NUCLEOSIDE CYCLICPHOSPHATES

• US 20100081628A1
• Filed: 06/05/2009
• Published: 04/01/2010
• Est. Priority Date: 06/11/2008
• Status: Active Grant

• Current Assignee: Gilead Sciences Inc.
• Original Assignee: Pharmasset Incorporated (Gilead Sciences Inc.)
• Inventors: DU, Jinfa, ROSS, Bruce S., PAMULAPATI, Ganapati REDDY, SOFIA, Michael Joseph, NAGARATHNAM, Dhanapalan
• Granted Patent: US 8,173,621 B2
• Time in Patent Office: Days
• US Class Current: 514/48
• CPC Class Codes: A61P 31/12 Antivirals
• CPC Class Codes: A61P 31/14 for RNA viruses
• CPC Class Codes: C07D 473/18 one oxygen and one nitrogen atom, e.g. guanine
• CPC Class Codes: C07H 19/10 with the saccharide radical esterified by phosphoric or polyphosphoric acids
• CPC Class Codes: C07H 19/20 with the saccharide radical esterified by phosphoric or polyphosphoric acids

Abstract

Cyclic phosphate of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof, represented by the following structure:

Claims

1. A compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, deuterated analogues, or crystalline forms thereof represented by formula I:

3. A composition for the treatment and/or prophylaxis of any of the viral agents disclosed herein said composition comprising a pharmaceutically acceptable medium selected from among an excipient, carrier, diluent, and equivalent medium and the compound of claim 1.

5. A use of the compound of claim 1 in the manufacture of a medicament for the treatment of any condition the result of an infection by hepatitis C virus, West Nile virus, yellow fever virus, dengue virus, rhinovirus, polio virus, hepatitis A virus, bovine viral diarrhea virus or Japanese encephalitis virus.

7. A method of treatment in a subject in need thereof, which comprises:

administering a therapeutically effective amount of the compound of claim 1 to the subject.

9. A process for preparing the compound of claim 1

said process comprising reacting III with R¹OP(NR₂)₂, and then oxidizing II to form I according to the following scheme

11. A composition obtained by the process of claim 9.

2. A compound its stereoisomer, salt, hydrate, solvate, or crystalline form thereof selected from among

4. A composition for the treatment and/or prophylaxis of any of the viral agents disclosed herein said composition comprising a pharmaceutically acceptable medium selected from among an excipient, carrier, diluent, and equivalent medium and the compound of claim 2.

6. A use of the compound of claim 2 in the manufacture of a medicament for the treatment of any condition the result of an infection by hepatitis C virus, West Nile virus, yellow fever virus, dengue virus, rhinovirus, polio virus, hepatitis A virus, bovine viral diarrhea virus or Japanese encephalitis virus.

8. A method of treatment in a subject in need thereof, which comprises:

administering a therapeutically effective amount of the compound of claim 2 to the subject.