Patent ID: 6569851
Filing Date: 2003-05-27
Classification: A61K,A61P,C07D,C07K

Abstract:
A method for inhibiting &bgr;-amyloid peptide release and/or its synthesis in a cell which method comprises administering to such a cell an amount of a compound or a mixture of compounds effective in inhibiting the cellular release and/or synthesis of &bgr;-amyloid peptide wherein said compounds are represented by the following formula: wherein R1 is selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, substituted alkyl, substituted alkenyl, substituted alkynyl, substituted cycloalkyl, substituted cycloalkenyl, optionally substituted aryl, optionally substituted heteroaryl and optionally substituted heterocyclic;Q is S or O; R15 is selected from the group consisting of hydrogen, alkyl, substituted alkyl, optionally substituted aryl, optionally substituted heterocyclic and optionally substituted heteroaryl; R15â€² is selected from the group consisting of hydrogen, hydroxyl, alkyl, substituted alkyl, optionally substituted aryl, optionally substituted heterocyclic and optionally substituted heteroaryl; R2 is independently selected from the group consisting of alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl and optionally substituted heterocyclic; and the moiety: is selected from the group having the formulas: â€ƒwherein Aâ€”B is selected from the group consisting of alkylene, alkenylene, substituted alkylene, substituted alkenylene, and â€”N&boxH;CHâ€”; each V is independently selected from the group consisting of hydroxy, acyl, acyloxy, alkyl, substituted alkyl, alkoxy, substituted alkoxy, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, amino, substituted amino, aminoacyl, optionally substituted alkaryl, optionally substituted aryl, optionally substituted aryloxy, carboxyl, carboxylalkyl, cyano, halo, nitro, optionally substituted heteroaryl, thioalkoxy, substituted thioalkoxy, and trihalomethyl; Rb is selected from the group consisting of alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, acyl, optionally substituted aryl, optionally substituted heteroaryl, and optionally substituted heterocyclic; Rc is selected from the group consisting of alkyl, substituted alkyl, alkenyl, substituted alkenyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclic, cycloalkyl, and substituted cycloalkyl; and t is an integer from 0 to 4; and the pharmaceutically salts thereof; with the following provisos: when R1 is trans-cinnamyl, R2 is methyl, and R15 is hydrogen, then W, together with >CH and >C&boxH;O, does not form a 2,3-dihydro-1-(3,3-dimethyl-2-oxobutyl)-5-(2-pyridyl)-1H-1,4-benzodiazepin-2-one when R1 is trans-cinnamyl, R2 is methyl, and R15 is hydrogen, then W, together with >CH and >C&boxH;O, does not form a 2,3dihydro-1-(2-N,N-diethylaminoethyl)-5-(2-pyridyl)-1H-1,4-benzodiazepin-2-one and when R1â€”N(R15â€²)C(Q) is (2,5-dimethoxyphenyl)aminocarbonyl and R2 is methyl, then W, together with >CH and >C&boxH;O, does not form a 2,3-dihydro-1-methyl-5-phenyl-1H-1,4-benzodiazepin-2-one.