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    PHENANTHROLINE DERIVATIVES
    1.
    发明公开
    PHENANTHROLINE DERIVATIVES 有权
    菲咯啉衍生物

    公开(公告)号：EP1027351A1

    公开(公告)日：2000-08-16

    申请号：EP98967153.2

    申请日：1998-10-26

    申请人： FIBROGEN, INC. ,  ZENECA LIMITED

    发明人： EDWARDS, Philip Neil ,  LARGE, Michael Stewart ,  HALES, Neil, James ,  MARTIN, George, R. ,  HUANG, Xinfan

    IPC分类号： C07D471/04

    CPC分类号： C07D471/04 ,  A61K31/4745

    摘要： The present invention provides a phenanthroline derivative of formula (I) wherein, for example, R1 is hydrogen, carboxy, cyano, nitro, (1-4C)alkyl, (1-6C)alkoxycarbonyl, (1-4C)alkylamino, (2-4C)alkanoyl, (1-4C)alkoxy-(2-4C)alkoxy-(2-4C)alkoxycarbonyl or N-[amino-(2-8C)alkyl]carbamoyl; R2 is, for example, hydrogen, carboxy, (1-6C)alkoxycarbonyl, carbamoyl, N-(1-8C)alkylcarbamoyl, N,N-di-(1-8C)alkylcarbamoyl, N-(1-4C)alkylcyclohexylcarbamoyl, 1,2,3,4,-tetrahydro-isoquinolin-2-ylcarbonyl or N,N-[di-(1-4C)alkyl]thiocarbamoyl; R?3 and R4¿, which may be the same or different, are, for example, hydrogen or halo; and R5 is, for example, hydrogen, di-(1-4C)alkylamino or halo; or a pharmaceutically-acceptable salt thereof. The invention further provides pharmaceutical compositions comprising phenanthroline derivatives, processes for making the same and their use in producing an anti-fibroproliferative effect.