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Ribavirin-interferon alfa combination therapy for eradicating detectable HCV-RNA in patients having chronic hepatitis C infection

A technology for chronic hepatitis C and interferon, applied in the direction of drug combination, organic active ingredients, carbohydrate active ingredients, etc.

Inactive Publication Date: 2002-01-09
SCHERING AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this combination therapy is not always effective due to ribavirin-related side effects, such as ribavirin-related hemolysis and anemia

Method used

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  • Ribavirin-interferon alfa combination therapy for eradicating detectable HCV-RNA in patients having chronic hepatitis C infection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1A

[0178] Example 1 A. Benzylidene Ribavirin

[0179] 20g ribavirin (1.87mmol), 200ml benzaldehyde and 20g ZnCl 2 mix. The resulting reaction mixture was stirred at room temperature for 24 hours. With stirring, the resulting solution was poured into 2.5L ether (Et 2 O). The resulting mixture was filtered with suction, and the solid precipitate was dried. The solid precipitate was mixed with 1.2 L of ice-cold 2N sodium hydroxide (NaOH) solution. The mixture was extracted with 2 x 0.75 L of cold ethyl acetate (EtOAc), and the organic layer was washed with brine. The organic layer was gravity filtered through a fluted filter, then concentrated in vacuo to a solid. With 0.5L Et 2 O grind the solid well, filter with suction, and wash with fresh Et 2 O washed the formed precipitate to give 23 g of compound 2 as a solid; C 15 h 16 N 4 o 5 Calculated value (332.32). MS (FAB) = 333.1.

[0180]

[0181] 0.5 g (2.8 mmol) of compound 2, 0.80 g (2.4 mmol)...

Embodiment 2

[0184] According to the method of Example 1A and 1B, but in Step B, with an equivalent amount of compound 6 (MeOCH 2 CH 2 OCHCO 2 H) Instead of compound 3, compound 8 is formed. Following the method of step C of Example 1, but substituting an equivalent amount of compound 7 for compound 4, compound 8 was formed.

Embodiment 3

[0186] At 5° C., a solution of 0.32 g (3.6 mmol) of compound 9 [2-(N, N’-dimethylamino) ethanol] in 10 mL of N, N-dimethylformamide (DMF) was treated with 0.58 g of carbonyldiimidazole ( 3.6 mmol) and the resulting solution was warmed to 20°C over 0.5 h. To the obtained reaction mixture was added 0.8 g (2.4 mmol) of compound 2 prepared according to Example 1A, and the resulting reaction mixture was stirred at room temperature for 24 hours. Concentrate in vacuo, add 50 mL of ether, and let the resulting mixture stand for 24 hours. The supernatant was decanted, and the residue was purified by column chromatography (silica gel, 10%-20% methanol-tetrahydrofuran gradient elution) to obtain 0.21 g of compound 10 as a solid; C 20 h 25 N 5 o 7 (447.44) calculated value. MS (FAB) = 448.1.

[0187] Following the procedure of Example 1C, but substituting an equivalent amount of compound 10 for compound 4, compound 11 was obtained.

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PUM

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Abstract

A method for treating a patient having chronic hepatitis C infection to eradicate detectable HCV-RNA involving a combination therapy using a therapeutically effective amount of ribavirin derivative of formula (I) and a therapeutically effective amount of interferon-alpha for a time period of from 20 up to 80 weeks.

Description

Background of the invention [0001] The present invention relates to a method for treating patients with chronic hepatitis C infection, the method comprising administering a therapeutically effective amount of a ribavirin derivative and a therapeutically effective amount of alpha-interferon for a period of time sufficient to At the end of the dosing period, detectable HCV-RNA is eradicated, and for at least 24 weeks after the end of the dosing period, there is no detectable HCV-RNA, as well as involving the ribavirin derivative represented by formula I. [0002] Chronic hepatitis C virus infection is an insidious, chronically exacerbating disease with serious impact on quality of life. It eventually leads to cirrhosis, decompensated liver disease and / or hepatocellular carcinoma. [0003] Reichard et al. (The Lancet 1998; 351; 83-87) and T. Poynard et al. (The Lancet 1998; Vol.352; Oct.31, P1426-1432) disclosed alpha-2b interferon and ribavirin combination therapy for the tre...

Claims

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Application Information

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IPC IPC(8): A61K31/7042A61K31/7052A61K31/7056A61K38/21A61P31/12A61P31/14A61P31/20A61P43/00C07H19/056
CPCC07H19/056A61P31/12A61P31/14A61P31/20A61P43/00
Inventor A·K·甘古利J·麦科尔米克R·G·罗维F·本尼特A·K·萨克塞纳V·M·吉里雅瓦拉班
Owner SCHERING AG
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