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公开(公告)号：US20120065358A1
公开(公告)日：2012-03-15
申请号：US13301315
申请日：2011-11-21
IPC分类号： C08G63/685
CPC分类号： A61K47/34 , A61K9/5146 , A61K31/711 , A61K31/713 , A61K47/59 , A61K47/593 , A61K47/6929 , B82Y5/00 , C08G63/685 , C08G73/02 , C08G73/0273 , C08G73/06 , C08G73/0611 , C08G73/0616 , C12N15/88
摘要： Poly(β-amino esters) prepared from the conjugate addition of bis(secondary amines) or primary amines to a bis(acrylate ester) are described. Methods of preparing these polymers from commercially available starting materials are also provided. These tertiary amine-containing polymers are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the poly(amine) nature of these polymers, they are particularly suited for the delivery of polynucleotides. Nanoparticles containing polymer/polynucleotide complexes have been prepared. The inventive polymers may also be used to encapsulate other agents to be delivered. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
摘要翻译： 描述了从双（仲胺）或伯胺向双（丙烯酸酯）共轭加成制备的聚（＆（bgr。 - 氨基酯））。 还提供了从市售的原料制备这些聚合物的方法。 这些含叔胺的聚合物优选是可生物降解的和生物相容的并且可以用于各种药物递送系统中。 鉴于这些聚合物的聚（胺）性质，它们特别适用于递送多核苷酸。 已经制备了含有聚合物/多核苷酸复合物的纳米颗粒。 本发明的聚合物也可以用于包封待递送的其它试剂。 考虑到缓冲其周围环境的pH值，它们特别适用于提供不稳定剂。
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公开(公告)号：US06998115B2
公开(公告)日：2006-02-14
申请号：US09969431
申请日：2001-10-02
IPC分类号： A61K31/765 , C08G69/44 , C08G63/44 , C07C327/00
CPC分类号： A61K47/34 , A61K9/5146 , A61K31/711 , A61K31/713 , A61K47/59 , A61K47/593 , A61K47/6929 , B82Y5/00 , C08G63/685 , C08G73/02 , C08G73/0273 , C08G73/06 , C08G73/0611 , C08G73/0616 , C12N15/88
摘要： Poly(β-amino esters) prepared from the conjugate addition of bis(secondary amines) or primary amines to a bis(acrylate ester) are described. Methods of preparing these polymers from commercially available starting materials are also provided. These tertiary amine-containing polymers are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the poly(amine) nature of these polymers, they are particularly suited for the delivery of polynucleotides. Nanoparticles containing polymer/polynucleotide complexes have been prepared. The inventive polymers may also be used to encapsulate other agents to be delivered. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
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公开(公告)号：US08557231B2
公开(公告)日：2013-10-15
申请号：US11099886
申请日：2005-04-06
IPC分类号： A61K31/785 , A61K31/765 , C08G69/08
CPC分类号： A61K47/34 , A61K9/5146 , A61K31/711 , A61K31/713 , A61K47/59 , A61K47/593 , A61K47/6929 , B82Y5/00 , C08G63/685 , C08G73/02 , C08G73/0273 , C08G73/06 , C08G73/0611 , C08G73/0616 , C12N15/88
摘要： Poly(β-amino esters) prepared from the conjugate addition of bis(secondary amines) or primary amines to a bis(acrylate ester) are described. Methods of preparing these polymers from commercially available starting materials are also provided. These tertiary amine-containing polymers are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the poly(amine) nature of these polymers, they are particularly suited for the delivery of polynucleotides. Nanoparticles containing polymer/polynucleotide complexes have been prepared. The inventive polymers may also be used to encapsulate other agents to be delivered. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
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公开(公告)号：US08287849B2
公开(公告)日：2012-10-16
申请号：US12507999
申请日：2009-07-23
IPC分类号： A61K31/765 , A61K9/00 , C08F26/00
CPC分类号： A61K47/34 , A61K9/5146 , A61K31/711 , A61K31/713 , A61K47/59 , A61K47/593 , A61K47/6929 , B82Y5/00 , C08G63/685 , C08G73/02 , C08G73/0273 , C08G73/06 , C08G73/0611 , C08G73/0616 , C12N15/88
摘要： Poly(β-amino esters) prepared from the conjugate addition of bis(secondary amines) or primary amines to a bis(acrylate ester) are described. Methods of preparing these polymers from commercially available starting materials are also provided. These tertiary amine-containing polymers are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the poly(amine) nature of these polymers, they are particularly suited for the delivery of polynucleotides. Nanoparticles containing polymer/polynucleotide complexes have been prepared. The inventive polymers may also be used to encapsulate other agents to be delivered. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
