Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as μ opioid receptor antagonists with improved opioid receptor selectivity profiles

Bertrand Le Bourdonnec,William M. Barker,Serge Belanger,Daniel D. Wiant,Nathalie C. Conway-James,Joel A. Cassel,Timothy J. O’Neill,Patrick J. Little,Robert N. DeHaven,Diane L. DeHaven-Hudkins,Roland E. Dolle

Bioorganic & Medicinal Chemistry Letters（2008）

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摘要

The discovery and SAR studies of a series of N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as novel μ opioid receptor antagonists, analogs of alvimopan, are reported.

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关键词

Opioid,μ receptors,Solid phase synthesis

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