公开(公告)号：US20150297595A1

公开(公告)日：2015-10-22

申请号：US14576707

申请日：2014-12-19

Applicant: Portola Pharmaceuticals, Inc.

Inventor： Zhaozhong J. Jia ,  Chandrasekar Venkataramani ,  Wolin Huang ,  Mukund Mehrotra ,  Yonghong Song ,  Qing Xu ,  Shawn M. Bauer ,  Jack W. Rose ,  Brian Kane ,  Anjali Pandey

IPC: A61K31/506

CPC classification number: A61K31/506 ,  C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

Abstract translation: 本发明涉及作为syk激酶抑制剂的式I-V化合物及其互变异构体或其药学上可接受的盐，酯和前药。 本发明还涉及用于制备这种化合物的中间体，这种化合物的制备，含有这种化合物的药物组合物，抑制syk激酶活性的方法，抑制血小板聚集的方法，以及预防或治疗数字的方法 至少部分通过syk激酶活性介导的病症，例如不期望的血栓形成和非霍奇金淋巴瘤。

公开(公告)号：US20130345191A1

公开(公告)日：2013-12-26

申请号：US13841472

申请日：2013-03-15

Applicant: PORTOLA PHARMACEUTICALS, INC.

Inventor： Zhaozhong J. Jia ,  Brian Kane ,  Jack Rose ,  Shawn M. Bauer ,  Yonghong Song ,  Qing Xu ,  Anjali Pandey

IPC: C07D253/075 ,  C07D413/12 ,  C07D405/12 ,  C07D401/12 ,  C07D471/04 ,  C07D413/14 ,  C07D417/12 ,  C07D405/14 ,  C07D401/14 ,  C07D403/14 ,  C07D409/12 ,  C07D403/12 ,  C07D495/04

CPC classification number: C07D253/075 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D495/04

Abstract: Provided are triazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.

Abstract translation: 提供用于抑制Syk激酶的三嗪化合物，用于制备这种化合物的中间体，其制备方法，其药物组合物，抑制Syk激酶活性的方法，以及至少部分地通过Syk激酶活性介导的病症的治疗方法。

公开(公告)号：US09868729B2

公开(公告)日：2018-01-16

申请号：US14561821

申请日：2014-12-05

Applicant: PORTOLA PHARMACEUTICALS, INC.

Inventor： Shawn M. Bauer ,  Anjali Pandey

IPC: A61K31/505 ,  C07D403/12 ,  C07D417/12 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/5355 ,  A61K31/5377 ,  A61K31/551 ,  C07D239/48 ,  C07D401/14 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14 ,  C07D401/12 ,  C07D405/12

CPC classification number: C07D417/12 ,  A61K31/4985 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5355 ,  A61K31/5377 ,  A61K31/551 ,  C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D413/12 ,  C07D413/14

Abstract: Provided are methods of treating inflammatory disorders, autoimmune disorders, or a hematological malignancies using compounds of formula I and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof. Such disorders and conditions include leukemia and Non Hodgkin's Lymphoma.

公开(公告)号：US20140323418A1

公开(公告)日：2014-10-30

申请号：US14360203

申请日：2012-11-23

Applicant: PORTOLA PHARMACEUTICALS, INC.

Inventor： Zhaozhong J. Jia ,  Brian Kane ,  Qing Xu ,  Shawn M. Bauer ,  Yonghong Song ,  Anjali Pandey ,  Ryan Dick

IPC: C07D239/48 ,  C07D403/14 ,  C07H15/26 ,  C07D401/14 ,  C07D413/12 ,  C07D495/04 ,  C07D471/04 ,  C07D405/12 ,  C07D405/14 ,  C07D417/14 ,  C07D403/12 ,  C07D417/12

CPC classification number: C07H15/26 ,  C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07H13/12

Abstract: Provided are pyrimidine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.

Abstract translation: 提供用于抑制Syk激酶的嘧啶化合物，用于制备此类化合物的中间体，其制备方法，其药物组合物，抑制Syk激酶活性的方法，以及至少部分由Syk激酶活性介导的病症的治疗方法。

公开(公告)号：US20140113931A1

公开(公告)日：2014-04-24

申请号：US13841867

申请日：2013-03-15

Applicant: Portola Pharmaceuticals, Inc.

Inventor： Yonghong Song ,  Qing Xu ,  Arvinder Sran ,  Shawn M. Bauer ,  Zhaozhong J. Jia ,  Brian Kane ,  Anjali Pandey

IPC: C07D417/12 ,  C07D471/04 ,  C07D417/14 ,  C07D413/14 ,  C07D401/12 ,  C07D413/12

CPC classification number: C07D417/12 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

Abstract: Provided are picolinamide compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.

Abstract translation: 提供了用于抑制Syk激酶的吡啶酰胺化合物，用于制备这种化合物的中间体，其制备方法，其药物组合物，抑制Syk激酶活性的方法，以及用于至少部分地通过Syk激酶活性介导的病症的治疗方法。

公开(公告)号：US20130131040A1

公开(公告)日：2013-05-23

申请号：US13684462

申请日：2012-11-23

Applicant: Portola Pharmaceuticals, Inc.

Inventor： Yonghong Song ,  Qing Xu ,  Zhaozhong J. Jia ,  Brian Kane ,  Shawn M. Bauer ,  Anjali Pandey

IPC: C07D241/28 ,  C07D403/12 ,  C07D495/04 ,  C07D413/12 ,  C07D405/14 ,  C07D409/14 ,  C07D405/12 ,  C07D403/14 ,  C07D413/14 ,  C07D401/14 ,  C07D401/12 ,  C07D417/12

CPC classification number: C07D241/28 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D513/04

Abstract: Provided are pyrazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.

