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1. 发明申请

WO2009040363A1 GLYCOPROTEINS AND GLYCOSYLATED CELLS AND A METHOD FOR THE PREPARATION OF THE SAME 审中-公开
标题翻译：糖蛋白和糖苷化细胞及其制备方法
公开(公告)号：WO2009040363A1
公开(公告)日：2009-04-02
申请号：PCT/EP2008/062728
申请日：2008-09-24
申请人： GLYCOM APS , DEKANY, Gyula , AGOSTON, Karoly , BAJZA, István , BØJSTRUP, Marie , KRÖGER, Lars
发明人： DEKANY, Gyula , AGOSTON, Karoly , BAJZA, István , BØJSTRUP, Marie , KRÖGER, Lars
IPC分类号： C07K1/107 , A61K47/48 , C07K14/62 , C07K14/765
CPC分类号： C07K1/1077 , A61K47/549 , C07K14/00
摘要： The present application discloses novel glycoproteins and a related glycosylcarbamoylation methodology suitable for the preparation of glycopeptides (in particular glycoproteins and glycosylated cells), as well as the use of such glycoproteins in medicine, e.g. as pharmaceuticals and diagnostics or in diagnostic kits. The method for the preparation of a carbohydrate-peptide conjugate comprises reacting a cyclic carbamate (1) (wherein R 3 and R 4 are hydroxyl, acetamido, or a carbohydrate moiety; and R 5 is hydrogen, methyl, hydroxymethyl, acetamidomethyl, carboxyl, or X-(CH 2 ) r -, wherein X is a carbohydrate moiety and r is an integer selected from 0, 1, 2 and 3) with a peptide comprising at least one primary amino group.
摘要翻译：本申请公开了适用于制备糖肽（特别是糖蛋白和糖基化细胞）的新型糖蛋白和相关的糖基氨基甲酰化方法，以及这些糖蛋白在医学中的应用。作为药物和诊断或诊断试剂盒。制备碳水化合物 - 肽缀合物的方法包括使环状氨基甲酸酯（1）（其中R 3和R 4是羟基，乙酰氨基或碳水化合物部分;和R 5是氢，甲基，羟甲基，乙酰胺基甲基，羧基或X- （CH 2）r - ，其中X是碳水化合物部分，r是选自0,1,2和3的整数）与包含至少一个伯氨基的肽。

2. 发明申请

WO2007104311A1 NOVEL LACTOSAMINE DERIVATIVES 审中-公开
标题翻译：新型乳糖胺衍生物
公开(公告)号：WO2007104311A1
公开(公告)日：2007-09-20
申请号：PCT/DK2007/000123
申请日：2007-03-13
申请人： GLYCOM APS , DEKANY, Gyula , AGOSTON, Karoly , BAJZA, István , BØJSTRUP, Marie , KRÖGER, Lars
发明人： DEKANY, Gyula , AGOSTON, Karoly , BAJZA, István , BØJSTRUP, Marie , KRÖGER, Lars
IPC分类号： C07H5/06 , C07H15/12
CPC分类号： C07H5/06 , C07H15/12
摘要： The present invention provides novel lactosamine derivatives and related methods suitable for the preparation, including large-scale production, of N-acetyllactosamine, lactosamine, numerous lactosamine salts and a number of lactosamine-containing oligosaccharides. Preferred compounds are: (I) wherein R 1 is selected from the group consisting of optionally substituted acyl and optionally substituted alkyloxy-carbonyl; R 2 is selected from the group consisting of optionally substituted benzyl, optionally substituted benzhydryl, optionally substituted trityl, and optionally substituted naphthylmethyl (or R 2 is hydrogen in the formula to the left); R 3 is selected from the group consisting of optionally substituted C 1-5 -alkyl, optionally substituted heteroalkyl, optionally substituted heterocyclyl, optionally substituted aryl, optionally substituted C 2-6 -acyl, and hydrogen; and Q 1 and Q 2 are independently selected from the group consisting of electron withdrawing substituents.
摘要翻译：本发明提供新的乳糖胺衍生物和适合于包括大规模生产N-乙酰基乳糖胺，乳糖胺，许多乳糖胺盐和多种含乳糖胺的寡糖的制备方法。优选的化合物是：（I）其中R 1选自任选取代的酰基和任选取代的烷氧基 - 羰基; R 2选自任选取代的苄基，任选取代的二苯甲基，任选取代的三苯甲基，和任选取代的萘甲基（或R 2）是式中的氢，剩下）; R 3选自任选取代的C 1-5 - 烷基，任选取代的杂烷基，任选取代的杂环基，任选取代的芳基，任选取代的C 1 -C 6 - 2-6-酰基和氢; Q 1和Q 2独立地选自吸电子取代基。

