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    Quinoline derivatives for modulating DNA methylation
    1.
    发明授权
    Quinoline derivatives for modulating DNA methylation 失效
    用于调节DNA甲基化的喹啉衍生物

    公开(公告)号：US07939546B2

    公开(公告)日：2011-05-10

    申请号：US12422067

    申请日：2009-04-10

    申请人： Pasit Phiasivongsa ,  Sanjeev G. Redkar ,  Swarna Gamage ,  Darby Brooke ,  William Denny ,  David J. Bearss ,  Hariprasad Vankayalapati ,  Yong Xu ,  Krzysztof Swierczek

    发明人： Pasit Phiasivongsa ,  Sanjeev G. Redkar ,  Swarna Gamage ,  Darby Brooke ,  William Denny ,  David J. Bearss ,  Hariprasad Vankayalapati ,  Yong Xu ,  Krzysztof Swierczek

    IPC分类号： A61K31/47

    CPC分类号： C07D401/12

    摘要： Quinoline derivatives, particularly 4-(4-(4-(quinolin-4-ylamino)benzamido)phenylthio)pyrrolidine-2-carboxylic acid; 3-(4-(4-(quinolin-4-ylamino)benzamido)phenylthio)pyrrolidine; N-(4-(piperidin-4-ylthio)phenyl)-4-(quinolin-4-ylamino)-benzamide; and N-(4-(piperidin-3-ylthio)phenyl)-4-(quinolin-4-ylamino)-benzamide, or a physiologically acceptable salt thereof, are provided. Such quinoline derivatives can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position, for example via selective inhibition of DNA methyltransferase DNMT1. Methods for synthesizing numerous 4-anilinoquinoline derivatives and for modulating DNA methylation are provided. Also provided are methods for formulating and administering these compounds or compositions to treat conditions such as cancer and hematological disorders.

    摘要翻译： 喹啉衍生物，特别是4-（4-（4-（喹啉-4-基氨基）苯甲酰氨基）苯硫基）吡咯烷-2-甲酸; 3-（4-（4-（喹啉-4-基氨基）苯甲酰氨基）苯硫基）吡咯烷; N-（4-（哌啶-4-基硫基）苯基）-4-（喹啉-4-基氨基） - 苯甲酰胺; 和N-（4-（哌啶-3-基硫基）苯基）-4-（喹啉-4-基氨基） - 苯甲酰胺或其生理上可接受的盐。 这样的喹啉衍生物可用于DNA甲基化的调节，例如通过选择性抑制DNA甲基转移酶DNMT1有效抑制C-5位上胞嘧啶的甲基化。 提供了合成大量4-苯胺基喹啉衍生物和调节DNA甲基化的方法。 还提供了用于配制和施用这些化合物或组合物以治疗诸如癌症和血液学疾病的病症的方法。

    Quinoline derivatives for modulating DNA methylation
    6.
    发明授权
    Quinoline derivatives for modulating DNA methylation 失效
    用于调节DNA甲基化的喹啉衍生物

    公开(公告)号：US07790746B2

    公开(公告)日：2010-09-07

    申请号：US11959181

    申请日：2007-12-18

    申请人： Pasit Phiasivongsa ,  Sanjeev G. Redkar ,  Swarna Gamage ,  Darby Brooke ,  William Denny ,  David J. Bearss ,  Hariprasad Vankayalapati

    发明人： Pasit Phiasivongsa ,  Sanjeev G. Redkar ,  Swarna Gamage ,  Darby Brooke ,  William Denny ,  David J. Bearss ,  Hariprasad Vankayalapati

    IPC分类号： A61K31/47

    CPC分类号： C07D401/12

    摘要： Quinoline derivatives, particularly 4-anilinoquinoline derivatives of formula (I), are provided: Such quinoline derivatives can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position, for example via selective inhibition of DNA methyltransferase DNMT 1. Methods for synthesizing numerous 4-anilinoquinoline derivatives and for modulating DNA methylation are provided. Also provided are methods for formulating and administering these compounds or compositions to treat conditions such as cancer and hematological disorders.

    摘要翻译： 提供了喹啉衍生物，特别是式（I）的4-苯胺基喹啉衍生物：这样的喹啉衍生物可用于DNA甲基化的调节，例如有效抑制胞嘧啶在C-5位甲基化，例如通过选择性抑制 DNA甲基转移酶DNMT 1.提供了合成大量4-苯胺基喹啉衍生物和调节DNA甲基化的方法。 还提供了用于配制和施用这些化合物或组合物以治疗诸如癌症和血液学疾病的病症的方法。