Use of cd38 enzyme inhibitors in the treatment of airway hyperresponsive diseases

A technology of airway hyperresponsiveness and inhibitor, which can be used in respiratory diseases, organic active ingredients, and medical preparations containing active ingredients, etc. It can solve the problems of complicated operation, long modeling time and low success rate.

Active Publication Date: 2018-03-30
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, researchers use more airway hyperresponse models as ovalbumin (OVA)-sensitized mouse and mouse models, but the disadvantages of this modeling method are long modeling time, low success rate and complicated operation

Method used

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  • Use of cd38 enzyme inhibitors in the treatment of airway hyperresponsive diseases
  • Use of cd38 enzyme inhibitors in the treatment of airway hyperresponsive diseases
  • Use of cd38 enzyme inhibitors in the treatment of airway hyperresponsive diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1: Physicochemical properties of compound T[5-(3-phenylpropionylamino)-N-(4-ethoxycarbonylphenyl)-1H-3-indolecarboxamide]

[0030] The structural formula of compound T is as figure 1 As shown, the molecular weight is 455.51, light yellow-white powder, melting point 192-194°C, soluble in DMF and acetone, slightly soluble in methanol and dichloromethane, insoluble in water, and decomposes in the presence of strong acid and strong alkali. Its solubility and acid-base stability can be proved by the following experiments.

[0031] 1. Solubility test

[0032] Purpose: To test the solubility of compound T in different solvents

[0033] Principle: At 20°C, the amount of dissolved solvent in 100g of solvent is 1-10g is soluble, 0.01g-1g is slightly soluble, and less than 0.01g is insoluble. Add a certain amount of solvent to the quantitative sample and observe the dissolution.

[0034] Method: Take 2mg sample, add solvent and shake, clear and transparent without soli...

Embodiment 2

[0045] Example 2: Pharmacodynamic evaluation of two CD38 enzyme inhibitors in mouse airway hyperresponsive disease model

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Abstract

The present invention relates to a medicine for treating airway hyperresponsiveness disease, 5-(3-phenylpropionylamino)-N-(4-ethoxycarbonylphenyl)-1H-3-indolecarboxamide. The drug is a CD38 enzyme inhibitor, which can treat airway hyperresponsiveness disease symptomatically by inhibiting the release of Ca2+ to dilate tracheal smooth muscle; we use ozone to create a mouse airway hyperresponsiveness model, and at the same time give the drug's emulsifier for intragastric treatment , it was found that the airway resistance of the mice treated with the drug was significantly reduced, the dynamic lung compliance was significantly increased, and the degree of lung lesions was reduced; The development value of land belongs to the field of medicine.

Description

Technical field: [0001] The invention relates to a medicine for treating airway hyperresponsive diseases, 5-(3-phenylpropionylamino)-N-(4-ethoxycarbonylphenyl)-1H-3-indolecarboxamide. The drug is a CD38 enzyme inhibitor, which mainly achieves the therapeutic purpose by dilating tracheal smooth muscle, and has anti-inflammation and anti-oxidation effects, and belongs to the field of drugs. Background technique: [0002] Airway hyperresponsiveness refers to the excessive response of the trachea and bronchi to various stimuli, including specific antigenic stimuli and non-specific stimuli, such as physical and chemical stimuli, which is an important feature that distinguishes patients with bronchial asthma from normal people [1] . Although the inducing factors of airway hyperresponsiveness are various, and the therapeutic effects of various drugs are different, and the research on new therapies is also multi-directional, but basically from anti-inflammatory, antihistamine, alle...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/404A61P11/00
Inventor 蒲小平张亮仁邓政朱志鹏
Owner PEKING UNIV
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