Piperidine derivatives

Details Piperidine derivatives Piperidine derivatives

C - Chemistry, Metallurgy

07

D

C07D 211/42 (2006.01) A61K 31/445 (2006.01) C07D 211/14 (2006.01) C07D 211/20 (2006.01) C07D 211/22 (2006.01)

Patent

CA 2343168

The present invention relates to compounds of general formula (I), wherein R1 is tetrahydronaphtyl; or -(CH2)n-C6H5-R4 wherein n is 0-4 and R4 is H, lower alkyl, or lower alkoxy; or C5-C12 cycloalkyl, optionally substituted by lower alkyl; R2 is H, OH, lower alkoxy, lower alkenyloxy or lower alkyl; R3 is C5-C7 cycloalkyl or phenyl, optionally substituted by OH, halogen, lower alkoxy, lower alkenyloxy, lower alkyl or -O-(CH2)n-C6H5 wherein n is 0-3; and their pharmaceutically acceptable acid addition salts. The compounds of general formula (I) are suitable for the treatment of memory and attention deficits, psychiatric, neurological and physiological disorders, such as anxiety and stress disorders, depression, memory loss due to Alzheimer's disease or other dementias such as vascular dementia and AIDS dementia complex, Parkinson's disease, epilepsy and convulsions, acute and/or chronic pain conditions, withdrawal symptoms of addictive drugs and reduction of their abuse/craving, control of water balance, Na+ excretion, arterial blood pressure disorders and metabolic disorders such as obesity.

L'invention porte sur des composés de formule générale (1) dans laquelle: R?1¿ est tétrahydronaphtyle; ou -(CH¿2?)¿n? -C¿6?H¿5?-R?4¿ où n est 0-4 et R?4¿ est H, alkyle inférieur, ou alkoxy inférieur; ou C¿5?-C¿12? cycloalkyle, facultativement substitué par alkyle inférieur; R?2¿ est H, OH, alkoxy inférieur, alcényloxy inférieur ou alkyle inférieur; R?3¿ est C¿5?-C¿7? cycloalkyle ou phényle, facultativement substitué par OH, halogène, alkoxy inférieur, alcényloxy inférieur, alkyle inférieur ou -O-(CH¿2?)¿n?-C¿6?H¿5? où n est 0-3; et leurs sels d'addition pharmacocompatibles. Lesdits composés conviennent au traitement des déficits d'attention et de mémoire, des troubles psychiatriques, neurologiques et physiologiques tels que l'angoisse, le stress, la dépression, les pertes de mémoires dues à la maladie d'Alzheimer et autres démences telles que la démence vasculaire et le complexe de démence du SIDA, la maladie de Parkinson, l'épilepsie et les convulsions, les algies aiguës et/ou chronique, les symptômes dus au sevrage des drogues, à la réduction de la consommation et à l'état de manque, la régulation de l'équilibre hydrique, l'excrétion du Na?+¿, les troubles de la tension artérielle, et les troubles du métabolisme tels que l'obésité.

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