F. Hoffmann-la Roche Ag

Genentech, Inc.

Piramed Limited

The Institute of Cancer Research: Royal Cancer Hospital

Timothy Colin Hancox

Stephen Joseph Shuttleworth

Stewart James Baker

Adrian Folkes

Irina Chuckowree

Sukhjit Sohal

Nan Chi Wan

Mohammed A Latif

Stephen Colin Price

Neil Anthony Pegg

Paul John Goldsmith

Toby Jonathan Blench

Mandy Christine Beswick

Elsa Amandine Dechaux

Janusz Jozef Kulagowski

Sukhjit Sohai

Janusz Josef Kulagowski

Jahusz Jozef Kulagowski

Paul Goldsmith

Alan Hudson

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

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 (I) wherein W and Rto Rare as defined in the claims, and the pharmaceutically acceptable salts thereof are inhibitors of PI3K and are selective for the p110&#x3b4; isoform, which is a class Ia PI3 kinase, over both other class Ia and class Ib kinases. The compounds may 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 function disorders and neurological disorders. 

Thienopyrimidine derivatives as P13K inhibitors

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

Thiazolopyrimidine compounds of formula I, where W represents a thiazole ring, selectively inhibit the p110 delta subtype of PI3 Kinase (PI3K), and are useful for treating 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 function disorders and neurological disorders. 

Thiazolopyrimidines and their use as inhibitors of phosphatidylinositol-3 kinase

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): 

Thiazolopyrimidines of formula (I): wherein W represents a thiazole ring; Rand Rform, together with the N atom to which they are attached, a group of the following formula (IIa): in which A is a ring system; m is 0, 1 or 2; Ris H or C-Calkyl; and Ris an indole group which is unsubstituted or substituted; and the pharmaceutically acceptable salts thereof are inhibitors of PI3K and are selective for the p110&#x3b4; isoform, which is a class Ia PD kinase, over both other class Ia and class Ib kinases. The compounds may 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 function disorders and neurological disorders. 

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.

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Slough, United Kingdom

Timothy Colin Hancox