Heterobifunctional cross-linking agent conjugate substituted...

A - Human Necessities – 61 – K

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A61K 47/48 (2006.01) A61K 39/00 (2006.01) A61K 49/00 (2006.01) C07D 307/00 (2006.01) C07D 487/08 (2006.01) C07F 5/02 (2006.01)

Patent

CA 2409255

The present invention relates to compounds comprising three components. Component (1) is a heterobifunctional cross-linking agent to which component (2) having immunomodulating function is linked by covalent link. Said compound also comprises a component (3) having a linking function to the cell surface. According to the invention, the links between component (1) and component (2) are labile depending on pH. The present invention further relates to methods for producing the above-mentioned compounds, a drug containing said compounds and the use thereof especially in the treatment of tumor diseases.

La présente invention concerne des composés qui comprennent trois composants. Le composant (1) est un agent de réticulation hétérobifonctionnel, auquel le composant (2), qui présente une fonction d'immunomodulateur, est lié par liaison covalente. Ledit composé comprend également un composant (3), qui présente une fonction de liaison à la surface des cellules. Selon cette invention, les liaisons entre le composant (1) et le composant (2) sont labiles en fonction du pH. La présente invention concerne également des procédés de production des composés susmentionnés, un médicament contenant de tels composés, ainsi que l'utilisation de tels composés, notamment dans le traitement de maladies tumorales.

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