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71. 发明申请

US20100330023A1 Multifunctional Forms of Polyoxazoline Copolymers and Drug Compositions Comprising the Same 有权
标题翻译：多官能团形式的聚恶唑啉共聚物和药物组合物组成
公开(公告)号：US20100330023A1
公开(公告)日：2010-12-30
申请号：US12787241
申请日：2010-05-25
申请人： Kunsang Yoon , Michael David Bentley , J. Milton Harris , Zhihao Fang , Tacey Viegas
发明人： Kunsang Yoon , Michael David Bentley , J. Milton Harris , Zhihao Fang , Tacey Viegas
IPC分类号： A61K31/785 , A61P35/00
CPC分类号： A61K47/48207 , A61K38/09 , A61K47/59 , C08G73/0233
摘要： The present disclosure provides copolymers of 2-substituted-2-oxazolines possessing two or three reactive functional groups which are also chemically orthogonal. The copolymers described may be random copolymers, block copolymers or a mixture of random and block copolymer configurations. Furthermore, the present disclosure provides novel methods for synthesizing the above polymers and for conjugating to molecules such as targeting, diagnostic and therapeutic agents.
摘要翻译：本公开提供了具有两个或三个也是化学正交的反应性官能团的2-取代-2-恶唑啉的共聚物。所述共聚物可以是无规共聚物，嵌段共聚物或无规嵌段共聚物构型的混合物。此外，本公开提供了用于合成上述聚合物并用于与靶标，诊断和治疗剂等分子缀合的新方法。

72. 发明申请

US20100298496A1 MULTI-ARMED, MONOFUNCTIONAL, AND HYDROLYTICALLY STABLE DERIVATIVES OF POLY(ETHYLENE GLYCOL) AND RELATED POLYMERS FOR MODIFICATION OF SURFACES AND MOLECULES 失效
标题翻译：聚（乙烯甘油）和相关聚合物的多臂，单功能和水解稳定性衍生物，用于修饰表面和分子
公开(公告)号：US20100298496A1
公开(公告)日：2010-11-25
申请号：US12849683
申请日：2010-08-03
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
CPC分类号： C08G65/48 , A61K47/60 , C08G65/329 , C12N9/96 , Y10S530/815 , Y10S530/816
摘要： Multi-armed, monofunctional, and hydrolytically stable polymers are described having the structure 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 polya and polyb, respectively, to central carbon atom, C, by hydrolytically stable linkages in the absence of aromatic rings 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 where mPEGa and mPEGb have the structure CH3O—(CH2CH2O)nCH2CH2— wherein n may be the same or different for polya- and polyb- and can be from 1 to about 1,150 to provide molecular weights of from about 100 to 100,000.
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的连接片段通过在连接片段中不存在芳环的水解稳定键而与中心碳原子C连接。 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mPEG二取代的赖氨酸，其具有结构，其中mPEGa和mPEGb具有结构CH 3 O-（CH 2 CH 2 O）n CH 2 CH 2 - ，其中n可以相同或不同，用于聚-α-和polyb-并且可以为1至约1,150，以提供分子约100至100,000的重量。

