Cytokinetics, Inc.

Genentech, Inc.

Smithkline Beecham Corporation

Array Biopharma Inc.

Seattle Genetics, Inc.

Glaxosmithkline LLC

Bainian Feng

Gustave Bergnes

Whitney Walter Smith

David John Morgans, Jr

Jeffrey T Finer

John Clifford Chabala

Steven David Knight

Dashyant Dhanak

Kenneth Allen Newlander

Andrew I McDonald

Christopher A Brook

Xiangping Qian

Pu-Ping Lu

John A Flygare

Lewis J Gazzard

Fady Malik

Erica Anne Kraynack

Frederick Cohen

Vickie Hsiao-Wei Tsui

Wayne J Fairbrother

Kathleen Ann Elias

Kurt Deshayes

Adam Lewis Tomasi

Alexandre Joseph Buckmelter

Li Ren

David A Moreno

Ellen Ruth Laird

Wendy B Young

Brad Newhouse

Simon Mathieu

Janet Gunzner

Joachim Rudolph

Jonas Grina

Zhaoyang Wen

Steven Mark Wenglowsky

Kateri Ahrendt

Michael Gerard Darcy

Joshua D Hansen

Kim Malesky

Jeongbeob Seo

Hongqi Tian

Jason De Meese

Paul Lunghofer

Gustav E Bergnes

Gustav S Bergnes

Kateri A Ahrendt

David J Morgans

Andrew Mcdonald

David J C Morgans

Kenneth A Glaxosmithkline Newlander

Dashyant Glaxosmithkline Dhanak

Christopher S Glaxosmithkline Brook

The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R, R, R, R, R', R, R&#x2032;, Rand R&#x2032; are as described herein.

Inhibitors of IAP

Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity. 

Methods and compositions utilizing quinazolinones

Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.

Compounds, compositions and methods

Quinazolinones of formulae 1, 1, 1and 1are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity. 

Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. 

Pyrazole [3, 4-B] pyridine Raf inhibitors

Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula (I) and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. 

Raf inhibitor compounds and methods of use thereof

Quinazolinones of formulae (a, b, c and d) are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity. 

Methods and compostions utilizing quinazolinones

The present invention provides heterocyclic linker compounds useful for linking drug moieties to ligands. The compounds also include drug-ligand conjugates comprising a ligand capable of targeting a selected cell population, and a drug connected to the ligand by a heterocyclic linker moiety. The linker moiety comprises a peptide sequence that is a substrate for an intracellular enzyme, for example a cathepsin, that cleaves the peptide at an amide bond. The peptide further contains a self-immolating moiety which connects the drug and the protein peptide sequence. Upon cleavage of the peptide sequence by an intracellular enzyme the self-immolating moiety cleaves itself from the drug moiety such that the drug moiety is in an underivatized and active form.

Heterocyclic self-immolative linkers and conjugates

Quinazolinone KSP inhibitors

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Foster City, CA, United States of America

Bainian Feng