PHARMACEUTICAL COMPOUNDS AND USE OF SAME IN CANCER AND TAUOPATHIES

摘要

Disclosed are compounds of formula (1)-(V): where the substituents are as provided herein. Further disclosed are methods of inhibiting tau aggregation, treating or ameliorating a tauopathy or cancer by administration of such a compound. Tau is a microtubule-binding protein that accumulates in a number of neurodegenerative disorders, including frontotemporal dementia and Alzheimer's disease (AD). The presence of abnormal tau correlates with neuron loss and memory deficits in patients with AD and other neurodegenerative disorders that involve tau accumulation.

主权项

1. A compound having a structure of formula (I):whereinR1, R2, and R3 are each selected from the group consisting of hydrogen, fluoro, chloro, methoxy, methyl, or trifluoromethyl,R4 and R5 are each selected from hydrogen, fluoro, and chloro,R6 is C1-C4 alkyl or CH2Ar;Ar is aryl;R7 is ethyl, allyl, or benzyl;X is a pharmaceutically acceptable anion, and m is 1, 2, or 3;with the proviso that
(1) if R6 is alkyl, R7 is ethyl, and each of R4 and R5 is hydrogen, then at least one of R1, R2, and R3 is other than hydrogen; and (2) when each of R1, R2, R3, R4, and R5 is hydrogen, R6 is CH2Ar.