On July 7, 2022, Huo, Changxin; Wang, Hexiang; Lv, Gang; Wang, Zhiwei; Liu, Huaqing published a patent.COA of Formula: C15H29N3O2 The title of the patent was Degradation of bruton’s tyrosine kinase (BTK) by conjugation of BTK inhibitors with E3 ligase ligand and methods of use. And the patent contained the following:
Disclosed herein are novel bifunctional compounds formed by conjugating BTK inhibitor moieties with E3 ligase ligand moieties, which function to recruit targeted proteins to E3 ubiquitin ligase for degradation, and methods of preparation and uses thereof. The title compounds I [ring A and B = (independently) an aromatic ring comprising 0-3 heteroatoms selected from N, S and O as ring member(s); Z1-Z4 = (independently) N or CRz; L = (independently) a bond, alkylene, O, etc.; m, n and q = (independently) 0-4; t = 0-2; R1 and R2 = (independently) H, alkyl, cycloalkyl, etc.; R3, R5 and R6 = (independently) H, halo, alkyl, etc.; Rz = the bond between moiety and Linker-Degron moiety, H, halo, etc.; the Linker = a bond or a divalent linking group; and the Degron = E3 Ubiquitin ligase moiety] or pharmaceutically acceptable salts thereof, were prepared E.g., a multi-step synthesis of II, starting from 4-phenoxybenzaldehyde and 4-methylbenzenesulfonohydrazide, was described. Exemplified compounds I were evaluated for their activity as BTK degradation (data given). Pharmaceutical composition comprising compound I was disclosed. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).COA of Formula: C15H29N3O2
The Article related to bifunctional compound preparation bruton’s tyrosine kinase btk degradation, targeted protein degrader btk e3 ubiquitin ligase bifunctional compound, btk inhibitor e3 ligase conjugation bifunctional compound preparation and other aspects.COA of Formula: C15H29N3O2
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics