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    • 9. 发明申请
    • ACYL DIHYDRO PYRROLE DERIVATIVES AS HCV INHIBITORS
    • WO2005103045A1
    • 2005-11-03
    • PCT/EP2005/004270
    • 2005-04-20
    • GLAXO GROUP LIMITEDHAIGH, DavidSLATER, Martin John
    • HAIGH, DavidSLATER, Martin John
    • C07D417/04
    • C07D417/04C07D417/14
    • Novel anti-viral agents of Formula (I) in which: A represents hydroxy; D represents aryl or heteroaryl; E represents hydrogen, C 1-6 alkyl, aryl, heteroaryl or heterocyclyl; G represents hydrogen or C 1-6 alkyl optionally substituted by one or more substituents selected from halo, OR 1 , SR 1 , C(O)NR 2 R 3 , CO 2 H, C(O)R 4 , CO 2 R 4 , NR 2 R 3 , NHC(O)R 4 , NHCO 2 R 4 , NHC(O)NR 5 R 6 , SO 2 NR 5 R 6 , SO 2 R 4 , nitro, cyano, aryl, heteroaryl and heterocyclyl; R 1 represents hydrogen, C 1-6 alkyl, arylalkyl, or heteroarylalkyl; R 2 and R 3 are independently selected from hydrogen, C 1-6 alkyl, aryl and heteroaryl; or R 2 and R 3 together with the nitrogen atom to which they are attached form a 5 or 6 membered saturated cyclic group; R 4 is selected from the group consisting of C 1-6 alkyl, aryl, heteroaryl, arylalkyl, and heteroarylalkyl; R 5 and R 6 are independently selected from the group consisting of hydrogen, C 1-6 alkyl, aryl, heteroaryl, arylalkyl, and heteroarylalkyl; or R 5 and R 6 together with the nitrogen atom to which they are attached form a 5 or 6 membered saturated cyclic group; and J represents C 1-6 alkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl; and salts, solvates and esters thereof; provided that when A is esterified to form -OR where R is selected from straight or branched chain alkyl, aralkyl, aryloxyalkyl, or aryl, then R is other than tert -butyl; processes for their preparation, pharmaceutical compositions comprising them, and methods of using them in HCV treatment are provided.
    • 式(I)的新型抗病毒剂,其中:A表示羟基; D表示芳基或杂芳基; E表示氢,C 1-6烷基,芳基,杂芳基或杂环基; G表示氢或任选被一个或多个选自卤素,OR 1,SR 1,C(O)NR 2 R 3,CO 2 H,C(O)R 4的取代基取代的C 1-6烷基 ,CO 2 R 4,NR 2 R 3,NHC(O)R 4,NHCO 2 R 4,NHC(O)NR 5 R 6,SO 2 NR 5 R 6 SO 2 R 4,硝基,氰基,芳基,杂芳基和杂环基; R 1表示氢,C 1-6烷基,芳烷基或杂芳基烷基; R 2和R 3独立地选自氢,C 1-6烷基,芳基和杂芳基; 或R 2和R 3与它们所连接的氮原子一起形成5或6元饱和的环状基团; R 4选自C 1-6烷基,芳基,杂芳基,芳烷基和杂芳基烷基; R 5和R 6独立地选自氢,C 1-6烷基,芳基,杂芳基,芳基烷基和杂芳基烷基; 或R 5和R 6与它们所连接的氮原子一起形成5或6元饱和环状基团; 并且J表示C 1-6烷基,杂环基烷基,芳基烷基或杂芳基烷基; 及其盐,溶剂化物和酯; 条件是当A被酯化形成-OR时,其中R选自直链或支链烷基,芳烷基,芳氧基烷基或芳基,则R不是叔丁基; 提供其制备方法,包含它们的药物组合物,以及在HCV治疗中使用它们的方法。