NOVEL THERAPEUTIC VECTORS AND PRODRUGS FOR TREATING CANCER Russian patent published in 2024 - IPC C07D405/14 A61K31/4025 A61P35/00 

FIELD: chemistry.

SUBSTANCE: present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, which can be used to treat cancer:

In formula IR_a is H or (C₁-C₁₂)alkyl group, in chain which optionally contains one or more oxygen atoms; L is a group having the formula (II) shown below:

where: A is an anti-cancer agent; Y is an electron-acceptor group; X is -O-; G is a glucuronyl radical or a derivative thereof selected from glucuronide ester radicals; L₁ is a linker of formula (III) shown below: -A₁-A₂-A₃-A₄-A₅-A₆-A₇- … (III) where: A₁ is a (C₁-C₆)alkylene radical; A₂ is a triazole radical; A₃ is a (C₁-C₆)alkylene radical; and 4 is selected from a group consisting of: -C(=O)-NR_b-, -C(=S)-NR_b-, -NR_b-C(=O)-, -NR_b-C(=S)- and NR_b, where R_b is H or (C₁-C₁₂) alkyl group; A₅ is a (C₁-C₃₂)alkylene radical, the chain of which contains at least one oxygen atom; A₆ is a triazole radical; A₇ is a (C₁-C₆)alkylene radical; L' is a group of formula (IV) shown below: -A₈-A₉-L'' … (IV), where: A₈ is a (C₁-C₂₆)alkylene radical, the chain of which contains at least one oxygen atom; and 9 is selected from a group consisting of -NR_c-, -O- and -S-, R_c is H or (C₁-C₁₂) alkyl group; L'' is a radical capable of reacting with an amino group, a hydroxyl or thiol group, and said radical has the following formula:

,

where L''' is a (C₁-C₁₂) alkylene radical, optionally substituted with an electron-acceptor group, or a phenylene radical, optionally substituted with an electron-acceptor group.

EFFECT: development of systems for selective release of anticancer agents in tumour microenvironment.

14 cl, 4 dwg