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1. 发明申请

US20090297609A1 Method of Biomolecule Immobilization On Polymers Using Click-Type Chemistry 有权
标题翻译：使用点击式化学的聚合物上生物分子固定的方法
公开(公告)号：US20090297609A1
公开(公告)日：2009-12-03
申请号：US11988207
申请日：2006-07-06
申请人： Molly S. Shoichet , Yumin Yuan , Meng Shi , Jordan Wosnick
发明人： Molly S. Shoichet , Yumin Yuan , Meng Shi , Jordan Wosnick
IPC分类号： A61K9/14 , A61K39/395 , A61K35/12 , A61K35/76 , A61K38/43 , A61K38/00 , A61K31/7088 , C08F18/24 , C08F24/00 , C08F116/02 , C08F20/58 , C07C43/00
CPC分类号： C08G63/912 , A61K47/48907 , A61K47/6935 , C08G63/64 , C08G64/0241 , C08G64/42
摘要： 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.
摘要翻译：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

US09290617B2 Method of biomolecule immobilization on polymers using click-type chemistry 有权
标题翻译：使用点击式化学的聚合物上生物分子固定的方法
公开(公告)号：US09290617B2
公开(公告)日：2016-03-22
申请号：US11988207
申请日：2006-07-06
申请人： Molly S. Shoichet , Yumin Yuan , Meng Shi , Jordan Wosnick
发明人： Molly S. Shoichet , Yumin Yuan , Meng Shi , Jordan Wosnick
IPC分类号： A61K47/00 , C08G64/00 , C08G63/91 , C08G63/64 , C08G64/02 , C08G64/42 , A61K47/48
CPC分类号： C08G63/912 , A61K47/48907 , A61K47/6935 , C08G63/64 , C08G64/0241 , C08G64/42
摘要： 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.
摘要翻译：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。

3. 发明申请

US20050048555A1 FRET imaging using an iterative estimation algorithm 审中-公开
标题翻译： FRET成像使用迭代估计算法
公开(公告)号：US20050048555A1
公开(公告)日：2005-03-03
申请号：US10920619
申请日：2004-08-18
申请人： Timothy Holmes , Yupeng Zhang , Yumin Yuan
发明人： Timothy Holmes , Yupeng Zhang , Yumin Yuan
IPC分类号： C12Q1/68 , G06T7/00 , C12M1/34 , G06K9/00
CPC分类号： G06T7/32 , C12Q1/6818
摘要： A method and method for processing fluorescence resonance energy transfer (FRET) image data. The method includes the steps of obtaining a set of FRET images and a set of calibration images for a biological sample; and generating a set of estimation images with an estimation algorithm that uses image data from the set of FRET images and the set of calibration images.
摘要翻译：用于处理荧光共振能量转移（FRET）图像数据的方法和方法。该方法包括以下步骤：获得用于生物样品的一组FRET图像和一组校准图像; 以及使用具有来自所述一组FRET图像和所述一组校准图像的图像数据的估计算法生成一组估计图像。

4. 发明授权

US08652504B2 Solid polymer delivery compositions and methods for use thereof 有权
标题翻译：固体聚合物输送组合物及其使用方法
公开(公告)号：US08652504B2
公开(公告)日：2014-02-18
申请号：US11525491
申请日：2006-09-21
申请人： Hong Li , William G. Turnell , Yumin Yuan , Geoffrey C. Landis , Ryan L. Knoy
发明人： Hong Li , William G. Turnell , Yumin Yuan , Geoffrey C. Landis , Ryan L. Knoy
IPC分类号： A61K48/00 , A61K39/395 , C08F20/00 , A61F2/02
CPC分类号： C08G69/44 , A61K9/0024 , A61K47/34 , A61L27/34 , A61L31/10 , C08L77/12 , C08L2666/02
摘要： The present invention provides an implantable solid polymer delivery composition that can be formulated to release a bioactive agent to an interior body site at a controlled rate over an extended period of time by adjusting the various components of the composition. The controlled delivery of the composition avoids an initial drug spike, resulting in a smooth delivery profile over time. Polymer layers in the composition can be porous and are both biodegradable in water and body enzymes and biocompatible. Methods of making the implantable solid polymer compositions and methods of delivering a bioactive agent at a controlled rate to an interior body site are also provided.
摘要翻译：本发明提供了一种可植入的固体聚合物递送组合物，其可通过调节组合物的各种成分而配制成在长时间内以受控的速率将生物活性剂释放到内部身体部位。组合物的受控输送避免了初始药物尖峰，导致随着时间的顺利递送。组合物中的聚合物层可以是多孔的，并且在水和身体酶中都是可生物降解的并且是生物相容的。还提供了制造可植入固体聚合物组合物的方法和将受控速率递送至内部身体部位的生物活性剂的方法。

