Antigen derivatives and processes for their preparation
AssigneeCiba-Geigy Corporation
InventorsGerhard Baschang, Felix M. Dietrich, Roland Gisler, Albert Hartmann, Jaroslav Stanek, Lajos Tarcsay
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Abstract
The invention relates to novel antigen derivatives comprising an antigen and at least one muramylpeptide covalently bonded thereto, if appropriate via a spacer, to pharmaceutical preparations which contain such compounds and to their use as a vaccine. The novel antigen derivatives produce a pronounced increase in the immuno-response to the antigen, and in particular also a cell-medicated immunity under clinically acceptable conditions of administration.
Claims15
A muramyl-peptide of the general formula ##STR10## in which X is a carbonyl group, R.sub.1, R.sub.4 and R.sub.6 are tri-lower alkyl-silyl, R.sub.2 is unsubstituted or substituted alkyl or carbocyclic aryl, R.sub.3 is hydrogen or alkyl, R.sub.7 and R.sub.13 are hydrogen or lower alkyl, R.sub.8 is hydrogen, lower alkyl, free, esterified or etherified hydroxy-lower alkyl, free, esterified or etherified mercapto-lower alkyl, free or acylated amino-lower alkyl, cycloalkyl having 5 or 6 carbon atoms, cycloalkyl-lower alkyl, of which the cycloalkyl radical contains 5 or 6 carbon atoms, unsubstituted or substituted aryl or aralkyl, nitrogen-containing heterocyclyl or heterocyclyl-lower alkyl, R.sub.7 and R.sub.8 together can also be alkylene having 3 or 4 carbon atoms, R.sub.9 is hydrogen or lower alkyl, the radicals R.sub.10 and R.sub.12 independently of one another are a carboxyl radical which may or may not be esterified or amidised, and R.sub.11 is hydrogen or a carboxyl radical which may or may not be esterified or amidised.
Dependencies are inferred from the claim text.