公开(公告)号：US20140221405A1

公开(公告)日：2014-08-07

申请号：US13956251

申请日：2013-07-31

Applicant: Portola Pharmaceuticals, Inc.

Inventor： Robert M. Scarborough ,  Hans-Michael Jantzen ,  Wolin Huang ,  David M. Sedlock ,  Charles K. Marlowe ,  Kim A. Kane-MaGuire

IPC: C07D487/04 ,  C07D409/12 ,  C07D471/04

CPC classification number: C07D487/04 ,  C07D209/48 ,  C07D239/22 ,  C07D239/48 ,  C07D239/50 ,  C07D239/96 ,  C07D333/34 ,  C07D333/62 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D495/04 ,  C07D521/00

Abstract: Novel compounds of formulae (I) to (VII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylfulfonamide derivatives which are effective platelet ADF receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.

Abstract translation: 式（I）至（VII）的新型化合物，其更具体地包括作为有效的血小板ADF受体抑制剂的磺酰脲衍生物，磺酰基硫脲衍生物，磺酰基胍衍生物，磺酰氰基胍衍生物，硫代酰基磺酰胺衍生物和酰基呋喃酰胺衍生物。 这些衍生物可用于各种药物组合物中，并且对于预防和/或治疗心血管疾病，特别是与血栓形成有关的疾病特别有效。 本发明还涉及一种用于预防或治疗哺乳动物血栓形成的方法，包括施用治疗有效量的式（I）至（VIII）化合物或其药学上可接受的盐的步骤。

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：US09579320B2

公开(公告)日：2017-02-28

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 ,  C07D487/04 ,  C07D471/04 ,  C07D239/48 ,  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：US20130165431A1

公开(公告)日：2013-06-27

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: C07D487/04 ,  C07D403/12 ,  C07D471/04 ,  C07D401/12 ,  C07D413/12 ,  C07D239/48 ,  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.

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。

公开(公告)号：US20130137673A1

公开(公告)日：2013-05-30

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: C07D417/14 ,  C07D417/12 ,  C07D401/12 ,  C07D405/12 ,  C07D239/48 ,  C07D403/12

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。

公开(公告)号：US10533001B2

公开(公告)日：2020-01-14

申请号：US15828154

申请日：2017-11-30

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: C07D239/28 ,  C07D403/02 ,  C07D413/02 ,  C07D279/12 ,  A61K31/506 ,  A61K31/501 ,  A61K31/5377 ,  A61K31/551 ,  A61K31/541 ,  C07D417/12 ,  A61K31/4985 ,  A61K31/505 ,  A61K31/5355 ,  C07D239/48 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14 ,  C07D401/12 ,  C07D405/12

Abstract: The present invention is directed to topical pharmaceutical compositions of Formula (If) or pharmaceutically acceptable salt thereof, which act as inhibitors of syk and/or JAK kinase activity. The described topical pharmaceutical compositions are useful in preventing or treating a number of conditions mediated at least in part by syk and/or JAK kinase activity.

公开(公告)号：US20140031361A1

公开(公告)日：2014-01-30

申请号：US13916926

申请日：2013-06-13

Applicant: Portola Pharmaceuticals, INC.

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

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

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。