On March 20, 2008, Whitney, James A.; Di Paolo, Julie; Valleca, Mark A.; Brittelli, David R.; Currie, Kevin S.; Darrow, James W.; Kropf, Jeffrey E.; Lee, Tony; Gallion, Steven L.; Mitchell, Scott A.; Pippen, Douglas A.I.; Blomgren, Peter A.; Stafford, Douglas Gregory published a patent.COA of Formula: C5H4Br2N2O The title of the patent was Preparation of substituted amides as Btk kinase inhibitors. And the patent contained the following:
Methods of inhibiting Btk activity by inhibiting phosphorylation of Y551 of Btk, methods of treating patients by inhibiting Btk activity by inhibiting phosphorylation of Y551 of Btk, chem. entities that bind to Btk and inhibited complexes are provided. Thus, the title compounds I [R = (un)substituted cycloalkyl, aryl, heteroaryl; M = a bond, CH:CH; Q = CR10R11NR12, NR12CR10R11, NR13CO, CONR13, NR14CONR15 (R10, R11 = H, alkyl, haloalkyl; R12-R15 = H, alkyl, haloalkyl, etc.); Z = (un)substituted phenylene, pyridylidene; W = (un)substituted heteroaryl other than imidazo[1,2-a]pyrazine; D = hydrogen bond donor other than H; with the proviso] were prepared E.g., a multi-step synthesis of II, starting from 3,5-dibromo-1H-pyridin-2-one, was given. Exemplified compounds I were tested in the Btk assay and certain of those compounds exhibited an IC50 value less than or equal to 1 μM. Some of the compounds I were tested in the B-cell proliferation assay and exhibited an IC50 value less than or equal to 10 μM. The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).COA of Formula: C5H4Br2N2O
The Article related to amide preparation bruton’s tyrosine kinase btk kinase inhibitor, y551 btk phosphorylation inhibitor amide preparation, b cell proliferation inhibitor amide preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.COA of Formula: C5H4Br2N2O