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    • 3. 发明申请
    • MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS
    • 丙型肝炎病毒大肠杆菌抑制剂
    • US20140113929A1
    • 2014-04-24
    • US14135826
    • 2013-12-20
    • Janssen R&D Ireland (formerly Tibotec Pharmaceuticals)
    • Pierre Jean-Marie RaboissonHerman Augustinus De KockDavid Craig Mc GowanLili HuAbdellah TahriSandrine Marie Helene VendevilleWim Van De Vreken
    • C07D491/056A61K31/427A61K31/4741C07D491/048
    • C07D491/056A61K31/427A61K31/4741C07D401/12C07D491/04C07D491/048Y02A50/385Y02A50/387Y02A50/389Y02A50/393A61K2300/00
    • Inhibitors of HCV replication of formula (I) and the salts and stereoisomers thereof, wherein each dashed line (represented by - - - - -) represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl; n is 3, 4, 5, or 6; R4 is C1-6alkyl or C3-7cycloalkyl; R5 is hydrogen, halo, C1-6alkyl, hydroxy, C1-6alkoxy, polyhaloC1-6alkyl; R6 is hydrogen, C1-6alkoxy, mono- or diC1-6alkylamino; or R5 and R6 may form a 5- or 6-membered unsaturated or partially unsaturated ring, optionally comprising one or two selected from O, N and S; R7 is hydrogen; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl; R8 is C3-7cycloalkyl optionally substituted with C1-6alkyl; C1-6alkyl optionally substituted with C3-7cycloalkyl; or —NR8aR8b; R8a and R8b are C1-6alkyl, or both may form a 5- or 6-membered saturated heterocyclic ring; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I).
    • 式(I)的HCV复制抑制剂及其盐和立体异构体,其中每个虚线(由 - - - - 表示)表示任选的双键; X为N,CH,X为双键,C为C; R1是-OR7,-NH-SO2R8; R2是氢,并且其中X是C或CH,R2也可以是C1-6烷基; R 3是氢,C 1-6烷基,C 1-6烷氧基C 1-6烷基,C 3-7环烷基; n为3,4,5或6; R4是C1-6烷基或C3-7环烷基; R5是氢,卤素,C1-6烷基,羟基,C1-6烷氧基,多卤代C 1-6烷基; R 6是氢,C 1-6烷氧基,单或二C 1-6烷基氨基; 或R 5和R 6可以形成5-或6-元不饱和或部分不饱和的环,任选地包含一个或两个选自O,N和S; R7是氢; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基取代的C 1-6烷基; R8是任选被C 1-6烷基取代的C 3-7环烷基; 任选被C 3-7环烷基取代的C 1-6烷基; 或-NR8aR8b; R8a和R8b是C1-6烷基,或两者可以形成5或6元饱和杂环; 含有化合物(I)的药物组合物和制备化合物(I)的方法。