Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1993-06-25
1995-12-12
Henley, III, Raymond
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
A61K 3134
Patent
active
054750261
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP92/0/382, filed Oct. 23, 1992.
TECHNICAL FIELD
This invention relates to an agent for treating hepatic diseases.
BACKGROUND ART
It is well-known that the liver is an important organ which controls the metabolism of the body. It is said that as many as 40,000 people die of hepatic diseases in Japan in a year. Hepatic diseases such as hepatonecrosis, fatty liver, disorders of bile secretion, and cirrhosis are caused by the fact that the liver is acutely or chronically diseased by various factors such as alcohol, lack of nutrients, infection by viruses, chemical toxins and the like. At present, no drug which exhibits a prominent pharmacological effect for the treatment and prophylaxis of these hepatic diseases when orally administered has been discovered.
DISCLOSURE OF THE INVENTION
The object of the present invention is to provide an agent for treating hepatic diseases, which has excellent effect for curing hepatic diseases, which is stable, which can be administered not only parenterally, but also orally and which is safe.
The present inventors made extensive studies for developing an agent for treating hepatic diseases having excellent effectiveness and practicality to discover that beraprost is stable and has a prominent effect for promoting the functions of the liver, thereby completing the present invention.
That is, the present invention provides an agent for treating hepatic diseases comprising as an effective ingredient beraprost or a pharmaceutically acceptable salt thereof.
The agent for treating hepatic diseases according to the present invention has excellent effect in curing various hepatic diseases and is safe. Further, it is chemically stable, so that it can be orally administered.
BEST MODE FOR CARRYING OUT THE INVENTION
The compound (.+-.)-(1R*,2R*, 3aS*,8bS*)-2,3,3a,8b-tetrahydro-2-hydroxy-1-[(E)-(3S*)-3-hydroxy-4methyl-1 -ocetene-6-inyl]-1H-cyclopenta[b]benzofuran-5-butyric acid (beraprost is used as an agent for inhibiting tumor metastasis. This compound has the following structure. ##STR1##
Beraprost is described in Japanese Laid-open Patent Application (Kokai) Nos. 58-32277, 57-144276 and 58-124778 and the like as a PGI.sub.2 derivative having a skeleton in which the exoenol moiety characteristic to beraprost is converted to an inter-m-phenylene structure. However, it is not known that beraprost has activity to cure hepatic diseases.
The beraprost which is an effective ingredient of compositions of the present invention includes not only the racemic form, but also d-form and 1-form. Beraprost can be produced by, for example, the method described in the above-mentioned Japanese Laid-open Patent Application (Kokai) No. 58-124778. The salts of beraprost include any pharmaceutically acceptable salts including alkaline metal salts such as sodium salt and potassium salt; alkaline earth metal salts such as magnesium salt and calcium salt; ammonium salt; primary, secondary and tertiary amine salts; and basic amino acid salts.
When orally or parenterally administered, beraprost exhibits prominent effect in promoting the functions of the liver. Alternatively, a reduction in decrease of liver function due to disease is observed upon administration of berapost. More particularly, the agent for treating hepatic diseases according to the present invention is effective for treating acute and chronic hepatic diseases such as fatty liver, alcoholic hepatitis, toxic hepatic disorders, congestive liver, disorders of bile secretion, stagnation hepatic disorders, ischemic hepatic disorders, hepatic insufficiency, fulminating hepatitis and cirrhosis. Further, the agent is also effective for promoting functions of the liver suffering from hepatic disorders after surgery, and in ameliorating the decline in liver function due to viral hepatic disease and liver cancer. The agent is also effective for the protection of the liver during transplantation and for promoting the functions of the liver after transplantation.
The dose of administration of the compound differ
REFERENCES:
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Database WPI, Week 8733, Derwent Pub. Ltd., AN 87-229612 & EP-A-0 232 776 (abstract) 1987.
Official Journal Of The American Association For The Study Of Liver Diseases, vol. 16, No. 4PT2, Oct. 1992, p. 161A.
American Physiological Society, H. Araki et al., 1980, pp. H176-H181: "Cytoprotective Actions Of Prostacyclin . . . Cat Liver".
Experimental and Molecular Pathology 42, 163-166 (1985), A. Divald et al., "Hepatoprotective Effects of Prostacyclins . . . in Rats".
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Gastroenterology 1981; 81:211-217, J. Stachura et al., "Protaglandin Protection of Carbon Tetrachloride-Induced Liver Cell Necrosis . . . ".
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Fujiwara et al., AASLD Abstract. Hepatology 16 (4 Part 2), 1992.
Nishio Shintaro
Ueno Shinya
Henley III Raymond
Spivack Phyllis G.
Toray Industries Inc.
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