Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-04-07
1998-06-30
Davis, Zinna Northington
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514291, 546153, 546156, 546 89, C07D21536, A61K 3147
Patent
active
057734496
DESCRIPTION:
BRIEF SUMMARY
This is a 371 application of PCT/JP95102052 filed on Oct. 6, 1995.
TECHNICAL FIELD
The present invention relates to novel thioquinolone derivatives represented by the formula I and having antibacterial activity against Helicobacter pylori or pharmaceutically acceptable salts thereof and antibacterial agents containing the derivatives as effective components: ##STR1## wherein R.sub.1 and R.sub.2 respectively represent hydrogen atom or R.sub.1 and R.sub.2 are joined to form --O--(CH.sub.2).sub.2 --; -C.sub.12 alkoxy group, lower alkylsulfonyloxy group, carboxy lower alkoxy group, lower alkylthio group, benzyloxy group, benzylthio group, phenoxy group, styryl group, nitro group, phenyl group, naphthyl group, piperazinyl group, morpholino group or hydroxyl group or represents --CH.sub.2 R.sub.5, --COR.sub.6 or --NR.sub.7 R.sub.8 wherein R.sub.5 represents benzyl group, phenyl group, hydroxyl group, lower alkoxy group, lower alkylcarbonyloxy group, phenoxy group, di-lower alkylamino group or benzimidazolylthio group, R.sub.6 represents lower alkyl group or amino group and R.sub.7 and R.sub.8 respectively represent lower alkyl group; and R.sub.3 to form cyclohexene ring, benzene ring or pyridine ring, position 6 or methoxy group at position 6 of the quinoline ring when R.sub.1, R.sub.2 and R.sub.4 are respectively hydrogen atom, the quinoline ring when R.sub.1 and R.sub.2 are respectively hydrogen atom and R.sub.4 is lower alkyl group.
BACKGROUND ART
Helicobacter pylori is a spiral, short rod-shaped, gram-negative bacterium having at its one pole several sheath flagella. The bacteria are detected both in the gastric mucous layer and on the surface of gastric epithelial cells.
The fact that spiral bacteria live on and in a gastric mucosa has been observed by many researchers. Firstly in 1983, Marshall et al. succeeded in cultivating spiral bacteria through isolation of the same from a gastric mucosa. The bacterium was originally named Campylobacter pylori since its shapes and biochemical characteristics are analogous to those of the genus Campylobacter which is one of known enteritis-causing bacterial genera. However, later bacterial taxonomic researches established a new independent genus including the bacterium, and the bacterium was renamed Helicobacter pylori.
In 1984, Marshall et al. detected the bacteria at high percentage from patients suffering from peptic ulcer such as gastric and duodenal ulcers and chronic gastritis, and suggested relevance of the bacteria to occurrence and reccurrence of these diseases. As conventional remedies against peptic ulcer, medical treatments with gastric secretion inhibitors have been utilized; advent of H.sub.2 -blocker such as cimetidine and proton-pump inhibitor such as omeprazole enhanced the cure rate up to 80-90%. However, it has been reported that about 50% of patients healed with administration of anti-ulcer agents have relapse or reccurrence of ulcers within twelve months and that, particularly, patients healed with gastric secretion inhibitors such as H.sub.2 -blockers and proton-pump inhibitors have relapse rate of as high as 70-90%. Thus, prevention of the relapse or reccurrence is one of greatest problems in the treatment.
There have, however, been recently increasingly reported that removal of Helicobacter pylori (hereinafter referred to as Hp) with an antibacterial Vol. 44, No. 2, pp. 295-302, (1989)!; and, in February 1994, NIH in U.S.A. advised necessity of eradicating Hp in the treatment of peptic ulcer. Hp-removing agents used nowadays are for example antibiotics and bismuth preparations. Antibiotics are not suitable for long-term use since they may also affect other intestinal bacteria and may cause advent of resistant bacteria. Treatment with bismuth preparations is rather problematic since the bismuth preparations are weak in antibacterial activity and may cause vomiting, diarrhea and/or side effects on central nervous system.
Anti-ulcer agents with antibacterial activities against Hp have been proposed for example in Japanese Patent Provisional P
REFERENCES:
patent: 4619994 (1986-10-01), Shortridge
patent: 5081121 (1992-01-01), Osawa et al.
patent: 5189210 (1993-02-01), Wright et al.
Fukuda Naoki
Imaizumi Kazuhiro
Kobayashi Hideshi
Konishi Masataka
Oku Yukio
Davis Zinna Northington
Zenyaku Kogyo Kabushiki Kaisha
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