537657-85-5Relevant articles and documents
BACE-1 inhibitors Part 1: Identification of novel hydroxy ethylamines (HEAs)
Clarke, Brian,Demont, Emmanuel,Dingwall, Colin,Dunsdon, Rachel,Faller, Andrew,Hawkins, Julie,Hussain, Ishrut,MacPherson, David,Maile, Graham,Matico, Rosalie,Milner, Peter,Mosley, Julie,Naylor, Alan,O'Brien, Alistair,Redshaw, Sally,Riddell, David,Rowland, Paul,Soleil, Virginie,Smith, Kathrine J.,Stanway, Steven,Stemp, Geoffrey,Sweitzer, Sharon,Theobald, Pam,Vesey, David,Walter, Daryl S.,Ward, John,Wayne, Gareth
, p. 1011 - 1016 (2008/12/20)
Inhibition of the aspartyl protease BACE-1 has the potential to deliver a disease-modifying therapy for Alzheimer's disease. Herein, is described the lead generation effort which resulted, with the support of X-ray crystallography, in the discovery of pot
3-(1,1-DIOXOTETRAHYDRO-1,2-THIAZIN-2-YL) or 3-(1,1-DOXO-ISOTHIAZOLIDIN-2YL) SUBSTITUTED BENZAMIDE COMPOUNDS AS ASP2 INHIBITORS
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Page/Page column 18, (2010/02/09)
The present invention relates to hydroxyethylene compounds of formula (I); having A sp2 (β-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterized by elevated β-amyloid levels or β-amyloid deposits, particularly Alzheimer's disease wherein R1 represents a group of formula Zc.
