[EN] LYSINE DERIVATIVES FUNCTIONALISED WITH LIPIDS<br/>[FR] DÉRIVÉS DE LYSINE FONCTIONNALISÉS AVEC DES LIPIDES
申请人:DSM IP ASSETS BV
公开号:WO2010112615A1
公开(公告)日:2010-10-07
The present invention relates to amino-acid derivatives functionalized with lipids. The amino-acid derivatives are functionalized with lipids via amide, urea or urethane bonds. The derivatives preferably have melting points in the range from 40 to 80 °C. The amino-acid derivative comprises protected lysinediisocyanate. The lipids are chosen from fatty alcohols, fatty amines, fatty acids, cholesterol or sterols. The invention also relates to a process for the preparation of amino-acid derivatives functionalized with lipids via amide, urea or urethane bonds by the reaction of a lipid with a protected lysinediisocyanate. The present invention further relates to the use of the amino acid derivatives in drug delivery.
本发明涉及与脂质功能化的氨基酸衍生物。氨基酸衍生物通过酰胺、脲或脲醚键与脂质功能化。这些衍生物的熔点优选在40至80°C范围内。氨基酸衍生物包括受保护的赖氨酸二异氰酸酯。脂质选择自脂肪醇、脂肪胺、脂肪酸、胆固醇或甾醇。本发明还涉及一种制备氨基酸衍生物与脂质功能化的方法,通过将脂质与受保护的赖氨酸二异氰酸酯反应形成酰胺、脲或脲醚键。本发明还涉及在药物输送中使用氨基酸衍生物。