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    • 9. 发明申请
    • COMPOSITIONS COMPRISING A PLATINUM COMPLEX, LIPID, AND SURFACTANT
    • 包含铂复合物,脂质和表面活性剂的组合物
    • WO2006084248A3
    • 2006-12-07
    • PCT/US2006004152
    • 2006-02-06
    • ANTIGENICS INCTRUNEH ALEMSEGEDDZIEWISZEK KRZYSZTOFLUI GUI
    • TRUNEH ALEMSEGEDDZIEWISZEK KRZYSZTOFLUI GUI
    • A61K9/127
    • A61K9/127A61K9/19
    • Disclosed are compositions comprising a lipid, a surfactant, and a platinum complex having the formula II: Pt R K9/ \ K7 (II) wherein R6 and R7 each independently represent a leaving group; wherein R8 and R9 are each amines substituted by a group selected from a substituted or unsubstituted alkyl, -aryl, -arylalkyl, heteroalkyl, heterocyclyl, heteroaryl, heteroarylalkyl, -alkenyl, -cycloalkyl, or -cycloalkenyl groups having between 4 and 20 carbon atoms; or R8 and R9 are linked together as represented by formula (Ha): (Ha) and wherein said lipid is capable of forming a liposome. The compositions of the invention are more stable (e.g., resistant to solids formation) than are conventional liposomal platinum compositions which do not contain a surfactant. Also disclosed are methods for making the compositions and the use of the compositions for treating or preventing cancer.
    • 公开了包含脂质,表面活性剂和具有式II的铂络合物的组合物:其中R 6和R 7各自独立地表示离去基团; 其中R8和R9各自被选自取代或未取代的烷基,芳基, - 芳基烷基,杂烷基,杂环基,杂芳基,杂芳基烷基, - 烯基, - 环烷基或具有4-20个碳原子的 - 环烯基 ; 或者R 8和R 9连接在一起,如式(IIa)所示:(IIa),并且其中所述脂质能够形成脂质体。 本发明的组合物比不含表面活性剂的常规脂质体铂组合物更稳定(例如耐固体形成)。 还公开了制备组合物和组合物用于治疗或预防癌症的方法。