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1. 发明授权

US11208530B2 Multi-arm polyethylene glycol, preparation method and uses thereof 有权
公开(公告)号：US11208530B2
公开(公告)日：2021-12-28
申请号：US13127349
申请日：2009-09-28
申请人： Xuan Zhao , Yuhe Zhao
发明人： Xuan Zhao , Yuhe Zhao
IPC分类号： C08G65/26 , C08G65/332 , C08G65/333 , C08G65/337 , C08G65/334 , A61K47/60
摘要： A novel multi-arm polyethylene glycol (PEG) (I) and preparation method thereof. Active derivatives (II) based on the multi-arm PEG. Gels formed of the active derivatives. Drug conjugates formed of the active derivatives and drug molecules and uses thereof in medical preparation. The multi-arm PEG is formed by polymerizing ethylene oxide with pentaerythritol oligomers as initiator, wherein PEG is the same or different and is a —(CH2CH2O)m-, the average value of m is an integer of 3-1000, l is an integer more than or equal to 2. An 8-arm PEG is preferred, wherein l is equal to 3. The active derivatives (II) comprise link groups X attached to PEG and active end groups F attached to X.

2. 发明申请

US20110286956A1 NOVEL MULTI-ARM POLYETHYLENE GLYCOL, PREPARATION METHOD AND USES THEREOF 审中-公开
标题翻译：新型多臂聚乙烯甘油，其制备方法及其用途
公开(公告)号：US20110286956A1
公开(公告)日：2011-11-24
申请号：US13127349
申请日：2009-09-28
申请人： Xuan Zhao , Yuhe Zhao
发明人： Xuan Zhao , Yuhe Zhao
IPC分类号： A61K31/77 , C08L71/02 , C08G65/333 , C08G65/332 , C12N9/96 , C08G65/28
CPC分类号： C08G65/2609 , A61K47/60 , C08G65/3322 , C08G65/33337 , C08G65/33396 , C08G65/3344 , C08G65/337 , C08G2650/24 , C08L2203/02
摘要： A novel multi-arm polyethylene glycol (PEG) (I) and preparation method thereof. Active derivatives (II) based on the multi-arm PEG. Gels formed of the active derivatives. Drug conjugates formed of the active derivatives and drug molecules and uses thereof in medical preparation. The multi-arm PEG is formed by polymerizing ethylene oxide with pentaerythritol oligomers as initiator, wherein PEG is the same or different and is a —(CH2CH2O)m-, the average value of m is an integer of 3-1000, l is an integer more than or equal to 2. An 8-arm PEG is preferred, wherein l is equal to 3. The active derivatives (II) comprise link groups X attached to PEG and active end groups F attached to X.
摘要翻译：一种新型多臂聚乙二醇（PEG）（I）及其制备方法。基于多臂PEG的活性衍生物（II）。由活性衍生物形成的凝胶。由活性衍生物和药物分子形成的药物偶联物及其在医疗制剂中的用途。多臂PEG通过将环氧乙烷与季戊四醇低聚物作为引发剂聚合形成，其中PEG相同或不同，为 - （CH 2 CH 2 O）m - ，m的平均值为3-1000的整数，l为整数大于或等于2.优选8-臂PEG，其中l等于3.活性衍生物（II）包含连接于PEG的连接基团X和连接至X的活性末端基团F.

3. 发明授权

US09586191B2 Magnetic core coated inorganic ion adsorbent for removing Cs ions in radioactive wastewater and preparation method thereof 有权
标题翻译：用于去除放射性废水中的Cs离子的磁芯涂覆的无机离子吸附剂及其制备方法
公开(公告)号：US09586191B2
公开(公告)日：2017-03-07
申请号：US14428437
申请日：2013-09-18
申请人： Xuan Zhao , Jiying Wei , Fuzhi Li
发明人： Xuan Zhao , Jiying Wei , Fuzhi Li
IPC分类号： B01J23/00 , B01J20/02 , B01J20/28 , B01J20/10 , B01J20/06 , B01J20/32 , C02F1/28 , C02F101/20 , C02F103/34
CPC分类号： B01J20/0229 , B01J20/06 , B01J20/103 , B01J20/28004 , B01J20/28007 , B01J20/28009 , B01J20/3204 , B01J20/3236 , B01J20/3289 , B01J20/3293 , C02F1/281 , C02F1/288 , C02F1/488 , C02F2101/006 , C02F2101/20 , C02F2103/34
摘要： The invention discloses a micron-grade magnetic core coated ferrocyanide adsorbent for removing Cs ions in radioactive wastewater and a preparation method thereof. The adsorbent takes magnetic Fe3O4 as a core, the surface is coated with a dense SiO2 single layer serving as a protective layer, and an active component is metal ion stabilized potassium ferrocyanide coated on the outer layer, wherein stabilized metal ions comprise Ti, Zn, Cu, Ni, Co, and Zr. The particle size of the adsorbent is 0.2-5 μm, the adsorbent in the outermost layer is conductive to improving the adsorption efficiency for Cs+ ions, and an external magnetic field is adopted for realizing solid-liquid phase separation. The preparation method comprises the following steps: coating a hydrated metal oxide of Ti, Zr or Co, Ni, Cu or Zn on the surface of Fe3O4SiO2 to form a composite magnetic material, wherein the hydrated oxide performs hydroxyl polymerization reaction with the surface of SiO2 to produce M—O—Si bonds to improve the bonding strength between M and the surface of SiO2; and finally reacting the composite magnetic material with a potassium ferrocyanide solution to form the required composite adsorbent, wherein the metal ions M achieve the effects of stabilizing the ferrocyanide and also achieve a bridge effect for bonding the ferrocyanide and the composite magnetic material together.
摘要翻译：本发明公开了一种用于去除放射性废水中的Cs离子的微米级磁芯涂层亚铁氰化物吸附剂及其制备方法。吸附剂采用磁性Fe3O4为核心，表面涂覆有作为保护层的致密SiO 2单层，活性组分是金属离子稳定化的亚铁氰化钾，其外部层包含稳定的金属离子，其中Ti，Zn， Cu，Ni，Co和Zr。吸附剂的粒径为0.2-5μm，最外层的吸附剂导电，提高Cs +离子的吸附效率，采用外部磁场实现固相分离。制备方法包括以下步骤：在Fe3O4SiO2表面涂覆Ti，Zr或Co，Ni，Cu或Zn的水合金属氧化物，形成复合磁性材料，其中水合氧化物与SiO2表面进行羟基聚合反应以产生M-O-Si键，以提高M与SiO2表面的结合强度; 最后使复合磁性材料与亚铁氰化钾溶液反应形成所需的复合吸附剂，其中金属离子M达到稳定亚铁氰化物的效果，并且还实现了将亚铁氰化物和复合磁性材料粘合在一起的桥接效应。

