Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders
US10647698B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Dec 1, 2017 |
| Grant date | May 12, 2020 |
| Priority date | — |
| Expiry date | Jan 30, 2038 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07K5/06034
- WIPO fieldPharmaceuticals
- 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 at least one of a Von Hippel-Lindau ligand, a cereblon ligand, Inhibitors of Apoptosis Proteins ligand, mouse double-minute homolog 2 ligand, or a combination thereof, 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.