NOVEL HETEROCYCLIC COMPOUNDS AS MONOACYLGLYCEROL LIPASE INHIBITORS Russian patent published in 2022 - IPC C07D498/04 A61K31/5365 A61K31/5377 A61P25/06 A61P25/08 A61P25/16 A61P25/24 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula (I), where (i) X is CR³; m is 0 or 1; n is selected from 0, 1 and 2; and L is selected from -(CH₂)_P-, -O-, -OCH₂-, -CH₂OCH₂-, -CF₂CH₂-, -CH₂=CH₂- and -(CR¹⁶R¹⁷)_q-CH₂O-; or (ii) X is N; m is equal to 1; n is equal to 1; and L is -(CH₂)_P-; p is selected from 1 and 2; q is 0 or 1; A is selected from: (i) phenyl substituted with R⁴, R⁵ and R⁶; (ii) 5–9 membered heteroaryl containing 1, 2 or 3 heteroatoms independently selected from O, S and N, substituted with R⁷, R⁸ and R⁹; and (iii) 6-membered heterocycloalkyl containing 1 heteroatom, which is N, substituted with R¹⁰, R¹¹ and R¹², where one of R¹⁰, R¹¹ and R¹² is hydrogen, and the other two are halogen; R¹ is hydrogen or C_1-6-alkyl; R² is selected from hydrogen and C_1-6-alkyl; R³ is selected from hydrogen, halogen, C_1-6-alkyl and halogen-C_1-6-alkyl; each of R⁴, R⁵, R⁶, R⁷, R⁸ and R⁹ is independently selected from hydrogen, halogen, cyano, hydroxy, C_1-6-alkyl, halogen-C_1-6-alkyl, C_1-6-alkanoyl, C_1-6-alkoxy, halogen-C_1-6-alkoxy, SF₅, C_3-10-cycloalkyl, 5–9-membered heterocycloalkyl, where 1 or 2 of said ring atoms are heteroatoms selected from N and O, 4–7-membered heterocycloalkyl, where 1 of said ring atoms is a heteroatom selected from N, substituted with R¹⁴ and R¹⁵, 5-member heteroaryl containing 2 or 3 heteroatoms selected from N, phenyl, phenoxy, halogen-phenyl and halogen-phenoxy; each of R¹⁴ and R¹⁵ is independently selected from C_1-6-alkyl, C_1-6-alkoxy and halogen; and R¹⁶ and R¹⁷ together with the carbon atom to which they are attached form C_3-10-cycloalkyl. Invention also relates to a method of producing said compounds of formula (I).

EFFECT: novel compounds which can be used in medicine to produce a drug for MAGL inhibition are obtained.

41 cl, 13 tbl, 278 ex