摘要 |
The present invention relates to compounds of the general formula (I) Wherein R1 is -(CHR')q-aryl or -(CHR')q-heteroaryl, which are unsubstituted or mono, di- or tri-substituted by lower alkyl, lower alkoxy, CF3 or halogen, or is lower alkyl, lower alkenyl, - (CH2)n-Si(CH3)3, -(CH2)n-O-lower alkyl, -(CH2)n-S-lower alkyl, -(CH2) q-cycloalkyl, -(CH2)n-[CH(OH)]m-(CF 2)p-CHqF(3-q), or is -(CH2)n-CR2- CF3, wherein the two R radicals form together with the carbon atom a cycloalkyl ring; R' is hydrogen or lower alkyl; n is 1, 2 or 3; in is 0 or 1; p is 0, 1, 2, 3, 4, 5 or 6; q is 0, 1, 2 or 3; R 2 is hydrogen or lower alkyl; R3 is hydrogen, lower alkyl, - CH2CF2CF3, CH2CF3, (CH 2)2CF3, CF3, CHF2, CF3, CHF2, CH2F, or is aryl, optionally mono, di or tri- substituted by halogen, or is (CH2)nNR5R 6, wherein R5 and R6 are independently from each other hydrogen or lower alkyl; R4 is one of the following groups wherein R7is hydrogen, lower akl, -(CH2)n- CF3 or -(CH2)n-cycloalkyl; R8 is hydrogen, lower alkyl, -C(O)-phenyl, -C(O)-lower alkyl, -C(O)O-(CH 2)n- cycloalkyl, -C(O)O-(CH2)n-lower alkyl, -C(O)NH-(CH2)n-lower alkyl or -C(O)NH(CH 2).-CyClOalkYl; R9 is hydrogen, lower alkyl, -(CH2) n-cycloalkyl or -(CH2)n-CF3; and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racernates or diastereomeric mixtures thereof for the treatment of Alzheimer's disease..
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