CAS: 50293-90-8; 2-(Hydroxymethyl)-4-{(1R)-1-Hydroxy-2-[(2-Methyl-2-Propanyl)Amino ]Ethyl}Phenol Hydrochloride (1:1)

该化合物是一种选择性的乙二亚乙二亚丁基激素,主要用作治疗哮喘和慢性阻塞性肺病(COPD)的支气管.它是舒喘和慢性阻塞性肺病(COPD)的支气管.它是一个舒喘醇的R-enantiomer,这意味着它有一个特定的三维安排,可以提高治疗效果,同时最大限度地减少副作用.该物质看上去是白色的,是白色的,在水中溶解,适合吸入配方.在支气管滑动肌肉中刺激乙二乙二亚丁基乙酰激素受体的行为,导致气道的放松和扩张,从而改善气流并缓解支气管的症状.它的药性肿瘤表明行动迅速开始,通常在几分钟内,效果持续数小时.普通的副作用可能包括激素,紧张性以及心率上升,尽管这些作用通常不如丙基丁醇那么明显.Leevalbuterol在病人身上产生更大的反向效果.

结构式图片

欧盟法规

C&L通报

合成工艺路线路线简述

    📜(R)-2-(Tert-Butylamino)-1-(2,2-Dimethyl-4H-Benzo[d][1,3]Dioxin-6-yl)Ethan-1-Ol置于盐酸体系中,用 水,乙酸乙酯 作为反应溶剂,化学反应 2.0H,以88.8%的收率获得产物盐酸左旋沙丁胺醇
    参考文献:一种盐酸左旋沙丁胺醇的制备方法
    标题:一种盐酸左旋沙丁胺醇的制备方法
    摘要:本发明属于医药化学领域,具体涉及盐酸左旋沙丁胺醇的制备方法.即采用不对称催化还原,只需少量的手性催化剂,即可得到高纯度的手性产物.通过本发明制备方法得到的产品符合美国药典usp43‑nf的质量标准,其纯度可达99.90%以上,最大单杂和异构体均在0.05%以下.

    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.

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Brunetti L, Poiani G, Dhanaliwala F, Poppiti K, Kang H, Suh DC. Clinical outcomes and treatment cost comparison of levalbuterol versus albuterol in hospitalized adults with chronic obstructive pulmonary disease or asthma. Am J Health Syst Pharm. 2015 Jun 15;72(12):1026-35. doi: 10.2146/ajhp140551. doi: 10.1111/jvim.14320. Epub 2016 Jun 9. Review. doi: 10.1345/aph.1S003. Epub 2013 Apr 23. doi: 10.1016/j.pupt.2012.11.003. Epub 2012 Nov 30. Review. doi: 10.1159/000362684. Epub 2014 Jun 20.
    10: Broski SE, Amundson DE. Paradoxical response to levalbuterol. J Am Osteopath Assoc. 2008 Apr;108(4):211-3. Erratum in: J Am Osteopath Assoc.2008 May;108(5): 266. doi: 10.3389/fendo.2014.00236. eCollection 2014.
    12: Pagán Rivera BL, Anselmi FJ, Torres Mdel M, Segarra A, Rivera JR. Usefulness Of Glucocorticoids In The Management Of Foreign Body Aspiration. Bol Asoc Med P R. 2015 Jul-Sep;107(3):24-7. Review. doi: 10.1016/j.jval.2014.08.376. Epub 2014 Oct 26. doi: 10.5863/1551-6776-16.3.191.

    合成参考文献


    参考文献:10.1007/bf02772200
    摘要:Bakale RP, Wald SA, Butler HT, Gao Y, Hong Y, Nie X, Zepp CM. Albuterol. A pharmaceutical chemistry review of R-, S-, and RS-albuterol. Clin Rev Allergy Immunol. 1996;14(1):7–35. doi: 10.1007/bf02772200.
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