Neurogen Corporation

Novartis International Pharmaceutical, Ltd.

LuYan Zhang

Scott A Mitchell

He Zhao

Andrew Y Thurkauf

Bingsong Han

Kevin S Currie

George D Maynard

Bertrand Leo Chenard

George P Luke

Kyungae Lee

Yang Gao

Linghong Xie

Suoming Zhang

Xiao Shu He

Robert Ohliger

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

Substituted tetrahydroisoquinolines and related compounds are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies:

Substituted tetrahydroisoquinolines as C5a receptor modulators

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Branford, CT, United States of America

LuYan Zhang