Compounds affecting pigment production and methods for treatment of bacterial diseases

Patent metadata

Field	Value
Publication number	US-11040949-B2
Application number	US-202017006985-A
Country	US
Kind code	B2
Filing date	Aug 31, 2020
Priority date	Jul 21, 2017
Publication date	Jun 22, 2021
Grant date	Jun 22, 2021

Abstract

Provided herein are compounds, derivatives thereof, composition comprising one or more of said compounds and derivatives, and methods for prevention and/or treatment of microbial infections and/or related diseases or conditions. The present compounds and/or derivatives thereof can be represented by Formula (II):The present methods include administering to a subject an effective amount of one or more compounds of Formula (II). In one embodiment, said microbial infections are bacterial infections. More specifically, said bacterial infections are staphylococcal infections.

First claim

The invention claimed is:

1. A composition comprising one or more compounds having Formula (II):

and prodrugs thereof,
wherein R1 is selected from:

wherein R3 and R4 are independently or jointly selected from Br,
X is selected from N or C,
A is single bond or double bond, and
wherein R2 is selected from:

wherein R6 and R7 are independently or jointly selected from 0 or absent;
R8 and R9 are independently or jointly selected from the group consisting of heteroalkyl; aryl; heterocyclyl; cycloalkyl; cycloalkenyl; cycloalkynyl; and tetrahydroquinolinyl,
or R8 and R9 are optionally bonded together to form a four-, five-, or six-membered heterocyclyl, cycloalkenyl, or cycloalkyl, and
Z is selected from C or S.

2. The composition of claim 1 , wherein the composition is administered to reduce a virulence of bacteria causing microbial infections and/or related disease or conditions in a subject.

3. The composition of claim 1 , wherein the composition further comprises one or more pharmaceutical acceptable carrier, salt, ester, excipient, vehicle, solvent, diluent, or any combination thereof.

4. The composition of claim 1 , wherein the one or more compounds and/or prodrugs thereof are anti-virulent agents for bacteria.

5. The composition of claim 2 , wherein the microbial infections and/or related diseases or conditions comprise infections of the skin and soft tissue, bone and joint, surgical wound, indwelling devices, lung and heart valves.

6. The composition of claim 2 , wherein the microbial infections are bacterial infections.

7. The composition of claim 6 , wherein the bacterial infections comprise Staphylococcus sp. Infections.

8. The composition of claim 7 , wherein the Staphylococcus sp. comprises Staphylococcus aureus or methicillin-resistant Staphylococcus aureus.

9. The composition of claim 1 , wherein the composition inhibits biosynthesis of staphyloxanthin in the Staphylococcus aureus.

10. The composition of claim 1 , wherein the composition blocks pigments production in Staphylococcus aureus.

11. The composition of claim 2 , wherein said subject is a mammal.

12. The composition of claim 2 , wherein said subject is human.

13. The composition of claim 2 , wherein the composition is administered to the subject through oral pathways in one or more forms comprising capsule, tablet, granule, spray, and/or syrup.

14. The composition of claim 1 , wherein the composition increases sensitivity and/or susceptibility of microbes causing said microbial infections and/or related diseases or conditions to oxidation and neutrophil killing.

15. A composition comprising the following compound:

16. A composition comprising a compound selected from the group consisting of:

Assignees

• Versitech Ltd

Inventors

• Kao Yi Tsun Richard
• Gao Peng
• Li Xuechen
• Liu Ming

Classifications

• C07D215/58

  with hetero atoms directly attached to the ring nitrogen atom · CPC title

• A61P31/04 Primary

  Antibacterial agents · CPC title

• C07D295/08 Primary

  substituted by singly bound oxygen or sulfur atoms · CPC title

• A61K47/14

  Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters · CPC title

• A61K9/0095

  Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches (A61K9/0007 takes precedence; eatable gels or foams A61K9/0056; oral mucosa adhesive forms A61K9/006) · CPC title