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    Quinone derivatives and pharmacological use
    25.
    发明公开
    Quinone derivatives and pharmacological use 失效
    喹诺酮衍生物和药理学用途

    公开(公告)号：EP0419905A3

    公开(公告)日：1992-06-24

    申请号：EP90117119.9

    申请日：1990-09-05

    申请人： Eisai Co., Ltd.

    发明人： Abe, Shinya ,  Okamoto, Yasushi ,  Tagami, Katsuya ,  Hibi, Shigeki ,  Nagakawa, Junichi ,  Hirota, Kazuo ,  Hishinuma, Ieharu ,  Miyamoto, Kaname ,  Yamanaka, Takashi ,  Yokohama, Hiromitsu ,  Yoshimura, Tsutomu ,  Horie, Tohru ,  Akita, Yasunori ,  Katayama, Koichi ,  Yamatsu, Isao

    IPC分类号： C07C66/00 ,  A61K31/19 ,  C07C59/90 ,  C07C59/68 ,  C07C65/21 ,  C07C69/736 ,  C07C255/38 ,  C07D309/00

    CPC分类号： C07D295/185 ,  C07C45/00 ,  C07C47/575 ,  C07C50/38 ,  C07C59/54 ,  C07C59/68 ,  C07C59/90 ,  C07C65/21 ,  C07C66/00 ,  C07C69/734 ,  C07C69/738 ,  C07C255/31 ,  C07C255/41 ,  C07C255/57 ,  C07C317/46 ,  C07C323/55 ,  C07C323/56 ,  C07C323/62 ,  C07C2601/14 ,  C07C2601/16 ,  C07D211/46 ,  C07D213/55 ,  C07D277/30 ,  C07D277/46 ,  C07D309/04 ,  C07D333/24

    摘要： The quinone compound is useful to treat hepatic disease and defined by the formula: wherein A is a group represented by the formula:
    (wherein R 3 , R 4 and R 5 which may be the same or different from each other are each a hydrogen atom, a lower alkyl group or a lower alkoxy group) or a group represented by the formula:
    (wherein R 3 , R 4 and R 5 which may be the same or different from each other are each a hydrogen atom, a lower alkyl group or a lower alkoxy group, X and Y which may be the same or different from each other are each a hydroxyl group, a group represented by the formula
    (wherein n is 0 or 1 and R 6 is a lower alkyl group), or an acyl group),
    R 1 is an alkyl group having 2 to 20 carbon atoms, a cycloalkyl group, a cycloalkylalkyl group, an alkenyl group, an alkynyl group, an arylalkyl group, a group represented by the formula
    (wherein p is an integer of 1 to 10), a heteroarylalkyl group, a group represented by the formula
    {wherein q is an integer of 1 to 6 and B is a group represented by the formula:
    (wherein r is 0 or an integer of 1 to 2, R 7 is a lower alkyl group, a cycloalkyl group or an aryl group), or a group represented by the formula -O-R 8 (wherein R 8 is a lower alkyl group or an aryl group)}, or a group represented by the formula (wherein s is an integer of 1 to 3), R 2 is a group represented by the formula -OR 8 (wherein R 8 is a hydrogen atom or a lower alkyl group) or a group represented by the formula:
    (wherein R 9 and R 10 which may be the same of different from each other are each a hydrogen atom, a lower alkyl group, a hydroxyalkyl group or a heteroaryl group, provided that R 9 and R 10 may be combined with each other to form a ring together with a nitrogen atom bonded thereto, which may further contain a nitrogen atom and/or an oxygen atom and may be substituted).

    摘要翻译： 醌化合物可用于治疗肝病并由下式定义：其中A是由下式表示的基团：其中R 3，R 4和R 5可以是 相同或不同的是氢原子，低级烷基或低级烷氧基）或由下式表示的基团：其中R 3，R 4和R 5如下： 可以相同或不同的是氢原子，低级烷基或低级烷氧基，可以相同或不同的X和Y各自为羟基，由 （其中n为0或1，R 6为低级烷基）或酰基），R 1为碳原子数2〜20的烷基，芳基 环烷基，环烷基烷基，烯基，炔基，芳基烷基，由式表示的基团，其中p为1〜10的整数，杂芳基烷基基团 p为由式＆lparstr＆CH 2＆rparstr＆B B表示的基团，其中q为1〜6的整数，B为下式所示的基团：其中r为0或1〜2的整数，R 或者由式-OR 8表示的基团（其中R 8为低级烷基或芳基）}，或者式 由式＆lparstr＆CH2-CH2-O）@ CH3表示的基团（其中s为1至3的整数），R 2为由式-OR 8表示的基团（其中R 8为 氢原子或低级烷基）或由下式表示的基团：其中可以彼此不同的（其中R 9和R 1 各自为氢原子， 低级烷基，羟基烷基或杂芳基，条件是R 9和R 1可以彼此结合形成与其键合的氮原子一起形成的环，其还可含有氮 原子和/或氧原子并且可以被取代）。

    Diphenyl-methane derivative, pharmaceutical composition and use
    29.
    发明公开
    Diphenyl-methane derivative, pharmaceutical composition and use 失效
    二苯甲烷衍生物，药物Zusammensetzung und Verwendung。

    公开(公告)号：EP0238973A2

    公开(公告)日：1987-09-30

    申请号：EP87103834.5

    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： C07C251/00 ,  C07C311/15 ,  C07C235/42 ,  C07C255/37 ,  C07C233/65 ,  C07D213/75 ,  C07C257/00 ,  C07C257/06 ,  C07C327/00 ,  C07C59/64 ,  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-NHSO2-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-C00R13, 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： 新的二苯基甲烷衍生物可用于抑制血液凝聚，并由式定义，包括二苯基乙烯衍生物和二苯甲酮肟醚衍生物。 其中R 1和R 2各自为氢，羟基或低级烷氧基，U为= XY =或NOW，X为氢，氰基或-COR 6，R6为羟基或氨基，Y为-R10-COOR3，R3 是氢或低级烷氧基，R10是具有1至3个碳原子的直链或支链的亚烷基，-CO-NR4R5，R4和R5各自为氢，低级烷基或低级芳基烷基，-CH2-NHSO2-C6H5或 - C（R8）= NR7，R7为低级烷氧基或芳基，R8为-VR9，V为氧，硫或氮，R9为烷基或芳基，W为-CH2-CO-CH2-C00R13，R13为 氢或低级烷基，-CH 2 -C（= NOR 14）-CH 2 -COOR 15，R 15为氢或低级烷基，R 14为低级烷基，-CH（CN） - （CH 2）q -COOR 16，R 16为氢或 低级烷基，q为1至3的整数，或 - （CH 2）pZ，Z为-SH，-SCN或衍生自五元或六元环的一价基团，其可被具有一个 或更多的硫原子，p为1或2.含有式（ XX）或其药学上可接受的盐作为活性成分，并且还公开了式（XX）化合物或其药学上可接受的盐在制备用于治疗由血液病症引起的疾病的药物中的用途。