DNA-PK INHIBITORS Russian patent published in 2017 - IPC C07D405/14 C07D401/14 C07D491/56 C07D413/14 C07D401/04 C07D403/04 C07D239/42 C07D409/04 C07D413/04 C07D413/10 C07D417/04 C07D417/14 C07D471/04 C07D491/48 A61K31/505 A61K31/506 A61K31/53 A61K31/5377 A61K31/517 A61P35/00 

FIELD: biotechnology.

SUBSTANCE: invention relates to a novel compound of formula (I) or a pharmaceutically acceptable salt thereof, inhibiting DNA-dependent protein kinase (DNA-PK). The compounds can be used in the treatment of cancer. The compounds have a radiosensitizing effect on the line of cancer cells sensitive to radiation and can be used to enhance the effect of the therapeutic regimen for the treatment of cancer. In general formula (I), X is N or CR^A5; R^A1is F, C_1-4-alkyl, C_3-5cycloalkyl, OC_1-4-alkyl, OC_1-4-alkyl-C_3-5cycloalkyl, NH₂, NHC_1-4-alkyl, NHC_1-4-alkyl-C_3-5cycloalkyl or C_0-4-alkylheterocyclyl, the said heterocyclic ring system being selected from oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, or morpholinyl, and each of the said alkyl, cycloalkyl or heterocyclyl is optionally substituted with a maximum of three F atoms, a maximum of three ²H atoms, a maximum of two non-hemin OH groups, or a maximum of two OC_1-2-alkyl; each R^A4 is independently H or ²H; R^A5 is hydrogen, F, C_1-4-alkyl or OC_1-4-alkyl, each of the said alkyls being optionally substituted with a maximum of three F atoms or a maximum of three ²H atoms; R^B3 is C (O) NHC_1-4-alkyl. The said alkyl is optionally substituted with a maximum of three F atoms, a maximum of three ²H atoms, a maximum of two non-hemin OH groups, or a maximum of two OC_1-2-alkyl; and each R^B4 is independently hydrogen, deuterium, F, or C_1-4-alkyl.

EFFECT: improved compound properties.

18 cl, 3 tbl, 14 ex