Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heavy metal containing doai
Patent
1994-07-13
1995-12-12
Nazario-Gonzales, Porfirio
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heavy metal containing doai
514894, 514925, 556119, 556130, A61K 31315, C07F 306
Patent
active
054750288
DESCRIPTION:
BRIEF SUMMARY
This application is a request for U.S. examination under 35 U.S.C. 371 of International application No. PCT/JP93/0057, filed on Jan. 13, 1993.
1. Technical Field
The present invention relates to a novel 2-aminoethanesulfonic acid zinc complex, to a process for producing the same and to an anti-hepatitis agent, liver function improving agent and anti-ulcer agent, which individually contain the same as an active ingredient.
2. Background Art
2-Aminoethanesulfonic acid (taurine) has already been known to possess liver-function protecting activity, but much cannot be expected of the compound as an excellent anti-hepatitis and liver-function improving agent, because of its weak physiological activity.
The present inventors, with a specific view to the development of excellent pharmaceuticals from 2-aminoethanesulfonic acid, synthesized numerous derivative compounds and tested them for their pharmacological activities. It was found that a novel 2-aminoethanesulfonic acid zinc complex, among them, can be synthesized by reacting 2-aminoethanesulfonic acid with an alkali agent and zinc compound or by reacting an alkali metal salt of 2-aminoethanesulfonic acid with bis(2-aminoethanesulfonic acid) zinc salt, and the subsequent investigation of its therapeutic effects, toxicological properties and the like revealed that the compound possesses marked anti-hepatitis, liver-function improving and anti-ulcer activities. Such findings, followed by further research work, resulted in the completion of the present invention.
DISCLOSURE OF THE INVENTION
The present invention relates to a 2-aminoethanesulfonic acid zinc complex represented by the general formula: ##STR2## (wherein M is an alkali metal atom), to a process for producing the said complex from 2-aminoethanesulfonic acid and to use of the complex as an anti-hepatitis agent, liver-function improving agent and anti-ulcer agent which individually contain the same as an active ingredient.
As the alkali metal atom represented by M in the general formula (I), there may be mentioned sodium, potassium and the like. The compound of the general formula (I) can be produced, for example, by reacting 2-aminoethanesulfonic acid (1 mole) with an alkali agent (1 mole) and zinc compound (0.25 mole). The reaction, when conducted with use of the zinc compound (0.5 mole), was also found to give the compound of the general formula (I) in the same yield. Referring to the alkali agent, there may preferably be used alkali metal alcoholates such as sodium methylate, sodium ethylate, potassium methylate, potassium ethylate and potassium t-butoxide, while as the zinc compound, zinc acetate is preferred but other zinc compounds may be utilized. The reaction is usually carried out in a suitable solvent such as methanol and ethanol at room temperature or under heating for several minutes to several hours, and after the conclusion of the reaction, the reaction product can be purified by conventional means. Also, the compound of the general formula (I) can be produced by reacting an alkali metal salt of 2-aminoethanesulfonic acid (1 mole) with bis(2-aminoethanesulfonic acid) zinc salt (0.5 mole), wherein as the alkali metal, use is made of sodium, potassium, etc. The reaction is normally conducted in a suitable solvent such as methanol and ethanol at room temperature or under heating for several minutes to several hours and after the reaction is completed, the reaction product can be purified by conventional means.
The compound of the general formula (I) according to the present invention exhibits improved anti-hepatitis, liver-function improving and anti-ulcer activities, while it shows reduced toxicity. The compound can be administered orally or parenterally either per se or after being admixed with pharmacologically acceptable excipients, carriers, diluents, etc. to process into various dosage forms such as tablets, capsules, granules, powders and syrups. The dosage amount varies with the symptoms, age and body weight of patients, route of administration, and the like, and the compound can u
REFERENCES:
Chemical Abstracts, vol. 74, No. 14, Abstract No. 71065p (1971).
International Search Report (1993).
Fujimura Hajime
Nagamura Yoichi
Tanaka Teruo
Yabuuchi Takahiro
Nazario-Gonzales Porfirio
Zaidan Hojin Seisan Kaihatsu Kagaku Kenkyusho
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