1013. Bazedoxifene
Nomenclature
CAS number: 198481-32-2
1-[[4-[2-(Hexahydro-1H-azepin-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-o1; 1-[4-(2-azepan-1-ylethoxy)benzyl]-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol. C30H34N2O3; mol wt 470.60.
C 76.57%, H 7.28%, N 5.95%, O 10.20%.
Description and references
Nonsteroidal selective estrogen receptor modulator (SERM). Prepn: C. P. Miller et al., EP 802183; eidem, US 5998402 (1997, 1999 both to American Home); C. P. Miller et al., J. Med. Chem. 44, 1654 (2001). Pharmacology and receptor binding study: B. S. Komm et al., Endocrinology 146, 3999 (2005). Clinical pharmacology: S. Ronkin et al., Obstet. Gynecol. 105, 1397 (2005). Review of pharmacology and clinical experience: A. L. Stump et al., Ann. Pharmacother. 41, 833-839 (2007).
Properties
mp 98-102°.Derivative
Acetate.Nomenclature
CAS number: 198481-33-3
TSE-424; WAY-140424; WAY-TSE-424; Viviant (Wyeth). C30H34N2O3.C2H4O2; mol wt 530.65.
C 72.43%, H 7.22%, N 5.28%, O 15.08%.
Properties
Crystals from acetone + acetic acid, mp 174-178°.Therapeutic Category
Antiosteoporotic.
Keywords
Antiosteoporotic; Selective Estrogen Receptor Modulator (SERM)