Preparation of oxime dual NK(1)/NK(2) antagonists with reduced NK(3) affinity |
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| Authors: | Reichard Gregory A Grice Cheryl A Shih Neng-Yang Spitler James Majmundar Sapna Wang Steven D Paliwal Sunil Anthes John C Piwinski John J |
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| Affiliation: | Schering-Plough Research Institute, Kenilworth, NJ 07033, USA. gregory.reichard@spcorp.com |
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| 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. |
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