abstract |
This invention relates to silylated aromatic fluoroketones of the formula (I)n 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. nX is H, Br, Cl, F, R₄, COR₅, CO₂R₅, CONHR₅ or COR₆; nR₁, R₂, R₃ and R₄ each are C₁₋₁₀ alkyl, or (CH₂)p aryl, with p being zero, one or two, nR₅ is H, C₁₋₁₀ alkyl, phenyl, benzyl or phenethyl, nR₆ is (NHCHR₇C(O)) q R₈ with R₇ being the residue of any natural occurring α-amino acid, q is one to four and R₈ is OR₅ or NHR₅, nY 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) x SiR₁R₂R₃with x being zero, one or two, possessing acetylcholinesterase properties and to their use in the treatment of Alzheimer's disease and senile dementia. |