Novel indoles for the treatment of neurodegenerative diseases

Patent Summary

Novel cis-2,3,4,3a,4,5,9b-hexahydro-1H-benzo[e]mdoles are claimed to be useful for the treatment of neurodegenerative diseases, specifically dementia and Alzheimer's disease. The compounds are stated to be AChE inhibitors. Enzyme inhibition was assessed according to the method of von Ellman and Johnson et al. [1a,1b]. Selected compounds gave IC₅₀ values of 30-0.4 nM, compared to the standard physostimine which gave an IC₅₀ of 18 nM. Full preparative details are presented and 45 worked examples are provided. Fourteen compounds are specifically claimed, including rac- cis-2,3,3a,4,5,9b-hexahydro-3-(6-phthalimidohexyl)-1H-benzo(e]indol-6-yldimethylcarbamate.