1067651-20-0Relevant articles and documents
Design and synthesis of potent and selective BACE-1 inhibitor
Bj?rklund, Catarina,Oscarson, Stefan,Benkestock, Kurt,Borkakoti, Neera,Jansson, Katarina,Lindberg, Jimmy,Vrang, Lotta,Hallberg, Anders,Rosenquist, Asa,Samuelsson, Bertil
experimental part, p. 1458 - 1464 (2010/08/03)
Highly potent BACE-1 protease inhibitors have been developed from an inhibitors containing a hydroxyethylene (HE) core displaying aryloxymethyl or benzyloxymethyl P1 side chain and a methoxy P1′ side chain. The target molecules were synthesized in good overall yields from chiral carbohydrate starting materials. The inhibitors show high BACE-1 potency and good, selectivity against cathepsin D, where the most potent inhibitor furnishes BACE-1 Ki ? 1 nM and displays > 1000-fold selectivity over cathepsin D.
AMIDE DERIVATIVES AS INHIBITORS OF ASPARTYL PROTEASES
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Page/Page column 63, (2008/12/04)
The invention provides compounds of the formula (I). N-oxides, addition salts, quaternary amines, metal complexes, stereochemically isomeric forms and metabolites thereof, wherein W is H,C 1-C 6 alkyl, C 3-C 6 cycloalkyl, aryl or heterocyclyl; Q is aryl or heterocyclyl; A is a five or six membered saturated, partially unsaturated or aromatic ring; D is (II) or (III) the other variables are as defined in the specification. The compounds of the invention are inhibitors of BACE and are among other things useful for the treatment and/or prevention of conditions associated with BACE activity such as Alzheimer's disease.