发明名称 Macrocyclic inhibitors of hepatitis C virus
摘要 Inhibitors of HCV replication of formula (I); wherein W is a heterocycle of formula ; and the remaining variables are as defined in the specification.
申请公布号 US8754116(B2) 申请公布日期 2014.06.17
申请号 US201213451660 申请日期 2012.04.20
申请人 Janssen R&D Ireland 发明人 Simmen Kenneth Alan;De Kock Herman Augustinus;Raboisson Pierre Jean-Marie Bernard;Surleraux Dominique Louis Nestor Ghislain;Van De Vreken Wim
分类号 A61K31/407;C07D487/04 主分类号 A61K31/407
代理机构 代理人 Kamage Andrea Jo
主权项 1. A compound having the formula an N-oxide, salt, or stereoisomer thereof, wherein each dashed line (represented by - - - - -) represents an optional double bond; X is CH and where X bears a double bond it is C; R1 is —OR11, or —NH—SO2R12; 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; W is a heterocycle of formula Q is N or CR4; R4 is hydrogen; phenyl optionally substituted with C1-6alkyl or with C1-6alkoxy; thiazolyl optionally substituted with C1-6alkyl; or pyridyl; R5 is phenyl optionally substituted with C1-6alkyl or with C1-6alkoxy; thiazolyl optionally substituted with C1-6alkyl; or pyridyl; one of R6, R7 is phenyl optionally substituted with C1-6alkyl or with C1-6alkoxy; thiazolyl optionally substituted with C1-6alkyl; or pyridyl; while the other of R6, R7 is hydrogen; phenyl optionally substituted with C1-6alkyl or with C1-6alkoxy; thiazolyl optionally substituted with C1-6alkyl; or pyridyl; one of R8, R9, R10 is phenyl optionally substituted with C1-6alkyl or with C1-6alkoxy; thiazolyl optionally substituted with C1-6alkyl; or pyridyl; while the other two of R8, R9, R10 independently are hydrogen; phenyl optionally substituted with C1-6alkyl or with C1-6alkoxy; thiazolyl optionally substituted with C1-6alkyl; or pyridyl; R11 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R12 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; each aryl as a group or part of a group is phenyl, optionally substituted with one, two or three substituents selected from halo, hydroxy, nitro, cyano, carboxyl, C1-6alkyl, C1-6alkoxy, C1-6alkoxyC1-6alkyl, C1-6alkylcarbonyl, amino, mono- or diC1-6alkylamino, azido, mercapto, polyhaloC1-6alkyl, polyhaloC1-6alkoxy, C3-7cycloalkyl, pyrrolidinyl, piperidinyl, piperazinyl, 4-C1-6alkyl-piperazinyl, 4-C1-6alkylcarbonyl-piperazinyl, morpholinyl; wherein the morpholinyl and piperidinyl groups may be optionally substituted with one or with two C1-6alkyl radicals; and each Het as a group or part of a group is 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, and being optionally substituted with one, two or three substituents each independently selected from the group consisting of halo, hydroxy, nitro, cyano, carboxyl, C1-6alkyl, C1-6alkoxy, C1-6alkoxyC1-6alkyl, C1-6alkylcarbonyl, amino, mono- or diC1-6alkylamino, azido, mercapto, polyhaloC1-6alkyl, polyhaloC1-6alkoxy, C3-7cycloalkyl, pyrrolidinyl, piperidinyl, piperazinyl, 4-C1-6alkyl-piperazinyl,4-C1-6alkylcarbonyl-piperazinyl, morpholinyl; wherein the morpholinyl and piperidinyl groups may be optionally substituted with one or with two C1-6alkyl radicalsand wherein said compound is other than a solvate.
地址 Little Cork, Co IE