On April 12, 2018, Crew, Andrew P.; Hornberger, Keith R.; Snyder, Lawrence B.; Zimmermann, Kurt; Wang, Jing; Berlin, Michael; Crews, Craig M.; Dong, Hanqing published a patent.Category: piperazines The title of the patent was Preparation of bifunctional compounds for the targeted degradation of androgen receptor. And the patent contained the following:
The invention relates to bifunctional compounds, which find utility to degrade and (inhibit) androgen receptor. In particular, the invention is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds androgen receptor, such that androgen receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of androgen receptor. The invention exhibits a broad range of pharmacol. activities associated with compounds according to the present invention, consistent with the degradation/inhibition of androgen receptor (data given). The invention compounds are claimed to be useful for the treatment of cancer or Kennedy’s disease, or both. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Category: piperazines
The Article related to protac modulator preparation targeted ubiquitination androgen receptor degradation inhibition, preparation bifunctional compound degradation androgen receptor, treatment cancer kennedy disease preparation bifunctional compound and other aspects.Category: piperazines
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics