Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-07-23
1999-03-23
Travers, Russell
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
A61K 3151
Patent
active
058860002
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP95/00085 filed Jan. 25, 1995.
TECHNICAL FIELD
The present invention relates to an anti-HIV (Human Immunodeficiency Virus) agent useful for prophylaxis of and treatment for Acquired Immune Deficiency Syndrome (AIDS), and an anti-HIV effect-potentiating agent.
BACKGROUND ART
AIDS is a disease caused by HIV infection, and the number of patients thereof is rapidly increasing since this disease was discovered in the United States of America in 1983. It has been known to use azidothymidine (AZT), didanosine (DDI) or the like, which is an anti-HIV agent, in treatment for such AIDS.
However, AZT is recognized to have a life-prolonging effect to a significant extent, but involves a problem that it has side effects such as headache, gastrointestinal disorders and a myelodepresant effect. Besides, since many of these anti-HIV agents, which have heretofore been studied, have been based on the action mechanism that DNA synthesis in the replication process of HIV is inhibited to suppress the proliferation of HIV, they have involved a problem that the DNA synthesis of normal cells is also suppressed at the same time as the inhibition of HIV, and normal cells of a patient hence decrease, and consequently, the patient still more falls into a dangerous condition.
It is accordingly an object of the present invention to provide a remedy for AIDS, which is excellent in safety and efficacy.
DISCLOSURE OF THE INVENTION
In view of the foregoing circumstances, the present inventors have screened anti-HIV effects of various compounds in accordance with a screening method for anti-HIV agents by Tat, which has recently been developed. As a result, it has been found that the following compounds (1) which are widely used as vitamin B.sub.1 derivatives, exhibit an anti-HIV effect by an action mechanism which is not found in the existing anti-HIV agents, have an effect of potentiating the effects of other anti-HIV agents and are useful for prophylaxis of and treatment for AIDS, thus leading to completion of the present invention.
Namely, the present invention is directed to an anti-HIV agent comprising, as an active ingredient, a vitamin B.sub.1 derivative represented by the following general formula (1): ##STR1## wherein X.sup.1 means a hydrogen atom, an acyl group having 1-18 carbon atom or a phosphono group, and R.sup.1 denotes an alkenyl group having 2-6 carbon atoms, a tetrahydrofurfuryl group, a 3-acetylthio-7-methoxycarbonylheptyl group or a group represented by the formula (2): ##STR2## in which X.sup.2 means a hydrogen atom, an acyl group having 1-18 carbon atom or a phosphono group, or a salt thereof, and an anti-HIV effect-potentiating agent comprising said compound.
The present invention is also directed to a prophylactic and remedial agent for AIDS, comprising, as an active ingredient, the vitamin B.sub.1 derivative or the salt thereof.
The present invention is further directed to use of the vitamin B.sub.1 derivative or the salt thereof for an anti-HIV agent, an anti-HIV effect-potentiating agent and a prophylactic and remedial agent for AIDS.
The present invention is still further directed to a method of inhibiting the proliferation of cells persistently infected with HIV, which comprises administering the vitamin B.sub.1 derivative or the salt thereof to the cells persistently infected with HIV.
BRIEF DESCRIPTION OF THE DRAWINGS
FIG. 1 illustrates the result of an cytotoxicity test of thiamine disulfide against CEM cells.
FIG. 2 illustrates the result of an cytotoxicity test of thiamine disulfide against CEM/LAV cells.
FIG. 3 illustrates an effect of thiamine disulfide on the proliferation of primarily infected CEM cells.
FIG. 4 illustrates the result of the detection of HIV-constituting proteins in the addition of thiamine disulfide by western immunoblotting.
BEST MODE FOR CARRYING OUT THE INVENTION
Examples of the acyl groups represented by X.sup.1 and X.sup.2 in the general formula (1) and having 1-18 carbon atoms include alkanoyl groups having 1-18 carbon atoms and aro
REFERENCES:
Merelr Index 10th Ed 1985 # 9130 & 9131.
Khaled, Mahnoz 1993, 118CA;87649v.
Anderson et al,1983, 99 CA193593w.
Anderson et al., "Effects of B-Complex Vitamins on Cellular and Humoral Immune Functions in vitro and in vivo", pp. 77-84, Immunology Section, Dept. Medical Microbiology. Institute of Pathology, University of Pretoria, Pretoria, Republic of S. Africa.
Kirk-Othmer, "Encyclopedia of Chemical Technology: Vitamins to Zone Refining", vol. 24, Third Edition, pp. 124-139, 1984.
Shoji Shozo
Tachibana Kuniomi
Nissui Pharmaceutical Co., Ltd,
Travers Russell
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