Title: Conivaptan
CAS Registry Number: 210101-16-9
CAS Name: N-[4-[(4,5-Dihydro-2-methylimidazo[4,5-d][1]benzazepin-6(1H)-yl)carbonyl]phenyl][1,1¢-biphenyl]-2-carboxamide
Additional Names: 4¢-[(2-methyl-1,4,5,6-tetrahydro-imidazo[4,5-d][1]benzazepin-6-yl)carbonyl]-2-phenylbenzanilide
Molecular Formula: C32H26N4O2
Molecular Weight: 498.57
Percent Composition: C 77.09%, H 5.26%, N 11.24%, O 6.42%
Literature 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. Invest. Drugs 6, 317-326 (2005).
Derivative Type: Hydrochloride
CAS Registry Number: 168626-94-6
Manufacturers' Codes: Cl-1025; YM-087; YM-35087
Trademarks: Vaprisol (Astellas)
Molecular Formula: C32H26N4O2.HCl
Molecular Weight: 535.04
Percent Composition: C 71.83%, H 5.09%, N 10.47%, O 5.98%, Cl 6.63%
Properties: Crystals, mp >250°.
Melting point: mp >250°
Therap-Cat: In treatment of congestive heart failure.
Keywords: Vasopressin Receptor Antagonist. |