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Next-generation spirobenzazepines: identification of RWJ-676070 as a balanced vasopressin V1a/V2 receptor antagonist for human clinical studies |
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| Authors: | Xiang Min Amy Rybczynski Philip J Patel Mona Chen Robert H McComsey David F Zhang Han-Cheng Gunnet Joseph W Look Richard Wang Yuanping Minor Lisa K Zhong H Marlon Villani Frank J Demarest Keith T Damiano Bruce P Maryanoff Bruce E |
| Institution: | Research and Early Development, Johnson & Johnson Pharmaceutical Research & Development, 8 Clarke Drive, Cranbury, NJ 08512, USA. |
| 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 V(1a)/V(2) receptor antagonist with favorable properties for clinical development. Compound 3 is currently undergoing human clinical investigation. |
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