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Abstract

SAR around 4,6-diaminopyrimidine derivatives allowed the discovery of the first potent dual M(3) antagonists and PDE4 inhibitors. Various chemical modulations around that scaffold led to the discovery of ucb-101333-3 which is characterized by the most interesting profile on both targets.

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PubMed ID:: 16439121

DOI:: 10.1016/j.bmcl.2006.01.006

ScienceOpen disciplines: Chemistry

Keywords: 3',5'-Cyclic-AMP Phosphodiesterases,antagonists & inhibitors,Cyclic Nucleotide Phosphodiesterases, Type 4,Enzyme Inhibitors,chemical synthesis,chemistry,pharmacology,Muscarinic Antagonists,Pyrimidines,Receptor, Muscarinic M3,Structure-Activity Relationship

First dual M3 antagonists-PDE4 inhibitors: synthesis and SAR of 4,6-diaminopyrimidine derivatives.

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Synthesis of 2-trifluoromethylated piperidines and azepanes

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