Abstract: 3-substituted-6-aryl pyridines of Formula I are provided: wherein R1, R2, R3, R8, R9, 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.

Abstract: Substituted biaryl amides of Formula I 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.

Abstract: This invention encompasses compounds of the formula: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 are variables;X and Y represent hydrogen, halogen, hydroxy or amino substituents, with the proviso that when Y is a hydrogen, halogen, or amino substituent, X is hydroxy; andW represent aryl groups unsubstituted or substituted with halogen, hydroxy, alkyl, alkoxy or amino groups.These compounds or prodrugs thereof are highly selective agonists, antagonists or inverse agonists or GaBAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorder, overdose with benzodiazepine drugs, and enchancement of memory.