abstract |
Formula (I) and Formula (II): Wherein R 1 , R 2 , R 3 , R 8 , R 9 , A and Ar are as defined herein are provided. To do. Such compounds are ligands for the C5a receptor. Preferred compounds of formula I and II bind to the C5a receptor with high affinity and exhibit neutral antagonist or inverse agonist activity at the C5a receptor. The present invention relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds to treat various inflammation, cardiovascular and immune system diseases. Furthermore, the present invention provides labeled 1-aryl-4-substituted isoquinolines that are useful as probes for C5a receptor localization. |