Triazole substituted quinoline derivatives for gastrointestinal

Details Triazole substituted quinoline derivatives for gastrointestinal Triazole substituted quinoline derivatives for gastrointestinal

1996-01-29

1998-11-03

Ivy, C. Warren

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

546153, A61K 3147, C07D40104

Patent

active

058309039

DESCRIPTION:

BRIEF SUMMARY
This application is 371 of PCT/HW94/00008 which is now published as WO94/22413.
The invention is related to pharmaceutical compositions for protection and treatment of lesions of gastrointestinal mucous membrans and having secretion inhibiting and cytoprotective activity. More particularly the invention is related to pharmaceutical compositions containing as active ingredient certain quinoline derivatives and their salts in a biologically effective quantity optionally together with other active pharmaceutical ingredients, processes for their preparation and methods of treatment to use them alone or in combination with other pharmaceutically active ingredients.
In this specification the substituents of varying interpretation stand always for the following: 2 or for a C.sub. 1-4-alkyl-group,
It is accepted knowledge that peptic ulcer of the upper digestive tract is caused as a result of a disequilibrium between the defensive factors (force of mucosal resistance) and agressive factors (gastric acid and pepsin secretion) /e.g. Nature 236, 358,1972/. Pharmaceuticals inhibiting secretion are well known. Part of them are anticholinergs and histamine H.sub.2 -receptor antagonists such as e.g. cimetidin, ranitidine, famotidin, others are potassium ATP-ase inhibitors such as omeprasole. These drugs are effective against gastric and intestinal ulcer however on terminating their administration the ulcers reappear in a high ratio of patients especially in cases where the patients do not receive antiacidic drugs (Med.Res.Rev.10., 1, 1990).
Another possibility to fight against ulcer resides in the intensification of the protective factors. Protective mechanism is accomplished through the mucosal barrier which protects the gastric mucous membrane from the noxious effects of the luminal pepsin and hydrogen ions. The protection stands under a multifactoral control: ensures a non-mixing layer on the surface, (pH=2,0) and the center of the mucous membrane cells (pH=7),
All four of the above are influenced by the synthesis of the so called cytoprotective prostaglandins. (Contemporary issues in Gastroenterology Vol 3, Chapters 5 to 8, New York, 1985, Ed: Cohen and Saloway).
The non-steroidal antiinflammatory drugs (NSAID) like aspirin, indomethacin, naproxen, piroxicam etc. act by inhibiting the activity of the cyclooxygenase enzyme controlling the synthesis of prostaglandins to a different extent. However it has been shown that as a consequence of inhibiting activity of the cyclooxygenase during treatment with NSAIDs, the local prostaglandin E.sub.2 concentration of the gastric mucous membran is decreased resulting in erosions and ulcers (e.g. Lancet,2, 1253-54, 1978).
There are but some prostaglandin derivatives known (e.g. misoprostol) which were able to stop the damage of the gastric mucous membrane when administered after NSAID treatment (Scand. J. Gastroenterol. 9.page 751, 1974; 94, page 1973, 1988). Most of the known gastroprotectives however have to be administered before NSAID treatment.
Thus there is a need for an effective biological agent which is able on the one side to decrease gastric acidity and on the other hand to intensify the protective factors of the mucosa. This might result in a drug which might be administered together or after NSAID treatment for effective prevention or therapy of gastroenteropathy induced by NSAIDs.


SUMMARY OF THE INVENTION

One object of the present invention are pharmaceutical compositions for the treatment or prevention of lesions of gastrointestinal mucous membranes having secretion inhibiting and cytoprotective activities containing in a biologically effective quantity a triazole-group-substituted quinoline derivative of general formula (I) or its salts.
According to a previous patented invention a greater group of certain quinoline-derivatives containing a triazole groups was disclosed including also those of general formula (I). Their use as analgesics and antiphlogistics was shown on various pharmacological tests along with their fungistatic activity against phytopathogenic

REFERENCES:
patent: 4772613 (1988-09-01), Parsons et al.
patent: 5104884 (1992-04-01), Korodi et al.

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