Patent highlights: August – September 2019

In this article, brought to BioTechniques users by Pharmaceutical Patent Analyst, Herman Mucke (HM Pharma Consultancy, Vienna, Austria) provides a snapshot of noteworthy recent developments in the patent literature.

Hermann Mucke discusses the latest instalment of his ongoing patent highlights series, published in Pharmaceutical Patent Analyst.

What uncommon or new drug targets have you seen addressed in patent documents published during the August/September 2019 period?

Firstly, GCN2, an IF2α kinase that is activated by amino acid deficiency, has been addressed in Merck GmbH’s (Darmstadt, Germany) WO/2019/148132 and WO/2019/148136. The development of ancillary antitumor agents is the intent, but the implications extend to cellular homeostasis in general.

Then there is GPR68, a proton-sensing orphan receptor that responds to extracellular acidity, which Novartis’ (Basel, Switzerland) inventors have now determined to also be an mechanotransducing flow sensor in the arteriolar endothelium (WO/2019/150309).

Additionally, WO/2019/169112 describes OLIG2, a basic helix-loop-helix transcription factor highly expressed in all diffuse gliomas but absent from normal brain and non-malignant tissues outside the CNS (Curtana Pharmaceuticals, TX, USA).

What notable patent documents addressed rare or neglected diseases?

In WO/2019/162945, Hanoch Kaphzan from the University of Haifa (Haifa, Israel), shows that an Na/K-ATPase inhibitor, marinobufagenin (an endogenous cardiotonic steroid), is beneficial in the cognitive symptoms of Angelman syndrome – a genetic disorder which primarily affects the nervous system. This is unusual because such inhibitors are associated with cognitive dysfunction in other conditions.

What interesting patent documents were published that are not (yet) reflected in the peer review literature?

Artax Biopharma (MA, USA) shed a light on TCR-Nck interaction-inhibiting chromene derivatives – which are claimed in WO/2019/169001.  Additionally, WO/2019/174277 shows that the antiseptic effect of cetylbromide and domiphen is due to binding to a hydrophobic pocket of a phosphoethanolamine transferase.

Which patent documents could trigger drug development with minimal delay, or reflect development that is already ongoing?

Grünenthals’s (Aachen, Germany) lipoxin A4 receptor (FPR2) inhibitors from WO/2019/170904, which might be clinical candidates for COPD and asthma.

From the journal; Patent highlights: August – September 2019

WO/2019/144842 – Thiazole-5-formic acid derivative, preparation method therefor and use thereof

Inventors: Hammack S, Laffitte B, Patapoutian A, Xu J

Assignee: The inventors, represented by Novartis AG (Basel, Switzerland)

Published: 8 August 2019

WO/2019/152680 – Methods and compositions for treating cancer using Chrna6 inhibitors

Inventors: Kahvejian A, Mata-Fink J, Hurov JB, Shu CJ, Fankhauser MA, Stanley JA

Assignee: Flagship Pioneering Innovations V, Inc. (MA, USA)

Published: 8 August 2019

WO/2019/157495 – Methods for preventing and/or treating bone loss conditions by modulating irisin

Inventors: Spiegelman BM, Kim H, Rosen C, Bonewald L

Assignee: Dana Faber Cancer Institute, Inc. (MA, USA); Indiana University (IN, USA); Maine Medical Center Research Institute (ME, USA)

Published: 15 August 2019

WO/2019/160840 –Paraspeckle component 1 (Pspc1) promoting epithelial-mesenchymal transition, stemness and metastasis as an anticancer agent

Inventors: Jou Y-S, Lang Y-D, Yeh H-W

Assignee: Academia Sinica (Taipei City, Taiwan)

Published: 22 August 2019

WO/2019/162945 – Methods for treating memory impairment and cognitive dysfunction

Inventor: Kaphzan H

Assignee: Carmel Haifa University Economic Corporation Ltd. (Haifa, Israel)

Published: 29 August 2019

WO/2019/165284 – Methods of treating nonalcoholic steatohepatitis and compositions therefore

Inventor: Barnea ER

Assignee: BioIncept LLC (NY, USA)

Published: 29 August 2019

WO/2019/169001 – Chromene derivatives as inhibitors of TCR-Nck interaction

Inventors: Castro J, Gegete Mateos A, Machin PL, Vandeusen CL

Assignee: Artax Biopharma, Inc. (MA, USA)

Published: 6 September 2019

WO/2019/169112 – Inhibition of Olig2 activity

Inventors: Beaton G, Mchardy SF, Lopez A Jr, Campos B, Wang H-YL

Assignee: Curtana Pharmaceuticals, Inc. (TX, USA)

Published: 6 September 2019

WO/2019/170904 – Piperidines or piperidones substituted with urea and phenyl

Inventors: Jakob F, Merla B, Rider D, Dunkern T, Wagener M

Assignee: Grünenthal GmbH (Aachen, Germany)

Published: 12 September 2019

WO/2019/174277 – Phosphoethanolamine transferase inhibitors

Inventors: Chen S, Chan K-F

Assignee: The Hong Kong Polytechnic University (Hong Kong, China)

Published: 19 September 2019

WO/2019/182191 – Pharmaceutical composition for prevention or treatment of neurodegenerative disease and comprising Cox2-acetylating agent as active ingredient

Inventors: Bae J-S, Jin HK, Lee JY

Assignee: Kyungpook National University Industry-Academic Cooperation (Daegu, South Korea)

Published: 26 September 2019

WO/2019/182947 – Arylnaphtalene compounds as vacuolar ATPase Inhibitors and the use thereof

Inventors: Davisson VJ, Lindstrom AR

Assignee: Purdue Research Foundation (IN, USA)

Published: 26 September 2019