| 摘要 |
The invention relates to malonamide derivatives of formula (I), wherein: Ris one of the following groups (Formulae a), b), c), d)); Ris lower alkyl, lower alkinyl, -(CH)-O-lower alkyl, -(CH)-S-lower alkyl, -(CH)-CN, -(CR'R"), -CF,-(CR'R")CHF, -(CR'R")- CHF, -(CH)-C(O)O-lower alkyl, -(CH)-halogen, or is -(CH)-cycloalkyl, optionally substituted by one or more substituents, selected from the group consisting of phenyl, halogen or CF; R',R" are independently from n and from each other hydrogen, lower alkyl. lower alkoxy, halogen or hydroxy; R, Rare independently from each other hydrogen, lower alkyl, lower alkoxy, phenyl or halogen; Ris hydrogen, lower alkyl, -(CH)-CFor -(СН)-cycloalkyl, Ris hydrogen or halogen; Ris hydrogen or lower alkyl; Ris hydrogen, lower alkyl, lower alkinyl, -(CH)-CF,-(CH)-cycloalkyl or -(CH)-phenyl. optionally substituted by halogen; Ris hydrogen, lower alkyl, -C(O)H, -C(O)-lower alkyl, -C(O)-CF,-C(O)-CHF,-C(O)-CHF,-C(O)-cycloalkyl,-C(O)-(CH)-O-lower alkyl.-C(O)O-(CH)-cycloalky], -C(O)-phenyl, optionally substituted by one or more substituents selected from the group consisting of halogen or -C(O)O-lower alkyl, or is -S(O)-lower alkyl, -S(O)-CF,-(CH)-cycloalkyl or is -(CH)-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 mixture thereof. These compounds may be used for the treatment of Alzheimer's disease. |
