Genentech, Inc.

F. Hoffmann-la Roche Ag

Hoffmann-la Roche Inc.

Piramed Limited

Array Biopharma Inc.

Curis, Inc.

Genetech, Inc.

F. Hoffmann-la Roche Sa

Alan G Olivero

Adrian Folkes

Daniel P Sutherlin

Steven T Staben

Richard A Goldsmith

Bing-Yan Zhu

Steven Huy Do

Aleksandr Kolesnikov

Chudi Obioma Ndubaku

Timothy Heffron

Robert Andrew Heald

Tim Heffron

Stephen Colin Price

Nicole Blaquiere

Danette Dudley

Georgette M Castanedo

Irina Chuckowree

Nan Chi Wan

Simon Mathieu

Tracy Bayliss

Michael Siu

Lan Wang

Janet Gunzner

Sally Oxenford

Shumei Wang

Jennafer Dotson

Mark Jones

Joseph P Lyssikatos

Anthony A Estrada

Snahel Patel

Dean R Artis

Richard Pastor

Kirk D Robarge

Kimberly Malesky

Paul Goldsmith

Neil Pegg

BinQing Wei

Vickie H Tsui

Terry Kellar

Malcolm Huestis

John A Flygare

Christian Wiesmann

Kevin X Chen

Yan Zhu

Graham Elgin Jones

Paul Gibbons

Thomas E Rawson

Aihe Zhou

Daniel Shore

Binqing Wei

Stephen Joseph Shuttleworth

Herbert Yajima

Tim Hancox

Andrew McClory

Michael S Dina

Remy Angelaud

Ignacio Aliagas-Martin

Stephen Shuttleworth

Wen Liu

Andreas Stumpf

Neville James McLean

Regina A Munroe

Kenneth J Weese

Liting Dong

Sussie Lerche Krintel

Laurent Salphati

Changyou Ma

Jun Liang

Ellen Ruth Laird

Jianwen A Feng

George T Topalov

Sushant Malhotra

Brad Newhouse

Naomi S Rajapaksa

Brent K Blackburn

Joy Drobnick

Yamin Zhang

Aijun Lu

Marian C Bryan

Alberto Gobbi

Jonas Grina

Mike Welch

James Richard Kiefer, Jr

Josh Hansen

Cheng Shao

Janet Gunzer-Toste

BinQuing Wei

Christian Weismann

Andrew Mcclory

Adrian J Folkes

Provided are fused ring compounds of Formula (I), Formula (II), or Formula (III), as further detailed herein, which are used for the inhibition of Ras proteins, as well as compositions comprising these compounds and methods treatment by their administration.

Fused ring compounds

The present disclosure provides for methods for preparing tricyclic PI3K inhibitor compounds in high yield and purity in aqueous solvent systems.

Process for the preparation of tricyclic PI3K inhibitor compounds and methods for using the same for the treatment of cancer

The present invention provides for compounds of Formula I-I and embodiments and salts thereof for the treatment of diseases (e.g., neurodegenerative diseases). R, R, R, X, X, A and Cy variable in Formula I-I all have the meaning as defined herein. 

Biheteroaryl compounds and uses thereof

Compounds of Formula 0, Formula I, and Formula II and methods of use as Interleukin-1 Receptor Associated Kinase (IRAK4) inhibitors are described herein.

Pyrazolo[1,5a]pyrimidine derivatives as IRAK4 modulators

The present invention provides for compounds of Formula I and embodiments and salts thereof for the treatment of diseases (e.g., neurodegenerative diseases). R, R, R, X, X, A and Cy variable in Formula all have the meaning as defined herein.

Compounds of Formulae Ia, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. 

Pharmaceutical compounds

Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Zis CRor N; Zis CRor N; Zis CRor N; Zis CRor N; and B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. 

Benzoxazepin PI3K inhibitor compounds and methods of use

Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions.  Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.

Tricyclic PI3K inhibitor compounds and methods of use

Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and Ris a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. 

Phosphoinositide 3-kinase inhibitor compounds and methods of use

Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. 

Benzopyran and benzoxepin PI3K inhibitor compounds and methods of use

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Half Moon Bay, CA, United States of America

Alan G Olivero