References of 2-[2-ethoxy-5-(4-ethylpiperazin-1-yl)sulfonylphenyl]-5-methyl-7-propyl-
1H-imidazo[5,1-f][1,2,4]triazin-4-one
Title: Vardenafil
CAS Registry Number: 224785-90-4
CAS Name: 1-[[3-(1,4-Dihydro-5-methyl-4-oxo-7-propylimidazo[5,1-
f][1,2,4]triazin-2-yl)-4-ethoxyphenyl]sulfonyl]-4-ethyl-piperazine
Molecular Formula: C23H32N6O4S
Molecular Weight: 488.60
Percent Composition: C 56.54%, H 6.60%, N 17.20%, O 13.10%, S 6.56%
Literature References: Orally active, selective phosphodiesterase type 5 (PDE5) inhibitor. Prepn: U. Niew?hner
et al., WO 9924433;
eidem,
US 6362178 (1999, 2002 both to Bayer AG). Effect on cGMP in human corpus cavernosum muscle cells: N. N. Kim
et al., Life Sci. 69, 2249 (2001). Pharmacology: E. Bischoff
et al., J. Urol. 165, 1316 (2001). Clinical trial in impotence: H. Porst
et al., Int. J. Impotence Res. 13, 192 (2001); in erectile dysfunction: C. Stief
et al., Int. J. Clin. Pract. 58, 230 (2004); F. Giuliano
et al., BJU Int. 95, 110 (2005). Review of clinical experience in erectile dysfunction: S. Markou
et al., Int. J. Impotence Res. 16, 470-478 (2004); M. Kendirci
et al., Expert Opin. Pharmacother. 5, 923-932 (2004).
Derivative Type: Hydrochloride trihydrate
CAS Registry Number: 330808-88-3; 224785-91-5 (anhydrous)
Manufacturers' Codes: Bay-38-9456
Trademarks: Levitra (Bayer); Nuviva (Bayer)
Molecular Formula: C23H32N6O4S.HCl.3H2O
Molecular Weight: 579.11
Percent Composition: C 47.70%, H 6.79%, N 14.51%, O 19.34%, S 5.54%, Cl 6.12%
Properties: Nearly colorless solid, mp 218°. Soly in water: 0.11 mg/ml.
Melting point: mp 218°
Therap-Cat: In treatment of male erectile dysfunction.
Keywords: Phosphodiesterase Inhibitor; Impotence Therapy.