790255-61-7Relevant academic research and scientific papers
Second generation of hydroxyethylamine BACE-1 inhibitors: Optimizing potency and oral bioavailability
Charrier, Nicolas,Clarke, Brian,Cutler, Leanne,Demont, Emmanuel,Dingwall, Colin,Dunsdon, Rachel,East, Philip,Hawkins, Julie,Howes, Colin,Hussain, Ishrut,Jeffrey, Phil,Maile, Graham,Matico, Rosalie,Mosley, Julie,Naylor, Alan,O'Brien, Alistair,Redshaw, Sally,Rowland, Paul,Soleil, Virginie,Smith, Kathrine J.,Sweitzer, Sharon,Theobald, Pam,Vesey, David,Walter, Daryl S.,Wayne, Gareth
supporting information; experimental part, p. 3313 - 3317 (2009/04/06)
BACE-1 inhibition has the potential to provide a disease-modifying therapy for the treatment of Alzheimer's disease. Optimization of a first generation of BACE-1 inhibitors led to the discovery of novel hydroxyethylamines (HEAs) bearing a tricyclic nonprime side. These derivatives have nanomolar cell potency and are orally bioavailable.
TRICYCLIC INDOLE DERIVATIVES AND THEIR USE IN THE TREATMENT OF ALZHEIMER’S DISEASE
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Page 20, (2010/02/09)
The present invention relates to novel hydroxyethylamine compounds having Asp2 (β-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 β- amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.
