On April 28, 2022, Weiss, Matthew M.; Zheng, Xiaozhang; Zhu, Xiao published a patent.Computed Properties of 87486-34-8 The title of the patent was Preparation of trifunctional compounds as IRAK4 degraders and uses thereof. And the patent contained the following:
The present application relates to novel trifunctional compounds, which function to recruit IRAK and BTK to E3 ubiquitin ligase for degradation, and methods of preparation and uses thereof. Compounds of formula I-IV wherein LBM is E3 ubiquitin ligase binding moiety; IBM is IRAK binding moiety capable of binding to one or more of IRAK1, IRAK2, IRAK3, IRAK4, preferably IRAK4; BBM is a BTK-binding moiety capable of binding to BTK; A is a bivalent moiety that connects LBM to IBM; B is a bivalent moiety that connects LBM to BBM; G is a bivalent moiety that connects IBM to BBM; D is a bivalent moiety that connects LBM to X; E is a bivalent moiety that connects IBM to X; F is a bivalent moiety that connects BBM to X; and X is a trivalent moiety that connects D, E, and F; and pharmaceutically acceptable salts thereof, are claimed. Example compound V was prepared by a multistep procedure (procedure given). All the invention compounds were evaluated for their targeted degradation of IRAK4 (data given). From the assay, it was determined that example compound V exhibited DC50 value of <1μM. The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).Computed Properties of 87486-34-8
The Article related to trifunctional compound preparation irak4 degrader, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Computed Properties of 87486-34-8