Sildenafil n-oxide as prodrug

Details Sildenafil n-oxide as prodrug Sildenafil n-oxide as prodrug

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A61K 31/519 (2006.01) A61P 11/00 (2006.01) A61P 15/10 (2006.01)

Patent

CA 2690294

The invention concerns sildenafil N-oxide as prodrug, to pharmaceutical compositions containing this compound, to methods for preparing it, and methods for preparing compositions. The invention relates to 1-[[3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyra-zolo[4,3-d]pyrimidin-5-yl)- 4-ethoxyphenyl]sulfonyl]-4-methyl-4-oxido-piperazine having formula (1A) and pharmacologically acceptable salts, hydrates and solvates thereof. The invention also relates to uses of the compound, and compositions containing it, particularly for the manufacture of medicaments useful in the treatment of affections or diseases effectively treatable - albeit with side effects - with sildenafil.

L'invention porte sur le N-oxyde de sildénafil comme promédicament, sur des compositions pharmaceutiques contenant ce composé, sur ses procédés de préparation, et sur des procédés de préparation des compositions. L'invention porte sur la 1-[[3-(6,7-dihydro-1-méthyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-éthoxyphényl]sulfonyl]-4-méthyl-4-oxydo-pipérazine ayant la formule (1A) et sur ses sels, hydrates et solvates, pharmacologiquement acceptables. L'invention porte également sur des utilisations du composé, et sur des compositions le contenant, en particulier pour la fabrication de médicaments utiles dans le traitement d'affections ou de maladies apte à être traitées efficacement - bien qu'avec des effets secondaires - par le sildénafil.

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