Patent Evaluation: Novel benz[cd]indoles as 5HT_1A Antagonists

Summary

Novelty: Novel, ring-substituted, 2-amino-1,2,3,4-tetrahydronaphthalenes, 3-aminochromanes and aminothiochromanes are disclosed and are claimed to be 5HT_1A agonists. The compounds are proposed to be useful for treating cognitive disorders, anxiety, depression and hypertension.

Biology: SHT_1A receptor binding was determined by the method of Wong et al using tritiated 8-hydroxy-2-dipropylamino-1,2,3,4-tetrahydronaphthalene(³H-8-OH-DP AT). The lowest IC₅₀ value given is 0.4 nM for 2-di-n-propylamino-8-(α-methylpropionyl)-1,2,3,4-tetrahydronaphthalene.

Chemistry: Thirteen preparative examples are given; all employ conventional methodology. Characterization is by mp and elemental analysis.

Structure: