On August 2, 2018, Qian, Yimin; Crew, Andrew P.; Crews, Craig M.; Dong, Hanqing; Hornberger, Keith R.; Wang, Jing published a patent.Related Products of 882518-89-0 The title of the patent was Preparation of substituted benzothiophenes as modulators of estrogen receptor proteolysis and associated methods of use. And the patent contained the following:
The disclosure relates to bifunctional compounds of formulas I and II, which find utility as modulators of estrogen receptor (target protein). In particular, the disclosure is directed to bifunctional compounds of formulas I and II, 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 resp. 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. Compounds of formulas I and II wherein ULM is a small mol. E3 ubiquitin ligase binding moiety that binds or targets and E3 ubiquitin ligase; L is a chem. linker; X is O and CO; X1 and X2 are independently N and HC; R1 is OH, alkanoyloxy, aroyloxy and lower alkoxy; R2 and R4 are independently H, OH, halo, CN, CF3, etc.; R3 and R5 are independently H and halo; with provisions; and pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, polymorphs and prodrugs thereof, are claimed. The disclosure exhibits a broad range of pharmacol. 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 disclosure. Example compound III was prepared by a general procedure (procedure given). The invention compounds were evaluated for their estrogen receptor proteolysis modulatory activity. From the assay, it was determined that compound III exhibited IC50 value of 12.7 nM. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).Related Products of 882518-89-0
The Article related to benzothiophene preparation estrogen receptor proteolysis modulator, Heterocyclic Compounds (One Hetero Atom): Areno- and Diarenothiophenes and other aspects.Related Products of 882518-89-0
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics