Patent Evaluation: Novel 2,2′-alkylenediindoles as anti-ulcer agents

Summary

Novelty: Novel 2,2′-alkylenediindole derivatives are claimed to be H⁺/K⁺ ATPase inhibitors. They are potentially useful as anti-ulcer agents.

Biology: An H⁺/K⁺ ATPase inhibitory activity assay was performed in vitro using a pig stomach preparation. Inhibition was determined colorimetrically. Results are given for twelve compounds. ATPase inhibition was 5-100% (dose 5–20 μg/ml).

Chemistry: A total of twenty-three compounds are disclosed. Syntheses are given in five examples. Characterization is by ¹H nmr and ms. None of the compounds are specifically claimed. 3-(2-Phenylethylaminoethyl)-2,2′-tetramethylenediindole is typical of the claim.