Dipeptidyl aldehydes for the treatment and/or prevention of parasitic diseases

A parasitic disease, anti-parasitic technology, applied in the field of treatment and/or prevention of parasitic diseases

Inactive Publication Date: 2018-11-23
AXIAVA PHARMA UG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, side effects and drug-resistant trypanosomes (depending on the species and the agent used) pose considerable problems in the treatment of trypanosomiasis

Method used

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  • Dipeptidyl aldehydes for the treatment and/or prevention of parasitic diseases
  • Dipeptidyl aldehydes for the treatment and/or prevention of parasitic diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] Example 1-In vitro effects on growth and vigor of Trichomonas (T.gallinae)

[0063] The effect of Z-FY-CHO on growth and viability was tested in vitro in two Trichomonas strains (Vienna strain and ATCC 30095). Trichomonas were cultured in vitro under sterile conditions. Both strains were in 2154 (LYI Entamoeba medium), which was prepared according to the recommendation of ATCC. The culture condition is an anaerobic environment at 37°C. Cultures were maintained in sterile 50ml plastic tubes with a total volume of 10ml. Trichomonas cultures were pre-passaged at regular intervals (two-day intervals) to maintain the strains under study.

[0064] Quantification of the total parasite number: The total parasite number was counted separately for each tube. Therefore, the contents of each tube were centrifuged and the pellet was resuspended in the given volume. Check the dilution of the subsamples in a Neubauer counting chamber, count the total number of parasites and the...

Embodiment 2

[0071] Example 2: In Vivo Efficacy Studies

[0072] Thirty domestic pigeons of both sexes (two groups of 15 each) were orally inoculated by syringe with 2 million strains of Trichomonas cultured from the Vienna strain. The initial age of the pigeons is 4-5 months. Two days later, the pigeons were dosed with Z-FY-CHO at 5 mg / kg orally twice daily or placebo (ie vehicle only) for 4 days. The formulation consisted of 50 mg dose and 4 g pre-warmed Solutol HS15 to which 1.0 ml 96 g / v % ethanol was added. The formulation was stirred to a clear solution and then topped up to a volume of 10 ml with pre-warmed distilled water. The solution was administered at 0.1 ml per 100 g of body weight (ie 5 mg / kg). The birds were subsequently subjected to general health checks and measurements of feed and water consumption twice daily. 14 days after infection, birds were euthanized and organs were examined histologically. Reflux occurred significantly more frequently in pigeons in the placeb...

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Abstract

Several parasites responsible for mammalian diseases are dependent on cysteine proteases for various life-cycle functions. Inhibition or decreasing function of specific cysteine proteases can be useful in the treatment and / or prevention of these parasitic diseases including trichomoniasis, histomoniasis, coccidiosis, trypanosomiasis (trypamonosis) and cryptosporidiosis. Compounds of formula I of the invention are capable of treating and / or preventing the above-identified diseases in mammals, e.g. in avian species as Galliformes including chickens, turkeys, ducks, geese, grouse, guinea fowl, peafowl, quail, partridges, and pheasants, Falconiformes, Passiformes, Columbiformes (i.e. Columba livia domestica), Psittaciformes, and in domestic mammals such as cattle, sheep, goats, horses, pigs, camels, lamas, alpacas, cats and dogs.

Description

technical field [0001] The present invention relates to dipeptidyl aldehyde compounds of formula I and their use for the treatment and / or prophylaxis of parasitic diseases including trichomoniasis, histomoniasis, coccidiosis, trypanosomiasis and crypto sporozoosis. Background technique [0002] Several parasites that are the etiology of mammalian disease depend on cysteine ​​proteases for various life cycle functions. These proteases, which are crucial to the activities of parasites, are mainly divided into cathepsin B-like and cathepsin L-like. These enzymes play important roles in various host-parasite interactions, such as evasion of host immune attack and adaptation to host and tissue invasion. Therefore, it can be expected that specific inhibitors of cathepsin L-like proteases, including cruzain, the Trypanosoma cruzi cathepsin L cysteine ​​protease, may be considered as potential new targets for antiparasitic therapy. Trichomonas gallinae has recently been found to ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P33/02A61K38/00A61K38/05
CPCA61K31/17A61K31/366A61K31/541A61K38/005A61K38/05A61K45/06A61P33/02Y02A50/30A61K2300/00
Inventor J·C·A·范梅尔B·S·J·范托尔
Owner AXIAVA PHARMA UG
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