21-Substituted steroid compound

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai

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536 5, 536 186, A61K 31705, C07J 500, C07J 700, C07J 900

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active

059454040

ABSTRACT:
A glycoside represented by formula (I), wherein dexamethasone or betamethasone is the aglycon and the 21-position is substituted by a simple sugar or an acylated sugar selected from the group consisting of glucose, galactose, mannose, rhamnose, fucose, N-acetylglucosamine, N-acetylgalactosamine, galacturonic acid, glucuronic acid and sialic acid. ##STR1##

REFERENCES:
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The Merck Index, 12.sup.th Edition, 1996, Therapeutic Category and Biological Activity Index, p. Ther-22.
Tozer et al., Pharm. Res., vol. 8(4): 445-454, (1991)(Abstract only).
Monosaccharides: Their Chemistry And Their Roles In Natural Products, ed. Collins & Ferrier, (John Wiley & Sons), p. 4 (1995).
The Merck Index (Eleventh Edition), pp. 184, 463, 464, 494-496 (1989).
Journal of Medicinal Chemistry, vol. 27, No. 3, Mar. 1984, "A Colon-Specific Drug Delivery System Based on Drug Glycosides and the Glycosidases of Colonic Bacteria", David R. Friend et al., pp. 261-266.
Journal of Medicinal Chemistry, vol. 28, No. 1, Jan. 1985, "Drug Glycosides: Potential Prodrugs for Colon-Specific Drug Delivery", David R. Friend et al., pp. 51-57.
J. Am. Chem. Soc. (1964), vol. 86, Sep. 20, 1964, 3903-3904.
J. Pharm. Pharmacol. vol. 43 (1991), "Relative anti-inflammatory effect of oral dexamethasone-.beta.-D-glucoside and dexamethasone in experimental inflammatory bowel disease in guinea pigs", D.R. Friend et al., pp. 353-355.

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