Next-generation spirobenzazepines: Identification of RWJ-676070 as a balanced vasopressin V1a/V2 receptor antagonist for human clinical studies
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.
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.
p. 6623 - 6628
(2008/03/18)
Synthesis and evaluation of spirobenzazepines as potent vasopressin receptor antagonists
A novel series of spirobenzazepines was synthesized and evaluated for V1a and V2 receptor antagonist activity. Compounds 8b, 8i, and 8k have shown selective V1a receptor antagonist activity. Compounds 8p and 8q were shown to be dual V1a/V2 receptor antagonists.
Xiang, Min Amy,Chen, Robert H.,Demarest, Keith T.,Gunnet, Joseph,Look, Richard,Hageman, William,Murray, William V.,Combs, Donald W.,Patel, Mona
p. 2987 - 2989
(2007/10/03)
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