Piperidine derivatives as neurotransmitter re-uptake inhibitors
    1.
    发明授权
    Piperidine derivatives as neurotransmitter re-uptake inhibitors 失效
    哌啶衍生物作为神经递质再摄取抑制剂

    公开(公告)号:US06376673B1

    公开(公告)日:2002-04-23

    申请号:US09415227

    申请日:1999-10-12

    IPC分类号: C07D21118

    CPC分类号: C07D211/28

    摘要: The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salt thereof; wherein R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl or 2-hydroxyethyl; R3 is —CR′═NOR″ wherein R′ and R″ each independently are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, cycloalkylalkenyl, alkynyl, cycloalkylalkynyl, aryl or benzyl; R4 is phenyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, amino, nitro, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, aryl and heteroaryl; 3,4-methylenedioxyphenyl; benzyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, amino, nitro, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, aryl and heteroaryl; heteroaryl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, amino, nitro, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, aryl and heteroaryl; or naphthyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, amino, nitro, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, aryl and heteroaryl. The compounds possess valuable pharmaceutical properties as monoamine neurotransmitter, i.e. dopamine, serotonin, noradrenaline, reuptake inhibitors.

    摘要翻译: 本发明涉及式(I)化合物或其药学上可接受的盐; 其中R是氢,烷基,烯基,炔基,环烷基,环烷基烷基或2-羟乙基; R3是-CR'= NOR“,其中R'和R”各自独立地为氢,烷基,环烷基,环烷基烷基,烯基,环烷基烯基,炔基,环烷基炔基,芳基或苄基; R4是可以被选自卤素,CF 3,CN,氨基,硝基,烷氧基,环烷氧基,烷基,环烷基,烯基,炔基,芳基和杂芳基的取代基取代一次或多次的苯基; 3,4-亚甲二氧基苯基; 苄基,其可以被选自卤素,CF 3,CN,氨基,硝基,烷氧基,环烷氧基,烷基,环烷基,烯基,炔基,芳基和杂芳基的取代基取代一次或多次; 可以被选自卤素,CF 3,CN,氨基,硝基,烷氧基,环烷氧基,烷基,环烷基,烯基,炔基,芳基和杂芳基的取代基取代一次或多次的杂芳基; 或萘基,其可以被选自卤素,CF 3,CN,氨基,硝基,烷氧基,环烷氧基,烷基,环烷基,烯基,炔基,芳基和杂芳基的取代基取代一次或多次。 该化合物具有作为单胺神经递质(即多巴胺,5-羟色胺,去甲肾上腺素,再摄取抑制剂)的有价值的药物性质。