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    • 73. 发明公开
    • METHODS FOR THE PREPARATION OF TARGETING AGENT FUNCTIONALIZED DIBLOCK COPOLYMERS FOR USE IN FABRICATION OF THERAPEUTIC TARGETED NANOPARTICLES
    • 过程与靶向药物的官能嵌段共聚物FOR USE在治疗的纳米粒子的生产PRODUCING
    • EP2285350A2
    • 2011-02-23
    • EP09794932.5
    • 2009-06-16
    • Bind Biosciences, Inc.
    • ALI, Mir, M.HRKACH, JeffZALE, Stephen, E.ALVAREZ DE CIENFUEGOS, Luis
    • 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.
    • (因此,通过被称为PEG),本申请提供了使用官能化的预聚(乙二醇)作为二嵌段共聚物的合成中的宏引发剂制备纳米颗粒的方法。 这些二嵌段共聚物包含聚(乙二醇)嵌段轴承在其末端和靶向剂的第二生物相容的和生物可降解的疏水性聚合物嵌段(例如,聚(酯))。 的聚(乙二醇)是异双功能与靶向部分(剂)共价结合到其α末端和聚合引发官能团(E. G.,羟基)存在于它的ω末端。 开环聚合反应得到所需的聚(酯)聚(乙二醇)靶向剂的聚合物并用于赋予靶向能力对治疗纳米颗粒。 这种方法“从聚合”采用典型地,靶向剂的前体worin靶向剂的官能团的反应性,使用的保护基团掩蔽。 如此描述为“耦合于”所使用的聚(乙二醇)靶向剂缀合物,其中所述靶向剂保持在其天然的未保护的形式。该方法使用“正交”化学确实表现出对通常发现的官能团没有交叉反应 中的定位感兴趣的代理商。 纳米颗粒产生的雅丁到盘游离缺失的方法以及它们在各种疾病的治疗中的用途因此被提供。