HETEROCYCLIC SPIRO COMPOUNDS AS MAGL INHIBITORS Russian patent published in 2020 - IPC C07D471/10 C07D493/10 C07D498/10 C07D401/12 A61K31/438 A61P25/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula I:

I

or a pharmaceutically acceptable salt thereof, where: ring A1 is cyclobutyl or 5–6-member heterocycloalkyl which contains 1 or 2 ring-forming heteroatoms selected from N and O; R¹ is R^1A or R^1B; R^1A is 1,1,1,3,3,3-hexafluoropropane-2-yl-; R^1B is 2,5-dioxopyrrolidin-1-yl; each R³ is C_1-4 alkyl; R⁴ is selected from a group consisting of R⁶, -N(R⁵)(C(=O)R⁶), -N(R⁵)(S(=O)₂R⁶), -C(=O)-R⁶, -S(=O)₂R⁶, -NR⁵R⁶, -SO₂NR⁵R⁶ and -OR⁶; R⁵ is selected from a group consisting of H or C_1-4 alkyl; R⁶ is selected from a group consisting of C_1-6 alkyl, C_3-10 cycloalkyl, 5–6-member heterocycloalkyl, phenyl, 5–6-member heteroaryl, (C_3-4 cycloalkyl) -C_1-4 alkyl-, (5–6-component heterocycloalkyl) -C_1-4 alkyl-, phenyl-C_1-4 alkyl- and (5–6-member heteroaryl) -C_1-4 alkyl-, wherein each of the selected versions is optionally substituted with one or more substitutes, each independently selected from a group consisting of halogen, -CN, C_1-4 alkyl, C_1-4 haloalkyl, C_1-4 alkoxy and C_1-4 haloalkoxy; where each of 5–6-member heteroaryl or 5–6-member heteroaryl moiety contains 1 or 2 ring-forming heteroatoms, each of which is independently selected from N, S and O, and where each of 5–6 membered heterocycloalkyl or 5–6-member heterocycloalkyl moiety includes 1 ring-forming O; t2 equals 0 or 1 and t3 equals 0 or 1.

EFFECT: disclosed are heterocyclic spiro compounds as MAGL inhibitors.

16 cl, 11 tbl, 14 ex