公开(公告)号：US20210147392A1

公开(公告)日：2021-05-20

申请号：US17076356

申请日：2020-10-21

Applicant: Portola Pharmaceuticals, Inc.

Inventor： Anjali Pandey ,  Arvinder Sran ,  Ying Chen ,  Daniele Poggiali ,  Tiziano Fumagalli

IPC: C07D403/12 ,  C07D239/47 ,  C07D239/48 ,  C07D239/42

Abstract: The present disclosure provides processes for the preparation of cerdulatinib, which is of formula I: or a salt thereof. The disclosure also provides intermediates and processes for the preparation of the intermediates useful in the preparation of cerdulatinib or a salt thereof.

公开(公告)号：US20200031804A1

公开(公告)日：2020-01-30

申请号：US16402684

申请日：2019-05-03

Applicant: Portola Pharmaceuticals, Inc.

Inventor： Anjali Pandey ,  Julian Scott Northen ,  Philippe Fernandes ,  Ying Chen ,  Yuelie Lu ,  Sami Karaborni ,  Gus Kodersha

IPC: C07D403/12

Abstract: Forms of cerdulatinib and salts or co-crystals thereof were prepared and characterized in the solid state. Also provided are processes of manufacture and methods of using the forms cerdulatinib and salts or co-crystals thereof.

公开(公告)号：US20180237381A1

公开(公告)日：2018-08-23

申请号：US15753768

申请日：2016-08-19

Applicant: Portola Pharmaceuticals, Inc.

Inventor： Thomas E. Barta ,  Jonathan William Bourne ,  Kyle D. Monroe ,  Michael M. Muehlemann ,  Anjali Pandey ,  Simeon Bowers

IPC: C07C237/20 ,  C07D213/64

Abstract: This invention is related to the field of PCSK9 biology and the composition and methods of use of small organic compounds as ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small organic compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small organic compound ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small organic compound ligands that can raise LDL levels.

公开(公告)号：US09644195B2

公开(公告)日：2017-05-09

申请号：US14723395

申请日：2015-05-27

Applicant: Portola Pharmaceuticals, Inc.

Inventor： Anjali Pandey ,  Jack W. Rose

IPC: C07D221/06 ,  C12N9/64 ,  C07D213/72 ,  B01J20/26 ,  B01J20/286 ,  C07D213/75

CPC classification number: C12N9/6432 ,  B01J20/267 ,  B01J20/286 ,  B01J2220/80 ,  C07D213/72 ,  C07D213/75 ,  C12N9/6424 ,  C12Y304/21006

Abstract: Disclosed herein are compounds, compositions, methods and kits for purifying a serine protease and serine proteases purified with the compounds, compositions and methods.

公开(公告)号：US20150352194A1

公开(公告)日：2015-12-10

申请号：US14762098

申请日：2013-03-13

Applicant: PORTOLA PHARMACEUTICALS, INC.

Inventor： Genmin Lu ,  Uma Sinha ,  Mark Karbarz ,  Anjali Pandey ,  Pamela B. Conley

IPC: A61K38/48 ,  A61K47/48 ,  A61K45/06

CPC classification number: A61K38/37 ,  A61K38/4846 ,  A61K45/06 ,  A61K47/50 ,  C12N9/6432 ,  C12Y304/21006 ,  A61K2300/00

Abstract: The present disclosure relates to compositions and methods for the treatment of bleeding disorders, such as hemophilia A, hemophilia B, von Willebrand (vWF) disease, and factor XII deficiency, by reducing the circulating concentration of tissue factor pathway inhibitor (TFPI), with a factor Xa derivative.

Abstract translation: 本公开涉及通过降低组织因子途径抑制剂（TFPI）的循环浓度来治疗出血性疾病如血友病A，血友病B，血管性血友病（vWF）疾病和因子XII缺乏症的组合物和方法， 一个因子Xa导数。

公开(公告)号：US20150337285A1

公开(公告)日：2015-11-26

申请号：US14723395

申请日：2015-05-27

Applicant: Portola Pharmaceuticals, Inc.

Inventor： Anjali Pandey ,  Jack W. Rose

IPC: C12N9/64 ,  B01J20/26 ,  B01J20/286 ,  C07D213/72

CPC classification number: C12N9/6432 ,  B01J20/267 ,  B01J20/286 ,  B01J2220/80 ,  C07D213/72 ,  C07D213/75 ,  C12N9/6424 ,  C12Y304/21006

Abstract: Disclosed herein are compounds, compositions, methods and kits for purifying a serine protease and serine proteases purified with the compounds, compositions and methods.

Abstract translation: 本文公开了用于纯化丝氨酸蛋白酶和用化合物，组合物和方法纯化的丝氨酸蛋白酶的化合物，组合物，方法和试剂盒。

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：US20190337930A1

公开(公告)日：2019-11-07

申请号：US16402880

申请日：2019-05-03

Applicant: Portola Pharmaceuticals, Inc.

Inventor： Anjali Pandey ,  Arvinder Sran ,  Ying Chen ,  Daniele Poggiali ,  Tiziano Fumagalli

IPC: C07D403/12

Abstract: The present disclosure provides processes for the preparation of cerdulatinib, which is of formula I: or a salt thereof. The disclosure also provides intermediates and processes for the preparation of the intermediates useful in the preparation of cerdulatinib or a salt thereof.

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.