公开(公告)号：US20120135988A1

公开(公告)日：2012-05-31

申请号：US13369941

申请日：2012-02-09

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： A61K31/5377 ,  A61P35/02 ,  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：US08440651B2

公开(公告)日：2013-05-14

申请号：US13030246

申请日：2011-02-18

申请人： Georgette Castanedo ,  Bryan Chan ,  Matthew C. Lucas ,  Brian Safina ,  Daniel P. Sutherlin ,  Zachary Sweeney

发明人： Georgette Castanedo ,  Bryan Chan ,  Matthew C. Lucas ,  Brian Safina ,  Daniel P. Sutherlin ,  Zachary Sweeney

IPC分类号： A61K31/397 ,  A61K31/5377 ,  C07D413/14

CPC分类号： C07D471/04 ,  C07D491/107

摘要： Formula I compounds, including stereoisomers, geometric isomers, 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 disorders, 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化合物，包括立体异构体，几何异构体，互变异构体，代谢物及其药学上可接受的盐，可用于抑制PI3K的δ同种型，以及用于治疗由脂质激酶如炎症，免疫学障碍和癌症介导的病症。 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：US20100305096A1

公开(公告)日：2010-12-02

申请号：US12787613

申请日：2010-05-26

申请人： Georgette Castanedo ,  Bryan Chan ,  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 ,  Bryan Chan ,  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： A61K31/5377 ,  C07D495/04 ,  C07D471/04 ,  C07D473/16 ,  A61K31/541 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61P35/00 ,  A61P37/00 ,  A61P9/00 ,  A61P31/12 ,  A61P29/00 ,  A61P3/00 ,  A61P5/00 ,  A61P25/00

CPC分类号： C07D513/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04

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, or (iv) X1 is CR7 and X2 is O, 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，X 2为S，（ii）X1为CR7，X2为S，（iii）X1为N，X2为NR2，或（iv）X1为CR7， X 2为O，包括立体异构体，互变异构体，代谢物及其药学上可接受的盐，可用于抑制PI3K的δ同种型，以及用于治疗由脂质激酶如炎症，免疫学和癌症介导的病症。 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：US20100305084A1

公开(公告)日：2010-12-02

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： A61K31/5377 ,  C07D513/04 ,  C07D498/10 ,  A61K31/5386 ,  A61K31/555 ,  A61P37/00 ,  A61P35/00 ,  A61P9/00 ,  A61P31/12 ,  A61P29/00 ,  A61P3/00 ,  A61P5/00 ,  A61P25/00

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：US20090318411A1

公开(公告)日：2009-12-24

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： A61K31/5377 ,  C07D473/00

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：US08802670B2

公开(公告)日：2014-08-12

申请号：US11789468

申请日：2007-04-24

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

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

IPC分类号： A61K31/535 ,  C07D413/14

CPC分类号： A61K31/5377 ,  A61K31/551 ,  A61K45/06 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04

摘要： 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.

摘要翻译： 式Ia和Ib的化合物及其立体异构体，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：US20120178736A1

公开(公告)日：2012-07-12

申请号：US13427081

申请日：2012-03-22

申请人： Georgette Castanedo ,  Bryan Chan ,  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 ,  Bryan Chan ,  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： A61K31/5377 ,  C07D487/04 ,  A61P29/00 ,  A61P37/00 ,  A61P37/06 ,  A61P37/08 ,  A61P1/04 ,  A61P1/00 ,  A61P17/00 ,  A61P11/06 ,  A61P19/04 ,  A61P25/00 ,  A61P7/02 ,  A61P7/00 ,  A61P11/00 ,  A61P17/06 ,  A61P19/02 ,  C07D495/04

CPC分类号： C07D513/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04

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, or (iv) X1 is CR7 and X2 is 0, 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，X 2为S，（ii）X1为CR7，X2为S，（iii）X1为N，X2为NR2，或（iv）X1为CR7， X 2为0，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，以及用于治疗由脂质激酶如炎症，免疫学和癌症介导的病症。 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：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：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：US08173650B2

公开(公告)日：2012-05-08

申请号：US12787613

申请日：2010-05-26

申请人： Georgette Castanedo ,  Bryan Chan ,  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 ,  Bryan Chan ,  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： C07D513/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04

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, or (iv) X1 is CR7 and X2 is O, 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，X 2为S，（ii）X1为CR7，X2为S，（iii）X1为N，X2为NR2，或（iv）X1为CR7， X 2为O，包括立体异构体，互变异构体，代谢物及其药学上可接受的盐，可用于抑制PI3K的δ同种型，以及用于治疗由脂质激酶如炎症，免疫学和癌症介导的病症。 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。