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    DC-89 derivatives as antitumoral agents
    1.
    发明公开
    DC-89 derivatives as antitumoral agents 失效
    DC-89衍。

    公开(公告)号：EP0468400A1

    公开(公告)日：1992-01-29

    申请号：EP91112235.6

    申请日：1991-07-22

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： Saito, Hiromitsu ,  Nagamura, Satoru ,  Asai, Akira ,  Kobayashi, Eiji ,  Gomi, Katsushige

    IPC分类号： C07D487/04 ,  C07D471/04 ,  A61K31/44

    CPC分类号： C07D471/04

    摘要： Novel DC-89 derivatives represented by general formula (I):
    wherein X represents Cλ or Br; R 1 represents hydrogen, CONR 2 R 3 (in which R 2 and R 3 independently represent hydrogen, a straight-chain or branched alkyl group having 1 to 4 carbon atoms or phenyl group),
    (in which n represents an integer of 4 to 7),
    (in which R 4 represents oxygen, N-CH 3 or N-CH 2 CH 2 NH 2 ),
    or SiR 5 R 6 R 7 (in which R 5 , R 6 and R 7 independently represent a straight-chain or branched alkyl group having 1 to 4 carbon atoms); and
    or
    (in which Y represents hydrogen or C0 2 CH 3 ); provided that when R 1 is hydrogen, CONR 2 R 3 or SiR 5 R 6 R 7 ,
    and pharmaceutically acceptable salts thereof have an excellent anti-tumor activity and are expected to be useful as anti-tumor compositions.

    摘要翻译： 由通式（I）表示的新型DC-89衍生物：其中X表示Cl或Br; R 1表示氢，CONR 2 R 3（其中R 2和R 3独立地表示氢，具有1至4个碳原子的直链或支链烷基或苯基）， （其中n表示4至7的整数），（其中R 4表示氧，N-CH 3或N-CH 2 CH 2 NH 2），CHEM或SiR 5 R 6 R 7（其中R 5，R 6和R 7独立地表示具有1至4个碳原子的直链或支链烷基）; 和（其中Y表示氢或CO 2 CH 3）; 条件是当R 1为氢时，CONR 2 R 3或SiR 5 R 6 R 7，CHEM及其药学上可接受的盐具有优异的抗肿瘤活性，并且预期 用作抗肿瘤组合物。