Abbott Laboratories Corporation

Novartis International Pharmaceutical, Ltd.

Novartis Ag

Neurogen Corporation

Peter Hrnciar

Jun Yuan

George D Maynard

Gavin C Hirst

David J Calderwood

Qin Guo

Michael Michaelides

Steven K Davidsen

Paul Rafferty

Michael L Curtin

Robin R Frey

Howard Robin Heyman

Kelly Mullen

Carol K Wada

Andrew Burchat

Heather M Davis

Patrick Betschmann

Melanie A Muckey

Alan J Hutchison

Bertrand Leo Chenard

Kyungae Lee

Nian Liu

Zihong Guo

Kurt Ritter

Richard W Dixon

David Wayne Borhani

Andreas Loew

Adelaine Leung

Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds analogues of the formula: wherein R, R, R, E, Z, Z, Z, and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds of the invention bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds, which are useful as probes for the localization of C5a receptors.

Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds

Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

Thienopyridine and furopyridine kinase inhibitors

3-substituted-6-aryl pyridines of Formula I are provided: wherein R, R, R, R, R, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.

3-substituted-6-aryl pyridines

The present invention relates to polypeptides which comprise the ligand binding domain of Lck, crystalline forms of these polypeptides, and the use of these crystalline forms to determine the three dimensional structure of the catalytic domain of Lck. The invention also relates to the use of the three dimensional structure of the Lck catalytic domain both alone, or in complex with inhibitors, in methods of designing and/or identifying potential inhibitors of Lck activity, for example, compounds which inhibit the binding of a native substrate to the Lck catalytic domain. The invention also relates to the use of the three dimensional structure of the Lck catalytic domain both alone, or in complex with inhibitors, in methods of designing and/or identifying potential selective inhibitors of Lck activity, for example, compounds which inhibit the binding of a native substrate to the Lck catalytic domain selectively.

Method of identifying inhibitors of Lck

3-substituted-6-aryl pyridines of Formula I are provided: wherein R, R, R, R, R, A and Ar are defined herein. Such compounds are ligands of C5a receptor. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.

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Hamden, CT, United States of America

Peter Hrnciar