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Title:
DI-SUBSTITUTED MALEIC AMIDE LINKER FOR ANTIBODY-DRUG CONJUGATING AND PREPARATION METHOD AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2018/095422
Kind Code:
A1
Abstract:
Provided in the present invention are a di-substituted maleic amide linker conjugated to an antibody and a preparation method and use thereof. In particular, the present invention conjugates a strongly cytotoxic active substance to a biomacromolecule through a class of new linkers. The class of linkers can selectively act simultaneously with disulphide chains, so as to greatly improve the substance homogeneity of a conjugate. The conjugate prepared by the linker of the present invention has a high inhibitory activity on a cell strain expressing the corresponding antigen. Also provided is a method for preparing the above-mentioned conjugate and the use.

Inventors:
SHEN, Jingkang (555 Zuchongzhi Road, Shanghai 3, 201203, CN)
MENG, Tao (555 Zuchongzhi Road, Shanghai 3, 201203, CN)
MA, Lanping (555 Zuchongzhi Road, Shanghai 3, 201203, CN)
WANG, Xin (555 Zuchongzhi Road, Shanghai 3, 201203, CN)
PENG, Hongli (555 Zuchongzhi Road, Shanghai 3, 201203, CN)
ZHANG, Yongliang (555 Zuchongzhi Road, Shanghai 3, 201203, CN)
YU, Ting (555 Zuchongzhi Road, Shanghai 3, 201203, CN)
CHEN, Lin (555 Zuchongzhi Road, Shanghai 3, 201203, CN)
DU, Zhiyan (555 Zuchongzhi Road, Shanghai 3, 201203, CN)
WANG, Ying (555 Zuchongzhi Road, Shanghai 3, 201203, CN)
Application Number:
CN2017/112958
Publication Date:
May 31, 2018
Filing Date:
November 24, 2017
Export Citation:
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Assignee:
SHANGHAI QINGRUN PHARMACEUTICAL TECHNOLOGY CO., LTD (F2 Building 3#, No.86 Faladi Road Pudong New Area, Shanghai 3, 201203, CN)
International Classes:
C07D207/456; A61K31/5365; A61K47/68; A61P35/00; C07D401/14; C07D403/14; C07D491/18; C07D519/00; C07K5/027; C07K7/02
Domestic Patent References:
WO2014197871A22014-12-11
WO2014197871A22014-12-11
Foreign References:
CN105102455A2015-11-25
CN104379168A2015-02-25
CN200480019814A2004-07-12
CN201380025774A2013-05-14
CN201310025021A2013-01-23
Other References:
MILLER ET AL., JOUR. OF IMMUNOLOGY, vol. 170, 2003, pages 4854 - 4861
JANEWAY, C.TRAVERS, P.WALPORT, M.SHLOMCHIK: "Immuno Biology", 2001, GARLAND PUBLISHING
OLAFSEN ET AL., PROTEIN ENG. DESIGN & SEL., vol. 17, no. 4, 2004, pages 315 - 323
"GenBank", Database accession no. GM832119.1
Attorney, Agent or Firm:
ZHEJIANG HANGZHOU JINTONG PATENT OFFICE CO., LTD (19th Floor, Shengkexie BuildingNo.8 Wulin Square, Xiacheng Distric, Hangzhou Zhejiang 3, 310003, CN)
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