Application of 4-(cyclohexyl)-aminoquinazoline compounds

A technology of aminoquinazolines and drugs, which is applied in the direction of medical preparations containing active ingredients, drug combinations, metabolic diseases, etc., can solve problems such as body damage, achieve significant effects, avoid immune responses, and suppress immune responses

Inactive Publication Date: 2012-08-22
林治华
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the immune response can also be damaging to the body in certain circumstances, such as autoimmune diseases and transplant rejection

Method used

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  • Application of 4-(cyclohexyl)-aminoquinazoline compounds
  • Application of 4-(cyclohexyl)-aminoquinazoline compounds
  • Application of 4-(cyclohexyl)-aminoquinazoline compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1: Mouse T cell proliferation inhibition test

[0041] After aseptically separating spleen cells from mice and lysing red blood cells, add them to 96-well culture plates, 1-2×10 5 Cells / 100 μL / well. Add anti-CD3 (final concentration 1 μg / mL), anti-CD28 monoclonal antibody (final concentration 1 μg / mL), recombinant IL-2 (final concentration 10 Unit / mL) to stimulate in vitro, 100 μL / well, suppose adding 4-(cyclohexyl)- Aminoquinazoline was the test group, 3 wells / group; no 4-(cyclohexyl)-aminoquinazoline was used as the control group, 3 wells / group. At the same time, set the group without the above in vitro stimulation and without adding 4-(cyclohexyl)-aminoquinazoline as the blank group, 3 wells / group.

[0042] Three groups of samples were placed at 37°C, 5% CO 2 Incubate under the condition for 66h, add 0.5-1μci3H-TdR 50μL to each well, and continue to cultivate for 12h. Use DYQ-II type multi-head cell harvester to collect samples of each group on 9999 type ...

Embodiment 2

[0044] Embodiment 2: human T cell proliferation inhibition test

[0045] Under sterile conditions, isolate peripheral blood mononuclear cells (PBMC) from heparin anticoagulated blood, and adjust the number of cells to 1-2×10 with 10% FCS RPMI1640 after washing 6 / mL, added to 96-well culture plate, 1-2×10 5 Cells / 100 μL / well. Add T cell mitogen PHA, 100 μL / well, set 4-(cyclohexyl)-aminoquinazoline as the test group, 3 wells / group; no 4-(cyclohexyl)-aminoquinazoline is the control group, 3 wells / group. At the same time, set the group without the above in vitro stimulation and without adding 4-(cyclohexyl)-aminoquinazoline as the blank group, 3 wells / group.

[0046] Three groups of samples were placed at 37°C, 5% CO 2 Incubate for 66h under the condition, add 0.5-1μci to each well 3 H-TdR 50μL, continue to culture for 12h. Use DYQ-II type multi-head cell harvester to collect samples of each group on 9999 type glass fiber filter paper, and count them with β liquid scintilla...

Embodiment 3

[0048] Example 3: Mouse FoxP3 + CD4 + Regulatory T cell induction assay

[0049] FoxP3 + CD4 + Regulatory T cells are a type of T cells with immunosuppressive effects. This type of cells participates in the regulation of immune response / immune tolerance in an "active" manner, not only participates in the regulation of autoimmune tolerance, but also plays an important role in transplantation immunity. In order to prove whether the formula I compound of the present invention can induce initial T cells to differentiate into FoxP3 + CD4 + Regulatory T cells, after the present invention isolates mouse splenocytes and stimulates them in vitro, FoxP3 is detected by flow cytometry (FACS) + CD4 + Differentiation of regulatory T cells. Specific steps are as follows:

[0050] According to the method of embodiment 1, be divided into control group, test group and blank group, cultivate with 24 well plate then, 1-2 * 10 6 / mL, 2mL / well. At 37°C, 5% CO 2 After incubating for 66 ...

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Abstract

The invention relates to the field of medical immunology, and discloses application of a compound shown as a formula (I) in preparing a medicament used for inducing T cells to be differentiated into FoxP3+CD4+ regulatory T cells and inhibiting the T cells from proliferating, wherein the compound shown as the formula (I) belongs to 4-(cyclohexyl)-aminoquinazoline compounds. The compound shown as the formula (I) plays a remarkable role in inhibiting the T cells from proliferating and inducing the T cells to be differentiated into the FoxP3+CD4+ regulatory T cells, and the medicament which is prepared by the compound and is used for inducing the T cells to be differentiated into the FoxP3+CD4+ regulatory T cells and inhibiting the T cells from proliferating can be used for autoimmune diseases and transplantation rejection.

Description

technical field [0001] The invention relates to the field of medical immunology, in particular to the preparation of 4-(cyclohexyl)-aminoquinazoline compounds for inducing T cell differentiation into FoxP3 + CD4 + Regulatory T cells and drugs that inhibit T cell proliferation. Background technique [0002] Immune response refers to the whole process in which the immune system of the body receives antigen stimulation, lymphocytes specifically recognize antigens, undergo activation, proliferation, differentiation or incapacity, apoptosis, and then exert biological effects. The immune response is divided into T cell-mediated cellular immunity and B cell-mediated humoral immunity. Although humoral immunity is mediated by B cells, it can only be produced with the help of T cells. It can be seen that T cells are a key type of lymphocytes in the entire immune response. [0003] The most basic biological significance of the immune response is to recognize "self" and "non-self" a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/517A61P37/00A61P37/06A61P3/10A61P25/00A61P29/00A61P19/02
Inventor 林治华马正伟许雪青朱波王锐
Owner 林治华
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