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Use of substituted aryl-morpholinos, thiomorpholinos or piperazino-propanones for the prophylactic treatment of Alzheimer's disease

机译:取代的芳基吗啉代,硫代吗啉代或哌嗪子基丙烷在预防阿尔茨海默氏病中的用途

摘要

Disclosed are compounds of formula I: IMAGE I wherein X is selected from oxygen, sulfur and NR; wherein R is selected from hydrogen, loweralkyl and CH2CH2COAr1; and Z is hydrogen; straight or branched chain alkyl having 1-6 carbon atoms; or Z and R1, R2 or R3 together represent CH2; CH2CH2; CH20; or CH2S forming a five or six membered ring and such ring may be optionally substituted with loweralkyl or phenyl; R24 is hydrogen; loweralkyl, or optionally substituted phenyl; each R10 is selected from hydrogen and loweralkyl; and Ar1 represents an aryl group or optionally substituted phenyl, thienyl or optionally substituted thienyl; or the pharmaceutically acceptable salts thereof, useful for preventing or decreaseing the production of abnormally phosphorylated paired helical filament (PHF) epitopes associated with Alzheimer's Disease and, therefore, useful for treating Alzheimer's Disease.
机译:公开了式I的化合物:式I,其中X选自氧,硫和NR;其中R选自氢,低级烷基和CH 2 CH 2 COAr 1; Z为氢;具有1-6个碳原子的直链或支链烷基; Z和R1,R2或R3一起表示CH2; CH2CH2; CH20;或形成5或6元环的CH 2 S,且该环可任选地被低级烷基或苯基取代; R24是氢;低级烷基或任选取代的苯基;每个R 10选自氢和低级烷基; Ar 1表示芳基或任选取代的苯基,噻吩基或任选取代的噻吩基;或其药学上可接受的盐,可用于预防或减少与阿尔茨海默氏病有关的异常磷酸化的成对螺旋丝(PHF)表位的产生,因此可用于治疗阿尔茨海默氏病。

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