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    PROCESS FOR THE MODIFICATION OF A GLYCOPROTEIN USING A ETA-(1,4)-N-ACETYLGALACTOSAMINYLTRANSFERASE OR A MUTANT THEREOF
    12.
    发明公开
    PROCESS FOR THE MODIFICATION OF A GLYCOPROTEIN USING A ETA-(1,4)-N-ACETYLGALACTOSAMINYLTRANSFERASE OR A MUTANT THEREOF 审中-公开
    方法进行修改使用一个BETA-（1.4）-ACETYLGALACTOSAMINYLTRANSFERASE或其突变体糖蛋白

    公开(公告)号：EP3177633A1

    公开(公告)日：2017-06-14

    申请号：EP15770973.4

    申请日：2015-08-04

    申请人： SynAffix B.V.

    发明人： WASIEL, Anna Agnieska ,  VAN DELFT, Floris Louis ,  VAN BERKEL, Sander Sebastiaan

    IPC分类号： C07H19/10 ,  C07K16/00 ,  C12P21/00

    CPC分类号： C07H19/10 ,  C07K16/32 ,  C07K2317/24 ,  C07K2317/41 ,  C12N9/1051 ,  C12P21/005

    摘要： The present invention relates to a process for the modification of a glycoprotein, using a β-(1,4)-N-acetylgalactosaminyltransferase or a mutant thereof.The process comprisesthe step of contacting a glycoprotein comprising a glycan comprising a terminal GlcNAc-moiety, in the presence of a β-(1,4)-N-acetylgalactosaminyl- transferase or a mutant thereof, with anon-natural sugar-derivative nucleotide.The non-natural sugar-derivative nucleotideis according to formula (3), wherein A is selected from the group consisting of -N
    3 ; -C(0)R
    3 ; -C=C-R
    4 ; -SH; -SC(0)R
    8 ; -SC(V)OR
    8 , wherein V is O or S; -X wherein X is selected from the group consisting of F, CI, Br and I; -OS(0)
    2 R
    5 ; an optionally substituted C
    2 - C
    24 alkyl group; an optionally substituted terminal C
    2 - C
    24 alkenyl group; and an optionally substituted terminal C
    3 - C
    24 allenyl group.

    摘要翻译： 本发明涉及一种用于糖蛋白的修饰，使用β-（1,4）-N-acetylgalactosaminyltransferase或接触的一种糖蛋白，其包括含有聚糖一个末端GlcNAc部分的突变体thereof.The过程comprisesthe步骤， 在一个β-（1,4）-N- acetylgalactosaminyl-转移或其突变体的存在下，与匿名天然糖衍生物nucleotide.The非天然糖衍生物nucleotideisgemäß到式（3）中，A是worin 选自的-N 3中选择; -C（O）R3; -C = C-R 4; SH; -SC（O）R 8; -SC（V）OR 8，worin V是O或S; -X worin X选自选自F，Cl，Br和I的选择; -OS（O）2 R 5; 在任选取代的C2 - C24烷基; OPTIONALLY substituiertem到端子C2 - C24链烯基; 并任选substituiertem终端C3 - C24丙二烯基。

    PROCESS FOR THE ATTACHMENT OF A GALNAC MOIETY COMPRISING A (HETERO)ARYL GROUP TO A GLCNAC MOIETY, AND PRODUCT OBTAINED THEREBY
    16.
    发明公开
    PROCESS FOR THE ATTACHMENT OF A GALNAC MOIETY COMPRISING A (HETERO)ARYL GROUP TO A GLCNAC MOIETY, AND PRODUCT OBTAINED THEREBY 审中-公开
    方法用于结合的GalNAc COMPONENT A（杂）芳基AT A的GalNAc COMPONENT从而GOT PRODUCT

    公开(公告)号：EP3097200A1

    公开(公告)日：2016-11-30

    申请号：EP15704105.4

    申请日：2015-01-26

    申请人： SynAffix B.V.

