公开(公告)号：US20060100193A1

公开(公告)日：2006-05-11

申请号：US11158274

申请日：2005-06-20

申请人： Bing-Yan Zhu ,  Shawn Bauer ,  Zhaozhong Jia ,  Gary Probst ,  Yanchen Zhang ,  Robert Scarborough

发明人： Bing-Yan Zhu ,  Shawn Bauer ,  Zhaozhong Jia ,  Gary Probst ,  Yanchen Zhang ,  Robert Scarborough

IPC分类号： A61K31/5377 ,  A61K31/506 ,  A61K31/496 ,  A61K31/453 ,  A61K31/4745 ,  A61K31/422 ,  A61K31/397 ,  A61K31/381 ,  C07D413/02 ,  C07D409/02

CPC分类号： C07D413/14 ,  C07D333/38 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

摘要： The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.

公开(公告)号：US20110172216A1

公开(公告)日：2011-07-14

申请号：US12865644

申请日：2009-01-29

申请人： Jennafer Dotson ,  Tim Heffron ,  Alan Olivero ,  Daniel P. Sutherlin ,  Shumei Wang ,  Bing-Yan Zhu ,  Irina Chuckowree ,  Adrian Folkes ,  Nan Chi Wan

发明人： Jennafer Dotson ,  Tim Heffron ,  Alan Olivero ,  Daniel P. Sutherlin ,  Shumei Wang ,  Bing-Yan Zhu ,  Irina Chuckowree ,  Adrian Folkes ,  Nan Chi Wan

IPC分类号： A61K31/541 ,  C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  C12N9/99 ,  A61P35/00 ,  A61P35/02 ,  A61P29/00 ,  A61P37/02 ,  A61P31/12 ,  A61P3/10 ,  A61P7/00 ,  A61P37/04 ,  A61P9/00 ,  A61P1/16

CPC分类号： C07D487/04 ,  C07D519/00

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 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，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，并用于治疗由脂质激酶介导的癌症等疾病。 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：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：US20110112085A1

公开(公告)日：2011-05-12

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 ,  A61P35/00 ,  A61P35/02

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：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：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：US08518977B2

公开(公告)日：2013-08-27

申请号：US13247937

申请日：2011-09-28

申请人： Bing-Yan Zhu ,  Penglie Zhang ,  Lingyan Wang ,  Wenrong Huang ,  Erick A. Goldman ,  Wenhao Li ,  Jingmei Zuckett ,  Yonghong Song ,  Robert M. Scarborough

发明人： Bing-Yan Zhu ,  Penglie Zhang ,  Lingyan Wang ,  Wenrong Huang ,  Erick A. Goldman ,  Wenhao Li ,  Jingmei Zuckett ,  Yonghong Song ,  Robert M. Scarborough

IPC分类号： C07D213/75 ,  A61K31/44

CPC分类号： A61K31/44 ,  A61K9/20 ,  A61K9/2013 ,  A61K9/2054 ,  A61K9/48 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/616 ,  A61K45/06 ,  A61K2201/094 ,  C07C237/42 ,  C07C255/60 ,  C07C257/18 ,  C07C259/18 ,  C07C311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C317/44 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D217/22 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D249/08 ,  C07D295/125 ,  C07D333/38 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14

摘要： Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.

摘要翻译： 描述了具有抗哺乳动物因子Xa活性的新型苯甲酰胺化合物，包括其药学上可接受的异构体，盐，水合物，溶剂合物和前药衍生物。 还描述了含有这些化合物的组合物。 化合物和组合物在体外或体内可用于预防或治疗凝血障碍。

公开(公告)号：US07285565B2

公开(公告)日：2007-10-23

申请号：US11035767

申请日：2005-01-14

申请人： Bing-Yan Zhu ,  Penglie Zhang ,  Lingyan Wang ,  Wenrong Huang ,  Erick A. Goldman ,  Wenhao Li ,  Jingmei Zuckett ,  Yonghong Song ,  Robert M. Scarborough

发明人： Bing-Yan Zhu ,  Penglie Zhang ,  Lingyan Wang ,  Wenrong Huang ,  Erick A. Goldman ,  Wenhao Li ,  Jingmei Zuckett ,  Yonghong Song ,  Robert M. Scarborough

IPC分类号： C07D213/02 ,  A61K31/44

CPC分类号： C07D213/75 ,  C07C311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C317/44 ,  C07D213/81 ,  C07D213/82 ,  C07D217/22 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D333/38 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14

摘要： Novel benzamide compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.

摘要翻译： 公开了与哺乳动物因子Xa有活性的新型苯甲酰胺化合物，其盐和与其有关的组合物。 该化合物在体外或体内可用于预防或治疗凝血障碍。

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：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。