Cycloalkyl-substituted aryl-piperazines, piperidines and...

Details Cycloalkyl-substituted aryl-piperazines, piperidines and... Cycloalkyl-substituted aryl-piperazines, piperidines and...

C - Chemistry, Metallurgy

07

D

C07D 295/12 (2006.01) A61K 31/495 (2006.01) C07D 209/08 (2006.01) C07D 211/22 (2006.01) C07D 295/13 (2006.01) C07D 319/18 (2006.01)

Patent

CA 2334254

This invention relates to compounds which have activity as 5-HT1A agonists and antagonists which may be useful for the treatment of anxiety, depression, cognitive deficits, and prostate cancer. Useful compounds are those of formula (I) where: X is selected from the group consisting of (1), (2), (3); n is selected from the integers 1 through 5; R1 is optionally substituted C6-C10- aryl or mono or bicyclic heteroaryl, with a proviso that heteroaryl is not thiadiazole; R2 is selected from the group consisting of H and C1-C6 alkyl; R3 is selected from the group consisting of H, COR5, COOR5, and CONR5R6; R4, R5 and R6 are as defined hereinabove; or an optical isomer; or a pharmaceutically acceptable salt thereof.

L'invention concerne des composés, un isomère optique ou un sel desdits composés, acceptables au plan pharmaceutique, possédant l'activité d'antagonistes et d'agonistes de 5-HT¿1A?, pouvant être utiles pour le traitement de l'anxiété, de la dépression, de déficits intellectuels et du cancer de la prostate. Les composés utiles sont ceux de la formule (I), dans laquelle X est choisi dans le groupe constitué de (1), (2) et (3); n est choisi parmi les entiers de 1 à 5; R?1¿ représente hétéroaryle mono ou bicyclique ou aryle C¿6?-C¿10? éventuellement substitué, à condition qu'hétéroaryle ne représente pas thiadiazole; R?2¿ est choisi dans le groupe constitué de H et alkyle C¿1?-C¿6?; R?3¿ est choisi dans le groupe formé de H, COR?5¿, COOR?5¿ et CONR?5¿R?6¿; R?4¿, R?5¿ et R?6¿ sont tels que définis ci-dessus.

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