Abstract: The present invention relates to the discovery that certain &bgr;-L-dioxolane nucleoside analogs which contain a uracil base, and preferably, a 5-halosubstituted uracil base, exhibit unexpectedly high activity against Epstein-Barr virus (EBV), Varciella-Zoster virus (VZV) and Herpes Virus 8 (HV-8). In particular, the compounds according to the present invention show potent inhibition of the replication of the virus (viral growth) in combination with very low toxicity to the host cells (i.e., animal or human tissue). Compounds are useful for treating EBV, VZV and HV-8 infections in humans.

Abstract: Pharmaceutical prodrug compositions are provided comprising azide derivatives of drugs which are capable of being converted to the drug in vivo. Azide derivatives of drugs having amine, ketone and hydroxy substituents are converted in vivo to the corresponding drugs, increasing the half-life of the drugs. In addition azide prodrugs are often better able to penetrate the blood-brain barrier than the corresponding drugs. Especially useful are azide derivatives of cordycepin, 2′-F-ara-ddI, AraA, acyclovir, penciclovir and related drugs. Useful azide prodrugs are azide derivatives of therapeutic alicyclic amines, ketones, and hydroxy-substituted compounds, including aralkyl, heterocyclic aralkyl, and cyclic aliphatic compounds, where the amine or oxygen moiety is on the ring, or where the amine or oxygen moiety is on an aliphatic side chain, as well as therapeutic purines and pyrimidines, nucleoside analogs and phosphorylated nucleoside analogs.

Abstract: The present invention relates to a compound having the formula: 1

Abstract: A method and composition for the treatment of HIV infection, HBV infection, or abnormal cellular proliferation in humans and other host animals is disclosed that includes the administration of an effective amount of a 1,3-oxaselenolane nucleoside or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.

Abstract: A method and composition for the treatment of HIV infection, HBV infection, or abnormal cellular proliferation in humans and other host animals is disclosed that includes the administration of an effective amount of a 1,3-oxaselenolane nucleoside or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.

Abstract: The present invention relates to the use of (-)-(2S,4S)-1-(2-hydroxymethyl-1,3-dioxolan-4-yl) cytosine to treat psoriasis, genital warts and other hyperproliferative keratinocyte diseases such as hyperkeratosis, ichthyosis, keratoderma or lichen planus.

Abstract: The present invention relates to the discovery that certain .beta.-L-dioxolane nucleoside analogs which contain a uracil base, and preferably, a 5-halosubstituted uracil base, exhibit unexpectedly high activity against Epstein-Barr virus (EBV), Varciella-Zoster virus (VZV) and Herpes Virus 8 (HV-8). In particular, the compounds according to the present invention show potent inhibition of the replication of the virus (viral growth) in combination with very low toxicity to the host cells (i.e., animal or human tissue). Compounds are useful for treating EBV, VZV and HV-8 infections in humans.

Abstract: A method and composition for the treatment of humans infected with HIV that includes the administration of an HIV treatment amount of an enantiomerically pure .beta.-D-dioxolanyl purine nucleoside of the formula: ##STR1## wherein R is OH, Cl, NH.sub.2, or H, or a pharmaceutically acceptable salt or derivative of the compound, optionally in a pharmaceutically acceptable carrier or diluent.

Abstract: (-)-(2S,4S)-1-(2-Hydroxymethyl-1,3-dioxolan-4-yl)cytosine (also referred to as (-)-OddC) and its use to treat cancer in animals, including humans.

Abstract: A method for stabilizing an oligonucleotide by including a .beta.-L-2'-deoxy-2'-fluoro-arabinofuranosyl nucleoside at the 5'-terminus, the 3'-terminus, or in the interior of the oligonucleotide. The oligonucleotide can be used in the modulation of gene expression through a process wherein a synthetic oligonucleotide is hybridized to a complementary nucleic acid sequence to inhibit transcription or replication of DNA or to inhibit translation or processing of RNA.

Abstract: The present invention relates to the discovery that certain .beta.-L-dioxolane nucleoside analogs which contain a uracil base, and preferably, a 5-halosubstituted uracil base, exhibit unexpectedly high activity against Epstein-Barr virus (EBV). In particular, the compounds according to the present invention show potent inhibition of the replication of the virus (viral growth) in combination with very low toxicity to the host cells (i.e., animal or human tissue). Compounds are useful for treating EBV infections in humans.

Abstract: A method and composition for the treatment of humans infected with HIV that includes the administration of an HIV treatment amount of an enantiomerically pure .beta.-D-dioxolanyl purine nucleoside of the formula: ##STR1## wherein R is OH, Cl, NH.sub.2, or H, or a pharmaceutically acceptable salt or derivative of the compound, optionally in a pharmaceutically acceptable carrier or diluent.

