On October 8, 2020, Yang, Bin; Hayhow, Thomas George Christopher; Fallan, Charlene; Scott, James Stewart; Diene, Coura; Barlaam, Bernard Christophe; Nissink, Johannes Wilhelmus Maria published a patent.Application of 1211568-27-2 The title of the patent was Pyrimidinyltetrahydropyridoindoles as estrogen receptor degrading PROTACs and their preparation. And the patent contained the following:
The specification relates to compounds of formula I and pharmaceutically acceptable salts thereof. This specification also relates to the use of such compounds and pharmaceutically acceptable salts thereof in methods of treatment of the human or animal body, for example in prevention or treatment of cancer. This specification also relates to processes and intermediate compounds involved in the preparation of such compounds and to pharmaceutical compositions containing them. Compounds of formula I wherein A and G are independently CR5 and N; E and Q are independently CH and N; R1 and R2 are H; R1R2 can be taken together to form oxo; R3 and R4 are independently H and OMe; R5 is H, F, Cl, CN, Me and OMe; R6 and R7 are independently H, Me and F; R6R7 can be taken together to form cyclopropyl and oxetanyl; R8 is H, Me, F, CH2F, CN, etc.; Linker is (un)substituted. (un)branched, (un)cyclized, (un)saturated 6 to 15 carbon atom moiety where 1 ot 6 carbon atoms may optionally be replaced with O, N and S; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their estrogen binding affinity and estrogen degradation activity. From the assay, it was determined that compound II exhibited IC50 values of 3.1 nM and 1.1 nM toward ER binding and ER degradation, resp. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Application of 1211568-27-2
The Article related to pyrimidinylpyridoindole preparation er degrading protac, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application of 1211568-27-2
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics