MTOR KINASE INHIBITORS FOR ONCOLOGIC INDICATIONS AND DISEASES ASSOCIATED WITH MTOR/PI3K/AKT BY METABOLISM Russian patent published in 2019 - IPC A61K31/4985 A61P29/00 A61P9/00 A61P25/28 C07D487/04 

FIELD: chemistry.

SUBSTANCE: invention relates to use of compounds of formula (I) or (II), where R¹ is a substituted phenyl, substituted or unsubstituted heterocyclyl which is an aromatic cycloalkyl containing 6 to 10 atoms in a ring and in which one to two carbon atoms in the cycle are independently substituted on N, where said substitutes are selected from C_1-8alkyl, triazolyl, halogen, aminocarbonyl, cyano or hydroxyalkyl; R² is H, substituted or unsubstituted C_1-8alkyl substituted with C_3-6cycloalkyl, unsubstituted heterocyclyl, which is a non-aromatic cycloalkyl containing from 5 to 6 atoms in a cycle and in which one to two carbon atoms in the cycle are independently substituted with N or O; unsubstituted heterocyclylalkyl, where heterocyclyl is a non-aromatic cycloalkyl containing 5 to 6 atoms in a ring and in which one to two carbon atoms in the cycle are independently substituted with N and O; substituted or unsubstituted phenylalkyl or substituted or unsubstituted C_3-6cycloalkylalkyl, where said substitutes are selected from C_1-4alkyl, CF₃, OR and NR₂, where R is H or C_1-4alkyl; R³ and R⁴, each independently represent H, unsubstituted C_1-8alkyl or R³ and R⁴ together with atom, to which they are attached form C_3-6cycloalkyl; or R² and one of R³ and R⁴ together with atoms to which they are bonded, form a substituted or unsubstituted heterocyclyl containing from 5 to 6 ring atoms and which may contain an additional heteroatom selected from O; where the substitutes are selected from -C(O)CH₂OCN₃, -CH₂CH₂OCN₃, OCH₃ or CH₃; provided that the compound is not 6-(4-hydroxyphenyl)-4-(3-methoxybenzyl)-3,4-dihydropyrazino[2,3-b]pyrazine-2(1H)-one, 6-(4-(1H-1,2,4-triazol-5-yl)phenyl)-3-(cyclohexylmethyl)-3,4-dihydropyrazino[2,3-b]pyrazine-2(1H)-one or (R)-6-(4-(1H-1,2,4-triazol-5-yl)phenyl)-3-(cyclohexylmethyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, to obtain a pharmaceutical composition for treating conditions mediated by mTOR kinase, selected from inflammatory conditions, neurodegenerative diseases and cardiovascular conditions.

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EFFECT: technical result is new activity of compounds of formula (I) or (II), which can be used in medicine for treating inflammatory conditions, immunological conditions, neurodegenerative diseases.

50 cl, 1 tbl, 20 ex