A Randomized, Double Blind, Placebo Controlled, Phase II, Dose-titration Trial to Explore the Safety, Tolerability, Pharmacokinetic Profile and Efficacy of M0002 in Cirrhotic Subjects With Ascites and Hypo- or Normonatraemia.

M0002, an orally active, selective non-peptidergic antagonist of the vasopressin V2 receptor inhibits vasopressin-induced water reabsorption from the kidney. Therefore the aquaretic effect of M0002 has a potential clinical benefit in the treatment of ascites and hyponatreamia in cirrhotic patients.

Start Date01 Jun 2007

Sponsor / Collaborator

Movetis NV

100 Clinical Results associated with RWJ-351647

100 Translational Medicine associated with RWJ-351647

100 Patents (Medical) associated with RWJ-351647

Literatures (Medical) associated with RWJ-351647

01 Dec 2007·Bioorganic & medicinal chemistry lettersQ4 · MEDICINE

Next-generation spirobenzazepines: Identification of RWJ-676070 as a balanced vasopressin V1a/V2 receptor antagonist for human clinical studies

Q4 · MEDICINE

Article

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

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.

01 Jun 2004·Bioorganic & medicinal chemistry lettersQ4 · MEDICINE

Potent nonpeptide vasopressin receptor antagonists based on oxazino- and thiazinobenzodiazepine templates

Q4 · MEDICINE

Article

Author: William J. Hoekstra ; William Hageman ; Alexey B. Dyatkin ; Charles H. Reynolds ; Richard Look ; Brenda L. Poulter ; Eric Ericson ; Lawrence de Garavilla ; Dennis J. Hlasta ; Leonard R. Hecker ; Jay M. Matthews ; Joseph W. Gunnet ; Keith T. Demarest ; Bruce E. Maryanoff ; Patricia Andrade-Gordon ; John B. Moore

Vasopressin receptor antagonists can elicit ion-sparing diuretic effects (i.e., aquaresis) in vivo by blunting the action of the circulating hypophyseal hormone arginine vasopressin. We have identified two new series of basic tricyclic benzodiazepines, represented by general structure 1, which contain compounds that bind with high affinity to human V2 receptors. For example, (S)-(+)-8 and 5 are potent and selective V2 receptor antagonists with pronounced aquaretic activity in rats on oral administration.

100 Deals associated with RWJ-351647

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Indication	Highest Phase	Country/Location	Organization	Date
Hepatic ascites	Phase 2	-	Movetis NV	01 Jun 2007

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