公开(公告)号：US20120035208A1

公开(公告)日：2012-02-09

申请号：US13129091

申请日：2009-11-19

申请人： Jennafer Dotson ,  Timothy Heffron ,  Alan G. Olivero ,  Daniel P. Sutherlin ,  Steven Staben ,  Shumei Wang ,  Bing-Yan Zhu ,  Irina S. Chuckowree ,  Adrian J. Folkes ,  Nan Chi Wan

发明人： Jennafer Dotson ,  Timothy Heffron ,  Alan G. Olivero ,  Daniel P. Sutherlin ,  Steven Staben ,  Shumei Wang ,  Bing-Yan Zhu ,  Irina S. Chuckowree ,  Adrian J. Folkes ,  Nan Chi Wan

IPC分类号： A61K31/437 ,  C12N9/99 ,  A61P35/00 ,  A61P35/02 ,  A61P29/00 ,  A61P3/10 ,  A61P25/00 ,  A61P9/00 ,  A61P1/16 ,  A61P31/12 ,  A61P7/00 ,  C07D471/04 ,  A61P37/02

CPC分类号： C07D471/04

摘要： 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 or inflammation 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.

摘要翻译： 式（I）化合物，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和其药学上可接受的盐可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗疾病如癌症或炎症介导 通过脂质激酶。 公开了使用式（I）化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理条件中的这种疾病的方法。

公开(公告)号：US08653098B2

公开(公告)日：2014-02-18

申请号：US13129091

申请日：2009-11-19

申请人： Jennafer Dotson ,  Timothy Heffron ,  Alan G. Olivero ,  Daniel P. Sutherlin ,  Steven Staben ,  Shumei Wang ,  Bing-Yan Zhu ,  Irina S. Chuckowree ,  Adrian J. Folkes ,  Nan Chi Wan

发明人： Jennafer Dotson ,  Timothy Heffron ,  Alan G. Olivero ,  Daniel P. Sutherlin ,  Steven Staben ,  Shumei Wang ,  Bing-Yan Zhu ,  Irina S. Chuckowree ,  Adrian J. Folkes ,  Nan Chi Wan

IPC分类号： A61K31/44 ,  C07D491/02 ,  C07D498/02

CPC分类号： C07D471/04

摘要： 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 or inflammation 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.

摘要翻译： 式（I）化合物，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和其药学上可接受的盐可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗疾病如癌症或炎症介导 通过脂质激酶。 公开了使用式（I）化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理条件中的这种疾病的方法。

公开(公告)号：US20120258966A1

公开(公告)日：2012-10-11

申请号：US13415672

申请日：2012-03-08

申请人： Stephen J. Shuttleworth ,  Adrian J. Folkes ,  Irina S. Chuckowree ,  Nan Chi Wan ,  Timothy C. Hancox ,  Stewart J. Baker ,  Sukhjit Sohal ,  Mohammed A. Latif

发明人： Stephen J. Shuttleworth ,  Adrian J. Folkes ,  Irina S. Chuckowree ,  Nan Chi Wan ,  Timothy C. Hancox ,  Stewart J. Baker ,  Sukhjit Sohal ,  Mohammed A. Latif

IPC分类号： A61K31/5377 ,  A61P35/00

CPC分类号： C07D495/04

摘要： Fused pyrimidines of formula (I): wherein R1-R3, 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.

摘要翻译： 式（I）的稠合嘧啶：其中R1-R3，A和n具有说​​明书中描述的任何值; 及其药学上可接受的盐; 具有作为PI3K抑制剂的活性，因此可用于治疗与PI3激酶例如癌症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌失调和神经系统疾病相关的异常细胞生长，功能或行为引起的疾病和障碍 疾病 还描述了合成化合物的方法。

公开(公告)号：US20100280027A1

公开(公告)日：2010-11-04

申请号：US12835533

申请日：2010-07-13

申请人： Stephen J. Shuttleworth ,  Adrian J. Folkes ,  Irina S. Chuckowree ,  Nan Chi Wan ,  Timothy C. Hancox ,  Stewart J. Baker ,  Sukhjit Sohal ,  Mohammed A. Latif

