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公开(公告)号：US5631322A
公开(公告)日：1997-05-20
申请号：US475177
申请日：1995-06-07
申请人： Francesco M. Veronese , Oddone Schiavon , Paolo Caliceti , Luciana Sartore , Elisabetta Ranucci , Paolo Ferruti
发明人： Francesco M. Veronese , Oddone Schiavon , Paolo Caliceti , Luciana Sartore , Elisabetta Ranucci , Paolo Ferruti
CPC分类号： C12N11/08 , A61K47/48176 , C08F120/58 , C08F2/38 , C08F20/58 , C08F6/04 , C08F8/30 , C08F2810/40
摘要： Polymers of the monomer N-acryloylmorpholine having a single reactive moiety at one end of the polymer chain have the following structure: ##STR1## wherein --Z--X--Y is a polymer capping moiety, such as mercaptan, X represents a saturated residue of a linear or branched aliphatic series of the general structure --C.sub.r H.sub.2r -- in which r is an integer from 1 to about 12, Y is a reactive moiety and typically will be one of the reactive moieties commonly known in PEG chemistry, such as an --OH, --COOH, or --NH.sub.2 group, Z is a moiety that readily reacts to cap a polymer free radical, and n is an integer from about 6 to 280, which yields a number average molecular weight ("M.sub.n ") of from about 1,000 to 40,000. The monofunctional polymer is a suitable alternative to monofunctional PEG for modification of substances having biological and biotechnical applications.
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2.发明授权Polymers of N-acryloylmorpholine activated at one end and conjugates with bioactive materials and surfaces 失效N-丙烯酰吗啉的聚合物在一端活化并与生物活性材料和表面共轭
公开(公告)号：US5629384A
公开(公告)日：1997-05-13
申请号：US243869
申请日：1994-05-17
申请人： Francesco M. Veronese , Oddone Schiavon , Paolo Caliceti , Luciana Sartore , Elisabetta Ranucci , Paolo Ferruti
发明人： Francesco M. Veronese , Oddone Schiavon , Paolo Caliceti , Luciana Sartore , Elisabetta Ranucci , Paolo Ferruti
CPC分类号： C12N11/08 , A61K47/48176 , C08F120/58 , C08F2/38 , C08F20/58 , C08F6/04 , C08F8/30 , C08F2810/40
摘要： Polymers of the monomer N-acryloylmorpholine having a single reactive moiety at one end of the polymer chain have the following structure: ##STR1## wherein -Z-X-Y is a polymer capping moiety, such as mercaptan, X represents a saturated residue of a linear or branched aliphatic series of the general structure --C.sub.r H.sub.2r -- in which r is an integer from 1 to about 12, Y is a reactive moiety and typically will be one of the reactive moieties commonly known in PEG chemistry, such as an --OH, --COOH, or --NH.sub.2 group, Z is a moiety that readily reacts to cap a polymer free radical, and n is an integer from about 6 to 280, which yields a number average molecular weight ("M.sub.n ") of from about 1,000 to 40,000. The monofunctional polymer is a suitable alternative to monofunctional PEG for modification of substances having biological and biotechnical applications.
