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Title:
BIOACTIVE CONJUGATE, PREPARATION METHOD THEREFOR AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2019/114666
Kind Code:
A1
Abstract:
The present invention relates to a bioactive conjugate, a preparation method therefor, and use thereof. In particular, the present invention relates to a novel type of bioactive molecular conjugates obtained by improving the coupling of a drug to a targeted moiety in ADC or SMDC, a preparation method therefor, and use thereof in the preparation of drugs for treating diseases associated with abnormal cellular activity.

Inventors:
CAI, Jiaqiang (No. 666, Xinhua Avenue Hai Xia Industrial Park, Wenjiang Distric, Chengdu Sichuan 8, 611138, CN)
SONG, Shuai (No. 666, Xinhua Avenue Hai Xia Industrial Park, Wenjiang Distric, Chengdu Sichuan 8, 611138, CN)
XUE, Tongtong (No. 666, Xinhua Avenue Hai Xia Industrial Park, Wenjiang Distric, Chengdu Sichuan 8, 611138, CN)
XIAO, Liang (No. 666, Xinhua Avenue Hai Xia Industrial Park, Wenjiang Distric, Chengdu Sichuan 8, 611138, CN)
DENG, Hanwen (No. 666, Xinhua Avenue Hai Xia Industrial Park, Wenjiang Distric, Chengdu Sichuan 8, 611138, CN)
TIAN, Qiang (No. 666, Xinhua Avenue Hai Xia Industrial Park, Wenjiang Distric, Chengdu Sichuan 8, 611138, CN)
WANG, Jing (No. 666, Xinhua Avenue Hai Xia Industrial Park, Wenjiang Distric, Chengdu Sichuan 8, 611138, CN)
LIU, Dengnian (No. 666, Xinhua Avenue Hai Xia Industrial Park, Wenjiang Distric, Chengdu Sichuan 8, 611138, CN)
LIU, Liping (No. 666, Xinhua Avenue Hai Xia Industrial Park, Wenjiang Distric, Chengdu Sichuan 8, 611138, CN)
YU, Haimin (No. 666, Xinhua Avenue Hai Xia Industrial Park, Wenjiang Distric, Chengdu Sichuan 8, 611138, CN)
YANG, Zhouning (No. 666, Xinhua Avenue Hai Xia Industrial Park, Wenjiang Distric, Chengdu Sichuan 8, 611138, CN)
CAO, Xu (No. 666, Xinhua Avenue Hai Xia Industrial Park, Wenjiang Distric, Chengdu Sichuan 8, 611138, CN)
ZHONG, Guoqing (No. 666, Xinhua Avenue Hai Xia Industrial Park, Wenjiang Distric, Chengdu Sichuan 8, 611138, CN)
WANG, Lichun (No. 666, Xinhua Avenue Hai Xia Industrial Park, Wenjiang Distric, Chengdu Sichuan 8, 611138, CN)
WANG, Jingyi (No. 666, Xinhua Avenue Hai Xia Industrial Park, Wenjiang Distric, Chengdu Sichuan 8, 611138, CN)
Application Number:
CN2018/120125
Publication Date:
June 20, 2019
Filing Date:
December 10, 2018
Export Citation:
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Assignee:
SICHUAN KELUN-BIOTECH BIOPHARMACEUTICAL CO., LTD. (No. 666, Xinhua Avenue Hai Xia Industrial Park, Wenjiang Distric, Chengdu Sichuan 8, 611138, CN)
International Classes:
C07K7/02; A61K31/506; A61K45/00; A61P35/00; C07D491/22; C07K5/062
Domestic Patent References:
WO2014144878A22014-09-18
Other References:
TODA, N. ET AL.: "Rapid, Stable, Chemoselective Labeling of Thiols with Julia-Kocienski-Like Reagents: A Serum-Stable Alternative to Maleimide-Based Protein Conjugation", ANGEWANDTE CHEMI INTERNATIONAL EDITION, vol. 52, no. 48, 2 October 2013 (2013-10-02), pages 12592 - 12596, XP055416940, DOI: doi:10.1002/anie.201306241
LI, XIULING ET AL.: "Site-Specific Dual Antibody Conjugation via Engineered Cysteine and Selenocysteine Residues", BIOCONJUGATE CHEMISTRY, vol. 26, no. 11, 18 November 2015 (2015-11-18), pages 2243 - 2248, XP055416982, DOI: doi:10.1021/acs.bioconjchem.5b00244
PATTERSON, J.T. ET AL.: "Improving the Serum Stability of Site-Specific Antibody Conjugates with Sulfone Linkers", BIOCONJUGATE CHEMISTRY, vol. 25, no. 8, 20 August 2014 (2014-08-20), pages 1402 - 1407, XP055338868, DOI: doi:10.1021/bc500276m
LIANG, XIAOFEI ET AL.: "Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3- (trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL- ABL-053) as a Potent, Selective, and Orally Available BCR-ABUSRC/p38 Kinase Inhibitor for Chronic Myeloid Leukemia", JOURNAL OF MEDICINAL CHEMISTRY, vol. 59, 31 December 2016 (2016-12-31), pages 1984 - 2004, XP055603365, DOI: doi:10.1021/acs.jmedchem.5b01618
Attorney, Agent or Firm:
CCPIT PATENT AND TRADEMARK LAW OFFICE (8th Floor, Vantone New World Plaza2 Fuchengmenwai Stree, Xicheng District Beijing 7, 100037, CN)
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