Array Biopharma Inc.

Genentech, Inc.

Mirati Therapeutics, Inc.

Loxo Oncology, Inc.

Pfizer Corporation

Vertex Pharmaceuticals, Inc.

Roche Palo Alto LLC

Eli Lilly and Company

Genetech, Inc.

Covenentech, Inc.

Genertech, Inc.

Tang, Tony P.

Hentemann, Martin F.

Blake, James F.

Banka, Anna

James F Blake

Eli M Wallace

Gabrielle R Kolakowski

Steven Wade Andrews

Yutong Jiang

Li Ren

David A Moreno

Julia Haas

Tony P Tang

Mark Joseph Chicarelli

Barbara J Brandhuber

Rui Xu

Adam Wade Cook

Andrew T Metcalf

Ian S Mitchell

Josef R Bencsik

Nicholas C Kallan

Peter J Mohr

Jeongbeob Seo

Jun Liang

John Joseph Gaudino

Dengming Xiao

Keith Lee Spencer

Joseph P Lyssikatos

Allison L Marlow

Elizabeth A McFaddin

Shelley Allen

John Peter Fischer

Jay Bradford Fell

Megan L McKenney

Indrani W Gunawardana

Oren T McNulty

Brian Salvatore Safina

Sean Douglas Aronow

Shane M Walls

Stephen T Schlachter

Michael Lyon

Huifen Chen

Jacob Bradley Schwarz

Bin Wang

Hong Woon Yang

Yvan Le Huerou

Macedonio J Mejia

Christine Chabot

Timothy S Kercher

Martha E Rodriguez

Allen A Thomas

Guy P A Vigers

Anna L Banka

Ginelle A Ramann

Matthew Arnold Marx

Martin F Hentemann

Shannon L Winski

Pavel Savechenkov

Ronald Jay Hinklin

Kevin W Hunt

James Gail Christensen

Brad Newhouse

Rustam Ferdinand Garrey

Steven Huy Do

Mark Laurence Boys

Birong Zhang

Erik James Hicken

Nisha Nanda

Laurence Edward Burgess

Kevin Ronald Condroski

Lewis J Gazzard

Kirk D Robarge

Aihe Zhou

Hong-Woon Yang

Jonas Grina

Steven Armen Boyd

Christopher Ronald Smith

Peter J Stengel

T Brian Hurley

Kin Chiu Fong

Lily Huang

Jeffrey O Saunders

Qian Zhao

John E Robinson

John David Lawson

Xiaolun Wang

John Michael Ketcham

Robert Than Hendricks

Aaron Craig Burns

Jun M Li

Stacey Spencer

Matthew Randolph Lee

Matthew Randolf Lee

Mike Welch

Alexandre Joseph Buckmelter

Xicheng David Sun

Kevin Koch

Wendy B Young

Mark C Munson

Frederick Cohen

Anthony D Piscopio

John A Josey

Chang Rao

Adam W Cook

Provided herein are 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives of the general Formula I; and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which Xis N and Ring A, Ring B, Ring C, X, X, R, L, and W have the meanings given in the specification, which are inhibitors of FGFR1, FGFR2, FGFR3 and/or FGFR4 and are useful in the treatment and prevention of diseases which can be treated with an FGFR inhibitor, such as e.g. cancer, e g. bladder cancer, brain cancer, breast cancer, cholangiocarcinoma, head and neck cancer, lung cancer, multiple myeloma, rhabdomyosarcoma, urethral cancer and uterine cancer. The present description discloses the preparation of exemplary compounds as well as pharmacological data thereof (e.g. pages 276 to 308; examples 1 to 30; examples A to E; tables CA to EE). An exemplary compound is e.g. 1-(3-(4-(4-(7-((3,5-dimethoxy phenyl) amino)quinoxalin-2-yl)-1H-pyrazol-1-yl)piperidine-1-carbonyl) azetidin-1-yl)prop-2-en-1-one (e.g. example 1).

Substituted quinoxaline compounds as inhibitors of FGFR tyrosine kinases

Compounds of Formula Ia or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative diseases. Methods of using compounds of Formula Ia or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt 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

Protein tyrosine phosphatase inhibitors

Provided herein are compounds of the general Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which Ring A, Ring B, Ring C, R, R, L, Y, and W have the meanings given in the specification, which are inhibitors of FGFR1, FGFR2, FGFR3 and/or FGFR4 and are useful in the treatment and prevention of diseases which can be treated with an FGFR inhibitor, including diseases or disorders mediated by FGFR1, FGFR2, FGFR3 and/or FGFR4.

Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of FGFR tyrosine kinases

Provided herein are compounds of the Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, X, X, X, X, Ring D, and E have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.

Substituted pyrazolo[1,5-a]pyridine compounds as RET kinase inhibitors

Provided herein are compounds of the Formula (I): (I) and tautomers, stereoisomers and pharmaceutically acceptable salts and solvates thereof, wherein R, R, W, X, Y, Z, Ring A and (AA) have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.

Fused heterocyclic compounds as RET kinase inhibitors

Compounds that inhibit KRas G12D. In particular, compounds that inhibit the activity of KRas G12D, pharmaceutical compositions comprising the compounds and methods of use therefor, and in particular, methods of treating cancer. The compounds have a general structure represented by Formula (I): or a pharmaceutically acceptable salt thereof.

KRas G12D inhibitors

The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.

KRas G12C inhibitors

Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt 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.

Provided herein are compounds of the Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, D, E, X, X, Xand Xhave the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including diseases or disorders mediated by a RET kinase.

Substituted pyrazolo[1,5-A]pyrazine compounds as ret kinase inhibitors

The invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R, R, Rand Rare as defined herein. The invention further relates to pharmaceutical compositions comprising such compounds and salts, and to methods and uses of such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer, in a subject in need thereof. The invention further relates to solid forms of 8-((2-fluoro-4-(methylthio)phenyl)amino)-2-(2-hydroxyethoxy)-7-methyl-3,4-dihydro-2,7-naphthyridine-1,6(2H,7H)-dione.

3,4-dihydro-2,7-naphthyridine-1,6(2H,7H)-diones as MEK inhibitors

Provided herein are compounds of the Formula I: or pharmaceutically acceptable salt or solvate thereof, wherein A, B, X, X, X, X, Ring D, E, R, R, n and m have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.

Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors

Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt 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. 

Provided herein are compounds of the Formula I: [INSERT FORMULA I] and tautomers, stereoisomers and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2 and Ry have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders. 

Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors

Provided herein are compounds of the Formula I: and tautomers and pharmaceutically acceptable salts and solvates thereof, wherein Rand Rhave the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders. 

Substituted pyrazolo[3,4-d]pyrimidines as RET kinase inhibitors

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Boulder, CO, United States of America

James F Blake