Boron containing small molecules

• US 8,895,534 B2
• Filed: 07/30/2010
• Issued: 11/25/2014
• Est. Priority Date: 06/20/2007
• Status: Active Grant

• Current Assignee: Anacor Pharmaceuticals, Inc. (Pfizer Inc.)
• Original Assignee: Anacor Pharmaceuticals, Inc. (Pfizer Inc.)
• Inventors: Baker, Stephen J., Hernandez, Vincent S., Sharma, Rashmi, Nieman, James A., Akama, Tsutomu, Zhang, Yong-Kang, Plattner, Jacob J., Alley, Michael Richard Kevin, Singh, Rajeshwar, Rock, Fernando
• Primary Examiner(s): Otton, Alicia L
• Application Number:
  US12/848,051
• Publication Number:
  US 20100292504A1
• Time in Patent Office: 1,579 Days
• Field of Search: None
• US Class Current: 514/64
• CPC Class Codes: A61K 31/69 Boron compounds
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 13/02 of urine or of the urinary tract, e.g. urine acidifiers
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 31/00 Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• CPC Class Codes: A61P 31/02 Local antiseptics
• CPC Class Codes: A61P 31/04 Antibacterial agents
• CPC Class Codes: A61P 31/10 Antimycotics
• CPC Class Codes: C07F 5/025 Boronic and borinic acid compounds
• CPC Class Codes: Y02A 50/30 Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

Novel monosubstituted and disubstutituted oxaboroles and pharmaceutical compositions containing such oxaboroles are provided, which are useful for treating bacterial infections, as well as combinations of these oxaboroles with at least one additional therapeutically effective agent.

Claims

1. A compound having a structure according to the formula:

2. A combination comprising a first therapeutically active agent which is the compound of claim 1, wherein the salt is a pharmaceutically acceptable salt thereof, together with at least one other therapeutically active agent.

3. A pharmaceutical formulation comprising:

a) the compound of claim 1 or a salt thereof, wherein said salt is a pharmaceutically acceptable salt thereof; and

b) a pharmaceutically acceptable excipient.

4. The pharmaceutical formulation of claim 3 wherein the pharmaceutical formulation is a unit dosage form.

5. A compound having a structure which is:

6. A compound which is

7. A combination comprising a first therapeutically active agent which is the compound of claim 6 or a salt thereof, wherein the salt is a pharmaceutically acceptable salt thereof, together with at least one other therapeutically active agent.

8. A pharmaceutical formulation comprising:

a) the compound of claim 6 or a salt thereof, wherein said salt is a pharmaceutically acceptable salt thereof; and

b) a pharmaceutically acceptable excipient.

9. The compound of claim 6, which is

10. A combination comprising a first therapeutically active agent which is the compound of claim 9 or a salt thereof, wherein the salt is a pharmaceutically acceptable salt thereof, together with at least one other therapeutically active agent.

11. A pharmaceutical formulation comprising:

a) the compound of claim 9 or a salt thereof, wherein said salt is a pharmaceutically acceptable salt thereof; and

b) a pharmaceutically acceptable excipient.

12. A compound which is

13. A combination comprising a first therapeutically active agent which is the compound of claim 12, wherein the salt is a pharmaceutically acceptable salt thereof, together with at least one other therapeutically active agent.

14. A pharmaceutical formulation comprising:

a) the compound of claim 12, wherein said salt is a pharmaceutically acceptable salt thereof; and

b) a pharmaceutically acceptable excipient.

15. The compound of claim 12, which is

16. A combination comprising a first therapeutically active agent which is the compound of claim 15 or a salt thereof, wherein the salt is a pharmaceutically acceptable salt thereof, together with at least one other therapeutically active agent.

17. A pharmaceutical formulation comprising:

a) the compound of claim 15 or a salt thereof, wherein said salt is a pharmaceutically acceptable salt thereof; and

b) a pharmaceutically acceptable excipient.

18. A compound which is

19. A combination comprising a first therapeutically active agent which is the compound of claim 18 or a salt thereof, wherein the salt is a pharmaceutically acceptable salt thereof, together with at least one other therapeutically active agent.

20. A pharmaceutical formulation comprising:

a) the compound of claim 18 or a salt thereof, wherein said salt is a pharmaceutically acceptable salt thereof; and

b) a pharmaceutically acceptable excipient.

21. The compound of claim 18, which is

22. A combination comprising a first therapeutically active agent which is the compound of claim 21 or a salt thereof, wherein the salt is a pharmaceutically acceptable salt thereof, together with at least one other therapeutically active agent.

23. A pharmaceutical formulation comprising:

a) the compound of claim 21 or a salt thereof, wherein said salt is a pharmaceutically acceptable salt thereof; and

b) a pharmaceutically acceptable excipient.

24. A compound which is

25. A combination comprising a first therapeutically active agent which is the compound of claim 24 or a salt thereof, wherein the salt is a pharmaceutically acceptable salt thereof, together with at least one other therapeutically active agent.

26. A pharmaceutical formulation comprising:

a) the compound of claim 24 or a salt thereof, wherein said salt is a pharmaceutically acceptable salt thereof; and

b) a pharmaceutically acceptable excipient.

27. The compound of claim 24, which is

28. A combination comprising a first therapeutically active agent which is the compound of claim 27 or a salt thereof, wherein the salt is a pharmaceutically acceptable salt thereof, together with at least one other therapeutically active agent.

29. A pharmaceutical formulation comprising:

a) the compound of claim 27 or a salt thereof, wherein said salt is a pharmaceutically acceptable salt thereof; and

b) a pharmaceutically acceptable excipient.