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公开(公告)号：US08653255B2
公开(公告)日：2014-02-18
申请号：US12897523
申请日：2010-10-04
申请人： Sanjay Jain , Peter Laing , Gregory Gregoriadis , Dale Howard Hreczuk-Hirst , Ioannis Papaioannou
发明人： Sanjay Jain , Peter Laing , Gregory Gregoriadis , Dale Howard Hreczuk-Hirst , Ioannis Papaioannou
IPC分类号： A61K31/702 , A61K31/726 , C07H5/06
CPC分类号： A61K47/4823 , A61K31/702 , A61K31/726 , A61K38/27 , A61K38/28 , A61K39/44 , A61K47/61 , A61K47/6807 , C07H3/06 , C07H5/06 , C07H15/04 , C07K17/12 , C08B37/00 , C08B37/0006 , C08B37/006 , C08B37/0063
摘要： Derivatives are synthesized of starting materials, usually polysaccharides, having sialic acid at the reducing terminal end, in which the reducing terminal unit is transformed into an aldehyde group. Where the polysaccharide has a sialic acid unit at the non-reducing end it may be passivated, for instance by converting into hydroxyl-substituted moiety. The derivatives may be reacted with substrates, for instance containing amine or hydrazine groups, to form non-cross-linked polysialylated compounds. The substrates may, for instance, be therapeutically useful drugs peptides or proteins or drug delivery systems.
摘要翻译： 衍生物由还原性末端具有唾液酸的原料（通常为多糖）合成，其中还原末端单元转化为醛基。 当多糖在非还原末端具有唾液酸单元时，其可以被钝化，例如通过转化成羟基取代的部分。 衍生物可以与底物反应，例如含有胺或肼基团，以形成非交联的聚唾液酸化化合物。 底物可以例如是治疗上有用的药物肽或蛋白质或药物递送系统。
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公开(公告)号：US07807824B2
公开(公告)日：2010-10-05
申请号：US10568043
申请日：2004-08-12
申请人： Sanjay Jain , Peter Laing , Gregory Gregoriadis , Dale Howard Hreczuk-Hirst , Ioannis Papaioannou
发明人： Sanjay Jain , Peter Laing , Gregory Gregoriadis , Dale Howard Hreczuk-Hirst , Ioannis Papaioannou
IPC分类号： A61K31/715 , C07H1/00 , C08B37/00 , C12P19/04
CPC分类号： A61K47/4823 , A61K31/702 , A61K31/726 , A61K38/27 , A61K38/28 , A61K39/44 , A61K47/61 , A61K47/6807 , C07H3/06 , C07H5/06 , C07H15/04 , C07K17/12 , C08B37/00 , C08B37/0006 , C08B37/006 , C08B37/0063
摘要： Derivatives are synthesised of starting materials, usually polysaccharides, having sialic acid at the reducing terminal end, in which the reducing terminal unit is transformed into an aldehyde group. Where the polysaccharide has a sialic acid unit at the non-reducing end it may be passivated, for instance by converting into hydroxyl-substituted moiety. The derivatives may be reacted with substrates, for instance containing amine or hydrazine groups, to form non-cross-linked polysialylated compounds. The substrates may, for instance, be therapeutically useful drugs peptides or proteins or drug delivery systems.
摘要翻译： 衍生物由还原性末端具有唾液酸的原料（通常为多糖）合成，其中还原末端单元转化为醛基。 当多糖在非还原末端具有唾液酸单元时，其可以被钝化，例如通过转化成羟基取代的部分。 衍生物可以与底物反应，例如含有胺或肼基团，以形成非交联的聚唾液酸化化合物。 底物可以例如是治疗上有用的药物肽或蛋白质或药物递送系统。
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公开(公告)号：US20100221808A1
公开(公告)日：2010-09-02
申请号：US12717073
申请日：2010-03-03
申请人： Dale Howard Hreczuk-Hirst , Sanjay Jain , Peter Laing , Gregory Gregoriadis , Ioannis Papaioannou
发明人： Dale Howard Hreczuk-Hirst , Sanjay Jain , Peter Laing , Gregory Gregoriadis , Ioannis Papaioannou
CPC分类号： C08B37/0006 , A61K31/715 , A61K47/61 , A61K47/68 , C07K1/006 , C07K1/1077 , C07K1/13 , C07K14/001 , C07K17/10 , C08B37/00 , C12N9/96
摘要： A polysialic acid compound is reacted with a hetero-bifunctional reagent to introduce a pendant functional group for site-specific conjugation to sulfhydryl groups, for instance side chains of cysteine units in drugs, drug delivery systems, proteins or peptides. The functional group is, for instance, an N-maleimide group.
