Author/Authors :
Min Amy Xiang، نويسنده , , Philip J. Rybczynski، نويسنده , , Mona Patel، نويسنده , , Robert H. Chen، نويسنده , , David F. McComsey، نويسنده , , Han-Cheng Zhang، نويسنده , , Joseph W. Gunnet، نويسنده , , Richard Look، نويسنده , , Yuanping Wang، نويسنده , , Lisa K. Minor، نويسنده , , H. Marlon Zhong، نويسنده , , Frank J. Villani Jr.، نويسنده , , Keith T. Demarest، نويسنده , , Bruce P. Damiano، نويسنده , , Bruce E. Maryanoff، نويسنده ,
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.
