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1. 发明申请

US20060239961A1 Hydrolytically degradable alkylene oxide based polymers 审中-公开
标题翻译：水解可降解的烯化氧基聚合物
公开(公告)号：US20060239961A1
公开(公告)日：2006-10-26
申请号：US10371996
申请日：2003-02-14
申请人： Michael Bentley , J. Harris , Xuan Zhao , William Battle , Siaoming Shen
发明人： Michael Bentley , J. Harris , Xuan Zhao , William Battle , Siaoming Shen
IPC分类号： A61K31/785 , C08G8/28
CPC分类号： C08G65/04 , A61K9/00 , A61K9/06 , A61K47/34 , C08G64/183 , C08G65/329 , C08G65/333 , C08G65/33337 , C08G65/33344 , C08G65/33396 , C08L2203/02
摘要： The present invention provides a water soluble, nonpeptidic polymer comprising two or more alkylene oxide-based oligomers linked together by hydrolytically degradable linkages such as carbonates. Typically, the oligomer portion of the polymer is an amphiphilic triblock copolymer having a central propylene oxide block or butylene oxide block positioned between two ethylene oxide blocks. The polymer can be hydrolytically degraded into oligomers under physiological conditions. In aqueous media, the polymer preferably forms thermally reversible, hydrolytically degradable hydrogels that can be used, for example, for drug delivery and related biomedical applications.
摘要翻译：本发明提供了一种水溶性非肽性聚合物，其包含通过可降解水解的键如碳酸酯连接在一起的两个或多个环氧烷基低聚物。通常，聚合物的低聚物部分是具有位于两个环氧乙烷嵌段之间的中心环氧丙烷嵌段或环氧丁烷嵌段的两亲性三嵌段共聚物。聚合物可以在生理条件下水解降解成低聚物。在水性介质中，聚合物优选形成热可逆的水解可降解的水凝胶，其可用于例如药物递送和相关的生物医学应用。

2. 发明申请

US20060178475A1 Branched polymers and their conjugates 有权
标题翻译：支链聚合物及其共轭物
公开(公告)号：US20060178475A1
公开(公告)日：2006-08-10
申请号：US11336695
申请日：2006-01-20
申请人： Michael Bentley , Xuan Zhao , Xiaoming Shen , William Battle
发明人： Michael Bentley , Xuan Zhao , Xiaoming Shen , William Battle
IPC分类号： C08G63/91 , C08G63/48 , C07C319/02 , C07C215/02
CPC分类号： C08G65/48 , A61K47/60 , A61K47/6901 , C07K17/08 , C08G65/329 , C08G65/3322 , C08L2203/02 , C12N9/96
摘要： The present invention is directed to branched reactive water-soluble polymers comprising at least two polymer arms, such as poly(ethylene glycol), attached to a central aliphatic hydrocarbon core molecule through heteroatom linkages. The branched polymers bear at least one functional group for reacting with a biologically active agent to form a biologically active conjugate. The functional group of the branched polymer can be directly attached to the aliphatic hydrocarbon core or via an intervening linkage, such as a heteroatom, -alkylene-, —O-alkylene-O—, -alkylene-O-alkylene-, -aryl-O—, —O— aryl-, (—O-alkylene-)m, or (-alkylene-O—)m linkage, wherein m is 1-10.
摘要翻译：本发明涉及包含通过杂原子键连接到中心脂族烃核心分子的至少两个聚合物臂（例如聚（乙二醇））的支链反应性水溶性聚合物。支链聚合物具有至少一个用于与生物活性剂反应以形成生物活性缀合物的官能团。支链聚合物的官能团可以直接连接到脂族烃核心上或通过插入键如杂原子， - 亚烷基 - ， - - 亚烷基-O-， - 亚烷基-O-亚烷基 - ， - 芳基 - O-，-O-芳基 - ，（ - - 亚烷基 - ） - 亚烷基或（ - 亚烷基-O - ） - ，其中m为1-10。

