Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Patent
1994-06-24
1997-09-09
Goldberg, Jerome D.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
A61K 3116
Patent
active
056657790
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP92/01703 filed Dec. 25, 1992.
TECHNICAL FIELD
This invention relates to a pharmaceutical composition for inhibiting infection with a virus causative of acquired human immunodeficiency syndrome, namely AIDS virus (hereinafter sometime abbreviated as HIV), which composition comprises D-.beta.-lysylmethanediamine, a salt or hydrate thereof as active ingredient. This invention also relates to a method for inhibiting the infection of human T-cells with AIDS virus, which comprises treating human T-cells with D-.beta.-lysylmethanediamine, a salt or hydrate thereof. This invention further includes use of D-.beta.-lysylmethanediamine, a salt or hydrate thereof in the manufacture of antiviral composition for inhibiting the infection with AIDS virus.
BACKGROUND ART
AIDS is a disease which is caused due to human T-cells being infected with AIDS virus. AIDS has brought about problems in human society. Several agents for inactivating HIV are reported. However, any of these HIV-inactivating agents is not necessarily satisfactory as a remedial agent for AIDS. Accordingly, there exists an outstanding demand to develope and provide such a new antiviral agent which is of low toxicity but can show a high activity to inhibit the infection of human T-cells with HIV.
On the other hand, D-.beta.-lysylmethanediamine as obtained earlier by the present inventors is an antibiotic which has weak antibacterial activity against Gram-positive bacteria. D-.beta.-Lysylmethanediamine has the unique structure represented by the following formula (I) ##STR2## This compound is a known antibiotic which is produced by a microorganism, Streptomyces nashvillensis and which was reported by the present inventors (see "Journal of Antibiotics" Vol. 39, No. 3, page 476 (1986) and Japanese patent application first publication "Kokai" Sho-62-114947 specification published 26 May 1987). D-.beta.-Lysylmethanediamine hemi-carbonate (1/2 H.sub.2 CO.sub.3) is in the form of a colorless powder which is hygroscopic but has no definite melting point measurable. Its specific optical rotation is [.alpha]sub.D.sup.26 -7.4.degree. (c 0.5, water).
An object of this invention is to provide a new antiviral agent which inhibits strongly the infection of human T-cells with HIV but exhibits a low toxicity to mammals and which is expectable to be useful as a remedial agent for AIDS. Another object of this invention is to provide a new pharmaceutical composition which inhibits the infection with AIDS virus. Further object of this invention is to provide a therapeutic method for inhibiting the infection of human T-cells with HIV. Further another objects of this invention will be clear from the following descriptions.
DISCLOSURE OF THE INVENTION
In order to achieve the above-mentioned objects, we, the present inventors, have made extensive investigations. In consequence, the present inventors, have now discovered that D-.beta.-lysylmethanediamine, a salt or hydrate thereof exhibits a high activity for inhibiting the infection of human T-cells with HIV but has a low toxicity to mammals. Thus, according to our experiments, it has been found that when human T-cells which have been treated with D-.beta.-lysylmethanediamine or a salt or hydrate thereof and then incubated in a culture medium are brought into contact with HIV, the infection of the human T-cells with HIV can be inhibited under the action of D-.beta.-lysylmethanediamine or salt or hydrate thereof. Therefore, D-.beta.-lysylmethanediamine, a salt and hydrate thereof have a high activity to inhibit the infection of human T-cells with HIV and, in a broad sense, have an antiviral activity against HIV.
According to a first aspect of this invention, therefore, there is provided a pharmaceutical composition for inhibiting the infection with AIDS virus, namely HIV, which comprises as active ingredient D-.beta.-lysylmethanediamine having the formula (I) ##STR3## or a salt or a hydrate thereof, in association with a pharmaceutically acceptable carrier for the active ingredient.
In a fu
Hamada Masa
Hoshino Hiroo
Ikeda Yoko
Kondo Shin-ichi
Takeuchi Tomio
Goldberg Jerome D.
Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
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