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公开(公告)号:US20130196948A1
公开(公告)日:2013-08-01
申请号:US13806240
申请日:2011-06-23
CPC分类号: C08B37/0021 , A61K9/06 , A61K9/1635 , A61K9/1641 , A61K9/1652 , A61K31/721 , A61K31/724 , C08B37/0012 , C08L5/00 , C08L5/02 , C08L5/16
摘要: Described herein are inventive compositions and methods relating to polymer conjugates and, in particular, to polymer conjugates having pendant side groups comprising ring moieties. In one aspect, embodiments are generally related to compositions that mimic naturally-occurring polyphenol compounds. The compositions comprise, in some embodiments, a polymer backbone having a plurality of hydroxyaromatic pendant side groups or derivatives thereof. For example, in some cases, a pendant side group may be a phenol or a substituted derivative thereof. In some cases, the pendant side group may be an oxidized hydroxyaromatic group, such as a quinone. In some embodiments, self-assembled structures comprising one or more of the polymer conjugates are provided. For example, the polymer conjugates may be combined with a complexing agent to form a particle. In some cases, a polymer conjugate may form a hydrogel. In some embodiments, the self-assembled structures may contain an agent, such as a pharmaceutically active agent. Also provided are methods and kits for forming the compositions, methods of using the compositions, and the like.
摘要翻译: 本文描述了与聚合物缀合物有关的本发明组合物和方法,特别是具有包含环部分的侧基的聚合物缀合物。 在一个方面,实施方案通常涉及模拟天然存在的多酚化合物的组合物。 在一些实施方案中,组合物包含具有多个羟基芳族侧基侧基或其衍生物的聚合物主链。 例如,在一些情况下,侧基可以是苯酚或其取代的衍生物。 在一些情况下,侧基可以是氧化的羟基芳族基团,例如醌。 在一些实施方案中,提供包含一种或多种聚合物共轭物的自组装结构。 例如,聚合物共轭物可以与络合剂组合以形成颗粒。 在一些情况下,聚合物缀合物可以形成水凝胶。 在一些实施方案中,自组装结构可以含有试剂,例如药物活性剂。 还提供了用于形成组合物的方法和试剂盒,使用组合物的方法等。
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公开(公告)号:US08450298B2
公开(公告)日:2013-05-28
申请号:US12716732
申请日:2010-03-03
申请人: Kerry Peter Mahon , Kevin Thomas Love , Christopher G. Levins , Kathryn Ann Whitehead , Robert S. Langer , Daniel Griffith Anderson
发明人: Kerry Peter Mahon , Kevin Thomas Love , Christopher G. Levins , Kathryn Ann Whitehead , Robert S. Langer , Daniel Griffith Anderson
IPC分类号: A61K38/00
CPC分类号: C07D295/13 , A61K9/107 , A61K9/1271 , A61K9/5123 , A61K31/7088 , A61K38/02 , A61K47/16 , A61K47/54 , A61K47/545 , A61K48/0025 , B01J2531/0252 , B01J2531/845 , C07C215/14 , C07C217/08 , C12N15/111 , C12N15/1137 , C12N15/88 , C12N2310/14 , C12N2310/3515 , C12N2320/32
摘要: Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. 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:US08969353B2
公开(公告)日:2015-03-03
申请号:US13128020
申请日:2009-11-06
申请人: Kerry Peter Mahon , Kevin Thomas Love , Christopher G. Levins , Kathryn Ann Whitehead , Robert S. Langer , Daniel Griffith Anderson
发明人: Kerry Peter Mahon , Kevin Thomas Love , Christopher G. Levins , Kathryn Ann Whitehead , Robert S. Langer , Daniel Griffith Anderson
