N-oxides of venlafaxine and o-desmethylvenlafaxine as prodrugs

Details N-oxides of venlafaxine and o-desmethylvenlafaxine as prodrugs N-oxides of venlafaxine and o-desmethylvenlafaxine as prodrugs

C - Chemistry, Metallurgy

07

C

C07C 291/04 (2006.01) A61K 31/135 (2006.01) A61P 25/24 (2006.01)

Patent

CA 2699961

The invention concerns venlafaxine-N-oxide and O-desmethylvenlafaxine-N-oxide as prodrugs of venlafaxine and its major (active) metabolite O-desmethylvenlafaxine respectively, to pharmaceutical compositions containing these N-oxides, to methods for preparing them, and methods for preparing compositions. The invention relates to N-oxide, having formula (1), wherein R1 is H or CH3, and tautomers, stereoisomers, hydrates and solvates thereof. The invention also relates to the uses of the N-oxides and compositions, particularly for the manufacture of medicaments useful in the treatment of affections or diseases effectively treatable - albeit with side effects - with venlafaxine.

L'invention porte sur le N-oxyde de venlafaxine et sur le N-oxyde de O-desméthylvenlafaxine comme promédicaments de respectivement venlafaxine et son O-desméthylvenlafaxine métabolite majeur (actif), sur des compositions pharmaceutiques contenant ces N-oxydes, sur leurs procédés de préparation, et sur des procédés de préparation des compositions. L'invention porte sur le N-oxyde, ayant la formule (1), dans laquelle R1 représente H ou CH3, et ses tautomères, stéréoisomères, hydrates et solvates. L'invention porte également sur les utilisations des N-oxydes et des compositions, en particulier pour la fabrication de médicaments utiles dans le traitement d'affections ou de maladies aptes à être traitées efficacement - bien qu'avec des effets secondaires - par la venlafaxine.

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