F. Hoffmann-la Roche Ag

Piramed Limited

Genentech, Inc.

Ludwig Institute for Cancer Research Limited

Astellas Pharma Gmbh

Cancer Research Technology Limited

The Institute of Cancer Research: Royal Cancer Hospital

Stephen Joseph Shuttleworth

Adrian Folkes

Irina Chuckowree

Timothy Colin Hancox

Stewart James Baker

Nan Chi Wan

Sukhjit Sohal

Mohammed A Latif

Paul John Goldsmith

Bing-Yan Zhu

Stephen Colin Price

Daniel P Sutherlin

Alan G Olivero

Georgette M Castanedo

Richard A Goldsmith

Simon Mathieu

Janet Gunzner

Tim Heffron

Sally Oxenford

Tim Hancox

Neil Anthony Pegg

Christian Wiesmann

Edward McDonald

Shumei Wang

Vickie H Tsui

Tracy Bayliss

Jennafer Dotson

Kimberly Malesky

Elsa Amandine Dechaux

Sukhjit Sohai

Jonathan M Large

Edward Mcdonald

Jonathan Martin Large

Fused pyrimidines of formula (I): wherein R-R, A and n have any of the values described in the specification; and pharmaceutically acceptable salts thereof; have activity as inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.

Pharmaceutical compounds

Compounds of Formulae Ia and Ib, 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 and Ib for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. 

Thienopyrimidines of formula (Ia) or (Ib): wherein R-Rhave any of the values described herein, and the pharmaceutically acceptable salt thereof have activity as inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behavior associated with PI3 kinase, in particular the p110 delta subtype, such as immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.

Thienopyrimidines of formula (Ia) or (Ib): wherein R-Rhave any of the values described herein, and the pharmaceutically acceptable salt thereof have activity as inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase, in particular the p110 delta subtype, such as immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.

Pyrimidine derivatives as PI3K inhibitors

Fused pyrimidines of formula (I): wherein R-R, A and n have any of the values described in the specification; and pharmaceutically acceptable salts thereof; have activity as inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behavior associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.

Fused pyrimidines of formula (I): wherein A, n, R, R, and Rhave any of the values defined herein and the pharmaceutically acceptable salts thereof have activity as inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behavior associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.

Substituted thieno- and furano- fused pyrimidines as PI3K inhibitors

Provided herein are methods of treating diseases or disorders arising from abnormal cell growth, function or behavior associated with PI3 kinase, which method includes administering to a patient in need thereof a compound that is a fused pyrimidine of formula (I): 

Compounds of Formulas Ia and Ib, and including 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 and Ib 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

A thienopyrimidine of formula (I): and the pharmaceutically acceptable salts thereof have activity as inhibitors of PI3K with selectivity for the P110&#x3b1; subtype, and may be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour, particularly those associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.

Fused pyrimidines of formula (I): where A is a thiophene or furan ring and R-Rand n are defined in the specification. These compounds have activity as inhibitors of PI3K and may thus be used to treat diseased and disorders arising from abnormal cell growth, function or behavior associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.

Fused pyrimidines of formula (I): wherein R-R, A and n have any of the values described in the specification; and pharmaceutically acceptable salts thereof, have activity as inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.

Pyrimidines of formula (I): wherein Rto R, X and Y are defined in the specification are inhibitors of P13K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behavior associated with P13 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.

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Slough, United Kingdom

Stephen Joseph Shuttleworth