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Compound as well as preparation method and application thereof

A compound and composition technology, applied in the field of medicine, can solve problems such as increasing the risk of blood clots in patients

Active Publication Date: 2018-03-13
MICROPORT SINICA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Both of the above two drugs can inhibit the proliferation of smooth muscle cells, endothelial cells, fibroblasts, etc.; however, these two drugs still cannot fully meet the above-mentioned needs for preventing restenosis of blood vessels in the lesion after stent implantation, especially for intravascular The inhibition of different types of cell proliferation is not selective, that is, these two drugs have a strong inhibitory effect on smooth muscle cells, but also have a strong inhibitory effect on endothelial cells. The risk of thrombosis, leading to the need for patients to continue to take antithrombotic and platelet drugs for a long time after stent implantation

Method used

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  • Compound as well as preparation method and application thereof
  • Compound as well as preparation method and application thereof
  • Compound as well as preparation method and application thereof

Examples

Experimental program
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Effect test

preparation example Construction

[0076] The preparation method of the medical device described in the present invention includes but not limited to:

[0077] Dissolving compound X in a solvent and coating it on the surface of the medical device by direct spraying, dipping or a combination of the two methods;

[0078] Or use electrostatic spraying or anodic polarization to spray or dip-coat the surface of the bracket. Soak for 48 hours to stop adsorption, and freeze-dry in a vacuum dryer at -55°C.

[0079] The solvent of the drug is alkanes, alkenes, alcohols, aldehydes, amines, esters, ethers, ketones, aromatic hydrocarbons, hydrogenated hydrocarbons, terpene hydrocarbons, halogenated hydrocarbons, heterocyclic compounds, nitrogen-containing compounds and sulfur-containing compounds, etc., preferably acetic acid Ethyl ester, n-propyl acetate, acetone, tetrahydrofuran, chloroform, dichloromethane.

[0080]The medical device described in the present invention can be one or more of medical devices such as hear...

Embodiment 1

[0092] Preparation of compound W

[0093]

[0094] A: NH 3 / MeOH heating back for 1h

[0095] B: Phosgene / THF

[0096] C: POCl 3 , Morpholine heated to reflux for 5h

[0097] D: methyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate, Pd(Pcy 3 ) 2 Cl 2 , CsF, NMP-water (9:1) 100℃48h

[0098] E: carbamoyl chloride, TEA, DCM reflux for 36h

[0099] The product was confirmed by LCMS, new peak Rf=15.754, M+=398.

Embodiment 2

[0101] Preparation of compound V

[0102]

[0103] A: NH 3 / MeOH heating back for 1h

[0104] B: Phosgene / THF

[0105] C: POCl 3 , Morpholine heated to reflux for 5h

[0106] D: methyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate, Pd(Pcy 3 ) 2 Cl 2 , CsF, NMP-water (9:1) 100℃48h

[0107] E:CH 3 COOOH / CH 3 COOH

[0108] The product was confirmed by LCMS, new peak Rf=12.013, M+=371.

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Abstract

The invention discloses a compound with a formula X structure or pharmaceutically acceptable salt thereof as well as a preparation method and an application thereof. R1 is a chemical structure which at least comprises one five-membered ring or one six-membered ring; R2 is a chemical structure whose molecular weight is greater than 100 and contains an electron-withdrawing group.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a compound that can be used for a drug stent and its preparation method and application. Background technique [0002] The intima of blood vessels is mainly composed of endothelial cells, and the media is mainly composed of smooth muscle cells and fibroblasts. After stent implantation, in order to prevent the restenosis of blood vessels in the lesion, it is hoped to inhibit the proliferation of smooth muscle cells to the lumen of the blood vessel to a relatively large extent; but in order to prevent the occurrence of thrombus, it is hoped that the lesion can be endothelialized as soon as possible, so it is not desirable The drug inhibits endothelial cells too strongly. [0003] At present, in clinical practice, drug stents are usually used to fight vascular restenosis, which requires that the drugs carried on the drug stents have less cytotoxicity, have good fat solubility, and...

Claims

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Application Information

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IPC IPC(8): C07D239/48A61K31/5377A61K31/541A61P9/10A61P7/02A61F2/82A61M31/00
CPCA61F2/82A61M31/00A61M2210/12C07D239/48
Inventor 陈陆李俊菲胡燕王婷
Owner MICROPORT SINICA CO LTD
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