INHIBITORY COMPOUNDS Russian patent published in 2021 - IPC C07D487/04 A61K31/519 A61P35/00 

FIELD: pharmaceutics.

SUBSTANCE: invention relates to a compound or its pharmaceutically acceptable salt represented by the structural formula (Id), in which R₁ is a group of the formula: -L-Y-Q, where: L is absent or is (1-5C)alkylene; Y is absent, and Q is hydrogen, (1-6C)alkyl, (3-10C)cycloalkyl or 4-6-element monocyclic and saturated heterocycpyl containing one nitrogen heteroatom; where Q is optionally substituted with one or more groups of substituents independently selected from (1-4C)alkyl, OR_c and C(O)OR_c; where R_c is independently selected from hydrogen, (1-6C)alkyl and (3-6C)cycloalkyl; X₄ is CR_n; where: R_n is selected from hydrogen, halogen and (1-4C)alkyl; R₂ is hydrogen; Q₃ is hydrogen, (1-6C)alkyl, (1-6C)alkoxy, phenyl, phenyl(1-2C)alkyl, (3-8C)cycloalkyl or 5-6-element heteroaryl containing 1-3 heteroatoms selected from nitrogen, oxygen and sulfur; wherein Q₃ is optionally substituted with one or more substituents independently selected from (1-4C)alkyl, halogen, (1-4C)halogenalkyl and OR_t, where R_t is independently selected from hydrogen, (1-4C)alkyl and (3-6C)cycloalkyl; or Q₃ is optionally substituted with a group of the formula: -L₄-L_Q4-Z₄, where: L₄ is absent or is (1-3C)alkylene; L_Q4 is absent or is O; and Z₄ is hydrogen, (1-6C)alkyl, phenyl or (3-8C)cycloalkyl. The invention also relates to a pharmaceutical composition having inhibitory activity against RET kinase based on the specified compound.

EFFECT: new compound and a pharmaceutical composition based on it are obtained, which can be used in medicine in the treatment of cancer, as well as other diseases or conditions, in which the activity of RET kinase is involved.

19 cl, 2 tbl, 60 ex