Quinoline derivative and antiulcer agent containing said quinoli

Details Quinoline derivative and antiulcer agent containing said quinoli Quinoline derivative and antiulcer agent containing said quinoli

1991-11-27

1993-06-01

Ivy, C. Warren

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

546160, 546161, A61K 3147, C07D21544

Patent

active

052159990

DESCRIPTION:

BRIEF SUMMARY
FIELD OF THE INVENTION

The present invention relates to a novel quinoline derivative, salt thereof and an antiulcer agent containing said quinoline derivative, and a method of producing said quinoline derivative.


DESCRIPTION OF THE PRIOR ART

As an antiulcer agent, there have been conventionally known quinoline derivatives disclosed by, for example, Japanese Unexamined Patent Applications Nos. 147222/1980 (and J. Med. Chem. 1990, 33, 527-533) and 40482/1989, European Laid-Open Patent Applications Nos. 0259174, 0330485 (and Austrian Laid-Open Patent Application No. 8930117), 0336544 and 0239129, and U.S. Patent Publications Nos. 4578381 and 473890. As so-called intermediate documents, there have been also known Japanese Unexamined Patent Applications Nos. 117663/1990 (laid-opened to the public on May, 2, 1990) and 17078/1991 (laid-opened to the public on Jan. 25, 1991).
As quinoline derivatives themselves, there have been known those set forth in Japanese Unexamined Patent Applications Nos. 22074/1988, 233960/1988 and 22589/1988, besides the documents above-mentioned.
It is an object of the present invention to provide a compound which is different in structure from any of the compounds above-mentioned, and which is useful as an antiulcer agent because it is superior in antiulcer function to any of the compounds above-mentioned.


DISCLOSURE OF THE INVENTION

The quinoline derivative in accordance with the present invention is a compound of the following general formula (1): ##STR2## wherein R.sup.1 is a lower alkoxy group, a halogen atom, a lower alkyl group, a lower alkylthio group, a lower alkanoyloxy-lower alkyl group, a halogen-substituted lower alkyl group or a hydroxy-group-substituted lower alkyl group; R.sup.2 and R.sup.3 may be same as or different from each other, and each is a hydrogen atom, a lower alkyl group, a halogen-substituted lower alkyl group, a cycloalkyl group having 3 to 8 carbon atoms, a cycloalkyl-lower alkyl group, a lower alkenyloxy group, a lower alkenyl group, a lower alkoxy-lower alkyl group, a phenyl lower alkyl group, a lower alkynyl group, a phenyl group having a lower alkyl group as a substituent group, or a hydroxy-group-substituted lower alkyl group; R.sup.4 is a phenyl, tetrahydronaphthyl or naphthyl group which may have, as a substituent group on the phenyl ring, one or two groups selected from the group consisting of a lower alkyl group, a halogen atom, a lower alkoxy group, a lower alkylthio group, a lower alkanoyl group, a phenyl group, a cyano group, a lower alkyl sulfinyl group, a lower alkoxycarbonyl group, a lower alkenylthio group, a phenyl lower alkylthio group, a benzoyl group, a hydroxy-group-substituted lower alkyl group, a lower alkanoyloxy-lower alkyl group, a lower alkanoyloxy group and a hydroxyl group; n is 0, 1 or 2.
The compound of the present invention is adapted to decrease gastric acid secretion stimulated by a gastric acid secretion accelerating substance such as histamine, tetragastrin or foods, causing the compound to be useful for prevention and cure of a digestive ulcer of a human being and a mammal. The compound of the present invention is characterized in that its acid secretion inhibitory action is superior to and effective for a longer period of time as compared with a conventional antiulcer agent. Further, the compound in accordance with the present invention is remarkably effective in prevention and cure of an ulcer such as an aspirin ulcer or the like caused by an antiphlogistic pain-killer.
The production of a hydrochlonic acid in the gastric mucous membrane is adjusted by a variety of pharmacological factors, but the biochemical mechanism in the [H.sup.+ ] ion production finally enters the rate-determining step. Recently, it has been found that ATPase adapted to be activated by H.sup.+ and K.sup.+ at the gastric wall cells controls the acid secretion. This enzyme is present specifically in the gastric wall cells and serves as a key enzyme of a proton pump. An inhibitor of this enzyme may serve as a useful acid secretion inhibitory

REFERENCES:
patent: 4284768 (1991-08-01), Santilli
patent: 4342804 (1982-08-01), Munson, Jr. et al.
patent: 4578381 (1986-03-01), Uchida
patent: 4738970 (1988-04-01), Uchida
patent: 5089504 (1992-02-01), Ife et al.
J. Med. Chem. 1990, 33, 527-533.
EP 0336 544 (abstract).
JP Laid-open 55-147222 (abstract).
JP Laid-open 63-22074.
JP Laid-open 63-22589 (abstract).
JP Laid-open 63-233960 (abstract).
JP Laid-open 64-40482
JP Laid-open 2-117663.
JP Laid-open 3-17078.

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