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    NEW PRODRUG FOR TREATING TUMOR AND INFLAMMATORY DISEASE
    1.
    发明专利
    NEW PRODRUG FOR TREATING TUMOR AND INFLAMMATORY DISEASE 失效

    公开(公告)号：JPH101495A

    公开(公告)日：1998-01-06

    申请号：JP5598397

    申请日：1997-03-11

    Applicant: HOECHST AG

    Inventor： BOSSLET KLAUS ,  CZECH JOERG ,  GERKEN MANFRED ,  STRAUB RAINER ,  MONNERET CLAUDE ,  FLORENT JEAN-CLAUDE ,  SCHMIDT FREDOERIC

    IPC: C07H15/203 ,  A61K31/70 ,  A61K31/7012 ,  A61K31/7028 ,  A61K31/7034 ,  A61K47/48 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07H15/26

    Abstract: PROBLEM TO BE SOLVED: To obtain a new compound, a glycosyl group-bearing specific active compound, high in stability and slight in side effects, and useful as a prodrug for preventing/treating tumors, autoimmune diseases and chronic inflammatory diseases such as chronic arthrorheumatism. SOLUTION: This new compound is shown by formula I [glycosyl is derived from a polysaccharide, oligosaccharide or monosaccharide each subject to scission by an enzyme; W is a 5- to 14-membered aromatic group, 5- to 14-membered heterocyclic group, 1-6C alkyl, 2-6C alkenyl, etc.; R is H, a 1-4C alkyl, phenyl, CN, OH, NO2 , halogen, etc.; X is O, NH, methyleneoxy, etc.; Y is O or NH; Z is a 1-4C alkylamino, N(CH3 ) or NH; (p) is 0 or 1; (n) is 0 or 1-3] and useful as a preventive/therapeutic agent for cancerous diseases, autoimmune diseases, chronic inflammatory diseases, etc. This compound is obtained by reaction of a compound of formula II with an active compound bearing activated carboxyl, amino or imino group in the presence of a solvent such as acetonitrile followed by eliminating the protecting group.

    5.
    发明专利
    未知

    公开(公告)号：TR199700178A2

    公开(公告)日：1997-09-21

    申请号：TR9700178

    申请日：1997-03-10

    Applicant: HOECHST AG

    Inventor： BOSSLET KLAUS ,  CZECH JOERG ,  GERKEN MANFRED ,  STRAUB RAINER ,  MONNERET CLAUDE ,  FLORENT JEAN-CLAUDE ,  SCHMIDT FREDERIC

    IPC: A61K31/70 ,  C07H15/203 ,  A61K31/7012 ,  A61K31/7028 ,  A61K31/7034 ,  A61K47/48 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07H15/26

    Abstract: Glycosyl derivatives of formula Glycosyl-YÄ-C(=Y)-X-Üp-W(R)n-Z-C(=Y)-active agent (I) and their salts are new: glycosyl = enzymatically cleavable poly-, oligo- or mono-saccharide; W = 5-14 membered aryl, naphthyl, indenyl, anthryl, phenanthryl, 5-14 membered heterocyclyl (containing 1-4 O, N or S), 1-6C alkyl, 2-6C alkenyl, 3-6C cycloalkyl or phenyl; R = H, 1-4C alkyl, phenyl, methoxy, carboxy, methyloxycarbonyl, CN, OH, NO2, F, Cl, Br, sulphonyl, sulphonamide or 1-4C sulphonalkylamide; p = 0-1; n = 0-3; X = O, NH, methyleneoxy, methyleneamino, methylene-1-4C alkylamino, 1-4C alkylamino, 3-6C cycloalkylamino; Y = O or NH; Z = 1-4C alkylamino, NCH3, C(CH3)2NH, CH(CH3)NH, C(CH3)2N(R ) or NH if W = 1-6C alkyl; R = 1-4C alkyl; and active agent = a compound with biological effect bonded via an oxygen, primary or secondary amine or an imino group.

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