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    NOVEL 3-AZABICYCLO[3.1.0]HEXANE DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES
    8.
    发明公开
    NOVEL 3-AZABICYCLO[3.1.0]HEXANE DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES 审中-公开
    NEUARTIGES 3-AZABICYCLO [3.1.0] HEXAN-DERIVAT UND VERWENDUNG DAVONFÜRMEDISINISCHE ZWECKE

    公开(公告)号：EP3072884A1

    公开(公告)日：2016-09-28

    申请号：EP14863377.9

    申请日：2014-11-19

    申请人： SANWA KAGAKU KENKYUSHO CO., LTD. ,  Ube Industries, Ltd.

    发明人： TANIKO, Kaori ,  MIYAZAWA, Toshiyuki ,  KANEKO, Tatsuroh ,  KURUMAZUKA, Daisuke ,  HARADA, Satoko ,  IZUCHI, Toru ,  OKABE, Morio ,  IWAMURA, Ryo ,  TSUZAKI, Yasunori ,  SETOGUCHI, Hiroyuki ,  IMURA, Yuuki ,  AKAZA, Hiroto ,  SHIMIZU, Motohisa ,  KIMURA, Tomio

    IPC分类号： C07D209/52 ,  A61K31/403 ,  A61K31/454 ,  A61P17/04 ,  A61P43/00 ,  C07D401/06 ,  C07D403/06

    摘要： The object of the present invention is to provide a compound having an antagonistic action against µ-opioid receptors, which causes less side effects and thus is highly safe.
    A compound represented by the general formula (I), or a pharmacologically acceptable salt thereof:

    wherein
    R 1 and R 2 are the same or different, and each represents a hydrogen atom or a halogen atom, provided that R 1 and R 2 are not simultaneously halogen atoms,
    R 3 represents a C 1 -C 3 alkyl group or a vinyl group, and
    R 4 represents the formula (II):

    wherein R 5 represents a hydroxy group or a C 1 -C 3 alkoxy group, and R 6 and R 7 are the same or different, and each represents a hydrogen atom or a halogen atom;
    or the formula (III):

    wherein Ring A represents a halogen atom(s)-substituted C 5 -C 7 cycloalkyl group which is optionally substituted by a C 1 -C 3 alkoxy group, or a halogen atom(s)-substituted 5- to 7-membered saturated heterocyclic group.

    摘要翻译： 本发明的目的是提供对μ-阿片受体具有拮抗作用的化合物，其副作用较小，因此是高度安全的。 由通式（I）表示的化合物或其药理学上可接受的盐：其中R 1和R 2相同或不同，并且各自表示氢原子或卤素原子，条件是R 1和R 2不为 同时卤素原子，R 3表示C 1〜C 3烷基或乙烯基，R 4表示式（II）：其中R 5表示羟基或C 1〜C 3烷氧基，R 6 和R 7相同或不同，各自表示氢原子或卤素原子; 或式（III）：其中环A表示任选被C 1 -C 3烷氧基取代的卤素原子 - 取代的C 5 -C 7环烷基或被卤素原子取代的5 至7元饱和杂环基。