Derivatives of indanyl-piperazines, the process for...

C - Chemistry – Metallurgy – 07 – D

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C07D 295/14 (2006.01) A61K 31/495 (2006.01) C07D 295/08 (2006.01)

Patent

CA 2541066

This invention relates to formula (I) compounds: (see formula I) where - R3 represents a hydrogen atom, and R1 and R2 together with the carbon atoms carrying them form a benzene, naphthalene or quinoline ring, with each of these rings eventually being substituted, or else R1 represents a hydrogen atom, and R2 and R3 together with the carbon atoms carrying them form a benzene, naphthalene or quinoline ring with each of these rings eventually being substituted, n represents 1 or 2, -X- represents a group selected from among -(CH2)m-O-Ak-, -(CH2)m-NR4-Ak-, -(CO)-NR4-Ak- and -(CH2)m-NR4-(CO)-, m represets an integer from 1 to 6 inclusive, Ak represents an alkylene chain which is eventually substituted, and R4 represents a hydrogen atom or an alkyl group, - Ar represents an aryl or heteroaryl group, its optical isomers, and its addition salts with a pharmaceutically acceptable acid. The invention also relates to the procedure for preparing the said compounds, the pharmaceutical compositions containing them, and their uses as serotonin recapture inhibitors and NK1 antagonists.

Composé de formule (I) (voir formule I) dans laquelle - R3 représente un atome d'hydrogène, et R1 et R2 forment ensemble, avec les atomes de carbone qui les portent, un cycle benzène, naphtalène ou quinoléine, chacun de ces cycles étant éventuellement substitué, ou bien R1 représente un atome d'hydrogène, et R2 et R3 forment ensemble, avec les atomes de carbone qui les portent, un cycle benzène, naphtalène ou quinoléine, chacun de ces cycles étant éventuellement substitué, - n représente 1 ou 2, - -X- représente un groupement choisi parmi -(CH2)m-O-Ak-, -(CH2)m-NR4-Ak-, - (CO)-NR4-Ak- et -(CH2)m-NR4-(CO)-, m représente un entier compris entre 1 et 6 inclus, Ak représente une chaîne alkylène éventuellement substituée, et R4 représente un atome d'hydrogène ou un groupement alkyle, - Ar représente un groupement aryle ou hétéroaryle, ses isomères optiques, ainsi que ses sels d'addition à un acide pharmaceutiquement acceptable. Médicaments.

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