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Application of a kind of ethyl ketone compound in preparation of medicine for treating inflammation

A compound, the technology of ethyl ketone, which is applied in the field of PI3Kγ-specific inhibitors, can solve the problems of limited drug effects in inflammatory diseases, and achieve the effect of inhibiting chemotaxis

Active Publication Date: 2022-06-03
CF PHARMTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In summary, traditional drugs for the treatment of inflammatory diseases have limited effects, and rational drug design based on PI3Kγ targets can provide new and efficient drugs for the treatment of inflammatory diseases

Method used

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  • Application of a kind of ethyl ketone compound in preparation of medicine for treating inflammation
  • Application of a kind of ethyl ketone compound in preparation of medicine for treating inflammation
  • Application of a kind of ethyl ketone compound in preparation of medicine for treating inflammation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] PI3Kγ blank group: use a 384-well plate, and set up 3 parallel experimental groups. Configure PI3K reaction system 5 μL, each well

[0029] PI3Kγ experimental group: use a 384-well plate, and set up 3 parallel experimental groups. Compound 1‑(5‑(3‑

[0034]

Embodiment 2

[0036] Using the RAW264.7 cells under the action of the chemokine C5a as a cell model for the specific activation of the PI3Kγ pathway,

Embodiment 3

[0040] Leukocytes, especially neutrophils and monocytes, are exposed to chemokines such as C5a, fMLP, CCL3, CXCL1-3

[0041] The experiment is divided into control group and administration group. First put the inner side of the Transwell chamber into a 24-well plate, and add the inner chamber to the 24-well plate.

[0042] The results are shown in Figure 2. The results show that macrophage RAW264.7 can produce chemotaxis under the action of chemokines.

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Abstract

The invention discloses 1-(5-(3-((4-chlorobenzyl)amino)-2-hydroxypropoxy)-2-methyl-1-(p-tolyl)-1hydro-indole- 3-yl) ethyl ketone for the treatment or prevention of inflammatory diseases, for the prevention and / or alleviation and / or auxiliary treatment and / or treatment of inflammatory diseases, such as bronchitis, pneumonia, hepatitis, rhinitis, enteritis, gastritis , nephritis, dermatitis, prostatitis, vaginitis, rheumatism, etc. The present invention 1-(5-(3-((4-chlorobenzyl) amino)-2-hydroxypropoxy)-2-methyl-1-(p-tolyl)-1 hydrogen-indole-3- Base) ethyl ketone has specific inhibitory effect on PI3Kγ, and has inhibitory effect on inflammatory cell proliferation and chemotaxis. The compound of the present invention can inhibit inflammatory response by inhibiting PI3Kγ.

Description

Application of an ethyl ketone compound in the preparation of a drug for treating inflammation technical field The present invention relates to the technical field of biomedicine, particularly relate to a kind of PI3Kγ specific inhibitor, have the and / or adjuvant therapy and / or treatment of inflammation, such as bronchitis, pneumonia, hepatitis, rhinitis, enteritis, gastritis, nephritis, Dermatitis, prostatitis, vaginitis, rheumatism, etc. Background technique [0002] PI3Ks are a class of lipases that catalyze the phosphorylation of the inositol ring of phosphoinositides and transduce signals as second messengers. PI3K is a large complex family, which can be divided into types I, II, and III according to their structure and substrate specificity. The most current research Broadly known as type I PI3Ks, this protein receives signals from tyrosine kinase-like receptors and G protein-coupled receptors to convert PI(4,5)P2 into It is converted into PI(3,4,5)P3, thereby...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4045A61P29/00
CPCA61K31/4045A61P29/00A61P11/00A61P1/16A61P11/02A61P1/00A61P1/04A61P13/12A61P17/00A61P13/08A61P15/02A61P19/02
Inventor 朱景宇陈蕴杨兆琪蔡燕飞
Owner CF PHARMTECH
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