Merck Sharp + Dohme Corp.

Lawrence Livermore National Security, LLC

Cidara Therapeutics, Inc.

Trius Therapeutics, Inc.

Thanh To Lam

Junhu Zhang

Xiaoming Li

Zhiyong Chen

Michael Trzoss

Leslie William Tari

Daniel Bensen

Allen Borchardt

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

Thomas P Brady

Zhi-Yong Chen

Leslie W Tari

Min Teng

Paul Aristoff

Wanlong Jiang

Quyen-Quyen Thuy Do

Voon Ong

Daniel C Bensen

Mark Stidham

Jason Cole

Les Tari

James M Balkovec

Lucy Aguirre Kohnen

Mark Cunningham

Alain Noncovich

Simon Doehrmann

Allen John Borchardt

Compositions and methods for the treatment of viral infections include conjugates containing inhibitors of viral neuraminidase (e.g., zanamivir, peramivir, or analogs thereof) linked to an Fc monomer, an Fc domain, and Fc-binding peptide, an albumin protein, or albumin-binding peptide. In particular, conjugates can be used in the treatment of viral infections (e.g., influenza viral infections).

Compositions and methods for the treatment of viral infections

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

Growing community of inventors

San Diego, CA, United States of America

Thanh To Lam