# US 9,751,898 B2 · Boron-containing small molecules

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 9,751,898 B2
- Document ID: US9751898B2
- Status: Granted
- Kind: B2
- Application number: 14/221,637
- Filed: 2014-03-21
- Published: 2014-10-23
- Granted: 2017-09-05
- Earliest claimed: 2010-09-07
- Assignees: Anacor Pharmaceuticals, Inc.
- Applicants: Anacor Pharmaceuticals, Inc.
- Inventors: Vincent S. Hernandez; Charles Ding; Jacob J. Plattner; Michael Richard Kevin Alley; Fernando Rock; Suoming Zhang; Eric Easom; Xianfeng Li; Ding Zhou
- Web page: https://patentgrep.com/patent/US9751898B2

## CPC

- C07F 5/025: {Boronic and borinic acid compounds}
- A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P 31/04: Antibacterial agents
- A61P 31/06: for tuberculosis
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07F: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM (metal-containing porphyrins C07D487/22)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

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

## Claims

### Claim 1

A compound having a structure which is:
wherein R3 is CH2NH2;
R4 is bromine;
Y is O; and
R5 is methyl;
C* is a carbon atom stereocenter which has a configuration which is (S) or a salt, hydrate or solvate thereof.

### Claim 2 (depends on 1)

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.

### Claim 3 (depends on 1)

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

### Claim 4 (depends on 1)

A pharmaceutical formulation comprising:
a) the compound of claim 1, or a pharmaceutically acceptable salt thereof; and
b) a pharmaceutically acceptable excipient.

### Claim 5 (depends on 1)

A method of inhibiting LeuRS, comprising: contacting the LeuRS with the compound of claim 1, thereby inhibiting the LeuRS.

### Claim 6 (depends on 1)

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.

### Claim 7 (depends on 1)

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.

### Claim 8 (depends on 7)

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