Broad spectrum antivirulence, anti-persistence compounds
AssigneesThe General Hospital Corporation, Aptuit (Verona) SRL, An Evotec Company
InventorsLaurence Rahme, Francois Lepine, Damien Maura, Carmela Napolitano, Antonio Felici, Michele Negri, Stefano Fontana, Daniele Andreotti
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Abstract
The present application provides malonamide compounds, and derivatives thereof (e.g., N-aryl malonamides (NAM), acetamides, oxalamides, and the like), that are useful, for example, for the treatment of acute, chronic/persistent, and/or relapsing infections. Pharmaceutical compositions, methods of treating diseases (e.g., bacterial infections), and methods of reducing bacterial virulence are also provided.
Claims14
A compound selected from any one of the following compounds:
- or a pharmaceutically acceptable salt thereof, wherein:
- Z1 is selected from the group consisting of O and S;
- L1 is selected from the group consisting of methylene, methylmethylene, fluoromethylmethylene, fluoromethylene, difluoromethylene, and aminomethylene;
- L2 is selected from the group consisting of NRN1C(O) and NRN1C(S);
- RN1 and RN2 are each independently selected from the group consisting of H and C1-4 alkyl;
- each R1 is independently selected from the group consisting of C1-4 haloalkyl, halo, CN, NO2, NH2, —COOH, —CONH2, and OH;
- and
- each R2 is independently selected from the group consisting of halo, CN, NH2, —COOH, —CONH2, —C(O)C1-4 haloalkyl, —NHC(O)C1-4 haloalkyl, —NHSO2-C1-4 alkyl, and phenoxy;
- wherein either R1 is CN or R2 is CN or phenoxy;
- and
- wherein the compound of Formula I is not:
A compound of formula:
- or a pharmaceutically acceptable salt thereof.
A compound selected from:
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.