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Selective copper ion chelating agent, preparation method of the selective copper ion chelating agent and application of selective copper ion chelating agent in pulmonary fibrosis

A technology of copper ions and chelating agents, applied in the field of medicine, can solve the problems of polymyositis and poor specificity, and achieve the effects of increasing lung blood supply, easy acceptance, and inhibiting pulmonary fibrosis

Active Publication Date: 2021-12-21
AFFILIATED HOSPITAL OF JINING MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently clinically commonly used copper ion chelating agents include penicillamine, trientine, dimercaptosuccinic acid, sodium dimercaptopropanesulfonate, and tetrathiomolybdate, but they all have the disadvantage of poor specificity. When used, it also complexes with iron, zinc, calcium, etc. in the body, so it is easy to cause side effects such as gastrointestinal reactions, lupus erythematosus, myasthenia gravis, polymyositis, etc.

Method used

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  • Selective copper ion chelating agent, preparation method of the selective copper ion chelating agent and application of selective copper ion chelating agent in pulmonary fibrosis
  • Selective copper ion chelating agent, preparation method of the selective copper ion chelating agent and application of selective copper ion chelating agent in pulmonary fibrosis
  • Selective copper ion chelating agent, preparation method of the selective copper ion chelating agent and application of selective copper ion chelating agent in pulmonary fibrosis

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] The synthesis of embodiment 1JYFY-001 compound

[0050] Acetic acid (0.24 g, 4.0 mmol), DMAP (0.49 g, 4.0 mmol) and EDCI (0.77 g, 4.0 mmol) were added to 6 mL of CH 2 Cl 2 , stirred at room temperature for 10 min. After adding 2-bromothieno[3,2-c]pyridin-4-amine (compound 1) (0.46 g, 2.0 mmol), the reaction was continued to stir at room temperature for 6 h. Spin dry CH 2 Cl 2 , added ethyl acetate, washed twice with water, and washed once with saturated NaCl solution. Anhydrous Na 2 SO 4 After drying, filter, concentrate under reduced pressure, and perform silica gel column chromatography (dichloromethane:methanol=100:1) to obtain white powdery solid N-(2-bromothieno[3,2-c]pyridin-4-yl ) Acetamide (Intermediate 2) 0.43g, yield 79.3%. Melting point: 178-180°C; 1 H NMR (400MHz, DMSO) δ8.42 (d, J = 5.5Hz, 1H), 8.16 (d, J = 5.5Hz, 1H), 7.84 (s, 1H), 2.19 (s, 3H); 13 C NMR (100MHz, DMSO) δ172.32, 150.56, 146.42, 142.87, 134.16, 124.78, 118.94, 118.72, 26.53; HRMS...

Embodiment 2

[0052] The establishment of embodiment 2 mouse pulmonary fibrosis model and administration treatment

[0053] In this study, a mouse model of pulmonary fibrosis was established, and the inducer was bleomycin (BLM). In this experiment, 30 mice were randomly divided into 3 groups, 10 in the blank group and 20 in the model group. The model of pulmonary fibrosis in mice induced by bleomycin, the mice in the model group were fasted for 16 hours in advance before modeling. The mice in the modeling group were given BLM aqueous solution (5 mg·kg-1) by tracheal perfusion, and the blank group was perfused with the same volume of normal saline in the same way.

[0054] On day 7, 20 mice in the model group were randomly divided into 2 groups. They are: model group 10, JYFY-001 group 10, ♀♂ half and half. On the 8th day, the JYFY-001 group was given 50 mg / kg dose of tail vein administration (weighed before administration), and the blank group and model group were given corresponding v...

Embodiment 3

[0055] Example 3 Histopathological evaluation of lung tissue pulmonary fibrosis degree observation

[0056] The lung tissues of mice in the three groups treated for 2 weeks were collected, fixed, routinely dehydrated, paraffin tissue sections were made, stained with hematoxylin-eosin (HE) and Masson, and the morphological changes of the lung tissues were observed under a microscope.

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Abstract

The invention discloses a selective copper ion chelating agent, a preparation method of the selective copper ion chelating agent and application of the selective copper ion chelating agent in pulmonary fibrosis, and the chelating agent is N-(2-(pyridine-3-yl) thieno [3, 2-c] pyridine-4-yl) acetamide. The JYFY-001 can improve and inhibit the pulmonary fibrosis level of an organism, inhibit excessive deposition of a pulmonary extracellular matrix, reduce inflammatory cells, inhibit proliferation of fibroblasts and improve pulmonary blood supply so as to relieve dyspnea and has a good treatment effect on pulmonary fibrosis, and in addition, the medicine is not only easy to accept by patients, but also small in toxic and side effects and low in price. In addition, the JYFY-001 will change the market pattern of the existing medicine for treating pulmonary fibrosis, and becomes a clinical medicine which can be taken for a long time and can effectively inhibit pulmonary fibrosis and improve the pulmonary function condition.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a selective copper ion chelating agent, its preparation method and its application in pulmonary fibrosis. Background technique [0002] Pulmonary fibrosis is the end-stage change of a large class of lung diseases characterized by fibroblast proliferation and accumulation of a large amount of extracellular matrix, accompanied by inflammatory damage and tissue structure destruction. Abnormal (Karampitsakos T, et al., Eur J Pharmacol. 2017 Aug 5; 808:35-43). Because its early clinical manifestations are usually non-specific symptoms of exertional dyspnea with or without dry cough, it is often overlooked or misdiagnosed as other diseases in the early stage. Severe pulmonary fibrosis is due to changes in normal lung tissue structure and loss of function. Fibrotic tissue without gas exchange function replaces alveoli, resulting in the inability of oxygen to enter the blood. As a r...

Claims

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Application Information

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IPC IPC(8): C07D495/04A61P11/00A61K31/444
CPCC07D495/04A61P11/00
Inventor 刘艳荣石小龙贾孟亭李莹孙涛张苗苗
Owner AFFILIATED HOSPITAL OF JINING MEDICAL UNIV
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