公开(公告)号：US20080269210A1

公开(公告)日：2008-10-30

申请号：US11951189

申请日：2007-12-05

申请人： Georgette Castanedo ,  Jennafer Dotson ,  Richard Goldsmith ,  Janet Gunzner ,  Tim Heffron ,  Simon Mathieu ,  Alan Olivero ,  Daniel P. Sutherlin ,  Shumei Wang ,  Bing-Yan Zhu ,  Steven Staben ,  Vickie Tsui ,  Tracy Bayliss ,  Irina Chuckowree ,  Adrian Folkes ,  Nan Chi Wan

发明人： Georgette Castanedo ,  Jennafer Dotson ,  Richard Goldsmith ,  Janet Gunzner ,  Tim Heffron ,  Simon Mathieu ,  Alan Olivero ,  Daniel P. Sutherlin ,  Shumei Wang ,  Bing-Yan Zhu ,  Steven Staben ,  Vickie Tsui ,  Tracy Bayliss ,  Irina Chuckowree ,  Adrian Folkes ,  Nan Chi Wan

IPC分类号： A61K31/5377 ,  C07D495/04 ,  C07D413/14 ,  A61P35/00 ,  A61K31/519

CPC分类号： C07D491/048 ,  C07D495/04

摘要： Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is 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.

摘要翻译： 式Ia-d的化合物，其中X是S或O，mor是吗啉基团，R 3是单环杂芳基，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的 其盐可用于调节脂质激酶（包括PI3K）的活性，以及​​用于治疗由脂质激酶介导的癌症等疾病。 公开了使用式Ia-d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状况中的这种疾病的方法。

公开(公告)号：US09487533B2

公开(公告)日：2016-11-08

申请号：US11951189

申请日：2007-12-05

申请人： Georgette Castanedo ,  Jennafer Dotson ,  Richard Goldsmith ,  Janet Gunzner ,  Tim Heffron ,  Simon Mathieu ,  Alan Olivero ,  Daniel P. Sutherlin ,  Shumei Wang ,  Bing-Yan Zhu ,  Steven Staben ,  Vickie Tsui ,  Tracy Bayliss ,  Irina Chuckowree ,  Adrian Folkes ,  Nan Chi Wan

发明人： Georgette Castanedo ,  Jennafer Dotson ,  Richard Goldsmith ,  Janet Gunzner ,  Tim Heffron ,  Simon Mathieu ,  Alan Olivero ,  Daniel P. Sutherlin ,  Shumei Wang ,  Bing-Yan Zhu ,  Steven Staben ,  Vickie Tsui ,  Tracy Bayliss ,  Irina Chuckowree ,  Adrian Folkes ,  Nan Chi Wan

IPC分类号： C07D491/048 ,  C07D495/04

CPC分类号： C07D491/048 ,  C07D495/04

摘要： Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is 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.

公开(公告)号：US07846929B2

公开(公告)日：2010-12-07

申请号：US11789427

申请日：2007-04-24

申请人： Adrian Folkes ,  Stephen Shuttleworth ,  Sally Oxenford ,  Tim Hancox ,  Tracy Bayliss ,  Georgette Castanedo ,  Richard Goldsmith ,  Janet Gunzner ,  Tim Heffron ,  Kimberly Malesky ,  Simon Mathieu ,  Alan Olivero ,  Daniel P. Sutherlin ,  Vickie Tsui ,  Shumei Wang ,  Christian Wiesmann ,  Bing-Yan Zhu ,  Jennafer Dotson

发明人： Adrian Folkes ,  Stephen Shuttleworth ,  Sally Oxenford ,  Tim Hancox ,  Tracy Bayliss ,  Georgette Castanedo ,  Richard Goldsmith ,  Janet Gunzner ,  Tim Heffron ,  Kimberly Malesky ,  Simon Mathieu ,  Alan Olivero ,  Daniel P. Sutherlin ,  Vickie Tsui ,  Shumei Wang ,  Christian Wiesmann ,  Bing-Yan Zhu ,  Jennafer Dotson

IPC分类号： A61K31/5377 ,  C07D413/14

CPC分类号： C07D491/04 ,  C07D495/04

摘要： 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.

摘要翻译： 式Ia和Ib的化合物，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的盐可用于抑制脂质激酶（包括PI3K）和用于治疗由脂质激酶介导的癌症等疾病。 公开了将式Ia和Ib化合物用于体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

公开(公告)号：US20110105464A1

公开(公告)日：2011-05-05

申请号：US12916125

申请日：2010-10-29

申请人： Georgette Castanedo ,  Richard Goldsmith ,  Janet Gunzner ,  Tim Heffron ,  Kimberly Malesky ,  Simon Mathieu ,  Alan Olivero ,  Daniel P. Sutherlin ,  Vickie Tsui ,  Shumei Wang ,  Christian Wiesmann ,  Bing-Yan Zhu ,  Jennafer Dotson ,  Adrian Folkes ,  Stephen Shuttleworth ,  Sally Oxenford ,  Tim Hancox ,  Tracy Bayliss

