| abstract |
The invention relates to compounds of general formula (I), wherein R1 is lower alkyl substituted by halogen, or is aryl or heteroaryl, unsubstituted or substituted by halogen; R2 is heterocycloalkyl, aryl or heteroaryl, which are unsubstituted or substituted by one or more substituents, selected from the group consisting of halogen, lower alkyloxy, lower alkyl substituted by halogen, O-lower alkyl substituted by halogen or are substituted by C(O)-NR'2, (CR2)m-C(O)-R’ heteroaryl or S(O)2-lower alkyl; R3/R3’ , R4/R4’ and R5/R5’ are independently from each other hydrogen or fluoro, wherein at least one of R4/R4’ or R5/R5’is always fluoro; R' is aryl or hydroxy; R' is hydrogen, cycloalkyl or is heterocycloalkyl; R is hydrogen or lower alkyl; m is 0, 1, 2 or 3; and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. It has been found that the compounds of general formula (I) are Ϝ-secretase inhibitors and the related compounds may be useful in the treatment of Alzheimer's disease or common cancers including but not limited to cervical carcinomas and breast carcinomas and malignancies of the hematopoietic system. |