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pubmed-article:17942308pubmed:abstractTextWe have continued to explore spirobenzazepines as vasopressin receptor antagonists to follow up on RWJ-339489 (2), which had advanced into preclinical development. Further structural modifications were pursued to find a suitable backup compound for human clinical studies. Thus, we identified carboxylic acid derivative 3 (RWJ-676070; JNJ-17158063) as a potent, balanced vasopressin V(1a)/V(2) receptor antagonist with favorable properties for clinical development. Compound 3 is currently undergoing human clinical investigation.lld:pubmed
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pubmed-article:17942308pubmed:articleTitleNext-generation spirobenzazepines: identification of RWJ-676070 as a balanced vasopressin V1a/V2 receptor antagonist for human clinical studies.lld:pubmed
pubmed-article:17942308pubmed:affiliationResearch and Early Development, Johnson & Johnson Pharmaceutical Research & Development, 8 Clarke Drive, Cranbury, NJ 08512, USA.lld:pubmed
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