Discovery of Potent, Non-Steroidal and Highly Selective Glucocorticoid Receptor Antagonists with Anti-Obesity Activity

To thwart phase II metabolism, Structure-Activity-Relationship (SAR) studies around the phenol of the potent glucocorticoid receptor (GR) antagonists CP-394531 and CP-409069 were examined. The discovery of the potent, selective, nonsteroidal GR antagonist (CP-472555) with anti-GR and anti-obesity activity in animal models is described.