4. 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。

5. 发明授权

US08034825B2 Chemically modified small molecules 有权
标题翻译：化学修饰的小分子
公开(公告)号：US08034825B2
公开(公告)日：2011-10-11
申请号：US12822935
申请日：2010-06-24
申请人： Michael D. Bentley , Tacey X. Viegas , Richard R. Goodin , Lin Cheng , Xuan Zhao
发明人： Michael D. Bentley , Tacey X. Viegas , Richard R. Goodin , Lin Cheng , Xuan Zhao
IPC分类号： A61K31/485 , C07D489/08
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。

6. 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）。

7. 发明申请

US20110009589A1 DEGRADABLE HETEROBIFUNCTIONAL POLY(ETHYLENE GLYCOL) ACRYLATES AND GELS AND CONJUGATES DERIVED THEREFROM 审中-公开
标题翻译：可降解的异戊二烯（乙二醇）丙烯酸酯和凝胶以及其衍生物
公开(公告)号：US20110009589A1
公开(公告)日：2011-01-13
申请号：US12860525
申请日：2010-08-20
申请人： J. Milton Harris , Xuan Zhao
发明人： J. Milton Harris , Xuan Zhao
IPC分类号： C08F20/58 , C08F22/20
CPC分类号： C08L71/02 , A61K47/60 , C08G65/329 , C08G65/3322 , C08L2203/02 , Y10S530/81 , Y10S530/816 , C08L2666/04
摘要： A heterobifunctional poly(ethylene glycol) is provided having a hydrolytically degradable linkage, a first terminus comprising an acrylate group, and a second terminus comprising a target such as a protein or pharmaceutical agent or a reactive moiety capable of coupling to a target. Hydrogels can be prepared. The hydrogels can be used as a carrier for a protein or a pharmaceutical agent that can be readily released in a controlled fashion.
摘要翻译：提供具有水解可降解键的异双功能聚（乙二醇），包含丙烯酸酯基的第一末端，和包含诸如蛋白质或药物的靶的第二末端或能够与靶偶合的反应性部分。水凝胶可以制备。水凝胶可用作可以以受控方式容易地释放的蛋白质或药剂的载体。

8. 发明申请

US20100152414A1 MULTI-ARM POLYMER PRODRUGS 有权
标题翻译：多臂聚合物原料
公开(公告)号：US20100152414A1
公开(公告)日：2010-06-17
申请号：US12709800
申请日：2010-02-22
申请人： Xuan Zhao , Michael D. Bentley , Zhongxu Ren , Tacey X. Viegas
发明人： Xuan Zhao , Michael D. Bentley , Zhongxu Ren , Tacey X. Viegas
IPC分类号： C08G73/10
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。

9. 发明申请

US20100105946A1 Hydrolytically Degradable Carbamate Derivatives of Poly(Ethylene Glycol) 有权
标题翻译：聚（乙二醇）的水解可降解的氨基甲酸酯衍生物
公开(公告)号：US20100105946A1
公开(公告)日：2010-04-29
申请号：US12559320
申请日：2009-09-14
申请人： Michael David Bentley , Xuan Zhao
发明人： Michael David Bentley , Xuan Zhao
IPC分类号： C07C69/63
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 pro-drugs 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 either 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 amine drug at a controllable rate as the gel degrades.
摘要翻译：公开了可用作水溶性前体药物的聚（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，当凝胶降解时，药物可以被捕获在凝胶中并通过扩散释放，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胺药物。

10. 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）。

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