On August 1, 2019, Gray, Nathanael S.; Wang, Jinhua; Dobrovolsky, Dennis published a patent.Reference of 3,5-Dibromo-1-methylpyrazin-2(1H)-one The title of the patent was Preparation of heterocycles as bifunctional compounds that targeting degradation of Bruton’s tyrosine kinase (BTK) by conjugation of BTK inhibitors with E3 ligase ligand for the treatment of BTK-mediated diseases. And the patent contained the following:
The invention relates to preparation of bifunctional compounds of formula (Targeting Ligand-Linker-Degron) wherein the Targeting Ligand is capable of binding to BTK; the Linker is a group that covalently binds to the Targeting Ligand and the Degron; and the Degron is capable of binding to a ubiquitin ligase, or an enantiomer, diastereomer, or stereoisomer thereof, or pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, which act as protein degradation inducing moieties for Bruton’s tyrosine kinase (BTK). The example compound I was prepared via three-steps synthetic procedure (procedure given). The present application also relates to methods for the targeted degradation of BTK through the use of bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to BTK which can be utilized in the treatment of disorders modulated by BTK. The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).Reference of 3,5-Dibromo-1-methylpyrazin-2(1H)-one
The Article related to dioxoindoline piperazine benzamide preparation btk modulator disease treatment prophylaxis, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Reference of 3,5-Dibromo-1-methylpyrazin-2(1H)-one