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    • 77. 发明申请
    • CYCLOPROPYL POLYMERASE INHIBITORS
    • 环丙基聚合酶抑制剂
    • US20110092460A1
    • 2011-04-21
    • US12999263
    • 2009-07-01
    • Tim Hugo Maria JonckersPierre Jean-Marie Bernard RaboissonKoen Vandyck
    • Tim Hugo Maria JonckersPierre Jean-Marie Bernard RaboissonKoen Vandyck
    • A61K31/513C07D405/04A61K31/675A61P31/12A61P31/14
    • C07H19/073
    • Compounds of formula I: wherein: R2 is hydrogen or C1-C4alkyl; R3 and R4 are hydrogen, —C(═O)R5, or —C(═O)CHR6—NH2; or R3 is hydrogen and R4 is a monophosphate-, diphosphate-, or triphosphate ester; or R3 is hydrogen, —C(═O)CHR5, or —C(═O)CHR6—NH2 and R4 is each R5 is hydrogen, C1-C6alkyl, or C3-C7cycloalkyl; R6 is hydrogen or C1-C6alkyl; R7 is optionally substituted phenyl; naphthyl; or indolyl; R8 and R8′ are hydrogen, C1-C6alkyl, benzyl; or R8 and R8′ combined form C3-C7cycloalkyl; R9 is C1-C6alkyl, benzyl, or optionally substituted phenyl; provided that R2, R3 and R4 are not all hydrogen; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical formulations with the compounds I; the use of compounds I, including the compounds of formula I wherein R2, R3 and R4 are all hydrogen, as HCV inhibitors.
    • 式I化合物:其中:R 2是氢或C 1 -C 4烷基; R3和R4是氢,-C(= O)R5或-C(= O)CHR6-NH2; 或R3是氢,R4是单磷酸酯,二磷酸酯或三磷酸酯; 或R 3为氢,-C(= O)CHR 5或-C(= O)CHR 6 -NH 2,且R 4各自为R 5为氢,C 1 -C 6烷基或C 3 -C 7环烷基; R6是氢或C1-C6烷基; R7是任选取代的苯基; 萘基; 或吲哚基; R8和R8'是氢,C1-C6烷基,苄基; 或R 8和R 8'组合形式的C 3 -C 7环烷基; R 9为C 1 -C 6烷基,苄基或任选取代的苯基; 条件是R2,R3和R4不都是氢; 或其药学上可接受的盐或溶剂化物; 具有化合物I的药物制剂; 使用化合物I,包括其中R2,R3和R4均为氢的式Ⅰ化合物作为HCV抑制剂。