| abstract |
the present disclosure refers to bifunctional compounds, which find utility as modulators of the estrogen receptor (target protein). in particular, the present disclosure is directed to bifunctional compounds that contain, at one end, a cereblon, a von hippel-lindau ligase binding fraction, apoptosis protein inhibitors, or mouse homologous 2-minute ligand 2, which binds to the respective ubiquitin ligase e3 and, at the other end, a fraction that binds to the target protein, so that the target protein is placed in proximity to the ubiquitin ligase to effect the degradation (and inhibition) of the target protein. the present disclosure presents a wide range of pharmacological activities associated with the degradation / inhibition of the target protein. diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with the compounds and compositions of the present disclosure. |