Title: Candesartan
CAS Registry Number: 139481-59-7
CAS Name: 2-Ethoxy-1-[[2¢-(1H-tetrazol-5-yl)[1,1¢-biphenyl]-4-yl]methyl]-1H-benzimidazole-7-carboxylic acid
Additional Names: 2-ethoxy-1-[4-[2-(1H-tetrazol-5-yl)phenyl]benzyl]-7-benzimidazolecarboxylic acid
Manufacturers' Codes: CV-11974
Molecular Formula: C24H20N6O3
Molecular Weight: 440.45
Percent Composition: C 65.45%, H 4.58%, N 19.08%, O 10.90%
Literature References: Angiotensin II type-1 receptor antagonist. Prepn: T. Naka et al., EP 459136; eidem, US 5196444 (1991, 1993 both to Takeda); K. Kubo et al., J. Med. Chem. 36, 2182, 2343 (1993). Pharmacology: Y. Shibouta et al., J. Pharmacol. Exp. Ther. 266, 114 (1993). Clinical pharmacology, pharmacokinetics: T. Ogihara et al., Clin. Ther. 16, 74 (1994). Pilot study of cilexetil ester in essential hypertension: idem et al., ibid. 15, 684 (1993). Series of clinical trials in chronic heart failure: Lancet 362, 759-781 (2003).
Properties: Colorless crystals from ethyl acetate + methanol, mp 183-185°.
Melting point: mp 183-185°
Derivative Type: 1-[[(Cyclohexyloxy)carbonyl]oxy]ethyl ester
CAS Registry Number: 145040-37-5
Additional Names: Candesartan cilexetil
Manufacturers' Codes: TCV-116
Trademarks: Atacand (AstraZeneca); Amias (Takeda); Kenzen (Takeda)
Molecular Formula: C33H34N6O6
Molecular Weight: 610.66
Percent Composition: C 64.91%, H 5.61%, N 13.76%, O 15.72%
Properties: Ester prodrug; hydrolyzed in vivo to the active carboxylic acid. Colorless crystals from ethanol + water, mp 163° (dec). Also reported as white to off-white powder, sparingly sol in methanol. Practically insol in water.
Melting point: mp 163° (dec)
Therap-Cat: Antihypertensive. In treatment of congestive heart failure.
Keywords: Angiotensin II Receptor Antagonist; Antihypertensive; Biphenyltetrazole Derivatives. |