# US 2018/0021277 A1 · Anti-virulence compositions and methods

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- Number: US 2018/0021277 A1
- Document ID: US20180021277A1
- Status: Published application
- Kind: A1
- Application number: 15/719,914
- Filed: 2017-09-29
- Published: 2018-01-25
- Earliest claimed: 2012-10-12
- Assignees: Case Western Reserve University
- Applicants: Case Western Reserve University
- Inventors: Menachem Shoham; Rajesh Viswanathan; Guanping Yu
- Web page: https://patentgrep.com/patent/US20180021277A1

## CPC

- A61K 31/192: having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid {(cannabinoids A61K31/658)}
- A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)}
- A61K 31/12: Ketones
- A61K 31/235: having an aromatic ring attached to a carboxyl group
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

A method of treating a bacterial infection in a subject in need thereof includes administering to the subject an AgrA antagonist.

## Claims

### Claim 1

A method of treating a bacterial infection in a subject in need thereof, the method comprising:
administering to the subject a compound having the formula:
wherein R3 is selected from the group consisting of substituted or unsubstituted 5C3-C6 alkyl; R4 is selected from the group consisting of halo, nitro, substituted or unsubstituted C1-C6 alkyl, C3-C20 aryl, COOH, OCH3, and COOCH3, p is an integer from 0-5; and pharmaceutically acceptable salts thereof.

### Claim 2 (depends on 1)

The method of claim 1, wherein R3 is selected from the group consisting of 5-Pr, and 5-Hexyl; R4 is selected from the group consisting of F, Cl, Br, I, NO2, Me, i-Pr, Ph, COOH, t-Bu, OCH3, and COOCH3; wherein p is an integer from 0-5; and pharmaceutically acceptable salts thereof.

### Claim 3 (depends on 1)

The method of claim 1, wherein the compound is provided in a topical composition with a pharmaceutically acceptable carrier and administered to the bacterial infection of the subject topically.

### Claim 4 (depends on 1)

The method of claim 1, further comprising administering an antibiotic to the bacteria.

### Claim 5 (depends on 1)

The method of claim 1, wherein the compound is administered at an amount to effective to inhibit biofilm formation of the bacteria.

### Claim 6 (depends on 1)

The method of claim 1, wherein the compound has the formula (4f):
wherein R10 is selected from F, Cl, Br, I, NO2, Me, i-Pr, Ph, COOH, t-Bu, OCH3, and COOCH3; p is an integer from 0-5, and pharmaceutically acceptable salts thereof.

### Claim 7 (depends on 1)

The method of claim 1, wherein the compound has a formula selected from the group consisting of:
and pharmaceutically acceptable salts thereof.

### Claim 8 (depends on 1)

The method of claim 1, wherein the compound has a formula selected from the group consisting of:
and pharmaceutically acceptable salts thereof.

### Claim 9 (depends on 1)

The method of claim 1, wherein the bacteria is methicillin-resistant Staphylococcus aureus.

### Claim 10

A method of inhibiting biofilm formation of bacteria, the method comprising:
administering to the bacteria a compound having the formula:
wherein R3 is selected from the group consisting of substituted or unsubstituted 5C3-C6 alkyl; R4 is selected from the group consisting of halo, nitro, substituted or unsubstituted C1-C6 alkyl, C3-C20 aryl, COOH, OCH3, and COOCH3, p is an integer from 0-5; and pharmaceutically acceptable salts thereof.

### Claim 11 (depends on 10)

The method of claim 10, wherein R3 is selected from the group consisting of 5-Pr, and 5-Hexyl; R4 is selected from the group consisting of F, Cl, Br, I, NO2, Me, i-Pr, Ph, COOH, t-Bu, OCH3, and COOCH3; wherein p is an integer from 0-5; and pharmaceutically acceptable salts thereof.

### Claim 12 (depends on 10)

The method of claim 10, wherein the compound is provided in a topical composition with a pharmaceutically acceptable carrier and administered to the bacteria topically.

### Claim 13 (depends on 10)

The method of claim 10, further comprising administering an antibiotic to the bacteria.

### Claim 14 (depends on 10)

The method of claim 10, wherein the compound has the formula (4f):
wherein R10 is selected from F, Cl, Br, I, NO2, Me, i-Pr, Ph, COOH, t-Bu, OCH3, and COOCH3; p is an integer from 0-5, and pharmaceutically acceptable salts thereof.

### Claim 15 (depends on 10)

The method of claim 10, wherein the compound has a formula selected from the group consisting of:
and pharmaceutically acceptable salts thereof.

### Claim 16 (depends on 10)

The method of claim 10, wherein the compound has a formula selected from the group consisting of:
and pharmaceutically acceptable salts thereof.

### Claim 17 (depends on 10)

The method of claim 10, wherein the bacteria is methicillin-resistant Staphylococcus aureus.