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Pharm Pat Anal. 2019 Jan;8(1):15-39. doi: 10.4155/ppa-2019-0003. Epub 2019 Mar 14.

Development of tau-directed small molecule modulators for Alzheimer's disease: a recent patent review (2014-2018).

Lee HE1,2, Lim D1,3, Lee JY3, Lim SM1,2, Pae AN1,2,3.

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Convergence Research Center for Diagnosis, Treatment & Care System of Dementia, Korea Institute of Science & Technology, Seoul 02792, Republic of Korea.
Division of Bio-Medical Science & Technology, KIST School, Korea University of Science & Technology, Seoul 02792, Republic of Korea.
KHU-KIST Department of Converging Science & Technology, Kyung Hee University, Seoul 02447, Republic of Korea.


Alzheimer's disease (AD) is a progressive neurodegenerative disease that is characterized by memory loss and cognitive impairment. As this disease is becoming a serious global health issue, development of disease modifying therapeutics is urgently required. AD is characterized by deposits of two protein, amyloid β and tau. Although amyloid β-based therapeutics have been extensively investigated so far, tau has also received great attention as one of promising molecular targets for AD. In this review, a variety of tau-directed strategies to rescue tau-mediated neurotoxicity will be reviewed especially focusing on small molecules. Subsequently, recent patents published from 2014 to 2018 that integrate efforts to develop tau-directed small molecules for the treatment of AD will be reviewed.


Alzheimer’s disease; aggregation; patent; post-translational modification; tau

[Indexed for MEDLINE]

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