发明名称 Macrocyclic inhibitors of hepatitis C virus
摘要 Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, 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—OR7 or—NH—SO2R8; 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; R4 is aryl or Het; n is 3, 4, 5, or 6; R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R8 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 optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms 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.
申请公布号 US8153800(B2) 申请公布日期 2012.04.10
申请号 US201113197226 申请日期 2011.08.03
申请人 SIMMEN KENNETH ALAN;DE KOCK HERMAN AUGUSTINUS;RABOISSON PIERRE JEAN-MARIE BERNARD;NILSSON KARL MAGNUS;SAMUELSSON BENGT BERTRIL;ROSENQUIST ASA ANNICA KRISTINA;TIBOTEC PHARMACEUTICALS LTD.;MEDIVAR AB 发明人 SIMMEN KENNETH ALAN;DE KOCK HERMAN AUGUSTINUS;RABOISSON PIERRE JEAN-MARIE BERNARD;NILSSON KARL MAGNUS;SAMUELSSON BENGT BERTRIL;ROSENQUIST ASA ANNICA KRISTINA
分类号 C07D215/00;C07C211/00;C07D277/00 主分类号 C07D215/00
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