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Title:
CAMPTOTHECIN DERIVATIVES THAT BIND TO DDX5 PROTEIN AND PRODRUGS THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/204631
Kind Code:
A1
Abstract:
The present invention relates to: (a) an active camptothecin derivative represented by chemical formula 1, which is designed to bind to a DDX5 protein or E3 ligase; (b) a prodrug thereof designed to release the active camptothecin derivative (a) at a target site in vivo; or (c) a complex containing a DDX5 protein-targeting ligand, in which the ability of the active camptothecin derivative (a) or an FL118 compound of chemical formula 2 to inhibit type 1 topoisomerase is inactivated by connecting a linker. The active camptothecin derivative designed according to the present invention can bind to the DDX5 protein in cells, thereby inducing cell death through DDX5 protein degradation.

Inventors:
JUNG DOO YOUNG (KR)
LEE JIN SOO (KR)
CHO HYUN YONG (KR)
LEE BYEONG SUNG (KR)
JUNG JIN KYO (KR)
SHIN SEUNG GUN (KR)
KWEN SO HUI (KR)
RAO MATHI GANGADHAR (KR)
Application Number:
PCT/KR2023/005380
Publication Date:
October 26, 2023
Filing Date:
April 20, 2023
Export Citation:
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Assignee:
PINOTBIO INC (KR)
International Classes:
C07D491/22; A61K31/4745; A61K47/65; A61K47/68; A61P35/00; G01N33/574
Domestic Patent References:
WO2022170971A12022-08-18
Foreign References:
KR20210053871A2021-05-12
KR20210006362A2021-01-18
US5496830A1996-03-05
Other References:
ZHAO XINGKAI, BAO MIAO, ZHANG FENGMIN, WANG WENBO: "Camptothecin induced DDX5 degradation increased the camptothecin resistance of osteosarcoma", EXPERIMENTAL CELL RESEARCH, ELSEVIER, AMSTERDAM, NL, vol. 394, no. 2, 1 September 2020 (2020-09-01), AMSTERDAM, NL , pages 112148, XP093098139, ISSN: 0014-4827, DOI: 10.1016/j.yexcr.2020.112148
LIU YUANQI, DUAN CHAOJUN, ZHANG CHUNFANG: "E3 Ubiquitin Ligase in Anticancer Drugdsla Resistance: Recent Advances and Future Potential", FRONTIERS IN PHARMACOLOGY, vol. 12, 15 April 2021 (2021-04-15), pages .645864, XP093098140, DOI: 10.3389/fphar.2021.645864
Attorney, Agent or Firm:
IPUS PATENT & LAW FIRM (KR)
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