PHENYLETHENYL OR PHENYLETHINYL HETEROARIL DERIVATIVES AS GLUTAMATE RECEPTOR ANTAGONISTS, THEIR USE, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

摘要

The present invention relates to compounds of formula (I): wherein R 1, R 2, R 3, R 4 and R 5 are each independently hydrogen, C 1-6 alkyl, - (CH 2) n halo, C 1-6 alkoxy, - (CH 2) nNRR1, - (CH2) nN (R) -C (O) -1-6 alkyl, aryl, or unsubstituted or substituted one or more C 1-6 alkyl substituted heteroaryl; R, R 'and R "are independently hydrogen or C 1-6 alkyl; A is -CH = CH- or -C? C-; and B is (B1), (B2), (B3), (B4), (B5) or (B6) wherein R6 is hydrogen, (C1-C6) alkyl, - (CH2) nC (O) OR or halogen; R7 is hydrogen, (C1-C6) alkyl, - (CH2) nC (O). ) OR ', halogen, nitro, or unsubstituted or heteroaryl substituted with C 1-6 alkyl or cycloalkyl; R 8 is hydrogen, C 1-6 alkyl, - (CH 2) n -OH, - (CH 2) n C (O) OR "a group or an aryl group; R 9 is C 1 -C 6 alkyl; R10 is hydrogen, (C1-C6) alkyl, or halogen; R 11 is hydrogen or C 1-6 alkyl; R 12 is - (CH 2) n -N (R) -C (O) - (C 1 -C 6) alkyl; R 13 is hydrogen or C 1-6 alkyl; R14, R15, R16 and R17 are each independently hydrogen, (C1-C6) -alkyl, - (CH2) n-halo or (C1-C6) -alkoxy; R18, R19, and R20 are each independently hydrogen, (C1-C6) alkyl, - (CH2) n-halo, or (C1-C6) alkoxy; R 21 is hydrogen or C 1-6 alkyl; R 22 is hydrogen, (C 1 -C 6) -alkyl or (C 1 -C 6) -alkyl substituted with one or more hydroxy and / or halogen; R23 is hydrogen, (C1-C6) alkyl, (C1-C6) alkanoyl, or nitro; R24, R25 and R26 are each independently hydrogen or C1-C6 alkyl] and their pharmaceutically acceptable salts for the preparation of a medicament for the treatment or prevention of mGluR5 receptor mediated disorders. The invention also relates to a process for preparing the compounds. HE