Synthesis and evaluation of nonpeptide substituted spirobenzazepines as potent vasopressin antagonists

Min Amy Xiang; Robert H Chen; Keith T Demarest; Joseph Gunnet; Richard Look; William Hageman; William V Murray; Donald W Combs; Philip J Rybczynski; Mona Patel

doi:10.1016/j.bmcl.2004.04.016

Synthesis and evaluation of nonpeptide substituted spirobenzazepines as potent vasopressin antagonists

Bioorg Med Chem Lett. 2004 Jun 21;14(12):3143-6. doi: 10.1016/j.bmcl.2004.04.016.

Authors

Min Amy Xiang¹, Robert H Chen, Keith T Demarest, Joseph Gunnet, Richard Look, William Hageman, William V Murray, Donald W Combs, Philip J Rybczynski, Mona Patel

Affiliation

¹ Endocrine Therapeutics and Metabolic Disorders, Johnson and Johnson Pharmaceutical Research and Development, LLC, 1000 Route 202, Bldg: PCC, Room: PC110, Raritan, NJ 08869, USA.

PMID: 15149662
DOI: 10.1016/j.bmcl.2004.04.016

Abstract

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.

MeSH terms

Animals
Antidiuretic Hormone Receptor Antagonists*
Benzazepines / chemical synthesis*
Benzazepines / metabolism
Benzazepines / pharmacology
Cell Line
Drug Evaluation, Preclinical / methods
Humans
Rats
Receptors, Vasopressin / metabolism

Substances

Antidiuretic Hormone Receptor Antagonists
Benzazepines
Receptors, Vasopressin