Abstract: Oligonucleotides that include a 2'-fluoro .beta.-L-arabinofuranosyl nucleoside at the 3'-terminus, the 5'-terminus or in the interior of the oligomer. A preferred nucleoside is 2'-fluoro-5-methyl-.beta.-L-arabinofuranosyluridine (also referred to as L-FMAU). This compound is a potent antiviral agent against HBV and EBV and exhibits low cytotoxicity. Other specific examples of active compounds include N.sub.1 -(2'-deoxy-2'-fluoro-.beta.-L-arabinofuranosyl)-5-ethyluracil, N.sub.1 -(2'-deoxy-2'-fluoro-.beta.-L-arabinofuranosyl)-5-iodocytosine), and N.sub.1 -(2'-deoxy-2'-fluoro-.beta.-L-arabinofuranosyl)-5-iodouracil.

Abstract: A method is provided for the synthesis of synthesis of acyclic purine nucleosides, particularly 9-(2-hydroxy-ethoxymethyl)-guanine (acyclovir) and 9-[(1,3-dihydroxy-2-propoxy)methyl]guanine ("DHPG") where the N.sup.2,N.sup.9 -diprotected guanine is reacted with CH.sub.3 C(O)OCH.sub.2 O(CH.sub.2).sub.2)OC(O)CH.sub.3 or 2-acetoxymethoxy-1,3-diacetoxypropane, respectively, in the presence of a mixture of an acid and acetic anhydride, or in the presence of an acid, where the acid can be phosphoric acid or polyphosphoric acid.

Abstract: A compound, and a pharmaceutical composition comprising an effective mount to treat HBV or EBV of a compound, of the formula: ##STR1## wherein R is selected from the group consisting of 5-methyluracil, adenine and cytosine, and R' is hydrogen, acyl, or alkyl or a monophosphate, diphosphate or triphosphate ester, or its pharmaceutically acceptable salt.

Abstract: A method is provided for the synthesis of synthesis of acyclic purine nucleosides, particularly 9-(2-hydroxyethoxymethyl)-guanine (acyclovir) and 9-[(1,3-dihydroxy-2-propoxy)methyl]guanine ("DHPG") where the N.sup.2,N.sup.9 -diprotected guanine is reacted with CH.sub.3 C(O)OCH.sub.2 O(CH.sub.2).sub.2)OC(O)CH.sub.3 or diacetoxypropane, respectively, in the presence of a mixture of an acid and acetic anhydride, or in the presence of an acid, where the acid can be phosphoric acid or polyphosphoric acid.

Abstract: A method for the treatment of a human infected with HBV that includes administering an HBV-treatment amount of an L-nucleoside of the formula: ##STR1## wherein R is selected from the group consisting of 5-methyluracil, adenine and cytosine, and R' is hydrogen, acyl, alkyl or a monophosphate, diphosphate or triphosphate ester, or its pharmaceutically acceptable salt.

Abstract: A method for the treatment of a human infected with EBV that includes administering an EBV-treatment amount of an L-nucleoside of the formula: ##STR1## wherein R is 5-methyluracil, and R' is hydrogen, acyl, alkyl or a monophosphate, diphosphate or triphosphate ester, or its pharmaceutically acceptable salt.

Abstract: A compound which exhibits antiviral activity having the formula: ##STR1## wherein; R.sub.1 is selected from the group consisting of alkyls and alkenyls containing from 8 to 22 carbon atoms;A is selected from the group consisting of O and S atoms;R.sub.2 is selected from the group consisting of alkyls and alkenyls containing from 8 to 22 carbon atoms; and theNucleoside is selected from the group consisting of 2',3'-dideoxynucleosides, 3'-azido-2',3'-dideoxynucleosides, and 2',3'-didehydro-2',3'-dideoxynucleosides.

Abstract: A method for preparing 2',3'-didehydrodideoxynucleosides and the corresponding reduced 2',3'-dideoxynucleosides which includesi) preparing a nucleoside derivative of the general structure ##STR1## wherein B is a nitrogen, oxygen, or sulfur heterocycle of from C.sub.1 to C.sub.15, Y is a suitable oxygen protecting group, each R is C(S)SR', where R' is an alkyl or cyanoalkyl group of C.sub.1 to C.sub.15, or both Rs together are >C.dbd.S: and thenii) deoxygenating the nucleoside derivative to the corresponding 2',3'-didehydrodideoxynucleoside.