专利号:WO-2023233371-A1 优先权日:2022-06-03 标 题:A continuous flow process for synthesis of organic azides 发明人:GNANAPRAKASAM BOOPATHY; PANDEY AKANKSHA M; MONDAL SHANKHAJIT 权利人:INDIAN INSTITUTE OF SCIENCE EDUCATION AND RES PUNE IISER PUNE 摘要:The present disclosure relates generally to the field of synthetic organic chemistry. More specifically, the disclosure is directed to a continuous flow process for synthesis of azides from alcohols and peroxides, wherein the process comprises azidation with trimethylsilyl azide and a catalyst Amberlyst-15. It is a non-hazardous, mild and controlled reaction giving good yields of azides. The azides can be further employed for synthesis of medicinally and industrially useful chemicals.
专利号:US-2024024497-A1 优先权日:2020-08-06 标 题:Methods for the synthesis of protein-drug conjugates 发明人:BORCHARDT ALLEN; HUGHES ROBERT MICHAEL 权利人:CIDARA THERAPEUTICS INC 摘要:The present invention relates to methods for the synthesis of conjugates useful for the treatment of viral infections, e.g., conjugates containing inhibitors of viral neuraminidase (e.g., zanamivir or an analog thereof) linked to an Fc domain monomer.
专利号:US-7888337-B2 优先权日:2007-08-31 标 题 :Synthesis of oseltamivir containing phosphonate congeners with anti-influenza activity 发明人:WONG CHI-HUEY; FANG JIM-MIN; SHIE JIUN-JIE; CHENG YIH-SHYUN EDMOND; JAN JIA-TSRONG 权利人:ACADEMIA SINICA 摘要:Novel phosphonate compounds are described. The compounds have activity as neuraminidase inhibitors against wild-type and H274Y mutant of H1N1 and H5N1 viruses. The present disclosure also provides an enantioselective synthetic route to known neuraminidase inhibitors oseltamivir and the anti-flu drug Tamiflu®, as well as novel phosphonate compounds, via D-xylose. Another efficient and flexible synthesis of Tamiflu and the highly potent neuraminidase inhibitor Tamiphosphor was also achieved in 11 steps and >20% overall yields from the readily available fermentation product (1S-cis)-3-bromo-3,5 -cyclohexadiene-1,2-diol. Most of the reaction intermediates were obtained as crystals without tedious purification procedures. The key transformations include an initial regio- and stereoselective bromoamidation of a bromoarene cis-dihydrodiol, as well as the final palladium-catalyzed carbonylation and phosphonylation.
专利号:WO-2025101716-A1 优先权日:2023-11-07 标题:Processes for synthesis of trifunctionalized sulfur(vi) compounds 发明人:LOPCHUK JUSTIN; SHULTZ ZACHARY; ATHAWALE PARESH 权利人:H LEE MOFFITT CANCER CT & RES 摘要:This disclosure describes processes for the asymmetric synthesis of trifunctionalized sulfur(VI) containing organic compounds of Formula I and Formula VI, as well as compounds of Formula I and Formula VI prepared by the processes described.
专利号:US-11311505-B2 优先权日:2017-02-24 标 题:Synergistic compositions to stimulate the synthesis of human lung and sinus surfactants to decrease coughing, increase FEV-1/FVC ratios, decrease lung fibrosis, by increasing apoptosis of myofibroblasts 发明人:MARTIN ALAIN 权利人:MARTIN ALAIN; CELLULAR SCIENCES INC 摘要:Methods for the treatment of patients with both Chronic Obstructive Pulmonary Disease (COPD) and pulmonary fibrosis, and of patients with idiopathic pulmonary fibrosis without COPD, by stimulating the synthesis of human and animal patient lung and sinus surfactants to increase lung functions, inhibiting fibrosis and reducing coughing and nasal erythema, include the following steps: A) analyzing and diagnosing a patient with a lung ailment selected from the group consisting of i) both COPD and pulmonary fibrosis; and ii) idiopathic pulmonary fibrosis without COPD; and, B) treating the patient to raise the patient's lung functions including FEV1/FVC ratio by contacting mammalian cells with a [therapeutically effective amount of a treatment] composition that includes: a) a pyruvate salt; b) a phosphate; c) a salt of calcium; and d) a salt of magnesium, in an aqueous carrier, containing no more than 2.2 grams of said pyruvate salt per liter.
专利号:WO-2011097717-A1 优先权日:2010-02-15 标 题 :Synthesis of bicyclic compounds and method for their use as therapeutic agents 发明人:WULFF JEREMY EARLE; BRANT MICHAEL GLENN; BROMBA CALEB MATTHEW; BOULANGER MARTIN JOHN 权利人:UNIV VICTORIA INNOVAT DEV; WULFF JEREMY EARLE; BRANT MICHAEL GLENN; BROMBA CALEB MATTHEW; BOULANGER MARTIN JOHN 摘要:Disclosed embodiments concern the synthesis and use of therapeutic compounds that for treating emerging flu strains and minimizing resistance to such strains. Methods for making the disclosed compounds concern using a base-mediated addition/cyclization sequence followed by functional group manipulation to develop functionalized compounds that can target neuraminidase, which makes them ideal candidates for treating influenza. Pharmaceutical compositions comprising the therapeutic compounds and biologically-acceptable materials are also described. Methods of inhibiting neuraminidase in subjects that are suspected of containing neuraminidase are also described. The use of metabolites of the disclosed compounds can also be used in diagnostic assays for therapeutic dosing of the disclosed compounds.
1: Esposito S, Principi N. Oseltamivir for influenza infection in children: risks and benefits. Expert Rev Respir Med. 2016;10(1):79-87. doi: 10.1586/17476348.2016.1126182. Epub 2015 Dec 19. Review. doi: 10.1002/cpt.179. Epub 2015 Jul 22. Review. doi: 10.1016/S0140-6736(14)62449-1. Epub 2015 Jan 30. Review. Erratum in: Lancet. 2015 May 2;385(9979):1728. Lancet. 2015 May 2;385(9979):1728. doi: 10.1542/peds.2014-2578. Review. doi: 10.2146/ajhp140390. Review. Epub 2015 Jan 19. Review. doi: 10.1053/j.semperi.2014.08.015. Epub 2014 Oct 1. Review. doi: 10.1002/pds.3673. Epub 2014 Jul 4. Review. [Epub ahead of print] Review. doi: 10.1136/bmj.g2545. Review. 11: Freemantle N, Shallcross LJ, Kyte D, Rader T, Calvert MJ. Oseltamivir: the real world data. BMJ. 2014 Apr 9;348:g2371. doi: 10.1136/bmj.g2371. Review. Review. Review. Review. doi: 10.1093/fampra/cms059. Epub 2012 Sep 20. Review. Review. Review. Review. Review. Review.
合成参考文献
摘要:Mori, Y.; Kobayashi, S., Science of Synthesis: Water in Organic Synthesis, (2012) 1, 837. 摘要:Bertau, M.; Jeromin, G. E., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 182. 摘要:Du, H., Science of Synthesis: Metal-Catalyzed Cyclization Reactions, (2016) 2, 257.