Boron-containing small molecules

Patent metadata

Field	Value
Publication number	US-9751898-B2
Application number	US-201414221637-A
Country	US
Kind code	B2
Filing date	Mar 21, 2014
Priority date	Sep 7, 2010
Publication date	Sep 5, 2017
Grant date	Sep 5, 2017

Abstract

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

First claim

What is claimed is:

1. A compound having a structure which is:

wherein R 3 is CH 2 NH 2 ;
R 4 is bromine;
Y is O; and
R 5 is methyl;
C* is a carbon atom stereocenter which has a configuration which is (S) or a salt, hydrate or solvate thereof.

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.

Assignees

• Anacor Pharmaceuticals Inc

Inventors

• Hernandez Vincent S
• Ding Charles
• Plattner Jacob J
• Alley Michael Richard Kevin
• Rock Fernando
• Zhang Suoming
• Easom Eric
• Li Xianfeng
• Zhou Ding

Classifications

• A61P31/06

  for tuberculosis · CPC title

• A61P31/04

  Antibacterial agents · CPC title

• A61P31/00

  Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• C07F5/025 Primary

  Boronic and borinic acid compounds · CPC title