CAS: 94749-08-3; 4-(1-Hydroxy-2-((6-(4-Phenylbutoxy)Hexyl)Amino)Ethyl)-2-(Hydroxymethyl)Phenol 1-Hydroxy-2-Naphthoate

该化合物是一种长效乙型-2肾上腺素抗激剂,主要用于治疗哮喘和慢性阻塞性肺病(COPD),其功能是放松支气管滑动肌肉,导致气管结裂,导致气管结裂和改善气流.该化合物的特点是对主要是在肺部发现的乙型-2肾上腺受体进行选择性行动.Salmeterol xinafate 通常通过吸入进行施用,允许有针对性地向呼吸系统交付.其行动持续时间很长,适合进行维护治疗,而不是对支气管帕进行急性减压.该物质往往与皮质科动物结合,以提高治疗效果和控制炎症.在物理特性方面,沙美色素xinafate是白色的,其溶性受到pH和其他配方因素的影响.与任何药物一样,必须考虑潜在的副作用,其中可能包括心血管效应和某些病人的矛盾支气管膜.

结构式图片

欧盟法规

C&L通报

上下游产品

salmeterol 1-hydroxy-2-naphthoic acid 6-bromohexyl 4-phenylbutyl ether 1 ,6-dibromohexane

合成工艺路线路线简述

    5-乙酰水杨酸甲酯置于palladium 10% On Activated Carbon,Potassium Iodide N-溴代丁二酰亚胺(Nbs),Lithium Aluminium Tetrahydride,硫酸,氢气,Potassium Carbonate体系中,用 四氢呋喃,甲醇,N,N-二甲基甲酰胺,丙酮,乙腈 作为反应溶剂,65.0 °C,588.41 Kpa 条件下,反应 10.0H,反应生成 昔美酸沙美特罗
    参考文献: Process For The Preparation Of Salmeterol And Its Intermediates[fr] Procédé Pour La Préparation De Salmétérol Et De Ses Produits Intermédiaires
    标题: Process For The Preparation Of Salmeterol And Its Intermediates[fr] Procédé Pour La Préparation De Salmétérol Et De Ses Produits Intermédiaires

    海关参考信息

    专利信息


    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:US-2025206743-A1
    优先权日:2022-03-25
    标 题:Tyk2 inhibitor synthesis and intermediates thereof
    发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
    权利人:TAKEDA PHARMACEUTICALS CO
    摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

    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-11628186-B2
    优先权日:2017-02-24
    标题 :Method and composition for the reduction of viral replication, duration and spread of the COVID-19 and the flu
    发明人:MARTIN ALAIN
    权利人:MARTIN ALAIN; CELLULAR SCIENCES INC
    摘要:A method for stimulating the synthesis of nasal nitric oxide and nasal and lung surfactants to inhibit the docking and adhesion of viruses to cellular receptors, including ACE2, to reduce viral replication, duration, spread and severity of infections, and also to inhibit lung fibrosis, increase the synthesis of serotonin to reduce coughing and mouth breathing, reduce the cytokine storm produced by LI-6 caused by viruses such as COVID-19 and flu in patients susceptible to these infections, including patients with hypoxemia, asthma, chronic obstructive pulmonary disease, cystic fibrosis, diabetics, interstitial lung disease, pulmonary fibrosis, allergic rhinitis, sinusitis, smokers, sleep apnea and lung cancer, which includes: contacting mammalian cells with a therapeutically effective amount of a composition, said composition including the following constituents: sodium pyruvate; a phosphate; a salt of calcium; and a salt of magnesium.

    专利号:US-9051302-B2
    优先权日:2008-01-15
    标 题 :Synthesis of resorcylic acid lactones useful as therapeutic agents
    发明人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN
    权利人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN; UNIV STRASBOURG
    摘要:Disclosed are macrocyclic compounds of formulae I, I′, II, II′, III, III′, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.

    专利号:WO-2021040673-A1
    优先权日:2019-08-26
    标 题:Methods for the treatment of chronic hypoxemia and inhibiting lung fibrosis in patients with pulmonary fibrosis with and without copd
    发明人:MARTIN ALAIN
    权利人:MARTIN ALAIN
    摘要:The present invention involves methods for the treatment of chronic hypoxemia, COPD and lung fibrosis in patients with both COPD and pulmonary fibrosis, and in patients with idiopathic pulmonary fibrosis without COPD, by stimulating the synthesis of human and animal patient lung and sinus surfactants to increase lung functions, prevent hypoxemia while reducing the sinus and lung infections, reducing some drug side effects, inhibiting fibrosis and reducing coughing and nasal erythema. These methods include the following steps: A) analyzing and diagnosing a patient with a lung ailment elected 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 therapeutically effective amount of each constituent of the composition.
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    主要参考文献


    1: Farias G, Ganley WJ, Price R, Conti DS, Mangal S, Bielski E, Newman B, Shur J. Microstructural Characterization of Dry Powder Inhaler Formulations Using Orthogonal Analytical Techniques. Pharm Res. 2024 Oct;41(10):2015-2029. doi: 10.1007/s11095-024-03776-1. Epub 2024 Oct 7.
    2: Yin Y, Ruan G, Su Q, Li L, Hong Y. Effect of Small Doses of Azithromycin on Pulmonary Ventilation Function and Inflammatory Factors IL-6, IL-13 in Children with Bronchial Asthma. Ann Clin Lab Sci. 2024 Jul;54(4):452-456. 51(5):426-432. doi: 10.1016/j.vaa.2024.05.009. Epub 2024 May 29. 21(9):4191-4198. doi: 10.1021/acs.molpharmaceut.4c00479. Epub 2024 Aug 12. 14(1):9845. doi: 10.1038/s41598-024-59588-1.
    6: Li S, Feng K, Lee J, Gong Y, Wu F, Newman B, Yoon M, Fang L, Zhao L, Gobburu JVS. Pharmacokinetic Models for Inhaled Fluticasone Propionate and Salmeterol Xinafoate to Quantify Batch-to-Batch Variability. AAPS J. 2024 Apr 26;26(3):56. doi: 10.1208/s12248-024-00913-x.

    合成参考文献


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    参考文献:10.1016/j.cct.2011.06.004
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    参考文献:10.1016/j.rmed.2011.06.005
    摘要:Price D, Gray A, Gale R, Asukai Y, Mungapen L, Lloyd A, Peters L, Neidhardt K, Gantner T. Cost-utility analysis of indacaterol in Germany: a once-daily maintenance bronchodilator for patients with COPD. Respir Med. 2011 Nov;105(11):1635–47. doi: 10.1016/j.rmed.2011.06.005.
    参考文献:10.1164/rccm.200509-1519oc
    摘要:Wechsler ME, Lehman E, Lazarus SC, Lemanske RF, Boushey HA, Deykin A, Fahy JV, Sorkness CA, Chinchilli VM, Craig TJ, DiMango E, Kraft M, Leone F, Martin RJ, Peters SP, Szefler SJ, Liu W, Israel E; National Heart, Lung, and Blood Institute's Asthma Clinical Research Network. beta-Adrenergic receptor polymorphisms and response to salmeterol. Am J Respir Crit Care Med. 2006 Mar 01;173(5):519–26.
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