Merck Sharp + Dohme Corp.

Lawrence Livermore National Security, LLC

Halozyme, Inc.

Kumquat Biosciences Inc.

Forge Therapeutics, Inc.

Warner-lambert Company

Trius Therapeutics, Inc.

Blacksmith Medicines, Inc.

Chinese Academy of Sciences

Ii-vi Incorporated

Xiaoming Li

Zhiyong Chen

Junhu Zhang

Thanh To Lam

Michael Trzoss

Leslie William Tari

Daniel Bensen

Min Teng

Michael E Jung

John M Finn

Sergio E Wong

Curtis B Thompson

Felice C Lightstone

Suk Joong Lee

Toan B Nguyen

Yi Liu

Pingda Ren

Gregory Ian Frost

David Thomas Puerta

John F Finn

Baogen Wu

Douglas W Phillipson

Baskar Nammalwar

Christopher John Creighton

Mark Hilgers

Harold Michael Shepard

Liansheng Li

Allen Borchardt

Holly Atton

Ian Yule

Serge Convers-Reignier

Adele Faulkner

Michelle Southey

Christian Perez

Paul Aristoff

Alastair Parkes

Siling Zhao

H Michael Shepard

Giovanni Barbarossa

Wen-Qing Xu

Louis Howard Bookbinder

Elgin E Eissler

Xiuwen Zhu

Robert Patrick Wardlaw

Yaxia Yin

Shailesh Patkar

Konstantin Taganov

Shuaifeng Zhang

Bogdan Roman Krasnowski

Yu-Guo Guo

Robert Arnold Brack

Yancheng Zhang

Voon Ong

Shaosong Chu

Mark Stidham

Kraig M Yager

Zhimin Zhu

Mysore Ramprasad

Mark Cunningham

Lucy Aguirre Kohnen

Les Tari

Krzysztof Appelt

Xiangzhu Wang

Curtis Thompson

Allen John Borchardt

Chyau Tzeng

Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds that are useful for inhibiting the growth of gram-negative bacteria. Furthermore, the subject compounds and compositions are useful for the treatment of bacterial infection, such as urinary tract infection and the like.

Antibacterial compounds

The present disclosure provides compounds and pharmaceutically acceptable salts thereof, and methods of using the same. The compounds and methods have a range of utilities as therapeutics, diagnostics, and research tools. In particular, the subject compositions and methods are useful for reducing signaling output of oncogenic proteins.

Heterocyclic compounds and uses thereof

The present disclosure provides compounds and pharmaceutically acceptable salts thereof, and methods of using the same. The compounds and methods have a range of utilities as therapeutics, diagnostics, and research tools. In particular, the subject compositions and methods are useful for reducing signaling output of certain oncogenic proteins.

The present disclosure provides compounds represented by Formula (I-1): and pharmaceutically acceptable salts thereof, and methods of using the same. The compounds and methods have a range of utilities as therapeutics, diagnostics, and research tools. In particular, the subject compositions and methods are useful for reducing signaling output of oncogenic proteins.

Substituted pyrido[2,3-d]pyrimidines as inhibitors of Ras pathway signaling

Provided herein are heterocyclic derivative compounds of Formula (II), and pharmaceutical compositions comprising said compounds that are useful for inhibiting the growth of gram-negative bacteria. Furthermore, the subject compounds and compositions are useful for the treatment of bacterial infection, such as urinary tract infection and the like. 

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

Provided herein are methods for ameliorating an adverse effect of systemic administration of a PEG hyaluronan degrading enzyme to a subject. The methods involve systemically administering a PEGylated hyaluronan degrading enzyme, particularly a PEGylated hyaluronidase, such as any of the animal or bacterial hyaluronidases, to the subject and administering an amount of a corticosteroid sufficient to ameliorate the adverse effect. Also provided are method of treating a hyaluronan-associated disease or condition for single-agent therapy or combination therapy.

Adverse side-effects associated with administration of an anti-hyaluronan agent and methods for ameliorating or preventing the side-effects

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: 

Provided are compositions and formulations or co-formulations containing a hyaluronan degrading enzyme. The compositions, formulations or co-formulations can also contain another therapeutic agent, such as one that is suitable for treatment of Benign Prostatic Hyperplasia, for example, a 5-alpha reductase inhibitor. The compositions and formulations can be used for the treatment of Benign Prostatic Hyperplasia. The compositions and formulations can be provided in combinations with one or more other agents for the treatment of Benign Prostatic Hyperplasia.

Composition and lipid formulation of a hyaluronan-degrading enzyme and the use thereof for treatment of benign prostatic hyperplasia

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San Diego, CA, United States of America

Xiaoming Li