Bisacyloxypropylcysteine conjugates and the use thereof
AssigneeGBF Gesellschaft fur Biotechnologische Forschung mbH
InventorsPeter Muhlradt, Michael Morr
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Abstract
The invention relates to novel lipopeptide conjugates, in which a cysteine that is double-substituted by a fatty acid is bonded by means of the carboxyl group to a highly soluble, physiologically compatible and non-immunogenic, polymeric conjugate group. The novel conjugates exhibit an excellent macrophage stimulant action and do not require additional solutizing. They can be used in a wide range of applications, in particular for stimulating macrophages, for stimulating antibody synthesis, for combating infection, as an immunostimulant, in particular in relation to tumours, for preventing and treating septicaemic shock, for wound healing and as an adjuvant for vaccines.
Claims10
A bisacyloxypropylcysteine conjugate according to formula (I),
- where R1 and R2 can be identical or different and are fatty acid radicals which are bonded by way of the carboxyl group,
- Y═—NH—, —O—, —S— or —OCO—,
- R3 is a covalently, ionically or associatively bonded conjugate radical, in particular a water-soluble and physiologically tolerated, covalently or ionically bonded polymer, in particular covalently bonded polyethylene glycol (polyoxyethylene), —(CH2—CH2—O)m—CH2—CH2—X,
- where X═OR, NR2, SR or COOR, and
- R═H, benzyl- or C1-6-alkyl, where several radicals R can be identical or different, a polyoxyethylene-polyoxypropylene copolymer, a dextran, a sugar, a polyvinylpyrrolidone, an alginate, a pectin or a collagen, and where the polymeric radical R3 is substituted once, twice or several times by
Dependencies are inferred from the claim text.