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    Imidazolidinonyl aminopyrimidine compounds for the treatment of cancer
    8.
    发明授权
    Imidazolidinonyl aminopyrimidine compounds for the treatment of cancer 失效
    咪唑烷酰氨基嘧啶化合物治疗癌症

    公开(公告)号：US08063212B2

    公开(公告)日：2011-11-22

    申请号：US12516251

    申请日：2007-12-11

    申请人： Harold Burns Brooks ,  Joyce Z. Crich ,  James Robert Henry ,  Hong-Yu Li ,  Jason Scott Sawyer ,  Yan Wang

    发明人： Harold Burns Brooks ,  Joyce Z. Crich ,  James Robert Henry ,  Hong-Yu Li ,  Jason Scott Sawyer ,  Yan Wang

    IPC分类号： C07D401/00

    CPC分类号： C07D409/14

    摘要： 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.

    摘要翻译： 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。