# US 2008/0188535 A1 · Modulation of pathogenicity

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

- Number: US 2008/0188535 A1
- Document ID: US20080188535A1
- Status: Published application
- Kind: A1
- Application number: 12/005,780
- Filed: 2007-12-28
- Published: 2008-08-07
- Earliest claimed: 2002-03-08
- Inventors: Aldo Ammendola; Katharina Aulinger-Fuchs; Astrid Gotschlich; Bernd Kramer; Martin Lang; Wael Saeb; Udo Sinks; Andreas Wuzik
- Web page: https://patentgrep.com/patent/US20080188535A1

## CPC

- A01N 43/54: 1,3-Diazines; Hydrogenated 1,3-diazines
- A01N 43/56: 1,2-Diazoles; Hydrogenated 1,2-diazoles
- A61K 8/49: containing heterocyclic compounds
- A61K 8/4973: {with oxygen as the only hetero atom}
- A61K 8/4986: {with sulfur as the only hetero atom}
- A61K 31/175: having the group [IMAGE cpc-sch-A61K-0950.gif] , >N—C(O)—N=N— or[IMAGE cpc-sch-A61K-0951.gif] , e.g. carbonohydrazides, carbazones, semicarbazides, semicarbazones; Thioanalogues thereof
- A61K 31/38: having sulfur as a ring hetero atom
- A61K 31/415: 1,2-Diazoles
- A61K 31/42: Oxazoles
- A61K 31/435: having six-membered rings with one nitrogen as the only ring hetero atom
- A61K 31/44: Non condensed pyridines; Hydrogenated derivatives thereof
- A61K 31/445: Non condensed piperidines, e.g. piperocaine
- A61K 31/505: Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61P 31/04: Antibacterial agents
- A61Q 17/005: {Antimicrobial preparations}
- A61Q 19/00: Preparations for care of the skin
- C07D 231/16: Halogen atoms or nitro radicals
- C07D 231/40: Acylated on said nitrogen atom
- C07D 307/68: Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
- C07D 333/38: Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D 333/70: attached in position 2
- C07D 403/12: linked by a chain containing hetero atoms as chain links
- C07D 409/04: directly linked by a ring-member-to-ring-member bond
- C07D 409/12: linked by a chain containing hetero atoms as chain links
- C07D 471/04: Ortho-condensed systems
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- A01N: PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF (preservation of food or foodstuff A23); BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES (preparations for medical, dental or toiletry purposes which kill or prevent the growth or proliferation of unwanted organisms A61K); PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

The present invention relates to the use of compounds of the general Formula (I): wherein in Formula (I), R is H, alkyl, cycloalkyl, aryl or heteroaryl; R1 is H, alkyl, cycloalkyl, aryl or heteroaryl; R2 is H, alkyl, cycloalkyl, aryl or heteroaryl; A1 and A2 each independently represent an optionally substituted C1-C20-alkyl group which may contain one or more group(s) Z, or a monocyclic or polycyclic optionally substituted aromatic or non-aromatic ring system which may contain one or more group(s) X, and in case of a polycyclic ring system, said system contains at least one aromatic ring; Z is selected from the group consisting of S, O, N, NR4, CO, CO2, CS, SO or SO2 X is selected from the group consisting of S, O, N, NR4, SO or SO2;

## Claims

### Claim at position 1

1-26. (canceled)

### Claim 27

A compound of Formula (I)
or a pharmaceutically acceptable salt or physiologically functional derivative thereof, wherein
A1 is pyrazolyl, which may be optionally substituted with one or more R3;
p is 0;
Y1 is C(O) or C(S);
R1 is H or alkyl, cycloalkyl, aryl, or heteroaryl, each of which may be optionally substituted with one or more R3;
n is 0;
A2 is heteroaryl, optionally substituted with one or more R3;
each R3 independently is OR4, SR4, hydroxyalkyl, hydroxyalkylamino, cycloalkyl, halogen, haloalkyl, haloalkoxy, NO2, CN, SO2NR4R5, CO2NR4R5, COR4, CO2R4, SO2R4, SO3R4, NR4R5, alkyl, aryl, aryl substituted with halogen, or heteroaryl;
each R4 independently is H, alkyl, cycloalkyl, aryl, or heteroaryl; and
each R5 independently is H, O-alkyl, O-aryl, alkyl, heteroaryl, or aryl.

### Claim 28 (depends on 27)

The compound of claim 27 wherein A2 is pyrazolyl, which is optionally substituted with one or more R3.

### Claim 29 (depends on 28)

The compound of claim 28 wherein A2 is pyrazolyl, which is N-substituted with alkyl.

### Claim 30 (depends on 27)

The compound of claim 27 wherein A1 is
wherein a is 0, 1, 2, or 3.

### Claim 31 (depends on 30)

The compound of claim 30 wherein a is 2 or 3.

### Claim 32 (depends on 31)

The compound of claim 31 wherein A1 is

### Claim 33 (depends on 27)

The compound of claim 27 wherein Y1 is C(O).

### Claim 34 (depends on 27)

The compound of claim 27 wherein R1 is H.

### Claim 35

A compound selected from:
or a pharmaceutically acceptable salt or physiologically acceptable derivative thereof.

### Claim 36 (depends on 27)

A method for inhibiting the production of a virulence factor comprising contact with a compound of claim 27.

### Claim 37 (depends on 35)

A method for inhibiting the production of a virulence factor comprising contact with a compound of claim 35.

### Claim 38 (depends on 36)

The method of claim 36 for the treatment or prevention of bacterial damage or disease.

### Claim 39 (depends on 37)

The method of claim 37 for the treatment or prevention of bacterial damage or disease.

### Claim 40 (depends on 38)

The method of claim 38 wherein the bacteria is Pseudomonas aeruginosa or Burkholderia cepacia.

### Claim 41 (depends on 39)

The method of claim 39 wherein the bacteria is Pseudomonas aeruginosa or Burkholderia cepacia.

### Claim 42 (depends on 27)

A composition for inhibiting biofilm formation comprising a compound of claim 27.

### Claim 43 (depends on 35)

A composition for inhibiting biofilm formation comprising a compound of claim 35.