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    • 1. 发明公开
    • THIOQUINOLONE DERIVATIVE
    • THIOCHINOLON,衍生金融工具
    • EP0786454A1
    • 1997-07-30
    • EP95933632.2
    • 1995-10-06
    • ZENYAKU KOGYO KABUSHIKI KAISHA
    • KONISHI, Masataka, Kenkyusho of Zenyaku Kogyo KKFUKUDA, Naoki, Kenkyusho of Zenyaku Kogyo KKOKU, Yukio, Kenkyusho of Zenyaku Kogyo KKYAMAZAKI, Hiroaki, Kenkyusho of Zenyaku Kogyo KKIMAIZUMI, Kazuhiro, Kenkyusho of Zenyaku Kogyo KKKOBAYASHI, Hideshi, Kenkyusho of Zenyaku Kogyo KK
    • C07D215/36C07D215/38C07D221/08C07D491/048A61K31/47A61K31/435
    • C07D401/12C07D215/36C07D215/38C07D221/08C07D471/04C07D491/04
    • Disclosed is a thioquinolone derivative which exhibits highly selective antibacterial activity against Helicobacter pylori and which is represented by the formula I


      wherein R 1 and R 2 respectively represent hydrogen atom or R 1 and R 2 are joined to form ―O―(CH 2 ) 2 -;
      R 3 represents halogen atom, C 1 -C 12 alkyl group, C 1 -C 12 alkoxy group, lower alkylsulfonyloxy group, carboxy lower alkoxy group, lower alkylthio group, benzyloxy group, benzylthio group, phenoxy group, styryl group, nitro group, phenyl group, naphthyl group, piperazinyl group, morpholino group or hydroxyl group or represents ―CH 2 R 5 , ―COR 6 or ―NR 7 R 8 wherein R 5 represents benzyl group, phenyl group, hydroxyl group, lower alkoxy group, lower alkylcarbonyloxy group, phenoxy group, di-lower alkylamino group or benzimidazolylthio group, R 6 represents lower alkyl group or amino group and R 7 and R 8 respectively represent lower alkyl group; and
      R 4 represents hydrogen atom or lower alkyl group or is coupled with R 3 to form cyclohexene ring, benzene ring or pyridine ring,
      R 3 being not halogen atom at any of positions 5 to 8, methyl group at position 6 or methoxy group at position 6 of the quinoline ring when R 1 , R 2 and R 4 are respectively hydrogen atom,
      R 3 and R 4 being not at positions 6 and 7 or positions 6 and 8 of the quinoline ring when R 1 and R 2 are respectively hydrogen atom and R 4 is lower alkyl group.
    • 本发明公开了一种对幽门螺旋杆菌具有高度选择性抗菌活性的噻喹诺酮衍生物,其由式I 表示,其中R1和R2分别表示氢原子或R1和R2连接形成-O-(CH 2)2 - ; R3表示卤原子,C1-C12烷基,C1-C12烷氧基,低级烷基磺酰氧基,羧基低级烷氧基,低级烷硫基,苄氧基,苄硫基,苯氧基,苯乙烯基,硝基,苯基,萘基 ,哌嗪基,吗啉代基或羟基,或表示-CH 2 R 5,-COR 6或-NR 7 R 8,其中R 5表示苄基,苯基,羟基,低级烷氧基,低级烷基羰基氧基,苯氧基,二低级烷基氨基或苯并咪唑硫基 R6代表低级烷基或氨基,R7和R8分别代表低级烷基; R4代表氢原子或低级烷基,或与R3结合形成环己烯环,苯环或吡啶环,R3不为5至8位任何位置的卤素原子,6位甲基或6位甲氧基 当R1,R2和R4分别为氢原子,当R1和R2分别为氢原子且R4为低级烷基时,R3和R4不在喹啉环的6位和7位或6位和8位的喹啉环。