发明公开
EP3335733A1 MODIFIED ANTIBODY, ANTIBODY-CONJUGATE AND PROCESS FOR THE PREPARATION THEREOF
审中-公开

基本信息:
- 专利标题: MODIFIED ANTIBODY, ANTIBODY-CONJUGATE AND PROCESS FOR THE PREPARATION THEREOF
- 申请号:EP17201445.8 申请日:2013-10-23
- 公开(公告)号:EP3335733A1 公开(公告)日:2018-06-20
- 发明人: VAN DELFT, Floris Louis , VAN GEEL, Remon , WIJDEVEN, Maria Antonia
- 申请人: SynAffix B.V.
- 申请人地址: Molenstraat 110 5342 CC Oss NL
- 专利权人: SynAffix B.V.
- 当前专利权人: SynAffix B.V.
- 当前专利权人地址: Molenstraat 110 5342 CC Oss NL
- 代理机构: Nederlandsch Octrooibureau
- 优先权: EP12189604 20121023; US201261717187P 20121023; EP13188607 20131014
- 主分类号: A61K47/68
- IPC分类号: A61K47/68
摘要:
The present invention relates to an antibody comprising a GlcNAc-S(A) x substituent, wherein S(A) x is a sugar derivative comprising x functional groups A wherein A is independently selected from the group consisting of an azido group, a keto group and an alkynyl group and x is 1, 2, 3 or 4, wherein said GlcNAc-S(A) x substituent is bonded to the antibody via C1 of the N-acetylglucosamine of said GlcNAc-S(A) x substituent, and wherein said N-acetylglucosamine is optionally fucosylated.
The invention also relates to an antibody-conjugate, in particular to an antibody-conjugate according to the Formula ( 20 ) or ( 20b ), wherein AB is an antibody, S is a sugar or a sugar derivative, D is a molecule of interest, and wherein said N-acetylglucosamine is optionally fucosylated (b is 0 or 1).
The invention further relates to a process for the preparation of a modified antibody, to a process for the preparation of an antibody-conjugate, and to said antibody-conjugate for use as a medicament.
In addition, the invention relates to a kit of parts comprising an azide-modified antibody and a linker-conjugate, wherein said linker-conjugate comprises a (hetero)cycloalkynyl group and one or more molecules of interest.
The invention also relates to an antibody-conjugate, in particular to an antibody-conjugate according to the Formula ( 20 ) or ( 20b ), wherein AB is an antibody, S is a sugar or a sugar derivative, D is a molecule of interest, and wherein said N-acetylglucosamine is optionally fucosylated (b is 0 or 1).
The invention further relates to a process for the preparation of a modified antibody, to a process for the preparation of an antibody-conjugate, and to said antibody-conjugate for use as a medicament.
In addition, the invention relates to a kit of parts comprising an azide-modified antibody and a linker-conjugate, wherein said linker-conjugate comprises a (hetero)cycloalkynyl group and one or more molecules of interest.
IPC结构图谱:
A | 人类生活必需 |
--A61 | 医学或兽医学;卫生学 |
----A61K | 医用、牙科用或梳妆用的配制品 |
------A61K47/00 | 以所用的非有效成分为特征的医用配制品,如载体、惰性添加剂 |
--------A61K47/50 | .非有效成分被化学键合到有效成分上,例如聚合物-药物结合物 |
----------A61K47/66 | ..该改性剂是靶向特定细胞的涉及肽或蛋白质的预靶向系统 |
------------A61K47/68 | ...该改性剂是抗体、免疫球蛋白或其片段,例如Fc-片段 |