Novel use of pyrrolopyridine derivatives for preventing or treating inflammatory diseases
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example 1
n of Inhibitory Activity of the Compounds According to the Present Invention on Various Kinases
[0109]Measuring the enzyme (kinase) selectivity and inhibitory activity of Compound 1 selected from among the example compound of the present invention was consigned to DiscoverX, and a scanMAX™ Kinase analysis panel was used to carry out the experiment. Here, the concentration of the drug used to treat the enzyme was 1 μM in DMSO; the percentage control (% control) was determined using the following method, and the results are shown in Table 2.
[(Example compound−positive control) / (negative control−positive control)×100]
[0110]Here, the positive control refers to a compound showing a percentage control of 0%, and the negative control indicates a percentage control of 100% with DMSO. Furthermore, regarding the enzyme selectivity of the present invention, if the percentage control for each enzyme was <41% (that is, less than 41%), the compound was judged to have activity with regard to such e...
example 2
n of Pro-Inflammatory Cytokine Inhibitory Activity of the Compounds According to the Present Invention
[0112]THP-1 cells were pre-treated with Compound 1 for 1 hour, and then treated with lipopolysaccharides (Lipopolysaccharides, LPS, 0.5 μg / ml), an inflammatory substance, for 24 hours to confirm the expression of the pro-inflammatory cytokines TNF-α and IL-6 by the THP-1 cells and the NF-κb signaling pathway associated with their expression.
[0113]When the THP-1 cells were treated with LPS, the expression of the inflammation-inducing pro-inflammatory cytokines TNF-α and IL-6 increased, and their expression was effectively inhibited by treatment with Compound 1 (FIG. 1a); the expression of such pro-inflammatory cytokines is increased through activation of the NF-κb signaling pathway, and it can be seen that intranuclear movement of p50 and p65, which are associated with the NF-κb signaling pathway, is effectively inhibited by Compound 1 (FIG. 1b). These results confirm that expression...
example 3
n of the Regulation Activity of the Compounds According to the Present Invention Against Regulatory T Cell and Th17 Cell Differentiation
[0114]Using naive T cells in the mouse spleen, Compound 1 was sufficiently dissolved in DMSO for the differentiation conditions of regulatory T cells and Th17 cells to confirm differentiation. The experiment was conducted using Harmine as a control.
[0115]In the results, as shown in FIG. 2, when treated with Compound 1, it was found that differentiation of regulatory T cells (Treg) increased and differentiation of Th17 cells decreased, indicating potential for use in treatment of inflammatory diseases such as autoimmune disease.
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