Analgesic with ester functionality

Patent US5045532 - Inner esters of gangliosides with analgesic-antiinflammatory activity

September 6, 2013 – 11:03

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BACKGROUND AND FIELD OF THE INVENTIONThe present invention concerns a new therapeutic application of the inner ester derivatives of gangliosides.

U.S. Pat. No. 4, 476, 119 and European Pat. No. 0072722 describe the preparation of the inner ester gangliosides and the use of the compounds as being valuable agents in the treatment of pathologies affecting the nervous system after trauma or diseases which in some way damage the nervous tissue, and as being more efficacious than gangliosides themselves.

The present invention reports the significant analgesic-antiinflammatory activity of individual inner ester gangliosides, in particular the inner ester of GM.sub.1, and of a mixture of inner ester gangliosides.

Gangliosides are a group of glycosphingolipids with a structure containing one saccharide part bound to a ceramide and to a sialic group. The saccharide part is composed of at least one galactose or glucose and of at least one N-acetylglucosamine or N-acetylgalactosamine.

The general structure of a ganglioside may therefore be represented by the following formula:

______________________________________ one mole of ceramide at least one mole of galactose or glucoseone mole of sialic acid at least one mole of N-acetylglucosamine or N-acetylgalactosamine______________________________________ in which these compounds are bound by glucosidic bonds.

Numerous gangliosides have been identified which have proved to be particularly abundant in the nervous tissue, especially in that of the brain. Various studies have demonstrated that the sialic groups most frequently encountered in gangliosides are N-acetylneuraminic acid (NANA) and to a lesser extent, N-glycolylneuraminic acid. Of the numerous gangliosides identified, the following gangliosides, classified by their international symbols, were found to exist in considerable measure in the mixtures derived from bovine brain tissue: ##STR1## where Glc stands for glucose, GalNAC stands for N-acetylgalactosamine, Gal stands for galactose, NANA stands for N-acetylneuraminic acid and the percentages in parenthesis indicate the quantity of each ganglioside found in a mixture of gangliosides extracted from bovine brain tissue.

It is well known that gangliosides play an important role in the nervous system and it has recently been shown that gangliosides are useful in therapy for pathologies of the peripheral and central nervous systems [Acta Psychiat. Scand., 55, 102, (1977); Brain Res. 197, 236, (1980); Drugs of Today 22, 73-107, (1986)].

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