DE KOCK, HERMAN AUGUSTINUS,戴寇克,戴寇克,SIMMEN, KENNETH ALAN,施艾伦,施艾倫,JOENSSON, CARL ERIK DANIEL,乔恩森,喬恩森,AYESA ALVAREZ, SUSANA,苏珊纳,蘇珊納,CLASSON, BJOERN OLOF,克雷森,克雷森,NILSSON, KARL MAGNUS,尼斯欧,尼斯歐,ROSENQUIST, A
申请号：
TW095127586
公开号：
TWI382025B
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 the N-oxides, salts, or stereoisomers thereof, wherein each dashed line represents an optional double bond X is N, CH and where X bears a double bond it is C R1 is -OR6, -NH-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 taken together with the nitrogen atom to which they are attached form a bicyclic ring system selected from wherein said ring system may optionally be substituted with 1-3 substituents 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 of which may be optionally substituted with 1-3 substituents Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms each independently selected from N, O or S, and being 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.式(I)之HCV複製抑制劑及其N-氧化物、鹽類或立體異構物,其中各虛線係表示視情況存在下之雙鍵;X係為N、CH且當X帶有雙鍵時其係為C;R1係為-OR6、-NH-SO2R7;R2係為氫,且當X係為C或CH時,R2亦可為C1-6烷基;R3係為氫、C1-6烷基、C1-6烷氧C1-6烷基或C3-7環烷基;n係為3、4、5或6;R4及R5與其所連接之氮原子一起形成選自下列者之雙環性環系統其中該環系統可視情況經1至3個取代基所取代;R6係為氫;芳基;Het;視情況經C1-6烷基取代之C3-7環烷基;或視情況經C3-7環烷基、芳基或經Het取代之C1-6烷基;R7係為芳基;Het;視情況經C1-6烷基取代之C3-7環烷基;或視情況經C3-7環烷基、芳基或經Het取代之C1-6烷基;aryl係為苯基或萘基,其各可視情況經1至3個取代基所取代;Het係為5或6員飽和、部分不飽和或完全不飽和雜環性環,其含有1至4個各獨立選自N、O或S之氫原子,且係視情況經1至3個取代基所取代含有化合物(I)之醫藥組成物及製備化合物(I)之方法。亦提供式(I)之HCV抑制劑與利妥那維亞(ritonavir)之生物可利用組合物。
