Biaryl compounds having anti-infective activity

• US 20060128747A1
• Filed: 08/01/2003
• Published: 06/15/2006
• Est. Priority Date: 08/02/2002
• Status: Active Grant

• Current Assignee: Genesoft Pharmaceuticals, Inc. (Oscient Pharmaceuticals Corporation)
• Original Assignee: Genesoft Pharmaceuticals, Inc. (Oscient Pharmaceuticals Corporation)
• Inventors: Burli, Roland W., Baird, Eldon E., McMinn, Dustin L., Kaizerman, Jacob A.
• Granted Patent: US 7,498,349 B2
• Time in Patent Office: Days
• US Class Current: 514/302
• CPC Class Codes: A61K 31/44 Non condensed pyridines; Hydrogenated derivatives thereof
• CPC Class Codes: A61P 31/04 Antibacterial agents
• CPC Class Codes: C07D 307/81 Radicals substituted by nitrogen atoms not forming part of a nitro radical
• CPC Class Codes: C07D 401/12 linked by a chain containing hetero atoms as chain links
• CPC Class Codes: C07D 405/12 linked by a chain containing hetero atoms as chain links
• CPC Class Codes: C07D 405/14 containing three or more hetero rings
• CPC Class Codes: C07D 409/12 linked by a chain containing hetero atoms as chain links
• CPC Class Codes: C07D 409/14 containing three or more hetero rings
• CPC Class Codes: C07D 417/12 linked by a chain containing hetero atoms as chain links
• CPC Class Codes: C07D 417/14 containing three or more hetero rings

Abstract

Aromatic compounds exemplified by exhibit antimicrobial activity.

Claims

1. A compound according to the formula

2. A compound according to claim 1, wherein at least one group R² contains an alkyl amine group.

3. A compound according to claim 1 or 2, wherein

4. A compound according to claim 1 or 2, wherein

5. A compound according to claim 1 or 2, wherein

6. A compound according to claim 1 or 2, wherein

7. A compound according to claim 1 or 2, wherein

8. A compound according to claim 1 or 2, wherein

9. A compound according to claim 1 or 2, wherein R³ is H.

11. A compound according to claim 1, 2 or 10, wherein N(R²)₂ is selected from the group consisting of

12. A compound according to claim 1, having a minimum inhibitory concentration of 4 μ

g/mL or less against at least one of Staphylococcus aureus (ATCC

     27660), Streptococcus pneumoniae (ATCC

     51422), and Enterococcus faecium (ATCC

     51559).

13. A method of treating a bacterial infection in a mammal, comprising administering to a patient in need of such treatment an effective amount of a compound according to claim 1, 2, or 10.

14. A method according to claim 13, wherein the bacterial infection is an infection by drug resistant bacteria.

15. A method according to claim 14, wherein the drug resistant bacteria is MRSA, PRSP, or VRE.

16. The use of a compound according to claim 1, 2, or 8 for the preparation of a medicament for the treatment of a bacterial infection in a mammal.

10. A compound according to a formula selected from the group consisting of