Synthesis and evaluation of nonpeptide substituted spirobenzazepines as potent vasopressin antagonists.

Bioorg Med Chem Lett

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

Published: June 2004

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.

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http://dx.doi.org/10.1016/j.bmcl.2004.04.016DOI Listing

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