    发明人： VAN DELFT, Floris Louis ,  VAN GEEL, Remon ,  WIJDEVEN, Maria Antonia ,  HEESBEEN, Ryan

    IPC分类号： C12P19/18 ,  C07H17/075 ,  C07H19/10 ,  C07K16/00 ,  C07K19/00

    CPC分类号： C12P19/18 ,  C07H17/075 ,  C07H19/06 ,  C07H19/10 ,  C07K16/22 ,  C07K16/241 ,  C07K16/2863 ,  C07K16/30 ,  C07K16/32 ,  C07K2317/21 ,  C07K2317/24 ,  C07K2317/41 ,  C07K2317/76 ,  C12N9/1051 ,  C12P19/305 ,  C12P21/005 ,  C12Y204/01

    摘要： The present invention relates to a process for attaching an N-acetylgalactosamine- (hetero)arylmoiety to an N-acetylglucosaminemoiety, the process comprising the step of contacting the N-acetylgalactosamine-(hetero)arylmoiety with the N- acetylglucosaminemoiety in the presence of a mutant galactosyltransferase, wherein the N-acetylglucosaminemoiety is according to Formula (1)the N- acetylgalactosamine-(hetero)arylmoiety is according to Formula (2): In a particularly preferred embodiment of the process according to the invention, the N-acetylgalactosamine-(hetero)arylmoiety comprises a 1,3-dipole functional group, and the N-acetylglucosaminemoiety is a terminal GlcNAc moiety of a glycoprotein glycan. The invention further relates to a productobtainable by the process according to the invention, in particular to glycoproteins. Also, the invention relates to several compounds comprising an N-acetylgalactosamine-(hetero)arylmoiety.

    摘要翻译： 本发明涉及一种用于附连到N-acetylgalactosamine-（杂）arylmoiety到N-acetylglucosaminemoiety，该方法包括使与N- acetylglucosaminemoiety的N acetylgalactosamine-（杂）arylmoiety中的存在的步骤 突变体半乳糖转移酶，worin的N acetylglucosaminemoiety是雅丁式（1）的N个acetylgalactosamine-（杂）arylmoiety是雅丁到式（2）：在这个过程中雅丁到本发明的一个特别优选的实施方式中，N-acetylgalactosamine- （杂）arylmoiety包括1.3偶极官能团，并且N acetylglucosaminemoiety是糖蛋白的聚糖的末端GlcNAc部分。 本发明还涉及到一个productobtainable由过程gemäß所述的发明，特别是糖蛋白。 所以，（杂）arylmoiety本发明涉及的几种化合物包含N- acetylgalactosamine-的。

    MODIFIED GLYCOPROTEIN, PROTEIN-CONJUGATE AND PROCESS FOR THE PREPARATION THEREOF
    20.
    发明公开
    MODIFIED GLYCOPROTEIN, PROTEIN-CONJUGATE AND PROCESS FOR THE PREPARATION THEREOF 审中-公开
    改良型糖蛋白，维他命C，维他命ZUR HERSTELLUNG DAVON

    公开(公告)号：EP2935608A1

    公开(公告)日：2015-10-28

    申请号：EP14790774.5

    申请日：2014-10-14

    申请人： SynAffix B.V.

    发明人： VAN DELFT, Floris Louis ,  VAN GEEL, Remon ,  WIJDEVEN, Maria Antonia ,  VERKADE, Jorge Merijn Mathieu ,  HEESBEEN, Ryan

    IPC分类号： C12P21/00 ,  C07K16/00 ,  A61P35/00

    CPC分类号： C07K16/40 ,  A61K47/6871 ,  C07K16/32 ,  C07K2317/41 ,  C12P21/00 ,  C12P21/005

    摘要： The invention relates to a glycoprotein comprising an optionally fucosylated glycan according to formula (105) or (106), wherein Su(A)x is a modified sugar moiety comprising one or more functional groups A. Functional group A is independently selected from the group consisting of a thiol group, a halogen, a sulfonyloxy group, a halogenated acetamido group, a mercaptoacetamido group and a sulfonated hydroxyacetamido group. The invention also relates to a glycoprotein-conjugate wherein a glycoprotein according to the invention is conjugated to a molecule of interest. Said molecule of interest may for example be an active substance. The invention further relates to a process for the preparation of a modified glycoprotein, and to a method for the preparation of a glycoprotein-conjugate. The invention particularly relates to modified antibodies, antibody-conjugates, antibody-drug conjugates and methods for the preparation thereof.

    摘要翻译： 本发明涉及包含根据式（105）或（106）的任选的岩藻糖基化聚糖的糖蛋白，其中Su（A）x是包含一个或多个官能团A的修饰的糖部分。官能团A独立地选自 由硫醇基，卤素，磺酰氧基，卤代乙酰氨基，巯基乙酰氨基和磺化羟基乙酰氨基组成。 本发明还涉及糖蛋白 - 缀合物，其中根据本发明的糖蛋白与感兴趣的分子缀合。 所述感兴趣的分子可以例如是活性物质。 本发明还涉及一种制备改性糖蛋白的方法，以及制备糖蛋白 - 共轭物的方法。 本发明特别涉及修饰的抗体，抗体缀合物，抗体 - 药物偶联物及其制备方法。