发明人： Stephen J. Shuttleworth ,  Adrian J. Folkes ,  Irina S. Chuckowree ,  Nan Chi Wan ,  Timothy C. Hancox ,  Stewart J. Baker ,  Sukhjit Sohal ,  Mohammed A. Latif

IPC分类号： A61K31/5377 ,  A61P35/00 ,  A61P37/00 ,  A61P9/00 ,  A61P3/00 ,  A61P25/00 ,  A61P29/00 ,  A61P31/12 ,  A61P3/10 ,  A61P3/04 ,  A61P35/02

CPC分类号： C07D495/04

摘要： 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):

摘要翻译： 本文提供了治疗由与PI3激酶相关的异常细胞生长，功能或行为引起的疾病或障碍的方法，该方法包括向有需要的患者施用作为式（I）的稠合嘧啶的化合物：

公开(公告)号：US07776856B2

公开(公告)日：2010-08-17

申请号：US11665657

申请日：2005-10-25

申请人： Stephen J. Shuttleworth ,  Adrian J. Folkes ,  Irina S. Chuckowree ,  Nan Chi Wan ,  Timothy C. Hancox ,  Stewart J. Baker ,  Sukhjit Sohal ,  Mohammed A. Latif

发明人： Stephen J. Shuttleworth ,  Adrian J. Folkes ,  Irina S. Chuckowree ,  Nan Chi Wan ,  Timothy C. Hancox ,  Stewart J. Baker ,  Sukhjit Sohal ,  Mohammed A. Latif

IPC分类号： A61K31/5377 ,  C07D413/14

CPC分类号： C07D495/04

摘要： Fused pyrimidines of formula (I): where A is a thiophene or furan ring and R1-R3 and 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.

摘要翻译： 式（I）的稠合嘧啶：其中A是噻吩或呋喃环，R1-R3和n在说明书中定义。 这些化合物具有作为PI3K抑制剂的活性，因此可用于治疗与由PI3激酶例如癌症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌紊乱相关的异常细胞生长，功能或行为引起的疾病和病症 和神经障碍。 还描述了合成化合物的方法。

公开(公告)号：US20100234370A1

公开(公告)日：2010-09-16

申请号：US12789773

申请日：2010-05-28

申请人： Stephen J. Shuttleworth ,  Adrian J. Folkes ,  Irina S. Chuckowree ,  Nan Chi Wan ,  Timothy C. Hancox ,  Stewart J. Baker ,  Sukhjit Sohal ,  Mohammed A. Latif

发明人： Stephen J. Shuttleworth ,  Adrian J. Folkes ,  Irina S. Chuckowree ,  Nan Chi Wan ,  Timothy C. Hancox ,  Stewart J. Baker ,  Sukhjit Sohal ,  Mohammed A. Latif

IPC分类号： A61K31/5377 ,  A61P35/00 ,  A61P37/00 ,  A61P9/00 ,  A61P31/12 ,  A61P29/00 ,  A61P3/00 ,  A61P25/00

CPC分类号： C07D495/04

摘要： Fused pyrimidines of formula (I): wherein R1-R3, 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.

摘要翻译： 式（I）的稠合嘧啶：其中R1-R3，A和n具有说​​明书中描述的任何值; 及其药学上可接受的盐; 具有作为PI3K抑制剂的活性，因此可用于治疗与PI3激酶例如癌症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌失调和神经系统疾病相关的异常细胞生长，功能或行为引起的疾病和障碍 疾病 还描述了合成化合物的方法。

公开(公告)号：US08153629B2

公开(公告)日：2012-04-10

申请号：US12789773

申请日：2010-05-28

申请人： Stephen J. Shuttleworth ,  Adrian J. Folkes ,  Irina S. Chuckowree ,  Nan Chi Wan ,  Timothy C. Hancox ,  Stewart J. Baker ,  Sukhjit Sohal ,  Mohammed A. Latif

发明人： Stephen J. Shuttleworth ,  Adrian J. Folkes ,  Irina S. Chuckowree ,  Nan Chi Wan ,  Timothy C. Hancox ,  Stewart J. Baker ,  Sukhjit Sohal ,  Mohammed A. Latif

IPC分类号： A61K31/535

CPC分类号： C07D495/04

摘要： Fused pyrimidines of formula (I): wherein R1-R3, 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.