3. 发明申请

US20060160983A1 Hydrolytically degradable polymers and hydrogels made therefrom 有权
标题翻译：水解可降解的聚合物和水凝胶
公开(公告)号：US20060160983A1
公开(公告)日：2006-07-20
申请号：US11377973
申请日：2006-03-17
申请人： J. Harris , Michael Bentley , Xuan Zhao , Xiaoming Shen
发明人： J. Harris , Michael Bentley , Xuan Zhao , Xiaoming Shen
IPC分类号： C08G64/00
CPC分类号： C08G64/0208 , C08G64/0216 , C08G64/183
摘要： A water soluble polymer is provided having two or more oligomers linked to each other by hydrolytically degradable carbonate linkages. The polymer can be hydrolytically degraded into oligomers (e.g., oligomers of ethylene oxide) under physiological conditions. The polymer can be conjugated to biologically active agents such as proteins or peptides to impart improved water solubility, reduced immunogenicity, reduced rate of renal clearance, and increased stability. The polymer is useful in making hydrolytically degradable hydrogels which can be used in drug delivery and related biomedical applications. On example of the polymer is a poly (ether carbonate) of the formula X—O—[(—CH2CH2-0-)n—CO2—]n—(CH2CH2))n-y where X and Y are independently H, alkyl, alkenyl, aryl, or a reactive moiety, and at least one of X and Y is a reactive moiety.
摘要翻译：提供了具有两个或多个通过可水解降解的碳酸酯键相互连接的低聚物的水溶性聚合物。在生理条件下，聚合物可以水解降解成低聚物（例如环氧乙烷的低聚物）。聚合物可以与生物活性剂如蛋白质或肽缀合以赋予改善的水溶性，降低的免疫原性，降低的肾清除率和增加的稳定性。该聚合物可用于制备可用于药物递送和相关生物医学应用的水解可降解水凝胶。聚合物的实例是式XO的聚（醚碳酸酯） - [（ - CH 2 CH 2 -O - ） - N - -CO 2 - - - - - （CH 2 CH 2）） - （CH 2 CH 2） -y其中X和Y独立地是H，烷基，烯基，芳基或反应性部分，X和Y中的至少一个是反应性部分。

4. 发明申请

US20050226843A1 Polymer-based compositions and conjuates of HIV entry inhibitors 有权
标题翻译：基于聚合物的组合物和HIV入口抑制剂的结合
公开(公告)号：US20050226843A1
公开(公告)日：2005-10-13
申请号：US11082229
申请日：2005-03-15
申请人： Michael Bentley , Xuan Zhao
发明人： Michael Bentley , Xuan Zhao
IPC分类号： A61K38/17 , A61K47/00 , A61K47/48 , C08F8/00 , C08G63/48 , C08G63/91
CPC分类号： A61K47/48215 , A61K47/60
摘要： Provided herein are water-soluble polymer conjugates and polymer-based compositions of HIV entry inhibitors. Also provided are methods for synthesizing and administering such conjugates and compositions.
摘要翻译：本文提供了HIV入口抑制剂的水溶性聚合物缀合物和基于聚合物的组合物。还提供了用于合成和施用这种缀合物和组合物的方法。

