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1. 发明申请

US20080227092A1 Solid-Phase Oligosaccharide Tagging: a Technique for Manipulation of Immobilized Carbohydrates 失效
标题翻译：固相寡糖标签：操作固定化碳水化合物的技术
公开(公告)号：US20080227092A1
公开(公告)日：2008-09-18
申请号：US11816049
申请日：2006-02-08
申请人： Anders Lohse , Malene Ryborg Jorgensen , Rita Martins , Ole Hindsgaul
发明人： Anders Lohse , Malene Ryborg Jorgensen , Rita Martins , Ole Hindsgaul
IPC分类号： C12Q1/68 , C07H1/00 , G01N30/00 , G01N33/566 , G01N33/50
CPC分类号： G01N33/6842 , G01N33/54353 , G01N33/6803 , Y10T436/145555 , Y10T436/24
摘要： The invention relates to methods of manipulating immobilised carbohydrates by derivatisation. Depending on the nature of the derivatisation, the carbohydrate may thereby be more easily detected and/or identified or handled. In particular, the invention relates to methods of preparing a reactive sugar comprising the steps of: i) providing a sample comprising a reducing sugar; ii) providing a solid support covalently attached to a linker comprising a capture group comprising an —NH2 group, wherein said linker optionally is attached to said solid support via a spacer; iii) reacting said reducing sugar with said —NH2 group, thereby obtaining an immobilised sugar; iv) reacting free —NH2 groups with a capping agent, wherein the capping agent comprises a reactive group capable of reacting with an —NH2 group; and v) reducing C═N bonds with a reducing agent, thereby obtaining an reactive sugar of the structure SugarCHn—NH— linked to a solid support via a linker and optionally a spacer, wherein n is 1 or 2.
摘要翻译：本发明涉及通过衍生化操作固定的碳水化合物的方法。根据衍生化的性质，可以更容易地检测和/或识别或处理碳水化合物。特别地，本发明涉及制备反应性糖的方法，包括以下步骤：i）提供包含还原糖的样品; ii）提供共价连接到包含-NH 2基团的捕获基团的接头的固体支持物，其中所述接头任选地经由间隔子连接到所述固体支持物上; iii）使所述还原糖与所述-NH 2基团反应，从而获得固定的糖; iv）使游离-NH 2基团与封端剂反应，其中封端剂包含能够与-NH 2基团反应的反应性基团; 和v）用还原剂还原CN键，从而通过连接体和任选的间隔基获得与固体支持物结合的反应性糖，其中n为1或2 。

2. 发明授权

US07893253B2 Solid-phase oligosaccharide tagging: a technique for manipulation of immobilized carbohydrates 失效
标题翻译：固相寡糖标签：用于操作固定化碳水化合物的技术
公开(公告)号：US07893253B2
公开(公告)日：2011-02-22
申请号：US11816049
申请日：2006-02-08
申请人： Anders Lohse , Malene Ryborg Jørgensen , Rita Martins , Ole Hindsgaul
发明人： Anders Lohse , Malene Ryborg Jørgensen , Rita Martins , Ole Hindsgaul
IPC分类号： C07H3/00 , C12Q1/68 , C12Q1/70 , G01N33/53
CPC分类号： G01N33/6842 , G01N33/54353 , G01N33/6803 , Y10T436/145555 , Y10T436/24
摘要： The invention relates to methods of manipulating immobilised carbohydrates by derivatisation. Depending on the nature of the derivatisation, the carbohydrate may thereby be more easily detected and/or identified or handled. In particular, the invention relates to methods of preparing a reactive sugar comprising the steps of: i) providing a sample comprising a reducing sugar; ii) providing a solid support covalently attached to a linker comprising a capture group comprising an —NH2 group, wherein said linker optionally is attached to said solid support via a spacer; iii) reacting said reducing sugar with said —NH2 group, thereby obtaining an immobilised sugar; iv) reacting free —NH2 groups with a capping agent, wherein the capping agent comprises a reactive group capable of reacting with an —NH2 group; and v) reducing C═N bonds with a reducing agent, thereby obtaining an reactive sugar of the structure SugarCHn-NH— linked to a solid support via a linker and optionally a spacer, wherein n is 1 or 2.
摘要翻译：本发明涉及通过衍生化操作固定的碳水化合物的方法。根据衍生化的性质，可以更容易地检测和/或识别或处理碳水化合物。特别地，本发明涉及制备反应性糖的方法，包括以下步骤：i）提供包含还原糖的样品; ii）提供共价连接到包含-NH 2基团的捕获基团的接头的固体支持物，其中所述接头任选地经由间隔子连接到所述固体支持物上; iii）使所述还原糖与所述-NH 2基团反应，从而获得固定的糖; iv）使游离-NH 2基团与封端剂反应，其中封端剂包含能够与-NH 2基团反应的反应性基团; 和v）用还原剂还原C = N键，从而通过接头和任选的间隔基获得与固体支持物结合的糖基-NH-NH-结构的反应性糖，其中n为1或2。

