公开(公告)号：US09487533B2

公开(公告)日：2016-11-08

申请号：US11951189

申请日：2007-12-05

Applicant: 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

Inventor： 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: C07D491/048 ,  C07D495/04

CPC classification number: C07D491/048 ,  C07D495/04

Abstract: 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：US08802670B2

公开(公告)日：2014-08-12

申请号：US11789468

申请日：2007-04-24

Applicant: 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

Inventor： 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: A61K31/535 ,  C07D413/14

CPC classification number: A61K31/5377 ,  A61K31/551 ,  A61K45/06 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04

Abstract: 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.

Abstract translation: 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：US08691847B2

公开(公告)日：2014-04-08

申请号：US13612597

申请日：2012-09-12

Applicant: Bing-Yan Zhu ,  Penglie Zhang ,  Lingyan Wang ,  Wenrong Huang ,  Erick A. Goldman ,  Wenhao Li ,  Jingmei Zuckett ,  Yonghong Song

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

IPC: C07D401/02 ,  A61K31/44

CPC classification number: 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

Abstract: 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.

Abstract translation: 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：US20130172310A1

公开(公告)日：2013-07-04

申请号：US13612597

申请日：2012-09-12

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

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

IPC: C07D213/75 ,  C07D401/12

CPC classification number: 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

Abstract: 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.

公开(公告)号：US08377974B2

公开(公告)日：2013-02-19

申请号：US13213927

申请日：2011-08-19

Applicant: Bing-Yan Zhu ,  Shawn M. Bauer ,  Zhaozhong J. Jia ,  Gary D. Probst ,  Yanchen Zhang

Inventor： Bing-Yan Zhu ,  Shawn M. Bauer ,  Zhaozhong J. Jia ,  Gary D. Probst ,  Yanchen Zhang ,  Robert M. Scarborough

IPC: A61K31/4025 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/4196 ,  C07D233/64 ,  C07D231/12 ,  C07D207/34

CPC classification number: C07D413/14 ,  C07D333/38 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

Abstract: 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：US20120178733A1

公开(公告)日：2012-07-12

申请号：US13213927

申请日：2011-08-19

Applicant: Bing-Yan Zhu ,  Shawn M. Bauer ,  Zhaozhong J. Jia ,  Gary D. Probst ,  Yanchen Zhang ,  Robert M. Scarborough

Inventor： Bing-Yan Zhu ,  Shawn M. Bauer ,  Zhaozhong J. Jia ,  Gary D. Probst ,  Yanchen Zhang ,  Robert M. Scarborough

IPC: A61K31/422 ,  C07D413/14 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/4545 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/506 ,  C07D417/14 ,  A61K31/541 ,  A61K31/553 ,  A61K31/551 ,  C07D409/14 ,  C07D409/12 ,  A61K31/4192 ,  C07D417/12 ,  A61K31/427 ,  A61K31/4178 ,  A61K31/4709 ,  A61P9/00 ,  A61P9/10 ,  A01N1/02 ,  A61P7/02 ,  C07D413/12

CPC classification number: C07D413/14 ,  C07D333/38 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

Abstract: 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.

Abstract translation: 本发明涉及由式I表示的化合物及其作为因子Xa抑制剂的药学上可接受的盐，溶剂合物，水合物和前药。 本发明还涉及用于制备这种化合物的中间体，含有这些化合物的药物组合物，预防或治疗多种不想要的血栓形成特征的病症的方法以及抑制血液样品凝固的方法。

公开(公告)号：US20110105464A1

公开(公告)日：2011-05-05

申请号：US12916125

申请日：2010-10-29

Applicant: 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

Inventor： 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: A61K31/5377 ,  A61P35/00 ,  A61P35/02 ,  A61P29/00 ,  A61P3/10 ,  A61P9/00

CPC classification number: C07D491/04 ,  C07D495/04

Abstract: 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.

Abstract translation: 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：US07749994B2

公开(公告)日：2010-07-06

申请号：US11503405

申请日：2006-08-14

Applicant: Thomas E. Rawson ,  Brian Safina ,  Jennafer Dotson ,  Aihe Zhou ,  Ignacio Aliagas-Martin ,  Jason Halladay ,  Jun Liang ,  Matthias Rueth ,  Bing-Yan Zhu ,  Frederick Brookfield ,  Michael Prime ,  Birong Zhang ,  Jun M. Li

Inventor： Thomas E. Rawson ,  Brian Safina ,  Jennafer Dotson ,  Aihe Zhou ,  Ignacio Aliagas-Martin ,  Jason Halladay ,  Jun Liang ,  Matthias Rueth ,  Bing-Yan Zhu ,  Frederick Brookfield ,  Michael Prime ,  Birong Zhang ,  Jun M. Li

IPC: A61K31/55 ,  A61K31/538 ,  A61K31/424 ,  A61K31/4188 ,  C07D498/22

CPC classification number: C07D487/04 ,  C07D491/04

Abstract: The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula I wherein A, X, Y, Z, Ra, Rb, Rc, R1, R2, R3 and m are defined herein.

Abstract translation: 本发明提供新的激酶抑制剂，其可用作例如治疗恶性肿瘤的治疗剂，其中化合物具有通式I，其中A，X，Y，Z，R a，R b，R c，R 1，R 2，R 3和m定义 这里。

公开(公告)号：US20100144732A1

公开(公告)日：2010-06-10

申请号：US12520194

申请日：2007-12-13

Applicant: Elaine B. Krueger ,  Thomas E. Rawson ,  Daniel J. Burdick ,  Jun Liang ,  Bing-Yan Zhu

Inventor： Elaine B. Krueger ,  Thomas E. Rawson ,  Daniel J. Burdick ,  Jun Liang ,  Bing-Yan Zhu

IPC: A61K31/5377 ,  A61K31/505 ,  C07D413/02 ,  C07D239/02 ,  A61P35/04

CPC classification number: C07D239/48

Abstract: The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula I wherein Q, X, Y, Z, R1, R2, R4, m and n are as defined herein.

Abstract translation: 本发明提供新的激酶抑制剂，其可用作例如治疗恶性肿瘤的治疗剂，其中化合物具有通式I，其中Q，X，Y，Z，R 1，R 2，R 4，m和n如本文所定义。

公开(公告)号：US20080242665A1

公开(公告)日：2008-10-02

申请号：US11951203

申请日：2007-12-05

Applicant: 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

Inventor： 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: A61K31/5377 ,  C07D495/04 ,  A61P35/04

CPC classification number: A61K31/5377 ,  A61K31/519 ,  C07D413/14 ,  C07D491/04 ,  C07D495/04

Abstract: 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.

Abstract translation: 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。