Merck Sharp + Dohme Corp.

Lawrence Livermore National Security, LLC

Trius Therapeutics, Inc.

Amplyx Pharmaceuticals, Inc.

Basilea Pharmaceutica International Ag, Allschwil

Michael Trzoss

Junhu Zhang

Xiaoming Li

Zhiyong Chen

Thanh To Lam

Leslie William Tari

Daniel Bensen

Michael E Jung

John M Finn

Sergio E Wong

Felice C Lightstone

Suk Joong Lee

Toan B Nguyen

John F Finn

Christopher John Creighton

Douglas W Phillipson

Mark Hilgers

Min Teng

Allen Borchardt

Jonathan A Covel

Peter J Webb

Paul Aristoff

Karen Joy Shaw

Voon Ong

Mark Stidham

Mark Cunningham

Les Tari

Lucy Aguirre Kohnen

Michael Jung

Felice Lightstone

Allen John Borchardt

John Finn

Described herein are heterocycle substituted pyridine derivative antifungal agents and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of fungal diseases and infections.

Heterocycle substituted pyridine derivative antifungal agents

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: 

The present disclosure provides compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R, Rand Z are as described herein. The disclosure also provides pharmaceutical compositions thereof; and methods for inhibiting DHFR activity; and methods for treating cell proliferative diseases, autoimmune disease, inflammatory disease or bacterial, fungal or parasitic infection by administering a compound of Formula I.

Dihydrofolate reductase inhibitors

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San Diego, CA, United States of America

Michael Trzoss