# US 5,703,058 A · Compositions containing 5-fluoro-2',3'-didehydro-2',3'-dideoxycytidine or a mono-, di-, or triphosphate thereof and a second antiviral agent > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 5,703,058 A - Document ID: US5703058A - Status: Granted - Kind: A - Application number: 08/379,276 - Filed: 1995-01-27 - Granted: 1997-12-30 - Earliest claimed: 1995-01-27 - Assignees: Emory University - Inventors: Raymond F. Schinazi; Dennis C. Liotta - Web page: https://patentgrep.com/patent/US5703058A ## CPC - A61K 31/7068: having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid - A61K 31/70: Carbohydrates; Sugars; Derivatives thereof (sorbitol A61K31/047) - A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca - A61P 31/12: Antivirals - A61P 31/14: for RNA viruses - A61P 31/18: for HIV - A61P 31/20: for DNA viruses - A61P 37/04: Immunostimulants - C07H 19/06: Pyrimidine radicals - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS - C07H: SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS (derivatives of aldonic or saccharic acids C07C, C07D; aldonic acids, saccharic acids C07C59/105, C07C59/285; cyanohydrins C07C255/16; glycals C07D; compounds of unknown constitution C07G; polysaccharides, derivatives thereof C08B; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification C12N15/00; sugar industry C13) ## Abstract A method and composition for the treatment of HIV and HBV infections in humans and other host animals is disclosed that includes the administration of an effective amount of a ›5-carboxamido or 5-fluoro!-2',3'-dideoxy-2',3'-didehydro-pyrimidine nucleoside or a ›5-carboxamido or 5-fluoro!-3'-modified-pyrimidine nucleoside, or a mixture or a pharmaceutically acceptable derivative thereof, including a 5' or N.sup.4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier. ## Claims ### Claim 1 A composition comprising an effective HIV or HBV treatment amount of a compound of the formula: ##STR3## wherein R is hydrogen, monophosphate, diphosphate, or triphosphate; in combination or alternation with a second compound selected from the group consisting of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, 2-hydroxymethyl-5-(cytosin-1-yl)-1,3-oxathiolane; 9-›4-(hydroxymethyl)-2-cyclopenten-1-yl!-guanine (carbovir), 9-›(2-hydroxyethoxy)methyl!guanine (acyclovir) interferon, 3'-deoxy-3'-azidothymidine (AZT), 2',3'-dideoxyinosine (DDI), 2',3'-dideoxycytidine (DDC), (-)-2'-fluoro-5-methyl-.beta.-L-ARAuridine (L-(-)-FMAU) and 2',3'-didehydro-2',3'-dideoxythymidine (D4T). ### Claim 2 (depends on 1) The composition of claim 1, wherein R is hydrogen. ### Claim 3 (depends on 1) The composition of claim 1, wherein R is monophosphate. ### Claim 4 (depends on 1) The composition of claim 1, wherein R is selected from the group consisting of diphosphate and triphosphate. ### Claim 5 (depends on 1) The composition of claim 1, wherein R is diphosphate. ### Claim 6 (depends on 1) The composition of claim 1, wherein the second compound is 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane. ### Claim 7 (depends on 1) The composition of claim 1, wherein the second compound is 2-hydroxymethyl-5-(cytosin-1-yl)-1,3-oxathiolane. ### Claim 8 (depends on 1) The composition of claim 1, wherein the second compound is carbovir. ### Claim 9 (depends on 1) The composition of claim 1, wherein the second compound is acyclovir. ### Claim 10 (depends on 1) The composition of claim 1, wherein the second compound is interferon. ### Claim 11 (depends on 1) The composition of claim 1, wherein the second compound is AZT. ### Claim 12 (depends on 1) The composition of claim 1, wherein the second compound is DDI. ### Claim 13 (depends on 1) The composition of claim 1, wherein the second compound is DDC. ### Claim 14 (depends on 1) The composition of claim 1, wherein the second compound is L-(-)-FMAU. ### Claim 15 (depends on 1) The composition of claim 1, wherein the second compound is D4T. ### Claim 16 (depends on 1) The composition of claim 1, wherein the combination is effective against HIV. ### Claim 17 (depends on 1) The composition of claim 1, wherein the alternation is effective against HIV. ### Claim 18 (depends on 1) The composition of claim 1, wherein the combination is effective against HBV. ### Claim 19 (depends on 1) The composition of claim 1, wherein the alternation is effective against HBV.