IP Library Patent Application 15685846
Patent Application
App. No. 15/685,846

BORON-CONTAINING SMALL MOLECULES

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Quick Facts
Patent No.
US None
App. No.
15/685,846
Abstract

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

Claims (29)

1 . A compound having a structure which is:

wherein R 3 is —CH 2 NH 2 ;

R 4 is selected from the group consisting of halogen, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy, and sec-butoxy;

Y is O; and

R 5 is

wherein a is 2, 3 or 4;

R 10 and R 11 is H; and

R 12 is selected from the group consisting of H, OH, NH 2 , methyl, ethyl, —NHS(O) 2 CH 3 , cyano, —NHC(O)CH 3 , —NHC(O)NHCH 2 CH 3 , —C(O)NH 2 , —C(O)OH, 4-(methoxy)phenyl, benzyl, benzoxy, —NHC(O)OCH 2 Ph, —C(O)NHCH 2 CH 2 OH and —C(NH 2 )(NH);

or a salt, hydrate or solvate thereof.

2 . The compound of claim 1 or a salt, hydrate or solvate thereof, having a structure which is:

wherein C* is a carbon atom stereocenter which has a configuration which is (R) or (S).

3 . The compound of claim 2 or a salt, hydrate or solvate thereof, wherein the C* stereocenter is in a (S) configuration.

4 . The compound of claim 1 or a salt, hydrate or solvate thereof, wherein R 4 is selected from the group consisting of fluorine, chlorine, bromine, and iodine.

5 . The compound of claim 1 or a salt, hydrate or solvate thereof, wherein R 4 is selected from the group consisting of methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl.

6 . A composition comprising:

a) a first stereoisomer of the compound of claim 3 or a salt, hydrate or solvate thereof,

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.

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

8 . A pharmaceutical formulation comprising:

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

b) a pharmaceutically acceptable excipient.

9 . A method of inhibiting the editing domain of a t-RNA synthetase, comprising: contacting the synthetase with an effective amount of a compound of claim 1 , or a pharmaceutically-acceptable salt thereof, thereby inhibiting the synthetase.

10 . The method of claim 9 , wherein the t-RNA synthetase is LeuRS.

11 . A method of killing and/or preventing the growth of a microorganism, comprising: contacting the microorganism with an effective amount of the compound of claim 1 , thereby killing and/or preventing the growth of the microorganism.

12 . The method of claim 11 , wherein the microorganism is Mycobacterium tuberculosis.

13 . A method of treating and/or preventing a disease 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 disease.

14 . The method of claim 13 , wherein the disease is tuberculosis

15 . The method of claim 13 , wherein the animal is a human.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 24, 2017
From: HERNANDEZ, VINCENT S.; DING, CHARLES; PLATTNER, JACOB J.; ALLEY, MICHAEL RICHARD KEVIN; ROCK, FERNANDO; ZHANG, SUOMING; EASOM, ERIC; LI, XIANFENG; ZHOU, DING
To: ANACOR PHARMACEUTICALS, INC.
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