利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

16 条记录 (耗时 0.028 秒)

    POLYCYCLIC CARBAMOYLPYRIDONE DERIVATIVE HAVING HIV INTEGRASE INHIBITORY ACTIVITY
    5.
    发明公开
    POLYCYCLIC CARBAMOYLPYRIDONE DERIVATIVE HAVING HIV INTEGRASE INHIBITORY ACTIVITY 审中-公开
    具有HIV整合酶抑制活性的多环氨基甲酰基吡啶酮衍生物

    公开(公告)号：EP3284519A1

    公开(公告)日：2018-02-21

    申请号：EP17195276.5

    申请日：2006-04-28

    申请人： VIIV Healthcare Company ,  Shionogi & Co., Ltd

    发明人： JOHNS, Brian Alvin ,  Kawasuji, Takashi ,  Taishi, Teruhiko ,  Taoda, Yoshiyuki

    IPC分类号： A61P31/18 ,  A61K31/4985 ,  C07D498/04

    CPC分类号： C07D498/14 ,  A61K9/0053 ,  A61K31/4985 ,  A61K31/519 ,  A61K31/5365 ,  A61K31/551 ,  A61K45/06 ,  C07D471/04 ,  C07D471/14 ,  C07D471/22 ,  C07D498/04 ,  C07D498/20 ,  C07D498/22

    摘要： The present invention is to provide a novel compound (I-1) shown below, having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof.

    wherein
    A ring is substituted ring of (a), (b) or (c)

    wherein Z is O or NR 19 ,
    R 19 is hydrogen, C 1-10 alkyl, C 2-8 alkenyl, C 1-10 alkylcarbonyl or C 1-10 alkylsulfonyl, and the other substituents on the A ring form a ring;
    R 14 and R X are hydrogen;
    a broken line represents the presence or absence of a bond, provided that when the broken line represents the presence of a bond, R X is not present;
    R 1 is hydrogen or C 1-10 alkyl;
    X is C 1-6 alkylene;
    R 2 is phenyl or phenyl substituted with at least halogen;
    R 3 is hydrogen, halogen, hydroxy, C 1-10 alkyl, C 2-8 alkenyl, C 1-10 alkoxy, C 2-8 alkenyloxy or amino;
    or a pharmaceutically acceptable salt, or solvate thereof.

    摘要翻译： 本发明提供具有抗病毒活性，特别是HIV整合酶抑制活性的以下所示的新型化合物（I-1），含有其的药物，特别是抗HIV药物，以及方法 及其中间物。 其中A环为（a），（b）或（c）的取代环，其中Z为O或NR19，R19为氢，C1-10烷基，C2-8链烯基，C1-10烷基羰基或C1-10烷基磺酰基， A环形成一个环; R14和RX是氢; 虚线表示存在或不存在键，条件是当虚线表示存在键时，RX不存在; R1是氢或C1-10烷基; X是C 1-6亚烷基; R2是苯基或至少被卤素取代的苯基; R3是氢，卤素，羟基，C1-10烷基，C2-8链烯基，C1-10烷氧基，C2-8链烯氧基或氨基; 或其药学上可接受的盐或溶剂化物。