Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ketone doai
Patent
1990-07-25
1992-04-28
Friedman, S. J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ketone doai
A61K 3112
Patent
active
051090252
DESCRIPTION:
BRIEF SUMMARY
DESCRIPTION
1. Technical Field
The present invention relates to a therapeutic agent for renal disorders. More particularly, it relates to a therapeutic agent for renal disorders drug which has a therapeutical activity for the therapy of kidney disease, antiallergic activity and antiulcer activity as well as general antiinflammatory activity.
2. Background Art
Many nonsteroidal antiinflammatory drugs (NSAID) have heretofore been developed and they have been used widely for clinical therapy of various inflammatory diseases. However, these NSAID have a defect that they tend to cause serious side effects such as gastric ulcer and it is difficult to use them continuously for a long period of time although they exhibit potent antiinflammatory activity against acute inflammation. They have almost no effect against chronic inflammation and organ inflammation. For kidney diseases, there have heretofore been known few drugs inclusive of antiinflammatory drugs and diuretics and adrenocortical steroids have been used for the therapy of kidney diseases. However, they each exhibit poor therapeutical effect instead of high side effects. Thus, development of effective drugs has been desired.
The present inventors have previously found that isoliquiritigenin, one of chalcone derivatives, is effective as an antiallergic drug (Japanese Patent No. 1570239; Japanese Patent Application, Second Publication No. Hei 1-52363, Japanese Pat. No. 1570239, U.S. Pat. No. 4,952,564); and further that isoliquiritigenin is effective in the therapy and prophylaxis of kidney and liver diseases and proposed their use (Japanese Patent Application, First Publication No. Hei 1-104010) U.S. Pat. No. 4,898,890.
Furthermore, it has become clear in recent years that the chalcone derivative 2', 3, 4, 4'-tetrahydroxychalcone, also known as butein, which has a chemical structure resembling that of isoliquiritigenin, has antiallergy activity (Japanese Patent Application, First Publication Serial No. Sho-63-10720), antiulcer activity (Japanese Patent Application, First Publication Serial No. Sho. 63-150241, Japanese Patent Application, First Publication Serial No. Sho 64-42422), as well as general antiinflammatory activity (U.S. Pat. No. 4,279,930). However, no therapeutic activity against renal disorders has previously been demonstrated for this compound.
DISCLOSURE OF INVENTION
The present inventors have made intensive investigation with view to developing a novel therapeutic agent for renal disorders which has a therapeutical effect for kidney diseases more potent than isoliquiritigenin and which has also general antiinflammatory activity and antiallergic activity but does not cause injury to digestive organs and is of low toxicity. As the result, it has now been found that 2',3,4,4'-tetrahydroxychalcone (hereafter, sometimes referred to as "THC"), which is also called as "butein", and its salts have a therapeutical effect for kidney diseases more potent than isoliquiritigenin, have also general antiinflammatory activity and antiallergic activity, do not cause injury to digestive organs, and have in addition antiulcer activity, thus serving as a desirable drug for clinical therapy. The present invention has been completed based on this discovery.
Therefore, the present invention provides a therapeutic agent for renal disorders comprising as active ingredient 2',3,4,4'-tetrahydroxychalcone represented by formula (I) ##STR1## or its pharmacologically acceptable salt.
Furthermore, the present invention provides a method for the therapy of kidney diseases comprising administering to warm blooded animal a therapeutically effective amount for the therapy of the objective disease or diseases of a therapeutic agent for renal disorders comprising as active ingredient 2',3,4,4'-tetrahydroxychalcone represented by formula (I) ##STR2## or its pharmacologically acceptable salt.
BRIEF DESCRIPTION OF DRAWINGS
Single figure is a graph representing the inhibitory activity of 2',3,4,4'-tetrahydroxychalcone against carragheenin plantar edema. In the figure, "THC"
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Komazawa et al., 1989, Chem. Abs. 110(3): "Antiulcer agents containing chalcone derivatives . . . "-refering to JP Applicn. with date of Dec. 12, 1986.
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Yokumoto et al., 1989, Chem. Abs. 110(11):88620a. "Allergy inhibitors containing chalcone derivatives,-referring to patent document with date of Jul. 1, 1986".
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Derwent Patent Abstracts, No. 89-059210 & Chemical Abstracts, vol. 111, No. 23, 4th Dec. 1989, p. 564, abstract No. 214230j, Columbus Ohio, U.S.; & JP-A-01 13 019 (Tsumura & Co.) Jan. 17, 1989 *Abstract*.
Chemical Abstracts, vol. 100, No. 19, Abstract No. 154304x (Chem. Abstr. 100 (19): 154304x), 7 May 1984, Brown, S., et al., Xenobiotica, 13 (11), 669 (1983).
Kakegawa Hisao
Matsumoto Hitoshi
Satoh Toshio
Dainippon Ink and Chemicals Inc.
Friedman S. J.
Nippon Hypox Laboratories Incorporated
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