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Use of 17-ketosteroids for the treatment of malaria and Trypanosomiasis

A technology of metabolites and compounds, applied in the production of steroids, bulk chemicals, and resistance to vector-borne diseases, etc., can solve the problems of no parasite therapeutic drugs found, ineffective, etc.

Inactive Publication Date: 2002-05-08
HOLLIS EDEN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Drugs effective against T. cruzi do not work in humans infected with T. cruzi; no therapeutic drugs have been found against the parasite

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 2

[0423] Example 2. BrEA formulation 2. A formulation containing 100 mg / mL of BrEA (10% w / w) in 30.4% w / w benzyl benzoate (USP), 30.7% w / w polyethylene glycol 300 (NF), approximately 28% w / w propylene glycol (USP) and 1.9% w / w benzyl alcohol (NF), this formulation, hereinafter referred to as "Formulation 2", was prepared as follows. A predetermined amount of BrEA (1.0 kg) was suspended in PEG300 (approximately 3.0 L) present in the dosing container, followed by mixing for at least 5 minutes at room temperature to form a homogeneous emulsion. Thereafter the necessary amount of propylene glycol (about 1.5 L) was added and mixing continued for at least 5 minutes to form a homogeneous suspension. Benzyl benzoate (approximately 3.0 L) was added and the contents of the vessel were mixed for approximately 5 minutes, resulting in a translucent suspension. Benzyl alcohol (about 200ml) was added and mixing continued for about 5 minutes to give a clear colorless solution. Propylene glyco...

Embodiment 3

[0424] Example 3. In Vitro Experiment Microtiter plate was used in in vitro antimalarial experiment. Drug concentrations were prepared as pMol / well following WHO standard methods (WHO, 1990). Test compounds were dissolved in 15% DMSO in sterile RPM11640. Chloroquine sensitive (WS / 97) and resistant (MN / 97) isolates were used in the experiments.

[0425]A. Schizont inhibition assay: Various concentrations of test compounds were pre-applied on microtiter plates. 50 μL of parasitized erythrocyte suspension in RPMI-1640 (0.2 ml erythrocytes + 0.3 ml serum + 4-5 ml RPMI-1640) was dispensed into microtiter wells containing various concentrations of drug. Each concentration was read three times in parallel.

[0426] b. 3 H-Hypoxanthine Mixture Test: This test was performed as described by Desiardins et al., 1979. After 30 h incubation at 37 °C, the same microtiter plate as for the schizont inhibition assay with additional triplicate wells was added 3 H-hypoxanthine overnight. W...

Embodiment 4

[0430] Example 4. For the 4-day in vivo protocol for Plasmodium burgdorferi, the 4-day inhibition assay is widely used because it can be performed over a period of 1 week. The experiment consisted of Monday, the first day of the experiment (D 0 ) to inoculate parasitized erythrocytes, followed by injection of test compound, and repeated administration on D+1, D+2, and D+3 days. On D+4 days (Friday), blood smears were taken and antimalarial activity was assessed by counting parasitemia or by scoring parasite numbers on a predetermined scale (ie 1-5). Peters (1970) discloses the basic method for using this 4-day experiment. plan

[0431] 1. Each test group consisted of 5 female TO mice.

[0432] 2. Parasites (P. burgdorferi HP15 ANKA) were collected by cardiac puncture in heparinized syringes from donor mice carrying 30+% parasitemia.

[0433] 3. Dilute the blood sample with diluent (50% HIFCS+50% sterile PBS) to a final concentration of 1% parasitemia or 1×10 per 0.2 mL of ...

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PUM

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Abstract

The present invention provides the application of 17-ketosteroids and their derivatives, metabolites and precursors and pharmaceutically acceptable salts of these compounds in the treatment of malaria, African trypanosomiasis and American trypanosomiasis, or in alleviating or alleviating a certain For the application of one or more symptoms associated with malaria parasite or trypanosome infection, the above-mentioned compounds are collectively referred to as "compounds of the present invention". The present invention further relates to the use of said compounds in the treatment or prevention of one or more parasites and / or one or more diseases caused by said parasites, against one or more mycoplasma and / or one or more A disease caused by said mycoplasma, and / or against one or more of the following indications or infections and all other indications and infections: (a) hairy leukoplakia, (b) oral candidiasis, (c) Mouth ulcers - aphthous / herpetic / bacterial, (d) fungal candida, (e) human papillomavirus, (f) molluscum contagiosum, (g) squamous oral carcinoma, (h) ) Kaposi's sarcoma oral lesions, (i) periodontitis, (j) necrotizing gingivitis, (k) orofacial herpes zoster, and (l) rotavirus. The compounds of the invention may also be used to alleviate or lessen one or more symptoms associated with the infections or diseases described herein.

Description

Background of the invention [0001] The present invention relates to 17-keto steroids and derivatives, metabolites and precursors of such compounds and pharmaceutically acceptable salts of any of them (collectively referred to as "compounds of the present invention") optionally in combination with one or more other Use of administration and / or treatment (as described below) in the treatment of malaria, African trypanosomiasis and American trypanosomiasis. The invention further relates to the usefulness of such compounds (and combinations) in the treatment of one or more parasites and / or one or more diseases caused by parasites, against one or more mycoplasma and / or one or more Diseases caused by such mycoplasma and / or against one or more of the following indications or infections: (a) hairy leukoplakia, (b) oral candidiasis, (c) oral ulcers (oral sores / herpes / bacteria sex), (d) fungal Candida, (e) human papillomavirus, (f) molluscum contagiosum, (g) squamous oral carcinoma, (h...

Claims

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Application Information

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IPC IPC(8): A61K31/353A61K31/357A61K31/56A61K31/565A61K31/566A61P31/00A61P33/00A61P33/02A61P33/06C07J1/00C07J3/00
CPCC07J1/0011A61K31/568A61K31/565C07J3/005A61K31/5685A61K31/56Y02P20/55A61P31/00A61P33/00A61P33/02A61P33/06Y02A50/30A61K2300/00
Inventor 克拉伦斯·纳撒尼尔·阿勒姆詹姆斯·马丁·弗林克帕特里克·T·普伦德加斯特
Owner HOLLIS EDEN PHARMA
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