Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
1998-11-06
2001-01-30
Krass, Frederick (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
C514S193000, C514S202000, C514S205000, C514S209000
Reexamination Certificate
active
06180621
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention relates to an anti-
helicobacter pylori
composition comprising 1-methylcarbapenem derivatives or pharmacologically acceptable salts or esters thereof as an active ingredient, use of the derivatives, salts or esters for the preparation of an anti-
helicobacter pylori
medicament and a method which comprises administering a pharmacologically effective amount of the derivatives, salts or esters to warm-blooded animals for treatment and prevention of infectious diseases caused by
helicobacter pylori.
2. Background Information
According to recent studies, there are a number of reports on the phenomenon that
helicobacter pylori
is detected at a high ratio in patients suffering from chronic gastritis or digestive ulcers, and that such gastrointestinal disorders are cured by the eradication of
helicobacter pylori;
and on the phenomenon that the recurrence ratio of digestive ulcers shows a drastic decrease as a result of the eradication of this bacterium. It is therefore thought that infection with this bacterium relates to chronic and digestive ulcers and, furthermore, it even has a close relationship with gastric cancer or gastritis (G. E. Buck et al., J. Infect. Dis., 153, 664-669(1986), G. Geis et al., J. Clinical Microbiology, 930-932(1990), etc.).
At present, it is reported that bismuth compounds such as bismuth citrate, nitroimidazole compounds such as metronidazole and antibiotics such as tetracycline, amoxicillin and clarithromycin are effective against
helicobacter pylori.
None of these compounds has sufficient antibacterial activity and each has a chemical structure markedly different from that of the 1-methylcarbapenem derivatives which are an active ingredient to be employed in the present invention.
The 1-methylcarbapenem derivatives, which are an active ingredient of the present invention, are known compounds (for example, Japanese Patent Publication No. Hei 745499, Japanese Patent Application Kokai No. Hei 2-223587, Japanese Patent Application Kokai No. Hei 4-279588, Japanese Patent Application Kokai No. Hei 8-53453 etc.), but their anti-
helicobacter pylori
activity is not known at all.
SUMMARY OF THE INVENTION
The present inventors have carried out an extensive investigation into the antibacterial activity of 1-methylcarbapenem derivatives. As a result, it has been found that specific 1-methylcarbapenem derivatives have excellent anti-
helicobacter pylori
activity and are useful as an active ingredient in an anti-
helicobacter pylori
composition (treatment or prevention of infectious diseases caused by
helicobacter pylori,
particularly, treatment).
The present invention provides an anti-
helicobacter pylori
composition comprising 1-methylcarbapenem derivatives or pharmacologically acceptable salts or esters thereof as an active ingredient, use of the derivatives, salts or esters for the preparation of an anti-
helicobacter pylori
medicament and a method comprising administering a pharmacologically effective amount of the derivatives, salts or esters to warm-blooded animals for treatment and prevention of infectious diseases caused by
helicobacter pylori.
1-Methylcarbapenem derivatives, an active ingredient of the present invention, have the following formula:
wherein R
1
represents a group of the following formula:
R
2
represents a hydrogen atom or a C
1
-C
6
alkyl group, and
R
3
represents a hydrogen atom or a C
1
-C
6
alkyl group.
REFERENCES:
patent: 5153187 (1992-10-01), Iwasaki et al.
patent: 5424306 (1995-06-01), Kawamoto et al.
patent: 5607671 (1997-03-01), Heino
patent: 642797 (1995-03-01), None
patent: 7-45499 (1990-02-01), None
patent: 2-223587 (1990-09-01), None
patent: 4-279588 (1992-10-01), None
patent: 8-53453 (1996-02-01), None
G.E. Buck et al., “Relation ofCampylobacter pyloridisto Gastritis and Peptic Ulcer”,J. Infect. Dis., 153, 664-669 (1986).
G. Geis et al., “Unusual Fatty Acid Substitution in Lipids and Lipopolysaccharides ofHelicobacter pylori”,J. Clinical Microbiology, 930-932 (1990).
Kawamoto Isao
Ohya Satoshi
Utsui Yukio
Frishauf, Holtz Goodman, Langer & Chick, P.C.
Krass Frederick
Sankyo Company Limited
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