On April 23, 2015, Bennett, Michael John; Betancort, Juan Manuel; Boloor, Amogh; Kaldor, Stephen W.; Stafford, Jeffrey Alan; Veal, James Marvin published a patent.Recommanded Product: 3,5-Dibromo-1-methylpyrazin-2(1H)-one The title of the patent was Heterocyclic compounds as bromodomain inhibitors and their preparation. And the patent contained the following:
The invention relates to substituted heterocyclic compounds of formula I, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease. Compounds of formula I wherein R2 is Me, ET, CH2CF3, etc.; X5 is CR5 and N; X6 is CR6 and N; X7 is CR7 and N; X8 is CR8 and N;, provided that no more than two of X5 – X8 are N; R5, R6 and R7 are independently H, halo, OH, CN, amino, alkyl, etc.; R8 is H, halo and alkyl; Ra is substituted Ph and substituted heteroaryl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by cross-coupling of 4-bromo-2-methylisoquinolin-1(2H)-one with (3-methoxyphenyl)boronic acid. The invention compounds were evaluated for their BRD4 inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value in the range of > 0.5 μM to ≤ 5.0 μM. The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).Recommanded Product: 3,5-Dibromo-1-methylpyrazin-2(1H)-one
The Article related to heterocycle preparation bromodomain inhibitor, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Recommanded Product: 3,5-Dibromo-1-methylpyrazin-2(1H)-one