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Phenoxazine analogs useful as inhibitors of amyloid aggregation and treatment of alzheimer's disease and amyloidosis-related disorders

机译:苯恶嗪类似物可用作淀粉样蛋白聚集的抑制剂,并治疗阿尔茨海默氏病和淀粉样变性病相关疾病

摘要

"Useful phenoxazine analogues as inhibitors of amyloid aggregation and treatment of Alzheimer's disease and amyloidosis-related dysfunctions". Compounds of Formula I wherein: R1 is hydrogen, lower alkyl, or cycloalkyl; R 2 is hydrogen, lower alkyl, lower alkoxy, halogen, hydroxyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, aryloxyxyl, heteroarylalkoxy, cyano, carboxyl, alkoxycarbonyl, carbamoyl, sulfamoyl, nitro, trifluoromethyl or amino alkylamino; and R 3 and R 4 are independently hydrogen, lower alkoxy, aryl, heteroaryl, halogen, hydroxyl, cyano, carboxyl, alkoxycarbonyl, carbamoyl, sulfamoyl, nitro, trifluoromethyl, amino, mono- or di-alkylamino or lower alkyl or unsubstituted or substituted lower alkenyl; or R4 and R4 together form a substituted or unsubstituted carbocyclic group. Also provided is a method of inhibiting aggregation of amyloid proteins using a compound of Formula I and a method of imaging amyloid deposits.
机译:“有用的吩恶嗪类似物作为淀粉样蛋白聚集的抑制剂和治疗阿尔茨海默氏病和淀粉样变性病相关的功能障碍”。式I的化合物,其中:R 1为氢,低级烷基或环烷基; R 2是氢,低级烷基,低级烷氧基,卤素,羟基,芳基,杂芳基,芳基烷基,杂芳基烷基,芳氧基二基,杂芳基烷氧基,氰基,羧基,烷氧基羰基,氨基甲酰基,氨磺酰基,硝基,三氟甲基或氨基烷基氨基; R 3和R 4独立地是氢,低级烷氧基,芳基,杂芳基,卤素,羟基,氰基,羧基,烷氧基羰基,氨基甲酰基,氨磺酰基,硝基,三氟甲基,氨基,单或二烷基氨基或低级烷基或未取代或取代的低级烯基; R 4和R 4一起形成取代或未取代的碳环基团。还提供了使用式I的化合物抑制淀粉样蛋白聚集的方法和成像淀粉样沉积物的方法。

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