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US4666892A Expired / Lapsed US ⏱️ 0.0 years remaining

Method and composition for hepatitis treatment with pyrimidine nucleoside compounds

Assignee: Memorial Sloan Kettering Cancer Center
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Filing: 1986-02-10
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Granted: 1987-05-19
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Expires: 2006-02-10
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Abstract

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.

Inventors

  • 👤 Jack J. Fox
  • 👤 Kyoichi A. Watanabe
  • 👤 Carlos Lopez
  • 👤 Christian G. Trepo

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-03 19:16
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/70; C; C07; C07H; C07H19/00; C07H19/02; C07H19/04; C07H19/06; C07H19/12

Claims Analysis

Total Claims: 13
Claim 1
Independent Claim 129 words
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 OR 3 , SR 3 , NR 3 R 4 or NHacyl wherein R 3 and R 4 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; R 1 and R 2 are the same or different and are hydrogen acyl or aroyl.
Claim 2
Independent Claim 129 words
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 OR 3 , SR 3 , NR 3 R 4 or NHacyl wherein R 3 and R 4 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; R 1 and R 2 are the same or different and are hydrogen acyl or aroyl.
Claim 3
Dependent Claim 12 words
The method of claim 1 wherein the pyrimidine compound is administered intravenously.
Claim 4
Dependent Claim 12 words
The method of claim 1 wherein the pyrimidine compound is administered orally.
Claim 5
Independent Claim 15 words
A method of treating hepatitis B virus infection comprising administering an effective amount of FIAC.
Claim 6
Independent Claim 15 words
A method of treating hepatitis B virus infection comprising administering an effective amount of FIAC.
Claim 7
Dependent Claim 17 words
The method of claim 4 wherein up to 400 mg/m 2 of FIAC are used per day.
Claim 8
Independent Claim 15 words
A method of treating hepatitis B virus infection comprising admininstering an effective amount of FMAU.
Claim 9
Independent Claim 15 words
A method of treating hepatitis B virus infection comprising admininstering an effective amount of FMAU.
Claim 10
Dependent Claim 17 words
The method of claim 6 wherein up to 32 mg/m 2 of FMAU are used per day.
Claim 11
Independent Claim 15 words
A method of treating hepatitis B virus infection comprising administering an effective amount of FIAU.
Claim 12
Independent Claim 15 words
A method of treating hepatitis B virus infection comprising administering an effective amount of FIAU.
Claim 13
Dependent Claim 17 words
The method of claim 1 wherein up to 400 mg/m 2 of FIAU are used per day.

References Cited (Backward Citations)

US4211771A Cited
US4093714A Cited
US4210638A Cited
US4211773A Cited
US4382925A Cited
US4468384A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1990-05-18 1990-11-17 1991-05-19 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1994-05-18 1994-11-17 1995-05-19 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1998-05-18 1998-11-17 1999-05-19 $7700.00 Window Closed / Lapsed

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