Patent Evaluation: New Diazines as Gastric Acid Secretion Inhibitors

Summary

Novelty: Novel pyrrolo[2,3-d]pyridazines are claimed and are said to possess anti-ulcer properties.

Biology: Data are tabulated for four compounds and show their anti-ulcer and acid secretion inhibition properties in the modified Shay-rat model. Data for five compounds are similarly presented from the pentagastrin-stimulated rat model. The compound shown below gave ED₅₀ values of 5.28 μM/kg and 0.6 μM/kg, respectively.

Chemistry: Twenty examples fully illustrate synthesis. The specified compound is 1-benzyl-7-benzyloxy-2,3-dimethyl-pyrrolo[2,3-d]pyridazine.

Structure: