BENZAMIDE DERIVATIVE, METHOD FOR PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING CANCER, CONTAINING THEREOF AS ACTIVE INGREDIENT Russian patent published in 2025 - IPC C07D209/14 C07D401/12 C07D401/14 C07D403/14 C07D413/14 A61K31/506 A61K31/497 A61K31/501 A61K31/4545 A61K45/06 A61P35/00 A23L33/10 

FIELD: chemistry.

SUBSTANCE: invention relates to a benzamide derivative of formula 1 or an optical isomer thereof. In formula 1, the values of the variables are as follows: X, Y and Z independently represent CH or N; R¹ is -H, halogen, C_1-10 alkyl, unsubstituted or substituted with one or more halogens, C_1-10 alkoxy, unsubstituted or substituted with one or more halogens, nitro, C_1-10 alkylsulfanyl, cyano or 5-membered heteroaryl containing 2 ring heteroatoms N; R² is a substituted phenyl or substituted 6-member heteroaryl containing 1–2 ring heteroatoms N, where said substituted phenyl is phenyl substituted with 1–2 substitutes selected from halogen, C_1-10 alkyl and amino-substituted piperidinyl, where said substituted 6-member heteroaryl is 6-member heteroaryl substituted with 1–2 substitutes selected from halogen, unsubstituted C_1-10 alkyl substituted C_1-10 alkyl, C_1-5 alkyl-substituted bicyclic 8-member heterocycloalkyl containing 2 ring heteroatoms N, and unsubstituted or substituted 4–8-membered fully or partially saturated heterocycloalkyl containing 1–2 heteroatoms N, where said substituted C_1-10 alkyl is substituted with 5–6 membered heterocycloalkyl containing 1 ring heteroatom N, which is substituted with 1 or 2 C_1-5 alkyl-substituted amino groups, where said substituted 4–8-membered fully or partially saturated heterocycloalkyl is 4–8-membered heterocycloalkyl substituted with one substituent selected from the group consisting of -OH, C_1-5 alkyl, C_1-5 alkyl substituted with 5–6-membered heterocycloalkyl containing 1–2 ring heteroatoms selected from N and O, amino, unsubstituted or substituted with 1 or 2 C_1-5 alkyl, 5–6-membered heterocycloalkyl containing 1 ring heteroatom N and unsubstituted or substituted C_1-5 alkyl, C_1-5 alkoxycarbonyl, 5–6 membered heteroaryl containing 1–3 ring heteroatoms N, phenylaminocarbonyl and C_1-5 alkoxy-C_1-5 alkoxy-phenyl; R³ is a halogen; R⁴ is -OH or C_1-15 alkoxy; R⁵ is -H; and R⁶ is -H or halogen. Also disclosed is the use of a compound of formula 1 or an optical isomer thereof for producing a drug for treating cancer with an EGFR mutation.

EFFECT: disclosed benzamide derivative can be used for preventing or treating cancer by suppressing the EGFR mutation and, when administered in combination with an EGFR antagonist, such as cetuximab, exhibits a significant synergistic anticancer effect.

8 cl, 2 tbl, 72 ex