发明名称 Macrocyclic inhibitors of hepatitis C virus
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 —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 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.
申请公布号 US7666834(B2) 申请公布日期 2010.02.23
申请号 US20060995827 申请日期 2006.07.28
申请人 TIBOTEC PHARMACEUTICALS LTD. 发明人 SIMMEN KENNETH ALAN;DE KOCK HERMAN AUGUSTINUS;RABOISSON PIERRE JEAN-MARIE BERNARD;JOENSSON CARL ERIK DANIEL;NILSSON KARL MAGNUS;SAMUELSSON BENGT BERTIL;ROSENQUIST ÅSA ANNICA KRISTINA;ANTONOV DMITRY;SALVADOR ODEN LOURDES;AYESA ALVAREZ SUSANA;CLASSON BJOERN OLOF
分类号 A61K38/00 主分类号 A61K38/00
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