Genentech, Inc.

Walter and Eliza Hall Institute of Medical Research

F. Hoffmann-la Roche Ag

Abbott Laboratories Corporation

Abbvie Inc.

Genetech, Inc.

Danette Dudley

Chudi Obioma Ndubaku

Stephen Colin Price

Alan G Olivero

Robert Andrew Heald

Adrian Folkes

Steven Huy Do

Aleksandr Kolesnikov

Steven T Staben

Timothy Heffron

Nicole Blaquiere

Lan Wang

Mark Jones

John A Flygare

Andrew J Souers

Keith G Watson

Steven Elmore

Jonathan Bayldon Baell

Wayne J Fairbrother

Richard A Goldsmith

Andrew M Petros

Brad E Sleebs

Chinh Thien Bui

Guillaume Laurent Lessene

Brian John Smith

Peter Colman

Peter Edward Czabotar

George Nikolakopoulos

Carl Steven Rye

BinQing Wei

Binqing Wei

Xilu Wang

Le Wang

Zhi-Fu Tao

Lisa A Hasvold

Tim Heffron

Kurt Deshayes

Adrian J Folkes

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

Benzoxepin compounds of Formula I, and 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 where (i) Xis N and Xis S, (ii) Xis S and Xis N, (iii) Xis CRand Xis S, (iv) Xis S and Xis CR; (v) Xis NRand Xis N, (vi) Xis N and Xis NR, (vii) Xis CRand Xis O, (viii) Xis O and Xis CR, (ix) Xis CRand Xis C(R), (x) Xis C(R)and Xis CR; (xi) Xis N and Xis O, or (xii) Xis O and Xis N, 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. 

Benzoxepin PI3K inhibitor compounds and methods of use

In one aspect, the present invention provides for a compound of Formula I in which in Formula I, the variables X, X, X, X, R, B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xproteins.

Compounds and methods of use

The invention provides novel compounds that are inhibitors of IAPs having the general formula: wherein X, X, X, Y, A, R, R, R, R, R, R, R, Rand Rare as described herein. The compouds of the invention may be used to induce apoptosis in cells (or sensitise cells to apoptosis) in which IAPs are overexpressed or otherwise implicated in resistance to normal apoptotic processes. Accordingly, the compounds may be provided in pharmaceutically acceptable compositions and used for the treatment cancers. 

Inhibitors of IAP

Benzoxepin compounds of Formula I, 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 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 P13K inhibitor compounds and methods of use

In one aspect, the present invention provides for a compound of Formula I in which the variable X, X, X, X, Q, A, R, B, L, E, and the subscripts m and n have the meanings as described herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xproteins.

Heterocyclic compounds and methods of use

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Pacifica, CA, United States of America

Danette Dudley