887913-53-3

Upstream product

• 2142-63-4 1-(3-Bromophenyl)ethanone 
• 1075230-53-3 (R)-N-(1-(3-bromophenyl)ethylidene)-2-methylpropane-2-sulfinamid 
• 1076160-64-9 (R)-N-(1-(3-bromophenyl)ethylidene)-2-methylpropane-2-sulfinamide 
• 1194044-35-3 (S)-methyl 3-(3-bromophenyl)-3-((R)-1,1-dimethylethylsuifinamido)butanoate 

Downstream Products

• 1392015-28-9 C₂₄H₂₉N₃O₄ 
• 1392015-29-0 (S)-2-imino-6-(3'-methoxy-[1,1'-biphenyl]-3-yl)-3,6-dimethyltetrahydropyrimidin-4(1H)-one.trifluroacetate 

Relevant academic research and scientific papers

Discovery of an orally available, brain penetrant BACE1 inhibitor that affords robust CNS Aβ reduction

Inhibition of BACE1 to prevent brain Aβ peptide formation is a potential disease-modifying approach to the treatment of Alzheimer's disease. Despite over a decade of drug discovery efforts, the identification of brain-penetrant BACE1 inhibitors that substantially lower CNS Aβ levels following systemic administration remains challenging. In this report we describe structure-based optimization of a series of brain-penetrant BACE1 inhibitors derived from an iminopyrimidinone scaffold. Application of structure-based design in tandem with control of physicochemical properties culminated in the discovery of compound 16, which potently reduced cortex and CSF Aβ40 levels when administered orally to rats.

PENTAFLUOROSULFUR IMINO HETEROCYCLIC COMPOUNDS AS BACE-1 INHIBITORS, COMPOSITIONS, AND THEIR USE

In its many embodiments, the present invention provides provides certain pentafluorosulfur imino heterocyclic compounds, including compounds Formula (I): and tautomers thereof, and solvates, prodrugs, esters, and deuterates of said compounds and said tautomers, and pharmaceutically acceptable salts of said compounds, tautomers, solvates, prodrugs, esters, and deuterates, wherein each of R1, R2, R3, R4, R5, R9, R11, ring A, ring B, m, n, p, q, r, -L1-,L2-, and L3- is selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimers Disease, are also disclosed.