Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
2000-05-23
2002-11-26
Fay, Zohreh (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
active
06486161
ABSTRACT:
BACKGROUND OF THE INVENTION
The present invention relates to a method for treating mastitis in a domestic animal (mammal), a therapeutic medicament for, or use of certain rifamycin derivatives for the manufacture of a therapeutic medicament for mastitis in a domestic animal. More particularly, the invention relates to a method for treating an inflammatory disease caused by infection with a bacterium in the mammary gland of a domestic animal such as a dairy cow or a goat, which comprises administering to the animal a pharmaceutical composition comprising as an active ingredient a rifamycin derivative or a physiologically acceptable salt thereof, and a physiologically acceptable carrier. Also, the present invention provides a therapeutic medicament for mastitis in a domestic mammal which comprises said rifamycin derivative, or use of said derivative for the manufacture of said therapeutic medicament.
Mastitis in domestic animals raised for obtaining milk such as a dairy cow and a goat is a disease in which the mammary glands in the animals are infected with Staphylococcus (e.g.,
Staphylococcus aureus
),
Escherichia coli,
or another pathogenic bacterium causing inflammation; or a disease related to such a bacterium. Mastitis is a very costly disease for the dairy industry due to its high incidence, and the resulting reduced milk production, reduced milk quality and increased culling (removal) of animals from dairy herds.
As described above, mastitis is a very serious disease in domestic animals, and a known therapy frequently used is the administration by infusion of an antimicrobial drug directly into the mammary gland of a domestic animal affected with mastitis. Most of the mastitis is cured or alleviated by such an infusion for treating mastitis. However, due to a change in the kind of bacterium causing mastitis and a lowering of susceptibility of a bacterium causing mastitis to existing antimicrobial drugs for treating mastitis, at present mastitis for which no therapeutic effect is obtained by known drugs has increased.
For instance, cefazolin which is a first-generation cephalosporin antibiotic has been used for treating this disease. However, cases wherein treatment of mastitis is difficult have increased because bacteria resistant to this antibiotic have appeared and increased at present. Also, although cefem antibiotics and the like have been used, their effect is not sufficient for treating mastitis. In order to develop more effective therapy, it is necessary to introduce a new, more effective therapeutic agent.
An object of the present invention is to provide a method for treating mastitis in a domestic animal in need of such a treatment, which comprises administering to the animal a pharmaceutical composition comprising a rifamycin derivative of the formula (1):
wherein R is an alkyl group having 1 to 7 carbon atoms or a physiologically acceptable salt thereof as an active ingredient, and a physiologically acceptable carrier. Also, the present invention provides a therapeutic medicament for mastitis in a domestic mammal which comprises said rifamycin derivative, or use of said derivative for the manufacture of said therapeutic medicament.
This and other objects of the present invention will become apparent from the following description.
SUMMARY OF THE INVENTION
In accordance with the present invention, there is provided a method for treating mastitis in a domestic animal in need of such a treatment, which comprises administering to the animal a pharmaceutical composition comprising a rifamycin derivative of the formula (1):
wherein R is an alkyl group having 1 to 7 carbon atoms or a physiologically acceptable salt thereof as an active ingredient, and a physiologically acceptable carrier. Also the present invention provides a therapeutic medicament for mastitis in a domestic mammal comprising said rifamycin derivative or use of said derivative for the manufacture of said therapeutic medicament.
DETAILED DESCRIPTION
The alkyl group having 1 to 7 carbon atoms in R in the rifamycin derivative (1) used in the present invention includes linear, branched and cyclic alkyl groups such as methyl group, ethyl group, propyl group, isopropyl group, cyclopropyl group, butyl group, isobutyl group, sec-butyl group, tert-butyl group, cyclobutyl group, cyclopropylmethyl group, pentyl group, isopentyl group, sec-pentyl group, tert-pentyl group, 1,2-dimethylpropyl group, 1-ethylpropyl group, cyclopentyl group, cyclobutylmethyl group, hexyl group, 4-methylpentyl group, cyclohexyl group, 3-methylcyclopentyl group, heptyl group, isoheptyl group, and the like. Methyl, ethyl, propyl, isopropyl, cyclopropyl and isobutyl groups are preferred.
The rifamycin derivative (1) used in the present invention for treating mastitis in a domestic animal can be obtained by methods disclosed in, for example, Japanese Examined Patent Publication (Kokoku) No. 57275/1993, Japanese Unexamined Patent Publication (Kokai) Nos. 007291/1991, 101681/1991 and 03589/1992, and Chem. Pharm. Bull., Vol. 41, 148 (1993), and the like.
The rifamycin derivative (1) is able to form a salt with either an acid or a base. As the acid or base which can be used for the salt formation, any one capable of forming a salt with the rifamycin derivative (1) can be used. Examples of the salt with a base are (1) metal salts, particularly alkali metal salts such as sodium salts and potassium salts and alkaline earth metal salts such as calcium salts, (2) ammonium salts, and (3) amine salts, particularly salts with methylamine, ethylamine, diethylamine, triethylamine, pyrrolidine, morpholine and hexamethyleneimine, and the like. Examples of the salt with an acid are (1) salts with mineral acids such as sulfuric acid and hydrochloric acid, and (2) salts with organic acids such as p-toluenesulfonic acid, trifluoroacetic acid and acetic acid.
A physiologically acceptable salt of the rifamycin derivative (1) which can be used in the present invention is selected from the above-mentioned salts which are physiologically acceptable.
The domestic animal to be treated in the present invention is preferably an animal kept and/or fed for obtaining milk, such as a dairy cow or a goat.
Each of the rifamycin derivatives (1) wherein each R is methyl group, ethyl group, propyl group, isopropyl group, cyclopropyl group or isobutyl group was orally administered to mice in a dose of 1,000 mg/kg. They did not show any toxicity, so it was confirmed that the rifamycin derivatives shown by the formula (1) have low toxicity.
The pharmaceutical composition used according to the present invention is administered orally or parenterally. In case of parenteral administration of the above-mentioned composition to a domestic animal in need of treatment for mastitis according to the present invention, the composition may be injected or infused hypodermically, intradermally, intramuscularly or through the lactiferous duct in the form of an injection preparation or an infusion preparation. However, the administration route is not limited to these examples.
The pharmaceutical composition which contains as an active ingredient the rifamycin derivative (1), or its physiologically acceptable salt, used according to the present invention may be, for example, in the form of an injection preparation or an infusion preparation such as an aqueous suspension preparation, an oily suspension preparation, an emulsion preparation or a solution preparation. The above-mentioned composition used according to the present invention may also be, for example, in the form of a preparation for oral administration such as powder, tablets including sugar-coated tablets, capsules, pills, fine granules, granules or syrup. A physiologically acceptable carrier contained in the pharmaceutical composition used in the present invention may be any carrier including a solvent which is usually used for preparing a pharmaceutical composition in the art. A solvent used in the injection or infusion preparation according to the present invention includes water, a water-miscible solvent and an oily solvent.
Fujii Kenji
Hosoe Kazunori
Watts Jeffrey L.
Yamashita Katsuji
Yancey, Jr. Robert J.
Armstrong Westerman & Hattori, LLP
Fay Zohreh
Kaneka Corporation
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