Array Biopharma Inc.

Eli Lilly and Company

Genentech, Inc.

Loxo Oncology, Inc.

Andrew T Metcalf

David A Moreno

Adam Wade Cook

Li Ren

James F Blake

Gabrielle R Kolakowski

Tony P Tang

Yutong Jiang

Julia Haas

Elizabeth A McFaddin

Steven Wade Andrews

Megan L McKenney

Oren T McNulty

Barbara J Brandhuber

Sean Douglas Aronow

Ginelle A Ramann

Shane M Walls

Kevin W Hunt

Indrani W Gunawardana

James Collier

Brett Joseph Prigaro

Brad Newhouse

Donghua Dai

Dean Russell Kahn

Huifen Chen

Lewis J Gazzard

Ellen Ruth Laird

Jacob Bradley Schwarz

Peter J Mohr

Erik James Hicken

Charles Todd Eary

Weidong Liu

Michael Lyon

Stacey Spencer

Mike Welch

Jane Schmidt

Zack Crane

Katelyn Chando

Sylvie Asselin

Kevin Ronald Condroski

John Joseph Gaudino

Bradley Jon Newhouse

Allen A Thomas

Spencer Phillip Pajk

Patrick Michael Barbour

Eugene Tarlton

Katie Keaton Brown

Robert Alan Hazlitt

Adedoyin David Abraham

Andrew Karl Dilger

Desta Doro Bume

Timothy Scott Kercher

Shane Michael Walls

Kaveri Balan Urkalan

Shelley Allen

Ronald Jay Hinklin

John E Robinson

Mark Laurence Boys

Elizabeth A Mcfaddin

David Fry

Oren Teague Mcnulty

Hailong Zhang

Steve Do

Megan L Mckenney

Brett Prigaro

Dean Kahn

Oren T Mcknulty

The present invention provides compounds of the formula: for use in the treatment of systemic sclerosis, fibrosis (e.g. pulmonary fibrosis), achondroplasia, thanatophoric dysplasia (e.g. type I), severe achondroplasia with developmental delay and acanthosis(SADDAN), muenke syndrome or cancer.

FGFR3 inhibitor compounds

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

The present invention provides compounds of the formula: for use in the treatment of systemic sclerosis, fibrosis (e.g. pulmonary fibrosis), achondroplasia, thanatophoric dysplasia (e.g. type I), severe achondroplasia with developmental delay and acanthosis nigricans (SADDAN), muenke syndrome or cancer.

In some embodiments, provided herein is a process for preparing a compound of Formula I or a pharmaceutically acceptable salt thereof, as disclosed herein.

Process for the preparation of 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile

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

Provided herein are compounds of the Formula I: and pharmaceutically acceptable salts, solvates and polymorphs thereof, wherein L, X, R, R, R, R, Rand Rare as defined herein, for the treatment of BRAF-associated diseases and disorders, including BRAF-associated tumors, including malignant and benign BRAF-associated tumors of the CNS and malignant extracranial BRAF-associated tumors.

Compounds for the treatment of BRAF-associated diseases and disorders

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

Provided herein are compounds of the Formula I: and tautomers and pharmaceutically acceptable salts and solvates thereof, wherein R, 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 pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors

Provided herein are compounds of the Formula (I): and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, wherein Ring A, X, X, X, R, Rand Rare as defined herein, which are inhibitors of one or more TAM kinases and are useful in the treatment and prevention of diseases which can be treated with a TAM kinase inhibitor. 

Bicyclic fused pyridine compounds as inhibitors of TAM kinases

Process for the preparation of 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbontrile

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Boulder, CO, United States of America

Andrew T Metcalf