| 摘要 |
Nanoparticles comprising a contrast and/or radiosensitizing agent, and a functionalization graft for targeting the nanoparticles consisting a grafted targeted molecule in the surface of the nanoparticles are new, where the targeted molecule is a quaternary ammonium compound (I) and the nanoparticles have a spherical structure with an average diameter of 1-50 nm, preferably 2-5 nm. Nanoparticles comprising a contrast and/or radiosensitizing agent, and a functionalization graft for targeting the nanoparticles consisting a grafted targeted molecule in the surface of the nanoparticles are new, where the targeted molecule is a quaternary ammonium compound of formula ((A-M1-N +>(R1)(R3)-R2)X1 ->) (I) and the nanoparticles have a spherical structure with an average diameter of 1-50 nm, preferably 2-5 nm. A : a function for covalent coupling of targeted molecule to the nanoparticles, preferably -NH 2, -CO 2H, -NCO, NCS, -COR4, -NHCOR4 or - NHCSR4; R4 : halo or a radical of p-nitrophenol, pentafluorophenol, 1-hydroxy-7-azabenzotriazole, 1-hydroxybenzotriazole or N-hydroxyimide such as N-hydroxysuccinimide radical; M1 : linear or branched 1-23C-alkyl, in which one or more -CH 2- groups are optionally replaced by S, O, -NR, -CO, -CO-NH-, -NH-CO-NH-, -CO 2-, -SO- or -SO 2-; R : linear or branched 1-6C alkyl; either R1-R3 : linear or branched 1-6C alkyl; or R1-R3 together with N : nitrogen-containing heterocyclic radical (optionally saturated and optionally substituted by 1-4C alkyl, 1-4C alkoxy or halo), preferably pyridine or piperidine; and X1 : halide or sulfonate. Independent claims are included for: (1) the preparation of nanoparticles; (2) a suspension of the nanoparticles; (3) a solid material obtained by elimination of a liquid, preferably by freeze-drying the suspension; and (4) an injectable pharmaceutical composition comprising the nanoparticles or the suspension of nanoparticles and a carrier. ACTIVITY : Cytostatic. MECHANISM OF ACTION : None given. |
