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    PROCESS FOR THE ATTACHMENT OF A GALNAC MOIETY COMPRISING A (HETERO)ARYL GROUP TO A GLCNAC MOIETY, AND PRODUCT OBTAINED THEREBY
    3.
    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
    5.
    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。

    MODIFIED GLYCOPROTEIN, PROTEIN-CONJUGATE AND PROCESS FOR THE PREPARATION THEREOF
    7.
    发明授权
    MODIFIED GLYCOPROTEIN, PROTEIN-CONJUGATE AND PROCESS FOR THE PREPARATION THEREOF 有权
    修饰的糖蛋白，蛋白质共轭物及其制备方法

    公开(公告)号：EP3058083B1

    公开(公告)日：2018-04-11

    申请号：EP14790775.2

    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

    IPC分类号： C12P21/00 ,  C07K16/30

    CPC分类号： A61K47/6855 ,  A61K47/6803 ,  A61K2039/505 ,  C07K16/32 ,  C07K2317/41 ,  C12P21/00 ,  C12P21/005

    摘要： Glycoproteins comprising a glycan of the formula (102) are disclosed; wherein b is 0 or 1; the GlcNAc residue optionally fucosylated; and Su(A)x is a sugar derivative comprising x functional groups A, wherein x is 1, 2, 3 or 4 and A is independently selected from the group consisting of an azido group, a keto group, an alkynyl group, a thiol group, a halogen, a sulfonyloxy group, a halogenated acetamido group, a mercaptoacetamido group and a sulfonylated hydroxyacetamido group. Protein-conjugates having glycoproteins according to the invention conjugated to a molecule of interest (e.g., an active substance) are also disclosed. Examples include modified antibodies, antibody-conjugates, and antibody-drug conjugates (ADCs). Processes for the preparation of the modified glycoproteins according to the invention and methods for the preparation of a protein-conjugate according to the invention are mentioned.

    PROCESS FOR THE MODIFICATION OF A GLYCOPROTEIN USING A GLYCOSYLTRANSFERASE THAT IS OR IS DERIVED FROM A (1,4)-N-ACETYLGALACTOSAMINYLTRANSFERASE
    10.
    发明公开
    PROCESS FOR THE MODIFICATION OF A GLYCOPROTEIN USING A GLYCOSYLTRANSFERASE THAT IS OR IS DERIVED FROM A (1,4)-N-ACETYLGALACTOSAMINYLTRANSFERASE 有权
    METHODS FOR MODIFICATION FROM A A-（1,4）-N- acetylgalactosaminyl转移酶糖基转移酶衍生的糖蛋白的一种手段

    公开(公告)号：EP3134520A1

    公开(公告)日：2017-03-01

    申请号：EP16722547.3

    申请日：2016-04-25

    申请人： SynAffix B.V.

    发明人： VAN BERKEL, Sander Sebastiaan ,  VAN GEEL, Remon ,  WIJDEVEN, Maria Antonia ,  VAN DELFT, Floris Louis

    IPC分类号： C12N9/10

    CPC分类号： C12P21/005 ,  A61K47/6803 ,  A61K47/6849 ,  C07K16/2878 ,  C07K16/32 ,  C07K2317/14 ,  C07K2317/41 ,  C12N9/1051 ,  C12Y204/01038 ,  C12Y204/01092

    摘要： The present invention relates to a process for the enzymatic modification of a glycoprotein. The process comprises the step of contacting a glycoprotein comprising a glycan comprising a terminal GlcNAc-moiety, in the presence of glycosyltransferasethat is,or is derived from,a β-(1,4)-N-acetylgalactosaminyltransferase, with anon-natural sugar-derivative nucleotide. Thenon-natural sugar-derivative nucleotide is according to formula (3): wherein A is selected from the group consisting of -N3, -C(O)R3, -(CH2)iC≡C-R4, - SH, -SC(O)R8, -SC(0)OR8, -SC(S)OR8, -F, -CI, -Br -I, -OS(O)2R5, terminal C2 - C24 alkenyl groups, C3 - C5 cycloalkenyl groups, C4 - C8 alkadienyl groups, terminal C3 - C24 allenyl groups and amino groups. The invention further relates to a glycoprotein obtainable by the process according to the invention, to a bioconjugate that can be obtained by conjugating the glycoprotein with a linker-conjugate, and to β-(1,4)-Ν- acetylgalactosaminyltransferases that can be used in preparing the the glycoprotein according to the invention.

    摘要翻译： 本发明涉及一种用于糖蛋白的酶修饰的方法。 该方法包括使一种糖蛋白，其包括含有聚糖一个末端GlcNAc部分，在glycosyltransferasethat是存在的步骤中，或者由一个β-（1,4）-N- acetylgalactosaminyltransferase衍生，具有匿名天然糖 衍生物的核苷酸。 扩散核武器天然糖衍生物核苷酸gemäß到式（3）：worin A被选自-N 3，C（O）R 3，所选择的 - （CH2）iC≡C-R4， - SH，-S（ O）R8，-SC（O）OR 8，-S-C（S）OR 8，-F，-Cl，-Br，-I，-OS（O）2 R 5，端子C2 - C24烯基，C3 - C5环烯基，C4 - C8链二烯基，端C3 - C24丙二烯基和氨基。 本发明进一步涉及由该方法gemäß本发明的糖蛋白可获得的，涉及一种生物共轭也可以通过用左缀合物缀合糖蛋白来获得，并以β-（1,4）-Ν-乙酰氨基半乳糖也可以使用 在制备糖蛋白gemäß于本发明。