首页> 外国专利> Tetravalent platinum compound-bicyclic double-bond-containing amphiphilic polymer prodrug, nano-micelle, preparation method and application thereof

Tetravalent platinum compound-bicyclic double-bond-containing amphiphilic polymer prodrug, nano-micelle, preparation method and application thereof

机译:四价铂复合 - 双环双键含两亲聚合物前药,纳米胶束,其制备方法和应用

摘要

A tetravalent platinum compound-bicyclic double-bond-containing amphiphilic polymer prodrug, which has the structure as shown in formula (I):; embedded image when m=1,; embedded image represents; embedded image when m=0,; embedded image represents; embedded image R represents —CH3 or —CH2CH3; L1 and L2 independently represent Cl, N3, NO3,; embedded image and n is from 10 to 80. A preparation method of the prodrug is also disclosed. The method includes a step of reacting an axially dihydroxy-coordinated tetravalent platinum compound with a bicyclic double-bond-containing orthoester precursor. In addition, a nano-micelle formed by the prodrug and an application thereof are further disclosed. The amphiphilic polymer prodrug and the micelle formed therefrom have pH hypersensitivity and reduction dual responsiveness.
机译:四价铂化合物 - 双环双键的两亲性聚合物前药,其具有如式(I)所示的结构: <化学ID =“Chem-US-00001”> “嵌入式图像”文件=“US10947261-20210316-C00001.gif”他=“19.13mm”ImgContent 当m = 1时,; <化学ID =“Chem-US-00002”> “嵌入图像”文件=“US10947261-20210316-C00002.gif”他=“8.38mm”imgContent 代表; <化学ID =“Chem-US-00003”> “嵌入图像”文件=“US10947261-20210316-C00003.gif”他=“9.65mm”ImgContent 当m = 0时,; <化学ID =“Chem-US-00004”> “嵌入图像”文件=“US10947261-20210316-C00004.gif”他=“8.21mm”imgContent 代表; <化学ID =“Chem-US-00005”> “嵌入式图像”文件=“US10947261-20210316-C00005.gif”他=“10.08mm”imgcontent R表示-CH 3 或-ch 2 ch 3 ; l 1 和l 2 独立表示CL,n 3 ,no 3 ,; <化学ID =“Chem-US-00006”> “嵌入图像”文件=“US10947261-20210316-C00006.gif”他=“18.71mm”ImgContent 并且N为10至80.还公开了前药的制备方法。该方法包括使轴向二羟基协调的含有双环双键的正烯酯前体反应的轴向二羟基协调的四价铂化合物的步骤。另外,进一步公开了由前药形成的纳米胶束和其应用。两亲性聚合物前药和由此形成的胶束具有pH超敏反应和减少双重反应性。

著录项

  • 公开/公告号US10947261B2

    专利类型

  • 公开/公告日2021-03-16

    原文格式PDF

  • 申请/专利权人 ANHUI UNIVERSITY;

    申请/专利号US201716476080

  • 发明设计人 RUPEI TANG;LIEFENG HU;

    申请日2017-12-29

  • 分类号A61K45/06;C07F15;C08G65/26;

  • 国家 US

  • 入库时间 2022-08-24 17:43:19

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