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    • 50. 发明申请
    • NOVEL 4-BENZHYDRYLOXY-TETRAALKYL-PIPERIDINE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS
    • 新型4-苄氧基 - 四氢吡啶衍生物及其作为单胺神经递质抑制剂的用途
    • US20110053984A1
    • 2011-03-03
    • US12921030
    • 2009-02-27
    • Dan PetersJohn Paul RedrobeElsebet Østergaard Nielsen
    • Dan PetersJohn Paul RedrobeElsebet Østergaard Nielsen
    • A61K31/445C07D211/46A61P25/00A61P29/00A61P13/00A61P15/00
    • C07D211/46
    • 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.
    • 本发明涉及式(I)的新型4-二苯甲氧基 - 四烷基 - 哌啶衍生物,其任何立体异构体或其立体异构体的任何混合物或其N-氧化物或其药学上可接受的盐,其中R a表示氢或C 1 -6-烷基; Rb和Rc彼此独立地表示苯基,该苯基任选被一个或多个独立地选自卤素,三氟甲基,三氟甲氧基,氰基,C 1-6 - 烷氧基和亚甲基二氧基的取代基取代; R',R“,R”“和R”“彼此独立地表示C 1-6 - 烷基; 并且条件是该化合物不是4-二苯甲基氧基-1,2,2,6,6-五甲基哌啶,其可用作单胺神经递质再摄取抑制剂。 在其它方面,本发明涉及这些化合物在治疗方法中的用途以及包含本发明化合物的药物组合物。