N2-(2-PHENYL)-PYRIDO[3,4-D]PYRIMIDINE-2,8-DIAMINE DERIVATIVES AND USE THEREOF AS MPS1 INHIBITOR Russian patent published in 2019 - IPC C07D471/04 A61K31/519 A61P35/00 

FIELD: chemistry; pharmaceutics.

SUBSTANCE: invention relates to a compound of formula I or a pharmaceutically acceptable salt thereof, wherein in formula IR₁ is selected from group comprising 5-member heteroaryl, optionally containing one or more (C₁-C₄) alkyl substitutes; R₂ is selected from a group comprising (C₁-C₃) alkoxy group or (C₁-C₃) fluoroalkoxy group; and R₃ and R₄ are linked to each other such that together with the nitrogen atom to which they are attached form 4-, 5-, 6- or 7-member heterocyclic ring bonded by the nitrogen atom, where said ring is optionally condensed with additional 3-member carbocyclic ring, to form a bicyclic heterocyclic system, or optionally linked through a spiran carbon atom with additional 4-, 5- or 6-member carbocyclic or heterocyclic ring to form a spirobicyclic ring system; and where the heterocyclic ring, bicyclic ring system or spirobicyclic ring system optionally contains one or more substitutes independently selected from a group comprising halogen, trifluoromethyl, difluoromethyl, cyano group, (C₁-C₄) alkyl, NR_iR_j, OR_i, where R_i and R_j all independently selected from a group comprising H or (C₁-C₄) alkyl; where each "heteroaryl" can contain from 1 to 4 heteroatoms independently selected from O, N and S atoms; and where each "heterocyclyl" or "heterocyclic group" can contain 1 or 2 heteroatoms independently selected from O, N and S. Invention also relates to methods of producing said compounds and a pharmaceutical composition for treating a disease or pathological condition associated with kinase activity Mps1, based on said compounds.

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EFFECT: technical result is obtaining novel compounds and pharmaceutical compositions based thereon, which can be used in medicine for treating and/or preventing proliferative diseases, such as cancer.

17 cl, 62 ex