Azole derivative or pharmaceutically acceptable salt thereof as well as preparation method and application of azole derivative or pharmaceutically acceptable salt thereof

A technology of azole derivatives and derivatives is applied in the field of nuclear transport regulator derivatives and their preparation, which can solve the problems of difficult gastrointestinal toxicity and achieve remarkable effects.

Pending Publication Date: 2021-03-23
SUZHOU AIHE PHARM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is highly toxic to neoplastic cells, but it is difficult to be

Method used

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  • Azole derivative or pharmaceutically acceptable salt thereof as well as preparation method and application of azole derivative or pharmaceutically acceptable salt thereof
  • Azole derivative or pharmaceutically acceptable salt thereof as well as preparation method and application of azole derivative or pharmaceutically acceptable salt thereof
  • Azole derivative or pharmaceutically acceptable salt thereof as well as preparation method and application of azole derivative or pharmaceutically acceptable salt thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1 of the present invention is the compound of the present invention or a pharmaceutically acceptable salt thereof, specifically including the preparation process and administration route of the compound.

[0040] The following is the synthesis method of the series 1 drug compound and the series 2 drug compound.

[0041] Such as figure 1 As shown, the route design and synthesis of the series 1 compound of this embodiment. The synthetic method of series 1 compound is: the cyano group of compound 1 generates thioformamide under the effect of sodium hydrosulfide and magnesium chloride, then reacts under the condition of hydrazine hydrate and formic acid to generate triazole 2, and triazole 2 is then reacted in Under the catalysis of triethylenediamine, it is coupled with (Z)-3-iodoethyl acrylate to generate compound 3, and then, the double bond part of compound 3 is added to liquid bromine, and then removed under the action of triethylamine Remove a molecule of...

Embodiment 2

[0087] Embodiment 2 of the present invention is a method for treating a variety of diseases, disorders or conditions related to CRM1 activity in a subject in need thereof, the method comprising administering to the subject in need A therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt or composition thereof.

[0088] The cell line inhibitory activity test is as follows:

[0089] 1. Cell cryopreservation

[0090] (1) After the cells were harvested, they were centrifuged at 1000 rpm for 5 minutes at room temperature and rinsed with PBS.

[0091] (2) Resuspend in 1640 medium containing 7% DMSO and 10% fetal bovine serum.

[0092] (3) Divide into cryopreservation tubes, put them into cell cryopreservation boxes at -80°C overnight, and store them in liquid nitrogen.

[0093] 2. Cell recovery and culture:

[0094] (1) Take the cryopreservation tube out of the liquid nitrogen tank, put it into warm water at 37°C and shake gently t...

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Abstract

The invention discloses an azole derivative or a pharmaceutically acceptable salt thereof and a preparation method of the azole derivative or pharmaceutically acceptable salt thereof. The structure ofthe azole derivative is as shown in the specification, and compared with the prior art, the invention provides an azole compound with a novel structure and a CRM1 protein inhibition function, and theazole compound is used as a CRM1 protein inhibitor and can block tumor cell proliferation and inhibit tumor cell apoptosis, and induce tumor cell apoptosis, and therefore, the compound can be used for treating and preventing various diseases of human and animals, such as malignant tumors, and the effect is remarkable and better.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to a derivative of a nuclear transport regulator, a preparation method thereof and a pharmaceutical application thereof. Background technique [0002] At present, malignant tumors are still one of the major diseases that threaten people's lives. Although the treatment of cancer has made great progress, it has not been able to treat cancer fundamentally. Although the currently marketed anticancer drugs have certain curative effects, most of them are cytotoxic drugs with serious toxic and side effects. Therefore, how to start from effective tumor targets to study targeted new anticancer drugs has become a top priority for medical workers. [0003] Most studies on CRM1 applied the natural product CRM1 inhibitor lebramycin B (LMB). It has high toxicity to tumor cells, but it is difficult to be accepted by animals due to significant gastrointestinal toxicity. Nuclear expo...

Claims

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Application Information

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IPC IPC(8): C07D401/06C07D403/06A61P29/00A61P35/00A61K31/506A61K31/4439
CPCA61P29/00A61P35/00C07D401/06C07D403/06
Inventor 王雪源杜晓
Owner SUZHOU AIHE PHARM TECH CO LTD
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