3. 发明申请

US20100047828A1 SOLID-PHASE DETECTION OF TERMINAL MONOSACCHARIDES CLEAVED FROM GLYCOSYLATED SUBSTRATES 失效
标题翻译：从胶体基质中清除终端单糖的固相检测
公开(公告)号：US20100047828A1
公开(公告)日：2010-02-25
申请号：US12373331
申请日：2007-07-10
申请人： Mads Detlef Sorensen , Rita Martins , Ole Hindsgaul
发明人： Mads Detlef Sorensen , Rita Martins , Ole Hindsgaul
IPC分类号： G01N33/58 , C07H1/00
CPC分类号： C12Q1/34 , G01N33/543 , G01N33/58 , Y10T436/143333 , Y10T436/144444
摘要： The present invention relates to a novel method for analysing carbohydrates. The invention is in particular useful in detecting a terminal monosaccharide which may be released from a glycosylated substrate for example using an exoglucosidase. After relase from the glycosylated substrate the terminal monosaccharide may be captured on a solid support, incubated with a boronate detection agent and detected by aid of the boronate detection agent. The methods of the invention are useful for a variety of purposes including sequencing of carbohydrates, wherein exoglycosidases with predetermined specificity are employed for the release.
摘要翻译：本发明涉及一种分析碳水化合物的新方法。本发明特别可用于检测可以例如使用外切葡糖苷酶从糖基底物释放的末端单糖。在从糖基化的底物上脱除后，末端单糖可以捕获在固体支持物上，与硼酸盐检测剂一起孵育并通过硼酸盐检测剂的检测。本发明的方法可用于多种目的，包括碳水化合物的测序，其中使用具有预定特异性的exoglycosidases用于释放。

4. 发明授权

US08445288B2 Solid-phase detection of terminal monosaccharides cleaved from glycosylated substrates 失效
标题翻译：从糖基底物切割的末端单糖的固相检测
公开(公告)号：US08445288B2
公开(公告)日：2013-05-21
申请号：US12373331
申请日：2007-07-10
申请人： Mads Detlef Sorensen , Rita Martins , Ole Hindsgaul
发明人： Mads Detlef Sorensen , Rita Martins , Ole Hindsgaul
IPC分类号： G01N33/00 , C12Q1/54
CPC分类号： C12Q1/34 , G01N33/543 , G01N33/58 , Y10T436/143333 , Y10T436/144444
摘要： The present invention relates to a novel method for analysing carbohydrates. The invention is in particular useful in detecting a terminal monosaccharide which may be released from a glycosylated substrate for example using an exoglucosidase. After relase from the glycosylated substrate the terminal monosaccharide may be captured on a solid support, incubated with a boronate detection agent and detected by aid of the boronate detection agent. The methods of the invention are useful for a variety of purposes including sequencing of carbohydrates, wherein exoglycosidases with predetermined specificity are employed for the release.
摘要翻译：本发明涉及一种分析碳水化合物的新方法。本发明特别可用于检测可以例如使用外切葡糖苷酶从糖基底物释放的末端单糖。在从糖基化的底物上脱除后，末端单糖可以捕获在固体支持物上，与硼酸盐检测剂一起孵育并通过硼酸盐检测剂的检测。本发明的方法可用于多种目的，包括碳水化合物的测序，其中使用具有预定特异性的exoglycosidases用于释放。

5. 发明授权

US06627453B1 Methods for screening compound libraries 失效
公开(公告)号：US06627453B1
公开(公告)日：2003-09-30
申请号：US09341916
申请日：2000-03-08
申请人： Ole Hindsgaul , David C. Schriemer
发明人： Ole Hindsgaul , David C. Schriemer
IPC分类号： G01N3002
CPC分类号： G01N33/6845 , B01J2219/00585 , B01J2219/00704 , B01J2219/00707 , B01J2219/00731 , B01J2219/00738 , B01J2219/00745 , B01J2219/00747 , C40B30/08 , C40B40/12 , C40B40/18 , G01N30/466 , G01N30/7266 , G01N33/538 , G01N33/54306 , G01N33/54366 , G01N33/68 , G01N33/6842 , G01N33/6848 , G01N33/6851 , G01N2030/628 , H01J49/00 , H01J49/0036 , Y10T436/24
摘要： Disclosed are methods for screening compound libraries using frontal chromatography in combination with mass spectrometry to identify and rank those members of the library that bind to a target receptor. Methods are also disclosed which permit a compound library to be rapidly screened to determine if any member of the library has an affinity for the target receptor as measured by a pre-selected indicator compound.

