Potent and selective isophthalamide S2 hydroxyethylamine inhibitors of BACE1
The design and synthesis of a novel series of potent BACE1 hydroxyethylamine inhibitors. These inhibitors feature hydrogen bonding substituents at the C-5 position of the isophthalamide ring with improved selectivity over cathepsin D.
Kortum, Steven W.,Benson, Timothy E.,Bienkowski, Michael J.,Emmons, Thomas L.,Prince, D. Bryan,Paddock, Donna J.,Tomasselli, Alfredo G.,Moon, Joseph B.,LaBorde, Alice,TenBrink, Ruth E.
p. 3378 - 3383
(2008/02/09)
HYDROXYETHYLAMINE DERIVATIVES FOR THE TREATMENT OF ALZHEIMER'S DISEASE
The present invention relates to novel hydroxyethylamine compounds of formula (I): (I) having Asp2 (-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated-amyloid levels or-amyloid deposits, particularly Alzheimer's disease.
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Page 39
(2010/02/07)
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