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1.发明公开NUCLEOPHILIC CATALYSTS FOR OXIME LINKAGE AND USE OF NMR ANALYSES OF THE SAME 审中-公开亲核催化剂结合和使用肟的NMR分析可知：
公开(公告)号：EP2849794A1
公开(公告)日：2015-03-25
申请号：EP13724491.9
申请日：2013-05-16
发明人： RAY, G., Joseph , ZHANG, Zhenqing , SZABO, Christina , SIEKMANN, Juergen , SCHEINECKER, Richard , HAIDER, Stefan , ROTTENSTEINER, Hanspeter , KOSMA, Paul
IPC分类号： A61K47/48
摘要： The invention relates to materials and methods of conjugating a water soluble polymer to an oxidized carbohydrate moiety of a therapeutic protein comprising contacting the oxidized carbohydrate moiety with an activated water soluble polymer under conditions that allow conjugation and analyzing the conjugation using 2D NMR analysis. More specifically, the present invention relates to the aforementioned materials and methods wherein the water soluble polymer contains an active aminooxy group and wherein an oxime or hydrazone linkage is formed between the oxidized carbohydrate moiety and the active aminooxy group on the water soluble polymer, and wherein the conjugation is carried out in the presence of a nucleophilic catalyst.
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2.发明公开MATERIALS AND METHODS FOR CONJUGATING A WATER SOLUBLE FATTY ACID DERIVATIVE TO A PROTEIN 审中-公开材料和方法水溶性脂肪酸衍生物的蛋白质的共轭
公开(公告)号：EP2654794A1
公开(公告)日：2013-10-30
申请号：EP11806103.5
申请日：2011-12-16
摘要： The invention relates to materials and methods of conjugating a water soluble fatty acid derivative to a therapeutic protein comprising contacting the therapeutic protein with an activated water soluble fatty acid derivative under conditions that allow conjugation.
摘要翻译： 本发明涉及的材料和缀合的水溶性脂肪酸衍生物对治疗性蛋白，其包含与在活化的水溶性脂肪酸衍生物接触所述治疗性蛋白质的条件下确实允许缀合的方法。
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公开(公告)号：EP2459224A2
公开(公告)日：2012-06-06
申请号：EP10738119.6
申请日：2010-07-26
IPC分类号： A61K47/48
CPC分类号： A61K47/4823 , A61K38/37 , A61K38/4846 , A61K47/60 , A61K47/61 , C08B37/0006 , C12N9/6437 , C12N9/644 , C12N9/96 , C12Y304/21021 , C12Y304/21022
摘要： The invention relates to materials and methods of conjugating a water soluble polymer to an oxidized carbohydrate moiety of a blood coagulation protein comprising contacting the oxidized carbohydrate moiety with an activated water soluble polymer under conditions that allow conjugation. More specifically, the present invention relates to the aforementioned materials and methods wherein the water soluble polymer contains an active aminooxy group and wherein an oxime linkage is formed between the oxidized carbohydrate moiety and the active aminooxy group on the water soluble polymer. In one embodiment of the invention the conjugation is carried out in the presence of the nucleophilic catalyst aniline. In addition the generated oxime linkage can be stabilized by reduction with NaCNBH
3 to form an alkoxyamine linkage.摘要翻译： 本发明涉及使水溶性聚合物与血液凝固蛋白的氧化碳水化合物部分缀合的材料和方法，包括使氧化碳水化合物部分与活化的水溶性聚合物在允许缀合的条件下接触。 更具体地说，本发明涉及上述材料和方法，其中水溶性聚合物含有活性氨氧基，并且其中在水溶性聚合物上的氧化碳水化合物部分和活性氨氧基之间形成肟键。 在本发明的一个实施方案中，缀合在亲核催化剂苯胺存在下进行。 另外，生成的肟键可以通过用NaCNBH 3还原形成烷氧基胺键来稳定。
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公开(公告)号：EP1835938A2
公开(公告)日：2007-09-26
申请号：EP05855442.9
申请日：2005-12-23
IPC分类号： A61K47/48
CPC分类号： C07K14/755 , A61K47/60 , C07K14/775
摘要： The present invention relates to a proteinaceous construc (also designated as polymer-VWF-conjugate) comprising plasmatic and/or recombinant von Willebrand factor (VWF), said VWF being bound to at least one physiologically acceptable polymer molecule, as well as to a complex said proteinaceous construc and at least one factor VIII (FVIII) protein. The physiologically acceptable polymer molecule can be, for instance, polyethylene glycol (PEG) or polysialic acid (PSA). Further the present invention relates to methods for prolonging the in vivo-half-life of VWF or FVIII in the blood of a mammal having a bleeding disorder associated with functional defects of or deficiencies of at least one of FVIII or VWF.
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公开(公告)号：EP2318050B1
公开(公告)日：2014-09-03
申请号：EP09790935.2
申请日：2009-07-29
发明人： TURECEK, Peter , SIEKMANN, Juergen
IPC分类号： A61K47/48 , C07K14/745
CPC分类号： A61K38/37 , A61K38/00 , A61K47/60 , A61K47/61 , C07K14/745
摘要： A composition comprising a conjugate comprising a native Factor VIII modified with a water soluble polymer bound thereto, said water soluble polymer attached to the modified Factor VIII via an oxidised carbohydrate moiety.
