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US 11,555,010 B2Granted
Diamide antimicrobial agents
AssigneesBrown University, Bryant University
InventorsAmit Basu, Christopher W. Reid, Nola Camille Iwasaki, Joseph Prete
Life of this patent
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Abstract
This invention is directed to compounds of Formula (I) pharmaceutically acceptable salts, esters, and prodrugs thereof, to their preparation, to pharmaceutical compositions comprising compounds of Formula I, and to their uses as antimicrobial agents.
Claims19
A compound of Formula I
- wherein:
- R1 represents aryl, wherein aryl is substituted with 1 to 3 substituents selected from a group consisting of H, —X, S(C1-6 alkyl), O(C1-6 alkyl), and CX3;
- R2 is selected from the group consisting of C1-C8 alkyl, C3-C8 cycloalkyl, C3-C8 hetero cycloalkyl, and polyethyleneglycol, wherein each of said R2 groups are independently substituted with 1-3 substituents selected from a group consisting of C1-C6 alkyl, H, C1-C6 alkenyl, (CH2—O—(CH2)1-4)6—OH, C1-C6 alkynyl, OH, O(C1-C6 alkyl), F, Cl, Br, I, NO2, —C(═O)H, —C(═O)OH, —C(═O)O(C1-C6 alkyl), —C(═O)NH2, —C(═O)NH(C1-C6 alkyl), and —C(═O)N(C1-C6 alkyl)(C1-C6 alkyl);
- R3 is selected from a group consisting of C1-6 alkyl-NH2, CH(CH3)—NH2, CH(CH2CH2CH3)—NH2, CH(CH2CH2CH2CH3)—NH2, (CH2)0-3— C3-C8 hetero cycloalkyl wherein each R3 group is independently substituted with 1-3 substituents independently selected from a group consisting of H, C1-C6 alkyl, OH, O(C1-C6 alkyl), F, Cl, Br, I, NO2, —C(═O)H, —C(═O)OH, —C(═O)O(C1-C6 alkyl), —C(═O)NH2, —C(═O)NH(C1-C6 alkyl), and —C(═O)N(C1-C6 alkyl)(C1-C6 alkyl);
- R4 is selected from the group consisting of C1-C6 alkyl, C3-C8 cycloalkyl, arylalkyl, and heteroaryl-alkyl, wherein each of the R4 groups is independently substituted with 1-3 substituents independently selected from the group consisting of C1-C6 alkyl, H, OH, O(C1-C6 alkyl), F, Cl, Br, I, NO2, —C(═O)H, —C(═O)OH, —C(═O)O(C1-C6 alkyl), —C(═O)NH2, —C(═O)NH(C1-C6 alkyl), and —C(═O)N(C1-C6 alkyl)(C1-C6 alkyl);
- R5 is H or methyl;
- and
- X is selected from Cl, I, Br, and F.
5 more elements
Dependencies are inferred from the claim text.