BIFUNCTIONAL LINKS FOR BTK DECLARATION VIA THE UBIQUITIN-PROTEOSOME SIGNAL PATHWAY
Patent Information
- Application Number
- DE602019065172
- Authority / Receiving Office
- DE · DE
- Patent Type
- Patents
- Current Assignee / Owner
- Filing Date
- 2019-11-08
- Publication Date
- 2025-01-22
- Estimated Expiration
- 2039-11-08
AI Technical Summary
There is a need for bifunctional molecules that can induce the proteolytic degradation of Bruton's tyrosine kinases (BTK) via a ubiquitin proteolytic pathway, as current methods may not effectively target all forms of BTK, including the C481S mutated form which confers resistance to inhibition by ibrutinib.
The development of bifunctional compounds of Formula (I) and their pharmaceutically acceptable salts, which recruit BTK to a ubiquitin ligase, promoting ubiquitylation and proteasomal degradation of BTK, thereby effectively degrading BTK protein and eliminating its kinase activity.
These compounds induce the proteolytic degradation of BTK, potentially offering a distinct mechanism of action compared to stoichiometric inhibition, and effectively targeting BTK, including the C481S mutated form, which is resistant to traditional inhibitors.