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    MORPHINAN DERIVATIVE
    4.
    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

    DRUG FOR PREVENTING, TREATING OR PREVENTING METASTASIS OF GIANT CELL TUMOR THAT OCCURS IN BONE OR SOFT PARTS, CHONDROSARCOMA, OR OSTEOSARCOMA, LOCAL INJECTION FOR ARTERIAL EMBOLIZATION, AND ARTIFICIAL BONE
    6.
    发明公开
    DRUG FOR PREVENTING, TREATING OR PREVENTING METASTASIS OF GIANT CELL TUMOR THAT OCCURS IN BONE OR SOFT PARTS, CHONDROSARCOMA, OR OSTEOSARCOMA, LOCAL INJECTION FOR ARTERIAL EMBOLIZATION, AND ARTIFICIAL BONE 有权
    药物预防，转移的骨巨细胞瘤柔嫩部位，软骨肉瘤或骨肉瘤，局部注射动脉人工骨栓塞治疗或预防

    公开(公告)号：EP3050573A1

    公开(公告)日：2016-08-03

    申请号：EP14847606.2

    申请日：2014-09-25

    申请人： Nippon Chemiphar Co., Ltd.

    发明人： TAKEUCHI, Akihiko ,  TSUCHIYA, Hiroyuki

    IPC分类号： A61K45/00 ,  A61K31/167 ,  A61K31/196 ,  A61K31/38 ,  A61K31/405 ,  A61K31/427 ,  A61K31/663 ,  A61K39/395 ,  A61L27/00 ,  A61L31/00 ,  A61P19/00 ,  A61P35/00 ,  G01N33/15 ,  G01N33/50 ,  G01N33/68 ,  G01N33/92

    摘要： The present invention provides an agent for prophylactic treatment, therapeutic treatment, or prevention of metastasis of giant cell tumor occurring in a bone and soft tissue, chondrosarcoma, or bone sarcoma, a local infusion for artery embolization, and an artificial bone, which comprises a substance having a PPARγ-agonistic activity and/or a PPARγ expression-inducing activity as an active ingredient. The agent for prophylactic treatment, therapeutic treatment, or prevention of metastasis, the local infusion for artery embolization, and the artificial bone of the present invention are a radical therapeutic agent or radical therapeutic material that can cause apoptosis in giant cell tumor occurring in a bone and soft tissue, chondrosarcoma, or bone sarcoma to make the tumor disappear, and can induce differentiation of the tumor into fat cells to make the tumor disappear.

    摘要翻译： 本发明提供了用于预防性治疗，治疗性治疗，或预防骨和软组织，软骨或骨肉瘤，局部输注动脉栓塞发生的巨细胞瘤转移的试剂，并在人造骨，它包括一个 具有PPAR³-激动活性和/或作为活性成分的PPAR³表达诱导活性的物质。 用于预防性治疗，治疗性治疗，或预防转移，局部输注动脉栓塞，并且本发明的人造骨的试剂是自由基治疗剂或自由基治疗材料也能引起细胞凋亡的巨细胞瘤在骨发生的 和软组织，软骨或骨肉瘤，使肿瘤消失，并能诱导肿瘤成脂肪细胞的分化，使肿瘤消失。

    METHOD FOR PRODUCING ZALTOPROFEN AND DERIVATIVE THEREOF
    8.
    发明公开
    METHOD FOR PRODUCING ZALTOPROFEN AND DERIVATIVE THEREOF 审中-公开
    VERFAHREN ZUR HERSTELLUNG VON ZALTOPROFEN UND DERIVAT DAVON

    公开(公告)号：EP2842952A1

    公开(公告)日：2015-03-04

    申请号：EP13780982.8

    申请日：2013-04-24

    申请人： Nippon Chemiphar Co., Ltd.

    发明人： TENDO, Atsushi

    IPC分类号： C07D337/14 ,  A61K31/38 ,  A61P29/00

    CPC分类号： C07D337/14

    摘要： The present invention relates to a method for preparing zaltoprofen or a zaltoprofen derivative by a Friedel-Crafts reaction type intramolecular cyclization reaction in an industrial scale at an industrially acceptable yield and a purity sufficient for use as an active ingredient of medicaments in a simple and economical manner, without generating a detectable amount of impurities such as dimmers, by using polyphosphoric acid in an amount of 6.5 times or less of amount of a starting material compound before cyclization. More specifically, the present invention relates to such a method for preparing zaltoprofen or a zaltoprofen derivative as mentioned above, which comprises cyclizing a starting material compound before cyclization by an intramolecular cyclization reaction thereof in the presence of one or more kinds of organic solvents selected from the group consisting of 1,1,2-trichloroethene, methylcyclohexane, cyclohexane, n-heptane and the like.

    摘要翻译： 本发明涉及一种以工业规模以工业上可接受的产率和纯度足以用作药物活性成分的纯粹和经济的方法，通过Friedel-Crafts反应型分子内环化反应制备扎洛芬或扎洛芬衍生物的方法 的方式，通过在环化前使用原料化合物的量的6.5倍以下的多磷酸，不产生可检测量的杂质如二聚体。 更具体地，本发明涉及如上所述的制备扎洛芬或扎洛芬衍生物的方法，其包括在环化前的原料化合物通过其分子内环化反应在选自以下的一种或多种有机溶剂存在下使原料化合物环化： 由1,1,2-三氯乙烯，甲基环己烷，环己烷，正庚烷等组成的组。