5. 发明申请

US20050147583A1 Hydrolytically degradable carbamate derivatives of poly(ethylene glycol) 有权
标题翻译：聚乙二醇的水解降解氨基甲酸酯衍生物
公开(公告)号：US20050147583A1
公开(公告)日：2005-07-07
申请号：US11033547
申请日：2005-01-10
申请人： Michael Bentley , Xuan Zhao
发明人： Michael Bentley , Xuan Zhao
IPC分类号： A61K9/06 , A61K31/77 , A61K47/32 , A61K47/34 , A61K47/36 , A61K47/42 , A61K47/44 , A61K47/48 , A61P5/00 , A61P5/38 , A61P9/00 , A61P25/22 , A61P29/00 , A61P31/04 , A61P31/10 , A61P31/12 , A61P35/00 , A61P43/00 , C08G65/329 , C08L101/16 , A61K38/17 , A61K31/785
CPC分类号： C08G65/33344 , A61K31/765 , A61K47/60 , C08G18/711 , C08G65/329 , C08G65/331 , C08G65/333 , C08G2210/00 , Y10S435/82
摘要： Poly(ethylene glycol) carbamate derivatives useful as water-soluble prodrugs are disclosed. These degradable poly(ethylene glycol) carbamate derivatives also have potential applications in controlled hydrolytic degradation of hydrogels. In such degradable hydrogels, drugs may be trapped in the gel and released by diffusion as the gel degrades, or they may be covalently bound through hydrolyzable carbamate linkages. Hydrolysis of these carbamate linkages releases the drug at a controllable rate as the gel degrades.
摘要翻译：公开了可用作水溶性前药的聚（乙二醇）氨基甲酸酯衍生物。这些可降解的聚（乙二醇）氨基甲酸酯衍生物在水凝胶的可控水解降解中也具有潜在的应用。在这种可降解的水凝胶中，药物可以被捕获在凝胶中并随着凝胶降解而被扩散释放，或者它们可以通过可水解的氨基甲酸酯键共价结合。当凝胶降解时，这些氨基甲酸酯键的水解以可控的速率释放药物。

6. 发明申请

US20050136031A1 Chemically modified small molecules 有权
标题翻译：化学修饰的小分子
公开(公告)号：US20050136031A1
公开(公告)日：2005-06-23
申请号：US11015196
申请日：2004-12-16
申请人： Michael Bentley , Tacey Viegas , Richard Goodin , Lin Cheng , Xuan Zhao
发明人： Michael Bentley , Tacey Viegas , Richard Goodin , Lin Cheng , Xuan Zhao
IPC分类号： A61K31/765 , A61K31/785 , A61K47/48 , C08G65/08
CPC分类号： C08G65/337 , A61K47/60 , C08G65/332 , C08G65/33317 , C08G65/33396 , C08L2203/02
摘要： The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer obtained from a monodisperse or bimodal water-soluble oligomer composition. A conjugate of the invention, when administered by any of a number of administration routes, exhibits a reduced biological membrane crossing rate as compared to the biological membrane crossing rate of the small molecule drug not attached to the water-soluble oligomer.
摘要翻译：本发明提供了通过共价连接由单分散或双峰水溶性低聚物组合物获得的水溶性低聚物进行化学修饰的小分子药物。当与多种施用途径中的任何一种施用时，本发明的缀合物与未附着于水溶性低聚物的小分子药物的生物膜交联率相比，显示出降低的生物膜交叉率。

7. 发明申请

US20050112088A1 Multi-arm polymer prodrugs 有权
标题翻译：多臂聚合物前药
公开(公告)号：US20050112088A1
公开(公告)日：2005-05-26
申请号：US10943799
申请日：2004-09-17
申请人： Xuan Zhao , Michael Bentley , Zhongxu Ren , Tacey Viegas
发明人： Xuan Zhao , Michael Bentley , Zhongxu Ren , Tacey Viegas
IPC分类号： A61K31/765 , A61K31/785 , A61K47/48 , C08L71/02
CPC分类号： C08L71/02 , A61K47/58 , A61K47/59 , A61K47/595 , A61K47/60 , A61K47/61
摘要： Provided herein are water-soluble prodrugs. The prodrugs of the invention comprise a water-soluble polymer having three or more arms, at least three of which are covalently attached to an active agent, e.g., a small molecule. The conjugates of the invention provide an optimal balance of polymer size and structure for achieving improved drug loading, since the conjugates of the invention possess three or more active agents releasably attached to a multi-armed water soluble polymer. The prodrugs of the invention are therapeutically effective, and exhibit improved properties in-vivo when compared to unmodified parent drug.
摘要翻译：本文提供水溶性前药。本发明的前药包含具有三个或更多个臂的水溶性聚合物，其中至少三个共价连接到活性剂例如小分子上。由于本发明的共轭物具有三种或更多种可释放地连接到多臂水溶性聚合物上的活性剂，本发明的共轭物提供聚合物尺寸和结构的最佳平衡以实现改善的药物负载。与未修饰的母体药物相比，本发明的前药在治疗上是有效的，并且在体内表现出改善的性质。

