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    3-HYDROXYISOTHIAZOLE-4-CARBOXAMIDINE DERIVATIVES AS CHK2 INHIBITORS
    3.
    发明申请
    3-HYDROXYISOTHIAZOLE-4-CARBOXAMIDINE DERIVATIVES AS CHK2 INHIBITORS 有权
    作为CHK2抑制剂的3-羟基异噻唑-4-羧酰胺衍生物

    公开(公告)号：US20090137041A1

    公开(公告)日：2009-05-28

    申请号：US12143672

    申请日：2008-06-20

    申请人： Jim Zhen Wu ,  Huanming Chen

    发明人： Jim Zhen Wu ,  Huanming Chen

    IPC分类号： C07D275/03 ,  C12N5/00

    CPC分类号： C07D275/03

    摘要： This invention provides compounds of Formula I which are inhibitors of Chk2 and are useful as a radiation protection agents in anticancer radiotherapy. A method of modulating Chk2 in vitro includes treating a substrate with Chk2 in the presence of compounds of formula I. A method of making a compound of formula I includes: a) forming a biaryl amine having an amino (NH2) group; b) converting the amino group to an isothiocyanate group; c) adding a cyanoacetamide to said isothiocyanate group to form a thioamide adduct; d) cyclizing said thioamide adduct to form an isothiazole having a cyano group; and e) adding an amine to said cyano group to form a carboxamidine group.

    摘要翻译： 本发明提供了作为Chk2抑制剂的式I化合物，可用作抗癌放射治疗中的放射防护剂。 在体外调节Chk2的方法包括在式I化合物存在下用Chk2处理底物。制备式I化合物的方法包括：a）形成具有氨基（NH 2）基团的联芳基胺; b）将氨基转化为异硫氰酸酯基团; c）向所述异硫氰酸酯基团加入氰基乙酰胺以形成硫代酰胺加合物; d）环化所述硫代酰胺加合物以形成具有氰基的异噻唑; 和e）向所述氰基中加入胺形成甲脒基。

    3-hydroxyisothiazole-4-carboxamidine derivatives as CHK2 inhibitors
    9.
    发明授权
    3-hydroxyisothiazole-4-carboxamidine derivatives as CHK2 inhibitors 有权
    3-羟基异噻唑-4-甲脒衍生物作为CHK2抑制剂

    公开(公告)号：US08067452B2

    公开(公告)日：2011-11-29

    申请号：US12143672

    申请日：2008-06-20

    申请人： Jim Zhen Wu ,  Huanming Chen

    发明人： Jim Zhen Wu ,  Huanming Chen

    IPC分类号： A61K31/425 ,  C07D275/03

    CPC分类号： C07D275/03

    摘要： This invention provides compounds of Formula I which are inhibitors of Chk2 and are useful as a radiation protection agents in anticancer radiotherapy. A method of modulating Chk2 in vitro includes treating a substrate with Chk2 in the presence of compounds of formula I. A method of making a compound of formula I includes: a) forming a biaryl amine having an amino (NH2) group; b) converting the amino group to an isothiocyanate group; c) adding a cyanoacetamide to the isothiocyanate group to form a thioamide adduct; d) cyclizing the thioamide adduct to form an isothiazole having a cyano group; and e) adding an amine to the cyano group to form a carboxamidine group.

    摘要翻译： 本发明提供了作为Chk2抑制剂的式I化合物，可用作抗癌放射治疗中的放射防护剂。 在体外调节Chk2的方法包括在式I化合物存在下用Chk2处理底物。制备式I化合物的方法包括：a）形成具有氨基（NH 2）基团的联芳基胺; b）将氨基转化为异硫氰酸酯基团; c）将氰基乙酰胺加入到异硫氰酸酯基中以形成硫代酰胺加合物; d）使硫代酰胺加合物环化以形成具有氰基的异噻唑; 和e）向氰基中加入胺形成甲脒基团。