9540. Tolvaptan
Nomenclature
CAS number: 150683-30-0
N-[4-[(7-Chloro-2,3,4,5-tetrahydro-5-hydroxy-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl]-2-methylbenzamide; 7-chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-1-benzazepine; OPC-41061. C26H25ClN2O3; mol wt 448.94.
C 69.56%, H 5.61%, Cl 7.90%, N 6.24%, O 10.69%.
Description and references
Nonpeptide arginine vasopressin V2-receptor antagonist. Prepn: H. Ogawa et al., WO 9105549; eidem, US 5258510 (1991, 1993 both to Otsuka); K. Kondo et al., Bioorg. Med. Chem. 7, 1743 (1999). Pharmacology: Y. Yamamura et al., J. Pharmacol. Exp. Ther. 287, 860 (1998). Clinical trial in heart failure: M. Gheorghiade et al., J. Am. Med. Assoc. 291, 1963 (2004); in hyponatremia: R. W. Schrier et al., N. Engl. J. Med. 355, 2099 (2006). Review of pharmacology and clinical experience in congestive heart failure: U. C. Rangasetty et al., Expert Opin. Invest. Drugs 15, 533-540 (2006).
Properties
Colorless prisms, mp 225.9°.Therapeutic Category
In treatment of congestive heart failure.
Keywords
Vasopressin Receptor Antagonist