5-HT4R modulators: a patent landscape

梅德林 神经药理学 医学 图书馆学 受体 药理学 生物信息学 神经科学 万维网 化学 生物 内科学 计算机科学 生物化学
作者
Patrick Dallemagne,Christophe Rochais
出处
期刊:Pharmaceutical patent analyst [Future Science Ltd]
卷期号:10 (4): 179-181 被引量:2
标识
DOI:10.4155/ppa-2021-0017
摘要

Pharmaceutical Patent AnalystVol. 10, No. 4 Editorial5-HT4R modulators: a patent landscapePatrick Dallemagne & Christophe RochaisPatrick Dallemagne https://orcid.org/0000-0002-4845-615XNormandie University, UNICAEN, CERMN, Caen, 14000, FranceSearch for more papers by this author & Christophe Rochais *Author for correspondence: Tel.: +33 231 566 813; E-mail Address: christophe.rochais@unicaen.frhttps://orcid.org/0000-0001-7996-2082Normandie University, UNICAEN, CERMN, Caen, 14000, FranceSearch for more papers by this authorPublished Online:9 Aug 2021https://doi.org/10.4155/ppa-2021-0017AboutSectionsView ArticleView Full TextPDF/EPUB ToolsAdd to favoritesDownload CitationsTrack CitationsPermissionsReprints ShareShare onFacebookTwitterLinkedInReddit View articleKeywords: 5-HT4Rdepressiongastrointestinal diseasesneurodegenerative diseasesstressPapers of special note have been highlighted as: • of interestReferences1. Dumuis A, Bouhelal R, Sebben M, Cory R, Bockaert J. A nonclassical 5-hydroxytryptamine receptor positively coupled with adenylate cyclase in the central nervous system. Mol. Pharmacol. 34(6), 880–887 (1988).Medline, CAS, Google Scholar2. Bockaert J, Claeysen S, Compan V, Dumuis A. 5-HT4 receptors: history, molecular pharmacology and brain functions. Neuropharmacology 55(6), 922–931 (2008).Crossref, Medline, CAS, Google Scholar3. Lanthier C, Dallemagne P, Lecoutey C, Claeysen S, Rochais C. Therapeutic modulators of the serotonin 5-HT 4 receptor: a patent review (2014-present). Expert Opin. Ther. Pat. 30(7), 495–508 (2020). • Recent review describes the most recent patent in the field.Crossref, Medline, CAS, Google Scholar4. Liu M, Geddis MS, Wen Y, Setlik W, Gershon MD. Expression and function of 5-HT 4 receptors in the mouse enteric nervous system. Am. J. Physiol. Liver Physiol. 289(6), G1148–G1163 (2005).Medline, CAS, Google Scholar5. Barnes NM, Ahern GP, Becamel C et al. International union of basic and clinical pharmacology classification of receptors for 5-hydroxytryptamine; pharmacology and function. Pharmacol. Rev. 73(1), 310–520 (2021).Crossref, Medline, CAS, Google Scholar6. Pascual-Brazo J, Castro E, Díaz Á et al. Modulation of neuroplasticity pathways and antidepressant-like behavioural responses following the short-term (3 and 7 days) administration of the 5-HT4 receptor agonist RS67333. Int. J. Neuropsychopharmacol. 15(05), 631–643 (2012).Crossref, Medline, CAS, Google Scholar7. Murphy SE, de Cates AN, Gillespie AL et al. Translating the promise of 5HT 4 receptor agonists for the treatment of depression. Psychol. Med. 51(7), 1111–1120 (2021).Crossref, Medline, Google Scholar8. Giannoni P, Gaven F, de Bundel D et al. Early administration of RS 67333, a specific 5-HT4 receptor agonist, prevents amyloidogenesis and behavioral deficits in the 5XFAD mouse model of Alzheimer's disease. Front. Aging Neurosci. 