On October 10, 2019, Crew, Andrew P.; Hornberger, Keith R.; Wang, Jing; Dong, Hanqing; Berlin, Michael; Crews, Craig M. published a patent.SDS of cas: 1211568-27-2 The title of the patent was Preparation of bifunctional compounds as modulators of proteolysis useful for treating cancer. And the patent contained the following:
The present disclosure relates to bifunctional compounds ULM-L-PTM [the ULM = a small mol. E3 ubiquitin ligase binding moiety that binds an E3 ubiquitin ligase;the PTM = a small mol. comprising a Kirsten rat sarcoma protein (KRas) targeting moiety; the L = a bond or a chem. linking moiety connecting the ULM and the PTM] or pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, polymorphs or prodrugs thereof, which find utility as modulators of Kirsten rat sarcoma protein (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, inhibitors of apoptosis proteins (IAP) 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. Over 500 title compounds were prepared E.g., a multi-step synthesis of I, starting from 2,2,5-trimethyl-4-oxo-3,8,11-trioxa-5-azatridecan-13-yl 4-methylbenzenesulfonate and 2-(2,6-dioxopiperidin-3-yl)-5-hydroxyisoindoline-1,3-dione, was described. The present disclosure exhibits a broad range of pharmacol. activities associated with degradation/inhibition of target protein (data given for representative title compounds). Diseases or disorders that result from aggregation, accumulation, and/or overactivation of the target protein are treated or prevented with compounds and compositions of the present disclosure. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).SDS of cas: 1211568-27-2
The Article related to bifunctional compound preparation kras modulator antitumor e3 ubiquitin ligase, von hippel lindau cereblon protein bifunctional compound preparation antitumor, apoptosis protein inhibitor antitumor bifunctional compound quinazolinamine preparation, mouse double minute 2 homolog mdm2 bifunctional compound preparation and other aspects.SDS of cas: 1211568-27-2
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Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics