Other

Pliva D.d.

Carlos H Faerman

Emanuele Perola

Manuel A Navia

Patrick Raymond Connelly

Lovorka Swenson

James P Griffith

Kumkum Saxena

Salvatore Anthony Marchese

Andrew Magee

Judith A Lippke

Scott T Moe

Paul Will

Michael Andrew Wynn

James Roger Black

Fan Lu

Paul J Ala

Janid A Ali

Jacob J Clement

Christopher Faraday

John V Gazzaniga

The invention relates to FMS-like tyrosine kinase (FLT3), FLT3 binding pockets or FLT3-like binding pockets. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to FMS-like tyrosine kinase protein, complexes of FMS-like tyrosine kinase protein, homologues thereof, or FLT-3-like protein or protein complexes. The invention also relates to crystallizable compositions and crystals comprising an FMS-like tyrosine kinase cytoplasmic domain or homologues thereof. The invention also relates to methods of identifying inhibitors of the cytoplasmic domain of FMS-like tyrosine kinase protein.

Crystal structure of FMS-like tyrosine kinase

The invention relates to D-Ala-D-Ala ligase inhibitors having the formula: wherein Ris NH; Ris NH; Ris selected from hydrogen, alkyl, amino, hydroxy, alkoxy, and alkylamino; and Rand Rare each independently hydrogen or a substituted or unsubstituted, linear, branched, or cyclic, alkyl, alkenyl, alkynyl, aryl, acyl, aralkyl, or alkaryl group wherein one or more carbon or hydrogen atoms may be substituted by a substituent selected from amino, alkylamino, hydroxyl, alkoxyl, thio, halogen, nitro, and carbonyl; wherein NRRincorporates a substituted or unsubstituted naphthyl group, wherein the substituents are selected from alkoxy, halogen, alkyl, and alkylene, and wherein said naphthyl group in NRRis bonded to N through a substituted or unsubstituted alkylene moiety. These compounds have antibacterial properties based on their ability to bind and inhibit D-Ala-D-Ala ligase, a critical pathway enzyme in bacterial cell-wall synthesis, and are suitable for various antibacterial uses.

Heterocyclic compounds and uses thereof as D-alanyl-D-alanine ligase inhibitors

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Acton, MA, United States of America

Carlos H Faerman