Novel acetylcholinesterase inhibitors.

摘要

This invention relates to silylated aromatic fluoroketones of the formula (I) <CHEM> and the pharmaceutically acceptable salts thereof, wherein each of m and n is zero or one with the proviso that the sum of m and n is less than two. X is H, Br, Cl, F, R4, COR5, CO2R5, CONHR5 or COR6; R1, R2, R3 and R4 each are C1-10 alkyl, or (CH2)p aryl, with p being zero, one or two, R5 is H, C1-10 alkyl, phenyl, benzyl or phenethyl, R6 is (NHCHR7C(O))qR8 with R7 being the residue of any natural occurring alpha -amino acid, q is one to four and R8 is OR5 or NHR5, Y is H, OH, C1-6 alkyl, C1-6 alkoxy, hydroxy C1-6 alkyl, amino C1-6 alkyl, NH2, azido, CN, CO2R5, COR5, -SO3H, Br, Cl, F or -(CH2)xSiR1R2R3with x being zero, one or two, possessing acetylcholinesterase properties and to their use in the treatment of Alzheimer's disease and senile dementia.