Improved specificity in treatment of diseases

A selective, drug-based technology that can be used to improve specific areas of disease treatment and address issues such as reducing effective doses

Inactive Publication Date: 2003-12-03
RIBAPHARM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, phosphorylated ribavirin tends to accumulate in red blood cells, significantly reducing the effective dose

Method used

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  • Improved specificity in treatment of diseases
  • Improved specificity in treatment of diseases
  • Improved specificity in treatment of diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0052] (a) as attached figure 2 An exemplary synthesis of the indicated ribavirin is shown below.

[0053] Methyl 1-(2,3,5-tri-O-acetyl-β-D-ribofuranosyl)-1,2,4-triazole- 3-Carboxylate (3) and

[0054] Methyl 1-(2,3,5-tri-O-acetyl-β-D-ribofuranosyl)-1,2,4-triazole-5- Carboxylate (4)

[0055] Methyl-1,2,4-triazole-3-carboxylate (25.4 g, 200 mmol) (1), 1,2,3,5-tetra-O-acetyl-β-D-ribofuranose ( A mixture of 63.66 g, 200 mmol) of (2) and bis(p-nitrophenyl)phosphate (1 g) was placed in a RB flask (500 mL). Place the flask in a preheated oil bath at 165-175°C and stir under water vacuum for 25 minutes. Displaced acetic acid was collected in an ice-cold trap placed between the aspirator and the RB flask. Remove the flask from the oil bath and cool. When the flask temperature was about 60-70 °C, EtOAc (300 mL) and saturated NaHCO 3 (150 mL), and extracted with EtOAc. The aqueous layer was extracted with EtOAc (200 mL). The combined EtOAc extracts were washed with satu...

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Abstract

A drug is modified by covalently coupling a blocking group to the drug via a nitrogen atom in the blocking group. The blocking group in the modified drug prevents metabolic conversion and sequestration of the drug in non-target cells, and the blocking group is enzymatically removed in the target cell. Particularly contemplated advantages of presented compounds and methods include reduction of cytotoxicity by inhibition of metabolic conversion to potentially cytotoxic metabolites, reduction of dosages of drugs by reduction of sequestration into non-target cells, and increase of selectivity of a drug.

Description

[0001] This application claims the benefit of the following applications: U.S. Provisional Application 60 / 226 948 (filed 08 / 22 / 00), U.S. Provisional Application 60 / 226 870 (filed 08 / 22 / 00) and U.S. Provisional Application 60 / 226 871 (filed 08 / 00) 22 / 00), the entire disclosure of which is hereby incorporated by reference. field of invention [0002] The present invention relates to improving the specificity of disease treatment. Background of the invention [0003] Although many treatments have been developed, liver diseases, especially viral hepatitis B and C, remain a serious threat. Depending on the drugs used, treatment can be classified as direct antiviral therapy, indirect antiviral therapy, or a combination of direct and indirect antiviral therapy. [0004] Direct antiviral therapy can interfere with viral replication and / or viral assembly. For example, nucleoside analogs can be used to reduce viral replication by inhibiting ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7056A61K31/7084A61K47/48A61K45/00A61P1/16A61P7/00A61P31/12A61P35/00A61P43/00C07H19/052C07H19/056
CPCC07H19/052C07H19/056A61P1/16A61P31/12A61P35/00A61P43/00A61P7/00A61K31/7052
Inventor J·劳Z·洪C·-C·林
Owner RIBAPHARM
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