Abstract translation: 提供用于抑制Syk激酶的吡嗪化合物，用于制备这种化合物的中间体，其制备方法，其药物组合物，抑制Syk激酶活性的方法，以及至少部分地通过Syk激酶活性介导的病症的治疗方法。

公开(公告)号：US09359375B2

公开(公告)日：2016-06-07

申请号：US14458163

申请日：2014-08-12

Applicant: PORTOLA PHARMACEUTICALS, INC.

Inventor： Zhaozhong J. Jia ,  Yonghong Song ,  Qing Xu ,  Brian Kane ,  Shawn M. Bauer ,  Anjali Pandey

IPC: C07D213/74 ,  C07D495/04 ,  C07D209/08 ,  C07D213/82 ,  C07D231/12 ,  C07D231/38 ,  C07D233/56 ,  C07D239/48 ,  C07D249/06 ,  C07D249/08 ,  C07D257/04 ,  C07D261/14 ,  C07D275/03 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07C237/30 ,  C07D209/40 ,  C07D277/42

CPC classification number: C07C237/42 ,  C07C237/30 ,  C07C2601/14 ,  C07D209/08 ,  C07D209/40 ,  C07D213/74 ,  C07D213/82 ,  C07D231/12 ,  C07D231/38 ,  C07D233/56 ,  C07D239/48 ,  C07D249/06 ,  C07D249/08 ,  C07D257/04 ,  C07D261/14 ,  C07D275/03 ,  C07D277/42 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04

Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.

Abstract translation: 本发明涉及作为Syk激酶抑制剂的式I化合物及其药学上可接受的盐，酯和前药。 本发明还涉及用于制备这些化合物的中间体，这种化合物的制备，含有这种化合物的药物组合物，抑制Syk激酶活性的方法，抑制血小板聚集的方法，以及预防或治疗数字的方法 的条件至少部分地由Syk激酶活性介导，例如非霍奇金淋巴瘤。

公开(公告)号：US20150094298A1

公开(公告)日：2015-04-02

申请号：US14561821

申请日：2014-12-05

Applicant: PORTOLA PHARMACEUTICALS, INC.

Inventor： Shawn M. Bauer ,  Zhaozhong J. Jia ,  Mukund Mehrotra ,  Yonghong Song ,  Qing Xu ,  Wolin Huang ,  Chandrasekar Venkataramani ,  Jack W. Rose ,  Anjali Pandey

IPC: C07D417/12 ,  C07D401/12 ,  C07D403/12 ,  C07D239/48 ,  C07D405/12

CPC classification number: C07D417/12 ,  A61K31/4985 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5355 ,  A61K31/5377 ,  A61K31/551 ,  C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D413/12 ,  C07D413/14

Abstract: The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

Abstract translation: 本发明涉及式I-II化合物及其药学上可接受的互变异构体，其盐或其立体异构体，其是syk和/或JAK激酶的抑制剂。 本发明还涉及用于制备这种化合物的中间体，这种化合物的制备，含有这种化合物的药物组合物，抑制性syk和/或JAK激酶活性的方法，抑制血小板聚集的方法以及预防方法 或治疗至少部分通过syk和/或JAK激酶活性介导的许多病症，例如不期望的血栓形成和非霍奇金淋巴瘤。

公开(公告)号：US08952027B2

公开(公告)日：2015-02-10

申请号：US13658730

申请日：2012-10-23

Applicant: Portola Pharmaceuticals, Inc.

Inventor： Zhaozhong J. Jia ,  Chandrasekar Venkataramani ,  Wolin Huang ,  Mukund Mehrotra ,  Yonghong Song ,  Qing Xu ,  Shawn M. Bauer ,  Jack W. Rose ,  Brian Kane ,  Anjali Pandey

IPC: A01N43/54 ,  A61K31/505 ,  C07D239/02 ,  C07D487/04 ,  C07D239/48 ,  C07D471/04 ,  C07D401/12 ,  C07D403/12 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

CPC classification number: A61K31/506 ,  C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

Abstract translation: 本发明涉及作为syk激酶抑制剂的式I-V化合物及其互变异构体或其药学上可接受的盐，酯和前药。 本发明还涉及用于制备这种化合物的中间体，这种化合物的制备，含有这种化合物的药物组合物，抑制syk激酶活性的方法，抑制血小板聚集的方法，以及预防或治疗数字的方法 至少部分通过syk激酶活性介导的病症，例如不期望的血栓形成和非霍奇金淋巴瘤。

公开(公告)号：US08853230B2

公开(公告)日：2014-10-07

申请号：US13717569

申请日：2012-12-17

Applicant: Portola Pharmaceuticals, Inc.

Inventor： Shawn M. Bauer ,  Jack W. Rose ,  Yonghong Song ,  Qing Xu ,  Mukund Mehrotra ,  Wolin Huang ,  Anjali Pandey

IPC: A01N43/54 ,  A61K31/505 ,  C07D403/12 ,  C07D417/14 ,  C07D403/14 ,  C07D401/12 ,  C07D213/82 ,  C07D417/12 ,  C07D239/48

CPC classification number: C07D417/14 ,  C07D213/82 ,  C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D417/12

Abstract: The present invention is directed to compounds of formula I and tautomers and pharmaceutically acceptable salts thereof which are selective inhibitors of JAK. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition JAK activity, and methods to prevent or treat a number of conditions mediated at least in part by JAK activity.

Abstract translation: 本发明涉及作为JAK的选择性抑制剂的式I化合物及其互变异构体及其药学上可接受的盐。 本发明还涉及用于制备这种化合物的中间体，这种化合物的制备，含有这种化合物的药物组合物，抑制JAK活性的方法，以及预防或治疗至少部分地由 JAK活动。