| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1377182 | Bioorganic & Medicinal Chemistry Letters | 2007 | 6 Pages |
Abstract
We 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 V1a/V2 receptor antagonist with favorable properties for clinical development. Compound 3 is currently undergoing human clinical investigation.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Min Amy Xiang, Philip J. Rybczynski, Mona Patel, Robert H. Chen, David F. McComsey, Han-Cheng Zhang, Joseph W. Gunnet, Richard Look, Yuanping Wang, Lisa K. Minor, H. Marlon Zhong, Frank J. Villani, Keith T. Demarest, Bruce P. Damiano, Bruce E. Maryanoff,