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    Methods and Intermediates for the Preparation of Optionally Radio-Labeled Imatinib
    3.
    发明申请
    Methods and Intermediates for the Preparation of Optionally Radio-Labeled Imatinib 审中-公开
    用于制备可选择的无线电标记的伊马替尼的方法和中间体

    公开(公告)号：US20120316338A1

    公开(公告)日：2012-12-13

    申请号：US13526115

    申请日：2012-06-18

    申请人： Rhys Salter ,  Maria Ines Rodriguez Perez ,  Thomas Moenius ,  Rolf Voges ,  Hendrik Andres ,  Kirk Bordeaux

    发明人： Rhys Salter ,  Maria Ines Rodriguez Perez ,  Thomas Moenius ,  Rolf Voges ,  Hendrik Andres ,  Kirk Bordeaux

    IPC分类号： C07D401/14

    CPC分类号： C07D295/155 ,  C07D401/04

    摘要： The invention relates to new processes for the manufacture of N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine (compound of formula I, new processes for the manufacture of metabolites of N-{5[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine observed after administration of the compound to warm-blooded animals as well as to intermediates used in said processes. New starting materials as well as processes for the preparation thereof are likewise the subject of this invention. The processes described herein are especially suitable to furnish said compounds having isotopic labeling. The such obtained labeled compounds are in particular suitable to track and to investigate into the metabolism of N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine and its pharmaceutically acceptable salts in clinical and pre-clinical studies.

    摘要翻译： 本发明涉及制备N- {5- [4-（4-甲基 - 哌嗪子基 - 甲基） - 苯甲酰氨基] -2-甲基苯基} -4-（3-吡啶基）-2-嘧啶 - 胺（ 式I化合物，用于制备N- {5- [4-（4-甲基 - 哌嗪子基 - 甲基） - 苯甲酰氨基] -2-甲基苯基} -4-（3-吡啶基）-2-嘧啶-2-甲酸的代谢物的新方法， 在将化合物给予温血动物以及在所述方法中使用的中间体后观察到胺，新的原料及其制备方法同样是本发明的主题，本文所述的方法特别适用于 所述具有同位素标记的化合物特别适用于追踪和研究N- {5- [4-（4-甲基 - 哌嗪子基 - 甲基） - 苯甲酰氨基] -2-甲基苯基} -2- 4-（3-吡啶基）-2-嘧啶胺及其药学上可接受的盐在临床和临床前研究中。

    METHODS AND INTERMEDIATES FOR THE PREPARATION OF OPTIONALLY RADIO-LABELED IMATINIB
    6.
    发明申请
    METHODS AND INTERMEDIATES FOR THE PREPARATION OF OPTIONALLY RADIO-LABELED IMATINIB 审中-公开
    用于准备无线电标签图像的方法和中间件

    公开(公告)号：US20090299064A1

    公开(公告)日：2009-12-03

    申请号：US11917353

    申请日：2006-06-13

    申请人： Rhys Salter ,  Maria Ines Rodriguez Perez ,  Thomas Moenius ,  Rolf Voges ,  Hendrik Andres ,  Kirk Bordeaux

    发明人： Rhys Salter ,  Maria Ines Rodriguez Perez ,  Thomas Moenius ,  Rolf Voges ,  Hendrik Andres ,  Kirk Bordeaux

    IPC分类号： C07D401/14 ,  C07D401/04 ,  C07D241/04

    CPC分类号： C07D295/155 ,  C07D401/04

    摘要： The invention relates to new processes for the manufacture of N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}4-(3-pyridyl)-2-pyrimidine-amine (compound of formula I, new processes for the manufacture of metabolites of N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine observed after administration of the compound to warm-blooded animals as well as to intermediates used in said processes. New starting materials as well as processes for the preparation thereof are likewise the subject of this invention. The processes described herein are especially suitable to furnish said compounds having isotopic labeling. The such obtained labeled compounds are in particular suitable to track and to investigate into the metabolism of N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}4-(3-pyridyl)-2-pyrimidine-amine and its pharmaceutically acceptable salts in clinical and pre-clinical studies.

    摘要翻译： 本发明涉及制备N- {5- [4-（4-甲基 - 哌嗪子基 - 甲基） - 苯甲酰氨基] -2-甲基苯基} -4-（3-吡啶基）-2-嘧啶 - 胺（化合物 的式I的制备N- {5- [4-（4-甲基 - 哌嗪子基 - 甲基） - 苯甲酰氨基] -2-甲基苯基} -4-（3-吡啶基）-2-嘧啶-4-甲酸的代谢物的新方法， 在将化合物给予温血动物以及在所述方法中使用的中间体后观察到胺，新的原料及其制备方法同样是本发明的主题，本文所述的方法特别适用于 所述具有同位素标记的化合物特别适用于追踪和研究N- {5- [4-（4-甲基 - 哌嗪子基 - 甲基） - 苯甲酰氨基] -2-甲基苯基} 4 - （3-吡啶基）-2-嘧啶胺及其药学上可接受的盐在临床和临床前研究中。