FIELD: chemistry.
SUBSTANCE: invention relates to compounds that affect latent defects in cellular processing of CFTR activity. What is proposed is a compound selected from N-(2,4-di-tert- butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide, characterized by at least one carbon atom substituted with silicon and the carbon substituted with silicon being a non-aromatic carbon; and optionally, one or more hydrogen atoms being replaced by deuterium. Also proposed are variants of the compound and a method for increasing the activity of the transmembrane regulator of cystic fibrosis using these compounds.
EFFECT: proposed compounds have an improved safety profile while maintaining biological efficacy compared to analogue compounds free of silicon.
16 cl, 2 tbl, 17 ex
| Title | Year | Author | Number |
|---|---|---|---|
| COMPOUNDS, COMPOSITIONS AND METHODS FOR INCREASING CFTR ACTIVITY | 2015 |
|
RU2767460C2 |
| COMPOUNDS, COMPOSITIONS AND METHODS FOR CFTR MODULATION | 2016 |
|
RU2752567C2 |
| 3-CARBOXAMIDE-4-OXOQUINOLINE DERIVATIVES, USEFUL AS MODULATORS OF REGULATOR OF TRANSMEMBRANE CYSTIC FIBROSIS CONDUCTIVITY | 2010 |
|
RU2518897C2 |
| METHOD OF MODULATING TRANSPORTERS OF ATP-BINDING CASSETTE | 2005 |
|
RU2525115C2 |
| MODULATORS OF ATP-BINDING CARTRIDGE TRANSPORTERS | 2005 |
|
RU2528046C2 |
| MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS | 2005 |
|
RU2556984C2 |
| ATP-BINDING CASETTE TRANSPORTER MODULATORS | 2005 |
|
RU2382779C2 |
| METHOD OF OBTAINING MODULATORS OF CYSTIC FIBROUSIS TRANSMEMBRANE CONDUCTANCE REGULATOR | 2010 |
|
RU2543714C2 |
| MODULATORS OF ATP-BINDING TRANSPORTERS | 2010 |
|
RU2552353C2 |
| PHARMACEUTICAL COMPOSITIONS FOR TREATING DISEASES MEDIATED BY CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR | 2015 |
|
RU2744460C2 |
