Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1990-09-12
1992-03-03
Goldberg, Jerome D.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
A61K 3144
Patent
active
050933426
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
The present invention relates to the new use of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]-sulfinyl]-1H-ben zimidazole (generic name: omeprazole) or a salt thereof as an antimicrobial agent and more particularly as an antimicrobial agent, which is particularly active against gram-negative bacteria.
BACKGROUND OF THE INVENTION
In view of the abuse or unscrupulous use of antimicrobial drugs in the treatment of infectious diseases or for other purposes and the consequent emergence of drug-resistant strains, increased incidence of microbial substitution due to disturbance of the bacterial flora, changes in profile of infectious diseases, etc., there has been a constant demand for the development of new antimicrobial agents.
This application is especially directed to the treatment of infections caused by Campylobacter pylori. Campylobacter pylori is a gram-negative spirilliform bacterium which colonises deeply in the gastric mucosa. Treatment with commonly used antibiotics has given insufficient effect.
PRIOR ART
Omeprazole and its pharmaceutically acceptable salts, which are used in accordance with the invention, are known compounds, e.g. from EP 5129 and EP 124495 and can be produced by known processes, for example by the process described in Japanese Patent Application No. 34956/1985.
OUTLINE OF THE INVENTION
The intensive research undertaken by the inventors of the present invention for accomplishing the above-mentioned object revealed surprisingly that 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]-sulfinyl]-1H-ben zimidazole (generic name: omeprazole) and pharmaceutically acceptable salts thereof, which are known to have gastric antisecretory activity known to be an antiulcer drug have excellent antimicrobial activity as well.
Heretofore, it has never been known that omeprazole or any compound analogous thereto has antimicrobial activity.
Predicated on the above finding, the present invention relates to an antimicrobial agent containing omeprazole or a salt thereof as an active ingredient.
The salt of omeprazole is virtually optional in kind but is preferably a pharmaceutically acceptable salt. Examples of such salts include inorganic salts, such as alkali metal salts, e.g. sodium salt, potassium salt etc., alkaline earth metal salts. e.g. calcium salt, magnesium salt etc., ammonium salt, organic salts such as organic amine salts, e.g. trimethylamine salt, triethylamine salt, pyridine salt, procaine acid, picoline salt, dicyclohexylamine salt, N,N-dibenzylethylenediamine salt, N-methylglucamine salt, diethanolamine salt, triethanolamine salt, tris(hydroxymethylamino)methane salt, phenylethylbenzylamine salt, dibenzylethylenediamine salt.
The antimicrobial agent according to the present invention is particularly active against gram-negative bacteria, especially microaerophilic bacteria, inter alia bacteria of the genus Campylobacter represented by C. pylori, and can be effectively utilized for the prevention and treatment of infectious diseases due to such bacteria in mammalian animals including man, cattle, horse, dog, mouse and rat, in the control and inhibition of environmental pollution, or as a disinfectant.
The antimicrobial agent according to the present invention can be made available in a pharmaceutical formulation comprising one or more active ingredients selected from the group consisting of omeprazole and salts thereof or in a formulation containing optional substances as additives (for example, a carrier).
For the treatment or prevention of bacterial infections, for instance, the antimicrobial agent of the invention is generally administered in the form of a pharmaceutical preparation containing omeprazole as such (i.e. the free base) or a salt thereof as an active ingredient in combination with a pharmaceutically acceptable carrier by the oral, rectal or parenteral route. The carrier mentioned above may be a solid, semi-solid or liquid diluent or a capsule. Compatible dosage forms include various types of tablets, capsules, granules,
Ikeda Yoshifumi
Tomoi Masaaki
Yokota Yoshiko
Aktiebolaget Hassle
Goldberg Jerome D.
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