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    MORPHINAN DERIVATIVE
    2.
    发明公开
    MORPHINAN DERIVATIVE 审中-公开
    吗啡喃衍生物

    公开(公告)号：EP3272750A1

    公开(公告)日：2018-01-24

    申请号：EP16765061.3

    申请日：2016-03-17

    申请人： University of Tsukuba ,  School Juridical Person Kitasato Institute ,  National Center of Neurology and Psychiatry ,  Nippon Chemiphar Co., Ltd.

    发明人： NAGASE, Hiroshi ,  FUJII, Hideaki ,  SAITOH, Akiyoshi ,  NAKATA, Eriko ,  HIROSE, Masaaki ,  OOI, Isao ,  HAYASHIDA, Kohei

    IPC分类号： C07D471/08 ,  A61K31/485 ,  A61P25/04 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00

    CPC分类号： C07D471/08 ,  A61K31/485

    摘要： A morphinan derivative represented by the following general formula (I):

    (wherein R 1 represents hydrogen, C 1-10 alkyl, cycloalkylalkyl where the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms, etc.,
    R 2 represents heterocyclic ring containing 1 to 4 heteroatoms selected from N, O and S and at least one carbon atom as ring-constituting atoms, containing at least one set of adjacent ring-constituting atoms bound by a double bond, and further substituted with at least one oxo group,
    Y binds to a carbon atom as a ring-constituting atom of R 2 ,
    R 3 , R 4 , and R 5 represent hydrogen; hydroxy, etc.,
    R 6a and R 6b represent hydrogen, etc.,
    R 7 and R 8 represent hydrogen, etc.,
    R 9 and R 10 , which are the same or different, represent hydrogen, etc.,
    X represents O or CH 2 , and
    Y represents C(=O)),
    a tautomer or stereoisomer of the compound, or a pharmaceutically acceptable salt thereof, or a solvate thereof is used as an anxiolytic drug, antidepressant, etc.

    摘要翻译： 下述通式（I）表示的吗啡喃衍生物:(式中，R 1表示氢，碳原子数1〜10的烷基，环烷基部分的碳原子数为3〜6，亚烷基部分的碳原子数为1〜5的环烷基烷基等） R 2表示含有1至4个选自N，O和S的杂原子和至少一个碳原子作为成环原子的杂环，其含有至少一个由双键连接的相邻成环原子，并且进一步被 至少一个氧代基团，Y与碳原子结合成为R2的成环原子，R3，R4和R5代表氢原子，羟基等，R6a和R6b代表氢原子等，R7和R8代表氢原子等 R9和R10相同或不同，表示氢等，X表示O或CH2，Y表示C（= O）），该化合物的互变异构体或立体异构体或其药学上可接受的盐， 或其溶剂化物用作抗焦虑药，抗抑郁药等

    NALFURAFINE-CONTAINING PERCUTANEOUS ABSORPTION PATCH
    7.
    发明公开
    NALFURAFINE-CONTAINING PERCUTANEOUS ABSORPTION PATCH 审中-公开
    含有氟化合物的经皮吸收贴片

    公开(公告)号：EP3315132A1

    公开(公告)日：2018-05-02

    申请号：EP16814498.8

    申请日：2016-06-24

    申请人： University of Tsukuba

    发明人： NAGASE, Hiroshi ,  TADA, Makiko ,  YASHIMA, Megumi ,  SAIKI, Takeshi

    IPC分类号： A61K31/485 ,  A61K9/70 ,  A61K47/32 ,  A61P17/04

    CPC分类号： A61K9/70 ,  A61K31/485 ,  A61K47/32

    摘要： The present invention relates to a nalfurafine-containing percutaneous absorption patch having a support, a drug layer and a control layer which are laminated successively, wherein the drug layer contains at least one kind of a drug selected from the group consisting of nalfurafine and a salt thereof, and capable of maintaining a given level of drug skin permeation amount without permeation of an excess amount of the drug through the skin in a short time even when applied to the skin in which the horny cell layer and the like are damaged and the skin barrier is insufficient.

    摘要翻译： 本发明涉及一种含有纳福呋喃的经皮吸收贴剂，其具有依次层叠的载体，药物层和对照层，其中药物层含有至少一种选自纳福拉芬和盐 ，即使在角质层等被损伤的皮肤和皮肤损伤的情况下，也能够在短时间内维持规定量的药物皮肤透过量而不会使过量的药物透过皮肤渗透， 屏障不足。