摘要翻译： 将多唾液酸化合物与异双功能试剂反应以引入用于位点特异性缀合的侧链官能团，例如巯基，例如药物，药物递送系统，蛋白质或肽中半胱氨酸单元的侧链。 官能团是例如N-马来酰亚胺基团。
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公开(公告)号：US07691826B2
公开(公告)日：2010-04-06
申请号：US10568111
申请日：2004-08-12
申请人： Dale Howard Hreczuk-Hirst , Sanjay Jain , Peter Laing , Gregory Gregoriadis , Ioannis Papaioannou
发明人： Dale Howard Hreczuk-Hirst , Sanjay Jain , Peter Laing , Gregory Gregoriadis , Ioannis Papaioannou
IPC分类号： A61K31/7008 , A61K31/7012 , A61K31/7028 , A61K31/7056 , A61K31/715
CPC分类号： C08B37/0006 , A61K31/715 , A61K47/61 , A61K47/68 , C07K1/006 , C07K1/1077 , C07K1/13 , C07K14/001 , C07K17/10 , C08B37/00 , C12N9/96
摘要： A polysialic acid compound is reacted with a hetero-bifunctional reagent to introduce a pendant functional group for site-specific conjugation to sulfhydryl groups, for instance side chains of cysteine units in drugs, drug delivery systems, proteins or peptides. The functional group is, for instance, an N-maleimide group.
摘要翻译： 将多唾液酸化合物与异双功能试剂反应以引入用于位点特异性缀合的侧链官能团，例如巯基，例如药物，药物递送系统，蛋白质或肽中半胱氨酸单元的侧链。 官能团是例如N-马来酰亚胺基团。
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公开(公告)号：US20070191597A1
公开(公告)日：2007-08-16
申请号：US10568043
申请日：2004-08-12
IPC分类号： C07H15/00
CPC分类号： A61K47/4823 , A61K31/702 , A61K31/726 , A61K38/27 , A61K38/28 , A61K39/44 , A61K47/61 , A61K47/6807 , C07H3/06 , C07H5/06 , C07H15/04 , C07K17/12 , C08B37/00 , C08B37/0006 , C08B37/006 , C08B37/0063
摘要： Derivatives are synthesised of starting materials, usually polysaccharides, having sialic acid at the reducing terminal end, in which the reducing terminal unit is transformed into an aldehyde group. Where the polysaccharide has a sialic acid unit at the non-reducing end it may be passivated, for instance by converting into hydroxyl-substituted moiety. The derivatives may be reacted with substrates, for instance containing amine or hydrazine groups, to form non-cross-linked polysialylated compounds. The substrates may, for instance, be therapeutically useful drugs peptides or proteins or drug delivery systems.
摘要翻译： 衍生物由还原性末端具有唾液酸的原料（通常为多糖）合成，其中还原末端单元转化为醛基。 当多糖在非还原末端具有唾液酸单元时，其可以被钝化，例如通过转化成羟基取代的部分。 衍生物可以与底物反应，例如含有胺或肼基团，以形成非交联的聚唾液酸化化合物。 底物可以例如是治疗上有用的药物肽或蛋白质或药物递送系统。
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公开(公告)号：US20080132696A1
公开(公告)日：2008-06-05
申请号：US11660133
申请日：2005-08-12
申请人： Sanjay Jain , Ioannis Papaioannou , Peter Laing
发明人： Sanjay Jain , Ioannis Papaioannou , Peter Laing
IPC分类号： C08B37/00
CPC分类号： C08B37/0006 , A61K47/61 , B01D15/361 , B01D15/362 , B01D15/363 , B01D15/424 , B01D15/426 , C07K1/18 , C07K14/61 , C08B37/0003
摘要： Polydisperse and charged polysaccharides are fractionated into low polydispersity fractions (preferably having pd
摘要翻译： 多分散和带电多糖被分级成低分散度级分（优选具有pd <1.1），每个分子含有窄范围分子量范围内的物质。 将多分散多糖的水溶液与柱中的离子交换树脂接触，并通过水洗脱缓冲液对多糖进行选择性洗脱。 选择性洗脱由具有不同和恒定离子强度和/或pH值的至少3个顺序洗脱缓冲液组成，其中随后的缓冲液具有比前述步骤的离子强度和/或pH高的离子强度和/或pH。 新制剂特别适用于生产用于人和动物的PSA衍生化治疗剂。
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公开(公告)号：US08652334B2
公开(公告)日：2014-02-18
申请号：US11660133
申请日：2005-08-12
申请人： Sanjay Jain , Ioannis Papaioannou , Peter Laing
发明人： Sanjay Jain , Ioannis Papaioannou , Peter Laing
CPC分类号： C08B37/0006 , A61K47/61 , B01D15/361 , B01D15/362 , B01D15/363 , B01D15/424 , B01D15/426 , C07K1/18 , C07K14/61 , C08B37/0003
摘要： Polydisperse and charged polysaccharides are fractionated into low polydispersity fractions (preferably having pd
摘要翻译： 多分散和带电多糖被分级成低分散度级分（优选具有pd <1.1），每个分子含有窄范围分子量范围内的物质。 将多分散多糖的水溶液与柱中的离子交换树脂接触，并通过水洗脱缓冲液对多糖进行选择性洗脱。 选择性洗脱由具有不同和恒定离子强度和/或pH值的至少3个顺序洗脱缓冲液组成，其中随后的缓冲液具有比前述步骤的离子强度和/或pH高的离子强度和/或pH。 新制剂特别适用于生产用于人和动物的PSA衍生化治疗剂。
