Discovery of potent, balanced and orally active dual NK 1/NK 3 receptor ligands

JU Peters, T Hoffmann, P Schnider, H Stadler…

Index: Peters, Jens-Uwe; Hoffmann, Torsten; Schnider, Patrick; Stadler, Heinz; Koblet, Andreas; Alker, Andre; Poli, Sonia Maria; Ballard, Theresa M.; Spooren, Will; Steward, Lucinda; Sleight, Andrew J. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 11 p. 3405 - 3408

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Citation Number: 10

Abstract

During a program directed at selective NK1 receptor antagonists, we serendipitously discovered an NK1 receptor ligand with additional affinity for the NK3 receptor. Recognising an opportunity for a drug discovery program aiming for dual NK1/NK3 receptor antagonists, we prepared a series of analogues from a novel, versatile building block. From this series emerged compounds with high and balanced affinities for the NK1 and the NK3 receptors. ...