Gilead Sciences, Inc.

Kronos Bio, Inc.

Jennifer R Lo

Scott A Mitchell

Seung H Lee

Zhongdong Zhao

Sundaramoorthi Swaminathan

Kevin S Currie

Peter A Blomgren

Jeffrey E Kropf

Jianjun Xu

Aaron C Schmitt

Jin-Ming Xiong

Jeff A Zablocki

Jayaraman Chandrasekhar

Gary Bruce Phillips

Rao V Kalla

Thao Perry

Musong Kim

Suet Chung Yeung

Julian Andrew Codelli

Mark J Bartlett

Joshua J Van Veldhuizen

Gayatri Balan

Jennifer Alissa Loyer-Drew

John H Conway

Patrick J Salvo

William John Watkins

Chandrasekar Venkataramani

Juan A Guerrero

Zhimin Du

Jennifer Leigh Cosman

Zachary A Kasun

Joshua A Kaplan

Kirk L Stevens

John O Link

Hyung-Jung Pyun

Scott E Lazerwith

Zheng-Yu Yang

Peiyuan Wang

Darryl Kato

Barton W Phillips

Sheila M Zipfel

Gregory Notte

Devan Naduthambi

Jiayao Li

Adam James Schrier

Michael Sangi

Ashley Anne Katana

Julie Farand

Julie A Di Paolo

John E Knox, Jr

Petr Jansa

Christopher T Clark

John Edward Knox, Jr

Astrid Clarke

Nicholas Mai

Daniel H Byun

Jennifer L Cosman Ellis

Megan E Neubig

JinMing Xiong

Nathaniel H Stanley

James L Bachman

Jinming Xiong

Compounds of formula: wherein the variable substituents are defined herein.

KHK inhibitors

The present disclosure relates to compounds that are Syk inhibitors or pharmaceutically acceptable salts or co-crystals thereof, and pharmaceutical compositions thereof, and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, a Syk inhibitor is a crystalline monomesylate salt of 6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo-[1,2-a]pyrazin-8-amine of formula 2:

Crystalline succinate salt of 6-(6-aminopyrazin-2-yl)-n-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine as a Syk inhibitor

The present disclosure relates generally to certain 6-azabenzimidazole compounds, pharmaceutical compositions comprising said compounds, and methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions disclosed herein may be used for the treatment or prevention of diseases, disorders, or infections modifiable by hematopoietic progenitor kinase 1 (HPK1) inhibitors, such as HBV, HIV, cancer, and/or a hyper-proliferative disease.

Substituted 6-azabenzimidazole compounds

The present disclosure relates to compounds that are Syk inhibitors or pharmaceutically acceptable salts or co-crystals thereof, and pharmaceutical compositions thereof, and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, a Syk inhibitor is a crystalline monomesylate salt of 6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo-[1,2-a]pyrazin-8-amine of formula 2: 

Crystalline succinate salt of 6-(6-aminopyrazin-2-yl)-n-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine

Crystalline monomesylate salt of 6-(6-aminopyrazin-2-yl)-n-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine

The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein R, R, R, and Rare as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts or co-crystals thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.

Substituted imidazo[1,2-a]pyrazines as Syk inhibitors

Compounds having the following formula (I) and methods of their use and preparation are disclosed: 

Tank-binding kinase inhibitor compounds

The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein X, X, X, R, R, R, R, and Y are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.

Syk inhibitors

The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein R, R, R, and Rare as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk. In certain embodiments, also disclosed are methods for treating a cancer in a subject (e.g., a human) in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof, in combination with a vinca-alkaloid, or a pharmaceutically acceptable salt thereof.

Growing community of inventors

Branford, CT, United States of America

Jennifer R Lo