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Summary
Novelty: Novel polycyclic derivatives which exhibit antihistaminic, anti-allergic, antiarrhythmic and antihypertensive activity and which are potentially useful in the treatment of allergic diseases or bronchial asthma are disclosed.
Biology: An assay for anti-histaminic activity, measuring the effect on the contractile response induced by histamine in isolated guinea pig ileum, is described (-log KB =7.3). The -log KB is less than amoxapine (8.37), clothiapine (8.87), perlapine (9.15) and mianserin (9.15) in the same assay. Anti-allergic activity in Wistar rats is also discussed (88.6% inhibition compared with 50.9% for amoxapine and 61.4% for mianserin).
Chemistry: 4-(2-Chlorodibenz[b,f][1,4]oxazepin-11-yl)-1-piperazine propanoic acid is one of eight specifically claimed compounds.
Structure: