FIELD: chemistry.
SUBSTANCE: invention relates to carboxamide derivatives of an isoxazoline series of general formula 1, having properties which enable to deactivate receptors PAR-2 (receptors activated by proteases), as well as to a method for decontaminating the PAR-2 receptor, as well as to an active component of formula 1, having anti-inflammatory action. In general formula 1, X represents nitrogen atom, or C-H, or C-Cl; R1 substitute is 2,6-dimethylphenyl, 4-methyl-2-chlorophenyl, mesityl, 4-methoxy-3-trifluoromethylphenyl, 3,4-dimethylphenyl, 2-methyl-6-chlorophenyl, 2-trifluoromethyl-4-chlorophenyl, 4-trifluoromethoxyphenyl, 3,4-dicyanophenyl, 4-chlorpyridin-2-yl, 4-isopropoxy-3-cyanophenyl, 3-chloro-4-cyanophenyl, 4-(trifluoromethylphenyl); R2 substitute, R3 can be selected from the following set - hydrogen, C1-C6 alkyl.
EFFECT: compounds can be used for treating inflammatory diseases, particularly rheumatoid arthritis, as well as other diseases, the treatment of which can be associated with deactivation of PAR2 receptors.
4 cl, 1 tbl, 6 ex
Title | Year | Author | Number |
---|---|---|---|
2-ARYL-SUBSTITUTED N-ARYLIMIDAZOLINES, SELECTIVE CYCLOOXYGENASE-2 INHIBITORS, METHODS FOR PRODUCTION AND USE THEREOF | 2014 |
|
RU2565667C1 |
IMIDAZOLINE DERIVATIVES HAVING CB-ANTAGONIST ACTIVITY | 2005 |
|
RU2357958C2 |
HETEROCYCLIC TGR5 BILE ACID RECEPTOR AGONISTS, PHARMACEUTICAL COMPOSITION, METHODS FOR PREPARING AND USING THEM | 2013 |
|
RU2543485C2 |
PHARMACEUTICAL COMPOSITION FOR PREVENTION OR TREATMENT MACULAR DEGENERATION | 2012 |
|
RU2576380C2 |
DERIVATIVES OF PYRAZOLINE, METHODS FOR THEIR PREPARING AND PHARMACEUTICAL COMPOSITION | 1999 |
|
RU2233272C2 |
BENZOPYRAZINE AND BENZOXEPINE PI3K INHIBITORS AND USE THEREOF | 2009 |
|
RU2506267C2 |
DERIVATIVES OF 4,5-DIHYDRO-1H-PYRAZOLE POSSESSING CB-ANTAGONISTIC ACTIVITY | 2002 |
|
RU2281941C2 |
THIENOPYRIDONE CARBOXAMIDES AND THEIR MEDICAL USE | 2005 |
|
RU2374250C2 |
NOVEL DERIVATIVES OF 4,5-DIHYDRO-1H-PYRAZOLE SHOWING CB-ANTAGONISTIC ACTIVITY | 2002 |
|
RU2299199C2 |
TETRASUBSTITUTED IMIDAZOLE DERIVATIVES AS CANNABINOID CB RECEPTOR MODULATORS, HIGHLY SELECTIVE TO SUBRANGE RECEPTORS CB/CB | 2005 |
|
RU2354650C2 |
Authors
Dates
2019-11-01—Published
2018-06-19—Filed