PYRAZOLOMORPHINAN DERIVATIVE
    1.
    发明公开

    公开(公告)号:EP4062972A1

    公开(公告)日:2022-09-28

    申请号:EP20890718.8

    申请日:2020-11-20

    摘要: The present invention provides a compound having a selective opioid δ receptor agonist effect. The present invention provides a pyrazolomorphinan derivative represented by general formula (1) (in the formula, (II) R 1 represents a hydrogen atom, an alkyl group, a cycloalkylmethyl group, or the like, R 2 represents a hydrogen atom or a hydroxy protecting group, R 3 represents a hydroxy group, an alkyl group, a partially unsaturated heterocyclic group, an aryl group, a heteroaryl group, or the like; and R 4 represents a hydrogen atom, an alkyl group, an aralkyl group, a cycloalkyl group, a cycloalkyl alkyl group, a saturated heterocyclic group, an aryl group, a heteroaryl group, or the like). The pyrazolomorphinan derivative can be used as an active ingredient in an analgesic, an antidepressant, an anxiolytic, or the like.

    MORPHINAN DERIVATIVE
    3.
    发明公开
    MORPHINAN DERIVATIVE 有权
    吗啡喃衍生物

    公开(公告)号:EP2966074A1

    公开(公告)日:2016-01-13

    申请号:EP13877360.1

    申请日:2013-10-15

    摘要: The present invention relates to a morphinan derivative represented by the following general formula (I), wherein R 1 represents hydrogen, C 1-6 alkyl, C 6-10 aryl, etc., R 2 and R 3 , which are the same or different, represent hydrogen, hydroxy, ect., R 4 and R 5 represent hydrogen, C 1-6 alkyl, etc., R 6 represents hydrogen, hydroxy, C 1 - 6 alkyl, etc., X represents O or CH 2 , Y represents C=O, C(=O)O, etc., and m and n, which are the same or different, represent an integer of 0 to 2 (m and n are not 0 at the same time), a tautomer or stereoisomer of the compound, or a pharmaceutically acceptable salt thereof, or a solvate thereof, as well as an analgesic, antianxiety drug, etc. containing the same as an active ingredient.

    摘要翻译: 本发明涉及下述通式(I)表示的吗啡喃衍生物,其中R 1表示氢,C 1-6烷基,C 6-10芳基等,R 2和R 3相同或不同,表示氢, 羟基等,R 4和R 5表示氢,C 1-6烷基等,R 6表示氢,羟基,C 1-6烷基等,X表示O或CH 2,Y表示C = O,C(= O) O等,m和n相同或不同,表示0〜2的整数(m和n同时不为0),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,以及含有该化合物作为活性成分的镇痛剂,抗焦虑药等。

    MORPHINAN DERIVATIVE
    5.
    发明公开
    MORPHINAN DERIVATIVE 有权
    MORPHINANDERIVAT

    公开(公告)号:EP2774926A1

    公开(公告)日:2014-09-10

    申请号:EP12829693.6

    申请日:2012-09-07

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

    (in the formula, R 1 represents hydrogen, C 1-6 alkyl, cycloalkylalkyl (the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms), aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like,
    R 2 represents hydrogen, C 1-6 alkyl, C 3-6 cycloalkyl, C 6-10 aryl, aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like,
    R 3 , R 4 and R 5 represent hydrogen, hydroxy, carbamoyl, C 1-6 alkoxy, C 6-10 aryloxy and the like,
    R 6a , R 6b , R 7 , R 8 , R 9 , and R 10 represent hydrogen and the like,
    X represents O or CH 2 , and
    Y represents C=O, SO 2 , an atomic bond and the like), or an acid addition salt thereof is used as an analgesic.

    摘要翻译: 由以下通式(I)表示的吗啡喃衍生物:(式中,R 1表示氢,C 1-6烷基,环烷基烷基(环烷基部分具有3〜6个碳原子,亚烷基部分具有1〜5个碳原子 原子),芳烷基(芳基部分具有6〜10个碳原子,亚烷基部分具有1〜5个碳原子)等,R 2表示氢,C 1-6烷基,C 3-6环烷基, 10芳基,芳烷基(芳基部分具有6至10个碳原子,亚烷基部分具有1至5个碳原子)等,R 3,R 4和R 5表示氢,羟基,氨基甲酰基,C 1-6烷氧基 ,C 6-10芳氧基等,R 6a,R 6b,R 7,R 8,R 9和R 10表示氢等,X表示O或CH 2,Y表示C = O,SO 2 ,原子键等)或其酸加成盐用作止痛剂。

    MORPHINAN DERIVATIVE
    6.
    发明公开

    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

    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
    7.
    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

    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

    MORPHINAN DERIVATIVE
    10.
    发明公开

    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

    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.