Patent Evaluation: Novel benimidazole angiotensin II antagonists that have been prepared in crystalline form

Summary

Novelty: Benzimidazole derivatives are claimed as angiotensin II antagonists. The compounds possess potentially useful antihypertensive and anti-ischaemic properties.

Biology: Antagonism of All is demonstrated by competition binding experiments in adrenal cortex preparations and by inhibition of All-induced hypertension in rats (compounds are effective at doses of 3 mg/kg po).

Chemistry: Synthesis of the compounds is outlined in twenty-six schemes forming a subsidiary part of the claim. Seventy-seven compounds are exemplified and numerous specifically claimed including ethyl 2-ethoxy-1-[[2′-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-benzimid-azole-7-carboxylate and in particular, a stable crystal of this ester, as described in terms of sixteen lattice spacing values.

Structure: