Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-08-08
1996-03-05
Goldberg, Jerome D.
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
054968500
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP92/01313 filed Oct. 9, 1992.
TECHNICAL FIELD
This invention relates to an antimetastasis agent of malignant tumors.
BACKGROUND ART
Metastasis of malignant tumors is positioned as the terminal phase in the process of progress of tumors, which is a malignant phenotype that leads the patients to death. At present, chemotherapy agents are mainly used for inhibiting metastasis accompanied by enucleation of tumors. However, satisfactory results are not always obtained. Thus, development of an antimetastasis agent having high effectiveness is desired.
Recently, it was reported that prostaglandin I.sub.2 (PGI.sub.2) and the like are effective against hematogenous metastasis of mouse tumors (see Science, Vol. 212, 1270, (1981)). However, these compounds are unstable so that they cannot be systemically administered as pharmaceuticals.
DISCLOSURE OF THE INVENTION
Accordingly, an object of the present invention is to provide an antimetastasis agent of malignant tumors, which effectively inhibits metastasis of malignant tumors and which is safe.
That is, the present invention provides an antimetastasis agent of malignant tumors comprising as an effective ingredient beraprost or a pharmaceutically acceptable salt thereof.
The antimetastasis agent according to the present invention prominently inhibits the metastasis of malignant tumors and is safe. Further, it is chemically stable.
BEST MODE FOR CARRYING OUT THE INVENTION
The compound name of beraprost which is used as an antimetastasis agent of malignant tumors according to the present invention is (.+-.)-(1R*,2R*,3aS*,8bS*)-2,3,3a,8b-tetrahydro-2-hydroxy-1-[(E)-(3S*)-3-h ydroxy-4-methyl-1-octene-6-inyl]-1H-cyclopenta[b]benzofuran-5-butyric acid. This compound has the following structure. ##STR1##
Berlaprost is described in Japanese Laid-open Patent Application (Kokai) Nos. 58-32277, 57-144276 and 58-24778 and the like as a PGI.sub.2 derivative having a structure in which the exoenol moiety characteristic to beraprost is converted to inter-m-phenylene structure. However, it is not known that beraprost has an activity to inhibit metastasis of malignant tumors.
The beraprost which is an effective ingredient of the agent of the present invention includes not only racemic body, but also d-body and 1-body. 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.
The term "malignant tumor" used herein includes all tumors such as melanoma, lung cancer, stomach cancer, liver cancer, breast cancer, colon cancer, brain cancer, head and neck cancer and the like. Further, the term also includes cancers of animals such as mouse, human, monkey, dog and the like in which the existence of malignant tumors have been confirmed. Thus, the term "malignant tumor" is not restricted by the organ or species originated therefrom.
To utilize an antimetastasis agent of malignant tumors according to the present invention, beraprost alone or a salt thereof may be used as it is, but it is usually used as orally administerable popular medical formulations together with an adjuvant, for example, with a vehicle, in the form of tablets, capsules, powder, granules, solutions and the like. These formulations can be prepared according to conventional methods. For example, when tablets are prepared, starch, lactose, crystalline cellulose or the like is used as the vehicle. An example of formulation containing 20 .mu.g of beraprost is described in the following examples. These tablets are orally administered usually 3 tablets at a time and 3 times a day per an adult.
The agent according to the present invention exhibits excellent therapeutic effect by oral administration. However,
REFERENCES:
Chemical Abstracts, vol. 118, No. 13, 29 Mar. 1993 abstract No. 116744e.
Dialog Information Services, File 155: Medline, accession No. 07133831' Abstract Aug. 1989.
Drugs of the Future, vol. 18. No. 1, 1993 pp. 29-48, Schneider et al.
Hattori Masakazu
Mutoh Masato
Nishio Shintaro
Ohno Kiyotaka
Goldberg Jerome D.
Toray Industries Inc.
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