Scientific article

Novel histone deacetylase 6 (HDAC6) selective inhibitors: a patent evaluation (WO2014181137)

Published inExpert opinion on therapeutic patents, vol. 27, no. 3, p. 229-236
Publication date2017

Histone deacetylases (HDACs) are known to deacetylate histones and other proteins, which makes HDAC inhibitors able to affect cell survival, cell signaling, transport, and gene expression. Those effects have been associated to the therapeutic success of HDAC inhibitors. Class I-selective or pan-HDAC inhibitors have been approved for cancer therapy by the US Food and Drug Administration (FDA). Moreover, HDAC6 selective inhibitors entered phase I and II clinical trials for treating multiple myeloma. The development of potent and selective HDAC inhibitors is a hot topic in current drug discovery. Areas covered: The invention described in this patent (WO2014181137) is related to hydroxamic acid derivatives with inhibitory activity towards HDACs, their synthetic process and pharmaceutical formulations, as well as a method for treating patients suffering from a list of selected tumoral, inflammatory, cardiac and chronic disorders. Expert opinion: The compounds disclosed within this patent are selective against HDAC6 and their structure is related to tubastatin A, a known HDAC6 selective inhibitor. They are newly synthesized diarylamines showing an improved selectivity profile compared to other diarylamines under clinical investigation.

  • Antineoplastic Agents/pharmacology
  • Drug Design
  • Histone Deacetylase Inhibitors/pharmacology
  • Histone Deacetylases/drug effects
  • Humans
  • Hydroxamic Acids/pharmacology
  • Neoplasms/drug therapy/pathology
  • Patents as Topic
Citation (ISO format)
SIMOES AVELLO, Claudia, BERTRAND, Philippe, CUENDET, Muriel. Novel histone deacetylase 6 (HDAC6) selective inhibitors: a patent evaluation (WO2014181137). In: Expert opinion on therapeutic patents, 2017, vol. 27, n° 3, p. 229–236. doi: 10.1080/13543776.2017.1282945
Main files (1)
Article (Published version)
ISSN of the journal1354-3776

Technical informations

Creation06/14/2017 9:45:00 AM
First validation06/14/2017 9:45:00 AM
Update time03/15/2023 1:47:26 AM
Status update03/15/2023 1:47:25 AM
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