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91. 发明授权

US06864350B2 Soluble, degradable poly (ethylene glycol) derivatives for controllable release of bound molecules into solution 有权
标题翻译：可溶性，可降解的聚（乙二醇）衍生物，用于将结合分子可控地释放到溶液中
公开(公告)号：US06864350B2
公开(公告)日：2005-03-08
申请号：US10318322
申请日：2002-12-12
申请人： J. Milton Harris
发明人： J. Milton Harris
IPC分类号： A61K47/48 , C08G65/333 , A61K31/74 , A61K31/765 , C08G73/10
CPC分类号： C08G65/33396 , A61K47/60 , C08G65/33317
摘要： PEG and related polymer derivatives having weak, hydrolytically unstable linkages near the reactive end of the polymer are provided for conjugation to drugs, including proteins, enzymes, small molecules, and others. These derivatives provide a sufficient circulation period for a drug-PEG conjugate and then for hydrolytic breakdown of the conjugate and release of the bound molecule. In some cases, drugs that previously had reduced activity when permanently coupled to PEG can have therapeutically suitable activity when coupled to a degradable PEG in accordance with the invention. The PEG of the invention can be used to impart water solubility, size, slow rate of kidney clearance, and reduced immunogenicity to the conjugate. Controlled hydrolytic release of the bound molecule in the aqueous environment can then enhance the drug delivery system.
摘要翻译：提供在聚合物的反应性末端附近具有弱的水解不稳定键的PEG和相关的聚合物衍生物用于与药物（包括蛋白质，酶，小分子等）共轭。这些衍生物为药物-PEG缀合物提供足够的循环周期，然后用于结合物的水解分解和结合分子的释放。在一些情况下，当与PEG偶联时，先前具有减少的活性的药物在与根据本发明的可降解的PEG偶联时可具有治疗上合适的活性。本发明的PEG可用于赋予水溶性，大小，缓慢的肾清除率，降低对缀合物的免疫原性。在水环境中控制的结合分子的水解释放可以增强药物递送系统。

92. 发明授权

US06362276B1 Degradable heterobifunctional poly(ethylene glycol) acrylates and gels and conjugates derived therefrom 有权
标题翻译：可降解的异双功能聚（乙二醇）丙烯酸酯和由其衍生的凝胶和共轭物
公开(公告)号：US06362276B1
公开(公告)日：2002-03-26
申请号：US09226341
申请日：1999-01-06
申请人： J. Milton Harris , Xuan Zhao
发明人： J. Milton Harris , Xuan Zhao
IPC分类号： C08K515
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。

93. 发明授权

US06214966B1 Soluble, degradable poly(ethylene glycol) derivatives for controllable release of bound molecules into solution 失效
标题翻译：可溶性，可降解的聚（乙二醇）衍生物，用于将结合分子可控地释放到溶液中
公开(公告)号：US06214966B1
公开(公告)日：2001-04-10
申请号：US08937846
申请日：1997-09-25
申请人： J. Milton Harris
发明人： J. Milton Harris
IPC分类号： A61K31765
CPC分类号： C08G65/33396 , A61K47/60 , C08G65/33317
摘要： PEG and related polymer derivatives having weak, hydrolytically unstable linkages near the reactive end of the polymer are provided for conjugation to drugs, including proteins, enzymes, small molecules, and others. These derivatives provide a sufficient circulation period for a drug-PEG conjugate and then for hydrolytic breakdown of the conjugate and release of the bound molecule. In some cases, drugs that previously had reduced activity when permanently coupled to PEG can have therapeutically suitable activity when coupled to a degradable PEG in accordance with the invention. The PEG of the invention can be used to impart water solubility, size, slow rate of kidney clearance, and reduced immunogenicity to the conjugate. Controlled hydrolytic release of the bound molecule in the aqueous environment can then enhance the drug delivery system.
摘要翻译：提供在聚合物的反应性末端附近具有弱的水解不稳定键的PEG和相关的聚合物衍生物用于与药物（包括蛋白质，酶，小分子等）共轭。这些衍生物为药物-PEG缀合物提供足够的循环周期，然后用于结合物的水解分解和结合分子的释放。在一些情况下，当与PEG偶联时，先前具有减少的活性的药物在与根据本发明的可降解的PEG偶联时可具有治疗上合适的活性。本发明的PEG可用于赋予水溶性，大小，缓慢的肾清除率，降低对缀合物的免疫原性。在水环境中控制的结合分子的水解释放可以增强药物递送系统。

94. 发明授权

US5932462A Multiarmed, monofunctional, polymer for coupling to molecules and surfaces 失效
标题翻译：用于偶联到分子和表面的多臂单功能聚合物
公开(公告)号：US5932462A
公开(公告)日：1999-08-03
申请号：US443383
申请日：1995-05-17
申请人： J. Milton Harris , Francesco Maria Veronese , Paolo Caliceti , Oddone Schiavon
发明人： J. Milton Harris , Francesco Maria Veronese , Paolo Caliceti , Oddone Schiavon
IPC分类号： A61K47/48 , C08G65/329 , C12N9/96 , A01N63/00 , C07K17/00 , C12N11/06
CPC分类号： C08G65/48 , A61K47/48215 , C08G65/329 , C12N9/96 , Y10S530/815 , Y10S530/816
摘要： Multi-armed, monofunctional, and hydrolytically stable polymers are described having the structure ##STR1## wherein Z is a moiety that can be activated for attachment to biologically active molecules such as proteins and wherein P and Q represent linkage fragments that join polymer arms poly.sub.a and poly.sub.b, respectively, to central carbon atom, C, by hydrolytically stable linkages in the absence of aromatic rings and ester groups in the linkage fragments. R typically is hydrogen or methyl, but can be a linkage fragment that includes another polymer arm. A specific example is an mPEG disubstituted lysine having the structure ##STR2## where mPEG.sub.a and mPEG.sub.b have the structure CH.sub.3 O--(CH.sub.2 CH.sub.2 O).sub.n CH.sub.2 CH.sub.2 -- wherein n may be the same or different for mPEG.sub.a and mPEG.sub.b and can be from 1 to about 1,150 to provide molecular weights of from about 100 to 100,000. The mPEG disubstituted lysine can be purified from a reaction mixture by chromatography in water, including gel filtration chromatography and ion exchange chromatography because the carboxyl group is ionizable. Impurities are removed, including unreacted mPEG and mPEG monosubstituted lysine, to provide the polymer in pure form. Ion exchange chromatography permits fractionation of a greater amount of polymer per run.
摘要翻译：描述了具有以下结构的多臂，单功能和水解稳定的聚合物，其中Z是可被激活以附着于生物活性分子如蛋白质的部分，并且其中P和Q分别表示分别连接聚合物臂polya和polyb的连接片段，通过在不存在芳环和通过连接片段中的酯基的水解稳定键连接到中心碳原子。 R通常是氢或甲基，但可以是包含另一聚合物臂的连接片段。具体实例是具有mPEGa和mPEGb具有CH 3 O-（CH 2 CH 2 O）n CH 2 CH 2结构的结构的mPEG二取代的赖氨酸，其中n可以相同或不同于mPEGa和mPEGb，并且可以为1至约1,150，以提供从约100到100,000。可以通过色谱法在水中从反应混合物中纯化mPEG二取代的赖氨酸，包括凝胶过滤色谱和离子交换色谱法，因为羧基是可离子化的。除去杂质，包括未反应的mPEG和mPEG单取代的赖氨酸，以提供纯的形式的聚合物。离子交换色谱法允许每次运行更大量的聚合物分级。

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