RABOISSON, PIERRE JEAN-MARIE,雷伯森,DE KOCK, HERMAN AUGUSTINUS,戴寇克,VENDEVILLE, SANDRINE MARIE HELENE,范海伦,范海倫,HU, LILI,胡丽丽,胡麗麗,VAN DE VREKEN, WIM,范玮恩,范瑋恩,MCGOWAN, DAVID CRAIG,麦大卫,麥大衛,TAHRI, ABDELL
申请号：
TW095127588
公开号：
TWI412534B
申请日:
2006.07.28
申请国别(地区):
TW
年份:
2013
代理人:
摘要：
Inhibitors of HCV of formula (I)and the N－oxides, salts, and stereochemically isomeric forms thereof, whereinR1is aryl or a saturated, a partially unsaturated or completely unsaturated 5 or 6 membered monocyclic or 8 to 12 membered bicyclic heterocyclic ring system containing one nitrogen, and optionally one to three oxygen, sulfur or nitrogen, wherein said ring system may be optionally substituted；Lis a direct bond, －O－, －O－C1－4alkanediyl－, －O－CO－, －O－C(＝O)－NR5a－or－OC(＝O)NR5a－Cl－4alkanediyl－；R2is hydrogen, －OR6, －C(＝O)－R6, －C(＝O)R7, －C(＝O)NR5aR5b, －C(＝O)NHR5c, －NR5aR5b－NHR5c, －NHSOpNR5aR5b, －NR5aSOpR8, or －B(OR6)2；R3andR4are hydrogen or C1－6alkyl； orR3andR4taken together may form a C3－7cycloalkyl ring；nis 3, 4, 5, or 6；pis 1 or 2；arylis phenyl, naphthyl, indanyl, or 1,2,3,4－tetrahydronaphthyl, each of which may be optionally substituted；Hetis 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, being optionally condensed with abenzene ring, and wherein the group Het as a whole may be optionally substituted； 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抑制劑：及其之N－氧化物、鹽類及立體化學異構形，其中R1為芳基或飽和、部分飽和或完全不飽和5或6員單環或8至12員雙環雜環系，其包含一個氮，與選擇性一至三個氧、硫或氮，其中該環系可選擇性經取代；L為一直接鍵、－O－、－O－C1－4烷二基－、－O－CO－、－O－C(＝O)－NR5a－或－O－C(＝O)－NR5a－C1－4烷二基；R2為氫、－OR6、－C(＝O)OR6、－C(＝O)R7、－C(＝O)NR5aR5b、－C(＝O)NHR5c、－NR5aR5b、－NHR5c、－NHSOpNR5aR5b、－NR5aSOpR8或－B(OR6)2；R3及R4為氫或C1－6烷基；或R3及R4一起形成一C3－7環烷基環；n為3、4、5或6；p為1或2；芳基為苯基、萘基、茚基或1,2,3,4－四氫－萘基，各自可選擇性經取代；Het為5或6員之包含1至4個雜原子(分別獨立地選自氮、氧和硫)之飽和、部分飽和或完全不飽和雜環，其選擇性與苯環縮合，且其中該基團Het(整體來看)可選擇性經取代；包含化合物(I)之醫藥組成物及製備化合物(I)之方法。亦提供式(I)之HCV抑制劑與利托那韋(ritonavir)之生物可
