FLUORINE-CONTAINING COMPOUND AND USE THEREOF IN CANCER MEDICINE Russian patent published in 2024 - IPC C07F9/564 A61K31/664 A61P35/00 

FIELD: chemistry.

SUBSTANCE: present invention relates to medical chemistry, specifically to a compound of formula II or III or a pharmaceutically acceptable salt thereof, where R₁ is C₆-C₁₀ aryl or Z-substituted C₆-C₁₀ aryl, six-membered nitrogen-containing heteroaryl, quinoline, isoquinoline, Z-substituted quinoline or Z-substituted isoquinoline; R₂ is a hydrogen atom, a halogen atom, cyano, C₁-C₆ alkyl or halogen-substituted C₁-C₆ alkyl, C₃-C₈ cycloalkyl or Z-substituted C₃-C₈ cycloalkyl, C₆-C₁₀ aryl or Z-substituted C₆-C₁₀ aryl, Z-substituted nitrogen-containing heteroaryl, halogen-substituted alkoxy, having from 1 to 6 carbon atoms, -CONR⁶R⁷; R₃ is a hydrogen atom; R₄ and R₅ each independently represents a hydrogen atom; R⁶ and R⁷ are each independently C₁-C₆ alkyl, C₆-C₁₀ aryl or R⁶ and R⁷ together with the atom to which they are attached form 4–6-membered heterocyclyl or Z-substituted 4–6-membered heterocyclyl; R₈ and R₁₀ each independently represent a hydrogen atom; R₉ is substituted C₆-C₁₀ aryl, which is substituted with at least one fluorine atom; substituent Z is a halogen atom, cyano, hydroxy, C₁-C₃ alkyl, phenyl or halogen-substituted C₁-C₃ alkyl, halogen-substituted C₁-C₃ alkoxy, C₃-C₈ cycloalkyl or substituted C₃-C₈ cycloalkyl, aromatic ring or substituted aromatic ring, wherein the substitution by its type is mono- or disubstitution on the same atom; substituent in substituted C₆-C₁₀ aryl in R₉ is a halogen atom. Invention also relates to an individual compound of formula , to use of the compound of formula II or III for preparing a medicinal agent, to a medicinal agent containing an effective amount of the compound of formula II or III, to a method of producing said compound.

EFFECT: development of DNA-alkylating agents activated under action of AKR1C3 enzyme, which can be used for cancer treatment.

16 cl, 1 tbl