L. Czollner, J. Fröhlich, U. Jordis, B. Küenburg:
"New benzazepine derivatives, medicaments containing the same and their use to prepare medicaments";
No. WO 9740049;
The synthesis of benzofuro[3a,3,2,ef]benzazepines (I) [R1,R2 = H, halo, CN, NC, OH, SH, SO3H, NH2, CF3, (un)substituted alkyl, (un)substituted alkoxy, (un)substituted aryl, (un)substituted aryloxy; R3 = OH, OMe; R4,R5 = H2, O, substituted O, (un)substituted alkyl, (un)substituted aryl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted hydrazone, (un)substituted oxime; X = H2, O] and diazabicyclo[2.2.1]heptanes (II) [R8 = CH2Ph, 4-MeC6H4SO2, H, (un)substituted alkyl, Me3CO2C; R9 = (un)substituted Ph, CH2Ph, CHPh2, Me3CO2C] are described. Thus, I (R1 = Br, R2 = H, R3 = OMe, R4 = OH, R5 = H, R6 = H, X = H2) (III) was prepd. by tartrate resoln. of ()-N-demethyl-8-bromogalanthamine. III in in vitro study showed an IC50 of >150 in mol for the inhibition of acetylcholine esterase. Also disclosed are medicaments which contain compds. of formulas (I) and/or (II) and may be successfully used for treating Alzheimer disease and related demential states, as well as the Langdon-Down syndrome.
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