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Cyclic depsipeptide compound and use thereof

A technology of peptide compounds, cyclic esters, applied in the field of treatment of chronic obstructive pulmonary disease or asthma

Inactive Publication Date: 2011-11-23
ASTELLAS PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, after this, there is no selective G other than the aforementioned cyclic ester peptides q / 11 Inhibitor reports, looking forward to G q / 11 Further clinical effects of inhibitors confirmed

Method used

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  • Cyclic depsipeptide compound and use thereof
  • Cyclic depsipeptide compound and use thereof
  • Cyclic depsipeptide compound and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0103] The following abbreviations are sometimes used in this specification. EtOAc = ethyl acetate, MeOH = methanol, LTD 4 =Leukotriene D 4 , PBS(-) = phosphate-buffered saline without calcium or magnesium, Methacholine = β-methacholine chloride.

preparation example

[0104] Preparation example: Preparation example of cyclic ester peptide compound examples 1 to 4 shown in formula (I)

[0105] (nourish)

[0106] Prepare the seed medium in this way: Add the medium containing 5g of yeast extract, 10g of polypeptone, 5g of salt and 1L of distilled water to a 100mL Erlenmeyer flask several times, 30mL each time, and sterilize with a pressure cooker at 121°C for 30 minutes .

[0107] Prepare the production medium in this way: add 50 g of soybean oil, 3.3 g of polypeptone, 7.8 g of yeast extract, 20 g of defatted soybean powder, 50 g of corn steep liquor, 0.65 g of lithium chloride and 1 L of distilled water into a Erlenmeyer flask with a capacity of 100 mL. Medium (pH 7.0), 30 mL each time, was sterilized in an autoclave at 121 °C for 30 minutes.

[0108] The slant culture of Chromobacterium sp.QS3666 strain was inoculated onto the seed medium with a platinum ear spoon, and cultured with shaking at 30°C for 2 days. Then, in each flask of the p...

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Abstract

Disclosed is a compound useful for the prevention and / or treatment of chronic obstructive pulmonary disease (COPD) or asthma. Also disclosed is a pharmaceutical composition containing the compound as an active ingredient. The pharmacological activities of natural fermented materials are examined extensively, and it is found that a cyclic depsipeptide compound derived from a soil bacterium belonging to the genus Chromobacterium which is collected in Okutama-machi, Tokyo, has both an inhibitory activity on airway contraction and an activity to prevent inflammation in the airway and is therefore effective as a prophylactic or therapeutic agent for COPD or asthma. Specifically disclosed is a pharmaceutical composition for preventing and / or treating COPD or asthma, which contains a cyclic depsipeptide compound or a salt thereof as an active ingredient and is intended to be applied by intratracheal administration, nasal drop administration or inhalation administration.

Description

technical field [0001] The present invention relates to a cyclic ester peptide compound and the use of the cyclic ester peptide compound for treating chronic obstructive pulmonary disease (COPD) or asthma. The cyclic ester peptide compound can be used as a pharmaceutical composition (especially for the treatment of COPD or asthma) Asthma pharmaceutical composition) active ingredient. Background technique [0002] Both COPD and asthma are diseases of restricted tracheal airflow. [0003] COPD is a disease with cough (accompanied by exertional dyspnea and sputum production) as the main symptom. When the condition worsens, cough, wheezing, and dyspnea increase, accompanied by an increase in the amount of expectoration and a change in its character to purulent. Tracheal symptoms such as coughing and wheezing are due to tracheal constriction and inflammation of the trachea with subsequent hypersecretion of the trachea. The disease is characterized by airflow limitation that is...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K11/02A61K38/00A61P11/00A61P11/06
CPCA61K38/12A61K38/15C07K11/00A61P11/00A61P11/06A61K38/00C07K11/02
Inventor 辻本晋谷口昌要平山良孝高崎淳川崎富久坂本宪俊西胁真哉北永行扩
Owner ASTELLAS PHARMA INC
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