Title:
DDX5 PROTEIN-BINDING CAMPTOTHECIN DERIVATIVES AND PRODRUGS THEREOF
Document Type and Number:
WIPO Patent Application WO/2024/014837
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 and E3 ligase; (b) a prodrug thereof designed to release the active camptothecin derivative (a) at a target site in vivo, and preferably an antibody-drug conjugate (ADC); 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 SOHUI (KR)
RAO MATHI GANGADHAR (KR)
LEE JIN SOO (KR)
CHO HYUN YONG (KR)
LEE BYEONG SUNG (KR)
JUNG JIN KYO (KR)
SHIN SEUNG GUN (KR)
KWEN SOHUI (KR)
RAO MATHI GANGADHAR (KR)
Application Number:
PCT/KR2023/009854
Publication Date:
January 18, 2024
Filing Date:
July 11, 2023
Export Citation:
Assignee:
PINOTBIO INC (KR)
International Classes:
C07D491/22; A61K31/4745; A61K47/65; A61K47/68; A61P35/00; G01N33/574
Domestic Patent References:
| WO2022121981A1 | 2022-06-16 | |||
| WO2022015110A1 | 2022-01-20 | |||
| WO2022170971A1 | 2022-08-18 |
Foreign References:
| US20170360770A1 | 2017-12-21 |
Other References:
LING, X. ET AL.: "FL118, a novel camptothecin analogue, overcomes irinotecan and topotecan resistance in human tumor xenograft models.", AMERICAN JOURNAL OF TRANSLATIONAL RESEARCH., vol. 7, no. 10, 2015, pages 1765 - 1781, XP055887850
ZHANG, Y ET AL.: "Self-assembling nanoparticles of dually hydrophobic prodrugs constructed from camptothecin analogue for cancer therapy", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 200, no. 112365, 30 April 2020 (2020-04-30), pages 1 - 11, XP086205559, DOI: 10.1016/j.ejmech.2020.112365
ZHANG, Y ET AL.: "Self-assembling nanoparticles of dually hydrophobic prodrugs constructed from camptothecin analogue for cancer therapy", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 200, no. 112365, 30 April 2020 (2020-04-30), pages 1 - 11, XP086205559, DOI: 10.1016/j.ejmech.2020.112365
Attorney, Agent or Firm:
IPUS PATENT & LAW FIRM (KR)
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