Preparation of Oxime Dual NK1/NK2 Antagonists with Reduced NK3 Affinity.

Abstract By employing a stereosimplification approach, a thorough SAR exploration of the piperidine region of Sch 206272 was possible through a practical and efficient synthesis of substituted cyclic ureas. This SAR study led to the identification of a benzimidazolinone series of compounds which display single digit nanomolar NK 1 /NK 2 affinity and near micromolar binding for the NK 3 receptor.