1,1,1-TRIFLUORO-3-HYDROXYPROPANE-2-YLCARBAMATE DERIVATIVES AS MAGL INHIBITORS Russian patent published in 2020 - IPC C07D401/08 C07D401/12 C07D491/10 A61K31/4747 A61P25/00 

Abstract RU 2720203 C1

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula I

I

or pharmaceutically acceptable salts thereof, where R1 is H; fragment M-1 of formula I

M-1 is a fragment of formula M-1a, M-1b or M-1c:

, , ,

each of R2A and R2C independently represents -NR3S(=O)2R4, -NR3C(=O)R4; R5 or -OR5; R2B is selected from a group comprising [4-(trifluoromethyl)-1H-pyrazol-1-yl]methyl,cyclopentylcarbonyl)(methyl)amino-(tert-butylsulfonyl)(methyl)amino-(2,2-dimethylpropanoyl)(methyl)amino-, 4-(trifluoromethyl)-1H-pyrazol-1-yl-, 4-fluoro-1H-pyrazol-1-yl-, 3-cyanophenyl-, 6-(trifluoromethyl)pyridin-2-yl-, 5-fluoropyridin-2-yl-, 4-(difluoromethyl)-1H-pyrazol-1-yl-, 4-tert-butyl-1H-pyrazol-1-yl-, 4-chloro-1H-pyrazol-1-yl-, 4-cyclopropyl-1H-pyrazol-1-yl-, 4-methyl-1H-pyrazol-1-yl-, 2-fluorophenyl-, 4-cyano-3-fluorophenyl-, 3-cyano-4-fluorophenyl-, 5-cyano-2-fluorophenyl-, 4-cyanophenyl-, 2,6-difluorophenyl-, 2,4-difluorophenyl-, 4-fluorophenyl-, 4-(difluoromethyl)pyridin-2-yl-, 6- (difluoromethyl)pyridin-3-yl-, 5-cyanopyridin-2-yl-, 5-(difluoromethyl)pyridin-2-yl-, 5-(trifluoromethyl)pyridin-2-yl-, pyridin-2-yl-, 3-tert-butyl-1H-pyrazol-1-yl-, 3-(trifluoromethyl)-1H-pyrazol-1-yl-, 3,4-dimethyl-1H-pyrazol-1-yl-,{[(3,3-difluorocyclobutyl)methyl]sulfonyl}(methyl)amino-, [(3,3-difluorocyclobutyl)carbonyl](methyl)amino-, 1H-indazol-1-yl-, 3-cyano-2-fluorophenyl-, and 4-cyano-2-fluorophenyl-; each R3 independently represents C1-3 alkyl; each R4 is independently selected from C1-6 alkyl, C3-7 cycloalkyl, (C3-7 cycloalkyl)-C1-2 alkyl-, (phenyl)-C1-2 alkyl- and phenyl, where each of the selected versions is substituted with 0, 1, 2 or 3 halogens; and each R5 is phenyl or 5- or 6-member heteroaryl, wherein each phenyl or 5- or 6-member heteroaryl is substituted with 0, 1, 2 or 3 substitutes (see claim 1); methods of producing; a composition containing such compounds and use thereof for treating MAGL mediated diseases and disorders.

EFFECT: compounds of the present invention can be used for treating MAGL-mediated diseases and disorders.

22 cl, 19 tbl, 19 ex

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RU 2 720 203 C1

Authors

Brodney, Michael Aaron

Butler, Christopher Ryan

Mcallister, Laura Ann

Helal, Christopher John

O'Neil, Steven Victor

Verhoest, Patrick Robert

Dates

2020-04-27Published

2018-01-08Filed