mTOR KINASE INHIBITORS FOR ONCOLOGICAL INDICATIONS AND DISEASES METABOLICALLY BOUND TO mTOR/PI3K/AKT Russian patent published in 2015 - IPC C07D487/04 A61K31/4985 A61P35/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: in general formulas R¹ represents substituted phenyl, substituted or unsubstituted heterocyclyl, which represents an aromatic cycloalkyl containing 6 to 10 atoms in the cycle and wherein one to two carbon atoms in the cycle are independently substituted by N, wherein the above substitutes are specified in C_1-8alkyl, triazolyl, halogen, aminocarbonyl, cyano or hydroxyalkyl; R² represents H, substituted or unsubstituted C_1-8alkyl, substituted C_3-6cycloalkyl, unsubstituted heterocyclyl, which represents non-aromatic cycloalkyl containing 5 to 6 atoms in the cycle and wherein one to two carbon atoms in the cycle are independently substituted by N or O; unsubstituted heteroyclylalkyl, wherein heterocyclyl represents non-aromatic cycloalkyl containing 5 to 6 atoms in the cycle and wherein one to two carbon atoms in the cycle are independently substituted by N and O; substituted or unsubstituted phenylalkyl or substituted or unsubstituted C_3-6cycloalkylalkyl, wherein the above substitutes are specified in C_1-4alkyl, CF₃, OR and NR₂, wherein R represents H or C_1-4alkyl; each R³ and R⁴ independently represents H, unsubstituted C_1-8 alkyl, or R³ and R⁴ together with the atom to which they are attached form C_3-6cycloalkyl; or R² and one of R³ and R⁴ together with the atom to which they are attached form substituted or unsubstituted heterocyclyl containing 5 to 6 atoms in the cycle and which can contain additional heteroatom specified in O; wherein the substitutes are specified in -C(O)CH₂OCH₃, -CH₂CH₂OCH₃, OCH₃ or CH₃.

EFFECT: invention refers to compounds of formula

and ,

a based pharmaceutical composition and to a method of treating or preventing cancer, immunological conditions, diabetes, obesity, neurological disturbances and age-related diseases, a method for mTOR kinase inhibition in a cell, a method of treating or preventing the condition, which can be treated or prevented by mTOR kinase metabolic path inhibition.

53 cl, 1 tbl, 20 ex