MALONAMIDE DERIVATIVES AS γ-SECRETASE INHIBITORS Russian patent published in 2012 - IPC C07D223/18 A61K31/55 A61P25/28 

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry and specifically to novel malonamide derivatives of formula and their pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomer mixtures, where A¹ denotes -CHR- or -C(O)-; A² denotes -C(O)-; and R²/R³ independently denote hydrogen, lower alkyl, halogen, hydroxy or lower alkoxy; or A² denotes -O-C(O)-, and R²/R³ independently denote hydrogen or lower alkyl; R denotes hydrogen or lower alkyl substituted with a halogen; R¹ denotes hydrogen, lower alkyl or -(CH₂)_n-aryl, optionally substituted with halogen; R⁴ denotes lower alkyl substituted with a halogen; n equals 0, 1 or 2. The invention also relates to a method of producing a compound of formula I, a medicinal agent based on the compound of formula I and use of the compound of formula I.

EFFECT: obtaining novel malonamide derivatives of formula I, having inhibiting action on γ-secretase and are useful in treating Alzheimer's disease.

13 cl, 72 ex