| abstract |
The invention relates to malonamide derivatives of the formula I in which R1 is one of the following groups a), b), c), d) R2 is lower alkyl, lower alkynyl, - (CH2) nO-lower alkyl, - ( CH2) nS-lower alkyl, - (CH2) n-CN,? (CR'R '') n-CF3, - (CR'R '') n-CHF2, - (CR'R '') n-CH2F , - (CH2) nC (O) O-lower alkyl, - (CH2) n-halogen, or is - (CH2) n-cycloalkyl, optionally substituted by one or more substituents chosen from the group consisting of phenyl, halogen and CF3 ; R ', R' 'independently of n and independently of each other are hydrogen, lower alkyl, lower alkoxy, halogen or hydroxy; R3, R4 independently of each other are hydrogen, lower alkyl, lower alkoxy, phenyl or halogen; R5 is hydrogen , lower alkyl, - (CH2) n-CF3 or - (CH2) n-cycloalkyl; R6 is hydrogen or halogen; R7 is hydrogen or lower alkyl; R8 is hydrogen, lower alkyl, lower alkynyl,? (CH2) n-CF3 , - (CH2) n-cycloalkyl or - (CH2) n-phenyl, optionally substituted by halogen; R9 is hydrogen, lower alkyl, -C (O) H, -C (O)-lower alkyl, -C (O) -CF3, -C (O) -CH2F, -C (O) -CHF2, -C (O) -cycloalkyl, -C (O) - (CH2) nO-lower alkyl, -C (O) O- (CH2 ) n-cycloalkyl, -C (O) -phenyl, optionally substituted by one or more substituents chosen from the group consisting of halogen and -C (O) O-lower alkyl, or is -S (O) 2-lower alkyl, -S (O) 2-CF3, - (CH2) n-cycloalkyl or is? (CH2) n-phenyl, optionally substituted by halogen; n is 0, 1, 2, 3 or 4; and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. These compounds can be used for the treatment of Alzheimer's disease. |