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Novel use of pyrrolopyridine derivatives for preventing or treating inflammatory diseases

Pending Publication Date: 2022-08-18
VORONOI CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention provides a compound (Formula 1) and its isomers or pharmaceutically acceptable salts that have excellent inhibitory activity against various protein kinases and inflammation-related factors. This compound is stable and safe, and can be used to develop pharmaceutical compositions for the prevention, treatment, and improvement of inflammatory diseases such as inflammatory bowel disease, psoriasis, rheumatoid arthritis, and lupus.

Problems solved by technology

When said stimuli are applied, vasoactive substances such as histamine, serotonin, and prostaglandin are released, increasing vascular permeability and causing inflammation.
However, long-term use of non-steroidal anti-inflammatory drugs may cause gastrointestinal disorders, and serious side effects such as secondary anemia, asthma, suppression of labor induction, adverse effects on the kidneys, liver damage, and hypersensitivity have been reported.

Method used

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  • Novel use of pyrrolopyridine derivatives for preventing or treating inflammatory diseases
  • Novel use of pyrrolopyridine derivatives for preventing or treating inflammatory diseases
  • Novel use of pyrrolopyridine derivatives for preventing or treating inflammatory diseases

Examples

Experimental program
Comparison scheme
Effect test

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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PUM

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Abstract

The present invention relates to a pharmaceutical composition for preventing and / or treating inflammatory disease, the composition comprising a pyrrolopyridine-derivative compound as an active ingredient; the compound represented by Chemical Formula 1 according to the present invention, enantiomers thereof or pharmaceutically acceptable salts thereof, which have excellent inhibitory activity against not only protein kinases but also inflammatory factors and inflammatory cytokines; therefore a pharmaceutical composition comprising the same as an active ingredient may be useful in prevention, treatment and / or improvement of inflammatory disease, in particular but not limited to inflammatory bowel disease, rheumatoid arthritis, or lupus.

Description

TECHNICAL FIELD OF THE INVENTION[0001]The present invention relates to a novel use of pyrrolopyridine derivative compounds for preventing and / or treating inflammatory diseases.BACKGROUND OF THE INVENTION[0002]Pyrrolopyridine derivatives are bicyclic compounds wherein pyridine and pyrrole are bonded and used for various pharmaceutical purposes. Accordingly, various pyrrolopyridine derivatives have been synthesized. Patent literature which discloses pyrrolopyridine derivatives include Korean Laid-open Patent Nos. 10-2018-0015142, 10-2017-0106452, and 10-2017-0058465.[0003]In most of the above patent literature, it can be known that pyrrolopyridine derivatives are used as inhibitors for protein kinases. Accordingly, the inventors set out to identify other physiological activities and pharmacological mechanisms of the pyrrolopyridine derivatives.[0004]Inflammation is the mechanism by which living tissue that has been damaged by physical action, chemical substance, or bacterial infection...

Claims

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Application Information

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IPC IPC(8): A61K31/5377A61K45/06A61P17/00A61P17/06A61P1/00A61P19/02
CPCA61K31/5377A61K45/06A61P19/02A61P17/06A61P1/00A61P17/00A61P1/04A61P29/00
Inventor KIM, SOO CHANKIM, DAE KWONSEO, DONG HYUKKIM, HYUN KYUNGKIM, SUNG HWANHWANG, HYE MINCHOI, JI EUN
Owner VORONOI CO LTD
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