Degradation of cyclin-dependent kinase 8 (CDK8) by conjugation of CDK8 inhibitors with E3 ligase ligand and methods of use
US11247991B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Oct 29, 2020 |
| Grant date | Feb 15, 2022 |
| Priority date | — |
| Expiry date | Oct 29, 2040 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P35/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The present application provides bifunctional compounds of Formula (Ia) or (Ib): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which act as protein degradation inducing moieties for cyclin-dependent kinase 8 (CDK8). The present application also relates to methods for the targeted degradation of CDK8 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to CDK8 which can be utilized in the treatment of disorders modulated by CDK8.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.