Novel, highly selective, muscarinic M₃ receptor antagonists

Abstract

A series of muscarinic receptor antagonists based upon a polyamide backbone linking a trityl group and a N-alkylpiperidine, or N,N-dialkylpiperidinium group, are claimed. The linking group may be constrained by the presence of one or two, pyrrolidine, or proline rings. These compounds are potent M₃antagonists with affinities in the 0.5 - 5 nM range and are highly selective relative to both M₁ (100 - 1000-fold) and M₂ (50 - 100-fold) receptors.

• bronchodilator
• COPD
• M3 receptor
• muscarinic antagonist
• urinary incontinence