摘要翻译： 式（I）的稠合嘧啶：其中R1-R3，A和n具有说​​明书中所述的任何值; 及其药学上可接受的盐; 具有作为PI3K抑制剂的活性，因此可用于治疗与PI3激酶例如癌症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌失调和神经系统疾病相关的异常细胞生长，功能或行为引起的疾病和障碍 疾病 还描述了合成化合物的方法。

公开(公告)号：US08101607B2

公开(公告)日：2012-01-24

申请号：US12835533

申请日：2010-07-13

申请人： Stephen J. Shuttleworth ,  Adrian J. Folkes ,  Irina S. Chuckowree ,  Nan Chi Wan ,  Timothy C. Hancox ,  Stewart J. Baker ,  Sukhjit Sohal ,  Mohammed A. Latif

发明人： Stephen J. Shuttleworth ,  Adrian J. Folkes ,  Irina S. Chuckowree ,  Nan Chi Wan ,  Timothy C. Hancox ,  Stewart J. Baker ,  Sukhjit Sohal ,  Mohammed A. Latif

IPC分类号： A61K31/5377

CPC分类号： C07D495/04

摘要： 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):

摘要翻译： 本文提供了治疗由与PI3激酶相关的异常细胞生长，功能或行为引起的疾病或障碍的方法，该方法包括向有需要的患者施用作为式（I）的稠合嘧啶的化合物：

公开(公告)号：US07872003B2

公开(公告)日：2011-01-18

申请号：US11893625

申请日：2007-08-16

申请人： Stephen J. Shuttleworth ,  Adrian J. Folkes ,  Irina S. Chuckowree ,  Nan Chi Wan ,  Timothy C. Hancox ,  Stewart J. Baker ,  Sukhjit Sohal ,  Mohammed A. Latif

发明人： Stephen J. Shuttleworth ,  Adrian J. Folkes ,  Irina S. Chuckowree ,  Nan Chi Wan ,  Timothy C. Hancox ,  Stewart J. Baker ,  Sukhjit Sohal ,  Mohammed A. Latif

IPC分类号： A61K31/535 ,  C07D413/14

CPC分类号： C07D495/04

摘要： Fused pyrimidines of formula (I): wherein R1-R3, 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.

摘要翻译： 式（I）的稠合嘧啶：其中R1-R3，A和n具有说​​明书中描述的任何值; 及其药学上可接受的盐; 具有作为PI3K抑制剂的活性，因此可用于治疗与PI3激酶例如癌症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌失调和神经系统疾病相关的异常细胞生长，功能或行为引起的疾病和障碍 疾病 还描述了合成化合物的方法。

公开(公告)号：US07750002B2

公开(公告)日：2010-07-06

申请号：US11893414

申请日：2007-08-16

申请人： Stephen J. Shuttleworth ,  Adrian J. Folkes ,  Irina S. Chuckowree ,  Nan Chi Wan ,  Timothy C. Hancox ,  Stewart J. Baker ,  Sukhjit Sohal ,  Mohammed A. Latif

发明人： Stephen J. Shuttleworth ,  Adrian J. Folkes ,  Irina S. Chuckowree ,  Nan Chi Wan ,  Timothy C. Hancox ,  Stewart J. Baker ,  Sukhjit Sohal ,  Mohammed A. Latif

IPC分类号： A61K31/535 ,  C07D413/14

CPC分类号： C07D495/04

摘要： Fused pyrimidines of formula (I): wherein R1-R3, 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.

摘要翻译： 式（I）的稠合嘧啶：其中R1-R3，A和n具有说​​明书中描述的任何值; 其药学上可接受的盐具有作为PI3K抑制剂的活性，因此可用于治疗与PI3激酶例如癌症，免疫疾病，心血管疾病，病毒感染，炎症等相关的异常细胞生长，功能或行为引起的疾病和病症， 代谢/内分泌紊乱和神经系统疾病。 还描述了合成化合物的方法。