Title: Valsartan
CAS Registry Number: 137862-53-4
CAS Name: N-(1-Oxopentyl)-N-[[2¢-(1H-tetrazol-5-yl)[1,1¢-biphenyl]-4-yl]methyl]-L-valine
Additional Names: N-[p-(o-1H-tetrazol-5-ylphenyl)benzyl]-N-valeryl-L-valine; (S)-N-(1-carboxy-2-methylprop-1-yl)-N-pentanoyl-N-[2¢-(1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]amine
Manufacturers' Codes: CGP-48933
Trademarks: Diovan (Novartis); Tareg (Novartis)
Molecular Formula: C24H29N5O3
Molecular Weight: 435.52
Percent Composition: C 66.19%, H 6.71%, N 16.08%, O 11.02%
Literature References: Nonpeptide angiotensin II AT1-receptor antagonist. Prepn: P. Bühlmayer et al., EP 443983; eidem, US 5399578 (1991, 1995 both to Ciba Geigy); idem et al., Bioorg. Med. Chem. Lett. 4, 29 (1994). Pharmacological profile: L. Criscione et al., Br. J. Pharmacol. 110, 761 (1993). HPLC determn in human plasma: A. Sioufi et al., J. Liq. Chromatogr. 17, 2179 (1994). Clinical pharmacology: P. Müller et al., Eur. J. Clin. Pharmacol. 47, 231 (1994). Clinical comparison with captopril, q.v., in high risk patients following myocardial infarction: M. A. Pfeffer et al., N. Engl. J. Med. 349, 1893 (2003). Review of pharmacology and clinical experience in heart failure: R. Latini et al., Expert Opin. Pharmacother. 5, 181-193 (2004).
Properties: Crystals from diisopropyl ether, mp 116-117°. Partition coefficient (n-octanol/aq phosphate buffer): 0.033. Sol in water at 25°.
Melting point: mp 116-117°
Log P: Partition coefficient (n-octanol/aq phosphate buffer): 0.033
Therap-Cat: Antihypertensive.
Keywords: Angiotensin II Receptor Antagonist; Antihypertensive; Biphenyltetrazole Derivatives. |