PRODRUG OF THE AMINO ACID DERIVATIVE Russian patent published in 2020 - IPC C07C229/50 C07C255/47 C07C271/24 C07D213/61 C07D213/64 A61K31/196 A61P25/00 A61P37/02 A61P43/00 

FIELD: pharmaceutics.

SUBSTANCE: invention relates to a compound of formula (I-A) or formula (I), or a pharmaceutically acceptable salt thereof, which can be used as a drug exhibiting antagonist action on group 2 metabotropic glutamate receptors. In formula (I-A), R¹ denotes a C_1-6 alkyl group, a pyridyl group optionally substituted with one halogen atom, or formula (IIIA), where R^x denotes a hydrogen atom, a halogen atom, a C_1-6 alkyl group or C_1-6 alkoxy group, where each of C_1-6 alkyl group and C_1-6 alkoxy group is optionally substituted with one to three halogen atoms, and R^y denotes a hydrogen atom, a fluorine atom, a C_1-6 alkyl group or C_1-6 alkoxy group, where each of the C_1-6 alkyl group and C_1-6 alkoxy group is optionally substituted with one to three halogen atoms, R^1' denotes a hydrogen atom or C_1-6 alkyl group, or R¹ and R^1' optionally form a C_3-8 cycloalkane together with a carbon atom adjacent thereto, R² denotes C_3-6 alkyl group, C_3-8 cycloalkyl group optionally substituted by one to three C_1-6 alkyl groups, C_3-8 cycloalkoxy group, optionally substituted with one to three C_1-6 alkyl groups and optionally having C_1-5 alkylene group connecting two different carbon atoms in the ring, adamantyl group, optionally substituted by one to three C_1-6 alkyl groups or a phenyl group, R³ represents a hydrogen atom or C_1-6 alkyl group, R⁴ denotes a hydrogen atom or a fluorine atom. Invention also relates to a medicinal agent having antagonistic action on group 2 metabotropic glutamate receptors, which contains said compounds, and to an agent for preventing or treating a condition in which group 2 metabotropic glutamate receptors are involved.

EFFECT: what is offered is a prodrug of an amino acid derivative.

19 cl, 8 tbl, 39 ex