HIV-1 mutations selected for by beta-2',3'-didehydro-2',3'-dideoxy-5-fluorocytidine
First Claim
Patent Images
1. A method for treating an HIV infection in a human comprising administering an effective amount of β
- -D-D4FC or its pharmaceutically acceptable prodrug or salt to the human, optionally in a pharmaceutically acceptable carrier, in combination or alternation with a drug that induces a mutation in HIV-1 at a location other than the 70(K to N), 90 or 172 codon of the reverse transcriptase region, and which is other than cis-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, cis-2-hydroxymethyl-5-(cytosin-1-yl)-1,3oxathiolane, 9-[4-(hydroxymethyl)-2-cyclopenten-1-yl)-guanine (carbovir), 9-[(2-hydroxyethoxy)methyl]guanine (acyclovir), interferon, 3′
-deoxy-3′
-azido-thymidine (AZT), 2′
,3′
-dideoxyinosine (DDI), 2′
,3′
-dideoxycytidine (DDC), (−
)-2′
-fluoro-5-methyl-β
-L-ara-uridine (L-FMAU) or 2′
,3′
-didehydro-2′
,3′
-dideoxythymidine (D4T).
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Abstract
The present invention discloses a method for treating HIV that includes administering μ-D-D4FC or its pharmaceutically acceptable salt or prodrug to a human in need of therapy in combination or alternation with a drug that induces a mutation in HIV-1 at a location other than the 70(K to N), 90 or the 172 codons of the reverse transcriptase region. Also disclosed is a method for using β-D-D4FC as “salvage therapy” to patients which exhibit drug resistance to other anti-HIV agents. β-D-D4FC can be used generally as salvage therapy for any patient which exhibits resistance to a drug that induces a mutation at other than the 70(K to N), 90 or the 172 codons.
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Citations
15 Claims
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1. A method for treating an HIV infection in a human comprising administering an effective amount of β
- -D-D4FC or its pharmaceutically acceptable prodrug or salt to the human, optionally in a pharmaceutically acceptable carrier, in combination or alternation with a drug that induces a mutation in HIV-1 at a location other than the 70(K to N), 90 or 172 codon of the reverse transcriptase region, and which is other than cis-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, cis-2-hydroxymethyl-5-(cytosin-1-yl)-1,3oxathiolane, 9-[4-(hydroxymethyl)-2-cyclopenten-1-yl)-guanine (carbovir), 9-[(2-hydroxyethoxy)methyl]guanine (acyclovir), interferon, 3′
-deoxy-3′
-azido-thymidine (AZT), 2′
,3′
-dideoxyinosine (DDI), 2′
,3′
-dideoxycytidine (DDC), (−
)-2′
-fluoro-5-methyl-β
-L-ara-uridine (L-FMAU) or 2′
,3′
-didehydro-2′
,3′
-dideoxythymidine (D4T).
- -D-D4FC or its pharmaceutically acceptable prodrug or salt to the human, optionally in a pharmaceutically acceptable carrier, in combination or alternation with a drug that induces a mutation in HIV-1 at a location other than the 70(K to N), 90 or 172 codon of the reverse transcriptase region, and which is other than cis-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, cis-2-hydroxymethyl-5-(cytosin-1-yl)-1,3oxathiolane, 9-[4-(hydroxymethyl)-2-cyclopenten-1-yl)-guanine (carbovir), 9-[(2-hydroxyethoxy)methyl]guanine (acyclovir), interferon, 3′
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2. A method for treating an HIV infection in a human comprising administering an effective amount of β
- -D-D4FC or its pharmaceutically acceptable salt to the human, optionally in a pharmaceutically acceptable carrier, in combination or alternation with a drug that induces a mutation in HIV-1 at codon 70 from lysine to asparagine (K to N), a mutation at codon 90 from valine to isoleucine (V to I), or mutation at codon 172 from arginine to lysine (R to K) of the reverse transcriptase region, and which is other than cis-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, cis-2-hydroxymethyl-5-(cytosin-1yl)-1,3-oxathiolane, 9-[4-(hydroxymethyl)-2-cyclopenten-1-yl)-guanine (carbovir), 9-[(2-hydroxyethoxy)methyl]guanine (acyclovir), interferon, 3′
-deoxy-3′
-azido-thymidine (AZT), 2′
,3′
-dideoxyinosine (DDI), 2′
,3′
-dideoxycytidine (DDC), (−
)-2′
-fluoro-5-methyl-β
-L-ara-uridine (L-FMAU) or 2′
,3′
-didehydro-2′
,3′
-dideoxythymidine (D4T).
