Boron-containing small molecules

• US 9,751,898 B2
• Filed: 03/21/2014
• Issued: 09/05/2017
• Est. Priority Date: 09/07/2010
• Status: Active Grant

• Current Assignee: Anacor Pharmaceuticals, Inc. (Pfizer Inc.)
• Original Assignee: Anacor Pharmaceuticals, Inc. (Pfizer Inc.)
• Inventors: Hernandez, Vincent S., Ding, Charles, Plattner, Jacob J., Alley, Michael Richard Kevin, Rock, Fernando, Zhang, Suoming, Easom, Eric, Li, Xianfeng, Zhou, Ding
• Primary Examiner(s): Pihonak, Sarah
• Assistant Examiner(s): Deck, Jason A
• Application Number:
  US14/221,637
• Publication Number:
  US 20140315860A1
• Time in Patent Office: 1,264 Days
• CPC Class Codes: A61P 31/00 Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• CPC Class Codes: A61P 31/04 Antibacterial agents
• CPC Class Codes: A61P 31/06 for tuberculosis
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: C07F 5/025 Boronic and borinic acid compounds

Abstract

This invention relates to, among other items, benzoxaborole compounds and their use for treating bacterial infections.

Claims

1. A compound having a structure which is:

2. A composition comprising:

a) a first stereoisomer of the compound of claim 1;

b) at least one additional stereoisomer of the first stereoisomer;

wherein the first stereoisomer is present in an enantiomeric excess of at least 80% relative to said at least one additional stereoisomer.

3. A combination comprising the compound of claim 1, or a pharmaceutically acceptable salt thereof, together with at least one other therapeutically active agent.

4. A pharmaceutical formulation comprising:

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

b) a pharmaceutically acceptable excipient.

5. A method of inhibiting LeuRS, comprising:

contacting the LeuRS with the compound of claim 1, thereby inhibiting the LeuRS.

6. A method of killing and/or preventing the growth of Mycobacterium tuberculosis comprising:

contacting the Mycobacterium tuberculosis with an effective amount of the compound of claim 1, thereby killing and/or preventing the growth of the Mycobacterium tuberculosis.

7. A method of treating and tuberculosis in an animal, comprising:

administering to the animal a therapeutically effective amount of the compound of claim 1, or a pharmaceutically-acceptable salt thereof, thereby treating and/or preventing the tuberculosis.

8. The method of claim 7, wherein the animal is a human.