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    • 4. 发明授权
    • Imidazolidinonyl aminopyrimidine compounds for the treatment of cancer
    • 咪唑烷酰氨基嘧啶化合物治疗癌症
    • US08063212B2
    • 2011-11-22
    • US12516251
    • 2007-12-11
    • Harold Burns BrooksJoyce Z. CrichJames Robert HenryHong-Yu LiJason Scott SawyerYan Wang
    • Harold Burns BrooksJoyce Z. CrichJames Robert HenryHong-Yu LiJason Scott SawyerYan Wang
    • C07D401/00
    • C07D409/14
    • 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.
    • 本发明提供了被认为具有通过抑制Plk1治疗癌症的临床用途的新型咪唑烷基氨基嘧啶化合物。 式(I)其中:R1是氨基甲基,(C1-C3烷基)氨基甲基,二(C1-C2烷基)氨基甲基,N-乙基-N-甲基 - 氨基甲基,1-氨基乙基,1-((C1-C2烷基)氨基) 乙基,3,3,3-三氟 - 丙氨基甲基,乙炔基,2-羟基 - 乙氧基,2-羟乙基氨基甲基,2-氰乙基氨基甲基,吗啉-4-基甲基,甲氧基甲氧基甲基,环丙基,1-氮杂环丁基甲基,1-吡咯烷基甲基, 3-二氧戊环-2-基; R2是氢或卤素; R3是氢或卤素; R2和R3中的至少一个是氢; R4是氢,甲基或卤素; 并且是存在或不存在的单键或其药学上可接受的盐。