Merck Sharp + Dohme Corp.

Pfizer Corporation

Agouron Pharmaceuticals, Inc.

Lawrence Livermore National Security, LLC

Trius Therapeutics, Inc.

Standard LLC

Tiger Pharmatech

Raythera, Inc.

Pfizer Products Inc.

Junhu Zhang

Xiaoming Li

Zhiyong Chen

Thanh To Lam

Michael Trzoss

Michael Bruno Plewe

Leslie William Tari

Daniel Bensen

Hai Wang

Michael E Jung

John M Finn

Sergio E Wong

Felice C Lightstone

Suk Joong Lee

Atsuo Kuki

Toan B Nguyen

Qiyue Hu

John F Finn

Christopher John Creighton

Douglas W Phillipson

Ted William Johnson

Mark Hilgers

Anle Yang

Min Teng

Steven Paul Tanis

Yufeng Hong

Haitao Li

Joseph Timothy Marakovits

Allen Borchardt

Klaus Ruprecht Dress

Xinqiang Li

Paul Aristoff

Dawn Marie Nowlin

Qing Dong

Indrawan James McAlpine

Chuangxing Guo

Liming Dong

Djamal Bouzida

Pengyu Yang

Chunfeng Yin

Susan Elizabeth Kephart

Mary Catherine Johnson

Voon Ong

Mark Stidham

Huichun Zhu

Les Tari

Lucy Aguirre Kohnen

Mark Cunningham

Venkat Bollu

Lynnie Trzoss

Allen John Borchardt

Jayashree Girish Tikhe

Described herein are modulators of TNF alpha activity and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of TNF alpha-mediated disorders or diseases.

Modulators of TNF alpha activity and uses thereof

The present disclosure provides novel compounds capable of functioning as Myocyte Enhancer Factor 2 (MEF2) modulators, as well as compositions, pharmaceutical formulations, methods of synthesis and kits.

Myocyte enhancer factor 2 (MEF2) modulators

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

The present invention is directed to low molecular weight and orally bioavailable 3H-[1,2,3]triazolo[4,5-d]pyrimidine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the tyrosine kinase MET. The invention is also directed to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

Protein kinase inhibitors

Pyrrole pyrazole compounds of formula I, compositions including these compounds and methods of their use are provided. Preferred compounds of formula I have activity as protein kinase inhibitors, including as inhibitors of PAK4. 

Pyrrolopyrazoles, potent kinase inhibitors

Pyrrolopyrazole, potent kinase inhibitors

The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus ('HIV') integrase enzyme.

Inhibitors of the HIV integrase enzyme

The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus ('HIV') integrase enzyme. 

Bicycling hydroxamate compounds represented by the Formula I: are described. The bicyclic hydroxamate compounds and compositions containing those compounds may be used to inhibit or modulate an enzyme activity of HIV Integrase and to treat HIV mediated diseases and conditions.

HIV-Integrase inhibitors, pharmaceutical compositions and methods for their use

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San Diego, CA, United States of America

Junhu Zhang