Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ketone doai
Patent
1995-06-09
1996-10-01
Cintins, Marianne M.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ketone doai
A61K 3112
Patent
active
055611648
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT GB92/02344, filed Dec. 17, 1992.
The present invention relates to the treatment and prophylaxis of protozoal infections caused by Kinetoplastida, Apicomplexa, Anaerobic protozoa and Microsporidia. More particularly the invention is concerned with the use of 2-[4-(4-chlorophenyl)cyclohexyl]-3-hydroxy-1,4-naphthoquinone and physiologically acceptable salts and physiologically functional derivatives thereof in the treatment and prophylaxis of protozoal infections caused by Kinetoplastida, Apicomplexa, Anaerobic protozoa and Microsporidia, and the use of said compound for the manufacture of medicaments for the treatment and prophylaxis of said protozoal infections.
Kinetoplastida include the Trypanosomes of which Trypanosoma rhodiense, Trypanosoma gambiense and Trypanosoma cruzi are of particular importance. T. rhodiense and T. gambiense cause sleeping sickness, which is fatal in humans unless treated. The trypanosome parasites live and multiply initially in the blood and tissue fluid of their host, producing a febrile condition which may be quite mild. After a few months (T. rhodiense) or a year or so (T. gambiense) the parasites invade the central nervous system and multiply in the cerebrospinal fluid, ultimately causing brain damage which leads to the coma from which the disease gets its name.
T. cruzi causes Chagas disease in humans. In children, the disease takes to form of an acute fever which can cause death. In adults, the infection is chronic, involves the heart or the alimentary tract and can be fatal.
The Kinetoplastida also include the genus Leishmania which cause leishmaniasis in humans. The parasites are also frequently found in dogs and rodents which may serve as reservoirs for the parasite. Leishmania parasites are ingested by the macrophage cells of their host, but instead of being destroyed the parasites thrive and multiply within the macrophages. In visceral leishmaniasis, caused by L. donovani, parasitized macrophages occur in all tissues, including the blood, and although the disease is slow, it is usually fatal unless treated. L. tropica causes cutaneous leishmaniasis in which the parasites are restricted to ulcers in the skin. In Brazil, L-Braziliensis causes mucocutaneous leishmaniasis which is a very severe disease; the mucous membranes of the nose-mouth and pharynx become infected and ultimately destroyed.
The Apicomplexa include the Babesia parasites which inhabit erythrocytes and which are of veterinary as well as medical importance. B. divergens is the European species that causes bovine babesiosis and, although not normally parasitic in man, it can cause a life threatening disease in splenectomized invididuals, for which there is no recommended chemotherapy. The disease is usually associated with anaemia, fever, enlargement of the spleen and blocking of the capillaries in various tissues (including the brain), which may damage the cells by depleting their oxygen supply. The anaemia may be accompanied by the lysis of erythrocytes and excretion of the released haemoglobin in the urine.
The Isospora are a genus of Apicomplexa which may infect humans and cause diarrhoea. Another genus of Apicomplexa which may infect humans are the Sarcocystis which commonly infect herbivores. All species of Sarcocystis are almost entirely restricted to the muscle fibres of their host. If the infection is heavy, degeneration of the surrounding muscle fibres and consequent muscular weakness results along with some pain.
Parasitic anaerobic protozoa include species of Acanthanamoeba which normally inhabit soil and mud but which can cause throat infections in humans, particularly in infants.
Entamoeba histolytica is an anaerobic protozoan which normally inhabits the gut as a harmless commensal. Occasionally however, the parasites penetrate the mucosa and invade the sub-mucosa where they multiply to form a flask-shaped lesion or ulcer. Secondary bacterial infection of the ulcer may also occur. As the submucosa is eroded, many blood vessels are broken and bloody dysentery re
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Dr. Trevor M. Jones--Presentation At Interims, Apr. 27th, 1989; 2 pages.
CA19(21):183497p Fry et al, "Potent and selective hydroxynaphthoquinone inhibitors of mitochondrial electron transport in Eimeria tenella " Biochem. Parasitol. Wellcome Res. Lab. 1984. Abstract only.
Gutteridge Winston E.
Hudson Alan T.
Latter Victoria S.
Pudney Mary
Cintins Marianne M.
Glaxo Wellcome Inc.
MacMillan Keith
Neuner George W.
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