N-Oxides of venlafaxine and O-Desmethylvenlafaxine as prodrugs

摘要

The invention concerns venlafexine-N-oxide and O-desmethylvenlafaxine-N-oxide as prodrugs of venlafexine 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 venlafexine.