6. 发明授权

US06303764B1 Synthesis of 4,7-dialkyl chromogenic glycosides of N-acetylneuraminic acids 失效
标题翻译： N-乙酰神经氨酸的4,7-二烷基显色糖苷的合成
公开(公告)号：US06303764B1
公开(公告)日：2001-10-16
申请号：US09406024
申请日：1999-09-24
申请人： Om Srivastava , Geeta Srivastava , Minghui Du , Ole Hindsgaul , David R. Bundle , Avraham Liav
发明人： Om Srivastava , Geeta Srivastava , Minghui Du , Ole Hindsgaul , David R. Bundle , Avraham Liav
IPC分类号： G07G300
CPC分类号： C07K14/005 , C12N2760/16122 , C12N2760/16222 , C12P19/14
摘要： The present invention provides an improved method of preparing a 4,7-di-O-alkyl chromogenic ketoside of N-acetylneuraminic acid (Neu5Ac) for use in detecting influenza virus types A and B. The ketosides are substrates that are selectively cleaved by a neuraminidase on influenza virus, but not be neuraminidases found on other viruses or on bacteria. The synthesis is efficient and provides large quantities of the ketoside for commercial development. The synthesis includes a step of alkylating the 4- and 7-hydroxyl groups of a protected alkyl ester alkyl ketoside derivative of Neu5Ac by a process that comprises contacting the derivative with a composition comprising an alkyl halide to form a 4,7-di-O-alkyl protected alkyl ester alkyl ketoside derivative of Neu5Ac. The synthesis alternatively includes protecting the 8- and 9-hydroxyl groups of an alkyl ester alkyl ketoside derivative of Neu5Ac by forming an 8,9-epoxide protected alkyl ester alkyl ketoside derivative of Neu5Ac.
摘要翻译：本发明提供一种制备用于检测A型和B型流感病毒的N-乙酰神经氨酸（Neu5Ac）的4,7-二-O-烷基显色酮面的改进方法。酮是一种由神经氨酸酶对流感病毒，但不是在其他病毒或细菌上发现的神经氨酸酶。该合成是有效的，并为商业开发提供大量的酮基。该合成包括通过包括使衍生物与包含烷基卤的组合物接触以形成4,7-二-O-的方法使得Neu5Ac的被保护的烷基酯烷基酮酮衍生物的4-和7-羟基烷基化的步骤烷基保护的烷基酯Neu5Ac的烷基酮基衍生物。合成交替地包括通过形成Neu5Ac的8,9-环氧化物保护的烷基酯烷基酮内酯衍生物来保护Neu5Ac的烷基酯烷基酮酮衍生物的8-和9-羟基。

7. 发明授权

US5874411A Oligosaccharide glycosides having mammalian immunosuppresive and tolerogenic properties 失效
标题翻译：具有哺乳动物免疫抑制和耐受性的寡糖糖苷
公开(公告)号：US5874411A
公开(公告)日：1999-02-23
申请号：US754097
申请日：1996-11-13
申请人： Om P. Srivastava , Geeta Srivastava , Roman Szweda , David R. Bundle , Ole Hindsgaul , H. Rizk Hanna , Kevin Holme , Frank W. Barresi , Minghui Du
发明人： Om P. Srivastava , Geeta Srivastava , Roman Szweda , David R. Bundle , Ole Hindsgaul , H. Rizk Hanna , Kevin Holme , Frank W. Barresi , Minghui Du
IPC分类号： C07H3/04 , C07H3/06 , C07H9/02 , C07H15/00 , A61K31/70
CPC分类号： C07H3/04 , C07H15/00 , C07H3/06 , C07H9/02
摘要： Disclosed are novel oligosaccharide glycosides having mammalian immunosuppressive and tolerogenic properties, pharmaceutical compositions containing such oligosaccharide glycosides and to methods of using such oligosaccharide glycosides to modulate cell-mediated immune responses in a mammal.
摘要翻译：公开了具有哺乳动物免疫抑制和耐受性的新型寡糖糖苷，含有这种寡糖糖苷的药物组合物以及使用这种寡糖糖苷来调节哺乳动物细胞介导的免疫应答的方法。

