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Compound for treating pneumonia and application thereof

A compound and heterocyclic compound technology, applied in the field of medicine, can solve problems such as severe adverse reactions, and achieve the effect of improving organ damage, pathological damage, and inflammatory indicators

Inactive Publication Date: 2020-06-23
WEST CHINA HOSPITAL SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] With the spread of viral pneumonia, the currently recommended therapeutic drugs are mainly chloroquine phosphate, tocilizumab and ritonavir, etc., but their adverse reactions are serious

Method used

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  • Compound for treating pneumonia and application thereof
  • Compound for treating pneumonia and application thereof
  • Compound for treating pneumonia and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] In this example, the preparation methods of Compound 1-Compound 24 are described in detail.

[0040] Preparation of Compound 1

[0041] Compound 1 has the following structure:

[0042]

[0043] The preparation process of compound 1 is as follows, and the main starting material for each step of the following reaction is calculated as 1 mmol.

[0044] ①1mmol of CNCH 2 COCH 3 (CH 2 CH 3 )CONH 2 The derivatives were cyclized in DMF (150mL) with NaOH (0.5mmol) as catalyst (reaction 3h); ②then 1mmol cyclization product was passed through H 2 SO 4 (120mL, reaction 9h) acidification; ③ the acidification product was passed through sodium nitrite (3mmol) in H 2 SO 4 Nitrosation (reaction 6h) was carried out under catalytic conditions (100mL); ④ by H 2 SO 4 (100mL) and iron (3mmol) reduce the nitrosation product (reaction 6h); 3 ) 2 SO 4 In the presence of (3mmol) and NaOH (0.5mmol), the formylation product was methylated (reaction 2h); ⑦ under the catalysis of Na...

Embodiment 2

[0131] This example describes in detail the effect of compounds 1 to 24 on improving viral pneumonia.

[0132] Experimental method: C57BL / 6 mice (20–25g) were randomly divided into 6 groups according to different body weights, namely: blank control group; HcoV-OC43 virus model group; drug group (compound 1-compound 24); positive drug effect Bavirin group; Positive drug oseltamivir group; Purine analog control group, the used contrast medicine of purine analog control group is: 1-propyl 3,7-dimethylxanthine (purine analog A), 1-isopropyl 3,7-dimethylxanthine (purine analog B), 3-ethyl 3,7-dimethylxanthine (purine analog C).

[0133] Animals in all groups were anesthetized with propofol tail vein, except for the blank control group, they were all infected with HcoV-OC43 virus solution (30 μL) by intranasal drip. Subsequent processing is as follows:

[0134]Mice in the HcoV-OC43 virus model group: intragastric administration of the same dose of normal saline in the drug interve...

Embodiment 3

[0145] This example describes in detail the effect of compounds 1 to 24 on improving bacterial pneumonia.

[0146] Experimental method: C57BL / 6 mice (20–25g) were randomly divided into 6 groups according to different body weights, namely: blank control group; Streptococcus pneumoniae model group; drug group (compound 1-compound 24); positive drug penicillin G group; Positive drug cefazolin group; Purine analog control group, the used contrast drug of purine analog control group is: 1-propyl 3,7-dimethylxanthine (purine analog A), 1-iso Propyl 3,7-dimethylxanthine (purine analogue B), 3-ethyl 3,7-dimethylxanthine (purine analogue C).

[0147] Animals in all groups were anesthetized with propofol tail vein, except for the blank control group, they were all infected with Streptococcus pneumoniae solution (30 μL, 109–1011 cfu / L) through nasal drip. Subsequent processing is as follows:

[0148] Streptococcus pneumoniae pneumonia model group mice: intragastric administration of th...

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Abstract

The invention discloses a compound for treating pneumonia and application thereof, and relates to the technical field of medicines. The compound for treating pneumonia is a heterocyclic compound, a pharmaceutically acceptable salt of the heterocyclic compound and / or a pharmaceutically acceptable carrier of the heterocyclic compound. The compound for treating pneumonia has a significant improvementeffect on bacterial pneumonia, viral pneumonia, fungal pneumonia, immune pneumonia, mycoplasma pneumonia, chlamydia pneumonia and other pathogen pneumonia, and especially can significantly improve pathological damage of viral bacterial pneumonia. The heterocyclic compound involved in the compound for treating pneumonia is simple in synthesis method, is suitable for industrial production, and is more stable than natural analogues; the activity of the compound is remarkably superior to that of ribavirin, oseltamivir, cefazolin and penicillin G which are clinically first-line medicines, and theactivity of the compound is also remarkably superior to that of purine analogues A, B and C.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a compound for treating pneumonia and its application. Background technique [0002] Pneumonia is a common and frequently occurring disease of the respiratory system, which is mainly a disease of inflammation in the lungs caused by infection by various pathogenic microorganisms (such as viruses, bacteria, fungi, parasites, etc.). The clinical symptoms of pneumonia are mainly cough, expectoration, chills, high fever, chest pain and dyspnea. Viral infections account for 90% of acute respiratory infections. Viral pneumonia is mainly caused by upper respiratory tract infection, which can be transmitted through close-range droplets or contact with respiratory secretions of patients. Viruses that cause pneumonia are rare, among which influenza virus is the most common, and others include rhinovirus, new coronavirus, adenovirus, parainfluenza virus, metapneumovirus, boca virus, etc. ...

Claims

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Application Information

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IPC IPC(8): C07D471/04C07D487/04C07D239/70C07D221/04C07D473/04C07D473/30C07D473/10C07D473/20C07D473/16C07D473/00C07D239/54C07C49/633A61K31/437A61K31/519A61K31/517A61K31/438A61K31/522A61K31/52A61K31/505A61K31/122A61P11/00A61P31/04A61P31/12A61P31/10
CPCA61P11/00A61P31/04A61P31/10A61P31/12C07C49/633C07D221/04C07D239/54C07D239/70C07D471/04C07D473/00C07D473/04C07D473/10C07D473/16C07D473/20C07D473/30C07D487/04C07C2602/24
Inventor 黄文
Owner WEST CHINA HOSPITAL SICHUAN UNIV
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