DAPD combination therapy with inosine monophosphate dehydrogenase inhibitor
OwnerPhilip A. Furman, Katyna Borroto-Esodainventors
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Abstract
It has been unexpectedly found that a drug resistant strain of HIV exhibits the behavior of drug-naïve virus when given the combination of a β-D-1,3-dioxolanyl nucleoside and an IMPDH inhibitor. In one nonlimiting embodiment, the HIV strain is resistant to a β-D-1,3-dioxolanyl nucleoside.
Claims27
A pharmaceutical composition for the treatment or prophylaxis of an HIV infection in a host, comprising an effective amount of a β-D-1,3-dioxolanyl purine of the formula:
- 8
- or its pharmaceutically acceptable salt, wherein
- R is H, OH, Cl, NH2 or NR1R2;
- R1 and R2 are independently hydrogen, alkyl or cycloalkyl, and R3 is H, alkyl, aryl, acyl, phosphate, including monophosphate, diphosphate or triphosphate or a stabilized phosphate moiety, including a phospholipid, or an etherlipidin combination with at least one inosine monophosphate dehydrogenase (IMPDH) inhibitor, optionally in a pharmaceutically acceptable carrier or diluent.
A method for the treatment or prophylaxis of a drug resistant strain of HIV infection in a host, comprising administering an effective amount of a β-D-1,3-dioxolanyl purine of the formula:
- 9
- or its pharmaceutically acceptable salt, wherein
- R is H, OH, Cl, NH2 or NR1R2;
- R1 and R2 are independently hydrogen, alkyl or cycloalkyl, and R3 is H, alkyl, aryl, acyl, phosphate, including monophosphate, diphosphate or triphosphate or a stabilized phosphate moiety in combination or alternation with an inosine monophosphate dehydrogenase (IMPDH) inhibitors, optionally in a pharmaceutically acceptable carrier or diluent.
A method for the treatment or prophylaxis of HIV infection in a host, comprising administering an effective amount of a β-D-1,3-dioxolanyl purine of the formula:
- 10
- or its pharmaceutically acceptable salt, wherein R is H, OH, Cl, NH2 or NR1R2;
- R1 and R2 are independently hydrogen, alkyl or cycloalkyl, and R3 is H, alkyl, aryl, acyl, phosphate, including monophosphate, diphosphate or triphosphate or a stabilized phosphate moiety in combination or alternation with an inosine monophosphate dehydrogenase (IMPDH) inhibitors, optionally in a pharmaceutically acceptable carrier or diluent.
Dependencies are inferred from the claim text.