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    • 3. 发明申请
    • ACYL ISOINDOLINE DERIVATIVES AND ACYL ISOQUINOLINE DERIVATIVES AS ANTI-VIRAL AGENTS
    • ACYL ISOINDOLINE DORIVATIVES和ACYL ISOQUINOLINE DERIVATIVES作为反病毒代理
    • WO2004096774A1
    • 2004-11-11
    • PCT/EP2004/004660
    • 2004-04-29
    • GLAXO GROUP LIMITEDBRAVI, GianpaoloCORFIELD, John, AndrewHAIGH, DavidLOVEGROVE, Victoria, Lucy, HelenSHAH, PritomSLATER, Martin, John
    • BRAVI, GianpaoloCORFIELD, John, AndrewHAIGH, DavidLOVEGROVE, Victoria, Lucy, HelenSHAH, PritomSLATER, Martin, John
    • C07D217/26
    • C07D401/04C07D209/44C07D217/26C07D401/12C07D405/04C07D417/12
    • Anti-viral agents of Formula (I) wherein: R 3 represents aryl or heteroaryl; R 4 represents one or two substituents independently selected from hydrogen, C 1 - 6 alkyl, halo, OR A , C(O)NR B R C , C(O)R D , CO 2 H, CO 2 R D , NR B R C , NR E C(O)R D , NR E CO 2 R D , NR E C(O)NR F R G , NR E SO 2 R D , SO 2 NR F R G , SO 2 R D , nitro, cyano, heterocyclyl, heteroaryl, aryl, arylalkyl heteroarylalkyl or CF 3 ; R 5 and R 6 independently represent hydrogen, C 1-6 alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; n represents 0 or 1; when n represents 0, R 1 represents C(O)R H and R 2 represents C 1-6 alkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl; when n represents 1, either i) R 1 represents C(O)R H ; R 2 represents C 1-6 alkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl; and R 7 and R 8 independently represent hydrogen, C 1-6 alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; or ii) R 1 and R 2 independently represent hydrogen, C 1-6 alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; R 7 represents C(O)R H ; and R 8 represents C 1-6 alkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl; R A represents hydrogen, C 1-6 alkyl, arylalkyl, heteroarylalkyl, aryl or heteroaryl; R B and R C independently represent hydrogen, C 1-6 alkyl, aryl or heteroaryl; or R B and R C together with the nitrogen atom to which they are attached form a 5 or 6 membered saturated cyclic group; R D is selected from the group consisting of C 1-6 alkyl, aryl, heteroaryl, arylalkyl, and heteroarylalkyl; R E represents hydrogen or C 1-6 alkyl; R F and R G are independently selected from the group consisting of hydrogen, C 1-6 alkyl, aryl, heteroaryl, arylalkyl, and heteroarylalkyl; or R F and R G together with the nitrogen atom to which they are attached form a 5 or 6 membered saturated cyclic group; R H represents hydroxy or NR B R C ; and salts, solvates and esters thereof; provided that when R H is hydroxy, which 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 and methods of using them in HCV treatment are provided.
    • 式(I)的抗病毒剂,其中:R 3表示芳基或杂芳基; R 4表示一个或两个独立地选自氢,C 1-6烷基,卤素,OR A,C(O)NR B,C(O)R D,CO 2 H, NRR,NR C,O,R D,NR E,CO 2 R D,NR C,C(O)NR F, 氰基,杂环基,杂芳基,芳基,芳基烷基杂芳基烷基或CF 3; R 3,R 3,R 4, R 5和R 6独立地表示氢,C 1-6烷基,芳基,杂芳基,芳烷基或杂芳基烷基; n表示0或1; 当n表示0时,R 1表示C(O)R H,R 2表示C 1-6烷基,杂环基烷基,芳烷基或杂芳基烷基; 当n表示1时,i)R 1表示C(O)R H; R 2表示C 1-6烷基,杂环基烷基,芳烷基或杂芳基烷基; R 7和R 8独立地表示氢,C 1-6烷基,芳基,杂芳基,芳基烷基或杂芳基烷基; 或ii)R 1和R 2独立地表示氢,C 1-6烷基,芳基,杂芳基,芳基烷基或杂芳基烷基; R 7表示C(O)R H; 并且R 8表示C 1-6烷基,杂环基烷基,芳烷基或杂芳基烷基; R A表示氢,C 1-6烷基,芳基烷基,杂芳基烷基,芳基或杂芳基; R B和R C独立地表示氢,C 1-6烷基,芳基或杂芳基; 或R B和R C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 D选自C 1-6烷基,芳基,杂芳基,芳基烷基和杂芳基烷基; R E表示氢或C 1-6烷基; R F和R G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 F和R G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 H表示羟基或NR B; 及其盐,溶剂化物和酯; 条件是当R H是羟基时,其被酯化以形成-OR,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。 提供其制备方法及其在HCV治疗中的使用方法。
    • 4. 发明申请
    • ACYL DIHYDRO PYRROLE DERIVATIVES AS HCV INHIBITORS
    • WO2003037893A1
    • 2003-05-08
    • PCT/EP2002/012171
    • 2002-10-30
    • GLAXO GROUP LIMITEDBRAVI, GianpaoloHOWES, Peter, DavidLOVEGROVE, Victoria, Lucy, HelenSHAH, PritomSLATER, Martin, John
    • BRAVI, GianpaoloHOWES, Peter, DavidLOVEGROVE, Victoria, Lucy, HelenSHAH, PritomSLATER, Martin, John
    • C07D417/04
    • C07D417/04
    • Novel anti-viral agents of Formula (I) wherein: A represents OR 1 , NR 1 R 2 , or R 1 wherein R 1 and R 2 are hydrogen, C 1-6 alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; or R 1 and R 2 together with the nitrogen atom to which they are attached form a 5 or 6 membered saturated cyclic group; B represents C(O)R 3 wherein R 3 is C 1-6 alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; D represents C 1-6 alkyl, aryl, heteroaryl or heterocyclyl; E represents OR 1 , NR 1 R 2 , or R 1 wherein R 1 and R 2 are hydrogen, C 1-6 alkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl; or R 1 and R 2 together with the nitrogen atom to which they are attached form a 5 or 6 membered saturated cyclic group; F represents hydrogen, C 1-6 alkyl, aryl or heteroaryl; and G represents hydrogen, C 1-6 alkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl; and salts and solvates thereof, processes for their preparation and methods of using them in HCV treatment are provided.
    • 式(I)的新型抗病毒剂,其中:A表示OR 1,NR 1 R 2或R 1,其中R 1和R 2为氢,C 1-6烷基, 芳基,杂芳基,芳基烷基或杂芳基烷基; 或R 1和R 2与它们所连接的氮原子一起形成5或6元饱和环状基团; B表示C(O)R 3,其中R 3是C 1-6烷基,芳基,杂芳基,芳烷基或杂芳基烷基; D表示C 1-6烷基,芳基,杂芳基或杂环基; E表示OR 1,NR 1 R 2或R 1,其中R 1和R 2是氢,C 1-6烷基,芳基,杂芳基,芳烷基或杂芳基烷基; 或R 1和R 2与它们所连接的氮原子一起形成5或6元饱和环状基团; F表示氢,C 1-6烷基,芳基或杂芳基; 和G表示氢,C 1-6烷基,杂环基烷基,芳基烷基或杂芳基烷基; 并提供其盐和溶剂化物,其制备方法及其在HCV治疗中的使用方法。