Array Biopharma Inc.

Genentech, Inc.

Peloton Therapeutics, Inc.

University of Kentucky Research Foundation

Genetech, Inc.

Covenentech, Inc.

Genertech, Inc.

Tang, Tony P.

Hentemann, Martin F.

Blake, James F.

Banka, Anna

Wallace, Eli M.

Bencsik, Josef R.

Mitchell, Ian S.

Xu, Rui

Rui Xu

James F Blake

Eli M Wallace

Ian S Mitchell

Stephen T Schlachter

Josef R Bencsik

Nicholas C Kallan

Jun Liang

Dengming Xiao

Keith Lee Spencer

Brian Salvatore Safina

John A Josey

Bin Wang

Hanbiao Yang

Paul Wehn

Christine Chabot

James P Rizzi

Darryl David Dixon

Jonas Grina

Anna L Banka

Martin F Hentemann

Tony P Tang

Steven Huy Do

Birong Zhang

James M Graham

Peter Anthony Crooks

Kin Chiu Fong

Yvan Le Huerou

Jun M Li

Mike Welch

Lisa A De Meese

Douglas McCord Sammond

Anna L Leivers

Steven Wade Andrews

Yutong Jiang

Gabrielle R Kolakowski

Shelley Allen

Kevin Ronald Condroski

Kevin Koch

Barbara J Brandhuber

George T Topalov

Mark C Munson

John E Robinson

John Peter Fischer

Anthony D Piscopio

Martha E Rodriguez

Linda P Dwoskin

Jay Bradford Fell

Peter J Stengel

Shannon L Winski

Chang Rao

Michael Lyon

Guy P A Vigers

Robert Kirk Delisle

Gregory F Miknis

Scott Miller

Yongxin Han

Jun Li

Vladimir P Grinevich

Joshua T Ayers

Bing Wang

Linda Dwoshin

April L Bernacki

Eli W Wallace

AnnaL Banka

StephenT Schlachter

The present disclosure relates to HIF-2α inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2α scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.

Aryl ethers and uses thereof

Disclosed herein are substituted indane derivatives useful as HIF-2&#x3b1; inhibitors. Pharmaceutical compositions comprising said indane derivatives and methods of using said indane derivatives for treating proliferative diseases, such as renal cell carcinoma and von Hippel-Lindau disease, and other conditions associated with HIF-2&#x3b1; activity are also disclosed.

Aromatic compounds and uses thereof

The present disclosure relates to HIF-2&#x3b1; inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2&#x3b1; scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.

Substituted pyridines that modulate HIF-2a activity, pharmaceutical compositions containing the substituted pyridines, and methods of using these chemical entities for treating proliferative diseases and conditions associated with HIF-2a activity are described herein.

Substituted pyridines and uses thereof

The present disclosure relates to cyclic sulfones and sulfoximines that are HIF-2a inhibitors and methods of making and using them for treating cancers. In another aspect, the present disclosure provides a pharmaceutical composition comprising a compound described herein and a pharmaceutically acceptable carrier or excipient. The compound may exist in an amorphous form, a crystalline form, or as a salt, solvate, or hydrate. In another aspect, the present disclosure provides a method of treating renal cell carcinoma by administrating a therapeutically effective amount of a compound described herein or a pharmaceutical composition thereof to a subject in need of such treatment.

Cyclic sulfone and sulfoximine analogs and uses thereof

Compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome. 

N-bicyclic aryl,N'-pyrazolyl urea, thiourea, guanidine cyanoguanidine compounds as TrkA kinase inhibitors

The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof.  Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

Pyrimidyl cyclopentanes as AKT protein kinase inhibitors

The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I:  Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

Hydroxylated and methoxylated pyrimidyl cyclopentanes as Akt protein kinase inhibitors

The present invention provides compounds of Formula I including tautomers, resolved enantiomers, resolved diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof.  Also provided are methods of using the compounds of this invention as Akt protein kinase inhibitors and for the treatment of Akt-mediated diseases, for example, hyperproliferative diseases such as cancer.

Pyrimidyl cyclopentanes as Akt protein kinase inhibitors

Compounds of Formula I are useful for inhibiting AKT protein kinases. Methods of using compounds of Formula I and stereoisomers 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. 

5H-cyclopenta[d]pyrimidines as AKT protein kinase inhibitors

The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula:  Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

Substituted piperazines as AKT inhibitors

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Boulder, CO, United States of America

Rui Xu