Scott, Jack D. published the artcileDiscovery of the 3-Imino-1,2,4-thiadiazinane 1,1-Dioxide Derivative Verubecestat (MK-8931)-A β-Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor for the Treatment of Alzheimer’s Disease, Formula: C8H8BNO2, the main research area is verubecestat preparation BACE1 inhibitor structure activity Alzheimer disease.
Verubecestat (MK-8931), a diaryl amide substituted 3-imino-1,2,4-thiadiazinane 1,1-dioxide derivative, is a high-affinity β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor currently undergoing Phase 3 clin. evaluation for the treatment of mild to moderate and prodromal Alzheimer’s disease. Although not selective over the closely related aspartyl protease BACE2, verubecesat has high selectivity for BACE1 over other key aspartyl proteases, notably cathepsin D, and profoundly lowers CSF and brain Aβ levels in rats and nonhuman primates, and CSF Aβ levels in humans. In this annotation, the authors describe the discovery of verubecesat, including design, validation, and selected SAR around the novel iminothiadiazinane dioxide core, as well as aspects of its preclin. and Phase 1 clin. characterization.
Journal of Medicinal Chemistry published new progress about Alzheimer disease. 917471-30-8 belongs to class pyridine-derivatives, name is (5-(Prop-1-yn-1-yl)pyridin-3-yl)boronic acid, and the molecular formula is C8H8BNO2, Formula: C8H8BNO2.