Abstract: The present invention relates to the surprising discovery that certain dideoxynucleoside analogs which contain a dideoxy ribofuranosyl moiety having an L-configuration (as opposed to the naturally occurring D- configuration) exhibit unexpected activity against Hepatitis B virus (HBV). In particular, the compounds according to the present invention show potent inhibition of the replication of the virus in combination with very low toxicity to the host cells (i.e., animal or human tissue). Compounds according to the present invention exhibit primary utility as agents for inhibiting the growth or replication of HBV, HIV and other retroviruses, most preferably HBV.

Abstract: Novel podophyllotoxin compounds and their use in treating tumors are disclosed. The analogs have the general formula: ##STR1## wherein NH--R is a selected aryl amine, dialkylaminoalkyleneamino, or dialkylaminoanilino group.

Abstract: Compounds which are analogs of etoposide and which exhibit anti-tumor activity are disclosed. These compounds having the following structure: ##STR1## wherein R is selected from ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each independently selected from H, CH.sub.3, C.sub.2 H.sub.5, C.sub.3 H.sub.7, i--C.sub.3 H.sub.7, C.sub.4 H.sub.9, CF.sub.3, OCH.sub.3, OC.sub.2 H.sub.5 , OC.sub.3 H.sub.7, OC.sub.4 H.sub.9, O--i--C.sub.3 H.sub.7, O--i--C.sub.4 H.sub.9, --OCH.sub.2 O--, --OCH.sub.2 CH.sub.2 O--, CH.sub.2 OH, C.sub.2 H.sub.4 OH, CH.sub.2 Cl C.sub.2 H.sub.4 Cl, CH.sub.2 F, C.sub.2 H.sub.4 F, CH.sub.2 OCH.sub.3, COCH.sub.3, COC.sub.2 H.sub.5, CO.sub.2 CH.sub.3, CO.sub.2 C.sub.2 H.sub.5, NO.sub.2, NH.sub.2, NH.sub.2.HCl, NH.sub.2.HAc, NH.sub.2.1/2H.sub.2 SO.sub.4 , NH.sub.2.1/3H.sub.3 PO.sub.4, N(CH.sub.3).sub.2, N(C.sub.2 H.sub.5).sub.2, OH, CN, N.sub.3, SO.sub.2 H, SO.sub.2 NH.sub.2 , SO.sub.

Abstract: Novel podophyllotoxin compounds and their use in treating tumors are disclosed.

Abstract: This invention relates to nucleoside and acyclo analogs containing 5- or 6-substituted 2-pyrazinone-4-N-oxide. These compounds are useful for treating various conditions including viral infections, cancer, fungal infections, bacterial infections, microbial infections and related disease states. This invention also relates to pharmaceutical formulations containing these compounds. In addition, this invention relates to methods of treating the above-described conditions in animals and in particular, humans.

Abstract: Compounds that are analogs of etoposide and exhibit antitumor activity are disclosed. The compounds of the present invention have the following formula: ##STR1## where: R.sub.1 is .beta.-OCH.sub.2 CH.sub.2 NH.sub.2 .beta.-NHCH(CH.sub.3)CH.sub.2 OH, .beta.-NHCH.sub.2 CH(CH.sub.3)OH, .beta.-Cl, .beta.-Br, .beta.-OH, .alpha.-OH, .beta.-NH, .alpha.-NH.sub.2, .beta.-NHCH.sub.2 CH.sub.2 OH, .alpha.-NHCH.sub.2 CH.sub.2 OH, .beta.-NHCH.sub.2 CH.sub.2 CH.sub.3, .beta.-NHCH.sub.2 CH.sub.2 OCH.sub.3, .beta.-NHCH.sub.2 CH.dbd.CH.sub.2, .beta.-NHCH.sub.2 CH(OH)CH.sub.3, .beta.-NHCH.sub.2 CH.sub.2 CH.sub.2 OH, .beta.-OCH.sub.2 CH.sub.2 OH, ##STR2## R.sub.2 is H, or Br; R.sub.1 is H, or Br;R.sub.4 is H, or Br;R.sub.5 is H, or Br; andR.sub.6 is H, or --CH.sub.3.

Abstract: The invention relates to a method of selectively inhibiting herpes simplex virus-specified thymidine kinase. The method comprises exposing mammalian cells infected with the virus to an effective amount of 5'-ethynylthymidine. The invention further relates to a pharmaceutical composition comprising 5'-ethynylthymidine as the active ingredient together with a pharmaceutically acceptable carrier.

Abstract: The nuceoside 1-(2-Deoxy-.beta.-D-ribofuranosyl)-5-(iodo)-2-pyrimidinone possesses a high level of antiviral activity and a low level of toxicity to the host cell making it an especially effective therapeutic agent for HSV-2.

Abstract: Compounds for inhibiting the replication of DNA viruses which induce the formation of thymidine kinase enzyme of the formula: ##STR1## wherein R.sub.1 is a radical selected from the group consisting of chloro, iodo, hydroxy, alkoxyalkyl, hydroxyalkyl, methylamino, formyl, nitro, and unsubstituted hydrocarbon groups of 2 to about 3 carbon atoms or halosubstituted hydrocarbon groups of 1 to about 3 carbon atoms; R.sub.2 is hydrogen or hydroxy; and R.sub.3 is hydroxy, --OP(O)(OH).sub.2, amino, or --OCOR.sub.4 where R.sub.4 is alkyl or alkoxyalkyl of 2 to about 18 carbon atoms.

Abstract: A method for inhibiting the replication of a DNA virus which induces formation of thymidine kinase enzyme, by exposing the virus to an effective concentration of a compound of the formula: ##STR1## wherein R.sub.1 is a radical selected from the group consisting of halogen, --SCH.sub.3, --OH, alkoxy, cyano, methylamino, carboxy, formyl, nitro and unsubstituted or halosubstituted hydrocarbon groups of 1 through 3 carbon atoms; R.sub.2 is hydrogen; halogen or hydroxy; and R.sub.3 is hydroxy, --OP(O)(OH).sub.2, amino, or --OOR.sub.4 where R.sub.4 is lower alkyl of 1 through 6 carbon atoms.

Abstract: Novel arabinofuranosyl nucleosides and nucleotides having 2'-azido,2'-amino, or 2'-hydrocarbylamino substituents, which have antitumor, antiviral, and antimicrobial properties, are prepared by condensation of a pyrimidine, purine, or 1,3-oxazine base with an acylated 2-azido-2-deoxyarabinofuranosyl halide, followed by deblocking and catalytic hydrogenation, where appropriate, to convert the 2'-azido group to a 2'-amino group and, if desired, alkylation or the like to convert the 2'-amino group to a 2'-hydrocarbylamino group.

Abstract: Novel arabinofuranosyl nucleosides and nucleotides having 2'-azido, 2'-amino, or 2'-hydrocarbylamino substituents, which have antitumor, antiviral, and antimicrobial properties, are prepared by condensation of a pyrimidine, purine, or 1,3-oxazine base with an acylated 2-azido-2-deoxyarabinofuranosyl halide, followed by deblocking and catalytic hydrogenation, where appropriate, to convert the 2'-azido group to a 2'-amino group and, if desired, alkylation or the like to convert the 2'-amino group to a 2'-hydrocarbylamino group.

Abstract: The compounds 5'-amino-2',5'-dideoxy-5-iodouridine; 5'-amino-2',5'-dideoxy-5-bromouridine; and the pharmaceutically acceptable acid addition salts thereof have been found to be potent inhibitors of herpes simplex virus.