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Eph receptor small molecule inhibitor and preparation method thereof

A technology of small molecule inhibitors and receptors, which is applied in the field of Eph receptor small molecule inhibitor compounds or their isomers, receptor tyrosine kinase Eph small molecule inhibitor compounds, and the preparation of such compounds, which can solve problems that cannot Selectively act on Eph kinase protein and other problems to achieve the effect of good reproducibility, inhibition of occurrence and development, and simple operation

Inactive Publication Date: 2017-04-19
ZHUHAI NOBEL INST OF BIOMEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, Eph kinase inhibitors that act on the intracellular tyrosine kinase region have been reported in the literature. However, such inhibitors, as competitive inhibitors of the binding of adenosine triphosphate (ATP) to tyrosine kinases, have no effect on other kinase family proteins. also has an effect, and does not selectively act on the Eph kinase protein

Method used

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  • Eph receptor small molecule inhibitor and preparation method thereof
  • Eph receptor small molecule inhibitor and preparation method thereof
  • Eph receptor small molecule inhibitor and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment

[0047] 1) In the following examples, all temperatures are in degrees Celsius unless otherwise specified.

[0048] 2) All starting materials and reagents are commercially available. Suppliers include but are not limited to: AlfaAesar, Bailingwei and other companies. Unless otherwise indicated, commercially available starting materials and reagents were used without further purification.

[0049] 3) Glassware is oven dried and / or heat dried. The size of the silica gel plate used in thin layer chromatography (TLC) is 0.15-0.2 mm, and the analytical thin layer chromatography is developed with an appropriate solvent ratio (v / v). Column chromatography generally uses 200-300 mesh silica gel as the carrier.

[0050] 4) 1 The HNMR spectrum is obtained by Bruker instrument (400MHz), and the chemical shift is expressed in ppm. Chloroform was used as reference standard (7.25 ppm) or tetramethylsilane internal standard (0.00 ppm). Other solvents commonly used for NMR can also be used...

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Abstract

The invention discloses an Eph receptor small molecule inhibitor compound or isomers, non-enantiomers, enantiomers, mesomers, racemes and mixtures thereof, or a pharmaceutically acceptable salt thereof. The Eph receptor small molecule inhibitor compound has the following structural formula: FORMULA. The Eph receptor small molecule inhibitor compound selectively acts on the extracellular binding region of an Eph receptor and an ephrin ligand for the treatment of nervous system diseases in mammals, treatment of vascular system diseases, and inhibition of the occurrence and development of tumor diseases. The invention also discloses a preparation method of the Eph receptor small molecule inhibitor compound at the same time, and the preparation method is simple to operate and good in reproducibility.

Description

technical field [0001] The present invention relates to the field of tyrosine kinase inhibition, in particular to a receptor tyrosine kinase Eph (erythropoietin-producing liver cell receptor) small molecule inhibitor compound, and the present invention provides such an Eph receptor small molecule inhibitor Compounds or their isomers, diastereomers, enantiomers, mesoforms, racemates, and mixtures thereof, or pharmaceutically acceptable salts thereof, and processes for the preparation of such compounds. Background technique [0002] The Eph receptor family is the largest known family of receptor tyrosine kinases (RPTKs). According to the difference in sequence homology, structure, expression and ligand binding properties, the Eph receptor family is divided into EphA receptor subfamily and EphB receptor subfamily, and its ligand is named Ephrin. The EphA receptor subfamily contains 10 members EphA1-EphA10, and the EphB receptor subfamily contains 6 members EphB1-EphB6. Nine Ep...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K5/068A61K38/05A61P25/00A61P9/00A61P35/00
CPCA61K38/00C07K5/06086Y02P20/55
Inventor 黄子为王娟徐岩安静阿龙·切哈诺沃
Owner ZHUHAI NOBEL INST OF BIOMEDICINE CO LTD
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