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Novel application of two quinoline ring drugs

A drug and application technology, applied in the field of medicinal chemistry, can solve problems such as unclear role of structural domains and reduction of TRPA1 current

Active Publication Date: 2016-12-14
SHANGHAI LEADO PHARMATECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

A 2-helical calcium-binding motif domain is present at the N-terminus of TRPA1, but the domain's role is unclear
In addition to the important functions of the N-terminus, it was found that the mutation of a single amino acid at the C-terminus of TRPA1 can greatly reduce the current of TRPA1

Method used

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  • Novel application of two quinoline ring drugs
  • Novel application of two quinoline ring drugs
  • Novel application of two quinoline ring drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0111] The compound (1-2) of the present invention inhibits the IC of the transient receptor potential channel protein TRPA1 activity 50 Determination of experimental results

[0112] Two kinds of listed drugs of the present invention are tested by IonWorks Barracuda (IWB) automatic patch clamp detection method, and IC is carried out. 50 Inhibitory activity test, the activity data is shown in Table 1, the two listed drugs have strong activity to inhibit TRPA1, and the half effective inhibitory concentration IC 50 were 11.67 μM and 32.56 μM.

[0113] Table 1. Inhibitory activity data (IC) of compounds (1-2) on TRPA1 50 , μM)

[0114]

Embodiment 2

[0116] Pill box

[0117] The following kind of medicine kit is prepared, and described medicine box comprises:

[0118] (1) A first container, and a first pharmaceutical formulation (eg, a tablet) within said container, the formulation containing the following active ingredients;

[0119]

[0120] Compound 1

[0121] (2) a second container, and a second pharmaceutical formulation (eg, a tablet) within said container, the formulation containing the following active ingredients;

[0122]

[0123] Compound 2

[0124] and (3) the instruction manual.

[0125] Compound 1 and Compound 2 of the present invention are two typical marketed drugs, which can potently inhibit the activity of the transient receptor potential channel protein TRPA1 in vitro, so it is expected to be developed into a new type of treatment for pain, inflammation, breathing disorders (asthma, cough, chronic obstructive pulmonary disease), pruritus associated with oxidative stress, drugs to lower urinary ...

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PUM

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Abstract

The invention provides novel application of quinoline ring drugs, and particularly provides application of a compound shown as the formula A (please see the formula in the description) or an optical isomer or raceme or solvate or pharmaceutically acceptable salt thereof. The compound or the optical isomer or the raceme or the solvate or the pharmaceutically acceptable salt thereof is used for preparing a pharmaceutical composition or preparation, and the pharmaceutical composition or preparation is used for inhibiting transient receptor potential channel protein TRPA1 and treating diseases related to the transient receptor potential channel protein, wherein definitions of all groups are shown in the description.

Description

technical field [0001] The present invention relates to the field of medicinal chemistry, more particularly to quinoline ring drugs and their application in inhibiting transient receptor potential channel protein TRPA1. Background technique [0002] Transient receptor potential (TRP) is a protein superfamily composed of important cation channels present on the cell membrane, which was first discovered by Minke et al. Subsequent studies identified a series of TRP family channel members. According to the sequence homology of about 30 TRP channels found in mammals, they are divided into 6 subfamilies, namely TRPC, TRPV, TRPM, TRPML, TRPA and TRPP. Both the C-terminus and N-terminus of TRP channels are located in the cell membrane and contain six transmembrane domains of S1-S6. The reaction site for ligand binding on domains S1-S4 may be through gated pores, but the S4 domain lacks positively charged amino acid residues as voltage-gated channels, and most TRPs have weak voltag...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D215/44C07D215/50A61K31/47A61K31/4706A61P29/00A61P11/00A61P13/02A61P17/04A61P1/00
CPCC07D215/44C07D215/50
Inventor 王友鑫曲振林张玲玲
Owner SHANGHAI LEADO PHARMATECH CO LTD
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