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    • 10. 发明公开
    • Pharmaceutical compositions
    • 药物组合物
    • EP0409499A3
    • 1991-03-27
    • EP90307685.9
    • 1990-07-13
    • BRITISH TECHNOLOGY GROUP LIMITED
    • Creighton, Andrew Malcolm
    • A61K31/495C07D241/08
    • A61K31/535A61K31/495A61K31/70C07D241/08A61K31/165A61K2300/00
    • Compounds of formula II:
      wherein n is 0, 1 or 2, R₁, R₂, R₃ and R₄ are each separately selected from hydrogen, unsubstituted acyclic aliphatic hydrocarbon groups having a maximum of six carbon atoms and C₁₋₆ alkyl groups substituted by a hydroxy group or a C₁₋₆ alkoxy group, or one of R₁ and R₂ and one of R₃ and R₄ is hydrogen and the others are a trimethylene, tetramethylene or pentamethylene bridging group, and R₅ as hydrogen or an unsubstituted acyclic aliphatic hydrocarbon group having a maximum of six carbon atoms, but with the provisos that (a) when n is 0 the combinations R₁ = R₂ = R₃ = R₄ = R₅ = H and R₁ = R₂ = R₃ = R₅ = H, R₄ = methyl are excluded, and (b) when n is 0, R₁, R₃ and R₅ are each hydrogen, and each of R₂ and R₄ is other than hydrogen the compound is in other than the meso or erythro configuration, or a salt thereof formed with a physiologically acceptable inorganic or organic acid, are of use in therapy, particularly as cardioprotective agents.
    • 式Ⅱ化合物:其中n为0,1或2,R 1,R 2,R 3和R 4分别选自氢,未取代的具有最多6个碳原子的无环脂族烃基和被羟基取代的C 1-6烷基 基团或C 1-6烷氧基,或R 1和R 2之一,R 3和R 4之一为氢,其它为三亚甲基,四亚甲基或五亚甲基桥基,R 5为氢或未取代的非环脂族烃基, (a)当n为0时,排除组合R 1 = R 2 = R 3 = R 4 = R 5 = H和R 1 = R 2 = R 3 = R 5 = H,R 4 =甲基,并且(b )当n是0时,R 1,R 3和R 5各自是氢,R 2和R 4各不是氢,该化合物不是中间或赤式构型,或其与生理学上可接受的无机或有机酸形成的盐 ,在治疗中有用,p 特别是作为心脏保护剂。