Certain substituted 1-aryl-3-morpholinopropanones to treat Alzheimer's Disease

Disclosed are compounds of formula I: 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...

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Hauptverfasser: DEBERNARDIS, JOHN FRANCIS, KERKMAN, DANIEL JOSEPH
Format: Patent
Sprache:eng
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Zusammenfassung:Disclosed are compounds of formula I: 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. Disclosed are compounds of formula I: 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.