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首页> 外国专利> New nanoparticles comprising contrast and/or radiosensitizing agent, and functionalization graft for targeting nanoparticles, useful in e.g. therapy or medical imagery, and for treating tumors by X-ray irradiation or gamma irradiation

New nanoparticles comprising contrast and/or radiosensitizing agent, and functionalization graft for targeting nanoparticles, useful in e.g. therapy or medical imagery, and for treating tumors by X-ray irradiation or gamma irradiation

机译：包含造影剂和/或放射增敏剂的新纳米颗粒，以及用于靶向纳米颗粒的官能化接枝，例如可用于药物治疗。治疗或医学影像，以及通过X射线或γ射线治疗肿瘤

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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.
机译：包含造影剂和/或放射增敏剂的纳米颗粒以及用于靶向纳米颗粒表面上由接枝的目标分子组成的纳米颗粒的官能化接枝是新的，其中目标分子是季铵化合物（I），并且纳米颗粒具有球形具有1-50nm，优选2-5nm的平均直径的结构。包含造影剂和/或放射增敏剂以及用于靶向纳米粒子的功能化接枝的纳米粒子是新型的，其中所述官能化接枝物包括在纳米粒子表面上组成的接枝目标分子，其中目标分子是式（（A-M1-N）的季铵化合物+>（R1）（R3）-R2）X1→）（I），并且纳米颗粒具有平均直径为1-50nm，优选2-5nm的球形结构。 A：将目标分子，优选-NH 2，-CO 2H，-NCO，NCS，-COR4，-NHCOR4或-NHCSR4共价偶联的功能; R4：对硝基苯酚，五氟苯酚，1-羟基-7-氮杂苯并三唑，1-羟基苯并三唑或N-羟基酰亚胺的卤素或基团，例如N-羟基琥珀酰亚胺基团; M1：直链或支链的1-23C-烷基，其中一个或多个-CH 2-基团任选地被S，O，-NR，-CO，-CO-NH-，-NH-CO-NH-，- CO 2-，-SO-或-SO 2-; R：直链或支链1-6C烷基; R1-R3：直链或支链1-6C烷基;或R1-R3与N：含氮杂环基（任选地饱和并任选地被1-4C烷基，1-4C烷氧基或卤素取代），优选吡啶或哌啶;或X1：卤化物或磺酸盐。独立权利包括：（1）纳米颗粒的制备; （2）纳米颗粒的悬浮液; （3）通过除去液体，优选通过将悬浮液冷冻干燥而获得的固体材料; （4）注射用药物组合物，其包含纳米粒子或纳米粒子的悬浮液和载体。活动：细胞静息。作用机理：未给出。

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