Compound for targeted degradation of Btk and anti-tumor application thereof

• Main Authors: LUO FENGJUN, SHU YONGZHI
• Format: Patent
• Language: Chinese; English
• Published: 21.02.2023
• 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

The invention provides a compound for targeted degradation of Btk and an anti-tumor application thereof, specifically, a series of compounds are prepared and screened, the inhibition and degradation activity of the compounds on Bruton's tyrosine protein kinase (Btk) is verified, and finally, the compounds with good druggability are found. The compound can be used for treating diseases related to the activity or expression quantity of Bruton's tyrosine protein kinase (Btk). 本发明提供了靶向降解Btk的化合物及其抗肿瘤用途，具体地，本发明制备并筛选了一系列的化合物，并验证了这些化合物对布鲁顿酪氨酸蛋白激酶(Btk)抑制和降解活性，最终发现了具备良好成药性的化合物，可以用于治疗与布鲁顿酪氨酸蛋白激酶(Btk)活性或表达量相关的疾病。