New conjugate comprising active substance that interacts with mitochondrial biomacromolecules, mitochondrial targeting signal peptide, and cell-penetrating transport system, useful for treating tumor and neurodegenerative diseases

摘要

Conjugate comprising (a) at least one active substance that interacts specifically with mitochondrial biomacromolecules, (b) at least one mitochondrial targeting signal peptide, which causes a specific uptake into mitochondria, and (c) at least one cell-penetrating transport system, is new. Conjugate comprising (a) at least one active substance that interacts specifically with mitochondrial biomacromolecules, (b) at least one mitochondrial targeting signal peptide, which causes a specific uptake into mitochondria, and (c) at least one cell-penetrating transport system, is new. The conjugate has a structure of formula (I). mts : mitochondrial targeting signal peptide; W1 : active substance; Z : cell-penetrating transport system; X : a stable bond; and Y1 : a biodegradable bond, where the bond between the active substance and the mitochondrial targeting signal peptide is a stable or biocompatible bond, such as amide, thioester or ester bond, and the linkage between the active substance and the cell-penetrating transport system is a biodegradable, cleavable linkage by enzymes, disulfides or esters. An independent claim is included for the preparation of conjugate. ACTIVITY : Cytostatic; Neuroprotective; Antiparkinsonian; Nootropic. MECHANISM OF ACTION : None given.