1. Academic Validation
  2. 4,10-dihydro-5H-thieno[3,2-c][1]benzazepine derivatives and 9,10-dihydro-4H-thieno[2,3-c][1]benzazepine derivatives as orally active arginine vasopressin receptor antagonists

4,10-dihydro-5H-thieno[3,2-c][1]benzazepine derivatives and 9,10-dihydro-4H-thieno[2,3-c][1]benzazepine derivatives as orally active arginine vasopressin receptor antagonists

  • Bioorg Med Chem Lett. 1999 Jul 5;9(13):1733-6. doi: 10.1016/s0960-894x(99)00278-4.
V Aranapakam 1 J D Albright G T Grosu P S Chan J Coupet T Saunders X Ru H Mazandarani
Affiliations

Affiliation

  • 1 Wyeth-Ayerst Research, Pearl River, NY 10965, USA.
Abstract

Synthesis and structure-activity relationships (SAR) of arginine Vasopressin Receptor (AVP) antagonists are described. Potent and orally active compounds are prepared when tricyclic 10,11-dihydro-5H-pyrrolo[2,1-c][1,4]benzodiazepine moiety in VPA-985 1 is replaced with a compound 7 or 12.

Figures