IPC分类号: A61K31/495 , C07D241/04 , A61K9/127 , A61K47/16 , C07C215/14 , C12N15/11 , C07C217/08 , A61K9/51 , C12N15/88 , C07D295/13 , A61K48/00
CPC分类号: C07D295/13 , A61K9/107 , A61K9/1271 , A61K9/5123 , A61K31/7088 , A61K38/02 , A61K47/16 , A61K47/54 , A61K47/545 , A61K48/0025 , B01J2531/0252 , B01J2531/845 , C07C215/14 , C07C217/08 , C12N15/111 , C12N15/1137 , C12N15/88 , C12N2310/14 , C12N2310/3515 , C12N2320/32
摘要: Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
摘要翻译: 氨基醇类固醇通过使胺与环氧化物封端的化合物反应来制备。 还提供了从市售的原料制备氨基醇类固醇的方法。 氨基醇类固醇可以由外消旋或立体化学纯环氧化物制备。 氨基醇类固醇或其盐形式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。 鉴于这些氨基醇类脂质化合物的氨基部分,它们特别适用于递送多核苷酸。 已经制备了含有本发明的类脂和多核苷酸的复合物,胶束,脂质体或颗粒。 本发明的类脂质也可用于制备用于药物递送的微粒。 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:US20120251560A1
公开(公告)日:2012-10-04
申请号:US13428695
申请日:2012-03-23
申请人: James E. Dahlman , Avraham D. Schroeder , Daniel Griffith Anderson , Robert S. Langer , Christopher G. Levins
发明人: James E. Dahlman , Avraham D. Schroeder , Daniel Griffith Anderson , Robert S. Langer , Christopher G. Levins
IPC分类号: A61K31/133 , C07D257/02 , C07D267/00 , A61K8/41 , A61K38/02 , A61K39/00 , A61P37/04 , A61P35/00 , C07C215/14 , A61K31/7088
CPC分类号: A61K47/22 , A61K9/0019 , A61K9/1272 , A61K47/34 , A61K47/543 , A61K47/59 , A61K47/6907 , A61K47/6911 , A61K47/6921 , C07D257/02 , C07D273/00 , C07D273/08 , C07D295/084 , C08G73/10 , C12N15/1137 , C12N15/1138 , C12N2310/14 , C12N2320/32
摘要: The present invention provides inventive conjugated polyethyleneimine (PEI) polymers and conjugated aza-macrocycles (collectively referred to herein as “conjugated lipomers” or “lipomers”) containing one or more groups of the formula (iii): wherein R3 and R4 are as defined herein. Also provided are compositions comprising the inventive conjugated lipomers, and methods of preparation and use.
摘要翻译: 本发明提供含有一个或多个式(ⅲ)的基团的本发明的共轭聚乙烯亚胺(PEI)聚合物和共轭氮杂 - 大环化合物(统称为共轭脂族或脂肪族),其中R 3和R 4如本文所定义。 还提供了包含本发明的共轭脂族物的组合物,以及制备和使用方法。
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公开(公告)号:US20110293703A1
公开(公告)日:2011-12-01
申请号:US13128020
申请日:2009-11-06
申请人: Kerry Peter Mahon , Kevin Thomas Love , Christopher G. Levins , Kathryn Ann Whitehead , Robert S. Langer , Daniel Griffith Anderson
发明人: Kerry Peter Mahon , Kevin Thomas Love , Christopher G. Levins , Kathryn Ann Whitehead , Robert S. Langer , Daniel Griffith Anderson
IPC分类号: A61K9/127 , C07C217/42 , C07C215/18 , C07H21/00 , A61K47/18 , A61K38/02 , A61K31/7088 , A61K31/7105 , C07D295/13 , C07C215/42
CPC分类号: C07D295/13 , A61K9/107 , A61K9/1271 , A61K9/5123 , A61K31/7088 , A61K38/02 , A61K47/16 , A61K47/54 , A61K47/545 , A61K48/0025 , B01J2531/0252 , B01J2531/845 , C07C215/14 , C07C217/08 , C12N15/111 , C12N15/1137 , C12N15/88 , C12N2310/14 , C12N2310/3515 , C12N2320/32
