申请人:Eli Lilly and Company
公开号:US08063212B2
公开(公告)日:2011-11-22
The present invention provides novel imidazolidinonyl aminopyrimidine compounds believed to have clinical use for treatment of cancer through inhibiting Plk1. Formula I wherein: R1 is aminomethyl, (C1-C3 alkyl)aminomethyl, di(C1-C2 alkyl)aminomethyl, N-ethyl-N-methyl-aminomethyl, 1-aminoethyl, 1-((C1-C2 alkyl)amino)-ethyl, 3,3,3-trifluoro-propylaminomethyl, ethynyl, 2-hydroxy-ethoxy, 2-hydroxyethylaminomethyl, 2-cyanoethylaminomethyl, morpholin-4-ylmethyl, methoxymethoxymethyl, cyclopropyl, 1-azetidinylmethyl, 1-pyrrolidinylmethyl, or 1,3-dioxolan-2-yl; R2 is hydrogen or halo; R3 is hydrogen or halo; provided that at least one of R2 and R3 is hydrogen; R4 is hydrogen, methyl, or halo; and is a single bond that is either present or absent, or pharmaceutically acceptable salt thereof.
本发明提供了一种新型咪唑啉基氨基嘧啶化合物,通过抑制Plk1,被认为具有治疗癌症的临床用途。其中,公式I中:R1是氨甲基,(C1-C3烷基)氨甲基,双(C1-C2烷基)氨甲基,N-乙基-N-甲基-氨甲基,1-氨基乙基,1-((C1-C2烷基)氨基)-乙基,3,3,3-三氟丙基氨甲基,乙炔基,2-羟基乙氧基,2-羟乙基氨甲基,2-氰基乙基氨甲基,吗啉-4-基甲基,甲氧基甲氧基甲基,环丙基,1-氮杂环戊基甲基,1-吡咯烷基甲基或1,3-二氧杂环戊烷-2-基;R2是氢或卤素;R3是氢或卤素;前提是R2和R3中至少一个是氢;R4是氢、甲基或卤素;且为可有可无的单键,或其药学上可接受的盐。