摘要翻译： 描述了从双（仲胺）或伯胺向双（丙烯酸酯）共轭加成制备的聚（＆（bgr。 - 氨基酯））。 还提供了从市售的原料制备这些聚合物的方法。 这些含叔胺的聚合物优选是可生物降解的和生物相容的并且可以用于各种药物递送系统中。 鉴于这些聚合物的聚（胺）性质，它们特别适用于递送多核苷酸。 已经制备了含有聚合物/多核苷酸复合物的纳米颗粒。 本发明的聚合物也可以用于包封待递送的其它试剂。 考虑到缓冲其周围环境的pH值，它们特别适用于提供不稳定剂。
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公开(公告)号：US20100036084A1
公开(公告)日：2010-02-11
申请号：US12507999
申请日：2009-07-23
IPC分类号： C08G63/685
CPC分类号： A61K47/34 , A61K9/5146 , A61K31/711 , A61K31/713 , A61K47/59 , A61K47/593 , A61K47/6929 , B82Y5/00 , C08G63/685 , C08G73/02 , C08G73/0273 , C08G73/06 , C08G73/0611 , C08G73/0616 , C12N15/88
摘要： Poly(β-amino esters) prepared from the conjugate addition of bis(secondary amines) or primary amines to a bis(acrylate ester) are described. Methods of preparing these polymers from commercially available starting materials are also provided. These tertiary amine-containing polymers are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the poly(amine) nature of these polymers, they are particularly suited for the delivery of polynucleotides. Nanoparticles containing polymer/polynucleotide complexes have been prepared. The inventive polymers may also be used to encapsulate other agents to be delivered. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
摘要翻译： 描述了从双（仲胺）或伯胺向双（丙烯酸酯）共轭加成制备的聚（β-氨基酯）。 还提供了从市售的原料制备这些聚合物的方法。 这些含叔胺的聚合物优选是可生物降解的和生物相容的并且可以用于各种药物递送系统中。 鉴于这些聚合物的聚（胺）性质，它们特别适用于递送多核苷酸。 已经制备了含有聚合物/多核苷酸复合物的纳米颗粒。 本发明的聚合物也可以用于包封待递送的其它试剂。 考虑到缓冲其周围环境的pH值，它们特别适用于提供不稳定剂。
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公开(公告)号：US20100234244A1
公开(公告)日：2010-09-16
申请号：US12788140
申请日：2010-05-26
CPC分类号： B01J19/0046
摘要： A microarray of polymeric biomaterials is provided. Specifically, a microarray of polymeric biomaterials that comprises a base with a cytophobic surface, and a plurality of discrete polymeric biomaterial elements bound to the cytophobic surface, is provided. Preferably said polymeric biomaterials comprise a synthetic polymer. Said polymeric biomaterials may also comprise other compounds covalently or non-covalently attached to said synthetic polymer. Methods of preparing the microarray of polymeric biomaterials of the present invention and uses of the microarray of polymeric biomaterials of the present invention are also provided.
摘要翻译： 提供了聚合物生物材料的微阵列。 具体地，提供了包含具有细胞疏松表面的基底的聚合物生物材料的微阵列和与细胞积极表面结合的多个离散的聚合物生物材料。 优选地，所述聚合物生物材料包含合成聚合物。 所述聚合物生物材料还可以包含与所述合成聚合物共价或非共价连接的其它化合物。 还提供了制备本发明的聚合物生物材料的微阵列的方法和本发明的聚合物生物材料的微阵列的用途。
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公开(公告)号：US20080182240A1
公开(公告)日：2008-07-31
申请号：US11676729
申请日：2007-02-20
CPC分类号： B01J19/0046
摘要： A microarray of polymeric biomaterials is provided. Specifically, a microarray of polymeric biomaterials that comprises a base with a cytophobic surface, and a plurality of discrete polymeric biomaterial elements bound to the cytophobic surface, is provided. Preferably said polymeric biomaterials comprise a synthetic polymer. Said polymeric biomaterials may also comprise other compounds covalently or non-covalently attached to said synthetic polymer. Methods of preparing the microarray of polymeric biomaterials of the present invention and uses of the microarray of polymeric biomaterials of the present invention are also provided.
摘要翻译： 提供了聚合物生物材料的微阵列。 具体地，提供了包含具有细胞疏松表面的基底的聚合物生物材料的微阵列和与细胞积极表面结合的多个离散的聚合物生物材料。 优选地，所述聚合物生物材料包含合成聚合物。 所述聚合物生物材料还可以包含与所述合成聚合物共价或非共价连接的其它化合物。 还提供了制备本发明的聚合物生物材料的微阵列的方法和本发明的聚合物生物材料的微阵列的用途。
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公开(公告)号：US07943179B2
公开(公告)日：2011-05-17
申请号：US11002542
申请日：2004-12-02
IPC分类号： A61K9/16
CPC分类号： A61K9/1617 , A61K9/1623 , A61K9/1647 , A61K9/1658
摘要： A drug delivery system comprising pH triggerable particles is described. The pH triggerable particles comprise and agent(s) to be delivered, which is encapsulated in a matrix comprising a pH trigger agent and a polymer. Agents including nucleic acids may be delivered intracellularly using the inventive pH triggerable particles. Upon exposure to an acidic environment such as the endosome or phagosome of a cell, the particles dissolve or disrupt due to protonation or an increase in solubility of the pH triggering agent. Pharmaceutical compositions and methods of preparing and administering these particles are also described. These particles may be particularly useful in genetic vaccination.
