利索-全球专利检索

  1. 登录
  2. 注册
发明授权
CN101273030B 丙型肝炎病毒的大环抑制剂 有权 转让

丙型肝炎病毒的大环抑制剂
摘要：
本发明涉及作为HCV复制抑制剂的式(I)化合物及其N-氧化物、盐和立体异构体，其中X是N、CH，当X带有双键时是C；R1是-OR5、-NH-SO2R6；R2是氢，且当X是C或CH时，R2也可为C1-6烷基；R3是氢、C1-6烷基、C1-6烷氧基C1-6烷基或C3-7环烷基；R4是任选被1、2或3个各自独立选自下述取代基取代的异喹啉基：C1-6烷基、C1-6烷氧基、羟基、卤素、多卤代C1-6烷基、多卤代C1-6烷氧基、氨基、单-或二-C1-6烷基氨基、单-或二-C1-6烷基氨基羰基、C1-6烷基羰基-氨基、芳基和Het；n是3、4、5或6；由-----表示的各虚线表示任选的双键；R5是氢；芳基；Het；任选被C1-6烷基取代的C3-7环烷基；或任选被C3-7环烷基、芳基或Het取代的C1-6烷基；R6是芳基；Het；任选被C1-6烷基取代的C3-7环烷基；或任选被C3-7环烷基、芳基或Het取代的C1-6烷基；各芳基是任选被1、2或3个取代基取代的苯基；且各Het是饱和的、部分不饱和或完全不饱和的5或6元杂环，所述杂环含有1-4个各自独立选自氮、氧和硫的杂原子，且任选被1、2或3个取代基取代；本发明还涉及含式(I)化合物的药物组合物及制备化合物(I)的方法；还提供了式(I)化合物与利托那韦的生物可用的HCV抑制剂组合。
摘要（英）：

Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers thereof, wherein X is N, CH and where X bears a double bond it is C; R<1> is -OR<5>, -NH-SO2R<6>; R<2> is hydrogen, and where X is C or CH, R<2> may also be C1-6alkyl; R<3> is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, or C3-7cycloalkyl; R4 is isoquinolinyl optionally substituted with one, two or three substituents each independently selected from C1-6alkyl, C1-6alkoxy, hydroxy, halo, polyhalo- C1-6alkyl, polyhaloC1-6alkoxy, amino, mono- or diC1-6alkylamino, mono- or DiC1-6alkylaminocarbonyl, C1-6alkylcarbonyl-amino, aryl, and Het; n is 3, 4, 5, or 6; each dashed line (represented by ) represents an optional double bond; R<5> is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R<6> is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; each aryl is phenyl optionally substituted with one, two or three substituents; and each Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms each independently selected from nitrogen, oxygen and sulfur, and being optionally substituted with one, two or three substituents; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.

公开/授权文献
0/0