Degradation of cyclin-dependent kinase 4/6 (CDK4/6) by conjugation of CDK4/6 inhibitors with E3 ligase ligand and methods of use
US10865204B2 · kind B2 · utility
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Key dates
| Filing date | Apr 21, 2017 |
| Grant date | Dec 15, 2020 |
| Priority date | — |
| Expiry date | Apr 21, 2037 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D487/04
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The present application provides bifunctional compounds of Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which act as protein degradation inducing moieties for cyclin-dependent kinase 4 (CDK4) and/or cyclin-dependent kinase 6 (CDK6). The present application also relates to methods for the targeted degradation of CDK4 and/or CDK6 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to CDK4 and/or CDK6 which can be utilized in the treatment of disorders modulated by CDK4 and/or CDK6.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.