Modulators of estrogen receptor proteolysis and associated methods of use
US10604506B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Jan 26, 2018 |
| Grant date | Mar 31, 2020 |
| Priority date | — |
| Expiry date | Jan 26, 2038 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D471/04
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The present disclosure relates to bifunctional compounds, which find utility as modulators of estrogen receptor (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a cereblon, Von Hippel-Lindau ligase-binding moiety, 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, 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 are treated or prevented with compounds and compositions of the present disclosure.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.