Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ether doai
Patent
1988-12-05
1991-02-12
Goldberg, Jerome D.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ether doai
A61K 31075
Patent
active
049924753
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to the chemical compounds consisting of butylhydroxyanisoles and their salts as agents suitable for the therapeutic treatment of the human or animal body. The compounds of the invention, designated compounds (I), comprise, in particular, tert-butylhydroxyanisoles such as 3-tert-butyl-4-hydroxyanisole (II), 2-tert-butyl-4-hydroxyanisole (III) and the mixture (IV) in variable proportions of these 2 products, this mixture sometimes being designated by the term B.H.A.
The subject of the invention is, in particular, the use of the compounds (I) for the treatment of diseases caused by retroviruses, for example for the treatment of AIDS.
The compounds of the invention and their salts, such as the alkali metal salts, are chemical compounds which have been known for a long time. The compounds (II) and (III) and a mixture thereof, in particular the compound (IV) known as B.H.A., possess very advantageous antioxidant properties, while having as little toxicity as possible towards man and animal. In particular, these studies have shown the absence of harmful effects of oral doses ranging, in rhesus monkeys up to 500 mg/kg/d for 1 month, in cynomolgus monkeys up to 400 mg/kg/d for 3 months, in pigs up to 400 mg/kg/d for 4 months, and in beagle dogs up to 220 mg/kg/d for 6 months. For this reason, they are widely used, such as B.H.A., as food additives for the preservation of edible fats and oils and of many other foods for human consumption. They are also used as preservatives in the manufacture of medicinal compounds. However, it appears that these compounds have never been used as active principles for a therapeutic purpose as regards man or animals.
It is known, moreover, that retroviruses, to which the AIDS virus (H.I.V. or H.T.L.V. III or L.A.V.) belongs, are enveloped viruses. Now, according to current knowledge, it would appear that the AIDS virus is pathogenic as the result of a 2-stage mechanism:
in a first stage, the envelope of the retrovirus adheres to a membrane receptor of cells such as T4 lymphocytes.
In a second stage, the retrovirus enters the cell and, as a result of the reverse transcriptase, its RNA is transcribed to DNA, which is integrated in the genome of the infected cell which, in consequence, is capable of providing for the multiplication of the virus.
Hitherto, therapeutic investigations relating to AIDS have been chiefly concerned with the second stage of the mechanism described above, use being made, in particular, of inhibitors of reverse transcriptase or of other enzymes involved in the replication, transcription and translation of nucleic acids.
It does not appear, on the other hand, that the first stage of the supposed mechanism of action of the AIDS retrovirus has hitherto given rise to detailed studies. Specifically in an in endeavor to develop a therapy for AIDS, the author of the present invention directed his attention towards the first stage of this mechanism, that is to say towards the adhesion of the viral envelope to the cell receptor, its mechanism, its biochemical substrate and the means of modifying it. The importance of this envelope is borne out by the size of the corresponding transcription unit (or gene, or "open reading frame"=orf). In effect, H.I.V. possesses at least 6 orfs: the bulkiest (or "pol") codes for reverse transcriptase, and the next bulkiest (or "env") codes for a precursor glycoprotein (g Pr 160) which is cleaved to an external glycoprotein (gp 120) and a transmembrane glycoprotein (gp 41), of unusual sizes.
It was then shown, and this forms the main subject of the present invention, that the compounds (I) as defined above, show exceptional and surprising properties, having the effect of abolishing, reducing or modifying the infectivity of the AIDS virus. This effect is very probably due to an alteration of the envelope of this retrovirus and, on this assumption, could hence intervene in the first stage of the mechanism stated above.
A related effect has, admittedly, been envisaged recently for 2,6-di-tert-butyl-4-methylphenol
REFERENCES:
Chemical Abstracts, 85:87941j (1976).
Reimund, The Lancet, Nov. 15, 1986, p. 1159.
Goldberg Jerome D.
Roussel Uclaf
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