(5,6-DIHYDRO)PYRIMIDO[4,5-E]INDOLYSINES Russian patent published in 2019 - IPC C07D471/14 A61K31/519 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula I or a pharmaceutically acceptable salt thereof, where R¹ is selected from a group consisting of:

R¹¹ is H, halogen, (1-2C)alkyl, (1-2C)alkoxy or OC²H₃, where all alkyl and alkoxy groups are optionally substituted with one or two halogens; R¹² is H; R¹³ is R¹³²O, R¹³³R¹³⁴N, R¹³⁵C(O), (2-7C)heterocycloalkyl selected from piperidinyl, piperazinyl, morpholinyl or azetidinyl, or (1-5C)heteroaryl, selected from pyrazolyl or isoxazolyl, where each heterocycloalkyl or heteroaryl is optionally substituted with 1-3 substituents (1-2C)alkyl, (1-2C)alkoxy, (1-6C)alkylcarbonyl, (1-6C)alkylsulfonyl, (1-5C)alkoxycarbonyl, (1-6C)alkylaminocarbonyl, (3-6C)cycloalkylcarbonyl or (2-7C)heterocycloalkylcarbonyl, in which said heterocycloalkyl is selected from azetidinyl or oxetanyl, where each alkylcarbonyl, cycloalkylcarbonyl or heterocycloalkylcarbonyl is optionally substituted with (1-2C)alkyl, fluoro or (1-2C)alkoxy; R¹³² is (1-6C)alkyl or (2-7C)heterocycloalkyl selected from piperidinyl, pyrrolidinyl, azetidinyl or tetrahydropyranyl, each of which is optionally substituted with one group selected from (1-2C)alkyl, (1-2C)alkoxy or di[(1-2C)alkyl]amino; R¹³³ is (1-6C)alkyl, optionally substituted with one group selected from di[(1-2C)alkyl]amino; R¹³⁴ is hydrogen or (1-2C)alkyl; R¹³⁵ is (2-7C)heterocycloalkyl selected from morpholine, thiazinane, diazepane or piperidine; (1-6C)alkylamino; di[(1-6C)alkyl]amino; (2-7C)heterocycloalkylamino, wherein said heterocycloalkyl is selected from piperidine, tetrahydropyran, azetidine and oxabicyclohexane; or (3-6C)cycloalkylamino, each of which is optionally substituted with one or two groups selected from (1-2C)alkyl, fluorine, hydroxyl, (1-2C)alkoxy, di[(1-2C)alkyl]amino, piperidinyl, oxo, cyano or amino; R¹⁴ is H, halogen or (1-2C)alkyl; R¹⁵ is H; R² is selected from a group consisting of:

R²¹ is H, halogen, (1-3C)alkyl, (1-2C)alkoxy, hydroxy(1-2C)alkyl or cyano; R²² is H; R²³ is H, halogen or (1-2C)alkyl; R²⁴ is H; R²⁵ is H, halogen or (1-3C)alkyl; R²⁶ is H, (1-6C)alkyl, azetidinyl, oxetanyl, (1-2C)alkoxy[(2-4C)alkoxy]_n(1-6C)alkyl, where n is integer of 1 or 2, all alkyl groups are optionally substituted with one group selected from (1-2C)alkoxy, hydroxyl, di[(1-2C)alkyl]amino or oxetanyl; provided that only one of R²¹ or R²⁵ in R² can be H. Invention also relates to a pharmaceutical composition as an inhibitor of TTK based on said compounds.

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EFFECT: novel compounds and a pharmaceutical composition based thereon, which can be used in medicine in treating cancer.

26 cl, 5 tbl, 163 ex