发明人： Georgette Castanedo ,  Richard Goldsmith ,  Janet Gunzner ,  Tim Heffron ,  Kimberly Malesky ,  Simon Mathieu ,  Alan Olivero ,  Daniel P. Sutherlin ,  Vickie Tsui ,  Shumei Wang ,  Christian Wiesmann ,  Bing-Yan Zhu ,  Jennafer Dotson ,  Adrian Folkes ,  Stephen Shuttleworth ,  Sally Oxenford ,  Tim Hancox ,  Tracy Bayliss

IPC分类号： A61K31/5377 ,  A61P35/00 ,  A61P35/02 ,  A61P29/00 ,  A61P3/10 ,  A61P9/00

CPC分类号： C07D491/04 ,  C07D495/04

摘要： 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.

摘要翻译： 公开了将式Ia和Ib化合物用于体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

公开(公告)号：US08383620B2

公开(公告)日：2013-02-26

申请号：US12978106

申请日：2010-12-23

申请人： Tracy Bayliss ,  Irina Chuckowree ,  Adrian Folkes ,  Sally Oxenford ,  Nan Chi Wan ,  Georgette Castanedo ,  Richard Goldsmith ,  Janet Gunzner ,  Tim Heffron ,  Simon Mathieu ,  Alan Olivero ,  Steven Staben ,  Daniel P. Sutherlin ,  Bing-Yan Zhu

发明人： Tracy Bayliss ,  Irina Chuckowree ,  Adrian Folkes ,  Sally Oxenford ,  Nan Chi Wan ,  Georgette Castanedo ,  Richard Goldsmith ,  Janet Gunzner ,  Tim Heffron ,  Simon Mathieu ,  Alan Olivero ,  Steven Staben ,  Daniel P. Sutherlin ,  Bing-Yan Zhu

IPC分类号： A61K31/535

CPC分类号： A61K31/5377 ,  A61K31/519 ,  C07D413/14 ,  C07D491/04 ,  C07D495/04

摘要： Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is 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.

公开(公告)号：US20080242665A1

公开(公告)日：2008-10-02

申请号：US11951203

申请日：2007-12-05

申请人： Tracy Bayliss ,  Irina Chuckowree ,  Adrian Folkes ,  Sally Oxenford ,  Nan Chi Wan ,  Georgette Castanedo ,  Richard Goldsmith ,  Janet Gunzner ,  Tim Heffron ,  Simon Mathieu ,  Alan Olivero ,  Steven Staben ,  Daniel P. Sutherlin ,  Bing-Yan Zhu

发明人： Tracy Bayliss ,  Irina Chuckowree ,  Adrian Folkes ,  Sally Oxenford ,  Nan Chi Wan ,  Georgette Castanedo ,  Richard Goldsmith ,  Janet Gunzner ,  Tim Heffron ,  Simon Mathieu ,  Alan Olivero ,  Steven Staben ,  Daniel P. Sutherlin ,  Bing-Yan Zhu

IPC分类号： A61K31/5377 ,  C07D495/04 ,  A61P35/04

CPC分类号： A61K31/5377 ,  A61K31/519 ,  C07D413/14 ,  C07D491/04 ,  C07D495/04

摘要： Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is 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.

摘要翻译： 式Ia-d的化合物，其中X是S或O，mor是吗啉基团，R 3是单环杂芳基，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的 其盐可用于调节脂质激酶（包括PI3K）的活性，以及​​用于治疗由脂质激酶介导的癌症等疾病。 公开了使用式Ia-d的化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

公开(公告)号：US08450315B2

公开(公告)日：2013-05-28

申请号：US12916125

申请日：2010-10-29

申请人： Georgette Castanedo ,  Richard Goldsmith ,  Janet Gunzner ,  Tim Heffron ,  Kimberly Malesky ,  Simon Mathieu ,  Alan Olivero ,  Daniel P. Sutherlin ,  Vickie Tsui ,  Shumei Wang ,  Christian Wiesmann ,  Bing-Yan Zhu ,  Jennafer Dotson ,  Adrian Folkes ,  Stephen Shuttleworth ,  Sally Oxenford ,  Tim Hancox ,  Tracy Bayliss

发明人： Georgette Castanedo ,  Richard Goldsmith ,  Janet Gunzner ,  Tim Heffron ,  Kimberly Malesky ,  Simon Mathieu ,  Alan Olivero ,  Daniel P. Sutherlin ,  Vickie Tsui ,  Shumei Wang ,  Christian Wiesmann ,  Bing-Yan Zhu ,  Jennafer Dotson ,  Adrian Folkes ,  Stephen Shuttleworth ,  Sally Oxenford ,  Tim Hancox ,  Tracy Bayliss

IPC分类号： A61K31/5377

CPC分类号： C07D491/04 ,  C07D495/04

摘要： 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.

