RABOISSON, PIERRE JEAN-MARIE,雷伯森,DE KOCK, HERMAN AUGUSTINUS,戴寇克,SIMMEN, KENNETH ALAN,施艾伦,施艾倫,JOENSSON, CARL ERIK DANIEL,乔恩森,喬恩森,NILSSON, KARL MAGNUS,尼斯欧,尼斯歐,ROSENQUIST, ASA ANNICA KRISTINA,庐森特
申请号：
TW095127584
公开号：
TWI375670B
申请日:
2006.07.28
申请国别(地区):
TW
年份:
2012
代理人:
摘要：
Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or 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 &mdash；OR6, &mdash；NH&mdash；SO2R7； R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl； R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, or C3-7cycloalkyl； n is 3, 4, 5, or 6； R4 and R5 independently from one another are hydrogen, halo, hydroxy, nitro, cyano, carboxyl, C1-6alkyl, C1-6alkoxy, C1-6alkoxyC1-6alkyl, C1-6alkylcarbonyl, C1-6alkoxy-carbonyl, amino, azido, mercapto, C1-6alkylthio, polyhaloC1-6alkyl, aryl or Het； W is aryl or Het； R6 is hydrogen； aryl； Het； C3-7cycloalkyl optionally substituted with C1-6alkyl； or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het； R7 is aryl； Het； C3-7cycloalkyl optionally substituted with C1-6alkyl； or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het； aryl is phenyl or naphthyl, each optionally substituted with 1-3 substituents； Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1-4 heteroatoms each independently selected from N, O or S, and optionally substituted with 1-3 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.本發明係提供式(I)之HCV複製抑制劑，；(I)；及其N-氧化物，鹽類，或立體異構物，其中，各個虛線(以-----代表)代表任意的雙鍵；X為N，CH且當X攜帶雙鍵時其為C；R1為-OR6，-NH-SO2R7；R2為氫，且當X為C或CH時，R2亦可為C1-6烷基；R3為氫，C1-6烷基，C1-6烷氧基C1-6烷基，或C3-7環烷基；n為3，4，5，或6；R4及R5各自獨立為氫，鹵素，羥基，硝基，氰基，羧基，C1-6烷基，C1-6烷氧基，C1-6烷氧基C1-6烷基，C1-6烷基羰基，C1-6烷氧基羰基，胺基，疊氮基，巰基，C1-6烷基硫基，多鹵素C1-6烷基，芳基或Het；W為芳基或Het；R6為氫；芳基；Het；任意的被C1-6烷基所取代之C3-7環烷基；或任意的被C3-7環烷基，芳基或被Het所取代之C1-6烷基；R7為芳基；Het；任意的被C1-6烷基所取代之C3-7環烷基；或任意的被C3-7環烷基，芳基或被Het所取代之C1-6烷基；芳基為苯基或萘基，各個任意的被1-3個取代基所取代；Het為含有1至4個各自獨立選自N，O或S之雜原子，且任意的被1-3個取代基所取代之5或6員飽和，部份不飽
