Preparation of oxime dual NK(1)/NK(2) antagonists with reduced NK(3) affinity.

Gregory A Reichard, Cheryl A Grice, Neng-Yang Shih, James Spitler, Sapna Majmundar, Steven D Wang, Sunil Paliwal, John C Anthes, John J Piwinski

Schering-Plough Research Institute, Kenilworth, NJ 07033, USA. gregory.reichard@spcorp.com

Bioorganic & medicinal chemistry letters 2002 Sep 2

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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.

Citation

Gregory A Reichard, Cheryl A Grice, Neng-Yang Shih, James Spitler, Sapna Majmundar, Steven D Wang, Sunil Paliwal, John C Anthes, John J Piwinski. Preparation of oxime dual NK(1)/NK(2) antagonists with reduced NK(3) affinity. Bioorganic & medicinal chemistry letters. 2002 Sep 2;12(17):2355-8