Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/33—Heterocyclic compounds
  • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom

Definitions

• the subject of the invention is a pharmaceutical composition intended for the treatment or prophylaxis of human retrovirus infections, in particular those with a virus which generates the acquired immunodeficiency syndrome (SIDA / AIDS). It also relates to, as medicaments for the treatment or prophylaxis of such infections, the heterocyclic compounds used in these compositions.
• SIDA / AIDS acquired immunodeficiency syndrome
• HIV retrovirus (LAV / HTLV III) seems to be one of the most worrying for civilization today: it is responsible for the acquired immunodeficiency syndrome (SIDA / Engl.: AIDS). It is mainly transmitted by sexual or blood pathway, it affects a growing number of people and its spread is today described as endemic.
• AZT has the disadvantage of being unstable when heated (it is generally stored at -20 ° C), of producing side effects that are poorly tolerated by individuals weakened by the disease and of being very expensive. AZT is also insoluble in water, which limits the forms of application.
• the present invention makes it possible to advantageously fill this gap by proposing, as a medicament intended for the treatment or prophylaxis of human retrovirus infections, at least one nitrogen-heterocyclic compound chosen from 3,6-diamino-10-methyl chloride. -acridinium, 3,6-diamino-acridine and 9-amino-acridine.
• ACD-y Acridine Yellow
• the compounds used in the context of the present invention all comprise at least one amino group attached to the nitrogen heterocycle; they can be represented as follows: Acriflavine (ACF)
• the anti-retroviral activity of the compounds mentioned in the context of the present invention has been demonstrated, inter alia, on the leukemigenic virus of Friends (spleen focus forming virus / SFFV-F) during in vivo experiments described below. .
• acriflavine (ACF) was found to be significantly more effective than AZT at a dose of comparable toxicity, the proflavin (PF) with activity similar to that of AZT.
• AIDS AIDS
• the nitrogen heterocyclic compounds proposed by the invention as medicaments have the great advantage of being readily available on the market and of being remarkably stable at room temperature.
• their toxicity has been the subject of numerous investigations: it is perfectly known and the same goes for possible side effects.
• Said compounds also have the advantage of being water-soluble, which facilitates their application all the more, by the oral or intravenous route for example.
• mice from the DBA 2 strain 0.2 ml of a 1% solution of a spleen extract contaminated with the leukemigenic retrovirus from Friends was inoculated into mice from the DBA 2 strain divided into groups of eight. . About 1 hour after this injection, each infected mouse was administered, intraperitoneally, an aqueous solution of the heterocyclic compound chosen, at the doses shown in the table below. A group of 8 infected mice was kept as such as a control sample.
• a blood plasma sample was taken from the treated and untreated infected mice, and 0.1 ml of this plasma, as is, injected, respectively, after 10% and 1% dilution, into uncontaminated mice from of the DBA2 strain. This injection was done intravenously.
• the number of viruses received by the latter was determined eight days after this injection, by counting the foci of unit formation in the spleen.
• the effect of the drug substances used in this experiment was expressed by means of the report between the number of outbreaks counted following injection of plasma from infected infected mice and the number of outbreaks counted following injection of plasma from "control" mice. The values obtained are expressed logarithmically and are reported in the attached figure.
• PF proflavin

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• Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Epidemiology (AREA)
• Life Sciences & Earth Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Applications Claiming Priority (2)

Publications (1)

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Cited By (4)

Citations (2)

• 1989
  • 1989-05-25 CH CH196589A patent/CH678275A5/fr not_active IP Right Cessation
• 1990
  • 1990-05-22 AU AU56309/90A patent/AU5630990A/en not_active Abandoned
  • 1990-05-22 WO PCT/CH1990/000132 patent/WO1990014086A1/fr unknown

Patent Citations (2)

Non-Patent Citations (4)

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