288296-21-9Relevant academic research and scientific papers
BACE-1 inhibitors part 2: Identification of hydroxy ethylamines (HEAs) with reduced peptidic character
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. 1017 - 1021 (2008)
This paper describes the discovery of non-peptidic, potent, and selective hydroxy ethylamine (HEA) inhibitors of BACE-1 by replacement of the prime side of a lead di-amide 2. Inhibitors with nanosmolar potency and high selectivity were identified. Dependi
HYDROXYETHYLAMINE DERIVATIVES FOR THE TREATMENT OF ALZHEIMER'S DISEASE
-
Page 42, (2010/02/07)
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.
Inhibitors of aspartyl protease
-
, (2008/06/13)
The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
