CAS: 139110-80-8; (2R,3R,4S)-3-Acetamido-4-Guanidino-2-((1R,2R)-1,2,3-Trihydroxypropyl)-3,4-Dihydro-2H-Pyran-6-Carboxylic Acid

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CAS号4023-02-3 1H-吡唑-1-甲脒盐酸盐 | CAS号139110-70-6 扎那米韦 | CAS号130525-58-5 5-乙酰氨基-7,8,9-O-... | CAS号1184-90-3 氨基(亚氨基)甲磺酸 | CAS号130525-62-1 扎那米韦中间体2 | CAS号78850-37-0 methyl (3aR,4R,... | CAS号66356-40-9 N-Acetyl-S-meth...

N-Acetyl Neuraminic Acid置于三氟甲磺酸三甲基硅酯,Sodium Carbonate,Sodium Amide,Sodium Hydroxide体系中,用 四氢呋喃,甲醇,水,乙酸乙酯 用作溶剂,化学反应 46.0H,反应生成扎那米韦
参考文献:扎那米韦中间体的制备方法和扎那米韦的制 备方法
标题:扎那米韦中间体的制备方法和扎那米韦的制 备方法
摘要:本发明涉及一种扎那米韦中间体乙酰化保护的氨基化合物的制备方法和扎那米韦的制备方法.本发明扎那米韦的制备方法是以唾液酸为原料,经过基团保护,环化生成环合物,用金属氨基物处理环合物一步得到乙酰化保护的氨基化合物,再脱去羟基保护剂乙酸酯,和脒基吡唑反应上呱基,得到扎那米韦.其中,用金属氨基物处理环合物一步得到乙酰化保护的氨基化合物是扎那米韦制备中的重大实质性突破,大幅缩短了合成步骤,简化了工艺操作.本发明用廉价的金属氨基物替代昂贵的三甲基叠氮硅开环,不仅降低了成本,也确保了生产工艺的安全性.本发明扎那米韦的制备方法总质量收率可达50%以上,比现有技术有大幅提高.

专利信息

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: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.

专利号:US-10813893-B2
优先权日:2017-02-24
标 题:Compositions and methods for the treatment and prevention of chronic hypoxemia and dyspnea
发明人：MARTIN ALAIN
权利人:MARTIN ALAIN; CELLULAR SCIENCES INC
摘要:The present invention has shown that not all salts of pyruvic acid enhance lung functions or enhance the synthesis of lung surfactants and that certain salts of pyruvic acid with the correct concentrations of calcium, phosphate and magnesium, are synergistic in their ability to enhance the synthesis of lung surfactants that will enhance lung alveoli functions, while decreasing coughing and lung tightness, and increasing oxygen saturation values to prevent hypoxemia. This patent demonstrates that the sodium pyruvate formula with calcium, phosphate and magnesium was superior over standard sodium pyruvate formula in saline alone in the removal of mucus, reduction of lung or sinus infections, and in reducing drug side effects and congestion. The use of this formula clearly demonstrated that it can be used to produce better efficacy in patients with hypoxemia, with lung and sinus diseases including, asthma, COPD, cystic fibrosis, interstitial lung disease, allergic rhinitis, sinusitis, Alzheimer's, disease, Parkinson's disease, brain trauma, nicotine addiction, sleep apnea, autism, migraine headaches, sleep disorders, lung and sinus infections, cancer therapy with cancer drugs, nicotine addiction, and medications that cause a decrease in lung surfactants.

专利号:US-2014073804-A1
优先权日:2011-02-24
标 题 :Process for the preparation of zanamivir
发明人：CHARAN GANPAT DAN SHIMBHU; TEHARE AJAY ONKARSINGH; SINGH KUMAR KEMLESH LAXMI
权利人:CHARAN GANPAT DAN SHIMBHU; TEHARE AJAY ONKARSINGH; SINGH KUMAR KEMLESH LAXMI
摘要:The present invention provides a process for preparing 5-(acetylamino)-4-[(aminoiminomethyl)amino]-2,6-anhydro-3,4,5-trideoxy-D-glycero-D-galacto-non-enonic acid Formula (I), which process comprises reducing compound of Formula (IV) by Lindlar catalyst in presence of hydrogen to obtain compound of Formula (V). reacting compound of Formula (V) with pyrazole-1H-carboxamidine or its suitable salt to obtain compound of Formula (VIII). hydrolyzing the compound of Formula (VIII) to give compound of Formula (I). The present invention also provides compounds of formula (VIII) which may be used in the synthesis of zanamivir. The present invention also provides process for preparing compound of formula (VIII) and process involving the use of Formula (VIII), including in the synthesis of zanamivir.