439687-69-1Relevant articles and documents
Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties
Oost, Thorsten,Backfisch, Gisela,Bhowmik, Swati,Van Gaalen, Marcel M.,Geneste, Herve,Hornberger, Wilfried,Lubisch, Wilfried,Netz, Astrid,Unger, Liliane,Wernet, Wolfgang
scheme or table, p. 3828 - 3831 (2011/08/02)
Herein we report the discovery of a novel series of vasopressin 1b (V1b) receptor antagonists, starting from potent but metabolically labile oxindole SSR149415. Masking the proline N,N-dimethyl amide moiety as an oxazole and attaching a benzylic amine moiety to the northern phenyl ring resulted in potent and selective V1b receptor antagonists with improved metabolic stability and improved pharmacokinetic properties in rat. Compound 18c was found to be efficacious in a rat model of anti-depressant activity.
Novel 1,3-dihydro-2h-indol-2-one derivatives and their use as ligands for v1b and v1a arginine-vasopressin receptors
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, (2008/06/13)
The invention relates to compounds of formula: as well as the possible salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, which have affinity for and selectivity towards the V1b receptors or towards both the V1b and V1a receptors of arginine-vasopressin. The invention also relates to the process for preparing them, to the intermediate compounds of formula (II) that are useful for preparing them, to pharmaceutical compositions containing them and to their use for the preparation of medicinal products.