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 having HIV integrase inhibitory activity

Patent metadata

Field	Value
Publication number	US-10927129-B2
Application number	US-201916400373-A
Country	US
Kind code	B2
Filing date	May 1, 2019
Priority date	Apr 28, 2005
Publication date	Feb 23, 2021
Grant date	Feb 23, 2021

Abstract

The present invention is directed to 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 of the formula:

or a pharmaceutically acceptable salt or stereoisomer thereof, and pharmaceutical compositions comprising the same. The present invention has HIV integrase inhibitory activity.

First claim

The invention claimed is:

1. A compound:

or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent together with the compound according to claim 1 , or a pharmaceutically acceptable salt thereof.

3. A compound:

4. A pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent together with the compound according to claim 3 .

5. A compound:

6. A pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent together with the compound according to claim 5 .

7. A compound:

or a pharmaceutically acceptable salt thereof.

8. A pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent together with the compound according to claim 7 , or a pharmaceutically acceptable salt thereof.

9. A compound:

10. A pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent together with the compound according to claim 9 .

11. A compound:

12. A pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent together with the compound according to claim 11 .

Assignees

• Shionogi & Co
• Viiv Healthcare Co
• Shinogi Co

Inventors

• Johns Brian A
• Kawasuji Takashi
• Taishi Teruhiko
• Taoda Yoshiyuki

Classifications

• C07D498/04

  Ortho-condensed systems · CPC title

• A61K45/06

  Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title

• A61P31/18

  for HIV · CPC title

• C07D471/04

  Ortho-condensed systems · CPC title

• A61K31/5365

  ortho- or peri-condensed with heterocyclic ring systems · CPC title