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    Quinone derivatives
    2.
    发明公开
    Quinone derivatives 失效
    希农衍。

    公开(公告)号：EP0503426A1

    公开(公告)日：1992-09-16

    申请号：EP92103555.6

    申请日：1992-03-02

    申请人： Eisai Co., Ltd.

    发明人： Okamoto, Yasushi ,  Tagami, Katsuya ,  Hibi, Shigeki ,  Numata, Hirotoshi ,  Kawahara, Tetsuya ,  Kobayashi, Naoki ,  Shinoda, Masanobu ,  Harada, Koukichi ,  Miyamoto, Kaname ,  Abe, Koichi

    IPC分类号： C07D213/55 ,  C07D213/56 ,  A61K31/44

    CPC分类号： C07D213/56 ,  C07D213/55

    摘要： The object of the present invention is to provide a quinone derivative exhibiting an excellent activity as a drug.
    The present invention provides a quinone derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof:

       wherein A stands for a group represented by the formula:

       (wherein R³, R⁴ and R⁵ is the same or different from each other and each stand for a hydrogen atom, a hydroxyl group, a lower alkyl group, a lower alkoxy group, an alkoxyalkyl group, an alkoxyalkoxy group, a cycloalkylalkoxy group, a thiol group or a thioalkyl group, with the proviso that a case wherein R³ and R⁴ are each a lower alkoxy group simultaneously is excepted) or a group represented by the formula:

       (wherein R³, R⁴ and R⁵ is the same or different from each other and each stand for a hydrogen atom, a hydroxyl group, a lower alkyl group, a lower alkoxy group, an alkoxyalkyl group, an alkoxyalkoxy group, a cycloalkylalkoxy group, a thiol group or a thioalkyl group, with the proviso that a case wherein R³ and R⁴ are each a lower alkoxy group simultaneously is excepted; X and Y is the same or different from each other and each stand for a hydroxyl group or a protected hydroxyl group);
    R¹ stands for a heteroarylalkyl group; and
    B stands for a carboxyl group or a protected carboxyl group.

    摘要翻译： 本发明的目的是提供作为药物具有优异活性的醌衍生物。 本发明提供由通式（I）表示的醌衍生物或其药理学上可接受的盐：其中A表示由下式表示的基团：其中R 3，R 4， R 5相同或不同，分别表示氢原子，羟基，低级烷基，低级烷氧基，烷氧基烷基，烷氧基烷氧基，环烷基烷氧基，硫醇基 或硫代烷基，条件是其中R 3和R 4同时为低级烷氧基的情况除外）或由下式表示的基团：其中R 3，R 4和R 5相同或不同，分别表示氢原子，羟基，低级烷基，低级烷氧基，烷氧基烷基，烷氧基烷氧基，环烷基烷氧基， 硫醇基或硫代烷基，条件是其中R 3和R 4各自为低级烷氧基， ;;;; X和Y彼此相同或不同，各自表示羟基或被保护的羟基）; R 1表示杂芳基烷基; B代表羧基或被保护的羧基。

    Diphenyl-methane derivative, pharmaceutical composition and use
    5.
    发明公开
    Diphenyl-methane derivative, pharmaceutical composition and use 失效
    二苯甲烷衍生物，药物组合物和用途

    公开(公告)号：EP0479332A3

    公开(公告)日：1992-04-15

    申请号：EP91119344.9

    申请日：1987-03-17

    申请人： Eisai Co., Ltd.

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

    IPC分类号： C07C235/34 ,  C07C311/17 ,  C07C257/14 ,  A61K31/15 ,  A61K31/18 ,  A61K31/275 ,  C07C235/38 ,  C07C257/06 ,  C07C69/618 ,  C07C57/42

    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： 新的二苯基甲烷衍生物可用于抑制血液凝聚，并由式（2）定义，包括二苯基乙烯衍生物和二苯甲酮肟醚衍生物。 其中R1和R2各自为氢，羟基或低级烷氧基，U为= CXY或= NOW，X为氢，氰基或-COR6，R6为羟基或氨基，Y为-R10-COOR3，R3为氢或 低级烷氧基，R 10为具有1至3个碳原子的亚烷基，直链或支链的-CO-NR 4 R 5，R 4和R 5各自为氢，低级烷基或低级芳烷基，-CH 2 -NHSO 2 -C 6 H 5或-C（R 8 ）= NR7，R7是低级烷氧基或芳基，R8是-VR9，V是氧，硫或氮，R9是烷基或芳基，W是-CH2-CO-CH2-COOR13，R13是氢或 低级烷基，-CH 2 -C（= NOR 14）-CH 2 -COOR 15，R 15是氢或低级烷基，R 14是低级烷基，-CH（CN） - （CH 2）q -COOR 16，R 16是氢或低级烷基 ，q为1至3的整数，或 - （CH 2）p Z，Z为-SH，-SCN或衍生自可被具有一个或多个硫的环取代的五元或六元环的一价基团 原子在环中，p为1或2.含有式（XX）化合物的药物组合物， 或其药学上可接受的盐作为活性成分，并且还公开了式（XX）的化合物或其药学上可接受的盐在制备用于治疗由血流障碍引起的疾病的药物中的用途。