- -D-D4FC or its pharmaceutically acceptable salt to the human, optionally in a pharmaceutically acceptable carrier, in combination or alternation with a drug that induces a mutation in HIV-1 at codon 70 from lysine to asparagine (K to N), a mutation at codon 90 from valine to isoleucine (V to I), or mutation at codon 172 from arginine to lysine (R to K) of the reverse transcriptase region, and which is other than cis-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, cis-2-hydroxymethyl-5-(cytosin-1yl)-1,3-oxathiolane, 9-[4-(hydroxymethyl)-2-cyclopenten-1-yl)-guanine (carbovir), 9-[(2-hydroxyethoxy)methyl]guanine (acyclovir), interferon, 3′
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3. A method for treating a patient infected with a strain of HIV virus that is resistant to an antiviral drug selected from the group consisting of (−
- )-cis-2-hydroxymethyl-5-(cytosin-1-yl)-1,3-oxathiolane, (3TC), AZT, cis-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane (FTC), 9-[4-(hydroxymethyl)-2-cyclopenten-1-yl]-guanine (Carbovir), 2′
,3′
-didehydro-2′
,3′
-didehydro-2′
,3′
-dideoxythymidine (D4T), 2′
,3′
-dideoxycytidine (DDC), 2′
,3′
-dideoxyinosine (DDI), 9-[(2-hydroxyethoxy)methyl]guanine (acyclovir), (−
)-2′
-fluoro-5-methyl-β
-L-ara-uridine (L-FMAU) and (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one (SUSTIVA™
) comprising administering an effective amount of β
-D-D4FC or its pharmaceutically acceptable prodrug or salt to the patient optionally in a pharmaceutically acceptable carrier. - View Dependent Claims (4, 5, 6, 7, 8, 9, 10, 11, 12, 13)
- )-cis-2-hydroxymethyl-5-(cytosin-1-yl)-1,3-oxathiolane, (3TC), AZT, cis-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane (FTC), 9-[4-(hydroxymethyl)-2-cyclopenten-1-yl]-guanine (Carbovir), 2′
-
14. A pharmaceutical composition for the treatment of HIV-1 in humans comprising an effective amount of β
- -D-D4FC or its pharmaceutically acceptable prodrug or salt, in a pharmaceutically acceptable carrier, in combination with an effective amount of a drug that induces a mutation in HIV-1 at a location other than the 70(K to N), 90 or 172 codon of the reverse transcriptase region, and which is other than cis-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, cis-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′
-azido-thymidine (AZT), 2′
,3′
-dideoxyinosine (DDI), 2′
,3′
-dideoxycytidine (DDC), (−
)-2′
-fluoro-5-methyl-β
-L-ara-uridine (L-FMAU) or 2′
,3′
-didehydro-2′
,3′
-dideoxythymidine (D4T).
- -D-D4FC or its pharmaceutically acceptable prodrug or salt, in a pharmaceutically acceptable carrier, in combination with an effective amount of a drug that induces a mutation in HIV-1 at a location other than the 70(K to N), 90 or 172 codon of the reverse transcriptase region, and which is other than cis-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, cis-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′
-
15. A pharmaceutical composition for the treatment of HIV-1 in humans comprising an effective amount of β
- -D-D4FC or its pharmaceutically acceptable salt, in a pharmaceutically acceptable carrier, in combination with an effective amount of a drug that induces a mutation in HIV-1 at codon 70 from lysine to asparagine (K to N), a mutation at codon 90 from valine to isoleucine (V to I), or mutation at codon 172 from arginine to lysine (R to K) of the reverse transcriptase region, and which is other than cis-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, cis-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′
-azido-thymidine (AZT), 2′
,3′
-dideoxyinosine (DDI), 2′
,3′
-dideoxycytidine (DDC), (−
)-2′
-fluoro-5-methyl-β
-L-ara-uridine (L-FMAU) or 2′
,3′
-didehydro-2′
,3′
-dideoxythymidine (D4T).
- -D-D4FC or its pharmaceutically acceptable salt, in a pharmaceutically acceptable carrier, in combination with an effective amount of a drug that induces a mutation in HIV-1 at codon 70 from lysine to asparagine (K to N), a mutation at codon 90 from valine to isoleucine (V to I), or mutation at codon 172 from arginine to lysine (R to K) of the reverse transcriptase region, and which is other than cis-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, cis-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′
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Current AssigneeEmory University
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Original AssigneeEmory University
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InventorsSchinazi, Raymond F., Liotta, Dennis C., Mellors, John W., Hammond, Jennifer L.
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Granted Patent
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Time in Patent OfficeDays
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Field of Search
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US Class Current514/151
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CPC Class CodesA61K 2300/00 Mixtures or combinations of...A61K 31/70 Carbohydrates; Sugars; Deri...A61K 31/7068 having oxo groups directly ...A61K 45/06 Mixtures of active ingredie...
