N,N'-dicyclohexyl-N-higher fatty acid ureide analogs and pharmaceutical application thereof

A fatty acid urea, dicyclohexyl technology, applied in the N field, can solve the problems of in vitro experiment influence, poor water solubility, etc., and achieve the effects of reducing dosage and toxic side effects, reducing infiltration, and reducing damage

Inactive Publication Date: 2014-07-02
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these compounds are poorly soluble in water. Although they are made into nano-preparations through microemulsification, they still have a certain impact on in vitro experiments.

Method used

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  • N,N'-dicyclohexyl-N-higher fatty acid ureide analogs and pharmaceutical application thereof
  • N,N'-dicyclohexyl-N-higher fatty acid ureide analogs and pharmaceutical application thereof
  • N,N'-dicyclohexyl-N-higher fatty acid ureide analogs and pharmaceutical application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1 The numbers of the compounds designed in the present invention are shown in Table 1.

[0035] Table 1 Design compound number of the present invention

[0036]

[0037]

[0038]

[0039]

[0040]

[0041]

[0042]

[0043]

Embodiment 2

[0044] Example 2 In vitro inhibition of T lymphocyte transformation experiment

[0045] This example is carried out using methods well known to those skilled in the art. The mouse spleen lymphocyte suspension was prepared by grinding method, the B cells were removed by nylon wool column, the eluted medium containing T cells was collected, centrifuged at 1800 rpm for 5 min; Suspend T cells (purity > 90%), count, adjust the cell concentration, according to 1 × 10 per well 6 Each was added to a 96-well culture plate, and then 5 μg / ml concanavalin A stimulator was added to stimulate the proliferation and differentiation of T cells, and a certain concentration of compounds of the present invention including numbers 1 to 48 were added, and the total volume of the culture solution in each well was 200 μl. Put in 5%CO 2 After culturing in the incubator for 72 hours, the proliferation of cells in each well was detected by BrdU assay, and the OD450 of each well was detected by a micro...

Embodiment 3

[0046] Example 3 In vitro inhibition of mixed lymphocyte culture experiment

[0047] This example is carried out using methods well known to those skilled in the art. The spleen lymphocyte suspensions of BALB / c mice and C57BL / 6 mice were prepared by grinding method, the B cells were removed by nylon wool column, the eluted culture medium containing T cells was collected, centrifuged at 1800 rpm for 5 min; Resuspend T cells (purity > 90%) in RPMI-1640 medium of bovine serum, count, adjust cell concentration, and obtain T lymphocytes. BALB / c mouse T lymphocytes were used as stimulator cells. 5 86-well culture plates were added to each well, and C57BL / 6 mouse T lymphocytes were used as reaction cells. 6 Each well was added to a 96-well culture plate, and at the same time, a certain concentration of the compounds of the present invention including numbers 1 to 48 was added, and the total volume of the culture solution in each well was 200 μl. Put in 5%CO 2 After culturing in t...

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PUM

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Abstract

The invention provides N,N'-dicyclohexyl-N-higher fatty acid ureide analogs and pharmaceutical application thereof, relating to therapeutic compounds. A pharmaceutical composition of the N,N'-dicyclohexyl-N-higher fatty acid ureide analogs, and pharmaceutically acceptable salts, solvates, hydrates or carriers thereof can be prepared by a method known by the technical personnel in the technical field. The invention relates to a pharmaceutical composition containing pharmaceutically effective amount of compounds disclosed as general formula I. The composition is used for regulating immune response reaction of the organism, and especially used for preparing organ transplantation immunological rejection inhibitors. The N,N'-dicyclohexyl-N-higher fatty acid ureide analogs can be used for preparing immunomodulating drugs, immunosuppressive drugs, drugs for treating immunological rejection reaction, drugs for treating rheumatic arthritis, anti-inflammatory agents, drugs for treating rheumatalgia, drugs for treating autoimmune disease, drugs for treating fever diseases, organ transplantation immunological rejection inhibitors and the like; and the N,N'-dicyclohexyl-N-higher fatty acid ureide analogs can be used in cytological experiments and experimental animal in-vivo researches.

Description

technical field [0001] The present invention relates to therapeutic compounds, in particular to N,N'-dicyclohexyl-N-higher fatty acid ureide analogs and their pharmaceutical uses. Background technique [0002] Regulation of the immune system is desired in many situations, from suppressing autoimmune responses, to controlling infectious diseases and suppressing graft / tissue rejection. The primary approach to alleviating rejection is to pharmacologically suppress the recipient's immune system. Based on this idea, most of the currently used immunomodulatory compounds are immunosuppressive. However, these drugs have serious side effects in their use, such as nephrotoxicity, neurotoxicity, hepatotoxicity, endocrine complications, and effects on bone (New Engl.j.Med.321:1725-1738, 1989; Surgery 97:125 , 1985). Therefore, there is a need to provide a new class of compounds with immunosuppressive effects but without the above-mentioned toxic and side effects for clinical use. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C275/66C07C281/06C07C275/64C07C275/50C07C381/00C07C309/46A61K31/17A61K31/175A61K31/277A61K31/19A61K31/185A61P37/02A61P37/06A61P19/02A61P29/00
Inventor 齐忠权夏俊杰秦箐马鹏飞邝晓聪谢集照王永志
Owner XIAMEN UNIV
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