摘要翻译： 描述了包含pH可触发颗粒的药物递送系统。 pH可触发颗粒包含待运送的试剂，其被包封在包含pH触发剂和聚合物的基质中。 包含核酸的试剂可以使用本发明的pH可触发颗粒在细胞内递送。 当暴露于诸如细胞的内体或吞噬体的酸性环境中时，由于质子化或pH引发剂的溶解度的增加，颗粒溶解或破坏。 还描述了制备和施用这些颗粒的药物组合物和方法。 这些颗粒在基因疫苗接种中可能特别有用。
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公开(公告)号：US07427394B2
公开(公告)日：2008-09-23
申请号：US10446444
申请日：2003-05-28
IPC分类号： A61K31/765 , C08G69/44 , C08G63/44 , C07C327/00
CPC分类号： C08G69/44 , A61K9/5138 , A61K47/59 , A61K47/593 , A61K47/645 , A61K47/6925 , B82Y5/00 , C08G63/40 , C08G63/6856 , C08G73/02 , C08G73/0273 , C08G73/028 , C08G73/06 , C08G73/0611 , C08G73/0616 , C08L67/02 , C08L67/04 , C08L77/04 , C08L79/02 , C08L89/00 , C08L99/00 , C12N15/88 , C08L2666/02
摘要： Poly(β-amino esters) prepared from the conjugate addition of bis(secondary amines) or primary amines to a bis(acrylate ester) are described. Methods of preparing these polymers from commercially available starting materials are also provided. These tertiary amine-containing polymers are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the poly(amine) nature of these polymers, they are particularly suited for the delivery of polynucleotides. Nanoparticles containing polymer/polynucleotide complexes have been prepared. The inventive polymers may also be used to encapsulate other agents to be delivered. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings. A system for preparing and screening polymers in parallel using semi-automated robotic fluid delivery systems is also provided.
摘要翻译： 描述了从双（仲胺）或伯胺向双（丙烯酸酯）共轭加成制备的聚（β-氨基酯）。 还提供了从市售的原料制备这些聚合物的方法。 这些含叔胺的聚合物优选是可生物降解的和生物相容的并且可以用于各种药物递送系统中。 鉴于这些聚合物的聚（胺）性质，它们特别适用于递送多核苷酸。 已经制备了含有聚合物/多核苷酸复合物的纳米颗粒。 本发明的聚合物也可以用于包封待递送的其它试剂。 考虑到缓冲其周围环境的pH值，它们特别适用于提供不稳定剂。 还提供了使用半自动机器人流体输送系统并行制备和筛选聚合物的系统。
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公开(公告)号：US06849272B1
公开(公告)日：2005-02-01
申请号：US09553552
申请日：2000-04-20
申请人： Robert S. Langer , David A. Putnam
发明人： Robert S. Langer , David A. Putnam
IPC分类号： A61K47/48 , C08F220/58 , C12N15/87 , A61K9/14
CPC分类号： C12N15/87 , A61K47/58 , A61K47/6931 , B82Y5/00 , C08F220/58
摘要： The present invention provides improved cell delivery compositions. In particular, the invention provides biocompatible endosomolytic agents. In a preferred embodiment, the endosomolytic agents are also biodegradable and can be broken down within cells into components that the cells can either reuse of dispose of. In one aspect, the present invention provides endosomolytic agents capable of effecting the lysis of an endosome in response to a change in pH, and methods for effecting the lysis of an endosome. These inventive endosomolytic agents obviate the need for known agents (i.e., chloroquine, fusogenic peptides, inactivated adenoviruses and polyethyleneimine) that can burst endosomes and have negative effects on cells. In another aspect, the present invention provides cell delivery compositions comprising an endosomolytic component that is capable of effecting the lysis of the endosome in response to a change in pH, and an encapsulating, or packaging, component capable of packaging a therapeutic agent to be delivered to cellular or subcellular components.
摘要翻译： 本发明提供了改进的细胞递送组合物。 特别地，本发明提供生物相容的内体细胞溶解剂。 在优选的实施方案中，内体细胞溶解剂也是可生物降解的，并且可以在细胞内分解成细胞可以重复使用的组分。 在一个方面，本发明提供了能够响应于pH变化而影响内体的裂解的内体分解剂，以及用于实现内体的裂解的方法。 这些本发明的内分泌溶解剂消除了可能破坏内体并对细胞具有负面影响的已知试剂（即氯喹，融合肽，失活的腺病毒和聚乙烯亚胺）的需要。 另一方面，本发明提供了细胞递送组合物，其包含能够响应于pH变化而影响内体的裂解的内体细胞分解成分，以及能够包装待递送的治疗剂的包封或包装成分 到细胞或亚细胞组分。
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