Boehringer Ingelheim Pharmaceuticals, Inc.

Boehringer Ingelheim International Gmbh

Scott E Jakes

Joachim Heider

Mark R Player

James M Rinker

Charles Lawrence Cywin

Bao-Ping Zhao

Michael Peter Winters

Mark A Bobko

Renee L Des Jarlais

Anthony S Prokopowicz

Jessi Marie Wildeson

Mark E Labadia

Martha Priscilla Brown

Jeffrey David Yingling

Donna Terenzio

Jessi Wildeson Jones

Disclosed are compounds of formula (I): wherein R, R, Rand Rare defined herein, which are useful as inhibitors SYK kinase and are thus useful for treating diseases resulting from inappropriate mast cell activation, which include allergic and inflammatory diseases. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.

1,6 Naphthridines useful as inhibitors of SYK kinase

1,6 naphthyridines useful as inhibitors of SYK kinase

The invention provides methods relating to a screening assay format that can be applied to broad members of the protein kinase gene family. The assay uses a series of labeled, active site probes described herein that can be displaced by an inhibitor agent. The Kfor the inhibitor compound is derived based on the Kof the probe for the kinase and the dose response of the inhibitor agent. The invention also provides active site probes suitable for use with the screening method.

Fluorescent probes for use in protein kinase inhibitor binding assay

This invention relates to screening assay methods that can be applied to broad members of the protein kinase gene family and are useful in the detection and evaluation of kinase inhibitors.

Methods for determining phosphoryltransferase activity using adenosine 5'-triphosphate (ATP)-gamma-S

1,6 Naphthyridines useful as inhibitors of SYK kinase

The invention provides methods relating to a novel screening assay format that can be applied to broad members of the protein kinase gene family. The assay uses a series of labeled, active site probes described herein that can be displaced by an inhibitor agent. The Kfor the inhibitor compound is derived based on the Kof the probe for the kinase and the dose response of the inhibitor agent. The invention also provides active site probes suitable for use with the screening method.

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Southbury, CT, United States of America

Scott E Jakes