NOVEL PYRIMIDINE-2,4-DIAMINE DERIVATIVES, METHOD FOR PREPARING THEM AND PHARMACEUTICAL COMPOSITION CONTAINING THEM AS ACTIVE INGREDIENT FOR PREVENTING OR TREATING CANCER Russian patent published in 2024 - IPC C07D401/12 C07D401/14 C07D403/12 C07D403/14 A61K31/506 A61P35/00 

FIELD: pharmaceutics.

SUBSTANCE: invention relates to a pyrimidine-2,4-diamine derivative of formula 1, method for its preparation and a pharmaceutical composition for preventing or treating cancer, containing it as an active ingredient. In formula 1, X is a sulphonyl or carbonyl; R¹ is halogen, C_1–10 straight or branched chain alkyl, unsubstituted or substituted with one or more halogens, carboxyl or C_1–10 alkoxycarbonyl with straight or branched chain; R² is -NR_b1R_b2, R_b1 and R_b2 each independently represent, unsubstituted or substituted C_1–10 alkyl with straight or branched chain, or R_b1 and R_b2 are taken together with the nitrogen atom to which they are bonded to form an unsubstituted or substituted 3–7 membered heterocycloalkyl containing 1 heteroatom, which is N, where the substituted C_1–10 alkyl with a straight or branched chain can be -NR_c1R_c2, and substituted 3–7 membered heterocycloalkyl substitute can be -NR_c1R_c2 or C_1–10 straight or branched chain alkyl, and R_c1 and R_c2 are each independently C_1–10 alkyl with a straight or branched chain, or R_c1 and R_c2 are taken together with a nitrogen atom to which they are attached, to form an unsubstituted or substituted 3–7 membered heterocycloalkyl containing 1 or 2 heteroatoms representing N, where substituted 3–7 membered heterocycloalkyl substitute can be C_1–10 straight or branched chain alkyl; and R³, R⁵ and R⁶ are each independently hydrogen, or C_1–10 alkoxy with a straight or branched chain; R⁴ is C_1–10 alkyl with a straight or branched chain; R⁷ and R⁸ are each independently hydrogen; n is integer from 0 to 3; and p and q each independently represent integer from 1 to 3.

EFFECT: pyrimidine-2,4-diamine derivative demonstrates high inhibitory ability against EGFR and HER2 mutations and can be successfully used in treating cancer in which EGFR and HER2 mutations have occurred.

12 cl, 7 tbl, 53 ex