637024-75-0

Upstream product

• 104293-43-8 (3R,5R,1'S)-5-<1-<<(tert-butyloxy)carbonyl>amino>-2-phenylethyl>-3-methyldihydrofuran-2(3H)-one 
• 176504-90-8 dimethyl [(3S)-4-phenyl-3-[N-(tert-butyloxycarbonyl)amino]-2-oxobutyl]phosphonate 
• 51987-73-6 (S)-2-tert-butoxycarbonylamino-3-phenyl-propionic acid methyl ester 
• 637024-71-6 ethyl (5S,2Z)-2-methyl-[5-(tert-butoxycarbonyl)amino]-4-oxo-6-phenylhex-2-enoate 
• 637024-72-7 (5R)-3-methyl-5-{(1S)-1-[(tert-butoxycarbonyl)amino]-2-phenylethyl}-2,5-dihydrofuran-2-one 
• 637024-74-9 (2S,3R,5R)-2-tert-butoxycarbonylamino-1-phenyl-5-methylhexan-3,6-diol 
• 18162-48-6 tert-butyldimethylsilyl chloride 

Downstream Products

• 637024-80-7 N-{(1S,2S,4R)-2-azido-1-benzyl-4-[(1S)-1-benzylcarbamoyl-2-methylpropylcarbamoyl]-pentyl}-N',N'-dipropyl-isophthalamide 
• 637024-79-4 (2R,4S,5S)-4-Azido-5-(3-dipropylcarbamoyl-benzoylamino)-2-methyl-6-phenyl-hexanoic acid 
• 637024-78-3 N-[(1S,2S,4R)-2-azido-1-benzyl-5-hydroxy-4-methyl-pentyl]-N',N'-dipropylisophthalamide 
• 637024-77-2 [(1S,2S,4R)-2-azido-1-benzyl-5-(tert-butyl-dimethyl-silanyloxy)-4-methyl-pentyl]-carbamic acid tert-butyl ester 
• 1026292-98-7 (2R,4S,5S)-5-Amino-4-azido-2-methyl-6-phenyl-hexan-1-ol 

Relevant academic research and scientific papers

Aminoethylenes: A tetrahedral intermediate isostere yielding potent inhibitors of the aspartyl protease BACE-1

A series of novel β-site amyloid precursor protein cleaving enzyme (BACE-1) inhibitors containing an aminoethylene (AE) tetrahedral intermediate isostere were synthesized and evaluated in comparison to corresponding hydroxyethylene (HE) compounds. Enzymat

Aspartyl protease inhibitors

The present invention provides compounds having the formula: wherein R1, R′, R2, R3, R3′, R4, X1, X2 and X3 are as defined herein, and pharmaceutical compositions thereof. The present invention also provides methods of inhibiting proteases, more specifically aspartyl proteases. In certain embodiments, compounds inhibit BACE (β-site APP-cleaving enzyme), and thus are useful in the treatment or prevention of a disease characterized by β-amyloid deposits in the brain (including, but not limited to, Alzheimer's Disease). The present invention also provides methods for preparing compounds of the invention.

ASPARTYL PROTEASE INHIBITORS

The present invention provides compounds having formula (I): wherein R’, R0, R1, X1, R2, R3, R3’, X2, X3, and R4 are as defined herein, and pharmaceuticals compositions thereof. The present invention also provides methods of inhibiting proteases, more specially aspartyl proteases. In certain embodiments, compounds inhibit BACE (β-site APP-cleaving enzyme), and thus are useful in the treatment or prevention of a disease characterized by β-amyloid deposits in the brain (including, but not limited to, Alzheimer’s Disease). The present invention also provides methods for preparing compounds of the invention.