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Purinone derivatives, their preparation method and their application in medicine

A technology of compound and general formula, applied in the field of TLR7 agonist, can solve problems such as side effects

Active Publication Date: 2021-02-26
JIANGSU HENGRUI MEDICINE CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Interferon α is one of the main drugs for the treatment of chronic hepatitis B or C, while TNF-α is a pro-inflammatory cytokine, excessive secretion may lead to serious side effects

Method used

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  • Purinone derivatives, their preparation method and their application in medicine
  • Purinone derivatives, their preparation method and their application in medicine
  • Purinone derivatives, their preparation method and their application in medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1，2

[0212] (E)-6-Amino-2-butoxy-9-(2-((2-(pyrrolidin-1-yl)ethoxy)aminoidene)propyl)-7,9-dihydro- 8H-purin-8-one 1

[0213] (Z)-6-Amino-2-butoxy-9-(2-((2-(pyrrolidin-1-yl)ethoxy)aminoidene)propyl)-7,9-dihydro- 8H-purin-8-one 2

[0214]

[0215] first step

[0216] 1-(6-Amino-2-butoxy-8-methoxy-9H-purin-9-yl)propan-2-one 1b

[0217] At 0°C, 2-butoxy-8-methoxy-9H-purin-6-amine trifluoroacetate 1a (450mg, 1.89mmol, prepared by the method disclosed in PCT patent application "WO2016075661" ) was dissolved in N,N-dimethylformamide, potassium carbonate (1.3g, 9.45mmol) was added, and 1-bromopropane-2-one (519mg, 3.79mmol) was added, and the reaction was stirred at room temperature for 12 hours. Add 50 mL of water to the reaction solution, extract with ethyl acetate (50 mL), wash the organic phase with water (30 mL×3) and saturated sodium chloride solution (30 mL×3) successively, dry over anhydrous sodium sulfate, filter, and concentrate the filtrate under reduced pressure , the re...

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Abstract

The present invention relates to purinone derivatives, their preparation method and their application in medicine. Specifically, the present invention relates to a novel purinone derivative represented by general formula (I), its preparation method, pharmaceutical composition containing the derivative and its use as a therapeutic agent, especially as a TLR7 agonist purposes, wherein each substituent of the general formula (I) is the same as defined in the description.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a new purinone derivative represented by general formula (I), its preparation method, a pharmaceutical composition containing the derivative and its use as a therapeutic agent, especially as a TLR7 agonist use. Background technique [0002] Toll-like receptors (toll-like receptors; TLRs) are an important class of protein molecules involved in innate immunity. TLRs are monomeric transmembrane non-catalytic receptors, usually expressed in sentinel cells such as macrophages and dendritic cells, which can recognize structurally conserved molecules produced by microorganisms. Once these microorganisms break through physical barriers such as skin or intestinal mucosa, they are recognized by TLRs, which in turn activate immune cell responses (Mahla, R S. et al., Front Immunol. 4:248 (2013)). The ability of the immune system to widely recognize pathogenic microorganisms is partly due to the wides...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D473/34A61K31/522A61P35/00A61P31/12A61P31/14A61P31/16A61P31/18A61P31/20
CPCA61P31/12A61P31/14A61P31/16A61P31/18A61P31/20A61P35/00C07D473/34
Inventor 张国宝费洪博贺峰陶维康
Owner JIANGSU HENGRUI MEDICINE CO LTD
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