Novel aryl piperazine-derived piperazide derivatives,...

C - Chemistry – Metallurgy – 07 – D

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C07D 295/20 (2006.01) A61K 31/495 (2006.01) C07D 295/18 (2006.01) C07D 295/185 (2006.01) C07D 295/205 (2006.01) C07D 295/215 (2006.01) C07D 317/66 (2006.01) C07D 319/18 (2006.01)

Patent

CA 2195427

Novel 5HT receptor antagonists of general formula (I) in which Ar1 and Ar2 are an aromatic residue, X is O, NH, CH2O or CH2NH, R1 is hydrogen, a linear or branched alkyl chain comprising 1-6 carbon atoms. The invention also concerns the salts, hydrates, solvates and physiologically acceptable bioprecursors for their therapeutic use, their geometric and optic isomers and their mixtures in all proportions and in racemic form. Also disclosed are methods for the preparation of these novel antagonists, their use as drugs and pharmaceutical compositions comprising them.

La présente invention concerne de nouveaux antagonistes des récepteurs 5HT, répondant à la formule générale (I) dans laquelle Ar1 et Ar2 représentent un résidu aromatique, X représente O, NH, CH2O ou CH2NH, R1 représente un hydrogène, une chaîne alkyle linéaire ou ramifiée comprenant de 1 à 6 atomes de carbone, et leurs sels, hydrates, solvates et bioprécurseurs physiologiquement acceptables pour leur usage thérapeutique, leurs isomères géométriques et optiques ainsi que leurs mélanges en toutes proportions et sous forme racémique. La présente invention concerne également leurs procédés de préparation, leur utilisation à titre de médicament et les compositions pharmaceutiques les comprenant.

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