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Antiviral agents for hepatitis B virus infection

A hepatitis B virus, application technology, applied in antiviral agents, medical preparations containing active ingredients, organic chemistry, etc., can solve problems such as failure and side effects

Active Publication Date: 2022-07-26
ANONCO SCI INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, even with first-line treatment options, pegylated interferon alfa-2a is effective in achieving serologic milestones in only one-third of treated patients and is often associated with severe side effects
Entecavir and tenofovir are highly effective HBV inhibitors, but long-term or possibly life-long treatment requires continuous suppression of HBV replication, which may eventually lead to failure due to the emergence of drug-resistant viruses

Method used

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  • Antiviral agents for hepatitis B virus infection
  • Antiviral agents for hepatitis B virus infection
  • Antiviral agents for hepatitis B virus infection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] The preparation of step one 3-(chlorosulfonyl) ethyl benzoate

[0019]

[0020] 3-(Chlorosulfonyl)benzoic acid (15.18 g, 0.069 mol, 1.0 eq.) was added to DCM (150 mL) at room temperature, cooled to 0-5 °C with an ice-water bath, and thionyl chloride (32.74 g, 0.27mol, 4.0eq.) and 1.5mL catalytic amount of DMF were added, and the temperature was raised to room temperature for overnight reaction for 16 hours. The reaction solution was evaporated to dryness, and the solvent was removed twice with toluene, poured into THF (150 mL), cooled to 0-5° C. with an ice-water bath, ethanol (30 mL) was added dropwise, and the reaction was completed at room temperature for 4-6 hours. The reaction solution was directly evaporated to dryness and purified by column chromatography (200-300 mesh silica gel, Heptane / EtOAc=10:1-5:1) to obtain 12.23 g of a yellow oily liquid with a yield of 71.5%.

[0021] The preparation of step two 3-sulfamoyl ethyl benzoate

[0022]

[0023] Ethyl ...

experiment example 1HB

[0042] Experimental Example 1 HBV virus replication inhibition experiment

[0043] DMEM / F12 (1:1) medium, PBS (1X), dual anti-penicillin-streptomycin, 0.5% trypsin (10X), qPCRSYBR Green Mix was purchased from ThermoFisher (Waltham, MA, USA). Certified fetal bovine serum (FBS) was purchased from Biological Industries (Israel). Hydrocortisone was purchased from Alfa. Insulin was purchased from Sigma. Doxycycline was purchased from Clontech. 96-well and 384-well cell culture plates were purchased from CORNING (USA). Primers were purchased from Nanjing GenScript Biotechnology Co., Ltd. qPCR 384-well plates were purchased from Roche. QuickExtract DNA extraction reagent was purchased from Lucigen.

[0044] "Growth medium" was DMEM / F12 (1:1), 10% FBS, 1X penicillin-streptomycin dual antibody, 350 nM hydrocortisone, 5 ug / mL insulin, 1 ug / mL doxycycline. The "treatment medium" was DMEM / F12 (1:1), 2% FBS, 1X penicillin-streptomycin dual antibody, 350 nM hydrocortisone, 5 ug / mL in...

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Abstract

The invention discloses an antiviral agent for hepatitis B virus infection, including pharmaceutically acceptable salts, esters, prodrugs, complexes, solvates, hydrates or isomer forms thereof, and preparation methods thereof Use in medicines for treating or inhibiting hepatitis B virus infection.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to an antiviral agent for hepatitis B virus infection. Background technique [0002] Hepatitis B virus (HBV) infection remains a major public health problem. Currently, there are an estimated 350 million people worldwide, including 1.4 million in the United States with chronic HBV. Without treatment, about one-third of these people will die from serious liver diseases, such as cirrhosis and liver cancer. [0003] Currently, seven drugs are available for the treatment of chronic hepatitis B, including two alpha-interferon formulations (standard and peg-modified) and five nucleoside analogs (lamivudine) that inhibit HBV DNA polymerase , adefovir, entecavir, telbivudine and tenofovir). Currently, the preferred first-line treatment options are entecavir, tenofovir, or pegylated interferon alfa-2a. However, even with first-line treatment options, pegylated interferon alfa-2a is eff...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D307/22A61K31/341A61P31/20
CPCC07D307/22A61P31/20
Inventor 杨正王婕李进刘浏杨民民
Owner ANONCO SCI INC