2507. Conivaptan

Nomenclature

CAS number: 210101-16-9
N-[4-[(4,5-Dihydro-2-methylimidazo[4,5-d][1]benzazepin-6(1H)-yl)carbonyl]phenyl][1,1′-biphenyl]-2-carboxamide; 4′-[(2-methyl-1,4,5,6-tetrahydro-imidazo[4,5-d][1]benzazepin-6-yl)carbonyl]-2-phenylbenzanilide.
C32H26N4O2; mol wt 498.57.
C 77.09%, H 5.26%, N 11.24%, O 6.42%.

Description and references

Nonpeptide, dual vasopressin V1a/V2 receptor antagonist. Prepn: A. Tanaka et al., WO 9503305; eidem, US 5723606 (1995, 1998 both to Yamanouchi); A. Matsuhisa et al., Chem. Pharm. Bull. 48, 21 (2000). Pharmacology: Y. Yatsu et al., Eur. J. Pharmacol. 321, 225 (1997). Binding specificity study: A. Tahara et al., Peptides 19, 691 (1998). Clinical pharmacokinetics: M. Burnier et al., Eur. J. Clin. Pharmacol.. 55, 633 (1999). Clinical evaluation in advanced heart failure: J. E. Udelson et al., Circulation 104, 2417 (2001). Review of clinical development: S. A. Doggrell, Curr. Opin. Investig. Drugs 6, 317-326 (2005).

Chemical structure

Derivative

Hydrochloride.

Nomenclature

CAS number: 168626-94-6
Cl-1025; YM-087; YM-35087; Vaprisol (Astellas).
C32H26N4O2.HCl; mol wt 535.04.
C 71.83%, H 5.09%, N 10.47%, O 5.98%, Cl 6.63%.

Properties

Crystals, mp >250°.

Therapeutic Category

In treatment of congestive heart failure.

Keywords

Vasopressin Receptor Antagonist