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Conjugates comprising nanoparticles coated with platinum containing compounds, processes for their preparation, pharmaceutical compositions comprising them and uses thereof

机译:包含包覆有含铂化合物的纳米颗粒的缀合物,其制备方法,包含它们的药物组合物及其用途

摘要

The present invention relates to conjugates of formula (I) having colloidal stability in a medium, wherein NP is a gold, silver or platinum nanoparticle; L is a linker selected from the group consisting of formula (II), formula (III), and a stereoisomer of any of the formulas (II) and (III), which is attached to the nanoparticle NP through sulfur atoms; wherein the meanings of X, n, p, Y and s are further specified in the description; and A is a platinum (II) biradical selected from the group consisting of formula (IV), formula (V) and formula (VI) including any of the stereoisomers of all of them, wherein the biradical is optionally in the form of a salt and is attached to the linker L through the single bonded oxygen atoms of the carboxyl groups. It also relates to a process for the preparation of the conjugates of formula (I) and to pharmaceutical compositions containing them. The conjugates of the invention are used for the treatment of cancer.
机译:本发明涉及在介质中具有胶体稳定性的式(I)的缀合物,其中NP是金,银或铂纳米颗粒。 L为选自由式(II),式(III)和式(II)和(III)中任一个的立体异构体组成的组的连接基,其通过硫原子连接至纳米颗粒NP;其中X,n,p,Y和s的含义在说明书中进一步规定;和A是选自由式(IV),式(V)和式(VI)组成的组的铂(II)双自由基,包括它们所有的立体异构体,其中双自由基任选地为盐的形式且通过羧基的单键合氧原子连接至接头L。本发明还涉及式(I)的缀合物的制备方法以及包含它们的药物组合物。本发明的缀合物用于治疗癌症。

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