6-(PYRIMIDINOAMINO-PYRIDINE)BENZOIMIDAZOLE DERIVATIVES, USEFUL FOR TREATMENT OF CANCER Russian patent published in 2018 - IPC C07D401/14 C07D471/08 C07D471/10 C07D487/04 C07D487/10 C07D498/04 C07D498/08 A61K31/496 A61K31/506 A61K31/5377 A61K31/5383 A61P35/00 

Abstract RU 2670762 C2

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry, specifically to 6-(pyrimidinoamino-pyridine)benzoimidazole derivatives of formula (I') or a stereoisomer thereof, wherein A1 and A2 are independently selected from nitrogen; R1 is selected from C1-6alkyl; R2 is selected from C1-6alkyl; R3 and R5 are independently selected from halogen; R4 is selected from a nitrogen-containing 5–6 membered heterocyclyl, optionally substituted with Q2, where the nitrogen-containing 5–6 membered heterocyclyl is a nitrogen-containing 5–6 membered heterocyclyl containing 1 to 2 nitrogen atoms; a nitrogen-containing 7–9 membered bridged heterocyclyl optionally substituted with Q2, where the nitrogen-containing 7–9 membered bridged heterocyclyl is a nitrogen-containing 7–9 membered bridged heterocyclyl containing 1 to 2 nitrogen atoms; 6–10-membered fused heterocyclyl which contains 1, 2 or 3 identical or different heteroatoms and is optionally substituted with Q2, wherein the heteroatoms are selected from a nitrogen atom and an oxygen atom, and comprise at least one nitrogen atom; a nitrogen-containing 7–11-membered spiro-heterocyclyl, optionally substituted with Q2, where the nitrogen-containing 7-11-membered spiro-heterocyclyl is a nitrogen-containing 7-11 membered spiro-heterocyclyl containing 1 to 2 nitrogen atoms; Q2 is selected from amino or di-C1-6alkylamino; or from C1-6alkyl, 3-8-membered cycloalkyl, oxacyclobutanyl, nitrogen-containing 5-6 membered heterocyclyl, or a nitrogen-containing 8-membered bridged heterocyclyl, each of which is optionally substituted with a substituent, wherein the substituent is selected from C1-6alkyl and 3-8 membered cycloalkyl; n is selected from 0, 1. Invention also relates to a pharmaceutical composition capable of inhibiting the activity of CDK4 and/or CDK6 kinases based on a compound of formula (I').

EFFECT: technical result is novel compounds useful for reducing or inhibiting the activity of CDK4/6 kinase in a cell and/or in the treatment and/or prevention of cancer related diseases mediated by CDK4/6 kinase.

23 cl, 12 tbl, 36 ex

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RU 2 670 762 C2

Authors

U Frank

Chen Bo

Dates

2018-10-25Published

2014-12-30Filed