title: The synthesis and vasopressin (AVP) antagonist activity of a novel series of N-aroyl-2,4,5,6-tetrahydropyrazolo[3,4-d]thieno[3,2-b]azepines.
abstract: Synthesis and SAR of N-[4-[(4,5-dihydropyrazolo[3,4-d]thieno[3,2-b]azepin-6(2H)-y l)carbonyl]phenyl]benzamides as arginine vasopressin (AVP) receptor antagonists are discussed. Potent orally active AVP receptor antagonists are produced when the benzamide moiety contains a phenyl group at the 2-position. Similar analogues of 4,6,7,8-tetrahydro-5H-thieno[3,2-b]azepine and VPA-985 are reported.
authors.affiliation: Chemical Sciences, Wyeth-Ayerst Research, Pearl River, NY 10965, USA. albrigj@war.wyeth.com
authors.forename: J D
authors.initials: JD
authors.lastname: Albright
authors.forename: E G
authors.initials: EG
authors.lastname: Delos Santos
authors.forename: J P
authors.initials: JP
authors.lastname: Dusza
authors.forename: P S
authors.initials: PS
authors.lastname: Chan
authors.forename: J
authors.initials: J
authors.lastname: Coupet
authors.forename: X
authors.initials: X
authors.lastname: Ru
authors.forename: H
authors.initials: H
authors.lastname: Mazandarani
mesh_terms: D000818:Animals; D001127:Arginine Vasopressin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D001381:Azepines / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D051381:Rats; D017483:Receptors, Vasopressin / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D001381:Azepines; D017483:Receptors, Vasopressin; D001127:Arginine Vasopressin