Synthesis and evaluation of nonpeptide substituted spirobenzazepines as potent vasopressin antagonists.
A series of substituted spirobenzazepines was prepared and evaluated as V(1a) and V(2) dual vasopressin receptor antagonists. Compounds 7p and 7q have been shown to be not only potent inhibitors of vasopressin receptors, but also have exhibited an excellent overall pharmaceutical suitability profile.
Xiang
Min Amy
MA
Endocrine Therapeutics and Metabolic Disorders, Johnson and Johnson Pharmaceutical Research and Development, LLC, 1000 Route 202, Bldg: PCC, Room: PC110, Raritan, NJ 08869, USA.
Chen
Robert H
RH
Demarest
Keith T
KT
Gunnet
Joseph
J
Look
Richard
R
Hageman
William
W
Murray
William V
WV
Combs
Donald W
DW
Rybczynski
Philip J
PJ
Patel
Mona
M
D000818:Animals; D065092:Antidiuretic Hormone Receptor Antagonists; D001552:Benzazepines / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D002460:Cell Line; D004353:Drug Evaluation, Preclinical / Q000379:methods; D006801:Humans; D051381:Rats; D017483:Receptors, Vasopressin / Q000378:metabolism
D065092:Antidiuretic Hormone Receptor Antagonists; D001552:Benzazepines; D017483:Receptors, Vasopressin