5, 96 (2013).Crossref, Medline, CAS, Google Scholar9. De Vadder F, Grasset E, Mannerås Holm L et al. Gut microbiota regulates maturation of the adult enteric nervous system via enteric serotonin networks. Proc. Natl Acad. Sci. USA 115(25), 6458–6463 (2018).Crossref, Medline, Google Scholar10. Denny Christine A, Gardier Alain M, David Denis J et al. WO/2020/210393 (2020). • First patent describes the use of 5-HT4R ligand against stress.Google Scholar11. In brief: tegaserod (Zelnorm) returns. Med. Lett. Drugs Ther. 61(1571), 72 (2019).Medline, Google Scholar12. Conlon K, De Maeyer JH, Bruce C et al. Nonclinical cardiovascular studies of prucalopride, a highly selective 5-hydroxytryptamine 4 receptor agonist. J. Pharmacol. Exp. Ther. 364(2), 156–169 (2018).Crossref, Medline, CAS, Google Scholar13. Fukudo S, Nakamura M, Hamatani T, Kazumori K, Miwa H. Efficacy and safety of 5-HT4 receptor agonist minesapride for irritable bowel syndrome with constipation in a randomized controlled trial. Clin. Gastroenterol. Hepatol. 19(3), 538–546.e8 (2021).Crossref, Medline, CAS, Google Scholar14. Lalut J, Karila D, Dallemagne P, Rochais C. Modulating 5-HT 4 and 5-HT 6 receptors in Alzheimer's disease treatment. Future Med. Chem. 9(8), 781–795 (2017).Link, CAS, Google Scholar15. Nirogi R, Mohammed AR, Shinde AK et al. Discovery and preclinical characterization of Usmarapride (SUVN-D4010): a potent, selective 5-HT 4 receptor partial agonist for the treatment of cognitive deficits associated with Alzheimer's disease. J. Med. Chem. https://doi.org/10.1021/acs.jmedchem.1c00703 (2021) (Epub ahead of print). • First description of Usmarapride structure and in vivo characterization.Crossref, Medline, Google Scholar16. Nirogi R, Mohammed AR, Yarlagadda S et al. US90798942 (2015).Google Scholar17. Nirogi R, Bhyrapuneni G, Muddana NR et al. First-in-human studies to evaluate the safety, tolerability, and pharmacokinetics of a novel 5-HT4 partial agonist, SUVN-D4010, in healthy adult and elderly subjects. Clin. Drug Investig. 41(5), 469–482 (2021).Crossref, Medline, CAS, Google Scholar18. Dallemagne P, Rochais C, Claeysen S. EP-36283151 (2020).Google Scholar19. Thompson S. WO2021030571 (2021).Google Scholar20. Rochais C, Lecoutey C, Hamidouche K et al. Donecopride, a Swiss army knife with potential against Alzheimer's disease. Br. J. Pharmacol. 177(9), 1988–2005 (2020).Crossref, Medline, CAS, Google ScholarFiguresReferencesRelatedDetailsCited ByHow nano-engineered delivery systems can help marketed and repurposed drugs in Alzheimer’s disease treatment?Drug Discovery Today, Vol. 27, No. 6Active Targeted Nanoemulsions for Repurposing of Tegaserod in Alzheimer’s Disease Treatment6 October 2021 | Pharmaceutics, Vol. 13, No. 10 Vol. 10, No. 4 Follow us on social media for the latest updates Metrics Downloaded 26 times History Received 22 July 2021 Accepted 23 July 2021 Published online 9 August 2021 Published in print July 2021 Information© 2021 Newlands PressKeywords5-HT4Rdepressiongastrointestinal diseasesneurodegenerative diseasesstressAcknowledgmentsThe authors gratefully acknowledge the Conseil Régional de Normandie, as well as the European Community (FEDER).Financial & competing interests disclosureThe authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.No writing assistance was utilized in the production of this manuscript.PDF download

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