[EN] NOVEL 4-BENZHYDRYLOXY-TETRAALKYL-PIPERIDINE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTATKE INHIBITORS<br/>[FR] NOUVEAUX DÉRIVÉS DE LA 4-BENZHYDRYLOXY-TETRAALKYL-PIPERIDINE ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE LA RECAPTURE DES NEUROTRANSMETTEURS MONOAMINES
申请人:NEUROSEARCH AS
公开号:WO2009109519A1
公开(公告)日:2009-09-11
This invention relates to novel 4-benzhydryloxy-tetraalkyl-piperidine derivatives of Formula (I), any of its stereoisomers or any mixture of its stereoisomers, or an N-oxide thereof, or a pharmaceutically acceptable salt thereof, wherein Ra represents hydrogen or C1-6-alkyl; Rb and Rc independent of each other represent a phenyl group, which phenyl group is optionally substituted with one or more substituents independently selected from the group consisting of halo, trifluoromethyl, trifluoromethoxy, cyano, C1-6-alkoxy and methylenedioxo; R', R", R'" and R"" independent of each other represent C1-6-alkyl; and with the proviso that the compound is not 4-benzhydryloxy-1,2,2,6,6-pentamethyl- piperidine, useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
本发明涉及具有以下结构的新颖的4-苄基氧基-四烷基-哌啶衍生物(I),其立体异构体中的任何一种或其立体异构体的混合物,或其N-氧化物,或其药学上可接受的盐,其中Ra代表氢或C1-6-烷基;Rb和Rc相互独立地代表苯基,该苯基可以选择性地取代一个或多个取代基,所述取代基独立地选自卤素、三氟甲基、三氟甲氧基、氰基、C1-6-烷氧基和亚甲二氧基;R'、R"、R'"和R""相互独立地代表C1-6-烷基;但该化合物不是4-苄基氧基-1,2,2,6,6-五甲基-哌啶,可用作单胺神经递质再摄取抑制剂。在其他方面,本发明涉及这些化合物在治疗方法中的使用,以及包含本发明化合物的药物组合物。