5. 发明申请

US20060177495A1 Polymer-lipid delivery vehicles 审中-公开
公开(公告)号：US20060177495A1
公开(公告)日：2006-08-10
申请号：US10496259
申请日：2002-12-23
申请人： Christine Allen , Murray Webb , Paul Tardi , Yumin Yuan
发明人： Christine Allen , Murray Webb , Paul Tardi , Yumin Yuan
IPC分类号： A61K9/127
CPC分类号： A61K31/7072 , A61K9/0019 , A61K9/127 , A61K9/1271 , A61K9/1272 , A61K9/5138 , A61K9/5146 , A61K31/00 , A61K31/337 , A61K31/4745 , A61K31/704 , A61K31/7048 , A61K31/7076 , A61K33/24 , A61K2300/00
摘要： Delivery vehicles comprising nanoparticles which are composed of: (a) a biodegradable hydrophobic polymer forming a core, and; (b) an outer amphiphilic layer surrounding the polymer core containing a stabilizing lipid are suitable for delivering active agents.

6. 发明申请

US20070134332A1 Polymer particles for delivery of macromolecules and methods of use 审中-公开
标题翻译：用于递送大分子的聚合物颗粒和使用方法
公开(公告)号：US20070134332A1
公开(公告)日：2007-06-14
申请号：US11603660
申请日：2006-11-21
申请人： William Turnell , Geoffrey Landis , Zaza Gomurashvili , Hong Li , Kristin DeFife , Vassil Vassilev , Yumin Yuan
发明人： William Turnell , Geoffrey Landis , Zaza Gomurashvili , Hong Li , Kristin DeFife , Vassil Vassilev , Yumin Yuan
IPC分类号： A61K48/00 , A61K38/28 , C08F20/00 , A61K9/14
CPC分类号： A61K9/167 , A61K9/1075 , A61K9/5146 , A61K38/28 , A61K47/59 , A61K47/593 , A61K47/595 , C08L77/12
摘要： The present invention provides biodegradable polymer particle delivery compositions for delivery of macromolecular biologics, for example in crystal form, based on polymers, such as polyester amide (PEA), polyester urethane (PEUR), and polyester urea (PEU) polymers, which contain amino acids in the polymer. The polymer particle delivery compositions can be formulated either as a liquid dispersion or a lyophilized powder of polymer particles containing bound water molecules with the macromolecular biologics, for example insulin, dispersed in the particles. Bioactive agents, such as drugs, polypeptides, and polynucleotides can also be delivered by using particles sized for local, oral, mucosal or circulatory delivery. Methods of delivering a macromolecular biologic with substantial native activity to a subject, for example orally, are also included.
摘要翻译：本发明提供了生物可降解的聚合物颗粒递送组合物，其用于输送大分子生物制剂，例如以晶体形式，基于聚合物，例如含有氨基的聚酯酰胺（PEA），聚酯聚氨酯（PEUR）和聚酯尿素（PEU）聚合物聚合物中的酸。聚合物颗粒递送组合物可以配制成分散在颗粒中的液体分散体或含有结合水分子的聚合物颗粒与大分子生物制剂例如胰岛素的冻干粉末。生物活性剂，例如药物，多肽和多核苷酸也可以通过使用尺寸适于局部，口服，粘膜或循环递送的颗粒递送。还可以包括向受试者例如口服递送具有大量天然活性的大分子生物学方法。

7. 发明申请

US20070077272A1 Solid polymer delivery compositions and methods for use thereof 有权
标题翻译：固体聚合物输送组合物及其使用方法
公开(公告)号：US20070077272A1
公开(公告)日：2007-04-05
申请号：US11525491
申请日：2006-09-21
申请人： Hong Li , William Turnell , Yumin Yuan , Geoffrey Landis , Ryan Knoy
发明人： Hong Li , William Turnell , Yumin Yuan , Geoffrey Landis , Ryan Knoy
IPC分类号： A61K48/00 , A61K39/395 , C08F20/00 , A61F2/02
CPC分类号： C08G69/44 , A61K9/0024 , A61K47/34 , A61L27/34 , A61L31/10 , C08L77/12 , C08L2666/02
摘要： The present invention provides an implantable solid polymer delivery composition that can be formulated to release a bioactive agent to an interior body site at a controlled rate over an extended period of time by adjusting the various components of the composition. The controlled delivery of the composition avoids an initial drug spike, resulting in a smooth delivery profile over time. Polymer layers in the composition can be porous and are both biodegradable in water and body enzymes and biocompatible. Methods of making the implantable solid polymer compositions and methods of delivering a bioactive agent at a controlled rate to an interior body site are also provided.
摘要翻译：本发明提供了一种可植入的固体聚合物递送组合物，其可通过调节组合物的各种成分而配制成在长时间内以受控的速率将生物活性剂释放到内部身体部位。组合物的受控输送避免了初始药物尖峰，导致随着时间的顺利递送。组合物中的聚合物层可以是多孔的，并且在水和身体酶中都是可生物降解的并且是生物相容的。还提供了制造可植入固体聚合物组合物的方法和将受控速率递送至内部身体部位的生物活性剂的方法。

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