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Review

A patent review of transient receptor potential vanilloid type 1 modulators (2014–present)

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Pages 169-187 | Received 19 Aug 2020, Accepted 18 Nov 2020, Published online: 30 Dec 2020

References

  • Aghazadeh Tabrizi M, Baraldi PG, Baraldi S, et al. Medicinal chemistry, pharmacology, and clinical implications of TRPV1 receptor antagonists. Med Res Rev. 2017;37:936–983.
  • Julius D. TRP channels and pain. Annu Rev Cell Dev Biol. 2013;29:355–384.
  • Moran MM, Szallasi A. Targeting nociceptive transient receptor potential channels to treat chronic pain: current state of the field. Br J Pharmacol. 2018;175:2185–2203.
  • Escelsior A, Sterlini B, Belvederi Murri M, et al. Transient receptor potential vanilloid 1 antagonism in neuroinflammation, neuroprotection and epigenetic regulation: potential therapeutic implications for severe psychiatric disorders treatment. Psychiatr Genet. 2020;30:39–48.
  • Caterina MJ, Schumacher MA, Tominaga M, et al. The capsaicin receptor: a heat-activated ion channel in the pain pathway. Nature. 1997;389:816–824.
  • Westaway SM. The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain. J Med Chem. 2007;50:2589–2596.
  • Brito R, Sheth S, Mukherjea D, et al. TRPV1: a potential drug target for treating various diseases. Cells. 2014;3:517–545.
  • Pappagallo M, Haldey EJ. Pharmacological management of postherpetic neuralgia. CNS Drugs. 2003;17:771–780.
  • Jensen PG, Larson JR. Management of painful diabetic neuropathy. Drugs Aging. 2001;18:737–749.
  • Szallasi A, Sheta M. Targeting TRPV1 for pain relief: limits, losers and laurels. Expert Opin Inv Drug. 2012;21:1351–1369.
  • Szallasi A, Cortright DN, Blum CA, et al. The vanilloid receptor TRPV1: 10 years from channel cloning to antagonist proof-of-concept. Nat Rev Drug Discov. 2007;6:357–372.
  • Holzer P. TRPV1 and the gut: from a tasty receptor for a painful vanilloid to a key player in hyperalgesia. Eur J Pharmacol. 2004;500:231–241.
  • Ji RR, Samad TA, Jin SX, et al. p38 MAPK activation by NGF in primary sensory neurons after inflammation increases TRPV1 levels and maintains heat hyperalgesia. Neuron. 2002;36:57–68.
  • Keeble J, Russell F, Curtis B, et al. Involvement of transient receptor potential vanilloid 1 in the vascular and hyperalgesic components of joint inflammation. Arthritis Rheum. 2005;52:3248–3256.
  • Wong GY, Gavva NR. Therapeutic potential of vanilloid receptor TRPV1 agonists and antagonists as analgesics: recent advances and setbacks. Brain Res Rev. 2009;60:267–277.
  • Walpole CS, Bevan S, Bovermann G, et al. The discovery of capsazepine, the first competitive antagonist of the sensory neuron excitants capsaicin and resiniferatoxin. J Med Chem. 1994;37:1942–1954.
  • Bevan S, Hothi S, Hughes G, et al. Capsazepine: A competitive antagonist of the sensory neurone excitant capsaicin. Br J Pharmacol. 1992;107:544–552.
  • Tominaga M, Caterina MJ, Malmberg AB, et al. The cloned capsaicin receptor integrates multiple pain-producing stimuli. Neuron. 1998;21:531–543.
  • Garami A, Shimansky YP, Rumbus Z, et al. Hyperthermia induced by transient receptor potential vanilloid-1 (TRPV1) antagonists in human clinical trials: insights from mathematical modeling and meta-analysis. Pharmacol Ther. 2020;208:107474.
  • Eid SR. Therapeutic targeting of TRP channels - the TR (i) P to pain relief. Curr Top Med Chem. 2011;11:2118–2130.
  • Serafini M, Griglio A, Aprile S, et al. Targeting Transient Receptor Potential Vanilloid 1 (TRPV1) channel softly: the discovery of passerini adducts as a topical treatment for inflammatory skin disorders. J Med Chem. 2018;61:4436–4455.
  • Antalgenics SL. TRPV1 modulator compounds. WO2018206742. 2018.
  • Axichem AB. Synthetic capsaicin analogs as TRPV1 agonists. WO2017160156. 2017.
