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US 6,673,923 B2Granted
Pyrazole antimicrobial agents
AssigneeTularik Inc.
InventorsLeping Li, Xiaoqi Chen, Serena T. Cutler
Life of this patent
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Abstract
The present invention provides pyrazole and pyrazolone derivatives. Preferred compounds of the invention are useful as RNA polymerase inhibitors. Further preferred compounds of the invention are useful as antimicrobial agents.
Claims3
A compound having the formula
- wherein
- R1 is selected from the group consisting of H and OR′, wherein R′ is selected from the group consisitng of H and susbtituted or unsubstituted lower alkyl;
- and
- R2 is selected from the group consisting of
- wherein
- R7, R8 and R9 are independently selected from the group consisting of hydroxyl, halogen, nitro, cyano, substituted or unsubstituted (C1-C6)alkyl, (C1-C6)haloalkyl, substituted or unsubstituted (C1-C6)heteroalkyl, (C1-C6)alkoxy, (C1-C6)haloalkoxy, (C1-C6)alkylthio, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, alkanoyl, alkoxycarbonyl, alkylcarbamoyl, sulfonyl, sulfamoyl and NR4R5,
- wherein at least one of R7, R8 and R9 is NR4R5;
- wherein R4 and R5 are independently selected from the group consisting of hydrogen, substituted or unsubstituted (C1-C8)alkyl, substituted or unsubstituted (C1-C8)heteroalkyl, and one or more of R4 and R5 are substituted or unsubstituted (C3-C6)alkyl or substituted or unsubstituted (C3-C6)heteroalkyl combined with the nitrogen atom to which it is attached to form a four-, five-, six- or seven-membered ring optionally having additional substituents selected from substituted or unsubstituted (C1-C8)alkyl, substituted or unsubstituted (C1-C8)heteroalkyl and substituted or unsubstituted phenyl;
- wherein at least one of R4 and R5 is selected from the group consisting of(C1-C8)alkyl and (C1-C8)heteroalkyl, comprising a substituent selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocycloalkyl;
- and
- R3 is substituted or unsubstituted aryl.
8 more elements
Dependencies are inferred from the claim text.