5,11-dihydrodibenzo[b,e][1,4]oxazepine derivatives and pharmaceu

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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Details

540550, A61K 31553, A61P 100, C07D26718

Patent

active

061273619

DESCRIPTION:

BRIEF SUMMARY
This application is a national stage entry under 35 U.S.C. .sctn.371 of PCT/JP97/00754 filed Mar. 11, 1997.


FIELD OF THE INVENTION

The present invention relates to 5,11-dihydrodibenzo[b,e][1,4]oxazepine derivatives, stereoisomers thereof, pharmacologically acceptable salts thereof or hydrates thereof, which have a calcium channel blocking activity and are useful for the therapy and the treatment of the digestive tract abnormal moving function diseases, especially the intestinal diseases such as the irritable bowel syndrome as well as a pharmaceutical composition containing the same as an active ingredient.


BACKGROUND OF THE INVENTION

For example, European Patent No. 0404359A1 discloses that 5,11-dihydrodibenzo[b,e][1,4]thiazepine derivatives are useful as a calcium channel blocker having a selectivity for the gastrointestinal tract. Quinn, P. et al., Brit. J. Pharmacol. 1994, 112(Suppl.), Abst p573 and Wallis, R. M. et al., Brit. J. Pharmacol. 1994, 112(Suppl.), Abst p574 disclose that (S)-5-[1-[2-(Methoxyphenyl)ethyl]pyrrolidin-2-ylmethyl]-5,11-dihydrodibenz o[b,e][1,4]thiazepine maleate which is one of the above-mentioned derivatives has the same activity as mentioned abov e. However, the above-mentioned compounds are problematic in that they exhibit an anticholinergic activity which gives a side effect such as hydrodipsia, mydriasis or the like.
In recent years, as the social environment has become complicated, a lot of people have come to be under great stress, and there have been a large number of patients suffering from an irritable bowel syndrome of which main symptoms are abnormal bowel movement, abdominal pain and the like. To cope with such diseases, an anticholinergic agent, a laxative agent, an antidiarrheal drug, a drug for controlling intestinal function, a mucosa paralyzant, a drug for controlling an intestinal tract moving function, an agent of controlling an autonomic nerve, a herb medicine, an antianxiety agent, an antidepressant, a hypnotic agent, a neuroleptic agent and the like have been used so far. However, clinical effects of these agents are insufficient, and these agents are not necessarily satisfactory in view of the side effects. Accordingly, the development of a new type of a drug which is free of a side effect and which has an excellent activity of improving a digestive tract moving function has been in demand.


DISCLOSURE OF THE INVENTION

An object of the present invention is to provide a novel compound having an excellent activity of improving a digestive tract moving function.
Another object of the present invention is to provide a novel compound which is free of a side effect and which has an excellent activity of improving a digestive tract moving function.
Another object of the present invention is to provide a pharmaceutical composition containing said compound.
These and other objects of the present invention will be apparent from the following description and examples.
It has been considered that since a calcium channel blocker exhibits an activity of inhibiting contraction of a smooth muscle, it is effective for treating diseases caused by abnormal acceleration of contraction of the intestinal tract, for example, intestinal diseases such as an irritable bowel syndrome. In fact, it has been reported that a calcium channel blocker such as nicardipine, verapamil or the like is effective for treating an irritable bowel syndrome [Am. J. Gastroenterol., 80, 317 (1985), Gut., 28, 1609 (1987), J. Clin, Psychiatry., 48, 388 (1987), and Pharmacol. Ther., 60, 121 (1993)]. Actually, however, this calcium channel blocker is little applied clinically owing to its main effect on the heart blood vessel system. Under these circumstances, the present inventors have assiduously conducted investigations to develop a calcium channel blocker which exhibits a low toxicity, namely which gives no influence to the heart blood vessel system and which has a selectivity for the intestinal tract as an agent of treating the digestive tract abnormal moving function diseases, especially the

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