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    • 6. 发明公开
    • 1-Azabicyclo(3.2.0)Hept-2-Ene-2-carboxylic acid compounds
    • (3.2.0)庚-2-烯-2-碳辛烷基。
    • EP0394991A1
    • 1990-10-31
    • EP90107824.6
    • 1990-04-25
    • FUJISAWA PHARMACEUTICAL CO., LTD.
    • Murata, MasayoshiChiba, ToshiyukiTsutsumi, HideoHattori, KohjiKuroda, SatoruOhtake, HiroakiShirai, Fumiyuki
    • C07D477/00C07D519/00C07F7/18A61K31/40C07F9/568
    • C07D477/14C07F7/186Y02P20/55
    • A compound of the formula :
      in which

      R 1 is carboxy, protected carboxy or carboxylato,
      R 2 is hydroxy(lower)alkyl or protected hydroxy(lower)alkyl,
      R 3 is hydrogen or lower alkyl,
      A is a group of the formula:
      wherein
      is N-containing aliphatic heterocyclic group optionally containing additional hetero atom(s),
      R 4 is hydrogen, hydroxy, protected hydroxy, hydroxy(lower)alkyl, protected hydroxy(lower)alkyl, lower alkyl, lower alkoxy(lower)alkyl, halogen, carbamoyl, mono- or di(lower)alkylcarbamoyl or imino-protective group,
      R 5 is hydrogen, lower alkenyl, carbamoyl, mono- or di(lower)alkylcarbamoyl, imino-protective group, or a group of the formula :
      wherein
      R 6 is hydrogen or lower alkyl optionally substituted by suitable substituent(s),
      R 7 is hydrogen, lower alkyl, cyano, hydroxy(lower)alkoxy(lower)alkyl or heterocyclic group,
      R 8 is lower alkyl, or
      R 7 is combined with R 6 or R 8 to form lower alkylene, and
      m and n are each an integer of 0 to 3, or pharmaceutically acceptable salts thereof,
      processes for their preparation and pharmaceutical compositions comprising them as active ingredient in association with a pharmaceutically acceptable carrier or excipient.
    • 下式的化合物:其中R 1是羧基,保护的羧基或羧基,R 2是羟基(低级)烷基或被保护的羟基(低级)烷基,R 3是氢或低级烷基 A是下式的基团:其中CHEM是任选含有另外的杂原子的含N脂肪族杂环基,R 4是氢,羟基,被保护的羟基,羟基(低级)烷基, 保护的羟基(低级)烷基,低级烷基,低级烷氧基(低级)烷基,卤素,氨基甲酰基,一或二(低级)烷基氨基甲酰基或亚氨基保护基,R 5是氢,低级烯基,氨基甲酰基, 二(低级)烷基氨基甲酰基,亚氨基保护基或下式基团:其中R 6为氢或任选被合适的取代基取代的低级烷基,R 7为氢,低级烷基, 氰基,羟基(低级)烷氧基(低级)烷基或杂环基,R 8为低级烷基,或R 7与R 6或R 8结合形成低级亚烷基,m和n为 各为0〜3的整数, 或其药学上可接受的盐,其制备方法和包含它们作为活性成分与药学上可接受的载体或赋形剂的药物组合物。