| abstract |
It has been discovered that compounds of formula (I) stimulate the release of the neurotransmitter acetylcholine and may therefore be useful in the treatment of human diseases such as Alzheimer's disease and other pathologies related to learning and cognition , in which lower than normal levels of this neurochemical have been detected. The compounds of this invention are described in formula (I) in which Q represents (a) or (b), A and B are independently selected from the group formed by H, R4, -OH and -OCOR4, or A and B together form = O, = S, = CH2, = CHR4, = C (R4), = NOH, = NOR4, 1,3-dioxane, 1,3-dioxolane, 1,3-dithiane or 1,3-dithiolane; R1 represents 4-, 3-, or 2-pyridyl, pyrimidyl, pyrazinyl, 2-fluoro-4-pyridyl or 3-fluoro-4-pyridyl; R2 represents alkyl comprising from 1 to 10 carbon atoms, cycloalkyl comprising from 3 to 8 carbon atoms, 2-, 3-, or 4-pyridyl, Phe or Phe-W, Phe represents a phenyl group; W represents F, Cl, Br, R4, -OH, -OR4, -NO2, -NH2, -NHR4, -NR4R4, -CN, -S (O) m-R4; R3 represents H, F, Cl, Br, -CN, -OH, -NO2, -NH2, -CF3, -NHR4, -NR4R4, R4, -OR4, -S (O) m-R4, R4 and R4 'represent alkyl comprising from 1 to 4 carbon atoms, CH2Phe-W or Phe-W; R5 represents - (CH2) m-Y or -OCOR4; Y represents H, OH, NH2, -NHR4, -NR4R4, -NHCOR4, -NHCO2R4, F, Cl, Br, OR4, -S (O) mR4, -CO2H, -CO2R4, -CN, -CONR4R4, -CONHR4, -CONH2, -COR4; -CH = CHCO2R4, -OCOR4, Phe, Phe-W, -C = CCO2R4, -CH = CHR4, or -C = CR4; m is 0, 1 or 2; n is between 1 and 7; provided that when Q represents indoxyl and R5 represents (CH2) nY, Y does not represent OH. The physiologically suitable salts of these compounds are also described in this invention. |