摘要: Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
摘要翻译: 氨基醇类固醇通过使胺与环氧化物封端的化合物反应来制备。 还提供了从市售的原料制备氨基醇类固醇的方法。 氨基醇类固醇可以由外消旋或立体化学纯环氧化物制备。 氨基醇类固醇或其盐形式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。 鉴于这些氨基醇类脂质化合物的氨基部分,它们特别适用于递送多核苷酸。 已经制备了含有本发明的类脂和多核苷酸的复合物,胶束,脂质体或颗粒。 本发明的类脂质也可用于制备用于药物递送的微粒。 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:US09238716B2
公开(公告)日:2016-01-19
申请号:US13428695
申请日:2012-03-23
申请人: James E. Dahlman , Avraham D. Schroeder , Daniel Griffith Anderson , Robert S. Langer , Christopher G. Levins
发明人: James E. Dahlman , Avraham D. Schroeder , Daniel Griffith Anderson , Robert S. Langer , Christopher G. Levins
IPC分类号: C08G73/10 , C07D257/02 , C07D273/08 , A61K9/00 , A61K47/34 , A61K47/48
CPC分类号: A61K47/22 , A61K9/0019 , A61K9/1272 , A61K47/34 , A61K47/543 , A61K47/59 , A61K47/6907 , A61K47/6911 , A61K47/6921 , C07D257/02 , C07D273/00 , C07D273/08 , C07D295/084 , C08G73/10 , C12N15/1137 , C12N15/1138 , C12N2310/14 , C12N2320/32
摘要: The present invention provides inventive conjugated polyethyleneimine (PEI) polymers and conjugated aza-macrocycles (collectively referred to herein as “conjugated lipomers” or “lipomers”) containing one or more groups of the formula (iii): wherein R3 and R4 are as defined herein. Also provided are compositions comprising the inventive conjugated lipomers, and methods of preparation and use.
摘要翻译: 本发明提供含有一个或多个式(ⅲ)基团的本发明共轭聚乙烯亚胺(PEI)聚合物和共轭氮杂 - 大环化合物(统称为“共轭脂族”或“脂聚合物”):其中R3和R4定义如上 这里。 还提供了包含本发明的共轭脂族物的组合物,以及制备和使用方法。
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公开(公告)号:USRE43612E1
公开(公告)日:2012-08-28
申请号:US12568481
申请日:2009-09-28
IPC分类号: A61K31/765 , C08G69/44 , C08G63/44 , C07C327/00
CPC分类号: C12N15/88 , A61K9/1641 , A61K9/5146 , A61K47/59 , A61K47/593 , A61K47/6935 , B82Y5/00 , C08G73/02 , C08G73/06 , C08G73/0611 , C08G73/0616 , C08G73/0627
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(&(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。 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:US08986988B2
公开(公告)日:2015-03-24
申请号:US12680249
申请日:2008-09-29
申请人: Rohit Nandkumar Karnik , Seungpyo Hong , Ying Mei , Daniel Griffith Anderson , Jeffrey Michael Karp , Robert S. Langer , Suman Bose
发明人: Rohit Nandkumar Karnik , Seungpyo Hong , Ying Mei , Daniel Griffith Anderson , Jeffrey Michael Karp , Robert S. Langer , Suman Bose
IPC分类号: C12N5/07 , C12N5/00 , C12N5/0735 , C12N5/078 , C12M1/00
CPC分类号: C12N5/0068 , B01L3/502715 , B01L3/502761 , B01L2200/0647 , B01L2300/0877 , B01L2300/16 , C12M23/16 , C12M47/02 , C12N5/0062 , C12N2501/58 , C12N2501/585 , C12N2533/50 , C12N2533/52 , C12N2535/10
摘要: The present invention provides systems for cell separation based on cell rolling on surfaces along edges of regions coated with cell adhesion molecules. A variety of designs of coated regions and edges are disclosed.
