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Anti-trypanosomiasis agent

An anti-trypanosomiasis and trypanosomiasis technology, applied in the direction of resistance to vector-borne diseases, anti-infective drugs, drug combinations, etc., can solve the problems of heavy physical and economic burden, harmful side effects, and high cost

Active Publication Date: 2008-01-16
FUJIFILM CORP +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Drugs currently used to treat African trypanosomiasis are unsatisfactory as they require hospital admission and long-term administration, are costly and often have harmful side effects
For example, pentamidine (Pentamidine) can be used in the initial treatment, but it needs to be administered in large quantities by intravenous injection or intramuscular injection several times within 3 weeks, which places a heavy physical and economic burden on the patient
In central nervous system diseases, arsenic-containing drug melarsoprol (melarsoprol) can be used, but it needs to be administered continuously for several weeks, and it inevitably has toxic side effects from arsenic

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] 1-1. Culture of African trypanosomiasis protozoa

[0069] In this example, the bloodstream-dwelling trypanomastigotes of the protozoa of Trypanosoma brucei rhodensiense (STIB900 strain) were used. The medium used in the experiment was filter-sterilized MEM medium supplemented with 25mM N-2-hydroxyethylpiperazine-2-ethanesulfonic acid (HEPES), 1g / L glucose, 1% MEM non- Essential amino acids, 0.2 mM 2-mercaptoethanol, 2 mM sodium pyruvate, 0.1 mM hypoxanthine, and 15% heat-treated horse serum. Protozoa were cultured in air with a CO2 concentration of 5% at a temperature of 37°C.

[0070] 1-2. African trypanosomiasis protozoan proliferation inhibition screening test

[0071] The compound of the present invention used in the test and the positive drug (Melarsoprol (Melarsoprol)) were dissolved in dimethyl sulfoxide (DMSO) to prepare a test solution with a predetermined concentration. Add the medium containing 8×103 protozoa and the test solution containing the drug at a ...

Embodiment 2

[0092] 2-1. Culture of Chagas disease protozoa

[0093] In this example, amastigotes and trypanomastigotes of the protozoa of Trypanosoma cruzi (Tulahuen C2C4 strain) infected with rat L6 cells were used. The medium used in the experiment was RPMI1640 medium containing L6 cells with L-glutamine (200 mM) added at a final concentration of 1%, fetal bovine serum at a final concentration of 10%, and cultured at 37°C.

[0094] 2-2. Screening test for protozoan proliferation inhibition of American trypanosomiasis

[0095] The compound of the present invention and the positive drug (Benznidazol) used in the test were dissolved in DMSO to prepare a test solution with a predetermined concentration. A culture medium containing 5×10 3 protozoa was added to the wells of a 96-well culture plate, and pre-cultured for 48 hours. After exchanging the medium, a test solution containing a drug at a predetermined concentration or DMSO without a drug was added. Divide the test solution into two...

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Abstract

An anti-trypanosomiasis agent which has highly selective toxicity to trypanosomiasis and produces a high preventive or therapeutic effect thereon. The agent is characterized by containing a compound represented by the following general formula (1) as an active ingredient. (In the formula, R<1>, R<2>, R<6>, and R<7> each independently represents hydrogen, C1-5 alkyl, etc., provided that they may be bonded to each other; R<3>, R<4>, and R<5> each independently represents C1-5 alkyl or C5-8 aryl; Y and Z each independently represents atoms necessary for the formation of a 5- or 6-membered heterocycle; m and n each is 0 or 1; Q represents a physiologically acceptable anion; and k is an integer of 0-2 which is necessary for making the charge of the whole molecule zero.

Description

technical field [0001] The present invention relates to a new usage of rhodacyanine (Rhodacyanine) pigments, in detail, it relates to an anti-trypanosomiasis useful in the effective prevention and treatment of trypanosomiasis infection which is not available in current effective therapy agent. Background technique [0002] Trypanosomiasis caused by trypanosomiasis protozoa can be roughly divided into two types according to the species of the parasite. The first category is African trypanosomiasis (African lethargy) caused by the parasitism of Trypanosoma brucei (Trypanosoma brucei), and due to the different forms of protozoa, it can also be subdivided into Trypanosoma brucei gambiense and Rhodes Trypanosoma brucei rhodesiense. The second category is Chagas disease (Chagas disease) in which the etiological parasite is Trypanosomac ruzi. These protozoans infect dogs, cats, horses, and cattle in addition to humans, and we are concerned about the spread of trypanosomiasis wo...

Claims

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Application Information

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IPC IPC(8): C07D417/14A61P33/00A61K31/428C07D277/84A61K31/4439C07D277/66A61K31/4709
CPCA61K31/4439C07D417/14A61K31/4709A61K31/428A61P33/00A61P33/02Y02A50/30
Inventor 井原正隆高须清诚卡尼塔·普多霍姆北口博司川上雅之佐藤幸蔵
Owner FUJIFILM CORP
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