Use of carbostyril to increase somatostatin or for inhibiting de

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514253, 544333, 544405, 546157, A61K 3147, A61K 31535, A61K 31495, C07D40100

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active

054768586

DESCRIPTION:

BRIEF SUMMARY
This application is a continuation of PCT/JP93/00545 filed Apr. 27, 1993.


TECHNICAL FIELD

This invention relates to an agent for increasing secretion of somatostatin or for inhibiting decrease of secretion of somatostatin in the bio-body. More particularly, it relates to a pharmaceutical composition useful for increasing secretion of somatostatin or for inhibiting decrease of section of somatostatin which comprises as an esstial active ingredient a carbostyril compound of the formula: ##STR2## wherein R is a halogen atom, and the propionic acid substituent is substituted at 3- or 4-position on the carbostyril nucleus, and the bond between 3- and 4-positions is single or double bond, or a pharmaceutically acceptable salt thereof, preferably 2-(4-chlorobenzoylamino)-3-(2-quinolon-4-yl)propionic acid or a pharmaceutically acceptable salt thereof.


PRIOR ART

It is known that somatostatin is a growth hormone-release inhibiting factor secreted in the bio-body and when the secretion of somatostatin is decreased, there are induced various diseases, such as esophagitis, Zollinger-Ellison syndrome, diarrhea, erethistic colitis, various cancers, hepatitis, portal hypertension, headache, migraine, Alzheimer's disease, presbyophrenia, pancreatitis, acromegalia.
The present inventors have intensively studied to find a new drug useful for treating the diseases associated with the decrease of somatostatin, and have found that the carbostyril compounds of the above formula (1), particularly 2-(4-chlorobenzoylamino)-3-(2-quinolon-4-yl)propionic acid or a pharmaceutically acceptable salt thereof, are useful as an agent for increasing secretion of somatostatin or for inhibibing decrease of secretion of somatostatin.
The carbostyril compounds of the formula (I) and processes for the preparation thereof are disclosed in Japanese Patent Second Publication (Kokoku) No. 35623/1988, wherein it is disclosed that the carbostyril compounds are useful as an anti-ulcer drug.


SUMMARY OF THE INVENTION

This invention provides an agent for increasing secretion of somatostatin or inhibiting decrease of secretion of somatostatin comprising as an essential active ingredient a carbostyril compound of the formula (I) or a pharmaceutically acceptable salt thereof, a method of the treatment of diseases associated with decrease of somatostatin by administering the agent as set forth above, and use of the agent for the treatment of diseases associated with decrease of somatostatin.


DETAILED DESCRIPTION OF THE INVENTION

The agent of this invention is usually in the form of conventional pharmaceutical preparations, for example, preparations suitable for oral administration such as tablets, pills, powders, granules, capsules, solutions, suspensions, emulsions, and preparations for parenteral administration such as suppositories and injections (e.g. solutions, suspensions, etc.). These preparations can be prepared by a conventional method with conventional pharmaceutically acceptable carriers or diluents, such as fillers, thickening agents, binders, wetting agents, disintegrators, surfactants, lubricants, and the like.
In order to form in tablets, there are used conventional pharmaceutically acceptable carriers such as vehicles (e.g. lactose, white sugar, sodium chloride, glucose, urea, starches, calcium carbonate, kaolin, crystalline cellulose, silicic acid, etc.), binders (e.g. water, ethanol, propanol, simple syrup, glucose solution, starch solution, gelatin solution, carboxymethyl cellulose, shellac, methyl cellulose, potassium phosphate, polyvinylpyrrolidone, etc.), disintegrators (e.g. dry starch, sodium arginate, agar powder, laminaran powder, sodium hydrogen carbonate, calcium carbonate, polyoxyethylene sorbitan fatty acid esters, sodium laurylsulfate, stearic monoglyceride, starches, lactose, etc.), disintegration inhibitors (e.g. white sugar, stearin, cacao butter, hydrogenated oils, etc.), absorption promoters (e.g. quaternary ammonium base, sodium laurylsulfate, etc.), wetting agents (e.g. glycerin, starches, etc.), adsorbents (st

REFERENCES:
patent: 4578381 (1986-03-01), Uchida et al.
patent: 4612302 (1986-09-01), Szabo et al.
Folia Pharmacol. Jpn. vol. 97, No. 6, 1991, pp. 371-380 S. Kawano et al. `Protective Effect Of Rebamipide (OPC-12759) On The Gastric Mucosa In Rats And Humans` see p. 377; table 3.
`Dorland's Illustrated Medical Dictionary, 26th Edition` 1985, W. B. Saunders Company, Philadelphia see p. 1222.
De,A,3 324 034 (Otsuka Pharmaceutical Co., Ltd.) Jan. 5, 1984 see pp. 24-25.

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