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    • 1. 发明公开
    • Quinone derivatives and pharmacological use
    • 喹诺酮衍生物和药理学用途
    • EP0419905A3
    • 1992-06-24
    • EP90117119.9
    • 1990-09-05
    • Eisai Co., Ltd.
    • Abe, ShinyaOkamoto, YasushiTagami, KatsuyaHibi, ShigekiNagakawa, JunichiHirota, KazuoHishinuma, IeharuMiyamoto, KanameYamanaka, TakashiYokohama, HiromitsuYoshimura, TsutomuHorie, TohruAkita, YasunoriKatayama, KoichiYamatsu, Isao
    • C07C66/00A61K31/19C07C59/90C07C59/68C07C65/21C07C69/736C07C255/38C07D309/00
    • C07D295/185C07C45/00C07C47/575C07C50/38C07C59/54C07C59/68C07C59/90C07C65/21C07C66/00C07C69/734C07C69/738C07C255/31C07C255/41C07C255/57C07C317/46C07C323/55C07C323/56C07C323/62C07C2601/14C07C2601/16C07D211/46C07D213/55C07D277/30C07D277/46C07D309/04C07D333/24
    • 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).
    • 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)。
    • 3. 发明公开
    • Quinone derivatives
    • 希农衍。
    • EP0503426A1
    • 1992-09-16
    • EP92103555.6
    • 1992-03-02
    • Eisai Co., Ltd.
    • Okamoto, YasushiTagami, KatsuyaHibi, ShigekiNumata, HirotoshiKawahara, TetsuyaKobayashi, NaokiShinoda, MasanobuHarada, KoukichiMiyamoto, KanameAbe, Koichi
    • C07D213/55C07D213/56A61K31/44
    • C07D213/56C07D213/55
    • 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.
    • 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。
    • 8. 发明公开
    • Quinone derivatives and pharmacological use
    • Chinonderivate und ihre pharmakologische Verwendung。
    • EP0419905A2
    • 1991-04-03
    • EP90117119.9
    • 1990-09-05
    • Eisai Co., Ltd.
    • Abe, ShinyaOkamoto, YasushiTagami, KatsuyaHibi, ShigekiNagakawa, JunichiHirota, KazuoHishinuma, IeharuMiyamoto, KanameYamanaka, TakashiYokohama, HiromitsuYoshimura, TsutomuHorie, TohruAkita, YasunoriKatayama, KoichiYamatsu, Isao
    • C07C66/00A61K31/19C07C59/90C07C59/68C07C65/21C07C69/736C07C255/38C07D309/00
    • C07D295/185C07C45/00C07C47/575C07C50/38C07C59/54C07C59/68C07C59/90C07C65/21C07C66/00C07C69/734C07C69/738C07C255/31C07C255/41C07C255/57C07C317/46C07C323/55C07C323/56C07C323/62C07C2601/14C07C2601/16C07D211/46C07D213/55C07D277/30C07D277/46C07D309/04C07D333/24
    • 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).
    • 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)。