Benzofuran derivative and medical application thereof

A technology of benzofuran and derivatives, which is applied in the field of benzofuran derivatives and their medical applications, can solve the problem of single compound structure, and achieve the effect of highlighting the substantial characteristics

Pending Publication Date: 2022-07-22
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since STING inhibitors are still in their infancy, the compound structure is relatively simple, and most of them are in the stage of cell activity verification

Method used

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  • Benzofuran derivative and medical application thereof
  • Benzofuran derivative and medical application thereof
  • Benzofuran derivative and medical application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 2

[0224] Inhibitory effect of compounds on cGAMP-stimulated STING pathway in THP1-Dual cells by luciferase assay

[0225] 1) 4*10 THP1-Dual cells in logarithmic growth phase 4 The samples / well were seeded in 96-well plates, and different concentrations of compounds were added, and the DMSO group was used as a blank control.

[0226] 2) The cells were transfected with 10ug / mL cGAMP and lipofectamine 2000 (Invitrogen) complex and cultured for 24h.

[0227] The preparation method of the transfection complex: 1ug cGAMP was added to 10uL Opit-MEM, 0.5uL Lipofectamine2000 was added to 10uL Opti-MEM, mixed and left to stand for 15 minutes, and 20uL of the complex was added to the 96-well plate.

[0228] 3) Using QUANTI-Luc TM Reagents to detect luciferase activity. Take 10uL of cell culture supernatant and add it to a 96-well opaque white plate, then add 50uL of QUANTI-Luc TM Reagents were read with a multi-plate reader (Thermo).

[0229] Calculation method of relative luciferase ...

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Abstract

The invention provides a benzofuran derivative and medical application thereof, the benzofuran derivative is a compound with a structural formula (I) or an enantiomer, a diastereoisomer, a raceme and a pharmaceutically acceptable salt of the compound in the formula (I), and the formula (I) is shown in the specification. The benzofuran derivative disclosed by the invention can be used as a cGAS-STING pathway targeting inhibitor and is used for treating inflammatory diseases and autoimmune diseases.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a benzofuran derivative and its medicinal use. Background technique [0002] As the center of the innate immune signaling pathway, the cGAS-STING signaling pathway has a wide range of roles in innate immunity and tumor immunotherapy. It recognizes the nucleic acid of bacteria or viruses in the cytoplasm through the key synthase cGAS (cyclic GMP-AMP synthase), and catalyzes GTP Synthesize cyclic guanylate (cyclic GMP-AMP, cGAMP) with ATP, activate interferon gene stimulator (stimulator of interferon genes, STING) to oligomerize, recruit TANK-binding kinase 1 (TANK-binding kinase 1, TBK1) , phosphorylates TBK1 and STING autophosphorylation, activates interferon regulatory factor 3 (IRF3) and nuclear factor kappa beta (NF-kB), induces type I interferon and immunostimulatory genes Express. In recent years, with the further understanding of this signaling pathway, research on sma...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/85A61K31/343A61P29/00A61P37/06A61P9/00A61P1/00A61P27/02A61P3/10A61P25/28A61P1/16A61P11/00A61P17/00A61P17/06A61P19/02A61P1/04
CPCC07D307/85A61P29/00A61P37/06A61P9/00A61P1/00A61P27/02A61P3/10A61P25/28A61P1/16A61P11/00A61P17/00A61P17/06A61P19/02A61P1/04
Inventor 尤启冬肖易倍徐晓莉冯子文田鑫健徐凤戴薇姜正羽郭小可王磊
Owner CHINA PHARM UNIV
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