Synthesis and structure-activity relationships of CP-122,721, a second-generation NK-1 receptor antagonist

  • Bioorg Med Chem Lett. 1998 Feb 3;8(3):281-4. doi: 10.1016/s0960-894x(98)00012-2.
T J Rosen  1 ,  K J Coffman ,  S McLean ,  R T Crawford ,  D K Bryce ,  Y Gohda ,  M Tsuchiya ,  A Nagahisa ,  M Nakane ,  J A Lowe 3rd
Affiliations
  • 1. Central Research Division, Pfizer Inc., Groton, CT 06340, USA.
PMID: 9871670 DOI: 10.1016/s0960-894x(98)00012-2
Abstract

The synthesis and SAR of benzylamine side chain analogs of the NK-1 receptor antagonist CP-99,994 are described. The 5-trifluoromethoxy analog, CP-122,721, shows superior in vivo blockade of NK-1 receptor mediated responses.