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.

开始日期2007-06-01

申办/合作机构

Movetis NV

100 项与 RWJ-351647 相关的临床结果

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100 项与 RWJ-351647 相关的转化医学

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100 项与 RWJ-351647 相关的专利（医药）

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项与 RWJ-351647 相关的文献（医药）

2007-12-01·Bioorganic & medicinal chemistry letters4区 · 医学

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

4区 · 医学

Article

作者: 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.

2004-06-01·Bioorganic & medicinal chemistry letters4区 · 医学

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

4区 · 医学

Article

作者: William J. Hoekstra ; Alexey B. Dyatkin ; William Hageman ; 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 项与 RWJ-351647 相关的药物交易

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