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公开(公告)号：US20110159130A1
公开(公告)日：2011-06-30
申请号：US12528763
申请日：2008-02-28
申请人： Sanjay Jain , Peter Laing , Gregory Gregoriadis
发明人： Sanjay Jain , Peter Laing , Gregory Gregoriadis
CPC分类号： C08B37/0006 , B01D15/363 , C08B37/0003
摘要： The present invention relates to process for reducing the endotoxin content of a sample of fermentation broth containing polysialic acid and endotoxin comprising the sequential steps: (i) adding to the sample a base having a pKa of at least 12 to form a basic solution having a pH of at least 12, incubating the solution for a pre-determined time at a pre-determined temperature; and (ii) recovery of PSA, suitably by (iii) passing the sample through an anion-exchange column whereby polysialic acid is absorbed on the ion exchange resin; (iv) washing the column with one washing buffer, whereby polysialic acid remains absorbed on the ion exchange resin; and (v) eluting the polysialic acid from the column using an elution buffer to provide a product solution of polysialic acid having reduced endotoxin content.
摘要翻译： 本发明涉及降低含有唾液酸和内毒素的发酵肉汤样品的内毒素含量的方法，其包括以下顺序步骤：（i）向样品中加入pKa至少为12的碱，以形成具有 pH至少为12，在预定温度下将溶液温育预定时间; 和（ii）PSA的回收，适当地通过（iii）使样品通过阴离子交换柱，由此唾液酸被吸收在离子交换树脂上; （iv）用一个洗涤缓冲液洗涤该柱，由此聚唾液酸保持吸收在离子交换树脂上; 和（v）使用洗脱缓冲液从柱洗脱聚唾液酸以提供具有降低的内毒素含量的聚唾液酸的产物溶液。
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公开(公告)号：US08299026B2
公开(公告)日：2012-10-30
申请号：US12375008
申请日：2007-07-25
CPC分类号： A61K47/61 , A61K38/00 , A61K38/1816 , A61K38/193 , A61K38/465 , C07K14/505 , C07K14/52 , C07K14/535 , C07K14/575 , C12N9/22 , C12Y301/21001 , Y02A50/473
摘要： The present invention relates to a compound which is a polysaccharide derivative of EPO, or of an EPO like protein, wherein the polysaccharide is anionic and comprises between 2 and 200 saccharide units. The present invention also relates to pharmaceutical compositions comprising the novel compounds, and methods for making the novel compounds.
摘要翻译： 本发明涉及作为EPO的多糖衍生物或EPO样蛋白质的化合物，其中所述多糖是阴离子型的，并且包含2至200个糖单元。 本发明还涉及包含新化合物的药物组合物和制备新化合物的方法。
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公开(公告)号：US09212232B2
公开(公告)日：2015-12-15
申请号：US13557149
申请日：2012-07-24
申请人： Sanjay Jain , Peter Laing , Gregory Gregoriadis
发明人： Sanjay Jain , Peter Laing , Gregory Gregoriadis
CPC分类号： C08B37/0006 , B01D15/363 , C08B37/0003
摘要： The present invention relates to process for reducing the endotoxin content of a sample of fermentation broth containing polysialic acid and endotoxin comprising the sequential steps: (i) adding to the sample a base having a pKa of at least 12 to form a basic solution having a pH of at least 12, incubating the solution for a pre-determined time at a pre-determined temperature; and (ii) recovery of PSA, suitably by (iii) passing the sample through an anion-exchange column whereby polysialic acid is absorbed on the ion exchange resin; (iv) washing the column with one washing buffer, whereby polysialic acid remains absorbed on the ion exchange resin; and (v) eluting the polysialic acid from the column using an elution buffer to provide a product solution of polysialic acid having reduced endotoxin content.
摘要翻译： 本发明涉及降低含有唾液酸和内毒素的发酵肉汤样品的内毒素含量的方法，其包括以下顺序步骤：（i）向样品中加入pKa至少为12的碱，以形成具有 pH至少为12，在预定温度下将溶液温育预定时间; 和（ii）PSA的回收，适当地通过（iii）使样品通过阴离子交换柱，由此唾液酸被吸收在离子交换树脂上; （iv）用一个洗涤缓冲液洗涤该柱，由此聚唾液酸保持吸收在离子交换树脂上; 和（v）使用洗脱缓冲液从柱洗脱聚唾液酸以提供具有降低的内毒素含量的聚唾液酸的产物溶液。
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