Trace amine associated receptor 1 (TAAR1) modulators: a patent review (2010-present)

References

• Aleksandrov AA, Dmitrieva ES, Volnova AB, et al. Effect of trace amine-associated receptor 1 agonist RO5263397 on sensory gating in mice. NeuroReport. 2019;30:1004–1007.
   Google Scholar
• Schwartz MD, Canales JJ, Zucchi R, et al. Trace amine-associated receptor 1: a multimodal therapeutic target for neuropsychiatric diseases. Expert Opin Ther Targets. 2018;22:513–526.
   PubMed Web of Science ®Google Scholar
• Rutigliano G, Accorroni A, Zucchi R. The case for TAAR1 as a modulator of central nervous system function. Front Pharmacol. 2018;8:987.
   PubMed Web of Science ®Google Scholar
• Scanlan TS, Suchland KL, Hart ME, et al. 3-Iodothyronamine is an endogenous and rapid-acting derivative of thyroid hormone. Nat Med. 2004;10:638–642.
   PubMed Web of Science ®Google Scholar
• Sabelli H, Fink P, Fawcett J, et al. Sustained antidepressant effect of PEA replacement. J Neuropsychiatry Clin Neurosci. 1996;8:168–171.
   PubMed Web of Science ®Google Scholar
• Berry MD. Mammalian central nervous system trace amines. Pharmacologic amphetamines, physiologic neuromodulators. J Neurochem. 2004;90:257–271.
   PubMed Web of Science ®Google Scholar
• Aleksandrov AA, Knyazeva VM, Volnova AB, et al. Trace amine-associated receptor 1 agonist modulates mismatch negativity-like responses in mice. Front Pharmacol. 2019;10:470.
   PubMed Web of Science ®Google Scholar
• Alvarsson A, Zhang X, Stan TL, et al. Modulation by trace amine-associated receptor 1 of experimental parkinsonism, L-DOPA responsivity, and glutamatergic neurotransmission. J Neurosci. 2015;35:14057–14069.
   PubMed Web of Science ®Google Scholar
• Bradaia A, Trube G, Stalder H, et al. The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system. Proc Natl Acad Sci USA. 2009;106:20081–20086.
   PubMed Web of Science ®Google Scholar
• Stalder H, Hoener MC, Norcross RD. Selective antagonists of mouse trace amine-associated receptor 1 (mTAAR1), discovery of EPPTB (RO5212773). Bioorg Med Chem Lett. 2011;21:1227–1231.
   PubMed Web of Science ®Google Scholar
• Lam VM, Mielnik CA, Baimel C, et al. Behavioral effects of a potential novel TAAR1 antagonist. Front Pharmacol. 2018;9:953.
   PubMed Web of Science ®Google Scholar
• Cichero E, Tonelli M. Targeting species-specific TAAR1 ligands: to date perspective of the rational drug design process. Future Med Chem. 2017;9:1507–1527.
   PubMed Web of Science ®Google Scholar
• Cichero E. Opportunities and challenges in the design of selective TAAR1 agonists: an editorial. Expert Opin Ther Pat. 2018;28:437–440.
   PubMed Web of Science ®Google Scholar
• Hart ME, Suchland KL, Miyakawa M, et al. Trace amine-associated receptor agonists: synthesis and evaluation of thyronamines and related analogues. J Med Chem. 2006;49:1101–1112.
   PubMed Web of Science ®Google Scholar
• Tan ES, Miyakawa M, Bunzow JR, et al. Exploring the structure-activity relationship of the ethylamine portion of 3-iodothyronamine for rat and mouse trace amine-associated receptor 1. J Med Chem. 2007;50:2787–2798.
   PubMed Web of Science ®Google Scholar
• Galley G, Stalder H, Goergler A, et al. Optimisation of imidazole compounds as selective TAAR1 agonists: discovery of RO5073012. Bioorg Med Chem Lett. 2012;22:5244–5248.
   PubMed Web of Science ®Google Scholar
• Cichero E, Tonelli M. New insights into the structure of the trace amine-associated receptor 2: homology modelling studies exploring the binding mode of 3-iodothyronamine. Chem Biol Drug Des. 2017;89:790–796.
   PubMed Web of Science ®Google Scholar
• Cichero E, Espinoza S, Tonelli M, et al. A homology modelling-driven study leading to the discovery of the first mouse trace amine-associated receptor 5 (TAAR5) antagonists. Med Chem Commun. 2016;7:353–364.
   Google Scholar
• Cichero E, Espinoza S, Gainetdinov RR, et al. Insights into the structure and pharmacology of the human trace amine-associated receptor 1 (hTAAR1): homology modelling and docking studies. Chem Biol Drug Des. 2013;81:509–516.
   PubMed Web of Science ®Google Scholar
• Tonelli M, Espinoza S, Gainetdinov RR, et al. Novel biguanide-based derivatives scouted as TAAR1 agonists: synthesis, biological evaluation, ADME prediction and molecular docking studies. Eur J Med Chem. 2017;127:781–792.
   PubMed Web of Science ®Google Scholar
• Guariento S, Tonelli M, Espinoza S, et al. Rational design, chemical synthesis and biological evaluation of novel biguanides exploring species-specificity responsiveness of TAAR1 agonists. Eur J Med Chem. 2018;146:171–184.