  • Aprile S, Serafini M, Pirali T. Soft drugs for dermatological applications: recent trends. Drug Discov Today. 2019;24:2234–2246.
  • Universita’ Degli Studi Di Siena, Universita’ Della Calabria. Biaryl amide or urea derivatives as TRPV1 ligands. WO2015162216. 2015.
  • Institute of Medical Biotechnology. Chinese academy of medical sciences. Aryl-substituted amide compound, preparing method thereof, medicine composition comprising same, and application thereof. CN105198786. 2015.
  • Yissum Research Development Company of Hebrew University of Jerusalem Ltd. Spirofuranone compounds, derivatives thereof and processes for their preparation. WO2016120879. 2016.
  • Grüenenthal GmbH. Aromatic aza compounds as VR1/TRPV1 ligands. EP3130590. 2017.
  • Grüenenthal GmbH. Heterocyclic aza compounds. EP3130589. 2017.
  • University of Pittsburgh. hTRPV1 chemical agents. WO2016127085. 2016.
  • Universidad De Concepcion. TRPV-1 receptor antagonist compound derived from 1,3,4-thiadiazole alkylamides and chalcones. US20160039778. 2016.
  • Ramot At Tel-Aviv University Ltd. Modulators of potassium ion and TRPVl channels and uses thereof. WO2019073471. 2019.
  • China Pharmaceutical University. Phenylquinoline class TRPV1 antagonist and its preparation method and application. CN107721919. 2017.
  • Henan University. 1,2,3,4-tetrahydro-9H-pyrido [3,4-b] indoles TRPV1 antagonist and its application. CN109761974. 2019.
  • Li J, Nie C, Qiao Y, et al. Design, synthesis and biological evaluation of novel 2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole triazole derivatives as potent TRPV1 antagonists. Eur J Med Chem. 2019;178:433–445.
  • Hainan Pharmaceutical Research Institute. Compound, preparation method and its usage. CN105906564. 2016.
  • Univ Chongqing Medical. TRPV1 antagonists and its production and usage. CN107522668. 2017.
  • Chongqing Medleader Biology Medicine Co., Ltd. Antagonist of transient receptor potential vanillic acid hypotype 1 and its production and usage. CN107522669. 2017.
  • Fuzhou Melalyn Biology Tech Co., Ltd. A kind of compound and preparation method thereof red and swollen for skin-whitening and alleviation. CN109021039. 2018.
  • University of Utah Reasearch Foundation. Antagonists of TRPV1 receptor. US20140121168. 2014.
  • Relieving pain in America: A blueprint for transforming prevention, care, education, and research. Mil Med. 2016;181:397–399.
  • Korlipara VL. Transient receptor potential vanilloid 1 channel modulation: a novel approach to pain therapy. Curr Bioact Compds. 2008;4:110–125.
  • Lee Y, Hong S, Cui M, et al. Transient receptor potential vanilloid type 1 antagonists: a patent review (2011–2014). Expert Opin Ther Pat. 2015;25:291–318.
  • Trevisani M, Gatti R. TRPV1 antagonists as analgesic agents. Open Pain J. 2013;6:108–118.
  • Arsenault P, Chiche D, Brown W, et al. NEO6860, modality-selective TRPV1 antagonist: a randomized, controlled, proof-of-concept trial in patients with osteoarthritis knee pain. Pain Rep. 2018;3:e696.
  • Argoff C. Mechanisms of pain transmission and pharmacologic management. Curr Med Res Opin. 2011;27:2019–2031.
  • Turnaturi R, Arico G, Ronsisvalle G, et al. Multitarget opioid/non-opioid ligands: a potential approach in pain management. Curr Med Chem. 2016;23:4506–4528.
  • Piscitelli F, Di Marzo V. “Redundancy” of endocannabinoid inactivation: new challenges and opportunities for pain control. Acs Chem Neurosci. 2012;3:356–363.
  • Ahn K, Johnson DS, Cravatt BF. Fatty acid amide hydrolase as a potential therapeutic target for the treatment of pain and CNS disorders. Expert Opin Drug Discov. 2009;4:763–784.
  • Lee H, Ahn S, Ann J, et al. Discovery of dual-acting opioid ligand and TRPV1 antagonists as novel therapeutic agents for pain. Eur J Med Chem. 2019;182:111634.

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