Degradation of bruton's tyrosine kinase (BTK) by conjugation of BTK inhibitors to E3 ligase ligands and methods of use

• Main Authors: WANG HEXIANG, GUO YUNHANG, WANG ZHIWEI, HUO CHANGXIN, QI RUIPENG
• Format: Patent
• Language: Chinese; English
• Published: 11.03.2022
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

Disclosed herein are novel bifunctional compounds formed by conjugating a BTK inhibitor moiety to an E3 ligase ligand moiety, which compounds are used to recruit a targeted protein to an E3 ubiquitin ligase for degradation; as well as a preparation method and use thereof. 本文公开了新颖的双官能化合物，其通过BTK抑制剂部分与E3连接酶配体部分缀合而形成，所述化合物用以将靶向蛋白质募集至E3泛素连接酶来进行降解；以及其制备方法和用途。