Rigel Pharmaceuticals, Incorporated

Myokardia, Inc.

Alexion Pharmaceuticals, Inc.

Portola Pharmaceuticals, Inc.

Arvinder Sran

Rajinder Paul Singh

David Carroll

Hui Li

Somasekhar Bhamidipati

Ankush Argade

Kin Tso

Sambaiah Thota

Vanessa Taylor

Robin Cooper

Jeffrey Clough

Holger Keim

Brian Wong

Robert S McDowell

Yonghong Song

Johan D Oslob

Danielle Aubele

Esteban Masuda

Robert G Anderson

Brian Kane

Marc Evanchik

Hector Rodriguez

Jonathan Charles Fox

Min Zhong

Jae Kim

Puping Lu

Anjali Pandey

Ying Chen

Daniele Poggiali

Tiziano Fumagalli

Robert Mcdowell

Johan Oslob

Donald G Payan

Simon Shaw

John Yudhistir Ramphal

Sarkiz D Issakani

Vadim Markovtsov

Jianing Huang

Pu-Ping Lu

Lyuben Tsvetkov

Robert Anderson

Provided are novel pyrimidine dione compounds and pharmaceutically acceptable salts thereof, that are useful for the treatment of hypertrophic cardiomyopathy (HCM) and conditions associated with left ventricular hypertrophy or diastolic dysfunction. The synthesis and characterization of the compounds and pharmaceutically acceptable salts thereof, are described, as well as methods for treating HCM and other forms of heart disease.

Pyrimidinedione compounds

The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.

Compositions and methods for inhibition of the JAK pathway

The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful.

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

The present invention provides novel 4-methylsulphone-substituted piperidine urea compounds that are useful for the treatment of dilated cardiomyopathy (DCM) and conditions associated with left and/or right ventricular systolic dysfunction or systolic reserve. The synthesis and characterization of the compounds is described, as well as methods for treating DCM and other forms of heart disease.

4-methylsulfonyl-substituted piperidine urea compounds

Disclosed are sulfonamidoquinoline compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein R, R, Rand Rare as described herein. In certain embodiments, a compound disclosed herein inhibits ubiquitination, and can be used to treat disease by blocking the degradation of tumor suppressors.

Ubiquitination inhibitors

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Fremont, CA, United States of America

Arvinder Sran