发明名称 GLYOXAMIDE SUBSTITUTED PYRROLAMIDE DERIVATIVES AND THE USE THEREOF AS MEDICAMENTS FOR THE TREATMENT OF HEPATITIS B
摘要 Inhibitors of HBV replication of Formula (IA);;including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein X and R1 to R6 have the meaning as defined herein.;The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy.
申请公布号 US2016176817(A1) 申请公布日期 2016.06.23
申请号 US201414907109 申请日期 2014.07.25
申请人 Janssen Sciences Ireland UC 发明人 VANDYCK Koen;KESTELEYN Bart Rudolf Romanie;PIETERS Serge Maria Aloysius;ROMBOUTS Geert;VERSCHUEREN Wim Gaston;RABOISSON Pierre Jean-Marie Bernard
分类号 C07D207/34;A61K31/454;A61K31/4025;C07D401/12;A61K31/40;C07D405/12 主分类号 C07D207/34
代理机构 代理人
主权项 1. A compound of Formula (IA)or a stereoisomer or tautomeric form thereof, wherein: each X independently is CR7; R1, R2 and R3 are independently selected from the group consisting of hydrogen, fluoro, chloro, bromo, —CHF2, —CH2F, —CF3, —CN, C1-C3alkyl and C3-C4cycloalkyl; R4 is selected from the group consisting of hydrogen, C1-C3alkyl and C3-C4cycloalkyl; R5 is hydrogen; R6 is selected from the group consisting of C1-C6alkyl and a 3-7 membered saturated ring optionally containing one or more heteroatoms each independently selected from the group consisting of O, S and N, said C1-C6alkyl or said 3-7 membered saturated ring is optionally substituted with one or more substituents selected from the group consisting of fluoro, C3-C4cycloalkyl, —OR8, oxo, —CN, —C(═O)—OR8, —C(═O)—N(R8)2 and C1-C3alkyl, wherein said C1-C3alkyl is optionally substituted with one or more fluoro; each R7 is independently selected from the group consisting of hydrogen, C3-C4cycloalkyl, —CN, fluoro, chloro, bromo and C1-C3alkyl, wherein said C1-C3alkyl is optionally substituted with one or more fluoro; R8 is hydrogen or C1-C3alkyl;or a pharmaceutically acceptable salt or a solvate thereof.
地址 Co Cork IE