摘要翻译： 公开了将式Ia和Ib化合物用于体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

公开(公告)号：US20110097349A1

公开(公告)日：2011-04-28

申请号：US12978106

申请日：2010-12-23

申请人： Tracy Bayliss ,  Irina Chuckowree ,  Adrian Folkes ,  Sally Oxenford ,  Nan Chi Wan ,  Georgette Castanedo ,  Richard Goldsmith ,  Janet Gunzner ,  Tim Heffron ,  Simon Mathieu ,  Alan Olivero ,  Steven Staben ,  Daniel P. Sutherlin ,  Bing-Yan Zhu

发明人： Tracy Bayliss ,  Irina Chuckowree ,  Adrian Folkes ,  Sally Oxenford ,  Nan Chi Wan ,  Georgette Castanedo ,  Richard Goldsmith ,  Janet Gunzner ,  Tim Heffron ,  Simon Mathieu ,  Alan Olivero ,  Steven Staben ,  Daniel P. Sutherlin ,  Bing-Yan Zhu

IPC分类号： A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61P35/00 ,  A61P35/02 ,  A61K39/00

CPC分类号： A61K31/5377 ,  A61K31/519 ,  C07D413/14 ,  C07D491/04 ,  C07D495/04

摘要： Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is 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.

摘要翻译： 式Ia-d的化合物，其中X是S或O，mor是吗啉基团，R3是单环杂芳基，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的盐可用于调节 脂质激酶（包括PI3K）的活性，以及​​用于治疗脂质激酶介导的疾病如癌症。 公开了使用式Ia-d的化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

公开(公告)号：US07888352B2

公开(公告)日：2011-02-15

申请号：US11951203

申请日：2007-12-05

申请人： Tracy Bayliss ,  Irina Chuckowree ,  Adrian Folkes ,  Sally Oxenford ,  Nan Chi Wan ,  Georgette Castanedo ,  Richard Goldsmith ,  Janet Gunzner ,  Tim Heffron ,  Simon Mathieu ,  Alan Olivero ,  Steven Staben ,  Daniel P. Sutherlin ,  Bing-Yan Zhu

发明人： Tracy Bayliss ,  Irina Chuckowree ,  Adrian Folkes ,  Sally Oxenford ,  Nan Chi Wan ,  Georgette Castanedo ,  Richard Goldsmith ,  Janet Gunzner ,  Tim Heffron ,  Simon Mathieu ,  Alan Olivero ,  Steven Staben ,  Daniel P. Sutherlin ,  Bing-Yan Zhu

IPC分类号： A61K31/535 ,  C07D413/14

CPC分类号： A61K31/5377 ,  A61K31/519 ,  C07D413/14 ,  C07D491/04 ,  C07D495/04

摘要： Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is 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.

摘要翻译： 式Ia-d的化合物，其中X是S或O，mor是吗啉基团，R3是单环杂芳基，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的盐可用于调节 脂质激酶（包括PI3K）的活性，以及​​用于治疗脂质激酶介导的疾病如癌症。 公开了使用式Ia-d的化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种疾病的方法。

公开(公告)号：US20080039459A1

公开(公告)日：2008-02-14

申请号：US11789427

申请日：2007-04-24

申请人： Adrian Folkes ,  Stephen Shuttleworth ,  Sally Oxenford ,  Tim Hancox ,  Tracy Bayliss ,  Georgette Castanedo ,  Richard Goldsmith ,  Janet Gunzner ,  Tim Heffron ,  Kimberly Malesky ,  Simon Mathieu ,  Alan Olivero ,  Daniel Sutherlin ,  Vickie Tsui ,  Shumei Wang ,  Christian Wiesmann ,  Bing-Yan Zhu ,  Jennafer Dotson

发明人： Adrian Folkes ,  Stephen Shuttleworth ,  Sally Oxenford ,  Tim Hancox ,  Tracy Bayliss ,  Georgette Castanedo ,  Richard Goldsmith ,  Janet Gunzner ,  Tim Heffron ,  Kimberly Malesky ,  Simon Mathieu ,  Alan Olivero ,  Daniel Sutherlin ,  Vickie Tsui ,  Shumei Wang ,  Christian Wiesmann ,  Bing-Yan Zhu ,  Jennafer Dotson

IPC分类号： C07D413/14 ,  A61K31/5377 ,  A61P17/00 ,  A61P25/00 ,  A61P3/00 ,  A61P3/10 ,  C12N9/99 ,  A61P31/00 ,  A61P35/00 ,  A61P41/00 ,  A61P9/00

CPC分类号： C07D491/04 ,  C07D495/04

摘要： 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.

摘要翻译： 式Ia和Ib的化合物，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的盐可用于抑制脂质激酶（包括PI3K）和用于治疗由脂质激酶介导的癌症等疾病。 公开了将式Ia和Ib化合物用于体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。