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New uses of naphthalene ring drugs

A pharmacy and compound technology, applied in the field of amide drugs and their application in inhibiting transient receptor potential channel proteins, can solve problems such as unclear domain functions

Active Publication Date: 2021-11-19
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
At present, there are few domestic studies, but foreign pharmaceutical companies have developed a series of pyrimidinedione TRPA1 inhibitors, and the TRPA1 channel has also become a research hotspot for new analgesics

Method used

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  • New uses of naphthalene ring drugs
  • New uses of naphthalene ring drugs
  • New uses of naphthalene ring drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0096] Using the method described above, compounds 1, 2 and 3 were subjected to IC 50 Inhibitory Activity Test.

[0097] The results are shown in Table 1 below: the compounds 1, 2 and 3 of the present invention are all transient receptor potential channel protein (TRPA1) activity inhibitors, and the compounds 1, 2 and 3 have significant inhibitory effect on the activity of TRPA1.

[0098] Table 1

[0099]

Embodiment 2

[0101] pill box

[0102] Prepare following a kind of medicine box, described medicine box comprises:

[0103] (1) a first container, and a first pharmaceutical preparation (tablet) located in said container, which preparation contains the following active ingredients;

[0104]

[0105] (2) a second container, and a first pharmaceutical preparation (such as a tablet) located in said container, which preparation contains the following active ingredients;

[0106]

[0107] and (3) instruction manual.

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PUM

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Abstract

The invention provides a new application of naphthalene ring drugs. Specifically, the present invention provides the use of the compound represented by formula A, or its optical isomer or its racemate, or its solvate, or its pharmaceutically acceptable salt, and they are used to prepare a medicine Composition or preparation, the pharmaceutical composition or preparation is used for (a) inhibiting the transient receptor potential channel protein TRPA1; (b) treating diseases related to the transient receptor potential channel protein, where each group is defined as in the description described in .

Description

technical field [0001] The invention relates to the field of medicinal chemistry, more specifically to amide drugs and their application in inhibiting transient receptor potential channel protein (TRPA1). Background technique [0002] Transient receptor potential channel (Transient receptor potential, TRP) is a kind of protein superfamily composed of important cation channels existing on the cell membrane. It was first discovered by Minke et al. when studying the visual transmission system of Drosophila. Subsequent studies have discovered a series of TRP family channel members. According to the sequence homology of about 30 TRP channels found in mammals, they are divided into six subfamilies, namely TRPC, TRPV, TRPM, TRPML, TRPA and TRPP. Both the C-terminal and N-terminal of the TRP channel are located in the cell membrane, and contain six transmembrane domains of S1-S6. The ligand-binding reaction sites on domains S1-S4 may be gated pores, but the S4 domain lacks positiv...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/341A61K31/381A61K31/138A61P25/04A61P29/00A61P11/00A61P17/04A61P13/02A61P1/00
Inventor 王友鑫曲振林张玲玲
Owner SHANGHAI LEADO PHARMATECH CO LTD
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