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    MORPHINAN DERIVATIVE
    3.
    发明公开
    MORPHINAN DERIVATIVE 审中-公开

    公开(公告)号：EP3498711A1

    公开(公告)日：2019-06-19

    申请号：EP17839452.4

    申请日：2017-08-08

    申请人： 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： C07D487/08 ,  A61K31/439 ,  A61P13/10 ,  A61P25/04 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P27/06 ,  C07D491/18

    摘要： A compound 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, or the like,
    R 2 represents a 4- to 7-membered saturated heterocycle containing one or two heteroatoms which may be the same or different and are selected from N, O, and S, and two or more carbon atoms as ring-constituting atoms,
    the heterocycle may be substituted with a substituent such as an oxo group,
    R 2 binds to Y via a carbon atom as a ring-constituting atom of R 2 ,
    R 3 , R 4 , and R 5 , which are the same or different, represent hydrogen; hydroxy; or the like,
    R 6a and R 6b , which are the same or different, represent hydrogen or the like,
    R 7 and R 8 , which are the same or different, represent hydrogen or the like,
    R 9 and R 10 , which are the same or different, represent hydrogen or the like,
    X represents O or CH 2 , and
    Y represents C(= O) or the like),
    a tautomer of the compound, a stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof is used as an anxiolytic, an antidepressant, or the like.

    MORPHINAN DERIVATIVE
    4.
    发明公开
    MORPHINAN DERIVATIVE 审中-公开

    公开(公告)号：EP3974430A1

    公开(公告)日：2022-03-30

    申请号：EP21203556.2

    申请日：2016-03-17

    申请人： 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

    摘要： A method of preparing a compound 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.,
    R6a 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.

    MORPHINAN DERIVATIVE
    5.
    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

    METHOD FOR PRODUCING MORPHINAN DERIVATIVE
    8.
    发明公开
    METHOD FOR PRODUCING MORPHINAN DERIVATIVE 审中-公开

    公开(公告)号：EP3984982A1

    公开(公告)日：2022-04-20

    申请号：EP20844453.9

    申请日：2020-07-17

    申请人： Nippon Chemiphar Co., Ltd.

    发明人： SAITO, Daisuke ,  HAYASHIDA, Kohei

    IPC分类号： C07B35/02 ,  C07D471/08

    摘要： Provided is, for example, a method for producing a morphinan derivative represented by General Formula (II), including the step of: allowing metal sodium and ethylenediamine to act on a morphinan derivative represented by General Formula (I) in presence of an auxiliary solvent.

    wherein R 1 represents a hydrogen atom, or a C 1-10 alkyl group, a C 3-6 cycloalkyl group, a C 2-6 alkenyl group, a C 6-10 aryl group, or a heteroaryl group optionally having a substituent, R 2 represents an amino protecting group, R 3 represents a methoxy group, R 4 and R 5 represent a hydrogen atom or a hydroxy group, R 6 and R 7 represent a hydrogen atom or an electron-donating group, wherein R 6 and R 7 are not simultaneously a hydrogen atom, and X represents O or CH 2 .

    T-TYPE CALCIUM CHANNEL BLOCKER
    9.
    发明公开
    T-TYPE CALCIUM CHANNEL BLOCKER 审中-公开

    公开(公告)号：EP3825303A1

    公开(公告)日：2021-05-26

    申请号：EP19838574.2

    申请日：2019-07-17

    申请人： Nippon Chemiphar Co., Ltd. ,  Kinki University

    发明人： TANAKA, Hiroto ,  OOI, Isao ,  SAITO, Daisuke ,  HAYASHIDA, Kohei ,  YAMAMOTO, Kohei ,  KAWABATA, Atsufumi

    IPC分类号： C07D205/04

    摘要： To provide a novel T-type calcium channel blocker.
    A compound represented by the following General Formula (I), a tautomer or a stereoisomer of the compound, a pharmaceutically acceptable salt of the compound, or a solvate of the compound, the tautomer, the stereoisomer, or the salt is used as a T-type calcium channel blocker.

    wherein A represents a phenyl which may have a substituent, a 4-membered to 6-membered heteroaryl ring composed of one to three identical or different heteroatoms selected from an oxygen atom, a sulfur atom, and a nitrogen atom and carbon atoms as ring-constituting atoms, or a heterocondensed ring composed of the heteroaryl ring and either a benzene ring or a 6-membered heteroaryl ring composed of one to two nitrogen atoms and carbon atoms, wherein the heteroaryl ring or the heterocondensed ring may have a substituent and is bonded to a nitrogen atom of the adjacent cyclic amino by means of a carbon atom constituting these rings;
    B represents a phenyl which may have a substituent, a 5-membered or 6-membered heteroaryl ring composed of one to three identical or different heteroatoms selected from an oxygen atom, a sulfur atom, and a nitrogen atom and carbon atoms as ring-constituting atoms, or a heterocondensed ring composed of the heteroaryl ring and either a benzene ring or a 6-membered heteroaryl ring composed of one to two nitrogen atoms and carbon atoms, wherein the heteroaryl ring or the heterocondensed ring may have a substituent and is bonded to the adjacent cyclopropyl ring by means of a carbon atom constituting these rings;
    R 1 and R 2 , which may be identical or different, each represent a hydrogen atom, a halogen atom, or the like;
    R 3 represents a hydrogen atom, a halogen atom, or the like;
    n and m, which may be identical or different, each represent 0 or 1; and p represents 1 or 2.