2006.01) A61K 31/506 (2006.01) A61K 31/5377 (2006.01) A61P 9/00 (2006.01) C07D 215/02 (2006.01) C07D 215/58 (2006.01) C07D 221/04 (2006.01) C07D 235/02 (2006.01) C07D 333/78 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07D 407/12 (2006.01) C07D 409/12 (2006.01) C07D 409/14 (2006.01) C07
Patent
CA 2494302
The present invention relates to acylated, heteroaryl-condensed cycloalkenylamines of the formula I, (I) in which A, R1, R2, R3, R4, R5 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.
L'invention concerne des cycloalcénylamines acylées et héteroaryle-condensées de formule I, (I) dans laquelle A, R?1¿, R?2¿, R?3¿, R?4¿, R?5¿ et n ont les significations présentées dans les revendications. Les composés de formule I sont des composés actifs ayant une valeur pharmacologique et sont utiles pour le traitement de divers états pathologiques notamment des troubles cardio-vasculaires, tels que l'athérosclérose, la thrombose, une maladie coronarienne, l'hypertension et l'insuffisance cardiaque. Ces composés régulent positivement l'expression de la synthase de l'oxyde nitrique (NO) endothéliale d'une enzyme et peuvent être appliqués pour des états dans lesquels une expression accrue de ladite enzyme ou un niveau accru de NO ou la normalisation d'un niveau diminué de NO est recherché. L'invention concerne également des procédés de préparation des composés de formule I, l'utilisation de ceux-ci notamment comme ingrédients actifs dans des produits pharmaceutiques et des préparations pharmaceutiques renfermant ceux-ci.
Strobel Hartmut
Wohlfart Paulus
Aventis Pharma Deutschland Gmbh
Bereskin & Parr Llp/s.e.n.c.r.l.,s.r.l.
Sanofi-Aventis Deutschland Gmbh
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