N-SUBSTITUTED DIBENZOXAZEPINES AS ANALGESIC PGE(2) ANTAGONISTS

Chlorodibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid, 2-acetylhydra zide (1, SC-19220) has been previously reported by us and others to be a PGE2 antagonist selective for the EP1 receptor subtype1 with antino ciceptive activities.2 Analogs of SC-19220, in which the acetyl moiety has been replaced with pyridylpropionyl groups and their homologs, ha ve been synthesized as illustrated by compounds 13 and 29. These and o ther members of this series have been shown to be efficacious analgesi cs and PGE2 antagonists of the EP1 subtype. This report discusses the structure activity relationships within this series.