ERBB/BTK INHIBITORS Russian patent published in 2022 - IPC C07D239/48 C07D251/48 C07D401/12 C07D403/12 C07D405/12 C07D487/00 A61K31/505 A61K31/506 A61P35/02 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound by the formula (I) or a pharmaceutically acceptable salt, ester, hydrate, solvate or stereoisomer thereof. In the formula (I): A₁ represents N or CR₈, each from A₂, A₃, A₄ and A₅ independently represents N or CR₉, wherein no more than one from A₂, A₃, A₄ and A₅ represents N, each from R₁ and R₂ independently represents hydrogen or a C_1-12alkyl, possibly monosubstituted with an -NR^aR^b, C_1-12alkyl, 3-10-membered saturated carbocyclyl or 3-6-membered saturated heterocyclyl containing one heteroatom selected from N and O, wherein each from the 3-10-membered saturated carbocyclyl and the 3-6-membered saturated heterocyclyl can be not substituted or be mono- or polysubstituted with a C_1-12alkyl, wherein each from R^a and R^b is independently selected from hydrogen or a C_1-12 alkyl, possibly monosubstituted or independently polysubstituted with deuterium or tritium, or R^a and R^b, taken together with the nitrogen atom whereto they are linked, form a 3-10-membered saturated heterocyclyl possibly monosubstituted with a C_1-12alkyl, or R₁ and R₂, taken together with the nitrogen atom whereto they are linked, form a 3-12-membered monocyclic or polycyclic ring, possibly containing one additional heteroatom selected from N and O, possibly monosubstituted or independently polysubstituted with a halogen, C_1-12alkyl, -NR^aR^b or a -C_1-12alkyl-NR^aR^b group, R₃ represents H, a C_1-12alkyl or -C_1-12alkyl-NR^aR^b, each from R₄ and R₅ independently represents a C_1-6alkyl, possibly monosubstituted or independently polysubstituted with one or more than one deuterium, tritium or halogen, or R₄ and R₅, taken together with the carbon atom whereto they are linked, form a 3-10-membered monocyclic ring, possibly containing one oxygen heteroatom O, possibly monosubstituted or independently polysubstituted with one or more than one deuterium or tritium, R₆ represents hydrogen, R₇ represents a C_1-12alkyl, possibly mono- or polysubstituted with deuterium or tritium, R₈ represents hydrogen, deuterium, tritium, halogen, cyano, C_1-12alkyl, C_1-12alkoxyl possibly monosubstituted or independently polysubstituted with one or more than one deuterium, tritium or a halogen, R₉ is absent or represents hydrogen, deuterium or tritium, n equals 0, 1, 2, 3, or 4, each R independently represents halogen, a C_1-12alkyl, 3-10-membered saturated carbocyclyl or 3-6-membered saturated or unsaturated heterocyclyl containing one hetero-atom N, wherein said heterocyclyl is condensed with a ring whereto it is linked, possibly monosubstituted or independently polysubstituted with one or more than one deuterium, tritium, halogen or a C_1-12alkyl. Also proposed are a pharmaceutical composition and a method for treating a tyrosine kinase-associated disease.

EFFECT: proposed ErbB and BTK inhibiting compounds can effectively treat diseases associated with ErbB (in particular, mutant forms of ErbB) or BTK, including cancer.

25 cl, 9 tbl, 104 ex