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    • 1. 发明公开
    • Isochromane derivatives
    • 等色素衍生物
    • EP0458387A1
    • 1991-11-27
    • EP91201119.4
    • 1991-05-10
    • Akzo Nobel N.V.
    • Laigle, Jean-ClaudeCombourieu, MichelSimbille, Nadine
    • C07D405/04C07D405/06C07D311/76A61K31/445A61K31/495
    • C07D405/06C07D311/76C07D493/04
    • The invention concerns an isochromane derivative having the general formula I
      in which R 1 is one to four substituents independently selected from hydrogen, hydroxy, alkyl (1-4 C), alkoxy (1-4 C), halogen, or CF 3 , or as two adjacent substituents together a methylenedioxy group; R 2 is one to four substituents independently selected from hydrogen, hydroxy, alkyl (1-4 C), alkoxy (1-4 C), halogen, or CF 3 , or as two adjacent substituents together a methylenedioxy group; R 3 is one to four substituents independently selected from hydrogen, hydroxy, alkyl (1-4 C), alkoxy (1-4 C), halogen, or CF 3 , or as two adjacent substituents together a methylenedioxy group; R 4 is selected from hydrogen or alkyl (1-4 C); A is a bond or an alkylene or alkylidene group with 1-6 carbon atoms; B is an alkylene or alkylidene group with 1-6 carbon atoms when Y is a bond, or B is an alkylene group with 2-6 carbon atoms when Y is a group selected from 0, S, or NRs; X is CH or N; and R 5 is selected from hydrogen or alkyl (1-4 C); or a pharmaceutically acceptable salt thereof.
    • 本发明涉及具有通式I的异苯并二氢吡喃衍生物,其中R 1是1-4个独立地选自氢,羟基,烷基(1-4C),烷氧基(1-4C),卤素或CF 3的取代基,或者是两个 相邻的取代基一起形成亚甲二氧基; R2是独立地选自氢,羟基,烷基(1-4C),烷氧基(1-4C),卤素或CF3的1至4个取代基,或者作为两个相邻的取代基一起形成亚甲二氧基; R3是独立地选自氢,羟基,烷基(1-4C),烷氧基(1-4C),卤素或CF3的1至4个取代基,或作为两个相邻的取代基一起形成亚甲二氧基; R4选自氢或烷基(1-4C); A是具有1-6个碳原子的键或亚烷基或亚烷基; 当Y是键时,B是具有1-6个碳原子的亚烷基或亚烷基,或者当Y是选自0,S或NRs的基团时,B是具有2-6个碳原子的亚烷基; X是CH或N; 和R5选自氢或烷基(1-4C); 或其药学上可接受的盐。
    • 3. 发明公开
    • New isochromane derivatives
    • 新的异色满衍生物
    • EP0450689A1
    • 1991-10-09
    • EP91200607.9
    • 1991-03-20
    • Akzo Nobel N.V.
    • Combourieu, MichaelLaigle, Jean-Claude
    • C07D311/76C07D493/04A61K31/35
    • C07D311/76
    • An isochromane derivative having the general formula I

      in which each of R₁, R₂, and R₃ is one to four substituents independently selected from hydrogen, hydroxy, alkyl (1-4 C), alkoxy (1-4 C), halogen, or CF₃, or represents a methylenedioxy group;
      R₄ is selected from hydrogen or alkyl (1-4 C);
      Alk is an alkylene group with 1-4 carbon atoms;
      Alk' is an alkylene group with 2-4 carbon atoms, when R₅ is selected from hydrogen or alkyl (1-4 C) and X is O or S; or
      Alk' is an alkylene group with 1-4 carbon atoms or a bond, when R₅ is an alkyl (1-4 C) group and X is CH₂ or a bond;
      or a pharmaceutically acceptable salt thereof.
    • 具有通式Ⅰ的异苯并二氢吡喃衍生物,其中R 1,R 2和R 3各自是1-4个独立地选自氢,羟基,烷基(1-4C),烷氧基(1-4C),卤素或CF 3的取代基 ,或代表亚甲基二氧基; R 4选自氢或烷基(1-4C); Alk是具有1-4个碳原子的亚烷基; 当R 5选自氢或烷基(1-4C)且X为O或S时,Alk'为具有2-4个碳原子的亚烷基; 或Alk'是具有1-4个碳原子的亚烷基或键,当R 5是烷基(1-4C)基团并且X是CH 2或键时; 或其药学上可接受的盐。