73. 发明申请

US20090054590A1 Multi-armed, monofunctional, and hydrolytically stable derivatives of poly (ethylene glycol) and related polymers for modification of surfaces and molecules 失效
标题翻译：聚（乙二醇）多官能，单官能和水解稳定的衍生物以及用于表面和分子修饰的相关聚合物
公开(公告)号：US20090054590A1
公开(公告)日：2009-02-26
申请号：US12284357
申请日：2008-09-20
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： C08L89/00 , C08G65/00 , C08G73/10 , C08G63/00 , C08G69/26
CPC分类号： C08G65/48 , A61K47/60 , C08G65/329 , C12N9/96 , Y10S530/815 , Y10S530/816
摘要： Multi-armed, monofunctional, and hydrolytically stable polymers are described having the structure 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 polya and polyb, respectively, to central carbon atom, C, by hydrolytically stable linkages in the absence of aromatic rings 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 where mPEGa and mPEGb have the structure CH3O—(CH2CH2O)nCH2CH2— wherein n may be the same or different for polya- and polyb- and can be from 1 to about 1,150 to provide molecular weights of from about 100 to 100,000.
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的连接片段通过在连接片段中不存在芳环的水解稳定键而与中心碳原子C连接。 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mPEG二取代的赖氨酸，其具有结构，其中mPEGa和mPEGb具有结构CH 3 O-（CH 2 CH 2 O）n CH 2 CH 2 - ，其中n可以相同或不同，用于聚-α-和polyb-，并且可以为1至约1,150，以提供分子约100至100,000的重量。

74. 发明授权

US07214388B2 Degradable heterobifunctional poly(ethylene glycol) acrylates 失效
公开(公告)号：US07214388B2
公开(公告)日：2007-05-08
申请号：US10684692
申请日：2003-10-14
申请人： J. Milton Harris , Xuan Zhao
发明人： J. Milton Harris , Xuan Zhao
IPC分类号： A61K9/00 , A61K47/48 , C12N11/00 , G01N33/543 , C07K17/00
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.

75. 发明授权

US07214366B2 Isolatable, water soluble, and hydrolytically stable active sulfones of poly(ethylene glycol) and related polymers for modification of surfaces and molecules 失效
标题翻译：用于改性表面和分子的聚（乙二醇）和相关聚合物的可分离，水溶性和水解稳定的活性砜
公开(公告)号：US07214366B2
公开(公告)日：2007-05-08
申请号：US11112118
申请日：2005-04-22
申请人： J. Milton Harris
发明人： J. Milton Harris
IPC分类号： A61K9/14 , A61K31/74 , A61K47/30 , A61K47/48 , C12N11/08
CPC分类号： C08G65/334 , A61K47/60 , C08G65/326 , C08G65/329 , Y10S530/815 , Y10S530/816
摘要： Water soluble activated polymers are provided containing an active ethyl sulfone moiety having a reactive site located at the second carbon from the sulfone group. In an embodiment, a poly(ethylene glycol) (PEG) derivative is disclosed that is activated with the active ethyl sulfone moiety for selective attachment to thiol moieties on molecules and surfaces. The activated PEG is water soluble, hydrolytically stable for extended periods, and forms hydrolytically stable linkages with thiol moieties. The linkages generally are not reversible in reducing environments. The PEG derivative is useful for modifying the characteristics of substances including modifying biologically active molecules and surfaces for biocompatibility.
摘要翻译：提供了含有活性乙基砜部分的水溶性活化聚合物，其具有位于来自砜基团的第二个碳的反应位点。在一个实施方案中，公开了用活性乙基砜部分活化的聚（乙二醇）（PEG）衍生物，用于选择性连接到分子和表面上的硫醇部分。活化的PEG水溶性，长时间水解稳定，与硫醇部分形成水解稳定的键。联系通常在减少环境中是不可逆的。 PEG衍生物可用于改变包括改变生物活性分子和表面的物质的生物相容性的特征。

76. 发明授权

US07074878B1 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：US07074878B1
公开(公告)日：2006-07-11
申请号：US10412642
申请日：2003-04-10
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。

