SIMMEN, KENNETH ALAN,施艾伦,施艾倫,DE KOCK, HERMAN AUGUSTINUS,戴寇克,戴寇克,RABOISSON, PIERRE JEAN-MARIE,卢伯森,盧伯森,TAHRI, ABDELLAH,艾德拉,艾德拉,NILSSON, KARL MAGNUS,尼斯欧,尼斯歐,SAMUELSSON, BENGT BERTI,贝帝尔,貝帝爾,ROSENQUIST, AS
申请号：
TW095127589
公开号：
TWI383980B
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)theN-oxides, salts, and stereochemically isomeric forms thereof, wherein each dashed line (representedby-----) represents an optional double bondXis N, CH and where X bears a double bond it is CR1is aryl or a saturated, a partially unsaturated or completely unsaturated 5 or 6 membered monocyclic or 9 to 12 membered bicyclic heterocyclic ring system wherein said ring system contains one nitrogen, and optionally one to three additional heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen, and wherein the remaining ring members are carbon atoms wherein said ring system may be optionally substituted on any carbon or nitrogen ring atom with one, two, three, or four substituentsLis a direct bond, -O-, -O-C1-4alkanediyl-, -O-C(=O)-, -O-C(=O)-NR4a- or -O-C(=O)-NR4aC1-4alkanediyl-R2is hydrogen, -OR5, -C(=O)OR5, -C(=O)R6, -C(=O)NR4aR4b, -C(=O)NHR4c, -NR4aR4b, -NHR4c, -NR4aSOpNR4aR4b, -NR4aSOpR7, or B (OR5)2R3is hydrogen, and whereXis C or CH,R3may also be C1-6alkylnis 3, 4, 5, or 6pis 1 or 2arylis phenyl, naphthyl, indanyl, or 1,2,3,4-tetrahydronaphthyl, each of which may be optionally substituted with one, two or three substituentsHetis 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 a benzene ring, and wherein the group Het as a whole may be 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,其中各個虛線(以-----代表者)代表一種選擇的雙鍵;X為N,CH且當其中X攜載雙鍵時,其為C;R1為芳基或一種飽和的、部分不飽和的或完全地不飽和的5或6成員的單環性或9至12成員的雙環性雜環環系,其中所述的環系含有一個氮原子,及選擇地一至三個另外的挑選自包括氧、硫及氮之雜原子,且其中剩餘的環成員為碳原子;其中該環系可選擇地經1,2,3,或4個取代基於任一碳或氮環原子上取代;L為直接鍵,-O-,-O-C1-4烷二基-,-O-C(