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公开(公告)号：EP2459226A2
公开(公告)日：2012-06-06
申请号：EP10739386.0
申请日：2010-07-26
发明人： JAIN, Sanjay , GREGORIADIS, Gregory , DWIVEDI, Archana , NATH, Srijit , SIEKMANN, Juergen , HAIDER, Stefan , ROTTENSTEINER, Hanspeter , TURECEK, Peter
IPC分类号： A61K47/48
CPC分类号： A61K47/6455 , A61K47/60 , A61K47/61 , A61K47/65
摘要： A water soluble polymer, in particular polysialic acid (PSA) or a modified PSA (mPSA), is conjugated to an oxidized carbohydrate moiety of a glycoprotein other than a blood coagulation protein or to a ganglioside or drug delivery system by contacting the oxidized carbohydrate moiety with the water soluble polymer, wherein said water soluble polymer contains an aminooxy group and an oxime linkage is formed between the oxidized carbohydrate moiety and the aminooxy group on the water soluble polymer or wherein said water soluble polymer contains a hydrazide group and a hydrazone linkage is formed between the oxidized carbohydrate moiety and the hydrazide group on the water soluble polymer. Conjugates of aminooxy- or hydrazide-water soluble polymer, such as PSA and mPSA, are thus obtained in which the PSA or mPSA is attached via a carbohydrate moiety.
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7.发明公开METHODS OF DETERMINING POLYDISPERSITY AND/OR MOLECULAR WEIGHT DISTRIBUTION OF A POLYETHYLENE GLYCOL SAMPLE 审中-公开法确定多分散性和/或聚乙二醇探头的分子量分布
公开(公告)号：EP2366105A1
公开(公告)日：2011-09-21
申请号：EP09760672.7
申请日：2009-11-18
发明人： KEMPTNER, Jasmin , MARCHETTI-DESCHMANN, Martina , SIEKMANN, Juergen , TURECEK, Peter , SCHWARZ, Hans-Peter , ALLMAIER, Guenter
IPC分类号： G01N33/68
CPC分类号： G01N27/624
摘要： Disclosed herein are methods of determining polydispersity (PDI) and molecular mass distribution (MMD) of reactive PEG samples using mass spectrometry. More specifically, a mass spectrometry method called GEMMA is used to determine PDI and MMD of PEG samples which provides more accurate measurements for high molecular weight PEG samples than prior known MALDI-TOF analysis.
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8.发明授权DETECTION OF PHYSIOLOGICALLY ACCEPTABLE POLYMER MOLECULES USING NEAR INFRARED SPECTROSCOPY 有权PROOF生理安全聚合物分子使用近红外光谱仪
公开(公告)号：EP2356467B1
公开(公告)日：2013-07-10
申请号：EP09768592.9
申请日：2009-12-11
IPC分类号： G01N33/86 , G01N33/68 , G01N21/00 , G01N33/487
CPC分类号： G01N33/6842 , G01N21/359 , G01N33/86 , G01N2333/745 , G01N2333/755 , G01N2333/76 , Y10T436/203332
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公开(公告)号：EP2598172A1
公开(公告)日：2013-06-05
申请号：EP11741727.9
申请日：2011-07-29
发明人： SIEKMANN, Juergen , HAIDER, Stefan , ROTTENSTEINER, Hanspeter , IVENS, Andreas , TURECEK, Peter , ZOECHLING, Oliver
IPC分类号： A61K47/48
摘要： The invention relates to materials and methods of conjugating a water soluble polymer to an oxidized carbohydrate moiety of a therapeutic protein comprising contacting the oxidized carbohydrate moiety with an activated water soluble polymer under conditions that allow conjugation. More specifically, the present invention relates to the aforementioned materials and methods wherein the water soluble polymer contains an active aminooxy group and wherein an oxime or hydrazone linkage is formed between the oxidized carbohydrate moiety and the active aminooxy group on the water soluble polymer, and wherein the conjugation is carried out in the presence of a nucleophilic catalyst.
摘要翻译： 本发明涉及将水溶性聚合物与治疗性蛋白质的氧化碳水化合物部分缀合的材料和方法，包括在允许缀合的条件下使氧化的碳水化合物部分与活化的水溶性聚合物接触。 更具体地说，本发明涉及上述材料和方法，其中水溶性聚合物含有活性氨基氧基，其中在水溶性聚合物上的氧化碳水化合物部分和活性氨基氧基之间形成肟或腙键，其中 共轭在亲核催化剂存在下进行。
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10.发明公开DETECTION OF ANTIBODY THAT BINDS TO WATER SOLUBLE POLYMER-MODIFIED POLYPEPTIDES 审中-公开AN水可溶聚合物证明修饰多肽结合抗体
公开(公告)号：EP2435833A1
公开(公告)日：2012-04-04
申请号：EP10727212.2
申请日：2010-05-25
发明人： LUBICH, Christian , SIEKMANN, Juergen , REIPERT, Birgit, Maria , SCHWARZ, Hans-Peter , EHRLICH, Hartmut
IPC分类号： G01N33/68
CPC分类号： G01N33/6854
摘要： The present invention provides analytical methods for detecting anti- polymer antibody in an individual. The methods involve contacting a sample from the individual with a water soluble polymer-modified carrier and detecting binding of antibody to the water soluble polymer on the water soluble polymer-modified carrier wherein binding is indicative of the presence of antibody to the water polymer-modified polypeptide. Antibody may be detected to water soluble polymers such as polyethylene glycol, polysialic acid, dextran, hydroxyalkyl starch, or hydroxyethyl starch. When antibody to the water soluble polymer polyethylene glycol is to be detected, the carrier is modified with a non-linear polyethylene glycol derivative.
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