8. 发明授权

US5795958A Library of glyco-peptides useful for identification of cell adhesion inhibitors 失效
标题翻译：用于鉴定细胞粘附抑制剂的糖肽图书馆
公开(公告)号：US5795958A
公开(公告)日：1998-08-18
申请号：US664303
申请日：1996-06-10
申请人： Narasinga Rao , Morten Meldal , Klaus Bock , Ole Hindsgaul
发明人： Narasinga Rao , Morten Meldal , Klaus Bock , Ole Hindsgaul
IPC分类号： G01N33/53 , A61K38/00 , A61K38/22 , A61P5/00 , A61P31/04 , A61P35/00 , C07K1/04 , C07K9/00 , C07K16/18 , A61K38/06
CPC分类号： C07K9/001 , C07K1/047 , A61K38/00
摘要： Glycopeptides having the following structure are described: ##STR1## wherein: X.sub.1 is hydrogen, an acetyl group, an acyl group or amino acid; R is .alpha.-L-fucose, .alpha.-D-fucose, .beta.-L-fucose or .beta.-D-fucose, wherein R is O-glucosidically linked to A.sub.1 ; A.sub.1 is serine, threonine, tyrosine, hydroxyproline, asparagine, glutamine, homeoserine and hydroxylysine; A.sub.2 is a glycine, an L-amino acid, a D-amino acid or a modified amino acid; A.sub.3 is L or D aspartic acid, glycine or glutamic acid; and X.sub.2 is a hydroxyl, an amine or an amino acid.
摘要翻译：描述了具有以下结构的糖肽：其中：X 1是氢，乙酰基，酰基或氨基酸; R是α-L-岩藻糖，α-D-岩藻糖，β-L-岩藻糖或β-D-岩藻糖，其中R是与α-糖苷键连接的; A1是丝氨酸，苏氨酸，酪氨酸，羟脯氨酸，天冬酰胺，谷氨酰胺，高丝氨酸和羟赖氨酸; A2是甘氨酸，L-氨基酸，D-氨基酸或修饰的氨基酸; A3是L或D天冬氨酸，甘氨酸或谷氨酸; X2是羟基，胺或氨基酸。

9. 发明授权

US5206356A Inhibitors for alpha-L-fucosyl transferase 失效
标题翻译： α-L-岩藻糖基转移酶的抑制剂
公开(公告)号：US5206356A
公开(公告)日：1993-04-27
申请号：US730227
申请日：1991-07-15
申请人： James M. Pierce , Ole Hindsgaul
发明人： James M. Pierce , Ole Hindsgaul
IPC分类号： A61K31/70 , C07H15/04 , C07H15/18
CPC分类号： C07H15/18 , A61K31/70 , C07H15/04
摘要： Synthetic glycosaminosyl transferase-V acceptors and inhibitors are disclosed. Minimal trisaccharide inhibitors and acceptors specific for GnT-V, which is associated with the ability of cells to metastasize are useful, in diagnosis and treatment of conditions characterized by metastatic cells.
摘要翻译：公开了合成的糖基糖基转移酶-V受体和抑制剂。与细胞转移能力相关的GnT-V特异性的最小三糖抑制剂和受体可用于诊断和治疗以转移细胞为特征的病症。

10. 发明授权

US06720190B1 Methods for screening compound libraries 失效
公开(公告)号：US06720190B1
公开(公告)日：2004-04-13
申请号：US09276444
申请日：1999-03-25
申请人： Ole Hindsgaul , David C. Schriemer
发明人： Ole Hindsgaul , David C. Schriemer
IPC分类号： G01N3002
CPC分类号： G01N33/68 , B01J2219/00585 , B01J2219/00704 , B01J2219/00707 , B01J2219/00731 , B01J2219/00738 , B01J2219/00745 , B01J2219/00747 , C40B30/08 , C40B40/12 , C40B40/18 , G01N30/466 , G01N30/7266 , G01N33/538 , G01N33/54306 , G01N33/54366 , G01N33/6845 , G01N33/6848 , G01N2030/628 , H01J49/00 , H01J49/0036 , Y10T436/24
摘要： Disclosed are methods for screening compound libraries using frontal chromatography in combination with mass spectrometry to identify and rank those members of the library that bind to a target receptor. Methods are also disclosed which permit a compound library to be rapidly screened to determine if any member of the library has an affinity for the target receptor as measured by a pre-selected indicator compound.

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