N-OXIDES OF VENLAFAXINE AND O-DESMETHYLVENLAFAXINE AS PRODRUGS

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 compositi...

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Bibliographische Detailangaben
Hauptverfasser:	TULP, MARTINUS TH.M, TURSKI, LECHOSLAW A, STOIT, AXEL, KRUSE, CORNELIS G, VADER, SANDER
Format:	Patent
Sprache:	eng ; fre ; ger
Schlagworte:	ACYCLIC OR CARBOCYCLIC COMPOUNDS CHEMISTRY HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Beschreibung
Zusammenfassung:	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.