Bisacyloxypropylcysteine conjugates and their use

A - Human Necessities – 61 – K

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A61K 47/48 (2006.01)

Patent

CA 2489010

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.

La présente invention concerne de nouveaux conjugués lipopeptidiques dans lesquels une cystéine doublement substituée par un acide gras est liée par un groupe carboxyle à un radical conjugué polymère, à bonne solubilité dans l'eau, toléré du point de vue physiologique et non immunogène. Les conjugués de l'invention ont un très bon effet stimulant sur les macrophages et ne nécessitent l'utilisation d'aucun agent de solubilisation supplémentaire. Ils ont de nombreuses applications, notamment pour stimuler des macrophages, pour stimuler la synthèse d'anticorps, pour lutter contre les infections, pour stimuler l'immunité, notamment contre des tumeurs, pour prévenir et traiter des chocs septiques, pour soigner des lésions, et en tant qu'adjuvants à des vaccins.

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