Title: Irbesartan
CAS Registry Number: 138402-11-6
CAS Name: 2-Butyl-3-[[2¢-(1H-tetrazol-5-yl)[1,1¢-biphenyl]-4-yl]methyl]-1,3-diazaspiro[4.4]non-1-en-4-one
Additional Names: 2-butyl-3-[p-(o-1H-tetrazol-5-ylphenyl)benzyl]-1,3-diazaspiro[4.4]non-1-en-4-one; 2-n-butyl-4-spirocyclopentane-1-[(2¢-(tetrazol-5-yl)biphenyl-4-yl)methyl]-2-imidazolin-5-one
Manufacturers' Codes: BMS-186295; SR-47436
Trademarks: Aprovel (Sanofi-Synthelabo); Avapro (Sanofi-Synthelabo)
Molecular Formula: C25H28N6O
Molecular Weight: 428.53
Percent Composition: C 70.07%, H 6.59%, N 19.61%, O 3.73%
Literature References: Angiotensin II type 1 (AII1)-receptor antagonist. Prepn: C. Bernhart et al., WO 9114679; eidem, US 5270317 (1991, 1993 both to Sanofi); eidem et al., J. Med. Chem. 36, 3371 (1993). HPLC determn in plasma and urine: S.-Y. Chang et al., J. Chromatogr. B 702, 149 (1997). Metabolism: T. J. Chando et al., Drug Metab. Dispos. 26, 408 (1998). Review of pharmacology and clinical efficacy: J. C. Gillis, A. Markham, Drugs 54, 885-902 (1997). Renoprotective effect in diabetic nephropathy: E. J. Lewis et al., N. Engl. J. Med. 345, 851 (2001); H.-H. Parving et al., ibid. 870.
Properties: Crystals from 96% ethanol, mp 180-181°.
Melting point: mp 180-181°
Therap-Cat: Antihypertensive.
Keywords: Angiotensin II Receptor Antagonist; Antihypertensive; Biphenyltetrazole Derivatives. |