摘要翻译： 在聚合物链的一端具有单个反应性部分的单体N-丙烯酰基吗啉的聚合物具有以下结构：其中-ZXY是聚合物封端部分，例如硫醇，X表示直链或支链的饱和残基 一般结构-CrH 2 r-的脂族系列，其中r是1至约12的整数，Y是反应性部分，并且通常将是PEG化学中通常已知的反应性基团之一，例如-OH，-COOH， 或-NH 2基团，Z是易于与聚合物自由基反应的部分，n为约6至280的整数，其数均分子量（“Mn”）为约1,000至40,000。 单官能聚合物是用于修饰具有生物和生物技术应用的物质的单官能PEG的合适替代物。
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3.发明授权Chain-terminated N-vinyl lactam polymers and graft-copolymers and methods for making same 失效链末端N-乙烯基内酰胺聚合物和接枝共聚物及其制备方法
公开(公告)号：US5631336A
公开(公告)日：1997-05-20
申请号：US112077
申请日：1993-08-26
申请人： Paolo Ferruti , Elisabetta Ranucci , Luciana Sartore , Paolo Caliceti , Oddone Schiavon , Francesco M. Veronese
发明人： Paolo Ferruti , Elisabetta Ranucci , Luciana Sartore , Paolo Caliceti , Oddone Schiavon , Francesco M. Veronese
IPC分类号： A61K47/48 , C08F2/38 , C08F26/06 , C08F126/06 , C08F126/10
CPC分类号： C08F26/06 , A61K47/48176
摘要： A water-soluble polyvinyl 5-membered lactam having a molecular weight ranging from about 1000 to about 20,000 and chain-terminated with a compound selected from the group consisting of compounds of the following formulas ##STR1## wherein R and R.sup.1 are C.sub.1 to C.sub.4 alkyl or substituted alkyl; n is 0 to 20; R.sup.II is ethylene; R.sup.III is C.sub.1 to C.sub.24 alkylene or substituted alkylene; and R.sup.IV is C.sub.1 to C.sub.4 alkyl or substituted alkyl; can be prepared by polymerizing an N-vinyl 5-membered lactam in a liquid solvent-chain terminator compound of the formula (I) or (II) in the presence of a free radical initiator. The lactam polymer so-obtained may be activated and grafted to (conjugated with) a drug or an enzyme to alter the properties thereof.
摘要翻译： 分子量为约1000至约20,000的水溶性聚乙烯基5元内酰胺，并用选自下式的化合物（I）和（IMAGE）（II） ）其中R和R 1是C 1 -C 4烷基或取代的烷基; n为0〜20; RII是乙烯; RIII是C1至C24亚烷基或取代的亚烷基; 且RIV为C 1至C 4烷基或取代的烷基; 可以通过在自由基引发剂的存在下在式（I）或（II）的液体溶剂 - 终止剂化合物中聚合N-乙烯基5元内酰胺来制备。 如此获得的内酰胺聚合物可以被活化并接枝到药物或酶的（与其结合）以改变其性质。
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公开(公告)号：US07317002B2
公开(公告)日：2008-01-08
申请号：US11011617
申请日：2004-12-15
CPC分类号： A61K47/60
摘要： A method is described for the site-specific preparation of hGRF-PEG conjugates containing one or more PEG units (per mole of hGRF) covalently bound to Lys12 and/or Lys21 and/or Nα, characterized in that the conjugation reaction between the hGRF peptide and activated PEG is carried out in solution and the desired hGRF-PEG conjugate can be purified by chromatography. The conjugates prepared by this method, as well as their use in the treatment, prevention of diagnosis of growth hormone deficiency, are also an object of the present invention.
摘要翻译： 描述了用于特异性地制备含有共价结合到Lys 12和/或Lys 21的一个或多个PEG单元（每摩尔hGRF）的hGRF-PEG缀合物的位点特异性制备的方法 >和/或Nαα，其特征在于hGRF肽和活化的PEG之间的缀合反应在溶液中进行，并且所需的hGRF-PEG缀合物可以通过色谱法纯化。 通过该方法制备的缀合物及其在治疗中的用途，预防生长激素缺乏的诊断也是本发明的目的。
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公开(公告)号：US20050159353A1
公开(公告)日：2005-07-21
申请号：US11011617
申请日：2004-12-15
CPC分类号： A61K47/60
摘要： A method is described for the site-specific preparation of hGRF-PEG conjugates containing one or more PEG units (per mole of hGRF) covalently bound to Lys12 and/or Lys21 and/or Nα, characterized in that the conjugation reaction between the hGRF peptide and activated PEG is carried out in solution and the desired hGRF-PEG conjugate can be purified by chromatography. The conjugates prepared by this method, as well as their use in the treatment, prevention of diagnosis of growth hormone deficiency, are also an object of the present invention.
