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    NOVEL FLUORESCENT DERIVATIVES OF POLYAMINES, METHOD FOR PREPARING SAME AND APPLICATIONS THEREOF AS DIAGNOSIS TOOLS IN THE TREATMENT OF CANCEROUS TUMORS
    5.
    发明申请
    NOVEL FLUORESCENT DERIVATIVES OF POLYAMINES, METHOD FOR PREPARING SAME AND APPLICATIONS THEREOF AS DIAGNOSIS TOOLS IN THE TREATMENT OF CANCEROUS TUMORS 审中-公开
    聚氨酯的新型荧光衍生物，其制备方法及其在治疗癌症肿瘤中的诊断工具的应用

    公开(公告)号：US20100202975A1

    公开(公告)日：2010-08-12

    申请号：US12670611

    申请日：2008-07-28

    申请人： Jean-Philippe Annereau ,  Jean-Marc Barret ,  Yves Guminski ,  Thierry Imbert

    发明人： Jean-Philippe Annereau ,  Jean-Marc Barret ,  Yves Guminski ,  Thierry Imbert

    IPC分类号： A61K49/00 ,  C07D271/12

    CPC分类号： C07D271/12

    摘要： The invention relates to novel fluorescent derivatives of polyamines having a benzoxadiazole group, to a method for preparing the same and to the use thereof as diagnosis tools for emphasising the polyamine transport system in cancerous cells in order to adapt the treatment thereof, and thus for selecting patients carrying such tumours in order to adapt their treatment. The derivatives are of the formula (I) or a pharmaceutically acceptable salt thereof, in which: R1 is one or more NO2 groups in position 4 or 6, or a SO2Ph, SO2NMe2, SO2NH2 or SO3H group; R2 is hydrogen, C1-6 alkyl, benzyl, a perfluoroalkyl group; the values of a, b, c range from 2 to 5 independently from each other and represent alkylene chains separating the amino groups, and the values of d and e can independently be 0 or 1.

    摘要翻译： 本发明涉及具有苯并恶二唑基团的多胺的新型荧光衍生物，其制备方法及其作为诊断工具，用于强调癌细胞中的多胺转运体系以适应其治疗，从而用于选择 携带这种肿瘤的患者为了适应其治疗。 衍生物具有式（I）化合物或其药学上可接受的盐，其中：R1是位置4或6中的一个或多个NO 2基团，或SO 2 Ph，SO 2 NMe 2，SO 2 NH 2或SO 3 H基团; R2是氢，C1-6烷基，苄基，全氟烷基; a，b，c的值彼此独立地为2至5，并且表示分隔氨基的亚烷基链，d和e的值可以独立地为0或1。

    Method for preparing 4β-amino-4′-demethyl-4-desoxypodophyllotoxin
    10.
    发明授权
    Method for preparing 4β-amino-4′-demethyl-4-desoxypodophyllotoxin 有权
    制备4'-二 - 氨基-4'-去甲基-4-脱氧鬼臼毒素的方法

    公开(公告)号：US07932406B2

    公开(公告)日：2011-04-26

    申请号：US11988942

    申请日：2006-07-19

    申请人： Yves Guminski ,  Martial Grousseaud ,  Thierry Imbert

    发明人： Yves Guminski ,  Martial Grousseaud ,  Thierry Imbert

    IPC分类号： C07D317/70

    CPC分类号： C07D493/04

    摘要： The invention relates to a method for synthesizing 4.beta.-amino-4′-demethyl-4-desoxypodophyllotoxin of formula (1), characterized by comprising the following successive steps: a) reacting, in a pure weak acid or in a mixture consisting of acid, water and of organic solvent, without another solvent, at a temperature higher than the ambient temperature, thiourea with 4.beta.-halogenoacetamido-4′-demethyl-4-desoxypodophyllotoxin, and; b) recovering the 4.beta.-amino-4′-demethyl-4-desoxypodophyllotoxin.

    摘要翻译： 本发明涉及一种合成式（1）的β-氨基-4'-脱甲基-4-脱氧鬼臼毒素的方法，其特征在于包括以下连续步骤：a）在纯的弱酸或混合物 由酸，水和有机溶剂组成，没有另一种溶剂，在高于环境温度的温度下，硫脲与4.β-卤代乙酰胺基-4'-去甲基-4-脱氧鬼臼毒素，和 b）回收4.β-氨基-4'-去甲基-4-脱氧鬼臼毒素。