DERIVATIVES OF 2,4-SUBSTITUTED PHENYLENE-1,5-DIAMINE AND THEIR USES, PHARMACEUTICAL COMPOSITIONS AND PHARMACEUTICALLY ACCEPTABLE COMPOSITIONS OBTAINED FROM THEM Russian patent published in 2018 - IPC C07D471/04 C07D401/14 C07D401/04 C07D403/12 C07D403/04 C07D403/14 C07D413/14 A61K31/506 A61K31/53 A61K31/5377 A61P35/00 A61P37/02 A61P25/28 A61P3/10 A61P9/00 

FIELD: chemical-pharmaceutical industry.

SUBSTANCE: invention relates to a novel derivative of a 2,4-substituted phenylene-1,5-diamine of formula (I) or a pharmaceutically acceptable salt thereof, having an inhibitory activity against tyrosine kinase EGFR. Such a disease is cancer, diabetes, immune system diseases, neurodegenerative diseases, cardiovascular diseases or a disease with acquired resistance during treatment using EGFR modulators. In this case, the disease with acquired resistance is caused by mutations of T790, encoded by the 20th exon EGFR, or the content of T790 mutations encoded by the 20th EGFR exon. In the compound of formula (I)

A is any chosen from

or

where Z₂ is a CR₅ or N; R₅ is hydrogen; Z₂₁ is N; each of R₄, R₄₂, R₄₃ is independently hydrogen or C_1-6 alkyl, 6-membered heterocycloalkyl containing a -NH group in the ring or C_1-6 haloalkyl; R₄₁ is hydrogen or halogen; R₀ is hydrogen; Z₁ is a CR₆, where R₆ is hydrogen, halogen, trifluoromethyl, methoxy or -CO₂C_1-10 alkyl; R₁ is hydrogen or is any selected from the group consisting of:

each of R₂ and R₃ independently represents hydrogen; R₁₂ is C_1-6 alkoxy.

EFFECT: compounds can be used in the manufacture of a medicament for controlling the activity of EGFR tyrosine kinase (epidermal growth factor receptor) or the treatment of EGFR-dependent diseases.

9 cl, 127 ex, 9 tbl