Phenoxazine analogs useful as amyloid aggregation inhibitors and treatment of alzheimer's disease and disorders related to amyloidosis
申请人:——
公开号:US20020143012A1
公开(公告)日:2002-10-03
Disclosed are compounds of the Formula I
1
wherein:
R
1
is hydrogen, lower alkyl, or cycloalkyl;
R
2
is hydrogen, lower alkyl, lower alkoxy, halogen, hydroxy, aryl, heteroaryl, arylalkyl, heteroarylalkyl, arylalkoxy, heteroarylalkoxy, cyano, carboxy, alkoxycarbonyl, carbamoyl, sulfamoyl, nitro, trifluoromethyl, amino, or mono- or dialkylamino; and
R
3
and R
4
independently are hydrogen, lower alkoxy, aryl, heteroaryl, halogen, hydroxy, cyano, carboxy, alkoxycarbonyl, carbamoyl, sulfamoyl, nitro, trifluoromethyl, amino, mono- or dialkylamino, or unsubstituted or substituted lower alkyl or lower alkenyl; or
R
3
and R
4
together form an unsubstituted or substituted carbocyclic group.
Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound of Formula I and a method of imaging amyloid deposits.
披露了公式I1的化合物,其中:R1是氢,低烷基或环烷基;R2是氢,低烷基,低烷氧基,卤素,羟基,芳基,杂芳基,芳烷基,杂芳烷基,芳烷氧基,杂芳烷氧基,氰基,羧基,烷氧基羰基,氨基甲酰基,磺酰氨基,硝基,三氟甲基,氨基,或单或二烷基氨基;和R3和R4独立是氢,低烷氧基,芳基,杂芳基,卤素,羟基,氰基,羧基,烷氧基羰基,氨基甲酰基,磺酰氨基,硝基,三氟甲基,氨基,单或二烷基氨基,或未取代或取代的低烷基或低烯基;或R3和R4共同形成一个未取代或取代的碳环基团。还提供了一种使用公式I的化合物抑制淀粉样蛋白聚集的方法和一种成像淀粉样沉积物的方法。