Novartis International Pharmaceutical, Ltd.

Neurogen Corporation

Suoming Zhang

Andrew Y Thurkauf

He Zhao

Yang Gao

Bingsong Han

Scott A Mitchell

George D Maynard

Bertrand Leo Chenard

George P Luke

Linghong Xie

Xiao Shu He

LuYan Zhang

The invention provides packaged pharmaceutical preparations of Aryl substituted imidazoles, pyrazoles, pyridizines and related compounds of the Formula where the variables are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of the invention act bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory and immune system disorders.

Aryl imidazoles and related compounds as C5a receptor modulators

Amino methyl imidazoles of Formula I are provided: wherein R, R, R, R, R, R, and Rare 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. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. Additionally, this invention provides labeled amino methyl imidazoles compounds, which are useful as probes for the localization of C5a receptors.

Amino methyl imidazoles and related compounds as C5a receptor modulators

Amino methyl imidazoles as C5a receptor modulators

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Branford, CT, United States of America

Suoming Zhang