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33 条记录 (耗时 0.042 秒)

    Substituted arylamino -1,2,3,4-tetrahydro naphthalenes and -2,3-dihydro-1H-indenes as potassium channel modulators
    7.
    发明申请
    Substituted arylamino -1,2,3,4-tetrahydro naphthalenes and -2,3-dihydro-1H-indenes as potassium channel modulators 有权
    取代的芳基氨基-1,2,3,4-四氢萘和2,3-二氢-1H-茚作为钾通道调节剂

    公开(公告)号：US20080146661A1

    公开(公告)日：2008-06-19

    申请号：US11810114

    申请日：2007-06-04

    申请人： Huanming Chen ,  Jean-Michel Vernier

    发明人： Huanming Chen ,  Jean-Michel Vernier

    IPC分类号： A61K31/27 ,  C07C271/30 ,  A61P43/00

    CPC分类号： C07C271/30 ,  C07C233/43 ,  C07C2601/08 ,  C07C2602/08 ,  C07C2602/10

    摘要： This invention provides compounds of formula I where Ar1 is a 5- to 10-member mono- or bicyclic aromatic group, optionally substituted; where the —NR3R4 group is situated ortho to the NHC(═X) group; n=1 or 2; X═O or S; Y is O or S; and q=1 or 0. The invention also provides pharmaceutical compositions comprising compounds of formula I and/or salts, esters, and prodrugs thereof. These compounds modulate the activation and inactivation of potassium channels. The compounds are useful for the treatment and prevention of diseases and disorders—such as seizure disorders—which are affected by modulation of potassium ion channels.

    摘要翻译： 本发明提供式I化合物，其中Ar 1是任选被取代的5至10元单环或双环芳基; 其中-NR 3 R 4 R 4基团位于NHC（-X）基团的邻位; n = 1或2; X-O或S; Y为O或S; 并且q = 1或0.本发明还提供包含式I化合物和/或其盐，酯和前药的药物组合物。 这些化合物调节钾通道的活化和失活。 这些化合物可用于治疗和预防受钾离子通道调节影响的疾病和病症（例如发作障碍）。

    3-hydroxyisothiazole-4-carboxamidine derivatives as CHK2 inhibitors
    10.
    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。