Title: Zopolrestat
CAS Registry Number: 110703-94-1
CAS Name: 3,4-Dihydro-4-oxo-3-[[5-(trifluoromethyl)-2-benzothiazolyl]methyl]-1-phthalazineacetic acid
Additional Names: 2-[4-oxo-3-[5-(trifluoromethyl)benzothiazol-2-ylmethyl]-3,4-dihydrophthalazin-1-yl]acetic acid
Manufacturers' Codes: CP-73850
Molecular Formula: C19H12F3N3O3S
Molecular Weight: 419.38
Percent Composition: C 54.41%, H 2.88%, F 13.59%, N 10.02%, O 11.45%, S 7.65%
Literature References: Aldose reductase inhibitor. Prepn: B. L. Mylari et al., EP 222576; E. R. Larson, B. L. Mylari, US 4939140 (1987, 1990 both to Pfizer); B. L. Mylari et al. J. Med. Chem. 34, 108 (1991). Pharmacology: B. Tesfamariam et al., J. Cardiovasc. Pharmacol. 21, 205 (1993); B. Tesfamariam et al., Am. J. Physiol. 265, H1189 (1993). Clinical pharmacokinetics: P. B. Inskeep et al., J. Clin. Pharmacol. 34, 760 (1994).
Properties: Crystals, mp 197-198°. pKa (dioxane/water): 5.46 (1:1); 6.38 (2:1). Log P (n-octanol/water): 3.43.
Melting point: mp 197-198°
pKa: pKa (dioxane/water): 5.46 (1:1); 6.38 (2:1)
Log P: Log P (n-octanol/water): 3.43
Therap-Cat: Treatment of diabetic complications.
Keywords: Aldose Reductase Inhibitor. |