3. 发明申请

WO2005121114A2 1,5 AND 1,4-ANHYDROKETOSES, METHODS FOR THE PREPARATION OF 1,5-AND 1,4-ANHYDROKETOSES, INTERMEDIATES, AND USES OF 1,5-AND 1,4-ANHYDROKETOSES 审中-公开
标题翻译： 1,5和1,4-ANHYDROKETOSES，1,5-和1,4-壬二酸的制备方法，中间体和1,5-二酮的用途
公开(公告)号：WO2005121114A2
公开(公告)日：2005-12-22
申请号：PCT/DK2005/000377
申请日：2005-06-07
申请人： GLYCOM APS , LUNDT, Inge , STÜTZ, Arnold , DEKANY, Gyula , THIEM, Joachim , AGOSTON, Karoly , ANDREASSEN, Mikkel
发明人： LUNDT, Inge , STÜTZ, Arnold , DEKANY, Gyula , THIEM, Joachim , AGOSTON, Karoly , ANDREASSEN, Mikkel
IPC分类号： C07D309/00
CPC分类号： C07D493/08
摘要： The present invention relates to 1,4- and 1,5-anhydro-D-ketoses (monosaccharides, oligosaccharides and various glycoconjugates), e.g. 1,5-anhydro-D-fructose. Moreover, the invention provides synthetic methods and novel intermediates and precursors suitable for their preparation. The methods include catalytic- and/or pyrolitic sulfenic acid elimination of corresponding ß-hydroxy sulfoxides, N-deprotection of N-substituted-aminoglycals, O-deprotection of carbohydrate enolethers and/or O-acyl-substituted carbohydrate enols, and regio- and stereoselective modification and subsequent chemical transformation of bicyclic and/or tricyclic 1,4- and 1,5-anhydro-glycoderivatives. Furthermore, the present invention provides novel applications of 1,4- and 1,5-anhydroketoses within pharmaceutical, food and cosmetic industries.
摘要翻译：本发明涉及1,4-和1,5-脱水-D-酮糖（单糖，寡糖和各种糖缀合物），例如 1,5-脱水-D-果糖。此外，本发明提供了合适的方法和适合其制备的新型中间体和前体。所述方法包括相应的β-羟基亚砜的催化和/或热解亚磺酸消除，N-取代的 - 氨基糖基的N-去保护，碳水化合物烯醇酯和/或O-酰基取代的碳水化合物烯醇的O-脱保护，以及区域和立体选择性修饰和随后的双环和/或三环1,4-和1,5-脱水 - 衍生物的化学转化。此外，本发明提供在制药，食品和化妆品工业中的1,4-和1,5-脱水酮糖的新应用。

