Modulation of Pathogenicity
OwnerAldo Ammendola, Katharina Aulinger-Fuchs +6inventors
InventorsAldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
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Abstract
The present invention relates to the use of compounds of the general Formula (XIII): In particular the invention refers to a family of compounds that block the quorum sensing system of Gram-negative bacteria, a process for their manufacture, pharmaceutical compositions containing them and to their use for the treatment and prevention of microbial damages and diseases, in particular for diseases where there is an advantage in inhibiting quorum sensing regulated phenotypes of pathogens.
Claims24
A compound of Formula XIII, or a pharmaceutically acceptable derivative thereof:
- wherein
- A7 is independently C═O, C═S, SO2, CH—OR13, C═NR12, or CH2—CHOR13;
- A8 is independently C(R14)2, O, S, or NR12;
- A9 is independently C═O, C═S, SO2, CH—OR13, C═NR12, or CH2—CHOR13;
- m is 0, or 1;
- q is 0, or 1;
- r is 0, or 1;
- R12 is independently H, CH3, CH2—CH3, C6H5, OCH3, OCH2—CH3, OH, SH or aryl group;
- R13 is independently H, CH3, or CH2—CH3;
- R14 is independently H, alkyl, alkoxy, OH, or SH;
- A5 is a C3-C16 alkyl group optionally substituted by one or more substituents R3;
- or A5 is an aryl ring which may be substituted by one or more substituents R8, R8′ or R9,
- A6 is an aryl ring which may be substituted by one or more substituents R8, R8′ or R9,
- R3 is independently OR4, SR4, hydroxyalkyl, hydroxyalkylamino, cycloalkyl, halogen, haloalkyl, haloalkyloxy, NO2, CN, SO2NR4R5, CONR4R5, COR4, CO2R4, SO2R4, SO3R4, NR4R5, alkyl, or aryl;
- R4 is H, alkyl, cycloalkyl, aryl or heteroaryl;
- R5 is H, alkyl, aryl or heteroaryl, O-alkyl, O-aryl, or O-heteroaryl;
- and
- R8, R8′, R9 is independently methyl, ethyl, t-butyl, CN, halogen, haloalkoxy, haloalkyl, OH, alkoxy, NR4R5, or COOR4.
Dependencies are inferred from the claim text.