N-(aryl/heteroaryl) amino acid derivatives and methods for inhibiting beta-amyloid peptide release or its synthesis

摘要

Provided are inhibitors of b-amyloid peptide release and/or its synthesis in a cell having the formula I depicted wherein: R1 is selected form the group consisting of optionally substituted phenyl, optionally substituted 2-naphthyl and optionally substituted heteroaryl, R2 is selected from hydrogen, alkyl, alkylyalkoxy, alkylthioalkoxy, optionally substituted aryl, and optionally substituted heteroaryl, R3 is selected from the group consisting of optionally substituted alkyl, alkenyl, and alkynyl, aryl, cycloalkyl, cycloalkenyl, heteroaryl and heterocyclic, and either X is -C(O)-Y, and Y is optionally substituted alkyl, optionally substituted alkoxy, optionally substituted thioalkoxy, hydroxy, aryl, heteroaryl, heterocyclic or NR'R", or X is -CR4R4Y' when R3 contains at least three carbon atoms, R4 is independently hydrogen, alkyl, cycloalkyl, aryl, heteroaryl and heterocyclic and Y' is hydroxy, amino, mercapto, -OC(O)R5, -SSR5, -SSC(O)R5 where R5 is optionally substituted alkyl, cycloalkyl, aryl, heteroaryl and heterocyclic.