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    • 1. 发明申请
    • METHODS FOR THE PREPARATION OF TARGETING AGENT FUNCTIONALIZED DIBLOCK COPOLYMERS FOR USE IN FABRICATION OF THERAPEUTIC TARGETED NANOPARTICLES
    • 制备用于制备治疗性靶向纳米颗粒的靶向功能性二嵌段共聚物的方法
    • WO2010005740A2
    • 2010-01-14
    • PCT/US2009/047554
    • 2009-06-16
    • BIND BIOSCIENCES, INC.ALI, Mir, M.HRKACH, JeffZALE, Stephen, E.
    • ALI, Mir, M.HRKACH, JeffZALE, Stephen, E.
    • A61K9/16A61K47/34A61P35/00
    • A61K47/34A61K9/5153A61K47/60A61K47/6911
    • This application provides methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. These diblock copolymers comprise a poly(ethylene glycol) block bearing a targeting agent at its terminus and a second biocompatible and biodegradable hydrophobic polymer block (e.g. a poly(ester)). The poly(ethylene glycol) is hetero-bifunctional with a targeting moiety (agent) covalently bound to its α terminus and a polymerization initiating functional group (e.g., a hydroxyl group) present on its ω terminus. 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. Nanoparticles produced according to the disclosed methods as well as their use in the treatment of various diseases are also provided.
    • 本申请提供了使用预官能化聚(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。 这些二嵌段共聚物包含在其末端具有靶向剂的聚(乙二醇)嵌段和第二生物相容性和可生物降解的疏水性聚合物嵌段(例如聚(酯))。 聚(乙二醇)与共价结合到其末端的靶向部分(试剂)和存在于其末端的聚合引发官能团(例如羟基)是异双官能的。 总站。 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。 还提供了根据所公开的方法制备的纳米颗粒及其在治疗各种疾病中的用途。