发明名称 PYRIMIDINE FGFR4 INHIBITORS
摘要 Provided herein are compounds of Formula I useful as FGFR4 inhibitors, as well as methods of use of the same.
申请公布号 US2016130237(A1) 申请公布日期 2016.05.12
申请号 US201615000659 申请日期 2016.01.19
申请人 EISAI R&D MANAGEMENT CO., LTD. 发明人 Reynolds Dominic;Hao Ming-Hong;Wang John;Prajapati Sudeep;Satoh Takashi;Selvaraj Anand
分类号 C07D239/48;C07D413/12;C07D403/12;C07D401/12;C07C53/18 主分类号 C07D239/48
代理机构 代理人
主权项 1. A compound of Formula I: wherein: R3 is selected from the group consisting of: C1-6alkyl, C1-6alkoxyC1-6alkyl, NR10R11C1-6alkyl, R10heterocyclylC1-6alkyl, R10arylC1-6alkyl, and R10heteroarylC1-6alkyl, wherein R10 and R11 are each independently selected from the group consisting of: hydrogen and C1-6alkyl;E is selected from the group consisting of: —NR13C(O)CR14═CHR15, and—NR13C(O)C≡CR14, wherein R13 is selected from the group consisting of: hydrogen and methyl, and R14 and R15 are each independently selected from the group consisting of: hydrogen, methyl, fluoro and chloro; R12 is selected from the group consisting of: hydrogen, halo, C1-6alkyl, C1-6alkoxy, hydroxyC1-6alkyl, hydroxyC1-6alkoxy, C1-6alkoxyC1-6alkoxy, C1-6alkoxyC1-6alkyl, R5R6heterocyclyl, —C(O)heterocyclylR5R6, R5R6heterocyclylC1-6alkyl, NR5R6, NR5R6C1-6alkyl, —C(O)NR5R6, and —NR5R6C1-6alkyoxy, wherein R5 and R6 are each independently selected from the group consisting of hydrogen, C1-6alkyl, hydroxyC1-6alkyl, aminoC1-6alkyl, —C(O)C1-6alkyl and C1-6alkylsulfonyl; andR1 is phenyl, wherein said phenyl is substituted 2, 3, or 4 times with independently selected halo or C1-6alkoxy, or a pharmaceutically acceptable salt thereof.
地址 Tokyo JP