公开(公告)号：US08158626B2

公开(公告)日：2012-04-17

申请号：US13006217

申请日：2011-01-13

申请人： Georgette M. Castanedo ,  Janet L. Gunzner ,  Kimberly Malesky ,  Simon Mathieu ,  Alan G. Olivero ,  Daniel P. Sutherlin ,  Shumei Wang ,  Bing-Yan Zhu ,  Irina Chuckowree ,  Adrian Folkes ,  Sally Oxenford ,  Nan Chi Wan

发明人： Georgette M. Castanedo ,  Janet L. Gunzner ,  Kimberly Malesky ,  Simon Mathieu ,  Alan G. Olivero ,  Daniel P. Sutherlin ,  Shumei Wang ,  Bing-Yan Zhu ,  Irina Chuckowree ,  Adrian Folkes ,  Sally Oxenford ,  Nan Chi Wan

IPC分类号： A61K31/5377

CPC分类号： C07D513/04

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：US08158625B2

公开(公告)日：2012-04-17

申请号：US12787608

申请日：2010-05-26

申请人： Georgette Castanedo ,  David Goldstein ,  Rama Kondru ,  Matthew Lucas ,  Wylie Palmer ,  Stephen Price ,  Brian Safina ,  Pascal Pierre Alexandre Savy ,  Eileen Mary Seward ,  Daniel P. Sutherlin ,  Zachary K. Sweeney

发明人： Georgette Castanedo ,  David Goldstein ,  Rama Kondru ,  Matthew Lucas ,  Wylie Palmer ,  Stephen Price ,  Brian Safina ,  Pascal Pierre Alexandre Savy ,  Eileen Mary Seward ,  Daniel P. Sutherlin ,  Zachary K. Sweeney

IPC分类号： A61K31/535 ,  C07D413/14

CPC分类号： C07D495/04 ,  C07D487/04 ,  C07D513/04

摘要： Formula I (Ia and Ib) compounds wherein (i) X1 is N and X2 is S, (ii) X1 is CR7 and X2 is S, (iii) X1 is N and X2 is NR2, (iv) X1 is CR7 and X2 is O, or (v) X1 is CR7 and X2 is NR2, including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological, and cancer. 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）和（Ib）化合物，其中（i）X1为N，X2为S，（ii）X1为CR7，X2为S，（iii）X1为N，X2为NR2，（iv）X1为CR7和X2 是O，或（v）X1是CR7，X2是NR2，包括立体异构体，互变异构体，代谢物和药学上可接受的盐可用于抑制PI3K的δ同种型，以及用于治疗脂质激酶介导的疾病，例如炎症，免疫学 ，和癌症。 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状况中的这种病症的方法。

公开(公告)号：US08158624B2

公开(公告)日：2012-04-17

申请号：US12474613

申请日：2009-05-29

申请人： Georgette Castanedo ,  Irina Chuckowree ,  Adrian Folkes ,  Daniel P. Sutherlin ,  Nan Chi Wan

发明人： Georgette Castanedo ,  Irina Chuckowree ,  Adrian Folkes ,  Daniel P. Sutherlin ,  Nan Chi Wan

IPC分类号： C07D473/34 ,  A61K31/52 ,  C07D473/40 ,  A61P35/00

CPC分类号： C07D473/32

摘要： Purine 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.

摘要翻译： 式I的嘌呤化合物，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，并用于治疗诸如由脂质激酶介导的癌症 。 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：US07928248B2

公开(公告)日：2011-04-19

申请号：US12414403

申请日：2009-03-30

申请人： Steven Do ,  Richard Goldsmith ,  Tim Heffron ,  Aleksandr Kolesnikov ,  Steven Staben ,  Alan G. Olivero ,  Michael Siu ,  Daniel P. Sutherlin ,  Bing-Yan Zhu ,  Paul Goldsmith ,  Tracy Bayliss ,  Adrian Folkes ,  Neil Pegg

发明人： Steven Do ,  Richard Goldsmith ,  Tim Heffron ,  Aleksandr Kolesnikov ,  Steven Staben ,  Alan G. Olivero ,  Michael Siu ,  Daniel P. Sutherlin ,  Bing-Yan Zhu ,  Paul Goldsmith ,  Tracy Bayliss ,  Adrian Folkes ,  Neil Pegg

IPC分类号： C07D333/00

CPC分类号： C07F5/02 ,  A61K31/381 ,  A61K31/4155 ,  A61K31/4196 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/429 ,  A61K31/4365 ,  A61K31/4436 ,  A61K31/496 ,  A61K31/53 ,  C07D495/04 ,  C07D495/14 ,  C07D513/14

摘要： Benzopyran and benzoxepin compounds of Formulas I and II, 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 Formulas I and II 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和II的苯并吡喃和苯并辛菌素化合物，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p110α和PI3K的其他同种型，并用于治疗疾病如癌症 由脂质激酶介导。 公开了使用式I和II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：US07893059B2

公开(公告)日：2011-02-22

申请号：US12236317

申请日：2008-09-23

申请人： Georgette M. Castanedo ,  Janet L. Gunzner ,  Kimberly Malesky ,  Simon Mathieu ,  Alan G. Olivero ,  Daniel P. Sutherlin ,  Shumei Wang ,  Bing-Yan Zhu ,  Irina Chuckowree ,  Adrian Folkes ,  Sally Oxenford ,  Nan Chi Wan

发明人： Georgette M. Castanedo ,  Janet L. Gunzner ,  Kimberly Malesky ,  Simon Mathieu ,  Alan G. Olivero ,  Daniel P. Sutherlin ,  Shumei Wang ,  Bing-Yan Zhu ,  Irina Chuckowree ,  Adrian Folkes ,  Sally Oxenford ,  Nan Chi Wan

IPC分类号： A61K31/5377 ,  C07D413/14

CPC分类号： C07D513/04

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：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：US20090118275A1

公开(公告)日：2009-05-07

申请号：US12236317

申请日：2008-09-23

申请人： Georgette M. Castanedo ,  Janet L. Gunzner ,  Kimberly Malesky ,  Simon Mathieu ,  Alan G. Olivero ,  Daniel P. Sutherlin ,  Shumei Wang ,  Bing-Yan Zhu ,  Irina Chuckowree ,  Adrian Folkes ,  Sally Oxenford ,  Nan Chi Wan

发明人： Georgette M. Castanedo ,  Janet L. Gunzner ,  Kimberly Malesky ,  Simon Mathieu ,  Alan G. Olivero ,  Daniel P. Sutherlin ,  Shumei Wang ,  Bing-Yan Zhu ,  Irina Chuckowree ,  Adrian Folkes ,  Sally Oxenford ,  Nan Chi Wan

IPC分类号： A61K31/5377 ,  C07D513/04 ,  A61P35/00

CPC分类号： C07D513/04

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。