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81. 发明授权

US07943141B2 Activated polyoxazolines and compositions comprising the same 有权
标题翻译：活性聚恶唑啉及其组合物
公开(公告)号：US07943141B2
公开(公告)日：2011-05-17
申请号：US12529001
申请日：2008-02-28
申请人： J. Milton Harris , Michael David Bentley , Kunsang Yoon , Zhihao Fang , Francesco Maria Veronese
发明人： J. Milton Harris , Michael David Bentley , Kunsang Yoon , Zhihao Fang , Francesco Maria Veronese
IPC分类号： A61K39/385
CPC分类号： A61K31/787 , A61K47/60 , C07D207/452 , C07D207/46 , C07D401/12 , C08G73/0233 , C08L79/02
摘要： The present disclosure provides terminally activated monofunctional POZ derivatives having a range of functional active groups allowing conjugation of the monofunctional POZ derivatives to a variety of target molecules under a wide range of reaction conditions to produce a hydrolytically stable target molecule-POZ conjugate. Furthermore, the present disclosure provides novel methods of synthesis for the disclosed terminally activated monofunctional POZ derivatives and hydrolytically stable target molecule-POZ conjugates created using the disclosed terminally activated monofunctional POZ derivatives.
摘要翻译：本公开提供具有一定范围的官能活性基团的末端活化单官能POZ衍生物，其允许在宽范围的反应条件下将单官能POZ衍生物缀合到多种靶分子以产生水解稳定的靶分子-POZ缀合物。此外，本公开提供了所公开的末端活化单官能POZ衍生物和使用所公开的末端活化单官能POZ衍生物产生的水解稳定的靶分子-POZ共轭物的合成新方法。

82. 发明申请

US20110009594A1 MULTIFUNCTIONAL FORMS OF POLYOXAZOLINE COPOLYMERS AND DRUG COMPOSITIONS COMPRISING THE SAME 有权
标题翻译：聚氧杂环丁烷共聚物的多功能形式和包含其的药物组合物
公开(公告)号：US20110009594A1
公开(公告)日：2011-01-13
申请号：US12744472
申请日：2009-01-12
申请人： Kunsang Yoon , J. Milton Harris , Michael David Bentley
发明人： Kunsang Yoon , J. Milton Harris , Michael David Bentley
IPC分类号： C08G75/02 , C08G73/06
CPC分类号： C08G73/0233 , C08G73/028
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。

83. 发明授权

US07786221B2 Multi-armed, monofunctional, and hydrolytically stable derivatives of poly (ethylene glycol) and related polymers for modification of surfaces and molecules 有权
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：US07786221B2
公开(公告)日：2010-08-31
申请号：US12284357
申请日：2008-09-18
申请人： J. Milton Harris , Francesco Maria Veronese , Paola Caliceti , Oddone Schiavon
发明人： J. Milton Harris , Francesco Maria Veronese , Paola Caliceti , Oddone Schiavon
IPC分类号： C08G65/34 , C08F283/00 , A61K31/40
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。

84. 发明授权

US07714088B2 Poly(ethylene glycol) derivatives with proximal reactive groups 有权
标题翻译：具有近端反应性基团的聚（乙二醇）衍生物
公开(公告)号：US07714088B2
公开(公告)日：2010-05-11
申请号：US12410438
申请日：2009-03-24
申请人： J. Milton Harris , Antoni Kozlowski
发明人： J. Milton Harris , Antoni Kozlowski
IPC分类号： C08F12/30 , C08F28/02 , C08F118/00 , C08F120/00 , C08F122/00 , C08F218/00
CPC分类号： C08G65/33396 , A61K47/60 , C08G65/329 , C08G65/33313 , C08G65/33337 , Y10S530/816
摘要： An activated, substantially water-soluble poly(ethylene glycol) is provided having of a linear or branched poly(ethylene glycol) backbone and at least one terminus linked to the backbone through a hydrolytically stable linkage, wherein the terminus is branched and has proximal reactive groups. The free reactive groups are capable of reacting with active moieties in a biologically active agent such as a protein or peptide thus forming conjugates between the activated (polyethylene glycol) and the biologically active agent.
摘要翻译：提供活化的，基本上水溶性的聚（乙二醇），其具有直链或支链的聚（乙二醇）主链和至少一个通过水解稳定键连接至主链的末端，其中末端是支链的并具有近端反应性团体游离反应性基团能够与生物活性剂如蛋白质或肽中的活性部分反应，从而在活化的（聚乙二醇）与生物活性剂之间形成共轭物。

85. 发明授权

US07642323B2 Heterobifunctional poly(ethylene glycol) derivatives and methods for their preparation 有权
标题翻译：异双功能聚（乙二醇）衍生物及其制备方法
公开(公告)号：US07642323B2
公开(公告)日：2010-01-05
申请号：US11016383
申请日：2004-12-17
申请人： Michael D. Bentley , J. Milton Harris , Antoni Kozlowski
发明人： Michael D. Bentley , J. Milton Harris , Antoni Kozlowski
IPC分类号： C08L71/02 , C08G65/32 , C07D207/00 , C07C211/00 , B01F17/00
CPC分类号： C08G65/3322 , C08G65/329
摘要： This invention provides a method for preparing, in high purity and high yield, heterobifunctional derivatives of poly(ethylene glycol) or related polymers. A chromatographic purification step is not necessary in the method. In accordance with the method of the invention, an intermediate polymer having a formula of W-Poly-OH is provided bearing a removable group W at one terminus. The intermediate polymer W-Poly-OH is first altered by modifying the OH group to a first functional group X, followed by the removal of W to generate a second hydroxyl group. The latter hydroxyl group may then be further converted to a second functional group Y, thus providing the desired heterobifunctional derivative.
摘要翻译：本发明提供一种以高纯度和高收率制备聚（乙二醇）或相关聚合物的异双功能衍生物的方法。在该方法中不需要色谱纯化步骤。根据本发明的方法，提供具有式W-聚-OH的中间体聚合物，其在一个末端具有可除去的基团W. 首先通过将OH基团改性为第一官能团X，随后除去W以产生第二羟基来改变中间体聚合物W-Poly-OH。然后可以将后一羟基进一步转化为第二官能团Y，从而提供所需的异双功能衍生物。

