3′,5-difluoro-2′,3′-didehydropyrimidine nucleosides and methods of treatment therewith
First Claim
Patent Images
1. A β
- -L or β
-D nucleoside of the structure;
wherein;
Y is O;
Z is O;
R1 is F;
R′
1 is H;
R2 is independently H, C1 to C6 alkyl, or C(O)(C1 to C6 alkyl); and
R3 is H, C(O)(C1 to C6 alkyl)2 alkyl, or mono-, di-, or triphosphate or the pharmaceutically acceptable suit thereof.
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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 N4 alkylated or acrylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier.
102 Citations
86 Claims
-
1. A β
- -L or β
-D nucleoside of the structure;
wherein; Y is O;
Z is O;
R1 is F;
R′
1 is H;
R2 is independently H, C1 to C6 alkyl, or C(O)(C1 to C6 alkyl); and
R3 is H, C(O)(C1 to C6 alkyl)2 alkyl, or mono-, di-, or triphosphate or the pharmaceutically acceptable suit thereof. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12)
- -L or β
-
13. A method for treating a host infected with human immunodeficiency virus comprising administering an effective amount of a β
- -L or β
-D nucleoside of the structure;
wherein; Y is O;
Z is O;
R1 is F;
R′
1 is H;
R2 is independently H, C1 to C6 alkyl, or C(O)(C1 to C6 alkyl); and
R3 is H, C(O)(C1 to C6 alkyl)2 alkyl, or mono-, di-, or triphosphate or the pharmaceutically acceptable salt thereof. - View Dependent Claims (14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 41)
- -L or β
-
27. A method for treating a host infected with hepatitis B virus comprising administering an effective amount of a β
- -L or β
-D nucleoside of the structure;
wherein; Y is O Z is O R1 is F;
R′
1 is H;
R2 is H, C1 to C6 alkyl- or C(O)(C1 to C6 alkyl); and
R3 is H, C(O)(C1 to C6 alkyl)2 alkyl, or mono-, di-, or triphosphate or the pharmaceutically acceptable salt thereof. - View Dependent Claims (28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40)
- -L or β
-
42. A pharmaceutical composition comprising an effective anti-HIV or anti-HBV treatment amount of a β
- -L or β
-D nucleoside of the structure;
wherein; Y is O Z is O R1 is F;
R′
1 is H;
R2 is independently H, C1 to C6 alkyl, or C(O)(C1 to C6 alkyl); and
R3 is H, C(O)(C1 to C6 alkyl)2 alkyl, or mono-, di-, or triphosphate or the pharmaceutically acceptable salt in combination with a pharmaceutically acceptable carrier. - View Dependent Claims (43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55)
- -L or β
-
56. A pharmaceutical composition comprising an effective anti-HIV or anti-HBV treatment amount of a β
- -L or β
-D nucleoside of the structure;
wherein; Y is O Z is O R1 is F;
R′
1 is H;
R2 is independently H, C1 to C6 alkyl, or C(O)(C1 to C6 alkyl); and
R3 is H, C(O)(C1 to C6 alkyl)2 alkyl, or mono-, di-, or triphosphate or its pharmaceutically acceptable salt in combination with a second antiviral agent, optionally in combination with a pharmaceutically acceptable carrier or diluent. - View Dependent Claims (57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70)
- -L or β
-
71. A method for treating a host infected with human immunodeficiency virus or hepatitis B virus comprising administering an effective amount of a β
- -L or β
-D nucleoside of the structure;
wherein; Y is O;
Z is O;
R1 is F;
R′
1 is H;
R2 is independently H, C1 to C6 alkyl, or C(O)(C1 to C5 alkyl); and
R3 is H, C(O)(C1 to C6 alkyl)2 alkyl, or mono-, di-, or triphosphate or the pharmaceutically acceptable salt thereof, in combination with a second antiviral agent, and optionally in combination with a pharmaceutically acceptable carrier or diluent. - View Dependent Claims (72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86)
- -L or β
Specification