On June 7, 2018, Crew, Andrew P.; Qian, Yimin; Dong, Hanqing; Wang, Jing; Hornberger, Keith R.; Crews, Craig M. published a patent.Related Products of 1251006-64-0 The title of the patent was Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders and their preparation. 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 formula I and II, 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 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. The disclosure exhibits a broad range of pharmacol. activities associated with degradation/inhibition of target protein. Compounds of formula I and II wherein ULM is a small mol. E3 ubiquitin ligase binding moiety that binds and E3 ubiquitin ligase; L is a bond and a chem. linking moiety; each X is independently CH and N; R1 is mono-, di- and trisubstitution and is independently OH, halo, alkoxy, MeO, EtO and acyloxy; R2 is mono- or disubstitution and is independently H, halo, CN, (un)branched alkyl, etc.; R3 is mono- or disubstitution and is independently H, and halo; R4 is H, alkyl, Me and Et; and pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, polymorphs, and prodrugs thereof, are claimed. Example compound III was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their estrogen receptor degradation activity. From the assay, it was determined that compound III exhibited IC50 value of 0.35 nM. The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).Related Products of 1251006-64-0
The Article related to tetrahydronaphthalene tetrahydroisoquinoline preparation estrogen receptor degrader, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Related Products of 1251006-64-0
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem