Portola Pharmaceuticals, Inc.

Millennium Pharmaceuticals Limited

Srx Cardio, LLC

Alexion Pharmaceuticals, Inc.

Kyowa Hakko Kogyo Co., Ltd.

Sudo Biosciences Limited

Ortho-mcneil Pharmaceutical Corp.

Ferro Therapeutics, Inc.

Other

Millenium Pharmaceuticals, Inc.

Kyowa Hakko Kirin Co., Limited

Anjali Pandey

Yonghong Song

Robert M Scarborough

Shawn M Bauer

Qing Xu

Zhaozhong Jon Jia

Mukund Mehrotra

Jack W Rose

Wolin Huang

Brian Kane

Chandrasekar Venkataramani

Thomas E Barta

Simeon Bowers

Jonathan William Bourne

Michael Mark Muehlemann

Kyle D Monroe

Shinichi Ide

Eiji Tsukuda

Yuji Nomoto

Michio Ichimura

Shoji Oda

Kenji Matsuno

Athisayamani Jeyaraj Duraiswamy

Junko Sasaki

Meenakshi S Venkatraman

James P Kanter

James Robinson

Gregory Dietsch

Ying Chen

Bruce E Maryanoff

Xiaoming Zhang

Uma Sinha

Julian Scott Northen

Han-Cheng Zhang

Sami Karaborni

Arvinder Sran

Zhiguo Jake Song

Philippe Fernandes

Chun Jiang

Bhaskar Chaudhuri

Gregory Coffey

David R Phillips

Genmin Lu

Patrick Andre

Pamela B Conley

Louisa Jane Quegan

Jiang Zhu

Mark Karbarz

Junko Irie

Seetharaman Manojveer

Sukesh Kalva

Mahesh Thakkar

Carroll Scarborough, Legal Representative

Biswajit Kalita

Ruihong Chen

Yuelie Lu

Gus Kodersha

Emilia P T Leitao

Jose Rato

Daniele Poggiali

Tiziano Fumagalli

Vincent R Capodanno

John J G Mullins

Andrew Steele

Richard G Ball

John T Curnutte

Hilary Cannon

Carroll Anna Crew, Legal Representative

Matthew Birrell

Janet Leeds

Glenn Michelson

Liam Corcoran

Michael McNevin

Itzia Zoraida Arroyo

Robert M Wenslow

Eric L Margelefsky

Timothy K Maher

Urvish Pandya

Jack Rose

Emilia P Leitao

Craig M Grant

Michael Mcnevin

M Scarborough Robert

James Kanter

Kenji Kyowa Hakko Kogyo Co Ltd Matsuno

Michio Kyowa Hakko Kogyo Co Ltd Ichimura

Yugi Kyowa Hakko Kogyo Co Ltd Nomoto

Eiji Kyowa Hakko Kogyo Co Ltd Tsukida

Junko Kyowa Hakko Kogyo Co Ltd Irie

Shoji Kyowa Hakko Kogyo Co Ltd Oda

Shinichi Kyowa Hakko Kogyo Co Ltd Ide

Provided herein are compositions and methods for treating a relapsed or refractory hematologic cancer in a human patient in need thereof. The methods entail administering to the patient a daily dose of about 10 mg to about 75 mg of cerdulatinib or a pharmaceutically acceptable salt thereof, wherein the patients suffer one or more of a B-cell malignancy, chronic lymphocytic leukemia (CLL), follicular lymphoma (FL), diffuse large B-cell lymphoma (DLBCL) or other transformed FL and/or have relapsed or not responded to a prior chemotherapy.

Cerdulatinib for the treatment of b-cell malignancies

Described herein are compounds of Formula (I) that are TYK2 inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of TYK2 activity.

Substituted pyridines, pyridazines, pyrimidines, and 1,2,4-triazines as TYK2 inhibitors

The present disclosure relates to novel compounds capable of binding to PCSK9, thereby modulating PCSK9 biological activity. Also provided are compositions comprising these compounds, methods of preparing the compounds, and methods for use of the compounds in the treatment of PCSK9-related conditions and diseases.

Compounds for the modulation of proprotein convertase subtilisin/kexin type 9 (PCSK9)

Described herein are compounds of Formula (XIV) that are TYK2 inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of TYK2 activity.

Substituted pyridines and pyridazines as TYK2 inhibitors

Described herein are compounds of Formula (XIII) that are TYK2 inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of TYK2 activity.

Substituted pyridines, pyridazines, and pyrimidines as TYK2 inhibitors

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 dysfunctions; thus, there is also utility for small organic compound ligands and can raise LDL levels.

Composition and methods of use of tetrahydroisoquinoline small molecules to bind and modulate PCSK9 protein activity

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.

Phenylalanine small organic compounds to directly modulate PCSK9 protein activity

Phenylpiperazine proprotein convertase subtilisin/kexin type 9 (PCSK9) modulators and their use

The present disclosure relates to novel compounds, methods, and compositions capable of binding to PCSK9, thereby modulating PCSK9 proprotein convertase enzyme activity, for treatment of a disease or condition mediated, at least in part, by PCSK9. The compounds of the disclosure include compounds Formula (I).

Compounds for binding proprotein convertase subtilisin/kexin type 9

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.

Solid forms of Cerdulatinib

Described herein are compounds of Formula (XVII) that are TYK2 inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of Using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of TYK2 activity. 

The present invention is directed to methods of treating multiple myeloma by administering a compound of Formula (I) or pharmaceutically acceptable salt thereof.

Inhibitors of protein kinases

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.

Synthesis of cerdulatinib

Compositions and methods for treating lymphoma, in particular, T-cell lymphoma and follicular lymphoma, in a human patient are provided. The methods entail administering to the patient an effective amount of cerdulatinib.

Methods for treating lymphoma

This present disclosure relates to compounds with ferroptosis inducing activity, a method of treating a subject with cancer with the compounds, and combination treatments with a second therapeutic agent.

Compounds and methods of use

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Fremont, CA, United States of America

Anjali Pandey