77. 发明授权

US06890518B2 Compositions of chemically modified insulin 失效
标题翻译：化学修饰胰岛素的组成
公开(公告)号：US06890518B2
公开(公告)日：2005-05-10
申请号：US10405190
申请日：2003-04-01
申请人： John S. Patton , Mei-Chang Kuo , J. Milton Harris , Chester Leach , Kimberly Perkins , Blaine Bueche
发明人： John S. Patton , Mei-Chang Kuo , J. Milton Harris , Chester Leach , Kimberly Perkins , Blaine Bueche
IPC分类号： A61K9/08 , A61K9/12 , A61K9/19 , A61K9/24 , A61K9/72 , A61K38/00 , A61K38/16 , A61K38/28 , A61K47/34 , A61K47/48 , A61L9/04 , A61P3/10 , C07K14/62
CPC分类号： A61K38/28 , A61K47/60
摘要： The present invention provides active, hydrophilic polymer-modified derivatives of insulin. The insulin derivatives of the invention are, in one aspect, suitable for delivery to the lung and exhibit pharmakokinetic and/or pharmacodynamic properties that are significantly improved over native insulin.
摘要翻译：本发明提供胰岛素的活性亲水性聚合物改性衍生物。在一个方面，本发明的胰岛素衍生物适合于递送至肺并表现出比天然胰岛素明显改善的药物动力学和/或药效学性质。

78. 发明授权

US06610281B2 Water soluble activated polymers containing an active ethyl sulfone moiety for modification of surfaces and molecules 失效
标题翻译：含有活性乙基砜部分用于表面和分子改性的水溶性活化聚合物
公开(公告)号：US06610281B2
公开(公告)日：2003-08-26
申请号：US09294188
申请日：1999-04-19
申请人： J. Milton Harris
发明人： J. Milton Harris
IPC分类号： A61K914
CPC分类号： C08G65/334 , A61K47/60 , C08G65/326 , C08G65/329 , Y10S530/815 , Y10S530/816
摘要： Water soluble activated polymers are provided containing an active ethyl sulfone moiety having a reactive site located at the second carbon from the sulfone group. In an embodiment, a poly(ethylene glycol) (PEG) derivative is disclosed that is activated with the active ethyl sulfone moiety for selective attachment to thiol moieties on molecules and surfaces. The activated PEG is water soluble, hydrolytically stable for extended periods, and forms hydrolytically stable linkages with thiol moieties. The linkages generally are not reversible in reducing environments. The PEG derivative is useful for modifying the characteristics of substances including modifying biologically active molecules and surfaces for biocompatibility.
摘要翻译：提供了含有活性乙基砜部分的水溶性活化聚合物，其具有位于来自砜基团的第二个碳的反应位点。在一个实施方案中，公开了用活性乙基砜部分活化的聚（乙二醇）（PEG）衍生物，用于选择性连接到分子和表面上的硫醇部分。活化的PEG水溶性，长时间水解稳定，与硫醇部分形成水解稳定的键。联系通常在减少环境中是不可逆的。 PEG衍生物可用于改变包括改变生物活性分子和表面的物质的生物相容性的特征。

79. 发明授权

US06515100B2 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：US06515100B2
公开(公告)日：2003-02-04
申请号：US09824297
申请日：2001-04-02
申请人： J. Milton Harris
发明人： J. Milton Harris
IPC分类号： A61K3174
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。

80. 发明授权

US08501899B2 Multifunctional forms of polyoxazoline copolymers and drug compositions comprising the same 有权
公开(公告)号：US08501899B2
公开(公告)日：2013-08-06
申请号：US13356552
申请日：2012-01-23
申请人： Kunsang Yoon , J. Milton Harris , Michael David Bentley , Zhihao Fang , Tacey Viegas
发明人： Kunsang Yoon , J. Milton Harris , Michael David Bentley , Zhihao Fang , Tacey Viegas
IPC分类号： C08G73/06 , C08G75/02 , C08G69/00
CPC分类号： A61K47/48207 , A61K38/09 , A61K47/59 , C08G73/0233
摘要： The present disclosure provides copolymers of 2-substituted-2-oxazolines possessing two or three reactive functional groups which are also chemically orthogonal. The copolymers described may be random copolymers, block copolymers or a mixture of random and block copolymer configurations. Furthermore, the present disclosure provides novel methods for synthesizing the above polymers and for conjugating to molecules such as targeting, diagnostic and therapeutic agents.

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