PYRAZOLINE DIONE DERIVATIVES AS NADPH-OXIDASE INHIBITORS Russian patent published in 2015 - IPC C07D471/14 C07D498/14 C07D403/04 C07D413/04 A61K31/551 A61K31/437 A61P35/00 A61P25/00 A61P11/00 A61P9/00 A61P5/00 

Abstract RU 2569855 C2

FIELD: chemistry.

SUBSTANCE: invention relates to pyrazoline dione derivative of formula

,

as well as to its pharmaceutically acceptable salt, where R1 is selected from hydrogen; possibly substituted C1-C6alkyl; possibly substituted phenyl; possibly substituted C1-C6alkylphenyl; possibly substituted phenylC1-C6alkyl; possibly substituted pyridyl; possibly substituted C1-C6alkylpyridyl; and possibly substituted pyridylC1-C6alkyl; R2 is hydrogen; R3 is hydrogen; R4, R5, R6 and R7 are hydrogen; R8, R9, R10 and R11 are independently selected from hydrogen atoms and C1-C6alkyls; R12 is selected from hydrogen; -CHR17R18; possibly substituted C1-C6alkoxy-carbonyl, possibly substituted -C(O)-phenyl; possibly substituted C1-C6alkylphenyl; possibly substituted phenylC1-C6alkyl, possibly substituted C1-C6alkylheteroaryl or possibly substituted heteroarylC1-C6alkyl, where heteroaryl is selected from pyridyl, pyrrolyl, pyrimidinyl, furyl, imidazolyl, oxazolyl, isoxazolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, 1,2,3-oxadiazolyl, 1,2,4-oxadiazolyl, 1,2,5-oxadiazolyl, 1,3,4-oxadiazolyl, 1,3,4-triazinyl and 1,2,3-triazinyl; R17 and R18 are independently selected from hydrogen; possibly substituted phenyl; possibly substituted heteroaryl, where heteroaryl is selected from pyridyl, pyrrolyl, pyrimidinyl, furyl, imidazolyl, oxazolyl, isoxazolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, 1,2,3-oxadiazolyl, 1,2,4-oxadiazolyl, 1,2,5-oxadiazolyl, 1,3,4-oxadiazolyl, 1,3,4-triazinyl and 1,2,3-triazinyl; X is selected from O, NR12, S and S(O)2; n is integer number, selected from 0 and 1; with term "substituted" meaning that said group is substituted with 1-5 substituents, selected from "C1-C6alkyl", "C1-C6alkoxy" and "halogens". Invention also relates to pharmaceutical composition, based on formula (I) compound, intermediate compound of formula

,

method of obtaining formula (I) and (II) compounds.

EFFECT: novel pyrazoline dione derivatives, useful for inhibition of activity or function of nicotinamide adenine dinucleotide phosphate-oxidase (NADPH-oxidase), have been obtained.

17 cl, 2 tbl, 23 ex

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RU 2 569 855 C2

Authors

Pazh Patrik

Gadzhini Francheska

Lale Benua

Dates

2015-11-27Published

2010-09-27Filed