[Zurück]

L. Czollner, B. Kaelz, S. Welzig, W. Frantsits, U. Jordis, J. Fröhlich:
"Preparation of N-alkylgalanthamines and related compounds for the treatment of central nervous system diseases";
Patent: PCT Int. Appl., Nr. WO2005030333; eingereicht: 09.09.2004, erteilt: 07.04.2005.

Title compds. I [R1, R2 = H, OH; X = H, Br; Z = CH2CCH; CH2C(CH2)CH3, CO(CH2)nCl, etc.; n = 0-6] and their pharmaceutically acceptable salts were prepd. For example, 4-bromobenzyl bromide N-alkylation of (-)-norgalanthamine, afforded alkylgalanthamine II in 70% yield. In acetylcholinesterase inhibition assays, 60-examples of compds. I exhibited IC50 values ranging from 0.016->100 mM, e.g., the IC50 value of alkylgalanthamine II was 0.016 mM. Compds. I are claimed to be useful for the treatment of Alzheimer's disease.