06-09-2018 дата публикации
Номер: US20180251423A1
Compounds of formula (I) having 1-sulfonamido-4-aryloxy as a basic backbone. A preliminary activity test showed that the compounds provide excellent interference of a binding of Nrf2 by Keap1, thereby activating Nrf2. The compounds have a potential anti-inflammatory activity and can be used to treat a plurality of inflammation-associated diseases, including chronic obstructive pulmonary disease (COPD), Alzheimer's disease, Parkinson's disease, atherosclerosis, chronic kidney disease (CKD), diabetes, gastroenteritis, rheumatoid arthritis, and the like. 2. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein Rrepresents 4-methoxy claim 1 , 4-bromo claim 1 , 4-chloro claim 1 , 4-fluoro claim 1 , 2 claim 1 ,4 claim 1 ,6-trimethyl claim 1 , 4-tert-butyl claim 1 , 2 claim 1 ,4 claim 1 ,6-trimethoxy claim 1 , 4-methyl claim 1 , 3 claim 1 ,4-dimethoxy claim 1 , 4-acetamido or 4-trifluoromethyl.3. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein Rrepresents 4-methoxy claim 1 , 4-ethoxy claim 1 , 4-isopropoxy claim 1 , 4-fluoro claim 1 , 4-chloro claim 1 , 4-bromo claim 1 , 4-acetamido claim 1 , 4-trifluoromethyl claim 1 , 4-hydroxyl claim 1 , 4-morpholinylmethoxy claim 1 , 4-morpholinylethoxy claim 1 , 4-amino claim 1 , or 4-benzylamino.5. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein n represents 0 or 1.6. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein the pharmaceutically acceptable salt is a sodium claim 1 , potassium or calcium carboxylates of the compound of Formula (I).8. A pharmaceutical composition claim 1 , comprising the compound according to or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier.9. A method for treating an inflammation-associated disease comprising administering to a patient in need thereof claim 1 , an effective amount of the compound ...
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