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    • 9. 发明申请
    • POLYMALIC ACID BASED NANOCONJUGATES FOR IMAGING
    • 基于聚合酸的纳米颗粒成像
    • WO2012139030A1
    • 2012-10-11
    • PCT/US2012/032573
    • 2012-04-06
    • CEDARS-SINAI MEDICAL CENTERBLACK, Keith L.LJUBIMOVA, Julia Y.LJUBIMOV, Alexander V.HOLLER, Eggehard
    • BLACK, Keith L.LJUBIMOVA, Julia Y.LJUBIMOV, Alexander V.HOLLER, Eggehard
    • A61K49/00C07C211/00
    • A61K49/16A61K47/593A61K49/128
    • Nanoconjugates include a polymalic-based molecular scaffold with one or more imaging moiety and one or more targeting modules attached to the scaffold. At least one imaging moiety and at least one targeting module is conjugated to the polymalicacid based molecular scaffold. Methods of synthesizing the nanoconjugate involve providing a polymalic acid having a plurality of pendant carboxyi groups. The method reacts a compound containing sulfhydryl groups and amino acid groups through the pendant carboxyi groups to add sulfhydryl groups to the polymalic acid to form an activated polymalic acid. The method reacts at least one imaging moiety containing a sulfhydryl binding group to the activated polymalic acid to form a preconjugate. The method may involve administering to the subject a nanoconjugate that includes a polymalic acid-based molecular scaffold, at least one imaging moiety, and at least one targeting module.
    • 纳米缀合物包括具有一个或多个成像部分和连接到支架的一个或多个靶向模块的基于聚丙烯的分子支架。 至少一个成像部分和至少一个靶向模块与基于聚缩水甘油的分子支架缀合。 合成纳米缀合物的方法涉及提供具有多个侧链羧基的聚丙酸。 该方法通过侧基羧基将含有巯基和氨基酸的化合物反应,以向聚丙酸中加入巯基以形成活化的聚丙酸。 该方法将含有巯基结合基团的至少一个成像部分与活化的聚丙酸反应形成预共轭物。 该方法可以包括向受试者施用包括基于聚丙酸的分子支架,至少一个成像部分和至少一个靶向模块的纳米缀合物。