86. 发明申请

US20090215988A1 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，用于可控释放结合的分子进入溶液
公开(公告)号：US20090215988A1
公开(公告)日：2009-08-27
申请号：US12414621
申请日：2009-03-30
申请人： J. Milton Harris
发明人： J. Milton Harris
IPC分类号： C07K1/113 , C07C69/708 , C07D207/40
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, followed by hydrolytic breakdown of the conjugate and release of the bound molecule. In some cases, drugs that demonstrate reduced activity when permanently coupled to PEG maintain a therapeutically suitable activity when coupled to a degradable PEG in accordance with the invention. The PEG derivatives of the invention can be used to impart improved water solubility, increased size, a slower rate of kidney clearance, and reduced immunogenicity to a conjugate formed by attachment thereto. Controlled hydrolytic release of the bound molecule into an aqueous environment can then enhance the drug's delivery profile by providing a delivery system which employs such polymers and utilizes the teachings provided herein.
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，随后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永久偶联时表现出降低的活性的药物在与根据本发明的可降解的PEG偶联时，保持治疗上合适的活性。本发明的PEG衍生物可用于赋予改善的水溶性，增加的尺寸，较慢的肾清除速率，以及降低对通过其附着形成的缀合物的免疫原性。然后通过提供使用这种聚合物并利用本文提供的教导的递送系统，将结合的分子控制的水解释放到水性环境中可以增强药物的递送分布。

87. 发明授权

US07419600B2 Method for purifying a branched water-soluble polymer 失效
标题翻译：纯化支链水溶性聚合物的方法
公开(公告)号：US07419600B2
公开(公告)日：2008-09-02
申请号：US10634970
申请日：2003-08-05
申请人： J. Milton Harris , Francesco Maria Veronese , Paola Caliceti , Oddone Schiavon
发明人： J. Milton Harris , Francesco Maria Veronese , Paola Caliceti , Oddone Schiavon
IPC分类号： B01D15/36 , A61K38/43 , C12N11/08 , C12N11/06 , C12N9/96 , C07K17/06 , C07K17/08
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表示连接聚合物臂的连接片段分别通过在连接片段中不存在芳环的水解稳定键，与中心碳原子C分别形成。 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。具体实例是具有以下结构的mPEG二取代赖氨酸，其中mPEG a和mPEG b具有结构CH 3 O-（CH 3） CH 2 CH 2 CH 2其中n可以相同或不同，或者可以相同或不同，对于聚<！ - SIPO - >和 - 和多个b - 不同，并且可以为1至约1,150，以提供约100至100,000的分子量。

88. 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。

89. 发明授权

US06864327B2 Heterobifunctional poly(ethylene glycol) derivatives and methods for their preparation 有权
标题翻译：异双功能聚（乙二醇）衍生物及其制备方法
公开(公告)号：US06864327B2
公开(公告)日：2005-03-08
申请号：US10071469
申请日：2002-02-08
申请人： Michael David Bentley , J. Milton Harris , Antoni Kozlowski
发明人： Michael David Bentley , J. Milton Harris , Antoni Kozlowski
IPC分类号： C08G65/329 , C08G65/32 , C08L71/02
CPC分类号： C08G65/329
摘要： This invention provides a method for preparing, in high purity and high yield, heterobifunctional derivatives of poly(ethylene glycol) or related polymers. A chromatographic purification step is not necessary in the method. In accordance with the method of the invention, an intermediate polymer having a formula of W-Poly-OH is provided bearing a removable group W at one terminus. The intermediate polymer W-Poly-OH is first altered by modifying the OH group to a first functional group X, followed by the removal of W to generate a second hydroxyl group. The latter hydroxyl group may then be further converted to a second functional group Y, thus providing the desired heterobifunctional derivative.
摘要翻译：本发明提供一种以高纯度和高收率制备聚（乙二醇）或相关聚合物的异双功能衍生物的方法。在该方法中不需要色谱纯化步骤。根据本发明的方法，提供具有式W-聚-OH的中间体聚合物，其在一个末端具有可除去的基团W. 首先通过将OH基团改性为第一官能团X，然后除去W以产生第二羟基来改变中间体聚合物W-Poly-OH。然后可以将后一羟基进一步转化为第二官能团Y，从而提供所需的异双功能衍生物。

90. 发明授权

US06437025B1 Poly(ethylene glycol) derivatives with proximal reactive groups 有权
公开(公告)号：US06437025B1
公开(公告)日：2002-08-20
申请号：US09992129
申请日：2001-11-05
申请人： J. Milton Harris , Antoni Kozlowski
发明人： J. Milton Harris , Antoni Kozlowski
IPC分类号： C08K320
CPC分类号： C08G65/33396 , A61K47/60 , C08G65/329 , C08G65/33313 , C08G65/33337 , Y10S530/816
摘要： An activated, substantially water soluble poly(ethylene glycol) is provided having of a linear or branched poly(ethylene glycol) backbone and at least one terminus linked to the backbone through a hydrolytically stable linkage, wherein the terminus is branched and has proximal reactive groups. The free reactive groups are capable of reacting with active moieties in a biologically active agent such as a protein or peptide thus forming conjugates between the activated poly(ethylene glycol) and the biologically active agent.

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