Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1993-11-23
1995-03-28
Ford, John M.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
544 12, A61K 3154, C07D28524
Patent
active
054017394
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to novel benzothiadiazine derivatives, hydrates thereof and acid addition salts thereof. The compounds of the present invention have activity to inhibit secretion of gastric acid and activity to protect the gastric mucosa and are useful for treating peptic ulcers.
BACKGROUND ART
Ulcers occurring in the stomach or duodenum are caused primarily by hypersecretion of gastric acid. Some drugs are known recently for inhibiting the secretion of gastric acid by blocking the activity of the histamine H.sub.2 receptor. Several kinds of drugs of this class, such as cimetidine and famotidine, are commercially available at present. However, although these histamine H.sub.2 receptor antagonists exhibit high curing effects, they have the problem of being very likely to permit subsequent recurrence, so that it has been attempted to use such antagonists in combination with an anti-ulcer drug having activity to protect the gastric mucosa. Accordingly, drugs for treating peptic ulcers should preferably have activity to inhibit gastric acid secretion and activity to protect the gastric mucosa, and it is strongly desired to develop drugs having both of these activities.
DISCLOSURE OF THE INVENTION
We have conducted intensive research in view of the foregoing problem of the background art and consequently found that novel benzothiadiazine derivatives represented by the general formula (I) given below, hydrates thereof and acid addition salts thereof have excellent activities to suppress gastric acid secretion and to protect the gastric mucosa and are useful as medicinals. Thus, the present invention has been accomplished.
More specifically, the present invention provides benzothiadiazine derivatives, hydrates thereof and acid addition salts thereof, the derivatives being represented by the general formula (I) ##STR2## wherein X is methylene or a nitrogen atom substituted with a lower alkyl, Y and Z are each methylene or carbonyl, A is phenylene or phenylene substituted with methoxycarbonyl, R.sub.4 is lower alkylene or lower alkenylene, R.sub.1 is a hydrogen atom, acetoxyacetyl, cyclohexylmethyl or benzyl wherein the benzene ring may be substituted with lower alkoxyl, halogen atom, nitro, lower alkyl, methylenedioxy or hydroxyl, R.sub.2 is lower alkyl or phenyl, and R.sub.3 is a hydrogen atom, halogen atom or lower alkoxyl with the exception of the case where X, Y and Z are each methylene, A is unsubstituted phenylene, R.sub.4 is lower alkylene and R.sub.1 is a hydrogen atom.
The compounds of the present invention represented by the general formula (I) have excellent activities to inhibit gastric acid secretion and to protect the gastric mucosa and are effective for treating peptic ulcer.
Accordingly, the present invention provides a peptic ulcer treating agent containing a compound of the general formula (I), hydrate thereof or acid addition salt thereof in an effective amount and a pharmacological carrier.
The present invention further provides a method of treating peptic ulcer characterized by administering an effective amount of the compound of the general formula (I) to a patient.
With reference to the general formula (I), examples of lower alkyl groups as the substituent for the nitrogen atom represented by X, examples of lower alkyl groups represented by R.sub.2 and examples of lower alkyl groups as the substituent on the benzene ring of R.sub.1 are straight-chain or branched alkyl groups having 1 to 6 carbon atoms, such as methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, isopentyl, n-hexyl and the like. Among these, methyl or n-butyl is preferred. Examples of lower alkoxyl groups represented by R.sub.3 and examples of lower alkoxyl groups as the substituent on the benzene ring of R.sub.1 are straight-chain or branched alkoxyl groups having 1 to 6 carbon atoms, such as methoxy, ethoxy, n-propoxy, isopropoxy, n-butoxy, isobutoxy, sec-butoxy, tert-butoxy, n-pentyloxy, isopentyloxy, n-hexyloxy and the like. Among these, methoxy is pr
REFERENCES:
patent: 4558044 (1985-12-01), King
patent: 4590192 (1986-05-01), Fake et al.
Ajioka Hirofusa
Fujiwara Kosuke
Kajitani Makoto
Ohno Tomoyasu
Yamada Shozo
Ford John M.
Taiho Pharmaceutical Co. Ltd.
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