Title:
BIFUNCTIONAL COMPOUND USING UBR BOX DOMAIN-BINDING LIGAND
Document Type and Number:
WIPO Patent Application WO/2023/074936
Kind Code:
A1
Abstract:
The present disclosure relates to a bifunctional compound using a UBR box domain-binding ligand. The UBR box domain is a domain commonly present in the UBR (Ubiquitin protein ligase E3 component n-recognin) protein of the N-end rule pathway. In this regard, the UBR box domain is known as a domain to which a substrate binds. The UBR box domain binds to the N-terminal residue of a substrate, playing an essential role in forming multi-ubiquitin chains in the substrate, and it is known that the substrate is degraded through this process. Employing the UBR box domain ligand that takes advantage of the UBR box domain function, the bifunctional compound can be used to induce a desired target protein (or peptide) to be more effectively degraded.
Inventors:
KWON YONG TAE (KR)
KIM HYUN TAE (KR)
NA JEONG EUN (KR)
JI CHANG HOON (KR)
CHOI HA RIM (KR)
LEE JI EUN (KR)
JUNG CHANG AN (KR)
KOH AH RA (KR)
PARK SEON HO (KR)
KIM HYUN TAE (KR)
NA JEONG EUN (KR)
JI CHANG HOON (KR)
CHOI HA RIM (KR)
LEE JI EUN (KR)
JUNG CHANG AN (KR)
KOH AH RA (KR)
PARK SEON HO (KR)
Application Number:
PCT/KR2021/015256
Publication Date:
May 04, 2023
Filing Date:
October 27, 2021
Export Citation:
Assignee:
AUTOTAC INC (KR)
SEOUL NAT UNIV R&DB FOUNDATION (KR)
SEOUL NAT UNIV R&DB FOUNDATION (KR)
International Classes:
C07D295/04; C07C311/49; C07C317/28; C07D207/04; C07D209/08; C07D209/34; C07D211/14; C07D231/14; C07D277/36; C07D471/04
Foreign References:
| US20180222857A1 | 2018-08-09 | |||
| KR20200071098A | 2020-06-18 |
Other References:
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ROBERTS BRETT L., MA ZHI-XIONG, GAO ANG, LEISTEN ERIC D., YIN DAN, XU WEI, TANG WEIPING: "Two-Stage Strategy for Development of Proteolysis Targeting Chimeras and its Application for Estrogen Receptor Degraders", ACS CHEMICAL BIOLOGY, vol. 15, no. 6, 19 June 2020 (2020-06-19), pages 1487 - 1496, XP055953688, ISSN: 1554-8929, DOI: 10.1021/acschembio.0c00140
G. RASTELLI, ET AL.: "Discovery of new inhibitors of aldose reductase from molecular docking and database screening", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 10, no. 5, 1 May 2002 (2002-05-01), AMSTERDAM, NL, pages 1437 - 1450, XP002294365, ISSN: 0968-0896, DOI: 10.1016/S0968-0896(01)00410-2
ROBERTS BRETT L., MA ZHI-XIONG, GAO ANG, LEISTEN ERIC D., YIN DAN, XU WEI, TANG WEIPING: "Two-Stage Strategy for Development of Proteolysis Targeting Chimeras and its Application for Estrogen Receptor Degraders", ACS CHEMICAL BIOLOGY, vol. 15, no. 6, 19 June 2020 (2020-06-19), pages 1487 - 1496, XP055953688, ISSN: 1554-8929, DOI: 10.1021/acschembio.0c00140
G. RASTELLI, ET AL.: "Discovery of new inhibitors of aldose reductase from molecular docking and database screening", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 10, no. 5, 1 May 2002 (2002-05-01), AMSTERDAM, NL, pages 1437 - 1450, XP002294365, ISSN: 0968-0896, DOI: 10.1016/S0968-0896(01)00410-2
Attorney, Agent or Firm:
IPLAY PATENT LAW FIRM (KR)
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