专利号:US-8759572-B2 优先权日:2009-12-18 标 题:Process for the preparation of thyroid hormones and salts thereof 发明人:VISCARDI CARLO FELICE; CAPPELLETTI ENRICO; GALIMBERTI LAURA; GAZZETTO SONIA; SINI LOREDANA 权利人:VISCARDI CARLO FELICE; CAPPELLETTI ENRICO; GALIMBERTI LAURA; GAZZETTO SONIA; SINI LOREDANA; BRACCO IMAGING SPA 摘要:The present invention generally refers to a process for the preparation of L-thyroxine derivatives. More in particular, the present invention relates to a iodination reaction of an aromatic derivative with an appropriate iodinating agent, so to afford the related iodinated compound as disodium salt, which may represent a useful intermediate for the synthesis of the L-thyroxine mono-sodium salt, and the free form thereof.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
1: Senese R, Cioffi F, de Lange P, Leanza C, Iannucci LF, Silvestri E, Moreno M, Lombardi A, Goglia F, Lanni A. Both 3,5-Diiodo-L-Thyronine and 3,5,3'-Triiodo-L-Thyronine Prevent Short-term Hepatic Lipid Accumulation via Distinct Mechanisms in Rats Being Fed a High-Fat Diet. Front Physiol. 2017 Sep 14;8:706. doi: 10.3389/fphys.2017.00706. eCollection 2017. 2: Fallahi P, Ferrari SM, Santini E, Camastra S, Frenzilli G, Puccini M, Goglia F, Lanni A, Marchetti P, Antonelli A. Both 3,5-diiodo-L-thyronine (T2) and T3 modulate glucose-induced insulin secretion. J Biol Regul Homeost Agents. 2017 Apr-Jun;31(2):503-508. doi: 10.1016/j.mce.2017.02.012. Epub 2017 Feb 10. eCollection 2016. 5: Cavallo A, Taurino F, Damiano F, Siculella L, Sardanelli AM, Gnoni A. Acute administration of 3,5-diiodo-L-thyronine to hypothyroid rats stimulates bioenergetic parameters in liver mitochondria. J Bioenerg Biomembr. 2016 Oct;48(5):521-529. Epub 2016 Nov 17. Review. doi: 10.1371/journal.pone.0140837. eCollection 2015.
合成参考文献
摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198 参考文献:10.1210/en.143.5.1660|10.1210/endo.143.5.8767 摘要:Incerpi S, De Vito P, Luly P, Spagnuolo S, Leoni S. Short-term effects of thyroid hormones and 3,5-diiodothyronine on membrane transport systems in chick embryo hepatocytes. Endocrinology. 2002 May;143(5):1660–8. doi: 10.1210/endo.143.5.8767. 参考文献:10.1210/en.143.5.1789|10.1210/endo.143.5.8770 摘要:Pinna G, Brödel O, Visser T, Jeitner A, Grau H, Eravci M, Meinhold H, Baumgartner A. Concentrations of seven iodothyronine metabolites in brain regions and the liver of the adult rat. Endocrinology. 2002 May;143(5):1789–800. doi: 10.1210/endo.143.5.8770. 参考文献:10.3181/0710-rm-266 摘要:Grasselli E, Canesi L, Voci A, De Matteis R, Demori I, Fugassa E, Vergani L. Effects of 3,5-diiodo-L-thyronine administration on the liver of high fat diet-fed rats. Exp Biol Med (Maywood). 2008 May;233(5):549–57. doi: 10.3181/0710-rm-266. 参考文献:10.1007/s12020-019-01990-1 摘要:Morris JC, Galton VA. The isolation of thyroxine (T4), the discovery of 3,5,3'-triiodothyronine (T3), and the identification of the deiodinases that generate T3 from T4: An historical review. Endocrine. 2019 Oct;66(1):3–9. doi: 10.1007/s12020-019-01990-1.