Vertex Pharmaceuticals, Inc.

Amgen Inc.

Gilead Connecticut, Inc.

Sirtris Pharmaceuticals, Inc.

Revolution Medicines, Inc.

Warp Drive Bio, Inc.

Other

David M Armistead

Jeffrey O Saunders

Perry M Novak

Steven M Ronkin

Randy Scott Bethiel

Michael C Badia

Catharine A Frank

Guy W Bemis

Jean E Bemis

Joseph J Nunes

Joshua S Boger

Keith P Wilson

Michael D Sintchak

Mark Andrew Fleming

Gregory Lawrence Verdine

Joseph L Kim

Brian Yichiun Chow

David W White

Mathew Edward Sowa

Deborah Palestrant

Chris K Varma

Roger D Tung

Pui Yee Ng

Kevin S Currie

Scott A Mitchell

Peter A Blomgren

Jeffrey E Kropf

Chi B Vu

Jianjun Xu

Jill C Milne

Seung H Lee

Zhongdong Zhao

Jeremy S Disch

Douglas Gregory Stafford

Gregory J Habgood

Roger Xie

Harold V Meyers

Antonio J M Barbosa, Jr

Thomas Salzmann

Leticia M Toledo-Sherman

Soumya Mitra

James P Harding

Vinod Francis Patel

Daniel Elbaum

Lucian V DiPietro

Stephanie Geuns-Meyer

John Allan Thomson

James P Griffith

Eunice E Kim

David A Pearlman

Matthew James Fitzgibbon

Doug Naegele

Xiaotian Zhu

John Laird Buchanan

Matthew W Harding

Antonio J Barbosa

Teresa L Marshall

Catherine A Frank

Douglas G Stafford

Jr Antonio J Barbosa

Disclosed herein are methods for identifying novel drug candidates.

Identifying new therapeutic agents

Provided are imidazopyrazine compounds, particularly including 6-(benzo[d]thiazol-5-yl)-N-(3,4-dimethoxyphenyl)imidazo[1,2-a]pyrazin-8-amine, structure below, and methods and formulations for their use in inhibiting Spleen Tyrosine Kinase in treating conditions including B-cell lymphomas or leukemias and inflammatory conditions: 

6-(benzo[d]thiazol-5-yl)-n-(3,4-dimethoxyphenyl)imidazo[1,2-a]pyrazin-8-amine

Certain imidazopyrazines having the structure of formula (I): or pharmaceutically acceptable salts thereof, wherein R, R, R, Rand Rare as defined herein, and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.

Imidazopyrizine syk inhibitors

Certain imidazopyrazines of Formula (I) and pharmaceutical compositions thereof are provided herein.  Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.

Imidazopyrazine Syk inhibitors

Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.

Sirtuin modulating compounds

Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benfit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.

The present invention relates to a data storage medium encoded with the corresponding structure coordinates of molecules and molecular complexes which comprise the active site binding pockets of IMPDH. Such data storage material is capable of displaying such molecules and molecular complexes, or their structural homologues, as a graphical three-dimensional representation on a computer screen. This invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. In addition, this invention relates to methods of using the structure coordinates to screen and design compounds, including inhibitory compounds, that bind to IMPDH or homologues thereof. This invention also relates to molecules and molecular complexes which comprise the active site binding pockets of IMPDH or close structural homologues of the active site binding pockets. This invention also relates to compounds and pharmaceutical compositions which are inhibitors of IMPDH.

Crystals of inosine monophosphate dehydrogenase/oxidized inosine monophosphate thiomidate intermediate/mycophenolic acid (IIMPDH/XMP*/MPA)

The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.

Inhibitors of IMPDH enzyme

The invention relates to inhibitors of kinases, compositions comprising the inhibitors, and methods of using the inhibitors and inhibitor compositions. The inhibitors and compositions comprising them are useful for treating disease or disease symptoms. The invention also provides for methods of making kinase inhibitor compounds, methods of inhibiting kinase activity, and methods for treating disease or disease symptoms.

Kinase inhibitors

Methods of using the structure coordinates of molecules comprising an IMPDH-like binding pocket

The invention relates to inhibitors of enzymes that bind to ATP or GTP and/or catalyze phosphoryl transfer, compositions comprising the inhibitors, and methods of using the inhibitors and inhibitor compositions. The inhibitors and compositions comprising them are useful for treating disease or disease symptoms. The invention also provides for methods of making phosphoryl transferase inhibitor compounds, methods of inhibiting phosphoryl transferase activity, and methods for treating disease or disease symptoms.

Growing community of inventors

Sudbury, MA, United States of America

David M Armistead