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    Benzophenone oxime derivatives, pharmaceutical compositions and use
    42.
    发明公开
    Benzophenone oxime derivatives, pharmaceutical compositions and use 失效
    Benzophenon Oxim Derivate，pharmaceuticalische Zusammensetzungen und ihre Verwendung。

    公开(公告)号：EP0478001A1

    公开(公告)日：1992-04-01

    申请号：EP91119345.6

    申请日：1987-03-17

    申请人： Eisai Co., Ltd.

    发明人： Yamagishi, Youji ,  Akasaka, Kozo ,  Suzuki, Takeshi ,  Miyamoto, Mitsuaki ,  Nakamoto, Kouji ,  Okano, Kazuo ,  Abe, Shinya ,  Ikuta, Hironori ,  Hayashi, Kenji ,  Yoshimura, Hiroyuki ,  Fujimori, Tohru ,  Harada, Koukichi ,  Yamatsu, Isao

    IPC分类号： C07C251/60 ,  C07C255/62 ,  C07D257/04 ,  C07D207/46 ,  C07D339/08 ,  A61K31/15

    CPC分类号： C07D257/04 ,  C07C59/64 ,  C07C235/14 ,  C07C235/34 ,  C07C251/40 ,  C07C251/60 ,  C07C255/00 ,  C07C255/41 ,  C07C255/62 ,  C07C257/06 ,  C07C257/18 ,  C07C311/13 ,  C07C311/17 ,  C07C327/58 ,  C07D207/46 ,  C07D213/40 ,  C07D213/75 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D339/08

    摘要： A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime ether derivative.


    in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is = CXY or = N-O-W,
    X is hydrogen, cyano or -COR6, R6 being hydroxyl or an amino, Y is -R10-COOR3, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, -CO-NR4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower arylalkyl, -CH2-NHS02-C6H5 or -C(R8)-= NR7, R7 being a lower alkoxy or an aryl, R8 is -VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,
    W is -CH2-CO-CH2-COOR13, R13 being hydrogen or a lower alkyl, -CH2-C(=NOR14)-CH2-COOR15, R15 being hydrogen or a lower alkyl, R14 being a lower alkyl, -CH(CN)-(CH2)q-COOR16, R16 being hydrogen or a lower alkyl, q being an integer of 1 to 3, or -(CH2)p-Z, Z being -SH, -SCN or a monovalent group derived from a five- or six-membered ring which may be substituted by a ring having one or more sulfur atoms in the ring, p being 1 or 2.

    A pharmaceutical composition containing compounds of formula (XX) or their pharmaceutically acceptable salts as active ingredients, and the use of compounds of formula (XX) or their pharmaceutically acceptable salts in the preparation of a medicament for treatment of diseases caused by blood stream disorders are also disclosed.

    摘要翻译： 二苯基甲烷衍生物。 式（I）的化合物是新的（其中R 1和R 2各自为H，OH或低级烷氧基; U = -CXY或= NOW; X = H，CN或-COR 6; R 6 = OH或NH 2; Y = COOR3，-CONR4R5，-CH2NHSO2-C6H5或-C（R8）= NR7; R3 = H或低级烷氧基; R10 =选择性支链的1-3C亚烷基; R4和R5各自为H，低级烷基或低级芳基烷基; R7 = 低级烷氧基或芳基; R8 = -VR9; V = O，S或N; R9 =烷基或芳基; W = -CH2-CO-CH2-COOR13，-CH2-C（= NOR14）-CH2-COOR15，-CH （CN） - （CH 2）q -COOR 16或 - （CH 2）pZ; R 13 = H或低级烷基; R 14 =低级烷基; R 15 = H或低级烷基; R 16 = H或低级烷基; q = = -SH，-SCN或衍生自5-或6-元环选择性的单价gp，通过环中具有1个或更多个S的环; p = 1或2。