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    Novel Lactosamine Derivatives
    3.
    发明申请
    Novel Lactosamine Derivatives 失效
    新型乳糖胺衍生物

    公开(公告)号：US20090234111A1

    公开(公告)日：2009-09-17

    申请号：US12225094

    申请日：2007-03-13

    申请人： Gyula Dekany ,  Karoly Agoston ,  Istvan Bajza ,  Marie Bøjstrup ,  Lars Kröger

    发明人： Gyula Dekany ,  Karoly Agoston ,  Istvan Bajza ,  Marie Bøjstrup ,  Lars Kröger

    IPC分类号： C07H5/06

    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 R1 is selected from the group consisting of optionally substituted acyl and optionally substituted alkyloxy-carbonyl; R2 is selected from the group consisting of optionally substituted benzyl, optionally substituted benzhydryl, optionally substituted trityl, and optionally substituted naphthylmethyl (or R2 is hydrogen in the formula to the left); R3 is selected from the group consisting of optionally substituted C1-5-alkyl, optionally substituted heteroalkyl, optionally substituted heterocyclyl, optionally substituted aryl, optionally substituted C2-6-acyl, and hydrogen; and Q1 and Q2 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，和任选取代的萘基甲基（或R2是下式中的氢）; 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 2-6 - 酰基和氢; 并且Q1和Q2独立地选自吸电子取代基。

    CARBOHYDRATE DERIVATIVES
    7.
    发明申请
    CARBOHYDRATE DERIVATIVES 有权
    碳氢化合物衍生物

    公开(公告)号：US20110060139A1

    公开(公告)日：2011-03-10

    申请号：US12741973

    申请日：2008-11-03

    申请人： Gyula Dekany ,  István Bajza ,  Marie Bøjstrup ,  Karoly Agoston ,  Lars Kröger ,  Figueroa Peréz ,  Christoph Röhrig ,  Paulo Vital ,  Erzsébet Czinege

    发明人： Gyula Dekany ,  István Bajza ,  Marie Bøjstrup ,  Karoly Agoston ,  Lars Kröger ,  Figueroa Peréz ,  Christoph Röhrig ,  Paulo Vital ,  Erzsébet Czinege

    IPC分类号： C07H5/06 ,  C08B37/00

    CPC分类号： C07H15/12 ,  C07H5/06 ,  C07H15/203

    摘要： A 1,2-dideoxy-1,2-diamino oligosaccharide or polysaccharide in its free base, salt or metal-complex form as shown in General Formula 1 and derivative thereof is described. R1, R2 and R3 are each independently selected from the group consisting of H and a carbohydrate moiety, with the proviso that at least one of the groups R1, R2 or R3 is a carbohydrate moiety; R4 is selected from the group consisting of: H, optionally substituted C1-20-alkyl, optionally substituted heteroalkyl, optionally substituted C2-20-alkenyl, optionally substituted C2-20-alkynyl, optionally substituted C3-10-cycloalkyl, optionally substituted heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl.

    摘要翻译： 描述了其通式1及其衍生物所示的其游离碱，盐或金属络合物形式的1,2-二脱氧-1,2-二氨基寡糖或多糖。 R 1，R 2和R 3各自独立地选自H和碳水化合物部分，条件是基团R 1，R 2或R 3中的至少一个是碳水化合物部分; R 4选自：H，任选取代的C 1-20 - 烷基，任选取代的杂烷基，任选取代的C 2-20 - 烯基，任选取代的C 2-20 - 炔基，任选取代的C 3-10 - 环烷基，任选取代的杂环基 ，任选取代的芳基和任选取代的杂芳基。

    CRYSTALLINE CARBOHYDRATE DERIVATIVE
    9.
    发明申请
    CRYSTALLINE CARBOHYDRATE DERIVATIVE 有权
    碳水化合物衍生物

    公开(公告)号：US20110166339A1

    公开(公告)日：2011-07-07

    申请号：US13054314

    申请日：2009-07-15

    申请人： Gyula Dekany ,  Karoly Agoston ,  Istvan Bajza ,  Marie Bøjstrup ,  Ignacio Fegueroa Pérez ,  Lars Kröger ,  Christoph H. Röhrig

    发明人： Gyula Dekany ,  Karoly Agoston ,  Istvan Bajza ,  Marie Bøjstrup ,  Ignacio Fegueroa Pérez ,  Lars Kröger ,  Christoph H. Röhrig

    IPC分类号： C07H5/06

    CPC分类号： C07H5/06 ,  C07H1/00

    摘要： α-Lactosamine hydrochloride, substantially free of β-lactosamine hydrochloride; a method of preparing α-lactosamine hydrochloride monohydrate from an anomeric mixture of lactosamine hydrochloride, including: preparing a solution including the anomeric mixture of lactosamine hydrochloride, water and at least one water-miscible organic solvent at a temperature of 0-100° C., and cooling the solution to cause crystallisation of α-lactosamine hydrochloride monohydrate; a method of preparing anhydrous α-lactosamine hydrochloride; and use of α-lactosamine hydrochloride as a food supplement or intermediate in synthesis.

    摘要翻译： α-乳糖胺盐酸盐，基本上不含β-乳糖胺盐酸盐; 一种从乳糖胺盐酸盐的端基异构体混合物制备α-乳糖胺盐酸盐一水合物的方法，包括：在0-100℃的温度下制备包括乳糖胺盐酸盐，水和至少一种水混溶性有机溶剂的端基异构体混合物的溶液 ，并冷却该溶液以引起α-乳糖胺盐酸盐一水合物的结晶; 制备无水α-乳糖胺盐酸盐的方法; 并使用盐酸α-乳糖胺作为食品添加剂或中间体。

    GLYCOPROTEINS AND GLYCOSYLATED CELLS AND A METHOD FOR THE PREPARATION OF THE SAME
    10.
    发明申请
    GLYCOPROTEINS AND GLYCOSYLATED CELLS AND A METHOD FOR THE PREPARATION OF THE SAME 有权
    糖蛋白和糖苷化细胞及其制备方法

    公开(公告)号：US20100261873A1

    公开(公告)日：2010-10-14

    申请号：US12733672

    申请日：2008-09-24

    申请人： Gyula Dekany ,  Karoly Agoston ,  István Bajza ,  Marie Bøjstrup ,  Lars Kröger

    发明人： Gyula Dekany ,  Karoly Agoston ,  István Bajza ,  Marie Bøjstrup ,  Lars Kröger

    IPC分类号： C07K9/00 ,  C07K1/00 ,  C08B37/00

    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 R3 and R4 are hydroxyl, acetamido, or a carbohydrate moiety; and R5 is hydrogen, methyl, hydroxymethyl, acetamidomethyl, carboxyl, or X—(CH2)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。