8. 发明申请

US20050008612A1 Sterically hindered poly(ethylene glycol) alkanoic acids and derivatives thereof 有权
标题翻译：受阻的聚（乙二醇）链烷酸及其衍生物
公开(公告)号：US20050008612A1
公开(公告)日：2005-01-13
申请号：US10813601
申请日：2004-03-30
申请人： Michael Bentley , Xuan Zhao , Xiaoming Shen , Lihong Guo
发明人： Michael Bentley , Xuan Zhao , Xiaoming Shen , Lihong Guo
IPC分类号： C12N9/36 , A61K47/48 , C08F8/00 , C08G65/324 , C08G65/329 , C08G65/332 , C08G85/00 , A61K38/17 , C07K14/47 , C08G63/48 , C08G63/91
CPC分类号： C08G65/324 , A61K47/60 , C08G65/32 , C08G65/329 , C08G65/332 , C08G65/3322 , C08G65/333
摘要： The invention provides a sterically hindered polymer that comprises a water-soluble and non-peptidic polymer backbone having at least one terminus covalently bonded to an alkanoic acid or alkanoic acid derivative, wherein the carbon adjacent to the carbonyl group of the acid or acid derivative group has an alkyl or aryl group pendent thereto. The steric effects of the alkyl or aryl group allow greater control of the hydrolytic stability of polymer derivatives. The polymer backbone may be poly(ethylene glycol).
摘要翻译：本发明提供一种空间位阻聚合物，其包含具有至少一个与链烷酸或链烷酸衍生物共价结合的末端的水溶性和非肽性聚合物主链，其中与酸或酸衍生物基团的羰基相邻的碳具有其上的烷基或芳基。烷基或芳基的空间效应允许更好地控制聚合物衍生物的水解稳定性。聚合物主链可以是聚（乙二醇）。

9. 发明授权

US08728493B2 Polymer based compositions and conjugates of non-steroidal anti-inflammatory drugs 有权
标题翻译：基于聚合物的组合物和非甾体抗炎药物的缀合物
公开(公告)号：US08728493B2
公开(公告)日：2014-05-20
申请号：US11454998
申请日：2006-06-15
申请人： Kevin Burton , Xuan Zhao , Michael Bentley
发明人： Kevin Burton , Xuan Zhao , Michael Bentley
IPC分类号： A61K9/00 , A01N43/38 , A61K31/40
CPC分类号： C08G65/329 , A61K47/60
摘要： Provided herein are water-soluble polymer conjugates and polymer-based compositions of non-steroidal anti-inflammatory drugs. Also provided are methods for synthesizing and administering such conjugates and compositions.
摘要翻译：本文提供的是非甾体抗炎药的水溶性聚合物缀合物和基于聚合物的组合物。还提供了用于合成和施用这种缀合物和组合物的方法。

10. 发明申请

US20070276116A1 Hydrolytically degradable polymers and hydrogels made therefrom 有权
标题翻译：水解可降解的聚合物和水凝胶
公开(公告)号：US20070276116A1
公开(公告)日：2007-11-29
申请号：US11890162
申请日：2007-08-03
申请人： J. Milton Harris , Michael Bentley , Xuan Zhao , Xiaoming Shen
发明人： J. Milton Harris , Michael Bentley , Xuan Zhao , Xiaoming Shen
IPC分类号： C08G64/00
CPC分类号： C08G64/0208 , C08G64/0216 , C08G64/183
摘要： A water soluble polymer comprising multiple degradable carbonate linkages in a backbone and, for each carbonate linkage in the backbone, an oligomer linked thereto by the carbonate linkage, wherein the oligomer is branched.
摘要翻译：在主链中包含多个可降解碳酸酯键的水溶性聚合物，并且对于骨架中的每个碳酸酯键，由碳酸酯键连接的低聚物，其中低聚物是支链的。

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