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    PYRAZOLE DERIVATIVES AS PROGESTERONE RECEPTOR ANTAGONISTS
    1.
    发明公开
    PYRAZOLE DERIVATIVES AS PROGESTERONE RECEPTOR ANTAGONISTS 审中-公开
    吡唑衍生物孕激素受体的拮抗剂

    公开(公告)号：EP1874732A1

    公开(公告)日：2008-01-09

    申请号：EP06744619.5

    申请日：2006-04-10

    申请人： Pfizer Limited

    发明人： BRADLEY, Paul A., Pfizer Global Res. and Devl. ,  DACK, Kevin N., Pfizer Global Res. and Devl. ,  MARSH, Ian R., Pfizer Global Res. and Devl.

    IPC分类号： C07D231/18 ,  C07D403/06 ,  C07D417/06 ,  A61K31/415 ,  A61P15/00

    CPC分类号： C07D231/28 ,  C07D231/18 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D413/06 ,  C07D417/06

    摘要： Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: R1 represents H, C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R2 represents H, C1-6alkyl (optionally substituted by R3), phenyl (optionally substituted by CN), or Het; R3 represents OH, CN, Het, -R4- C1-6alkyl, or CONR5R6; R4 represents ―CO2-, or ―O-; R5 and R6 independently represent H, C1-6alkyl (optionally substituted by OR7) or C3-8cycloalkyl; R7 represents H or C1-6alkyl; Het represents a five or six membered aromatic heterocyclic group containing (i) from one to four nitrogen heteroatom(s) or (ii) one or two nitrogen heteroatom(s) and one oxygen or one sulphur heteroatom or (iii) one or two oxygen or sulphur heteroatom (s), said heterocyclic group being optionally substituted by one or more groups selected from CN and C1-6alkyl; R8 represents C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R9 and R10 independently represent H, C1-6alkyl, C1-6alkyloxy, CN, CF3 or halo; may be useful for treating endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), or chronic pelvic pain syndrome.