PROPOSED 3,4-DIHYDRO-2,7-NAPHTHYRIDINE-1,6(2H,7H)-DIONES AS MEK INHIBITORS Russian patent published in 2024 - IPC C07D471/04 A61K31/4375 A61P35/00 

Abstract RU 2826000 C1

FIELD: organic chemistry.

SUBSTANCE: group of inventions includes a compound of formula I, a compound of formula II, 8-((2-fluoro-4-(methylthio)phenyl)amino)-2-(2-hydroxyethoxy)-7-methyl-3,4-dihydro-2,7-naphthyridine-1,6(2H,7H)-dione and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them, method of treatment and use based on 8-((2-fluoro-4-(methylthio)phenyl)amino)-2-(2-hydroxyethoxy)-7-methyl-3,4-dihydro-2,7-naphthyridine-1,6(2H,7H)-dione. In formula I R1 represents H, Br, C1-C6 alkyl or phenyl; R2 is H, halogen or CH3-; R3 is H, hydroxyC1-C6 alkyl-, hydroxyC1-C6 alkoxy-, C1-C6 alkoxy, fluoroC1-C6 alkoxy, C3-C6 cycloalkyl or (C3-C6 cycloalkyl)C1-C6 alkoxy-; R4 is phenyl substituted with 1, 2 or 3 substituents, independently selected from halogen, C1-C6 alkyl, C1-C6 alkylthio, fluoroC1-C6 alkylthio, fluoroC1-C6 alkyl, C1-C6 alkoxy, fluoroC1-C6 alkoxy, C3-C6 cycloalkyl and C1-C6 alkyl-C(=O)-. In formula II, R1 is H, Br, C1-C6 alkyl or phenyl; R2 is H, halogen or CH3-; R3 is H, hydroxyC1-C6 alkyl-, hydroxyC1-C6 alkoxy-, C1-C6 alkoxy, fluoroC1-C6 alkoxy, C3-C6 cycloalkyl or (C3-C6 cycloalkyl)C1-C6 alkoxy-; Ra and Rb are independently selected from halogen, C1-C6 alkyl, C1-C6 alkylthio, fluoroC1-C6 alkyl, C1-C6 alkoxy, fluoroC1-C6 alkoxy, C3-C6 cycloalkyl and C1-C6 alkyl-C(=O)-.

EFFECT: derivatives of 3,4-dihydro-2,7-naphthyridine-1,6(2H,7H)-dione, having MEK inhibitory activity.

36 cl, 5 dwg, 8 tbl, 77 ex

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RU 2 826 000 C1

Authors

Allen, Shelley

Blake, James Francis

Blanche, Sydney Taylor

Boys, Mark Laurence

Clark, Wesley Dewitt

Cowdrey, Connor James

Dahlke, Joshua Ryan

Doerner Barbour, Patrick Michael

Kellum, Alex Andrew

Knapp, Ellen Margaret

Moreno, David Austin

O'Leary, Jacob Matthew

Ren, Li

Witkos, Faith Elizabeth

Fulton, Jennifer Lynn

Dates

2024-09-03Published

2022-03-30Filed