1-(benzothiazol-2-yl)-4-(1-phenylmethyl)piperazines:...

C - Chemistry – Metallurgy – 07 – D

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C07D 277/82 (2006.01) A61K 31/495 (2006.01) C07D 277/68 (2006.01)

Patent

CA 2336150

Disclosed are compounds of formula (A) or pharmaceutically acceptable addition salts thereof wherein: R1 and R2 are the same or different and represent hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylthio, hydroxy, amino, mono- or di(C1-C6) alkylamino, cyano or trifluoromethyl; Ar represents aryl or heteroaryl, each of which is optionally substituted with R3, R4 and/or R6; R3, R4, and R6 independently represent hydrogen, halogen, hydroxy, C1-C6 alkyl, C1- C6 alkoxy, perfluoro (C1-C6) alkyl, perfluoro (C1-C6) alkoxy, or SO2NH2; or R3 and R4 together with the atoms to which they are attached represent a ring having 5-7 atoms; and R5 represents hydrogen or C1-C6 alkyl, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.

L'invention concerne des composés de la formule (A) ou des sels d'addition acides pharmaceutiquement acceptables desdits composés. Dans ladite formule, R¿1? et R¿2? sont identiques ou différents et représentent hydrogène, halogène, alkyle C¿1?-C¿6?, alcoxy C¿1?-C¿6?, alkylthio C¿1?-C¿6?, hydroxy, amino, mono ou dialkylamino(C¿1?-C¿6?), cyano ou trifluorométhyle; Ar est aryle ou hétéroaryle, chacun étant éventuellement substitué par R¿3?, R¿4? et/ou R¿6?; R¿3?, R¿4? et R¿6? sont, indépendamment, hydrogène, halogène, hydroxy, alkyle C¿1?-C¿6?, alcoxy C¿1?-C¿6?, perfluoro-alkyle C¿1?-C¿6?, perfluoro-alcoxy C¿1?-C¿6?, ou SO¿2?NH¿2?; ou R¿3? et R¿4? forment ensemble, avec les atomes auxquels ils sont liés, un noyau de 5 à 7 atomes; et R¿5? est hydrogène ou alkyle C¿1?-C¿6?. Ces composés sont utiles pour le traitement et/ou la prévention de troubles neuropsychologiques, y compris, entre autres, la schizophrénie, la manie, la démence, la dépression, l'anxiété, le comportement compulsif, l'abus de substances psychoactives, les troubles moteurs apparentés à la maladie de Parkinson et les troubles moteurs associés à l'usage de neuroleptiques antipsychotiques.

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