Rutgers, the State University of New Jersey

Provid Pharmaceuticals Inc.

Yon W Ebright

Richard H Ebright

David Degen

Yu Feng

Yu Zhang

Gary Olson

Christopher Self

Juan Shen

James Bacci

Anne-Cecile Hiebel

William Solvibile

Joel S Freundlich

Ricardo Gallardo-Macias

Richard Wilde

Shao-Gang Li

Shengjian Li

Soma Mandal

Chih-Tsung Lin

The invention provides salts of formula Ia, Ib, Ic, or Id: wherein variables are as described in the specification, as well as compositions comprising a salt of formula Ia-Id, methods of making such salts, and methods of using such salts as, e.g., inhibitors of bacterial RNA polymerase and as antibacterial agents.

Antibacterial agents: soluble salts and aqueous formulations of pyronins

The invention provides compounds of formula Ia, Ib, Ic, or as well as compositions comprising a compound of formula Ia-Id, methods of making such compounds, and methods of using such compounds, e.g., as inhibitors of bacterial RNA polymerase and as antibacterial agents.

Antibacterial agents: O-alkyl-deuterated pyronins

The invention provides compounds of formula (I) or (II) and tautomers and salts thereof, wherein variables are as described in the specification, as well as compositions comprising a compound of formula (I) or (II) or a tautomer or salt thereof, methods of making a compound of formula (I) or (II) or a tautomer or salt thereof, and methods of using a compound of formula (I) or (II) or a tautomer or salt thereof as, e.g., inhibitors of bacterial RNA polymerase or as antibacterial agents. 

Antibacterial agents: arylalkylcarboxamido phloroglucinols

The invention provides bipartite, dual-targeted inhibitors of bacterial RNA polymerase having the general structural formula (I): X-&#x3b1;-Y (I) wherein X is an moiety that binds to the Rif target of a bacterial RNA polymerase; Y is a moiety that binds to the bridge-helix N-terminus target of a bacterial RNA polymerase; and is a covalent bond or a linker. The invention also provides compositions comprising such compounds, methods of making such compounds, and methods of using said compounds. The invention has applications in control of bacterial gene expression, control of bacterial growth, antibacterial chemistry, and antibacterial therapy.

Antibacterial agents: dual-targeted RNA polymerase inhibitors

The invention provides bipartite inhibitors of bacterial RNA polymerase having the general structural formula (I):X-&#x3b1;-Y&#x2003;&#x2003;(I)wherein X is an moiety that binds to the rifamycin binding site of a bacterial RNA polymerase, Y is a moiety that binds to the GE23077 binding site of a bacterial RNA polymerase, and &#x3b1; is a linker. The invention also provides compositions comprising such compounds, methods of making such compounds, and methods of using said compounds. The invention has applications in control of bacterial gene expression, control of bacterial growth, antibacterial chemistry, and antibacterial therapy.

Bipartite inhibitors of bacterial RNA polymerase

The invention provides compounds having activity as bacterial RNA polymerase inhibitors and antibacterial agents, as well as compositions comprising the compounds and methods for their use. Specifically, phenylalanineamide and tyrosinamide compounds are disclosed that have inhibitory activity towardRNA polymerase. Use of these compounds in the treatment or prevention ofinfections in a mammal, is disclosed.

Antibacterial agents: N&#x3b1;-aroyl-N-aryl-phenylalaninamides

The invention provides compounds of formula (I): and salts thereof, wherein X and Y have any of the values defined herein. The compounds inhibit bacterial RNA polymerase, inhibit bacterial growth, and have applications in, analysis of RNA polymerase structure and function, control of bacterial gene expression, control of bacterial growth, antibacterial chemistry, antibacterial therapy, and drug discovery.

Antibacterial agents: salinamide derivatives

The invention provides compounds of formula Ia, Ib and Ic: and salts thereof, wherein variables are as described in the specification, as well as compositions comprising a compound of formula Ia-Ic, methods of making such compounds, and methods of using such compounds, e.g., as inhibitors of bacterial RNA polymerase and as antibacterial agents.

Antibacterial agents: aryl myxopyronin derivatives

The invention provides bipartite inhibitors of bacterial RNA polymerase having the general structural formula (I): X-&#x3b1;-Y (I) wherein X is an moiety that binds to the rifamycin binding site of a bacterial RNA polymerase, Y is a moiety that binds to the GE23077 binding site of a bacterial RNA polymerase, and is a linker. The invention also provides compositions comprising such compounds, methods of making such compounds, and methods of using said compounds. The invention has applications in control of bacterial gene expression, control of bacterial growth, antibacterial chemistry, and antibacterial therapy.

The invention provides compounds of formula la, lb and Ic: [Formula Ia, Ib, and Ic] and salts thereof, wherein variables are as described in the specification, as well as compositions comprising a compound of formula Ia-Ic, methods of making such compounds, and methods of using such compounds, e.g., as inhibitors of bacterial RNA polymerase and as antibacterial agents.

The invention provides compounds of formula (I):X-&#x3b1;-Y&#x2003;&#x2003;(I)wherein X, Y, and a have any of the values defined in the specification and salts thereof. The compounds are inhibitors of bacterial RNA polymerase.

Bipartite inhibitors of bacterial RNA polymerase: Sal-target-inhibitor/nucleoside-analog-inhibitor conjugates

The invention provides compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein R, R, R, R, R, and G are as described in the specification, as well as compositions comprising a compound of formula I, methods of making such compounds, and methods of using such compounds, e.g., as inhibitors of bacterial RNA polymerase and as antibacterial agents.

Antibacterial agents: sidechainfluorinated myxopyronin derivatives

The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein Ya, Yb, R1, R2, and G are as described in the specification, as well as compositions comprising a compound of formula (I). The compounds are useful as inhibitors of bacterial RNA polymerase and as antibacterial agents. 

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North Brunswick, NJ, United States of America

Yon W Ebright