4. 发明申请

WO2007104311A8 NOVEL LACTOSAMINE DERIVATIVES 审中-公开
标题翻译：新型乳糖胺衍生物
公开(公告)号：WO2007104311A8
公开(公告)日：2007-11-22
申请号：PCT/DK2007000123
申请日：2007-03-13
申请人： GLYCOM APS , DEKANY GYULA , AGOSTON KAROLY , BAJZA ISTVAN , BOEJSTRUP MARIE , KROEGER LARS
发明人： DEKANY GYULA , AGOSTON KAROLY , BAJZA ISTVAN , BOEJSTRUP MARIE , KROEGER LARS
IPC分类号： C07H5/06 , C07H15/12
CPC分类号： C07H5/06 , C07H15/12
摘要： The present invention provides novel lactosamine derivatives and related methods suitable for the preparation, including large-scale production, of N-acetyllactosamine, lactosamine, numerous lactosamine salts and a number of lactosamine-containing oligosaccharides. Preferred compounds are: (I) wherein R 1 is selected from the group consisting of optionally substituted acyl and optionally substituted alkyloxy-carbonyl; R 2 is selected from the group consisting of optionally substituted benzyl, optionally substituted benzhydryl, optionally substituted trityl, and optionally substituted naphthylmethyl (or R 2 is hydrogen in the formula to the left); R 3 is selected from the group consisting of optionally substituted C 1-5 -alkyl, optionally substituted heteroalkyl, optionally substituted heterocyclyl, optionally substituted aryl, optionally substituted C 2-6 -acyl, and hydrogen; and Q 1 and Q 2 are independently selected from the group consisting of electron withdrawing substituents.
摘要翻译：本发明提供了适用于制备（包括大规模生产）N-乙酰乳糖胺，乳糖胺，许多乳糖胺盐和许多含有乳糖胺的寡糖的新型乳糖胺衍生物和相关方法。优选的化合物是：（I）其中R 1选自任选取代的酰基和任选取代的烷氧基羰基; R 2选自任选取代的苄基，任选取代的二苯甲基，任选取代的三苯甲基和任选取代的萘基甲基（或者R 2是式中的氢至剩下）; R 3选自任选取代的C 1-5烷基，任选取代的杂烷基，任选取代的杂环基，任选取代的芳基，任选取代的C 1-5烷基， 2-6个 - 酰基和氢; 并且Q 1和Q 2独立地选自吸电子取代基。

5. 发明申请

WO2005121114A3 1,5 AND 1,4-ANHYDROKETOSES, METHODS FOR THE PREPARATION OF 1,5-AND 1,4-ANHYDROKETOSES, INTERMEDIATES, AND USES OF 1,5-AND 1,4-ANHYDROKETOSES 审中-公开
标题翻译： 1,5和1,4-ANHYDROKETOSES，1,5-和1,4-壬二酸的制备方法，中间体以及1,5-1,4-苯并二氢吡喃酮的用途
公开(公告)号：WO2005121114A3
公开(公告)日：2006-10-12
申请号：PCT/DK2005000377
申请日：2005-06-07
申请人： GLYCOM APS , LUNDT INGE , STUETZ ARNOLD , DEKANY GYULA , THIEM JOACHIM , AGOSTON KAROLY , ANDREASSEN MIKKEL
发明人： LUNDT INGE , STUETZ ARNOLD , DEKANY GYULA , THIEM JOACHIM , AGOSTON KAROLY , ANDREASSEN MIKKEL
IPC分类号： C07D309/30 , C07D493/08 , C07D493/18
CPC分类号： C07D493/08
摘要： The present invention relates to 1,4- and 1,5-anhydro-D-ketoses (monosaccharides, oligosaccharides and various glycoconjugates), e.g. 1,5-anhydro-D-fructose. Moreover, the invention provides synthetic methods and novel intermediates and precursors suitable for their preparation. The methods include catalytic- and/or pyrolitic sulfenic acid elimination of corresponding ß-hydroxy sulfoxides, N-deprotection of N-substituted-aminoglycals, O-deprotection of carbohydrate enolethers and/or O-acyl-substituted carbohydrate enols, and regio- and stereoselective modification and subsequent chemical transformation of bicyclic and/or tricyclic 1,4- and 1,5-anhydro-glycoderivatives. Furthermore, the present invention provides novel applications of 1,4- and 1,5-anhydroketoses within pharmaceutical, food and cosmetic industries.
摘要翻译：本发明涉及1,4-和1,5-脱水-D-酮糖（单糖，寡糖和各种糖缀合物），例如 1,5-脱水-D-果糖。此外，本发明提供了合适的方法和适于其制备的新型中间体和前体。这些方法包括相应的β-羟基亚砜的催化和/或热解亚磺酸消除，N-取代的 - 氨基糖的N-去保护，碳水化合物烯醇酯和/或O-酰基取代的碳水化合物烯醇的O-去保护，以及区域和双环和/或三环1,4-和1,5-脱水 - 糖基化衍生物的立体选择性修饰和随后的化学转化。此外，本发明提供在制药，食品和化妆品工业中的1,4-和1,5-脱水酮糖的新应用。

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