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Last Updated: June 18, 2021

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Claims for Patent: 8,410,103


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Summary for Patent: 8,410,103
Title:(3S,11aR)-N-[2,4-difluorophenyl)methyl]-6-hydroxy-3-methyl-5,7-dioxo-2,3,5- ,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide useful as anti-HIV agent
Abstract: The present invention is directed to a substituted 2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2 -a]pyrido[1,2-d]pyrazine-5,7-dione useful as an anti-HIV agent, which has the formula: ##STR00001## as well as pharmaceutically acceptable salts thereof, compostions thereof, and methods of use thereof.
Inventor(s): Johns; Brian Alvin (Research Triangle Park, NC), Kawasuji; Takashi (Osaka, JP), Taishi; Teruhiko (Osaka, JP), Taoda; Yoshiyuki (Osaka, JP)
Assignee: Shionogi & Co., Ltd. (Osaka, JP) VIIV Healthcare Company (Research Triangle Park, NC)
Application Number:13/352,686
Patent Claims: 1. A compound which is (3S,11aR)--N-[(2,4-Difluorophenyl)methyl]-6-hydroxy-3-methyl-5,7-dioxo-2,- 3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxami- de or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprising (3S,11aR)--N-[(2,4-Difluorophenyl)methyl]-6-hydroxy-3-methyl-5,7-dioxo-2,- 3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxami- de or a pharmaceutically acceptable salt thereof together with a pharmaceutically acceptable carrier or diluent.

3. A method of treatment of an HIV infection in a human comprising administering to said human an antiviral effective amount of (3S,11aR)--N-[(2,4-Difluorophenyl)methyl]-6-hydroxy-3-methyl-5,7-dioxo-2,- 3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxami- de or a pharmaceutically acceptable salt thereof.

4. A compound which is (3S,11aR)--N-[(2,4-Difluorophenyl)methyl]-6-hydroxy-3-methyl-5,7-dioxo-2,- 3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxami- de sodium salt.

5. A pharmaceutical composition comprising (3S,11aR)--N-[(2,4-Difluorophenyl)methyl]-6-hydroxy-3-methyl-5,7-dioxo-2,- 3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxami- de sodium salt together with a pharmaceutically acceptable carrier or diluent.

6. A method of treatment of an HIV infection in a human comprising administering to said human an antiviral effective amount of (3S,11aR)-N-[(2,4-Difluorophenyl)methyl]-6-hydroxy-3-methyl-5,7-dioxo-2,3- ,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamid- e sodium salt.

7. A compound of the formula: ##STR00209##

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