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Title

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

Authors
Bertrand, Philippe
Published in Expert Opinion on Therapeutic Patents. 2017, vol. 27, no. 3, p. 229-236
Abstract 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.
Keywords Antineoplastic Agents/pharmacologyDrug DesignHistone Deacetylase Inhibitors/pharmacologyHistone Deacetylases/drug effectsHumansHydroxamic Acids/pharmacologyNeoplasms/drug therapy/pathologyPatents as Topic
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PMID: 28092474
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SIMOES AVELLO, Claudia, BERTRAND, Philippe, CUENDET LICEA, 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. https://archive-ouverte.unige.ch/unige:94969

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Deposited on : 2017-06-20

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