摘要翻译: 本发明提供了基于在细胞粘附分子包被的区域的边缘上的表面上的细胞滚动的细胞分离系统。 公开了涂覆区域和边缘的各种设计。
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公开(公告)号:US09193827B2
公开(公告)日:2015-11-24
申请号:US13819280
申请日:2011-08-26
CPC分类号: C08G73/0206 , A61K9/1273 , A61K31/7088 , A61K47/34 , A61K47/59 , A61L31/10 , C08G59/22 , C08G59/306 , C08G59/50 , C08G73/02 , C09D5/1637 , C09D179/02 , Y10T428/31725
摘要: A new class of poly(beta-amino alcohols) (PBAAs) has been prepared using combinatorial polymerization. The inventive PBAAs may be used in biotechnology and biomedical applications as coatings (such as coatings of films or multilayer films for medical devices or implants), additives, materials, excipients, non-biofouling agents, micropatterning agents, and cellular encapsulation agents. When used as surface coatings, these PBAAs elicited different levels of inflammation, both in vitro and in vivo, depending on their chemical structures. The large chemical diversity of this class of materials allowed us to identify polymer coatings that inhibit macrophage activation in vitro. Furthermore, these coatings reduce the recruitment of inflammatory cells, and reduce fibrosis, following the subcutaneous implantation of carboxylated polystyrene microparticles. These polymers may be used to form polyelectrolyte complex capsules for cell encapsulation. The invention may also have many other biological applications such as antimicrobial coatings, DNA or siRNA delivery, and stem cell tissue engineering.
摘要翻译: 使用组合聚合制备了一类新的聚(β-氨基醇)(PBAAs)。 本发明的PBAAs可用于生物技术和生物医学应用中,作为涂层(例如用于医疗装置或植入物的膜或多层膜的涂层),添加剂,材料,赋形剂,非生物污垢剂,微图案化剂和细胞包封剂。 当用作表面涂层时,这些PBAAs根据其化学结构在体外和体内引起不同程度的炎症。 这类材料的大化学多样性使我们能够鉴定体外抑制巨噬细胞活化的聚合物涂层。 此外,在皮下植入羧化聚苯乙烯微粒之后,这些涂层减少了炎性细胞的募集,并减少了纤维化。 这些聚合物可用于形成用于细胞包封的聚电解质复合物胶囊。 本发明还可以具有许多其他生物学应用,例如抗微生物涂层,DNA或siRNA递送以及干细胞组织工程。
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公开(公告)号:US08562966B2
公开(公告)日:2013-10-22
申请号:US13312224
申请日:2011-12-06
CPC分类号: C12N15/87 , A61K9/5138 , A61K47/34 , C08G63/6856 , C08G73/02 , C08L79/02
摘要: Poly(beta-amino esters) are end-modified to form materials useful in the medical as well as non-medical field. An amine-terminated poly(beta-amino ester) is reacted with an electrophile, or an acrylate-terminated poly(beta-amino ester) is reacted with a nucleophile. The inventive end-modified polymers may be used in any field where polymers have been found useful including the drug delivery arts. The end-modified polymers are particularly useful in delivery nucleic acids such as DNA or RNA. The invention also provides compositions including the inventive end-modified polymers, methods of preparing the inventive polymers, and method of using the inventive polymers.
摘要翻译: 聚(β-氨基酯)被末端修饰以形成用于医疗和非医学领域的材料。 使胺封端的聚(β-氨基酯)与亲电子试剂或丙烯酸酯封端的聚(β-氨基酯)与亲核试剂反应。 本发明的末端改性聚合物可用于已经发现聚合物有用的任何领域,包括药物递送领域。 末端修饰的聚合物特别可用于递送核酸如DNA或RNA。 本发明还提供包含本发明的端基改性聚合物,制备本发明聚合物的方法和使用本发明聚合物的方法的组合物。
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