Application of N-substituted phenyl-2-pyridone compounds or pharmaceutically acceptable salts thereof in treatment of pulmonary fibrosis

A pulmonary fibrosis and compound technology, applied in the field of medicine, can solve the problem of irreversible pulmonary fibrosis, and achieve the effect of improving the degree of pulmonary fibrosis, improving safety and protecting the lungs

Pending Publication Date: 2022-07-08
DALIAN UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since its launch, pirfenidone can delay pulmonary failure and reduce the progression of the disease, but it still cannot reverse the course of pulmonary fibrosis

Method used

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  • Application of N-substituted phenyl-2-pyridone compounds or pharmaceutically acceptable salts thereof in treatment of pulmonary fibrosis
  • Application of N-substituted phenyl-2-pyridone compounds or pharmaceutically acceptable salts thereof in treatment of pulmonary fibrosis
  • Application of N-substituted phenyl-2-pyridone compounds or pharmaceutically acceptable salts thereof in treatment of pulmonary fibrosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] The synthetic method of compound P adopts prior art, and synthetic general formula and process are as follows:

[0037]

[0038] Compound 1 (20 g), iodobenzene derivative 2 (1.5 equiv.), potassium carbonate (1.1 equiv.), cuprous chloride (10 mol%) and DMF (300 mL) were placed in a 500 mL reaction flask under argon protection , 150 ℃ reflux reaction for 10 hours. After the reaction was completed, it was cooled to room temperature, filtered with suction, the filter cake was washed three times with DMF, the filtrates were combined, and activated carbon was added to decolorize. The decolorized solution was evaporated to dryness under reduced pressure, 100 mL of 10% acetic acid was added, and the mixture was stirred at 70° C. for 30 minutes. After standing for layers, the upper aqueous phase was taken, the lower oily substance was extracted twice with 10% acetic acid, and the aqueous phases were combined. The aqueous phase was adjusted to pH 13 by adding sodium hydroxid...

Embodiment 2

[0071] Animal grouping, surgical modeling and administration: Mice were randomly divided into blank control group, model control group, pirfenidone treatment group, and new drug treatment group. Mice were acclimated for 3 days (weight about 20 g), and the model was operated on the 4th day. The method was as follows: after weighing the mice, anesthetized by intraperitoneal injection of sodium pentobarbital, put the anesthetized mice in a supine position, and fix the limbs and head of the mice with a mouse plate, with the head high and the feet low, fully exposing the neck skin. The anterior cervical area of ​​the mice was routinely depilated and disinfected, and a median longitudinal incision was made, and the muscles and tissues were bluntly separated until the trachea was exposed. Bleomycin solution (2mg / ml) was prepared with sterile normal saline, the syringe was inserted into the trachea through the tracheal cartilage ring gap towards the heart end, and after the air was wi...

Embodiment 3

[0087] The test data of other compounds are given in the form of the following table, wherein, the test process and method refer to Example 2.

[0088] Table 1 Properties data table of other compounds

[0089]

[0090]

[0091]

[0092] It can be seen from the experimental data in the table that the degree of fibrosis of the lung tissue has been relieved to a great extent after the treatment with the above N-substituted phenyl-2-pyridone compound.

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PUM

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Abstract

The invention discloses application of N-substituted phenyl-2-pyridone compounds or pharmaceutically acceptable salts thereof in treatment of pulmonary fibrosis, and belongs to the technical field of medicines. The invention provides an application of the compound in treatment of pulmonary fibrosis, and the compound can delay the progress of pulmonary fibrosis, has a good effect of preventing and treating pulmonary fibrosis, and also has good safety. Compared with a clinical first-line anti-pulmonary fibrosis drug pirfenidone, the drug provided by the invention has a better anti-pulmonary fibrosis curative effect, is expected to be developed into an efficient drug for treating pulmonary fibrosis, and provides a better drug choice for preventing and treating pulmonary fibrosis.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to the application of a class of N-substituted phenyl-2-pyridone compounds or their pharmaceutically acceptable salts in the treatment of pulmonary fibrosis. Background technique [0002] Pulmonary fibrosis is characterized by proliferation of fibroblasts and massive accumulation of extracellular matrix. It is also seen as abnormal repair of normal alveolar tissue resulting in abnormal structural scarring. The etiology of the vast majority of pulmonary fibrosis is unknown, and this disease is also known as idiopathic interstitial inflammation, of which idiopathic pulmonary fibrosis is the most common pulmonary fibrotic lesion. Idiopathic pulmonary fibrosis is a severe interstitial lung disease that can lead to progressive loss of lung function. Pulmonary fibrosis seriously affects people's respiratory function, and the morbidity and mortality of idiopathic pulmonary fibrosis are gra...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/64A61P11/00A61K31/4418
CPCC07D213/64A61P11/00A61K9/0053A61K9/0019
Inventor 王磊安晋·U·阿卡亚
Owner DALIAN UNIV OF TECH
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