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, —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, 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 US9353103(B2) 申请公布日期 2016.05.31
申请号 US201514684649 申请日期 2015.04.13
申请人 Janssen Sciences Ireland UC;Medivir AB 发明人 Simmen Kenneth Alan;De Kock Herman Augustinus;Raboisson Pierre Jean-Marie Bernard;Hu Lili;Tahri Abdellah;Surleraux Dominique Louis Nestor Ghislain;Nilsson Karl Magnus;Samuelsson Bengt Bertil;Rosenquist Asa Annica Kristina;Ivanov Vladimir;Pelcman Mikael;Belfrage Anna Karin Gertrud Linea;Johansson Per-Ola Mikael;Vendeville Sandrine Marie Helene
分类号 A61K31/465;C07D417/14;C07D245/04;C07D277/56;C07D417/04;C07D487/04;A61K31/427;A61K31/4709;A61K38/21;C07D401/14;A61K45/06;A61K38/05;C07K5/078 主分类号 A61K31/465
代理机构 Baker & Hostetler LLP 代理人 Baker & Hostetler LLP
主权项 1. A method of treating a hepatitis C virus (HCV) infection in a patient comprising administering to the patient: a compound having the formula  or a pharmaceutically acceptable salt thereof; and another anti-HCV agent.
地址 Little Island, Co. Cork IE