Verubecestat 3 (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 …

Accumulation of amyloid β peptides (Aβ) is thought to be one of the causal factors of
Alzheimer's disease (AD). The aspartyl protease β-site amyloid precursor protein cleaving …

β-Amyloid (Aβ) peptides are thought to be critically involved in the etiology of Alzheimer's
disease (AD). The aspartyl protease β-site amyloid precursor protein cleaving enzyme 1 …

After identification of lead compound 6, 5-amino-1, 4-oxazine BACE1 inhibitors were
optimized in order to improve potency, brain penetration, and metabolic stability. Insertion of …

Using fragment-based screening of a focused fragment library, 2-aminoquinoline 1 was
identified as an initial hit for BACE1. Further SAR development was supported by X-ray …

The amyloid hypothesis has long been the central dogma in drug discovery for Alzheimer's
disease (AD), leading to many small-molecule and biological drug candidates. One major …

Inhibition of the aspartyl protease BACE-1 has the potential to deliver a disease-modifying
therapy for Alzheimer's disease. We have recently disclosed a series of transition-state …

A hallmark of Alzheimer's disease is the brain deposition of amyloid beta (Aβ), a peptide of
36–43 amino acids that is likely a primary driver of neurodegeneration. Aβ is produced by …

Alzheimer's disease (AD) is an irreversible, progressive neurological disorder characterized
by amyloid plaques, hyperphosphorylated tau protein (hyper p-tau), neuronal damage …

β-Site amyloid precursor protein cleaving enzyme1 (BACE1) is one of the key enzymes
involved in the processing of the amyloid precursor protein (APP) and formation of amyloid β …