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Title:
OLIGOSACCHARIDE LINKER AND SIDE-CHAIN HYDROPHILIC FRAGMENT COMBINED GLYCOSITE-SPECIFIC ANTIBODY-DRUG CONJUGATE, AND PREPARATION METHOD THEREFOR AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/011639
Kind Code:
A1
Abstract:
Provided in the present invention are a class of new oligosaccharide linkers and a linking method. By taking a conserved glycosylation site on an antibody as a coupling site, a biantennary oligosaccharide as a linker structure, and structures such as an aldehyde group with a terminal modified with sialic acid and a terminal modified with galactose as a linking residue, a series of small molecule compounds are coupled. In addition, provided in the present invention are a method for synthesizing the oligosaccharide linker, a method for preparing a small molecule drug, and a method for preparing an antibody-drug conjugate. In addition, provided in the present invention are a test result of a candidate compound at a cell activity level and the use of the antibody-drug conjugate or a drug combination in anti-tumor drugs, anti-inflammatory drugs, antiviral drugs, anti-infection drugs or other immunotherapy drugs.

Inventors:
HUANG WEI (CN)
TANG FENG (CN)
SHI WEI (CN)
LI WANZHEN (CN)
Application Number:
PCT/CN2022/110600
Publication Date:
February 09, 2023
Filing Date:
August 05, 2022
Export Citation:
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Assignee:
SHANGHAI INST MATERIA MEDICA CAS (CN)
International Classes:
C08B37/00; A61K47/54; A61K47/68
Domestic Patent References:
WO2020196474A12020-10-01
Foreign References:
CN107778372A2018-03-09
CN109462989A2019-03-12
CN112714649A2021-04-27
Other References:
TANG FENG: "Engases-Catalyzed Glycoengineering of Glycoproteins and Novel Antibody Drug Discovery", CHINESE DOCTORAL DISSERTATIONS FULL-TEXT DATABASE, UNIVERSITY OF CHINESE ACADEMY OF SCIENCES, CN, no. 12, 15 December 2018 (2018-12-15), CN , XP093032341, ISSN: 1674-022X
TANG FENG; ZHOU MANG; QIN KEN; SHI WEI; YASHINOV ANSOR; YANG YANG; YANG LIYUN; GUAN DONGLIANG; ZHAO LEI; TANG YUBO; CHANG YUJIE; Z: "Selective-glycan editing on living cell surfaces to probe glycoconjugate function", NATURE CHEMICAL BIOLOGY, NATURE PUBLISHING GROUP US, NEW YORK, vol. 16, no. 7, 1 June 2020 (2020-06-01), New York, pages 766 - 775, XP037175987, ISSN: 1552-4450, DOI: 10.1038/s41589-020-0551-8
"Methods Mol Biol", vol. 2033, 23 July 2019, HUMANA PRESS, Totowa, NJ, ISBN: 978-1-62703-562-0, ISSN: 1064-3745, article TANG FENG, SHI WEI, HUANG WEI: "Homogeneous Antibody–Drug Conjugates via Glycoengineering", pages: 221 - 238, XP009543195, DOI: 10.1007/978-1-4939-9654-4_15
TANG FENG; WANG LAI-XI; HUANG WEI: "Chemoenzymatic synthesis of glycoengineered IgG antibodies and glycosite-specific antibody–drug conjugates", NATURE PROTOCOLS, NATURE PUBLISHING GROUP, GB, vol. 12, no. 8, 27 July 2017 (2017-07-27), GB , pages 1702 - 1721, XP037551079, ISSN: 1754-2189, DOI: 10.1038/nprot.2017.058
SONG YAKAI, DENG XIAOJIE, SHI WEI, TANG FENG, HUANG WEI, GONG LIKUN, QIN QIUPING: "A homogeneous time-resolved fluorometric energy transfer assay for the binding assessment of FcRn with IgG antibodies", JOURNAL OF IMMUNOLOGICAL METHODS, ELSEVIER SCIENCE PUBLISHERS B.V.,AMSTERDAM., NL, vol. 499, 1 December 2021 (2021-12-01), NL , pages 113180, XP093032337, ISSN: 0022-1759, DOI: 10.1016/j.jim.2021.113180
Attorney, Agent or Firm:
XU & PARTNERS, LLC. (CN)
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