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Use of aryl urea derivatives for preparing medicines for treating transplant rejection

A technology of transplant rejection and application, applied in the direction of drug combination, allergic diseases, etc.

Inactive Publication Date: 2015-09-09
NEW FOUNDER HLDG DEV LLC +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Tests have found that these newly developed drugs also have similar problems to CsA

Method used

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  • Use of aryl urea derivatives for preparing medicines for treating transplant rejection
  • Use of aryl urea derivatives for preparing medicines for treating transplant rejection
  • Use of aryl urea derivatives for preparing medicines for treating transplant rejection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1: In vitro culture of dendritic cells and the effect of the compound of formula I of the present invention on its surface molecule expression

[0023] 50ml / person of healthy adult peripheral blood was extracted intravenously, anticoagulated with EDTA-K3, PBMCs were separated with Ficoll-Hypaque, and the cells were suspended in complete RPMI1640, and the cell concentration was adjusted to 2×10 6 / ml, add to 24-well culture plate, 0.5ml per well, incubate at 37°C, 5% CO2 incubator for 2h, make the monocytes adhere to the wall, gently wash the culture plate with warm serum-free RPMI1640 solution to Remove non-adherent cells to obtain adherent monocytes, add AIM-V medium containing rhGM-CSF 1000IU / ml and rh-IL-4800IU / ml to the culture plate, and incubate at 37°C with 5% CO2 In the box, half of the culture medium was replaced every other day. On the 3rd and 5th day of culturing, LPS (1 μ g / ml) was added to each hole, and it was divided into two groups, respectively...

Embodiment 2

[0032] Clean-grade healthy male Wistar rats were used as donors, weighing 180-230g, and clean-grade healthy male SD rats were used as recipients, weighing 220-260g. According to previous studies (Tao Ran. Animal Model of Liver Transplantation / / Zheng Shusen. Liver Transplantation. Beijing: People's Medical Publishing House. 2001: 140-143), using the modified double cannula method to establish a model of orthotopic liver transplantation in rats.

[0033] The rat model of liver transplantation was randomly divided into 5 groups, 9 in each group, wherein 3 groups were given formula I compound 2.0, 10.0 and 50.0 mg / kg / d respectively, and the other 2 groups were given CsA (10.0 mg / kg / d) respectively And normal saline (0.5ml / d) as a control, both were administered by intraperitoneal route. The survival time of rats in each group was observed, and the results are shown in Table 2.

[0034] Table 2 Comparison of survival time of liver transplanted rats

[0035]

[0036]Comparing...

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Abstract

The invention discloses a new use of an aryl urea derivative in the preparation of a medicine for treating transplant rejection. The aryl urea derivative is 1-(3-(trifluoromethyl)-4-chloro-phenyl)-3-(3-(6-(1-methyl-4-pyrazolyl)-4-oxypyrimidine)-6-fluorine-phenyl) urea. The compound disclosed by the invention can obviously relieve the rejection reaction of the body to transplanted organs and improve the functions of transplanted organs and can be used for preparing the medicine for preventing and curing organ transplant rejection reaction, in particular the medicine for preventing immune rejection reaction after kidney, liver or heart transplant.

Description

technical field [0001] The present invention relates to the application of aryl urea derivatives in the preparation of immunosuppressive drugs, especially the application in the preparation of immunosuppressive drugs for preventing and treating rejection of organ transplantation. Background technique [0002] In the past 30 years, with the research progress of immunobiology of transplanted organ rejection, especially the clinical use of anti-immune rejection drugs, the number, type and success rate of organ transplantation have been significantly increased. At present, the most commonly used anti-immune rejection drug is cyclosporine (CsA). CsA is actually an immunosuppressant, which improves the function of transplanted organs and prolongs the survival time by inhibiting immune rejection in the body. However, the dose-dependent hepatotoxicity and nephrotoxicity caused by CsA, as well as the high price limit the use of CsA. [0003] At present, nearly 30 immunosuppressants ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/506A61P37/06
Inventor 易崇勤王振国金松华
Owner NEW FOUNDER HLDG DEV LLC
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