Preparation of dual-targeting ERK1 and ERK5 inhibitor and anti-tumor application of dual-targeting ERK1 and ERK5 inhibitors

An anti-tumor drug and application technology, applied in the field of anti-tumor pharmacy, can solve problems such as the lack of development of dual-target ERK1 and ERK5 inhibitors, and achieve the effect of inhibiting growth and obvious inhibitory effect

Active Publication Date: 2020-05-12
WEST CHINA HOSPITAL SICHUAN UNIV
View PDF5 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Likewise, to date there has been no development of dual-ta

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Preparation of dual-targeting ERK1 and ERK5 inhibitor and anti-tumor application of dual-targeting ERK1 and ERK5 inhibitors
  • Preparation of dual-targeting ERK1 and ERK5 inhibitor and anti-tumor application of dual-targeting ERK1 and ERK5 inhibitors
  • Preparation of dual-targeting ERK1 and ERK5 inhibitor and anti-tumor application of dual-targeting ERK1 and ERK5 inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0050] Example 1 Synthesis of Preferred Compounds.

[0051] Preferred compounds are synthesized using the following reaction formula:

[0052]

[0053] i ethanol, heated to reflux; ii DIEA, acid chloride, room temperature; iii methanol saturated hydrochloric acid solution, 0°C; iv benzyl chloride, K2CO3, DMF, 80°C; v isothiocyanate, DIEA, dichloromethane, room temperature.

[0054] 1. General synthesis of intermediates 1-3

[0055]In anhydrous ethanol (200 mL) solution was added tert-butyl 4-opopiperidine-1-carboxylate (30.0 mmol), 2-cyanoacetamide (30.0 mmol) and sulfur (30.0 mmol), morpholine (30.0 mmol) mmol). The mixture was stirred and refluxed for 8 hours, the mixture was cooled to room temperature, filtered, washed three times with 30 ml of ethanol, and the filtrate was suspended and concentrated to dryness. The crude product was diluted with 95% ethanol (30 mL) and filtered to give Intermediate 1 as a white solid.

[0056] Intermediate 1 (10 mmol) and DIEA (20 m...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

The invention relates to preparation and application of a dual-targeting ERK1 and ERK5 inhibitor, and belongs to the technical field of antitumor pharmacy. The technical problem to be solved by the invention is to provide a compound used as a double-targeting ERK1 and ERK5 inhibitor. The compound comprises a compound as shown in the specification or a pharmaceutically acceptable salt thereof. Thecompound or the pharmaceutically acceptable salt thereof can be used as an inhibitor of ERK1 and ERK5, has antitumor activity, and can effectively inhibit the growth of tumor cells. The compound is preferably an anti-tumor compound, and the characteristic of the corresponding tumor type is high expression of ERK1 and/or ERK5.

Description

technical field [0001] The invention relates to the preparation and application of a dual-target ERK1 and ERK5 inhibitor, belonging to the technical field of antitumor pharmacy. Background technique [0002] Tumor is one of the main chronic diseases that affect health, seriously affects the healthy life of human beings, and brings a heavy burden to society and families. Surgical resection combined with radiotherapy and chemotherapy will bring great harm to the patient's body and mind. Targeted therapy is a new type of treatment method, which has the advantages of clear targets, few side effects, and can directly act on diseased tissues. It has become the first choice for tumor treatment. important research direction. At present, the most important problem facing tumor targeted therapy is the lack of alternative drug targets and the lack of research on corresponding targeted small molecules. Therefore, discovering new therapeutic targets and designing targeted drugs are impo...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): C07D495/04A61P35/00A61K31/4365A61K31/506A61K31/444
CPCC07D495/04A61P35/00
Inventor 欧阳亮王贯赵玉倩
Owner WEST CHINA HOSPITAL SICHUAN UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap