6,7-DIHYDROPYRAZOLO[1,5-A]PYRAZINE-4(5H)-ONE COMPOUNDS AND USE THEREOF AS NEGATIVE ALLOSTERIC MODULATORS OF mGluR2 RECEPTORS Russian patent published in 2020 - IPC C07D487/04 A61K31/4985 A61K31/4178 A61P25/00 

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry and specifically to a compound of formula (I)

or a stereoisomeric form thereof or a tautomer or a pharmaceutically acceptable salt thereof. In the compound of formula (I): R¹ is phenyl optionally substituted with one or more substituents, each of which is independently selected from a group consisting of halogen, C_1-4alkyl, monohalogen-C_1-4alkyl, polyhalogen-C_1-4alkyl and -CN; R² is selected from a group consisting of H; C_1-4alkyl; C_3-7cycloalkyl; -CN; -NR^aR^b; -C(O)NR^cR^d; -C_1-4alkyl-OC_1-4alkyl; aryl; Het and C_1-4alkyl, substituted with one or more substitutes, each of which is selected from halogen; where each of R^a, R^b, R^c and R^d is independently selected from H and C_1-4alkyl; aryl is phenyl; Het is 6-membered aromatic heterocyclyl substitute selected from a group consisting of pyridinyl and pyrazinyl, each of which can be optionally substituted with one substitute selected from a group consisting of C_1-4alkyl and -NR^eR^f; each of R^e and R^f is hydrogen; R³ is selected from a group consisting of hydrogen, halogen, C_1-4alkyl and -CN; R⁴ is hydrogen; and R⁵ is C_1-4alkyl. Also disclosed are a pharmaceutical composition, use thereof and a method for production thereof, and use of the compound of formula (I).

EFFECT: technical result is obtaining novel derivatives of 6,7-dihydropyrazolo[1,5-a]pyrazine-4(5H)-one as negative allosteric modulators (NAM) of metabotropic glutamate receptors of subtype 2 ("mGluR2").

14 cl, 8 tbl, 8 ex