HDAC inhibitors: a 2013-2017 patent survey

Area of Science:

• Medicinal Chemistry
• Pharmacology
• Biochemistry

Background:

• Histone deacetylase (HDAC) inhibitors are a significant class of biologically active compounds.
• Four HDAC inhibitors have received FDA approval, highlighting their therapeutic importance.
• HDAC inhibitors are utilized in various human disease treatments.

Purpose of the Study:

• To review recent advancements in the synthesis and applications of HDAC inhibitors.
• To cover the period from 2013 to 2017.
• To explore emerging trends in HDAC inhibitor development.

Main Methods:

• Literature review of scientific publications and patents.
• Analysis of synthetic methodologies for HDAC inhibitors.
• Evaluation of reported applications and therapeutic targets.

Main Results:

• Current synthetic strategies aim for selectivity towards specific HDAC isoforms, particularly HDAC6.
• Medicinal chemists are focused on developing zinc-binding groups with improved pharmacokinetic profiles and potency.
• Emerging applications include treatments for neurological and metabolic disorders, and immune system stimulation.

Conclusions:

• HDAC inhibitors remain a key area in drug discovery for various diseases.
• The development of isoform-selective inhibitors and dual-target agents is a significant trend.
• The therapeutic potential of HDAC inhibitors extends beyond oncology.