Merck Sharp + Dohme Corp.

Lawrence Livermore National Security, LLC

Daniel Bensen

Junhu Zhang

Xiaoming Li

Zhiyong Chen

Leslie William Tari

Thanh To Lam

Michael Trzoss

John M Finn

Sergio E Wong

Felice C Lightstone

Suk Joong Lee

Toan B Nguyen

Michael E Jung

Douglas W Phillipson

Min Teng

John F Finn

Allen Borchardt

Christopher John Creighton

Mark Hilgers

Paul Aristoff

Voon Ong

Allen John Borchardt

Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. In addition, species of tricyclic gyrase inhibitors compounds are also disclosed herein. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.

Tricyclic Gyrase inhibitors

Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.

Tricyclic gyrase inhibitors

Novel gyrase inhibitors and related compositions and methods are useful for impeding bacterial growth. Compounds of Formula (I), are disclosed: Formula (I), wherein Y is N or CH; Z is N or CR; Ris H, a substituted or unsubstituted hydrocarbyl residue (1-3C) containing 0-2 heteroatoms selected from O, S and N, or is an inorganic residue; L is O, S, NR, or CRR; Ris H or Calkyl; Rand Rare each independently H or Calkyl; Ris H, a hydrocarbyl residue (1-40C) containing 0-10 heteroatoms selected from O, S and N optionally substituted with an inorganic residue; Ris H, an inorganic residue, or a hydrocarbyl residue (1-30C) containing 0-12 heteroatoms selected from O, S and N and containing 0-10 inorganic residues, wherein Rand Rtogether may join to form a fused ring; and Ris selected from the group consisting of H, Calkyl, Calkenyl, Calkynyl, halo Calkyl, halo Calkenyl, halo Calkynyl, Chydroxyalkyl, Calkyl chloride, Calkenyl chloride, and Calkynyl chloride; or a pharmaceutically-acceptable salt, ester, or prodrug thereof. 

Gyrase inhibitors

Novel gyrase inhibitors and related compositions and methods are useful for impeding bacterial growth. Compounds of Formula I are disclosed: 

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Carlsbad, CA, United States of America

Daniel Bensen