Derivatives of 14.15-dihydro 20.21-dinoreburnamenin-14-ol,...

C - Chemistry – Metallurgy – 07 – D

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Details

C07D 461/00 (2006.01) A61K 31/437 (2006.01) A61P 25/18 (2006.01) A61P 25/24 (2006.01)

Patent

CA 2563491

The invention relates to novel derivatives of 14,15-dihydro 20,21 dinoreburnamenin-14-ol, having formula (I), in which R represents a radical -AR', wherein A represents a heteroatom and R' represents a group selected from the group comprising alkyl radicals at C¿1?-C¿6?, alkenyls at C¿1?-C¿6?, alkynyls at C¿1?-C¿6?, aralkyls; esters having formula -R¿1?-CO-O-R¿2?; amides having formula -R¿3?-CO-NZY, wherein Y and Z together can form a cycloalkyl radical or a heterocyclic radical, optionally substituted by one or more alkyl radicals; a radical selected from the group comprising alkyl radicals, alkenyls or alkynyls, substituted by at least one amine having formula -NZY; or one of the pharmaceutically-acceptable salts thereof, including the isomers, enantiomers and diastereoisomers thereof and mixtures of same. The invention also relates to the use of said novel derivatives for the preparation of a pharmaceutical composition which is intended, in particular, for the treatment and/or prevention of depression, sleep/wake cycle disorders and symptomatic frontal disorders in cognitive components among humans.

L'invention a pour objet de nouveaux dérivés du 14,15-dihydro 20,21 dinoréburnaméninl4-ol, de formule (I) dans laquelle R représente un radical - AR', dans lequel A représente un hétéroatome et R' représente un groupement choisi dans le groupe constitué par les radicaux alkyles en C1-C6, alcényles en C1-C6, alcynyles en C1-C6, aralkyles; les esters de formule - R1-CO-O-R2 ; les amides de formule -R3-CO-NZY dans laquelle Y et Z peuvent former ensemble un radical cycloalkyle ou un radical hétérocyclique, éventuellement substitué par un ou plusieurs radicaux alkyles; un radical choisi dans le groupe constitué par les radicaux alkyles, alcényles ou alcynyles, substitués par au moins une amine de formule -NZY; ou l'un de ses sels pharmaceutiquement acceptables, y compris ses isomères, ses énantiomères, ses diastéréoisomères et leurs mélanges. L'invention a également pour objet l'utilisation de ces nouveaux dérivés pour la préparation d'une composition pharmaceutique, notamment destinée au traitement et/ou la prévention chez l'Homme des dépressions, des troubles du cycle veille-sommeil et des troubles symptomatiques frontaux dans leur composantes cognitives.

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