Sloan-kettering Institute for Cancer Research

Research, Incorporated

Institut National De La Sante Et De La Recherche Medicale

Memorial Sloan Kettering Cancer Center

Jack J Fox

Kyoichi A Watanabe

Chung K Chu

Carlos A Lopez

Uri Reichman

Christian G Trepo

Joseph H Burchenal

Richard W Price

Jasenka Matulic-Adamic

Kosaku Hirota

The present invention relates to a composition for, and a method of, treating a hepatitis viral infection in a subject using 1-(2'-deoxy-2'-fluoro-beta-D-arabinofuranosyl)-5-ethyluracil [FEAU].

Method for treating hepatitis B virus infections using

2'-Deoxy-2'-fluoro-.beta.-D-arabinofuranosyl nucleosides of the following structure are disclosed: ##STR1## wherein X and Y are the same or different and are hydrogen, OR.sup.3, SR.sup.3, NR.sup.3 N.sup.4 or NHacyl wherein R.sup.3 and R.sup.4 are the same or different and are hydrogen, lower alkyl of 1 to 7 carbon atoms, aralkyl, or aryl;

2'-fluoro-arabinofuranosyl purine nucleosides

A method for synthesizing monofluoromethyl- and difluoromethyluracil nucleosides from the corresponding thymine nucleosides is developed. These compounds which contain a partially fluorinated methyl group at the C-5 position (a new class of nucleosides) are potential antiviral and/or anticancer agents. The major features of the preparative route involve bromination of suitably protected thymine nucleosides followed by fluoride treatment.

Nucleosides of 5-monofluoromethyluracil and 5-difluoromethyluracil

2'-Deoxy-2'-fluoro-.beta.-D-arabinofuranosyl nucleosides of the following structure are disclosed: ##STR1## wherein X and Y are the same or different and are hydrogen, OR.sup.3, SR.sup.3, NR.sup.3 R.sup.4 or NHacyl wherein R.sup.3 and R.sup.4 are the same or different and are hydrogen, lower alkyl of 1 to 7 carbon atoms, aralky, or aryl;

2-fluoro-arabinofuranosyl purine nucleosides

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.

Method and composition for hepatitis treatment with pyrimidine

Veterinarian composition for the treatment of herpes virus in animals comprising a pyrimidine nucleoside, or veterinarianically acceptable acid addition salte thereof, of the formula ##STR1## wherein A is OR.sup.3, SR.sup.3, NR.sup.3 R.sup.4 or NHacyl wherein R.sup.3 and R.sup.4 are the same or different and are hydrogen, lower alkyl of 1 to 7 carbon atoms, aralkyl, or aryl;

Anti-herpes virus compositions containing 5-substituted

Pyrimidine nucleosides exhibiting anti-viral and anti-tumor effects have the formula ##STR1## wherein A is OR.sup.3, SR.sup.3, NR.sup.3 R.sup.4 or NHacyl wherein R.sup.3 and R.sup.4 are the same or different and are hydrogen, lower alkyl of 1 to 7 carbon atoms, aralkyl, or aryl;

5-Substituted

There is provided a novel process for pyrimidine to pyrimidine transformations by the displacement of the 1,2,3-portion of a pyrimidine by a 1,3-ambident nucleophile. The novel process requires that the 1 and 3 nitrogens of the pyrimidine moiety be substituted. The novel process makes available, inter alia, novel uracils, simple methods of radioisotopically labeling pyrimidine nuclei, a simple and inexpensive method of preparing the important antiviral and antileukemic material pseudoisocytidine and its new active analog 2'-deoxypseudoisocytidine.

Pyrimidine to pyrimidine transformation process

A novel derivative of 1-.beta.-D-arabinofuranose namely the 5-fluorocytosine derivative has been prepared and found to have excellent activity against mouse leukemia.

2,2'-Anhydro-.beta.-D-arabinofuranosyl-5-fluorocytosine

Pseudo-isocytidine is disclosed as well as methods and intermediates useful in its preparation. The novel compound pseudo-isocytidine, preferably the beta-anomer thereof, is an active cytostatic and anti-leukemic agent.

Growing community of inventors

White Plains, NY, United States of America

Jack J Fox