05-03-2020 дата публикации
Номер: US20200071264A1
Принадлежит:
Benzylamino-oxoethyl benzamide compounds for use in treating diseases and conditions associated with abnormal cell function related to endoplasmic reticulum (ER) stress. For example, the compounds can be used as suppressors of ER stress-induced pancreatic β-cell dysfunction and death, for example in the treatment of Type 1 and Type 2 diabetes. The compounds can also be used in treatments for chronic heart disease, neurodegenerative diseases, retinal degeneration, and other metabolic disorders associated with ER stress. 2. The compound of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and R=H claim 1 , R=OH claim 1 , R=CF claim 1 , and n=1.3. The compound of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and R=H claim 1 , R=OH claim 1 , and R=CF claim 1 , and n=1.4. The compound of claim 1 , wherein n=1 claim 1 , R=H claim 1 , R=CF claim 1 , and Rand Rare selected from the group consisting of H and OH claim 1 , with the proviso that one of Rand R=H claim 1 , and one of Rand R=OH.5. The compound of of disposed in a pharmaceutically-acceptable carrier claim 1 , diluent or vehicle claim 1 , forming a composition.6. A conjugate claim 1 , comprising the compound of covalently linked to a targeting molecule claim 1 , wherein the targeting molecule is able to bind to a target cell or a portion of a target cell.7. The conjugate of claim 6 , wherein the targeting molecule targets a pancreatic β-cell.9. The method of claim 8 , wherein in chemical structure I: R claim 8 , R claim 8 , R claim 8 , R claim 8 , R claim 8 , R claim 8 , R claim 8 , and R=H claim 8 , R=OH claim 8 , R=CF claim 8 , and n=1.10. The method of claim 8 , wherein in chemical structure I: R claim 8 , R claim 8 , R claim 8 , R claim 8 , R claim 8 , R claim 8 , R claim 8 , R claim 8 , and R=H claim 8 , R=OH claim 8 , R=CF claim 8 , and n=1.11. The method of claim 8 , wherein in chemical ...
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