Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heavy metal containing doai
Patent
1994-12-20
1996-04-09
Nazario-Gonzales, Porfirio
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heavy metal containing doai
514925, 514926, 556132, 556134, A61K 31315, C07F 306
Patent
active
055062644
DESCRIPTION:
BRIEF SUMMARY
This application is a request for U.S. examination filed under 35 U.S.C. .sctn.371 of International application No. PCT/JP93/00852 filed on Jun. 21, 1993.
TECHNICAL FIELD
The present invention relates to a novel zinc tranexamate compound and its pharmacologically acceptable organic acid salts, to a process for producing the same and to anti-inflammatory and anti-ulcer agents which individually contain the same as an active ingredient.
BACKGROUND ART
Tranexamic acid inhibits the bonding of plasminogen or plasmin with fibrin to lower their fibrinolytic activities, and thus suppress bleeding. By way of such a mechanism, the compound suppresses vascular fragility and also develops anti-allergic and anti-inflammatory activities. Specifically, the compound is considered to be effective against hyperemia, reddening, swelling and ache accompanying by tonsillitis, pharyngo-laryngitis, stomatitis, aphtha in the mucosa of the mouth. However, no report has been made so far on the anti-gastritic and anti-peptic/duodenal ulcer activities of tranexamic acid, with no paper being published on the synthesis and pharmacological activities of the zinc tranexamate compound.
The present inventors, with a specific view to the development of an excellent anti-ulcer agent and anti-gastritis agent, synthesized a large number of zinc compounds and investigated their therapeutic effects, and, as a result, found that zinc tranexamate, among others, exhibits distinctly marked therapeutic activities. The finding was followed by further research work, leading to the completion of the present invention.
DISCLOSURE OF THE INVENTION
The present invention relates to a novel zinc tranexamate compound as represented by the formula (I): ##STR2## and its pharmacologically acceptable salts with organic acids, to a process for producing the same and to an anti-inflammatory agent and anti-ulcer agent which individually contain the same as an active ingredient.
The compound of formula (I) is produced by reacting a compound of formula (II): ##STR3## with an alkali agent and zinc compound. 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, use is normally made of zinc salts soluble in a reaction solvent such as zinc acetate, zinc chloride, zinc bromide and zinc iodide, but other zinc compounds may be utilized. The reaction is preferably carried out in a water-free solvent and 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 conclusion of the reaction, the compound of the formula (I) that crystallizes out can be purified by conventional means.
The present invention is understood to cover pharmacologically acceptable organic-acid salts of the compound of the formula (I), and their examples include salts with aliphatic carboxylic acids, such as acetic acid; glycolic acid, lactic acid, succinic acid, malic acid, tartaric acid, maleic acid and fumaric acid; amino acids; such as aspartic acid and glutamic acid; and aromatic carboxylic acids such as benzoic acid and phthalic acid.
Organic-acid salts of the compound (I) are obtained, for example, by adding the compound (I) to an organic acid dissolved in methanol or another anhydrous solvent to allow them to react.
The compound of the formula (I) according to the present invention and its organic-acid salts possess excellent anti-aphtha activity, anti-gastric/duodenal ulcer activity, and anti-gastritis/duodenitis activity, while they exhibit lower toxicity. The compound of the formula (I) and its organic-acid salts can be administered orally or parenterally either per se or after being admixed with pharmacologically acceptable, appropriate excipients, carriers, diluents, etc. to process into various dosage forms such as tablets, capsules, granules and powders. Also, the organic acid salts of the compound of the formula (I
REFERENCES:
Database WPI, week 8220, Derwent Publications Ltd., London, GB AN82-40390E & JP-A-57-059-847 (Hisamitsu Pharm) Abstract (1982).
Fujimura Hajime
Tanaka Teruo
Yabuuchi Takahiro
Nazario-Gonzales Porfirio
Zaidan Hojin Seisan Kaihatsu Kaguki Kenkyusho
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