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New application of phenyl ketone medicines

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

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
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 application of phenyl ketone medicines
  • New application of phenyl ketone medicines
  • New application of phenyl ketone medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0098] Using the method described above, compounds 1 and 2 were subjected to IC 50 Inhibitory Activity Test.

[0099] The results are shown in Table 1 below: the compounds 1, 2, 3 and 4 of the present invention are all transient receptor potential channel protein (TRPA1) activity inhibitors, and the compounds 1 and 2 have significant inhibitory effect on the activity of TRPA1.

[0100] Table 1. Compound (1-2) inhibitory activity data to TRPA1 (IC 50 ,μM)

[0101]

Embodiment 2

[0103] pill box

[0104] Prepare following a kind of medicine box, described medicine box comprises:

[0105] (1) a first container, and a first pharmaceutical preparation (tablet) located in said container, which preparation contains the following active ingredients;

[0106]

[0107] (2) a second container, and a first pharmaceutical preparation (such as a tablet) located in said container, which preparation contains the following active ingredients;

[0108]

[0109] and (3) instruction manual.

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PUM

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Abstract

The invention provides a new application of phenyl ketone medicines, and particularly provides a compound shown in the formula A (please see the formula A in the description), or an optical isomer of the compound, or a raceme of the compound, or a solvate of the compound, or application of pharmaceutically-accepted salt of the compound. The compound, optical isomer, raceme, solvate and pharmaceutically-accepted salt are used for preparing a pharmaceutical composition or preparation. The pharmaceutical composition or preparation is used for restraining transient receptor potential channel protein TRPA1 and treating diseases related to the transient receptor potential channel protein. In the formula, the definitions of all groups are described in the description.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, more specifically to benzophenone drugs and their application in inhibiting the 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 lack...

Claims

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Application Information

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IPC IPC(8): A61K31/4453A61K31/451A61P29/00A61P25/04A61P11/00A61P17/04A61P13/02A61P1/00
CPCA61K31/4453A61K31/451
Inventor 王友鑫曲振林张玲玲
Owner SHANGHAI LEADO PHARMATECH CO LTD
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