PREPARATION AND USE OF KINASE INHIBITOR Russian patent published in 2019 - IPC C07D401/12 C07D473/28 C07D473/32 C07D473/36 C07D487/04 A61K31/52 A61K31/5377 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention refers to compounds of formula I or their pharmaceutically acceptable salts, which possess CDK4 kinase inhibiting activity. In formula IR₁ and R₂ are bound to a neighboring N atom, forming a C1-C8-alkyl substituted or unsubstituted 3–12-member saturated heterocycle, wherein said heterocycle refers to a ring structure containing 0–3 heteroatoms selected from a group consisting of N or O, in addition to a nitrogen atom attached to the nucleus; R₃ is selected from C1-C8-alkyl, CN, CONR₁₃R₁₄, C(O)R₁₅; R₁₃ and R₁₄ are independently selected from H or unsubstituted C1-C8-alkyl; R₁₅ is selected from unsubstituted 3–12-membered saturated heterocycle, wherein said heterocycle contains at least one heteroatom selected from a group consisting of N and O; R₄ is H; R₅ is H; X is CR₁₆; A, B and Z are independently selected from N or CR₁₆; R₁₆ is H or C1-C4-alkyl; L is absent or is C1-C6-alkylene; Y is where when W is O, then R₆ is absent, when W is N, then R₆ is H, unsubstituted C1-C8-alkyl or C(O)R₂₄; R₂₄ is unsubstituted C1-C8-alkoxy; R₇ can be 0-3 substitutes, which are unsubstituted C1-C8-alkyl; Ya is N; n and t independently represent 0, 1 or 2.

EFFECT: invention also relates to a method of producing said compounds, use thereof for preparing a medicament for treating a disease associated with CDK4 kinase activity or expression value; for preparation of inhibitor, targeted CDK4 kinase; and/or for treating a disease associated with CDK4 kinase activity or expression value, a pharmaceutical composition and methods of inhibiting CDK4 kinase activity and tumor cells in vitro using said compounds.

10 cl, 2 tbl, 3 ex