NOVEL 3-AZABICYCLO[3.1.0]HEXANE DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES
    2.
    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

    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。