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1.发明公开VON WILLEBRAND FACTOR- AND FACTOR VIII-POLYMER CONJUGATES HAVING A RELEASABLE LINKAGE 有权血管性血友病因子和因子VIII WITH聚合物缀合物可分离的连接
公开(公告)号：EP2114458A2
公开(公告)日：2009-11-11
申请号：EP07868153.3
申请日：2007-12-27
发明人： BOSSARD, Mary, J. , STEPHENSON, Gayle , FANG, Zhihao , ZAPPE, Harold , MITCHELL, Stacy , ZHANG, Ping , SCHEIFLINGER, Friedrich , TURECEK, Peter , SIEKMANN, Juergen , VARADI, Katalin , GRITSCH, Herbert
CPC分类号： C07K14/755 , A61K47/60
摘要： The present invention provides von Willebrand Factor-polymer conjugates and Factor VIII-polymer conjugates, each having a releasable linkage. Methods of making conjugates, methods for administering conjugates, are also provided.
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2.发明授权VON WILLEBRAND FACTOR- AND FACTOR VIII-POLYMER CONJUGATES HAVING A RELEASABLE LINKAGE 有权血管性血友病因子和因子VIII WITH聚合物缀合物可分离的连接
公开(公告)号：EP2114458B1
公开(公告)日：2014-02-26
申请号：EP07868153.3
申请日：2007-12-27
发明人： BOSSARD, Mary, J. , STEPHENSON, Gayle , FANG, Zhihao , ZAPPE, Harold , MITCHELL, Stacy , ZHANG, Ping , SCHEIFLINGER, Friedrich , TURECEK, Peter , SIEKMANN, Juergen , VARADI, Katalin , GRITSCH, Herbert
IPC分类号： A61K47/48 , A61P7/00 , C07K14/755
CPC分类号： C07K14/755 , A61K47/60
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3.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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4.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：EP1345982A2
公开(公告)日：2003-09-24
申请号：EP01994295.2
申请日：2001-12-18
IPC分类号： C08G65/329
CPC分类号： C08G65/329 , A61K47/56
摘要： High molecular weight derivatives of activated poly(ethylene glycol) and the like polymers are prepared in high purity by conjugating a large PEG molecule to a small PEG molecule. Most of the reaction steps can be accomplished on the more readily purified small molecule to avoid laborious purification of the high molecular weight derivatives.
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公开(公告)号：EP1345982B1
公开(公告)日：2007-04-25
申请号：EP01994295.2
申请日：2001-12-18
IPC分类号： C08G65/329
CPC分类号： C08G65/329 , A61K47/56
摘要： High molecular weight derivatives of activated poly(ethylene glycol) and the like polymers are prepared in high purity by conjugating a large PEG molecule to a small PEG molecule. Most of the reaction steps can be accomplished on the more readily purified small molecule to avoid laborious purification of the high molecular weight derivatives.
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7.发明公开METHODS FOR THE FORMATION OF HYDROGELS USING THIOSULFONATE COMPOSITIONS AND USES THEREOF 有权用于生产水凝胶OFF硫代组合物及其用途
公开(公告)号：EP1578843A1
公开(公告)日：2005-09-28
申请号：EP03800398.4
申请日：2003-12-31
发明人： BENTLEY, Michael, D. , FANG, Zhihao
IPC分类号： C08G65/334 , C08G65/329 , A61L26/00 , A61L15/00 , A61K47/48
CPC分类号： C08G65/3342 , A61K47/60 , A61L24/0031 , A61L24/046 , C08G65/329 , C08J3/24 , C08J2300/14 , C08J2381/00 , C08L2203/02 , C08L81/08
摘要： The present invention provides both crosslinked polymer compositions capable of forming hydrogels upon exposure to an aqueous environment and thiosulfonate hydrogel-forming components. The thiosulfonate hydrogel-forming components of the invention are preferably multi-arm thiosulfonate polymer derivatives that form a crosslinked polymer composition when exposed to a base without requiring the presence of a second cross-linking reagent, redox catalyst, or radiation. Methods for forming hydrogel compositions, as well as methods for using the hydrogels, are also provided.
