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71. 发明授权

US08273833B2 Branched Polymers 有权
标题翻译：支链聚合物
公开(公告)号：US08273833B2
公开(公告)日：2012-09-25
申请号：US12963170
申请日：2010-12-08
申请人： Michael David Bentley , Xuan Zhao , Xiaoming Shen , William Dudley Battle, III
发明人： Michael David Bentley , Xuan Zhao , Xiaoming Shen , William Dudley Battle, III
IPC分类号： C08G63/91 , C08G2/30 , C08F234/00 , C08F265/06
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 ether 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，其通过醚键连接到中心脂族烃核心分子上。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 - ）m或（ - 亚烷基-O-）m键，其中m为1-10。

72. 发明申请

US20110207896A1 Sterically Hindered Poly(ethylene glycol) Alkanoic Acids and Derivatives Thereof 有权
标题翻译：受阻的聚（乙二醇）烷酸及其衍生物
公开(公告)号：US20110207896A1
公开(公告)日：2011-08-25
申请号：US13099965
申请日：2011-05-03
申请人： Michael David Bentley , Xuan Zhao , Xiaoming Shen , Lihong Guo
发明人： Michael David Bentley , Xuan Zhao , Xiaoming Shen , Lihong Guo
IPC分类号： 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 polymers and conjugates formed therefrom that comprise a water-soluble and non-peptidic polymer backbone having at least one terminus covalently bonded to an alkanoic acid or alkanoic acid derivative prior to conjugation, 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和由其形成的共轭物，其包含水溶性和非肽性聚合物主链，其在共轭之前具有至少一个与链烷酸或链烷酸衍生物共价结合的末端，其中与羰基相邻的碳的酸或酸衍生物基团具有与其相邻的烷基或芳基。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）。

73. 发明授权

US07674879B2 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：US07674879B2
公开(公告)日：2010-03-09
申请号：US12215086
申请日：2008-06-25
申请人： Michael D. Bentley , Xuan Zhao , Xiaoming Shen , Lihong Guo
发明人： Michael D. Bentley , Xuan Zhao , Xiaoming Shen , Lihong Guo
IPC分类号： C08F6/14 , C08G65/34 , C08G65/324 , C08G65/329 , C08G65/332
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）。

74. 发明授权

US07259224B2 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：US07259224B2
公开(公告)日：2007-08-21
申请号：US11377973
申请日：2006-03-17
申请人： J. Milton Harris , Michael David Bentley , Xuan Zhao , Xiaoming Shen
发明人： J. Milton Harris , Michael David 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-O-)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。

75. 发明授权

US07056500B2 Polymer conjugates of opioid antagonists 有权
公开(公告)号：US07056500B2
公开(公告)日：2006-06-06
申请号：US10274296
申请日：2002-10-18
申请人： Michael David Bentley , Michael James Roberts , Xiaoming Shen , Lin Cheng
发明人： Michael David Bentley , Michael James Roberts , Xiaoming Shen , Lin Cheng
IPC分类号： A81K31/74
CPC分类号： A61K47/60
摘要： The invention provides polymer conjugates of opioid antagonists comprising a polymer, such as poly(ethylene glycol), covalently attached to an opioid antagonist. The linkage between the polymer and the opioid antagonist is preferably hydrolytically stable. The invention also includes a method of treating one or more side effects associated with the use of opioid analgesics, such as constipation, nausea, or pruritus, by administering a polymer conjugate of the invention.

76. 发明授权

US06495659B2 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：US06495659B2
公开(公告)日：2002-12-17
申请号：US09741933
申请日：2000-12-20
申请人： Michael David Bentley , Xuan Zhao , Xiaoming Shen , Lihong Guo
发明人： Michael David Bentley , Xuan Zhao , Xiaoming Shen , Lihong Guo
IPC分类号： C08G6534
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）。

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