PHARMACEUTICAL COMPOUNDS Russian patent published in 2024 - IPC C07D487/04 A61K31/4985 A61K31/5377 A61P35/00 

FIELD: pharmaceutics.

SUBSTANCE: invention relates to a compound of formula (I), or a tautomer thereof, or a pharmaceutically acceptable salt, where X is CH or N; R¹ is hydrogen, -CH₃ or -CH₂OH, but, when X is N, then R¹ is selected from -CH₃ and -CH₂OH; R₂ and R₃ are either (i) independently selected from hydrogen; or (ii) together form a one-to-three-membered bridging group selected from C_1-3alkylene; Q is C or N; wherein when Q is C, then either (i) R⁴ is hydrogen or C_1-4alkyl, optionally substituted with amino; R⁵ is amino, hydroxyl or C_1-4 alkyl, optionally substituted with 1 group selected from amino; provided that R⁴ and R⁵ must not both be selected from amino and C_1-4alkyl substituted with amino; or (ii) R⁴ and R⁵ together with Q form a four-to-six-member nitrogen-containing heterocyclic ring; and wherein when Q is N, then R⁴ is absent; R⁵ is hydrogen; and R² and R³ together form a one-to-three-member bridging group; R⁶ and R⁷ are independently selected from halogen and hydroxyl provided that, when Q is N, then R⁶ or R⁷ are not halogen or hydroxyl; a is selected from 0, 1 and 2; b is selected from 0 and 1; ring A is either (i) a five-membered nitrogen-containing heterocyclic ring, where the heterocyclic ring optionally contains one or two additional heteroatoms selected from N, O and S, or (ii) a six-membered aromatic nitrogen-containing heterocyclic ring, where the heterocyclic ring optionally contains one additional heteroatom selected from N; R⁸ is selected from -CH₃ and halogen; R⁹ is selected from hydrogen, C_1-4alkyl and halogen; R¹⁰ is independently selected from halogen, cyano, cyanoC_1-4alkyl, =O (oxo), C_1-4alkyl, C_1-4alkoxy, hydroxylC_1-4alkyl, C_1-4alkoxyC_1-4alkylene, diC_1-4alkylamino, -C_1-4alkylene-C(=O)NH_(2−q)(C_1-6alkyl)_q), C_1-4alkyl, substituted with an optionally substituted five- or six-membered unsaturated heterocyclic group containing 2 or 3 heteroatoms selected from O and N, where the optional substitute is selected from C_1-4alkyl, and an optionally substituted four to six-membered saturated heterocyclic group containing 1 or 2 heteroatoms selected from O and N; q is selected from 1 and 2; and c is selected from 0, 1, 2 and 3. Invention also relates to a method of producing said compound, a pharmaceutical combination and a composition based thereon.

EFFECT: novel compounds and a pharmaceutical composition based thereon, which can be used in medicine for treating cancer, are obtained.

48 cl, 18 tbl, 150 ex