On September 21, 2006, Brittelli, David R.; Currie, Kevin S.; Darrow, James W.; Kropf, Jeffrey E.; Lee, Seung H.; Gallion, Steven L.; Mitchell, Scott A.; Pippin, Douglas A. I.; Blomgren, Peter A. published a patent.Electric Literature of 87486-34-8 The title of the patent was Preparation of substituted amides as Btk inhibitors. And the patent contained the following:
At least one chem. entity chosen from compounds I [R = (un)substituted cycloalkyl, aryl, heteroaryl; M = a bond, CH:CH; Q = CR10R11NR12, NR12CR10R11, NR13CO, CONR13, NR14CONR15 (wherein R10, R11 = H, alkyl, haloalkyl; R12-R15 = H, alkyl, haloalkyl, Ph, etc.); Z = (un)substituted phenylene, pyridylidene; W = (un)substituted heteroaryl other than imidazo[1,2-a]pyrazine; D = hydrogen bond donor other than hydrogen; with the provision] and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof is described herein. 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 biochem. assay and certain of those compounds exhibited an IC50 value less than or equal to 1 μM. Some of the compounds I were also tested for inhibition of B-cell proliferation and T-cell proliferation. Pharmaceutical compositions comprising at least one chem. entity of the invention, together with at least one pharmaceutically acceptable vehicle chosen from carriers adjuvants, and excipients, are also described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described. The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).Electric Literature of 87486-34-8
The Article related to amide preparation bruton’s tyrosine kinase btk inhibitor, b cell proliferation inhibitor amide preparation, t cell proliferation inhibitor amide preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Electric Literature of 87486-34-8