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公开(公告)号：EP1968644A2
公开(公告)日：2008-09-17
申请号：EP06847728.0
申请日：2006-12-18
IPC分类号： A61K47/48 , C07C323/12 , C07D213/70 , C07K14/605 , A61P3/10
CPC分类号： C07K17/08 , A61K47/60 , C07K14/605
摘要： Conjugates of a GLP-I moiety may be covalently attached to one or more water-soluble polymers. For instance, a GLP-I polymer conjugate may include a GLP-I moiety releasably attached at its N-terminus to a water-soluble polymer. The GLP-I polymer conjugate may include a GLP-I moiety covalently attached to a water-soluble polymer, wherein the GLP-I moiety possesses an N-methyl substituent. The GLP-I polymer conjugate may include a GLP-I moiety covalently attached at a polymer attachment site to a water-soluble polymer, wherein the GLP-I moiety is glycosylated at a site separate from the polymer attachment site.
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9.发明授权METHODS FOR THE FORMATION OF HYDROGELS USING THIOSULFONATE COMPOSITIONS AND USES THEREOF 有权用于生产水凝胶OFF硫代组合物及其用途
公开(公告)号：EP1578843B1
公开(公告)日：2008-07-09
申请号：EP03800398.4
申请日：2003-12-31
发明人： BENTLEY, Michael, D. , FANG, Zhihao
IPC分类号： C08G65/334 , C08G65/329 , A61L26/00 , A61L15/00 , A61K47/48
CPC分类号： C08G65/3342 , A61K47/60 , A61L24/0031 , A61L24/046 , C08G65/329 , C08J3/24 , C08J2300/14 , C08J2381/00 , C08L2203/02 , C08L81/08
摘要： The present invention provides both crosslinked polymer compositions capable of forming hydrogels upon exposure to an aqueous environment and thiosulfonate hydrogel-forming components. The thiosulfonate hydrogel-forming components of the invention are preferably multi-arm thiosulfonate polymer derivatives that form a crosslinked polymer composition when exposed to a base without requiring the presence of a second cross-linking reagent, redox catalyst, or radiation. Methods for forming hydrogel compositions, as well as methods for using the hydrogels, are also provided.
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10.发明公开METHODS FOR DETERMINING ACTIVE INGREDIENTS IN PRO-DRUG PEG PROTEIN CONJUGATES WITH RELEASABLE PEG REAGENTS (IN VITRO DE-PEGYLATION) 审中-公开用于确定活性成分药物同可释放PEG试剂前体的PEG蛋白质结合物（体外DEPEGYLIERUNG）方法
公开(公告)号：EP2350658A2
公开(公告)日：2011-08-03
申请号：EP09752561.2
申请日：2009-10-20
发明人： VARADI, Katalin , SCHRENK, Gerald , ROTTENSTEINER, Hanspeter , TURECEK, Peter , WEBER, Alfred , ANDERLE, Heinz , CULBERTSON, Sean, M. , FANG, Zhihao , ZAPPE, Harold , ZHANG, Ping , BOSSARD, Mary, J.
IPC分类号： G01N33/542 , G01N33/58 , G01N33/68 , G01N33/86
CPC分类号： G01N33/68 , G01N33/542 , G01N33/582 , G01N33/86 , G01N2333/76
摘要： The invention relates to the development of in vitro assay systems that force the release of a water-soluble polymer, such as polyethylene glycol (PEG) and polysialic acid (PSA), from proteins modified with a reversibly-linked water-soluble polymer. The invention includes methods for analyzing the release of the water- soluble polymer and measuring regained protein activity. The invention further includes methods appropriate for the quality control of proteins modified with releasable water-soluble polymers, including polymers like PEG and PSA.
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