发明名称 6,7-dihydrobenzo[a]quinolizin-2-one derivatives for the treatment and prophylaxis of hepatitis B virus infection
摘要 The invention provides novel compounds having the general formula:; wherein R1 to R6, W and X are as described herein and their pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.
申请公布号 US9637485(B2) 申请公布日期 2017.05.02
申请号 US201514926393 申请日期 2015.10.29
申请人 Hoffmann-LA Roche Inc. 发明人 Han Xingchun;Jiang Min;Wang Jianhua;Zhou Chengang;Wang Yongguang;Yang Song
分类号 A61K31/4985;C07D471/04 主分类号 A61K31/4985
代理机构 代理人 Duffield Jonathan
主权项 1. A compound of formula (I)wherein R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen, halogen, C1-6alkyl, diC1-6alkylamino, cyano, N-containing monocyclic heterocycloalkyl and OR7, wherein R7 is hydrogen; C1-6alkyl; or C1-6alkyl which is substituted one or more times by fluoro, C3-7cycloalkyl, phenyl, hydroxyl, amino, C1-6alkoxy, C1-6alkylsulfanyl, C1-6alkylsulfonyl, diC1-6alkylamino, C1-6alkoxycarbonylamino, monocyclic heterocycloalkyl, pyrazoyl or imidazolyl; R5 is hydrogen or C1-6alkyl; R6 is hydrogen, C1-6alkyl, phenyl-CxH2x—, C1-6alkylcarbonyl, C1-6alkylsulfonyl, benzoyl or monocyclic heterocycloalkyl, wherein x is 1-6; W is a bond, CyH2yC(R8)(R9)CzH2z or CyH2yCH(R8)CH(R9)CzH2z, wherein R8 and R9 are independently selected from the group consisting of hydrogen, fluoro, hydroxy and C1-6alkyl, y is 0-6; z is 0-6; X is a bond; O; S; S(O)2; or NR10, wherein R10 is hydrogen or C1-6alkyl; or R6 and R10, together with the nitrogen to which they are attached, form monocyclic heterocycloalkyl; with the proviso that when X is a bond, R6 is not hydrogen, C1-6alkyl or phenyl-CxH2x—; or a pharmaceutically acceptable salt, enantiomer, or diastereoisomer thereof.
地址 Little Falls NJ US