Triaza- and tetraaza-anthracenedione derivatives, their...

C - Chemistry – Metallurgy – 07 – D

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C07D 471/14 (2006.01) A61K 31/519 (2006.01) A61P 9/00 (2006.01) C07D 487/04 (2006.01)

Patent

CA 2523196

The present invention relates to triaza- and tetraaza-anthracenedione derivatives of the formula (I), in which A, B and R1 to R5 have the meanings indicated in the claims. The compounds of formula (I) are valuable pharmacologically active compounds. They 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 a trait à des dérivés de triaza- and tétraaza-anthracènedione de formule (I), dans laquelle : A, B et R?1¿ à R?5¿ sont tels que définis dans les revendications. Les composés de formule (I) sont des composés actifs pharmaceutiquement utiles. Ils sont utiles dans le traitement de diverses maladies comprenant les troubles cardio-vasculaires tels que l'athérosclérose, la thrombose, la maladie de l'artère coronaire, l'hypertension et l'insuffisance cardiaque. Ils assurent la régulation positive de l'expression de l'enzyme de la monoxyde d'azote synthase endothéliale et peuvent être utilisés dans des conditions dans lesquelles une expression accrue de ladite enzyme ou une niveau accru de monoxyde d'azote ou la normalisation d'un niveau réduit de monoxyde d'azote est souhaitable. L'invention a également trait à des procédés de préparation de composés de formule (I), leur utilisation, notamment en tant que principes actifs dans des produits pharmaceutiques, et des préparations pharmaceutiques les comprenant.

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