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    IMIDAZOL-4-YLMETHANOLS USED AS INHIBITORS OF STEROID C17-20 LYASE
    3.
    发明授权
    IMIDAZOL-4-YLMETHANOLS USED AS INHIBITORS OF STEROID C17-20 LYASE 有权
    FOR USE AS类固醇C17-20裂解酶咪唑-4-甲醇衍生物抑制剂

    公开(公告)号：EP1222174B1

    公开(公告)日：2009-05-27

    申请号：EP00969903.4

    申请日：2000-10-19

    申请人： Takeda Pharmaceutical Company Limited

    发明人： TASAKA, Akihiro ,  OJIDA, Akio ,  KAKU, Tomohiro ,  KUSAKA, Masami ,  YAMAOKA, Masuo

    IPC分类号： C07D233/54 ,  A61P5/26 ,  A61P5/30 ,  A61P35/00 ,  C07D405/10 ,  C07D409/10 ,  C07D403/10 ,  C07D413/10 ,  C07D295/18 ,  C07D417/12 ,  C07D405/06

    CPC分类号： C07D233/64 ,  C07D403/10 ,  C07D405/06 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/12 ,  Y02P20/55

    摘要： The present invention provides a compound represented by formula (I), wherein R is a hydrogen atom or a protecting group, R1 is a lower alkyl group or a cyclic alkyl group, R2 is a group represented by formula (1), (wherein a ring A1 is a 5- or 6-membered ring containing an oxygen atom optionally having substituents, and a ring A2 and a ring A3 may have substituents), a group represented by formula (2), (wherein the ring B1 is a 5- or 6-membered ring containing an oxygen atom optionally having substituents and a ring B2 and a ring B3 may have substituents) or a group of formula (3), (wherein each of R?3 and R5¿ is a hydrogen atom, a lower alkyl group optionally having substituents, a hydroxyl group optionally having substituents, a thiol group optionally having substituents, an amino group optionally having substituents, an acyl group or a halogen atom, R4 is an aromatic hydrocarbon group optionally having substituents, a heterocyclic group optionally having substituents or a carbamoyl group optionally having substituents, R6 is an optionally halogenated lower alkyl group and n is an integer of 0 to 3), or a salt thereof, which has an inhibitory activity of steroid C¿17-20?-lyase and are useful for preventing and treating a mammal suffering from, for example, primary tumor, its metastasis and recurrence thereof, and various symptoms accompanied with these cancer, various diseases such as prostatic hypertrophy, virilism, hirsutism, male pattern alopecia, precocious puberty, endometriosis, uterus myoma, mastopathy, polycystic ovary syndrome, etc.