B. Blass
Jan 14, 2016
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Journal
ACS medicinal chemistry letters
Abstract
Title: Cyclopropanamine Compounds and Use Thereof Patent Application Number: WO2015156417Al Publication date: October 15th, 2015 Priority Application: JP2014-082057 Priority date: April 11th, 2014 Inventors: Matsumoto, S.; Hattori, Y.; Toyofuku, M.; Morimoto, S.; Daini, M.; Kojima, T.; Kaku, T.; Ito, M. Assignee Company: Takeda Pharmaceuticals Disease Area: CNS Biological Target: Lysine-specific demethylase-1 Summary: Packaging of DNA into nucleosomes in eukaryotic cells is dependent upon the proper utilization of histones. These highly basic proteins are the primary component of chromatin, act as spool for DNA winding, and are regulated via methylation and demethylation processes. Lysine-specific demethylase 1 (LSD1) is an FAD dependent enzyme that demethylates monoand dimethylated lysines in histone 3. Inhibition of this enzyme causes an increase in histone 3 methylation. Further, changes in methylation content of histone 3 have been linked to alterations in gene expression. LSD1 inhibitors are currently being examined as novel therapeutic agent for the treatment of a number of disease states including schizophrenia, Rett’s syndrome, fragile X syndrome, Alzheimer’s disease, epilepsy, and drug addiction. The present disclosure describes a series of functionalized cyclopropanamine inhibitors of LSD1 and their method use in treating the aforementioned conditions.