Heterocyclic acetamide and benzamide derivatives as potent and selective beta3-adrenergic receptor agonists with improved rodent pharmacokinetic profiles

  • Bioorg Med Chem Lett. 2010 Mar 15;20(6):1895-9. doi: 10.1016/j.bmcl.2010.01.130.
Stephen D Goble  1 ,  Liping Wang ,  K Lulu Howell ,  Alka Bansal ,  Richard Berger ,  Linda Brockunier ,  Jerry DiSalvo ,  Scott Feighner ,  Bart Harper ,  Jiafang He ,  Amanda Hurley ,  Donna Hreniuk ,  Emma Parmee ,  Michael Robbins ,  Gino Salituro ,  Anthony Sanfiz ,  Eric Streckfuss ,  Eloisa Watkins ,  Ann E Weber ,  Mary Struthers ,  Scott D Edmondson
Affiliations
Abstract

A series of amide derived beta(3)-adrenergic receptor (AR) agonists is described. The discovery and optimization of several series of compounds derived from 1, is used to lay the SAR foundation for second generation beta(3)-AR agonists for the treatment of overactive bladder.