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Compounds for inhibiting HCV (hepatitis C virus), pharmaceutical composition and application of compounds or pharmaceutical composition

A technology for hepatitis C virus and compounds, which is applied in the fields of compounds of elements of Group 4/14 of the periodic table, active ingredients of silicon compounds, antiviral agents, etc., can solve the problem of no effective drugs for inhibiting hepatitis C virus, etc., and achieve a good market. The effect of developing prospects

Inactive Publication Date: 2019-01-18
周龙兴 +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The technical problem to be solved by the present invention is to provide a compound, pharmaceutical composition and application thereof that are completely different from the prior art for inhibiting hepatitis C virus in order to overcome the defect that there is no effective drug for inhibiting hepatitis C virus in the prior art

Method used

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  • Compounds for inhibiting HCV (hepatitis C virus), pharmaceutical composition and application of compounds or pharmaceutical composition
  • Compounds for inhibiting HCV (hepatitis C virus), pharmaceutical composition and application of compounds or pharmaceutical composition
  • Compounds for inhibiting HCV (hepatitis C virus), pharmaceutical composition and application of compounds or pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0088]

[0089] At 0°C, add bis(trichloromethyl)carbonate (solid phosgene, 11.88g, 40mmol), anhydrous dichloromethane (80ml) and deuterated methanol (4.87ml, 120mmol) into the reaction flask, stir A solution of pyridine (120 mmol) in dichloromethane (30 ml) was added dropwise, and the temperature was kept at 0° C. during the dropwise addition. After the dropwise addition, stirring was continued at 0° C. for 1 hour, and then stirred at room temperature for 2 hours. After the reaction was complete, dichloromethane (100ml) was added, washed with ice water, dried over anhydrous sodium sulfate, filtered, and the solvent was evaporated to obtain a colorless oil S1-2 (10.2g, 87%).

Embodiment 2

[0091]

[0092] An aqueous solution (120ml) of D-phenylglycine (20g, 32.2mmol) in sodium hydroxide (42.4g, 0.53mol) was cooled to 0°C with an ice bath, and methyl chloroformate (10.4 ml, 266mmol). After the reaction mixture was stirred at 0°C for 1 hour, it was acidified with pre-cooled concentrated hydrochloric acid (50ml, 600mmol), the mixture was extracted with ethyl acetate (3x 150ml), dried over anhydrous magnesium sulfate, filtered, and concentrated under reduced pressure to give a white solid S1 -5 (25.3 g, 92%). 1 H NMR (DMSO-d 6 ,400MHz):12.79(br s,1H),7.96(d,J=12,1H),7.40-7.29(m,5H),5.13(d,J=12,1H),3.55(s,3H).

Embodiment 3

[0094] Deuterated compound S1-6 (87%) was prepared in the same way using deuterated methyl chloroformate 2. 1 HNMR (DMSO-d 6 ,δ=2.5ppm,400MHz):12.65(br s,1H),7.92(d,J=12,1H),7.38-7.26(m,5H),5.11(d,J=12,1H).

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Abstract

The invention discloses compounds for inhibiting HCV (hepatitis C virus), pharmaceutical composition and an application of the compounds or the pharmaceutical composition. The compounds are compoundsshown in formula (I) or a stereoisomer, geometric isomer, a tautomer, an enantiomer, sulfur oxide, nitrogen oxide, hydrate, solvate, metabolite, pharmaceutically acceptable salt or prodrug of the compounds shown in formula (I); the compounds are effective antiviral drugs, especially can be used for inhibiting the function of NS5A protein encoded by the HCV, thereby effectively inhibiting the HCV.The method for preventing and / or treating drugs or diseases associated with the HCV by the compounds or the composition containing the new compounds has good market development prospects.

Description

technical field [0001] The present invention relates to antiviral compounds, in particular to a compound capable of inhibiting the function of NS5A protein encoded by hepatitis C virus (HCV), a pharmaceutical composition containing the compound, and a method for inhibiting the function of NS5A protein and its application. Background technique [0002] Hepatitis C virus (HCV) is the major pathogen that causes most non-A, non-B hepatitis. Hepatitis C virus infection causes chronic liver disease, and a substantial fraction of these HCV-infected individuals develops severe progressive liver disease, including cirrhosis and hepatocellular carcinoma, thus, chronic HCV infection is the leading cause of death from liver disease worldwide . Approximately 170 million people worldwide are infected with HCV (five times the number of human immunodeficiency virus HIV infections), so HCV infection can be considered an urgent human health problem (cf. Lavanchy et al, J. Viral Hepatitis, 1...

Claims

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Application Information

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IPC IPC(8): C07D513/04C07D498/04C07F7/10A61K31/542A61K31/5365A61K31/695A61P31/14
CPCC07D498/04C07D513/04C07F7/0812C07F7/0814
Inventor 周龙兴陈昊蔡建华
Owner 周龙兴
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