   PubMed Web of Science ®Google Scholar
• Hoener M, Raab S, Risterucci C, et al. Pharmaceutical combination. US2012/0028964 A1. 2012.
   Google Scholar
• F. Hoffmann-La Roche AG. Combinations comprising atypical antipsychotics and TAAR1 agonists. WO2012/016879 A1. 2012.
   Google Scholar
• Nettekoven M, Norcross R, Polara A Dihydrooxazol-2-amine derivatives. US2012/0108609 A1. 2012.
   Google Scholar
• F. Hoffmann-La Roche AG. Heterocyclic amine derivatives. WO2012/126922 A1. 2012.
   Google Scholar
• F. Hoffmann-La Roche AG. Pyrazole derivatives. WO2012/168260 A1. 2012.
   Google Scholar
• F. Hoffmann-La Roche AG. Substituted benzamide derivatives. WO2012/168265 A1. 2012.
   Google Scholar
• F. Hoffmann-La Roche AG. Substituted benzamide derivatives. WO2011/076678 A1. 2011.
   Google Scholar
• F. Hoffmann-La Roche AG. Process for the preparation of chiral 2-aryl morpholines. WO2015/086495 A1. 2015.
   Google Scholar
• F. Hoffmann-La Roche AG. Heterocyclic derivatives as trace amine associated receptors (TAARS). WO2013/104591 A1. 2013.
   Google Scholar
• F. Hoffmann-La Roche AG. Pyrazole carboxamide derivatives as TAAR modulator for use in the treatment of several disorders, such as depression, diabetes and Parkinson’s disease. WO2014/041007 A1. 2014.
   Google Scholar
• F. Hoffmann-La Roche AG. Triazole carboxamide derivatives. WO2014/041106 A1. 2014.
   Google Scholar
• F. Hoffmann-La Roche AG. Pyrazine derivatives. WO2014/072257 A1. 2014.
   Google Scholar
• F. Hoffmann-La Roche AG. Morpholino-pyridine derivatives. WO2015/165085 A1. 2015.
   Google Scholar
• F. Hoffmann-La Roche AG. Morpholino-pyridine derivatives. WO2015/165835 A1. 2015.
   Google Scholar
• F. Hoffmann-La Roche AG. 2-Oxa-5-azabicyclo[2.2.1]heptan-3-yl derivatives. WO2016/015333 A1. 2016.
   Google Scholar
• F. Hoffmann-La Roche AG. 2-Oxa-5-azabicyclo[2.2.1]heptan-3-yl derivatives. WO2016/016292 A1. 2016.
   Google Scholar
• F. Hoffmann-La Roche AG. 6-Amino-5,6,7,8-tetrahydronaphthalen-2-yl or 3-aminochroman-7-yl derivatives as TAAR modulators. WO2016/016162 A1. 2016.
   Google Scholar
• F. Hoffmann-La Roche AG. Substituted pyrazino[2,1-A]isoquinoline derivatives for the treatment of CNS disorders. WO2016/030306 A1. 2016.
   Google Scholar
• F. Hoffmann-La Roche AG. Substituted azetidine derivatives as TAAR ligands. WO2016/030310 A1. 2016.
   Google Scholar
• Chiellini G, Rapposelli S, Zucchi R Synthetic analogues of 3-iodothyronamine and uses thereof. WO2015/151068 A1. 2015.
   Google Scholar
• Purdue Pharma L.P. Oxazoline pseudodimers, pharmaceutical compositions and the use thereof. WO2017/192858 A1. 2017.
   Google Scholar
• Purdue Pharma L.P. Trace amine associated receptor 1 agonists and partial agonists for pain treatment. WO2017/210616 A1. 2017.
   Google Scholar
• F. Hoffmann-La Roche AG. 5-Ethyl-4-methyl-pyrazole-3-carboxamide derivative having activity as agonist of TAAR. WO2017/157873 A1. 2017.
   Google Scholar
• Leo D, Mus L, Espinoza S, et al. Taar1-mediated modulation of presynaptic dopaminergic neurotransmission: role of D2 dopamine autoreceptors. Neuropharmacology. 2014;81:283–291.
   PubMed Web of Science ®Google Scholar
• Espinoza S, Ghisi V, Emanuele M, et al. Postsynaptic D2 dopamine receptor supersensitivity in the striatum of mice lacking TAAR1. Neuropharmacology. 2015;93:308–313.
   PubMed Web of Science ®Google Scholar
• Espinoza S, Lignani G, Caffino L, et al. TAAR1 modulates cortical glutamate NMDA receptor function. Neuropsychopharmacology. 2015;40:2217–2227.
   PubMed Web of Science ®Google Scholar
• Berry MD, Gainetdinov RR, Hoener MC, et al. Pharmacology of human trace amine-associated receptors: therapeutic opportunities and challenges. Pharmacol Ther. 2017;180:161–180.
   PubMed Web of Science ®Google Scholar
• Dedic N, Jones PG, Hopkins SC, et al. SEP-363856, a novel psychotropic agent with a unique, non-D2 receptor mechanism of action. J Pharmacol Exp Ther. 2019;371:1–14.
   PubMed Web of Science ®Google Scholar