Method and composition for hepatitis treatment with pyrimidine nucleoside compounds

• US 4,666,892 A
• Filed: 02/10/1986
• Issued: 05/19/1987
• Est. Priority Date: 03/06/1984
• Status: Expired due to Term

• Current Assignee: Institut National De La Sante Et De La Recherche Medicale (Inserm) (Allianz Global Investors GmbH)
• Original Assignee: Memorial Sloan-Kettering Cancer Center
• Inventors: Lopez, Carlos, Trepo, Christian G., Watanabe, Kyoichi A., Fox, Jack J.
• Primary Examiner(s): BROWN, JOHNNIE
• Application Number:
  US06/828,569
• Time in Patent Office: 463 Days
• Field of Search: 514/49, 514/50
• US Class Current: 514/49
• CPC Class Codes: A61K 31/70 Carbohydrates; Sugars; Derivatives thereof sorbitol A61K31/047
• CPC Class Codes: C07H 19/06 Pyrimidine radicals
• CPC Class Codes: C07H 19/12 Triazine radicals

Abstract

The invention relates to 5-substituted-1-(2'"'"'-deoxy-2'"'"'-substituted-beta-D-Arabinofuranoysyl) pyrimidine compounds and their use in a method for the treatment of hepatitis B viruses.

Claims

1. A method for the treatment of hepatitis B virus infection in an infected human comprising

administering an effective amount to inhibit hepatitis B virion replication, 5-substituted-1-(2'"'"'-deoxy-2'"'"'-substituted-beta-D-arabinofuranosyl)pyrimidine compound of the formula ##STR1## wherein A is OR³, SR³, NR³ R⁴ or NHacyl wherein R³ and R⁴ are the same or different and are hydrogen, lower alkyl of 1 to 7 carbon atoms, aralkyl, or aryl;

NHacyl is alkanoyl or aroyl amide;

B is oxygen or sulfur;

X is halogen

Y is halogen, amino, monoalkyl- or monoaralkylamino, dialkylamino, aminomethyl, hydroxymethyl, lower alkyl, aryl, aralkyl, vinyl and substituted vinyl or ethynyl and substituted ethynyl;

Z is methyne or nitrogen;

R¹ and R² are the same or different and are hydrogen acyl or aroyl.

2. The method of claim 1 wherein the pyrimidine compound is administered intravenously.

3. The method of claim 1 wherein the pyrimidine compound is administered orally.

9. The method of claim 1 wherein up to 400 mg/m² of FIAU are used per day.

4. A method of treating hepatitis B virus infection comprising administering an effective amount of FIAC.

5. The method of claim 4 wherein up to 400 mg/m² of FIAC are used per day.

6. A method of treating hepatitis B virus infection comprising admininstering an effective amount of FMAU.

7. The method of claim 6 wherein up to 32 mg/m² of FMAU are used per day.

8. A method of treating hepatitis B virus infection comprising administering an effective amount of FIAU.