849409-80-9

Upstream product

• 51814-55-2 tert-butyl (S)-[1-(benzylamino)-1-oxopropan-2-yl]carbamate 
• 271601-65-1 (2R,4S,5S)-5-[(tert-butyloxycarbonyl)amino]-4-[(tert-butyldimethylsilyl)oxy]-2,7-dimethyloctanoic acid 
• 881009-00-3 (2R,4S,5S)-5-tert-Butoxycarbonylamino-4-hydroxy-2,7-dimethyl-octanoic acid 
• 169057-47-0 (3R,5S,1'S)-5-[1'-[(tert-butyloxycarbonyl)amino]-3'-methylbutyl]-3-methyldihydrofuran-2(3H)-one 
• 18162-48-6 tert-butyldimethylsilyl chloride 
• 105018-81-3 (5S,1'S)-5-<1'--3'-methylbutyl>dihydrofuran-2(3H)-one 

Downstream Products

• 364635-79-0 {(S)-1-[(1S,2S,4R)-4-((S)-1-Benzylcarbamoyl-ethylcarbamoyl)-2-hydroxy-1-isobutyl-pentylcarbamoyl]-2-carbamoyl-ethyl}-carbamic acid tert-butyl ester 
• 527674-73-3 tert-butyl (1S,2S,4R)-5-{[(1S)-2-(benzylamino)-1-methyl-2-oxoethyl]amino}-2-hydroxy-1-isobutyl-4-methyl-5-oxopentylcarbamate 

Relevant academic research and scientific papers

Structure-based design: Potent inhibitors of human brain memapsin 2 (β-secretase)

Memapsin 2 (β-secretase) is one of two proteases that cleave the β-amyloid precursor protein (APP) to produce the 40-42 residue amyloid-β peptide (Aβ) in the human brain, a key event in the progression of Alzheimer's disease. On the basis of the X-ray crystal structure of our lead inhibitor (2, OM99-2 with eight residues) bound to memapsin, we have reduced the molecular weight and designed potent memapsin inhibitors. Structure-based design and preliminary structure-activity studies have been presented.

NOVEL SULFONE AMIDE DERIVATIVES CAPABLE OF INHIBITING BACE

The present invention relates to novel derivatives of sulfone amide of Formula 1 as defined in this disclosure which inhibit the activity of BACE (or beta-secretase). These sulfone amide derivatives are useful for the treatment and prevention of Alzheimer's disease and related diseases caused by production of beta-amyloid, by inhibiting the activity of BACE.