RABOISSON, PIERRE JEAN-MARIE,雷伯森,DE KOCK, HERMAN AUGUSTINUS,戴寇克,DORANGE, ISMET,杜麦特,杜麥特,VENDEVILLE, SANDRINE MARIE HELENE,范海伦,范海倫,SURLERAUX, DOMINIQUE LOUIS NESTOR GHISLAIN,苏奈杜,蘇奈杜,TAHRI, ABDEL
申请号：
TW095127590
公开号：
TWI393723B
申请日:
2006.07.28
申请国别(地区):
TW
年份:
2013
代理人:
摘要：
Inhibitors of HCV replication of formula (I)and theN－oxides, salts, and stereoisomers thereof, whereinXis N, CH and where X bears a double bond it is C；R1is －OR5, －NH－SO2R6；R2is hydrogen, and where X is C or CH, R2may also be C1－6alkyl；R3is hydrogen, C1－6alkyl, C1－6alkoxyC1－6alkyl, or C3－7cycloalkyl；R4is isoquinolinyl optionally substituted with one, two or three substituents each independently selected from C1－6alkyl, C1－6alkoxy, hydroxyl, halo, polyhalo－C1－6alkyl, polyhaloC1－6alkoxy, amino, mono－ or diC1－6alkylamino, mono－ or diC1－6alkylaminocarbonyl, C1－6alkylcarbonyl－amino, aryl, and Het；nis 3, 4, 5, or 6； each dashed line (represented by......) represents an optional double bond；R5is hydrogen； aryl； Het； C3－7cycloalkyl optionally substituted with C1－6alkyl； or C1－6alkyl optionally substituted with C3－7cycloalkyl, aryl or with Het；R6is 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.具式(I)之HCV複製之抑制劑類及其N－氧化物類、鹽類、及立體異構物類，其中X為N，CH，而其中X攜載雙鍵時，其為C；R1為－OR5，－NH－SO2R6；R2為氫，且其中X為C或CH，R2也可以是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；R4為選擇地經1、2或3個各自獨立地挑選自下述取代基取代之異喹啉基：C1－6烷基，C1－6烷氧基，羥基，鹵基，多鹵基C1－6烷基，多鹵基C1－6烷氧基，胺基，單－或二－C1－6烷基胺基，單－或二－C1－6烷基胺基羰基，C1－6烷基羰基－胺基，芳基，及Het；n為3，4，5，或6；各個虛線(以－－－－－代表者)代表一種選擇的雙鍵；R5為氫；芳基；Het；選擇地經C1－6烷基取代之C3－7環烷
