Rutgers, the State University of New Jersey

Other

Provid Pharmaceuticals Inc.

Bioarray Solutions Ltd.

Richard H Ebright

Yon W Ebright

David Degen

Juan Shen

Yu Feng

Konstantin Severinov

Yu Zhang

Gary Olson

Christopher Self

Joel S Freundlich

Anne-Cecile Hiebel

William Solvibile

James Bacci

Michael Seul

Ekaterina Semenova

Katherine Y Ebright

Dongye Wang

Jayanta Mukhopadhyay

Olga Pavlova

Nisha Mittal

Soma Mandal

Elena Sineva

Richard Wilde

Chih-Tsung Lin

Ricardo Gallardo-Macias

Mark Jaskowski

Shengjian Li

Shao-Gang Li

P Shannon Pendergrast

Y W Ebright

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 a compound of formula (I): or a salt thereof, wherein R-Rhave any of the values described in the specification, as well as compositions comprising a compound of formula (I). The compounds are useful as RNA polymerase inhibitors and antibacterial agents. 

Arylpropionyl-triketone antibacterial agents

The invention provides compounds that are inhibitors of bacterial RNA polymerase. 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.

Inhibitors of bacterial RNA polymerase: arylpropanoyl, arylpropenoyl, and arylcyclopropanecarboxyl phloroglucinols

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

A method and apparatus for the physico-chemical encoding of a collection of beaded resin ('beads') to determine the chemical identity of bead-anchored compounds by in-situ interrogation of individual beads. The present invention provides method and apparatus to implement color-coding strategies in applications and including the ultrahigh-throughput screening of bead-based combinatorial compounds libraries as well as multiplexed diagnostic and environmental testing and other biochemical assays.

Color-encoding and in-situ interrogation of matrix-coupled chemical compounds

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

It has been determined that co-administration of a rifamycin and a switch-region inhibitor 1) results in synergistic antibacterial effects, enabling efficacy at low, subtoxic doses, and/or 2) results in a low spontaneous resistance frequency, enabling treatment of high-titer infections without treatment failure due to spontaneous resistance. Accordingly, certain embodiments provide a composition comprising a rifamycin and a switch region inhibitor, as well as methods of use thereof.

Antibacterial agents: combination of a rifamycin and a switch region inhibitor

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 a compound of formula I: or a salt thereof, wherein R-Rhave any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful as antibacterial agents.

Antibacterial agents: phloroglucinol 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.

Growing community of inventors

New Brunswick, NJ, United States of America

Richard H Ebright