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1.发明授权THIOESTER-TERMINATED WATER SOLUBLE POLYMERS AND METHOD OF MODIFYING THE N-TERMINUS OF A POLYPEPTIDE THEREWITH 有权水溶性聚合物硫酯末稍AND METHOD FOR改性的多肽的N-末端，以便
公开(公告)号：EP1434589B1
公开(公告)日：2008-12-10
申请号：EP02795502.0
申请日：2002-10-09
IPC分类号： A61K31/74 , C08G65/334
摘要： The invention provides reagents and methods for conjugating a polymer specifically to the ≡-amine of a polypeptide. The invention provides monofunctional, bifunctional, and multifunctional PEGs and related polymers having a terminal thioester moiety capable of specifically conjugating to the ≡-amine of a polypeptide having a cysteine or histidine residue at the N-terminus. The invention provides reactive thioester-terminated PEG polymers that have suitable reactivity with an N-terminal cysteine or histidine residue of a polypeptide to produce an amide bond between the PEG molecule and the polypeptide.
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公开(公告)号：EP1411075B1
公开(公告)日：2008-07-02
申请号：EP03028370.9
申请日：1999-03-11
IPC分类号： C08G65/333 , C08G65/329 , A61K47/48
CPC分类号： C08G65/33396 , A61K47/60 , C08G65/329 , C08G65/33313 , C08G65/33337 , Y10S530/816
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公开(公告)号：EP1885403A2
公开(公告)日：2008-02-13
申请号：EP06749809.7
申请日：2006-04-11
发明人： BOSSARD, Mary, J. , MITCHELL, Stacy
CPC分类号： A61K47/48215 , A61K38/00 , A61K47/60 , C12N9/52
摘要： Provided herein are water-soluble polymer conjugates and polymer-based compositions of antimicrobial agents. Also provided are methods for synthesizing and administering such conjugates and compositions.
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公开(公告)号：EP1861125A2
公开(公告)日：2007-12-05
申请号：EP06739738.0
申请日：2006-03-23
发明人： BOSSARD, Mary J. , ZHANG, Ping
摘要： Conjugates of an hGH moiety and one or more non-peptidic water soluble polymers are provided. Typically, the non-peptidic water soluble polymer is poly(ethylene glycol) or a derivative thereof. Also provided are compositions comprising such conjugates, methods of making the conjugates, and methods of administering compositions comprising such conjugates to a mammalian subject.
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5.发明公开
公开(公告)号：EP1756173A2
公开(公告)日：2007-02-28
申请号：EP05711695.6
申请日：2005-01-21
IPC分类号： C08F8/00
CPC分类号： C08F8/14 , C08G65/3322
摘要： The invention provides methods for preparing polymers bearing a terminal propionic acid. The method involves first reacting a water soluble and non-peptidic polymer comprising at least one hydroxyl group with a tertiary alkyl acrylate in the presence of a catalyst to form a propionic acid ester of the polymer, wherein the polymer has a weight average molecular weight of at least about 10,000 Da; and then treating the propionic acid ester of the polymer with a strong acid to form a propionic acid of the polymer.
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公开(公告)号：EP1692206A1
公开(公告)日：2006-08-23
申请号：EP04810369.1
申请日：2004-11-05
IPC分类号： C08G65/332
CPC分类号： C08G63/91 , A61K31/765 , C08F251/00 , C08F261/04 , C08F265/00 , C08F271/00 , C08F283/06 , C08F289/00 , C08F291/00 , C08G65/30 , C08G65/332 , C08G65/3322 , C08G65/3346
摘要： Methods for preparing water soluble, non-peptidic polymers carrying carboxyl functional groups, particularly carboxylic acid functionalized poly(ethylene glycol) (PEG) polymers, are disclosed, as are the products of these methods. In general, an ester reagent R(C=O)OR', where R' is a tertiary group and R comprises a functional group X, is reacted with a water soluble, non-peptidic polymer POLY-Y, where Y is a functional group which reacts with X to form a covalent bond, to form a tertiary ester of the polymer, which is then treated with a strong base in aqueous solution, to form a carboxylate salt of the polymer. Typically, this carboxylate salt is then treated with an inorganic acid in aqueous solution, to convert the carboxylate salt to a carboxylic acid, thereby forming a carboxylic acid functionalized polymer.
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公开(公告)号：EP1476489A1
公开(公告)日：2004-11-17
申请号：EP03709198.0
申请日：2003-02-14
发明人： BENTLEY, Michael, D. , HARRIS, J., Milton , ZHAO, Xuan , BATTLE, William, Dudley, III , SHEN, Xiaoming
CPC分类号： C08G65/04 , A61K9/00 , A61K9/06 , A61K47/34 , C08G64/183 , C08G65/329 , C08G65/333 , C08G65/33337 , C08G65/33344 , C08G65/33396 , C08L2203/02
摘要： The present invention provides a water soluble, nonpeptidic polymer comprising two or more alkylene oxide-based oligomers linked together by hydrolytically degradable linkages such as carbonates. Typically, the oligomer portion of the polymer is an amphiphilic triblock copolymer having a central propylene oxide block or butylene oxide block positioned between two ethylene oxide blocks. The polymer can be hydrolytically degraded into oligomers under physiological conditions. In aqueous media, the polymer preferably forms thermally reversible, hydrolytically degradable hydrogels that can be used, for example, for drug delivery and related biomedical applications.
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公开(公告)号：EP1441772A2
公开(公告)日：2004-08-04
申请号：EP02776357.2
申请日：2002-10-29
IPC分类号： A61K47/48
CPC分类号： A61K47/60
摘要： The invention provides polymer conjugates of protein kinase C (PKC) inhibitors comprising a polymer, such as poly(ethylene glycol), covalently attached to a PKC inhibitor, such as a bisindolylmaleimide molecule. The linkage between the polymer and the PKC inhibitor is preferably hydrolytically degradable. The invention also includes a pharmaceutical composition comprising a polymer conjugate of a PKC inhibitor and a method of treating any condition responsive to a PKC inhibitor by administering a polymer conjugate of the invention.
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9.发明公开THIOESTER-TERMINATED WATER SOLUBLE POLYMERS AND METHOD OF MODIFYING THE N-TERMINUS OF A POLYPEPTIDE THEREWITH 有权水溶性聚合物硫酯末稍AND METHOD FOR改性的多肽的N-末端，以便
公开(公告)号：EP1434589A2
公开(公告)日：2004-07-07
申请号：EP02795502.0
申请日：2002-10-09
IPC分类号： A61K31/74
摘要： The invention provides reagents and methods for conjugating a polymer specifically to the ≡-amine of a polypeptide. The invention provides monofunctional, bifunctional, and multifunctional PEGs and related polymers having a terminal thioester moiety capable of specifically conjugating to the ≡-amine of a polypeptide having a cysteine or histidine residue at the N-terminus. The invention provides reactive thioester-terminated PEG polymers that have suitable reactivity with an N-terminal cysteine or histidine residue of a polypeptide to produce an amide bond between the PEG molecule and the polypeptide.
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公开(公告)号：EP1355671A2
公开(公告)日：2003-10-29
申请号：EP01998208.1
申请日：2001-11-30
IPC分类号： A61K47/48
CPC分类号： A61K47/60
摘要： The present invention provides water-soluble polymer conjugates of triazine derivatives using water soluble and non-peptidic polymer backbones, such as polyethylene glycol). The invention includes conjugates made using mPEG, bifunctional PEG, branched or multi-arm PEG, and forked PEG. The invention further includes a method of forming such conjugates and a method of treating conditions responsive to triazine derivatives using the conjugates.
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