Bifunctional degraders with electrophilic PROTACs
Summary
The USPTO has published a patent application (US20260083722A1) detailing bifunctional degraders comprising electrophilic PROTACs that engage DCAF1. The application was filed on May 19, 2023, and published with a projected application date of March 26, 2026.
What changed
This document is a publication of a United States patent application (US20260083722A1) filed on May 19, 2023, concerning bifunctional degraders with electrophilic PROTACs that engage DCAF1. The application describes compounds of Formula A-B-C, where A is a ligand to a protein of interest, B is a linker, and C is a ligand to DCAF1, specifically comprising an azetidinyl acrylamide that forms a covalent bond with C1113 of DCAF1 via Michael addition.
As this is a patent application publication, it does not impose immediate regulatory obligations or compliance deadlines on regulated entities. However, it signals potential future patent protection and innovation in the field of targeted protein degradation, which may impact drug development strategies for pharmaceutical companies and drug manufacturers. Compliance officers should note this as a development in intellectual property within the pharmaceutical sector.
Archived snapshot
Mar 26, 2026GovPing captured this document from the original source. If the source has since changed or been removed, this is the text as it existed at that time.
BIFUNCTIONAL DEGRADERS COMPRISING ELECTROPHILIC PROTACS THAT ENGAGE DCAF1 AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME
Application US20260083722A1 Kind: A1 Mar 26, 2026
Inventors
Benjamin F. CRAVATT, Yongfeng TAO, Xiaoyu ZHANG, Dave REMILLARD, Ekaterina VINOGRADOVA, Minoru YOKOYAMA, Bruno MELILLO, Stuart SCHREIBER
Abstract
Disclosed are bifunctional degraders comprising electrophilic PRO-TACs that engage DCAF1 and pharmaceutical compositions comprising the same. The bifunctional degraders are of Formula A-B-C wherein, A is a ligand to a protein of interest, B is a linker that is a bond or a chemical linker that is chemically linked to A and C, and C is a ligand to the E3 ligase substrate receptor DCAF1, wherein the protein of interest is any protein having a ligand that can form a covalent bond with the linker B; and C comprises an azetidinyl acrylamide that forms a covalent bond with C1113 of DCAF1 through a Michael addition reaction.
CPC Classifications
A61K 31/4709 A61K 31/4725 A61K 31/501 A61K 31/506 A61K 31/541 A61K 31/551 A61K 31/635 A61K 47/545 A61K 47/64 C07D 401/12 C07D 401/14 C07D 405/14
Filing Date
2023-05-19
Application No.
18866614
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