摘要翻译： 描述了用于特异性地制备含有共价结合到Lys 12和/或Lys 21的一个或多个PEG单元（每摩尔hGRF）的hGRF-PEG缀合物的位点特异性制备的方法 和/或Nα，其特征在于hGRF肽和活化的PEG之间的缀合反应在溶液中进行，并且可以通过色谱法纯化所需的hGRF-PEG缀合物。 通过该方法制备的缀合物及其在治疗中的用途，预防生长激素缺乏的诊断也是本发明的目的。
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公开(公告)号：US06869932B2
公开(公告)日：2005-03-22
申请号：US10299790
申请日：2002-11-20
IPC分类号： A61K8/00 , G01N33/566 , A61K38/04 , A61K47/48 , A61P5/06 , G01N33/74 , A61K38/25 , C07K17/08
CPC分类号： A61K47/60
摘要： A method is described for the site-specific preparation of hGRF-PEG conjugates containing one or more PEG units (per mole of hGRF) covalently bound to Lys12 and/or Lys21 and/or Nα, characterized in that the conjugation reaction between the hGRF peptide and activated PEG is carried out in solution and the desired hGRF-PEG conjugate can be purified by chromatography. The conjugates prepared by this method, as well as their use in the treatment, prevention or diagnosis of growth hormone deficiency, are also an object of the present invention.
摘要翻译： 描述了含有共价结合至Lys 12和/或Lys 21和/或Nalpha的一个或多个PEG单元（每摩尔hGRF）的hGRF-PEG缀合物的位点特异性制备的方法，其特征在于， hGRF肽和活化的PEG之间的缀合反应在溶液中进行，并且可以通过色谱法纯化所需的hGRF-PEG缀合物。 通过该方法制备的缀合物及其在治疗，预防或诊断生长激素缺乏中的用途也是本发明的目的。
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8.发明授权Method to maintain the activity in polyethylene glycol-modified proteolytic enzymes 失效保持聚乙二醇修饰蛋白水解酶活性的方法
公开(公告)号：US5514572A
公开(公告)日：1996-05-07
申请号：US256834
申请日：1994-09-19
IPC分类号： C12N9/64 , C12N9/72 , C12N9/76 , C12N9/96 , C12N9/46 , C12N9/48 , C12N9/66 , C12N9/68 , C12N9/70 , C12N9/74
CPC分类号： C12N9/6427 , A61K47/48215 , C07K1/1077 , C12N9/6456 , C12N9/96
摘要： A method for preparing protease-polyethylene glycol adducts is presented wherein the immobilized reversible inhibitor, benzamidine, prevents reaction of activated polyethylene glycol with the active site of the protease. Improved activity against macromolecular substrates is obtained compared to when the benzamidine is in solution during the conjugation reaction.
摘要翻译： PCT No.PCT / EP93 / 00205 Sec。 371日期1994年9月19日 102（e）1994年9月19日PCT 1993年1月29日PCT PCT。 公开号WO93 / 15189 日期：1993年8月5日。提出了一种制备蛋白酶 - 聚乙二醇加合物的方法，其中固定的可逆抑制剂苄脒防止活化的聚乙二醇与蛋白酶活性位点的反应。 与共轭反应期间苯甲脒在溶液中相比，获得了与大分子底物相反的活性。
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9.发明授权
公开(公告)号：US5932462A
公开(公告)日：1999-08-03
申请号：US443383
申请日：1995-05-17
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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10.发明授权Multi-armed, monofunctional, and hydrolytically stable derivatives of poly(ethylene glycol) and related polymers for modification of surfaces and molecules 失效聚（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：US08354477B2
公开(公告)日：2013-01-15
申请号：US12849683
申请日：2010-08-03
IPC分类号： C08G65/34 , C08F283/00
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。
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