发明名称 Phenyl ethynyl derivatives as hepatitis C virus inhibitors
摘要 Inhibitors of HCV replication of formula I; including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R* have the meaning defined in the claims. ;The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in the treatment or prophylaxis of HCV.
申请公布号 US9045463(B2) 申请公布日期 2015.06.02
申请号 US201013389269 申请日期 2010.08.06
申请人 Janssen R&D Ireland 发明人 McGowan David;Demin Samuel Dominique;Last Stefaan Julien;Vandyck Koen;Raboisson Pierre Jean-Marie Bernard
分类号 A61K31/4178;C07D403/14;C07D403/04;C07D405/14;C07D413/14 主分类号 A61K31/4178
代理机构 代理人
主权项 1. A compound of formula I: or a stereoisomer thereof, wherein: R and R* are each independently —CR1R2R3, C1-4alkylamino, benzylamino, arylamino, aryl optionally substituted with 1 or 2 substituents selected from halo and methyl, hetero C4-7cycloalkyl; wherein R1 is selected from C1-4alkyl; phenyl optionally substituted with 1, 2 or 3 substituents independently selected from halo, C1-4alkyl, C1-4alkoxy, trifluoromethoxy or 2 substituents on adjacent ring atoms form a 1,3-dioxolane group; benzyl optionally substituted with halo or methoxy; phenylsulfonylmethyl; heteroaryl; heteroarylmethyl; and C3-6cycloalkyl;R2 is selected from hydrogen, hydroxyl, amino, mono- and di-C1-4alkylamino, C1-4alkylcarbonylamino, C1-4alkyloxycarbonylamino, C1-4alkylamino-carbonylamino, piperidin-1-yl or imidazol-1-yl;R3 is hydrogen, or alternatively,R2 and R3 together form an oxo group; orR1 and R3 together form cyclopropyl;provided that when either one of R or R* represents —CH(C6H5)N(CH3)2 then the other cannot be —CH(C6H5)NHC(═O)OCH3; and when R and R* are identical, then R1 is other than phenyl when R2 is hydroxyl, acetylamino, methoxycarbonylamino or tert. butoxycarbonylamino and R3 is hydrogen; and R1 is other than C1-4alkyl when R2 is C1-4alkylcarbonylamino and R3 is hydrogen; or a pharmaceutically acceptable salt thereof.
地址 Little Island, Co. Cork IE