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    Quinone derivatives and pharmacological use
    4.
    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）。

    Aminobenzoic acid derivatives
    6.
    发明公开
    Aminobenzoic acid derivatives 失效
    氨基苯甲酸衍生物

    公开(公告)号：EP0645391A2

    公开(公告)日：1995-03-29

    申请号：EP94111783.0

    申请日：1994-07-28

    申请人： Eisai Co., Ltd.

    发明人： Miyazawa, Shuhei ,  Hoshino, Yorihisa ,  Shibata, Hisashi ,  Hirota, Kazuo ,  Kameyama, Takaaki ,  Abe, Shinya ,  Yamanaka, Takashi

    IPC分类号： C07D498/08 ,  C07D451/14 ,  C07D471/08 ,  C07D211/58 ,  C07D451/04 ,  C07D221/24 ,  C07D207/14 ,  C07D491/08 ,  C07D451/02 ,  C07D471/18 ,  A61K31/46

    CPC分类号： C07D451/02 ,  C07D207/14 ,  C07D211/58 ,  C07D221/24 ,  C07D451/04 ,  C07D451/14 ,  C07D471/08 ,  C07D491/08 ,  C07D498/08

    摘要： To provide a compound which exhibits a serotonin antagonism and an acetylcholine release accelerating activity at a well-balanced activity ratio. An aminobenzoic acid derivative represented by the general formula (I) or (II) or a pharmacologically acceptable salt thereof:



    [wherein R 1 represents a group represented by the formula:

    etc., {wherein A represents a group represented by formula -CH 2 -X-CH 2 - (wherein X represents O, >N-R 6 or >CHR 7 (wherein R 6 represents lower alkyl and R 7 represents hydrogen or lower alkoxy)), etc.; D and E each represents a group represented by formula -(CH 2 ) 3 -, etc., and R 2 represents lower alkyl, etc.}; R 9 represents alkynyl; R 10 represents amino, etc.; R 11 represents halogen; R 12 and R 13 each represent lower alkyl; a is an integer of 1 to 5; and b is an integer of 0 to 5].

    摘要翻译： 提供在平衡良好的活性比下显示血清素拮抗作用和乙酰胆碱释放促进活性的化合物。 由通式（I）或（II）表示的氨基苯甲酸衍生物或其药理学上可接受的盐：[其中R1代表由式：代表的基团，其中A代表式-CH2-X -CH2-（其中X代表O，> N-R6或> CHR7（其中R6代表低级烷基，R7代表氢或低级烷氧基））等。 D和E各自表示由式 - （CH 2）3 - 等表示的基团，并且R 2表示低级烷基等。 R9代表炔基; R10代表氨基等; R11代表卤素; R12和R13各代表低级烷基; a是1至5的整数; b是0〜5的整数]。

    Aminobenzoic acid derivatives
    7.
    发明公开
    Aminobenzoic acid derivatives 失效
    氨基苯甲酸衍生物。

    公开(公告)号：EP0554794A1

    公开(公告)日：1993-08-11

    申请号：EP93101312.2

    申请日：1993-01-28

    申请人： Eisai Co., Ltd.

    发明人： Miyazawa, Shuhei ,  Hibi, Shigeki ,  Yoshimura, Hiroyuki ,  Mori, Takashi ,  Hoshino, Yorihisa ,  Nagai, Mitsuo ,  Kikuchi, Kouichi ,  Shibata, Hisashi ,  Hirota, Kazuo ,  Yamanaka, Takashi ,  Yamatsu, Isao ,  Mizuno, Masanori

    IPC分类号： C07D451/04 ,  A61K31/46

    CPC分类号： C07D451/04

    摘要： An aminobenzoic acid derivative represented by the following general formulas (I), (I-2) or (I-3), or a pharmacologically acceptable salt thereof, which exhibits a serotonin antagonism and an acetylcholine release accelerating activity at a well-balanced activity ratio and which is efficacious as a drug for patients with gastrointestinal unindentified complaints:

    and

       wherein R¹ represents a group such as an alkynyl or cyanoalkyl group; R² represents a group such as an amino or acylamino group; R³ represents a halogen atom; X represents -O- or -NH-; and A represents an oxygen or sulfur atom.

    摘要翻译： 由以下通式（I），（I-2）或（I-3）表示的氨基苯甲酸衍生物或其药理学上可接受的盐，其平衡活性显示出5-羟色胺拮抗作用和乙酰胆碱释放促进活性 并且其作为胃肠道未认知的患者的药物是有效的：和其中R 1表示诸如炔基或氰基烷基的基团; R 2表示例如氨基或酰氨基的基团; R 3表示卤原子; X表示-O-或-NH-; A表示氧或硫原子。

    Quinone derivatives and pharmacological use
    9.
    发明公开
    Quinone derivatives and pharmacological use 失效
    Chinonderivate und ihre pharmakologische Verwendung。

    公开(公告)号：EP0419905A2

    公开(公告)日：1991-04-03

    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）。