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    • 59. 发明公开
    • Sulfonamide derivatives
    • 磺酰胺衍生物
    • EP0469901A1
    • 1992-02-05
    • EP91307061.1
    • 1991-08-01
    • TAISHO PHARMACEUTICAL CO. LTDNIPPON SUISAN KAISHA, LTD.
    • Sato, MasakazuKawashima, YutakaGoto, JunChiba, YoshiyukiSatake, MikioIwata, ChuzoImanishi, Takeshi
    • C07C323/49C07C317/28C07C317/44C07C323/20C07D213/71A61K31/18
    • C07C317/44C07C317/28C07C323/49C07C323/62C07D213/71
    • Sulfonamide derivative, useful as blood platelet aggregation inhibitors, have the formula:

      in which A is a naphthyl group, a pyridyl group, a phenyl group, a phenyl group substituted by 1 to 5 substituents selected from halogen atoms, alkyl groups having 1 to 4 carbon atoms, alkoxy groups having 1 to 4 carbon atoms, nitro groups and acetamido groups, or an alkyl group having 1 to 20 carbon atoms; B is an alkylene group having 1 to 3 carbon atoms, a group -OCH₂- or a group -CH=CH-; X and Y are the same or different, and each is a hydrogen or fluorine atom; R is a carboxy group, an alkyoxycarbonyl group having 2 to 5 carbon atoms, a hydroxymethyl group or a group of the formula
      (in which R¹ is a hydrogen atom or an alkyl group having 1 to 3 carbon atoms; R² is a hydrogen atom, a hydroxyl group, an alkyl group having 1 to 3 carbon atoms, a carboxymethyl group or an alkoycarbonylmethyl group having 3 to 6 carbon atoms); m is 0, 1 or 2; n is 0,1,2 or 3; or salts thereof.
      This invention also provided intermediates for the preparation of the sulfonamide, which intermediates are thiophenols of the formula:

      (in which R, X and Y are as defined above).
    • 可用作血小板聚集抑制剂的磺酰胺衍生物具有下式:其中A是萘基,吡啶基,苯基,被1至5个选自卤素原子的取代基取代的苯基,具有1至4个碳原子的烷基 碳原子,具有1至4个碳原子的烷氧基,硝基和乙酰氨基,或具有1至20个碳原子的烷基; B是具有1-3个碳原子的亚烷基,基团-OCH 2 - 或基团-CH = CH-; X和Y相同或不同,并且各自是氢或氟原子; R为羧基,具有2至5个碳原子的烷氧基羰基,羟甲基或下式基团(其中R 1为氢原子或具有1至3个碳原子的烷基; R 2为氢原子, 羟基,碳原子数为1〜3的烷基,羧甲基或碳原子数为3〜6的烷基羰甲基)。 m是0,1或2; n是0,1,2或3; 或其盐。 本发明还提供了用于制备磺酰胺的中间体,其中间体是下式的苯硫酚:(其中R,X和Y如上所定义)。