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Title:
NOVEL SIALYLSTEROID
Document Type and Number:
WIPO Patent Application WO/1993/021198
Kind Code:
A1
Abstract:
Sialic acid derivatives of cortison, dexamethasone and vitamin D3 represented by general formula (I), wherein R1 represents a steroid residue selectd from among cortisone, dexamethasone and vitamin D3; R2 represents hydrogen or acetyl; and R3 represents hydrogen or lower alkyl. These derivatives not only retain the drug effects inherent in the steroids, but also exhibit no or little side effects even after being used for long and have an improved solubility in water. Further, the sialylated vitamin D3 has a long half-life period in blood.

Inventors:
NUMATA MASAAKI (JP)
ISHII TAKAYUKI (JP)
SUGIMOTO MAMORU (JP)
SUGAI KEI (JP)
SUGIYAMA NAOKAZU (JP)
OGAWA TOMOYA (JP)
Application Number:
PCT/JP1993/000466
Publication Date:
October 28, 1993
Filing Date:
April 13, 1993
Export Citation:
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Assignee:
KANTO ISHI PHARMA CO LTD (JP)
NUMATA MASAAKI (JP)
ISHII TAKAYUKI (JP)
SUGIMOTO MAMORU (JP)
SUGAI KEI (JP)
SUGIYAMA NAOKAZU (JP)
OGAWA TOMOYA (JP)
International Classes:
A61K31/57; A61K31/70; A61K31/7028; A61K31/7034; A61P29/00; A61P37/06; A61P37/08; C07C401/00; C07H15/203; C07H15/207; C07J7/00; C07J17/00; C07J41/00; (IPC1-7): C07H15/203; C07J17/00
Foreign References:
EP0123485A11984-10-31
EP0112332A11984-07-04
Other References:
BIOCHEMISTRY, Vol. 8, (No. 3), pp. 1188-99, (1969), V.R. MATTOX et al., "Synthesis of C-21Glucosiduronates of Cortisone and Related Corticosteroids".
HELVETICA CHIMICA ACTA, Vol. 66, (No. 7), pp. 2093-2102, (1983), A. FUERST et al., "Synthesis of Beta-D-Glucopyranosides of Some Hydroxylated Vitamin D Compounds.
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