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    • 10. 发明授权
    • Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles
    • 制备用于制备治疗靶向纳米颗粒的靶向剂官能化二嵌段共聚物的方法
    • US08734846B2
    • 2014-05-27
    • US13667299
    • 2012-11-02
    • Bind Biosciences, Inc.
    • Mir M. AliJeff HrkachStephen E. ZaleLuis Alvarez de Cienfuegos
    • A61K9/14
    • A61K47/34A61K9/5153A61K47/60A61K47/6911
    • This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization from” approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling to” that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonal” chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.
    • 本申请提供纳米颗粒和使用预官能化聚(乙二醇)(也称为PEG)作为二嵌段共聚物合成的大分子引发剂制备纳米颗粒的方法。 开环聚合产生用于赋予治疗性纳米颗粒靶向能力的所需聚(酯) - 聚(乙二醇) - 靶向剂聚合物。 这种“聚合”方法通常使用靶向剂的前体,其中靶向剂的官能团的反应性使用保护基掩蔽。 还描述了使用聚(乙二醇) - 靶向剂缀合物的“偶联”,其中靶向剂保持其天然未保护形式。 该方法使用对正常感兴趣的靶向剂中通常发现的官能团没有交叉反应性的“正交”化学。