Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
US11173211B2 · kind B2 · utility
Assignees
Inventors
Key dates
| Filing date | Sep 7, 2019 |
| Grant date | Nov 16, 2021 |
| Priority date | — |
| Expiry date | Sep 7, 2039 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D519/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The present disclosure relates to bifunctional compounds, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A-RAF and/or B-RAF; the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein RAF, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein, or the constitutive activation of the target protein, are treated or prevented with compounds and compositions of the present disclosure.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.