O-sulfated gangliosides and lyso-ganglioside derivatives
AssigneeFidia S.p.A.
InventorsAurelio Romeo, Gunter Kirschner, Carlo Chizzolini, Hari Manev, Laura Facci
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AssigneeFidia S.p.A.
InventorsAurelio Romeo, Gunter Kirschner, Carlo Chizzolini, Hari Manev, Laura Facci
Estimating the term…
Disclosed are derivatives of gangliosides and of N-acyl-N-lyso-gangliosides, of N'-acyl-N'-lyso-gangliosides and N,N'-di- or poly-acyl-N,N'-di-lyso-gangliosides, in which at least one of the hydroxyl groups in the saccharide, sialic or ceramide residues is esterified with sulfuric acid, functional derivatives thereof, and their salts with either inorganic or organic bases and the acid addition salts, except persulfated derivatives at the hydroxyl, sialic and ceramide groups of the GM.sub.1, GD.sub.1a, GD.sub.1b and GT.sub.1b gangliosides. Such compounds have antineurotoxic and neurotogenic activity and may therefore be used in pharmaceutical preparations. Also a marked modulating effect on the expression of the CD.sub.4 molecule in immune system cells has been shown.
Sulfated ester derivatives of gangliosides, N-acyl-N-lyso-gangliosides, N'-acyl-N'-lyso-gangliosides, N-acyl-N,N'-dilyso-gangliosides, N'-acyl-N,N'-dilyso-gangliosides, N,N'-di-lyso-gangliosides and poly-acyl-N,N'-di-lyso-gangliosides having saccharide, sialic and ceramide residues with hydroxyl groups, wherein at least one of the hydroxyl groups is esterified with sulfuric acid to form sulfate groups so that the molar ratio of sulfate groups to sialic residues is from 1:1 to 5:1;
A compound having a sulfated hydroxyl group selected from the group consisting of mono-sulfated derivatives of:
A compound having one or more sulfated hydroxyl groups selected from the group consisting of mono- and poly-sulfated derivatives of:
A compound having one or more sulfated hydroxyl groups selected from the group consisting of mono- and polysulfated derivatives of
Compounds having one or more sulfated hydroxyl groups selected from the group consisting of mono-sulfated and polysulfated derivatives of a ganglioside selected from the group consisting of the following gangliosides:
A method for inhibiting glutamate induced and N-methyl-D-aspartate induced neurocytotoxicity which comprises administering to a patient in need thereof sulfated GM.sub.1, GD.sub.1a, GD.sub.1b and GT.sub.1b gangliosides having the hydroxyl sialic acid and ceramide groups thereof esterified with sulfuric acid, wherein the molar ratio of sulfate groups to sialic residues is from 1:1to 5:1.
Pharmaceutical preparations containing as the active ingredients a compound selected from the group consisting of
Dependencies are inferred from the claim text.