ChemInform Abstract: 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.

Abstract

Active Arginine Vasopressin Receptor Antagonists.-In continuation of developing vasopressin antagonists, the tricyclic pyrrolobenzodiazepine moiety in VPA-985 is replaced by the thienobenzazepine derivatives (IV) and (X). These ring systems are prepared by novel routes, the structure-activity relationship is described. Thienobenzazepines (XII) possess potent V 1a and V 2 receptor binding activity. Compound (XIIc) is a potent, orally active and highly selective V 2 antagonist. -(ARANAPAKAM, VENKATESAN; ALBRIGHT, J. DONALD; GROSU, GEORGE T.; CHAN, PETER S.; COUPET, JOSEPH; SAUNDERS, TRINA; RU, XUN; MAZANDARANI, H.; Bioorg. Med. Chem.