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Claims for Patent: 7,964,580

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Claims for Patent: 7,964,580

Title:Nucleoside phosphoramidate prodrugs
Abstract: Disclosed herein are phosphoramidate prodrugs of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomer, salt (acid or basic addition salt), hydrate, solvate, or crystalline form thereof, represented by the following structure: ##STR00001## Also disclosed are methods of treatment, uses, and processes for preparing each of which utilize the compound represented by formula I.
Inventor(s): Sofia; Michael Joseph (Doylestown, PA), Du; Jinfa (New Hope, PA), Wang; Peiyuan (Glen Rock, NJ)
Assignee: Pharmasset, Inc. (Princeton, NJ)
Application Number:12/053,015
Patent Claims: 1. (S)-2-{[(2R,3R,4R,5R)-5-(2,4-Dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-4-fl- uoro-3-hydroxy-4-methyl-tetrahydro-furan-2-ylmethoxy]-phenoxy-phosphorylam- ino}-propionic acid isopropyl ester or a stereoisomer thereof.

2. A composition comprising the compound or a stereoisomer thereof as claimed in claim 1 and a pharmaceutically acceptable medium.

3. A composition for treating a hepatitis C virus, which comprises an effective amount of the compound or a stereoisomer thereof as claimed in claim 1 and a pharmaceutically acceptable medium.

4. A method of treating a subject infected by a virus, which comprises: administering to the subject an effective amount of the compound or a stereoisomer thereof as claimed in claim 1; wherein the virus is selected from among hepatitis C virus, West Nile virus, a yellow fever virus, a dengue virus, a rhinovirus, a polio virus, a hepatitis A virus, a bovine viral diarrhea virus, and a Japanese encephalitis virus.

5. A method of treating a hepatitis C virus infection in a subject in need thereof, which comprises: administering to the subject an effective amount of the compound or a stereoisomer thereof as claimed in claim 1.

6. A process for preparing the compound or a stereoisomer thereof as claimed in claim 1, said process comprising: reacting a compound 4'' with a nucleoside analog 5' ##STR00092## wherein X' is a leaving group.

7. A product comprising the compound or a stereoisomer thereof as claimed in claim 1 obtained by a process comprising: reacting a compound 4'' with a nucleoside analog 5' ##STR00093## wherein X' is a leaving group.

8. (S)-isopropyl 2-(((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-4-flu- oro-3-hydroxy-4-methyltetrahydrofuran-2-yl)methoxy)(phenoxy)phosphoryl)ami- no)propanoate.

9. A composition comprising the compound as claimed in claim 8 and a pharmaceutically acceptable medium.

10. A composition for treating a hepatitis C virus, which comprises an effective amount of the compound as claimed in claim 8 and a pharmaceutically acceptable medium.

11. A method of treating a subject infected by a virus, which comprises: administering to the subject an effective amount of the compound as claimed in claim 8; wherein the virus is selected from among hepatitis C virus, West Nile virus, a yellow fever virus, a dengue virus, a rhinovirus, a polio virus, a hepatitis A virus, a bovine viral diarrhea virus, and a Japanese encephalitis virus.

12. A method of treating a hepatitis C virus infection in a subject in need thereof, which comprises: administering to the subject an effective amount of the compound as claimed in claim 8.

13. A process for preparing the compound as claimed in claim 8, said process comprising: reacting a compound 4'' with a nucleoside analog 5' ##STR00094## wherein X' is a leaving group.

14. A product comprising the compound as claimed in claim 8 obtained by a process comprising: reacting a compound 4'' with a nucleoside analog 5' ##STR00095## wherein X' is a leaving group.
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