abstract |
The present invention pertains to compounds of formula (I) wherein X is O, NH, N(C1-4)alkyl, CO or CHOH, Y is CH or N, A and B are each hydrogen or together form a second bond between the carbon atoms to which they are attached, R1 is hydrogen or (C1-4)alkyl, R2 is optionally substituted (C1-8)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-4)alkyl, aryl or heteroaryl, R3 is CH(Re)CONRaRb or (CH2)nNRc,Rd, n is 0, 1 or 2, Ra, Rb, Rc and Rd, independently, are hydrogen or optionally substituted (C1-8)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-4)alkyl, (C7-9)bicycloalkyl, 1-aza-(C7-9)bicycloalkyl, aryl, aryl(C1-4)alkyl, heteroaryl, heteroaryl(C1-4)alkyl or heterocyclyl, or Ra, Rb, Rc and Rd, together with the nitrogen to which they are attached, form an optionally substituted pyrrolidinyl, piperidino, morpholino or piperazinyl group, Re is (C1-8)alkyl, (C1-4)alkoxy(C1-4)alkyl, (C3-7)cycloalkyl or (C3-7)cycloalkyl(C1-4)alkyl, and R4, R5, R6, R7, R8 and R9, independently, are hydrogen, (C1-4)alkyl, (C1-4)alkoxy, (C1-4)alkyl-SO2, cyano, nitro or halogen; to a process for the preparation of such compounds of formula (I), their use as a pharmaceuticals, especially in the treatment of neurological and vascular disorders related to beta-amyloid generation and/or aggregation, and to pharmaceutical compositions and combinations comprising such compounds of formula (I). |