Patent Evaluation: Indole Derivatives as Leukotriene Biosynthesis Inhibitors

Summary

Novelty: Novel pharmaceutical compositions for preventing or treating gastrointestinal disorders induced by nonsteroidal anti-inflammatory drugs in humans are disclosed. The composition consists of a NSAID with an antacid buffering agent. Methods of treating the symptoms of this condition and arthritic disorders using these pharmaceutical compositions are also given.

Biology: NSAID induced gastric mucosal damage was determined in an exteriorized rabbit colon direct contact gastrointestinal irritancy model and a five day oral gastrointestinal irritation study in cynomolgus monkeys.

Chemistry: In preferred embodiments, ibuprofen or naproxen is used in combination with calcium carbonate, magnesium oxide or magnesium carbonate