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    • 1. 发明申请
    • Method of Biomolecule Immobilization On Polymers Using Click-Type Chemistry
    • 使用点击式化学的聚合物上生物分子固定的方法
    • US20090297609A1
    • 2009-12-03
    • US11988207
    • 2006-07-06
    • Molly S. ShoichetYumin YuanMeng ShiJordan Wosnick
    • Molly S. ShoichetYumin YuanMeng ShiJordan Wosnick
    • A61K9/14A61K39/395A61K35/12A61K35/76A61K38/43A61K38/00A61K31/7088C08F18/24C08F24/00C08F116/02C08F20/58C07C43/00
    • C08G63/912A61K47/48907A61K47/6935C08G63/64C08G64/0241C08G64/42
    • The present invention provides a method for the covalent immobilization of biomolecules on polymers for delivery of the biomolecules, which has the advantage of being simple, highly efficient, environmentally friendly and free of side products relative to traditional immobilization techniques. The invention provides a modified micro/nanoparticle system, which uses a functionalized polymer formed into micro or nanoparticles to bind a molecule to the particles using uses facile chemistry, the Diels-Alder cycloaddition between a diene and a dienophile with the polymer being functionalized with one of them and the molecule with the other, or the Huisgen 1,3-dipolar cycloaddition between a terminal alkyne and an azide to bind the molecule to the particle. The molecules and/or other therapeutic agents may be encapsulated within the polymer particles for intravenous therapeutic delivery. The invention also provides a novel synthetic biodegradable polymer, a furan/alkyne-functionalized poly(trimethylene carbonate) (PTMC)-based polymer, whose composition can be designed to meet the defined physical and chemical property requirements. In one example, the particle system self-aggregates from functionalized PTMC-based copolymers containing poly(ethylene glycol) (PEG) segments. The composition of the copolymers can be designed to meet various particle system requirements, including size, thermodynamic stability, surface PEG density, drug encapsulation capacity and biomolecule immobilization capacity.
    • 本发明提供了生物分子共价固定在聚合物上用于递送生物分子的方法,其具有相对于传统固定技术简单,高效,环保且无副产物的优点。 本发明提供了一种修饰的微/纳米颗粒体系,其使用形成微米或纳米颗粒的官能化聚合物使用易于使用的化学方法将分子与颗粒结合,二烯与亲双烯体之间的Diels-Alder环加成与聚合物被一个官能化 的分子和另一个分子,或者在末端炔烃和叠氮化物之间的Huisgen 1,3-偶极环加成以将分子结合到颗粒。 分子和/或其它治疗剂可以包封在聚合物颗粒内用于静脉内治疗递送。 本发明还提供了一种新型的合成可生物降解聚合物,呋喃/炔官能化的聚(碳酸亚丙基酯)(PTMC)(PTMC))聚合物,其组合物可以被设计成满足规定的物理和化学性质要求。 在一个实例中,颗粒系统自聚集于含有聚(乙二醇)(PEG)链段的官能化的基于PTMC的共聚物。 共聚物的组成可以设计成满足各种颗粒系统的要求,包括尺寸,热力学稳定性,表面PEG密度,药物包封能力和生物分子固定能力。
    • 2. 发明授权
    • Method of biomolecule immobilization on polymers using click-type chemistry
    • 使用点击式化学的聚合物上生物分子固定的方法
    • US09290617B2
    • 2016-03-22
    • US11988207
    • 2006-07-06
    • Molly S. ShoichetYumin YuanMeng ShiJordan Wosnick
    • Molly S. ShoichetYumin YuanMeng ShiJordan Wosnick
    • A61K47/00C08G64/00C08G63/91C08G63/64C08G64/02C08G64/42A61K47/48
    • C08G63/912A61K47/48907A61K47/6935C08G63/64C08G64/0241C08G64/42
    • The present invention provides a method for the covalent immobilization of biomolecules on polymers for delivery of the biomolecules, which has the advantage of being simple, highly efficient, environmentally friendly and free of side products relative to traditional immobilization techniques. The invention provides a modified micro/nanoparticle system, which uses a functionalized polymer formed into micro or nanoparticles to bind a molecule to the particles using uses facile chemistry, the Diels-Alder cycloaddition between a diene and a dienophile with the polymer being functionalized with one of them and the molecule with the other, or the Huisgen 1,3-dipolar cycloaddition between a terminal alkyne and an azide to bind the molecule to the particle. The molecules and/or other therapeutic agents may be encapsulated within the polymer particles for intravenous therapeutic delivery. The invention also provides a novel synthetic biodegradable polymer, a furan/alkyne-functionalized poly(trimethylene carbonate) (PTMC)-based polymer, whose composition can be designed to meet the defined physical and chemical property requirements. In one example, the particle system self-aggregates from functionalized PTMC-based copolymers containing poly(ethylene glycol) (PEG) segments. The composition of the copolymers can be designed to meet various particle system requirements, including size, thermodynamic stability, surface PEG density, drug encapsulation capacity and biomolecule immobilization capacity.
    • 本发明提供了生物分子共价固定在聚合物上用于递送生物分子的方法,其具有相对于传统固定技术简单,高效,环保且无副产物的优点。 本发明提供了一种修饰的微/纳米颗粒体系,其使用形成微米或纳米颗粒的官能化聚合物,以使用易于使用的化学,二烯和亲二烯体之间的Diels-Alder环加成,聚合物被一个官能化 的分子和另一个分子,或者在末端炔烃和叠氮化物之间的Huisgen 1,3-偶极环加成以将分子结合到颗粒。 分子和/或其它治疗剂可以包封在聚合物颗粒内用于静脉内治疗递送。 本发明还提供了一种新型的合成可生物降解聚合物,呋喃/炔官能化的聚(碳酸亚丙基酯)(PTMC)(PTMC))聚合物,其组合物可以被设计成满足规定的物理和化学性质要求。 在一个实例中,颗粒系统自聚集于含有聚(乙二醇)(PEG)链段的官能化的基于PTMC的共聚物。 共聚物的组成可以设计成满足各种颗粒系统的要求,包括尺寸,热力学稳定性,表面PEG密度,药物包封能力和生物分子固定能力。