该化合物是一种具有抗炎和免疫抑制特性的合成花生类固醇,主要用于治疗哮喘和鼻炎等呼吸条件,其特点是能够减少炎症并缓解与这些条件有关的症状,该物质通常通过吸入或鼻喷施用,允许采取局部行动,同时尽可能少地系统吸收.化学上,该物质是倍氯米松的衍生物,含有两种可增加其脂性与药效的气态酯组.Beclomothaons dipromoate des diopriate 表现出一种高度的亲近性,导致炎反应中基因表达的调节.该物质的致癌性表明行动迅速开始,尽管全面治疗效应可能需要数天才能显现出来.常见的副作用可能包括局部的刺激或糖尿病,但由于其定向投放,其系统效应一般会最小化.
9β,11β-Epoxy-17α,21-Dihydroxy-16β-Methylpregna-1,4-Diene-3,20-Dione 17,21-Dipropionate 反应生成 丙酸倍氯米松 参考文献:Novel 9.Alpha.-Fluoro-Or Chloro-Corticosteroid Esters And A Process For 标题:Novel 9.Alpha.-Fluoro-Or Chloro-Corticosteroid Esters And A Process For 摘要:9.Alpha.-氟和氯皮质类固醇的新酯化合物的公式为##str1##其中y是氯或or.Sub.1,R.Sub.1和r.Sub.2代表2-6个碳原子的酰基或苯甲酰基,其中r.Sub.1和r.Sub.2可以在同一分子中相同或不同,R.Sub.3是甲基或氟在α-或β-取向中,X是氯或氟,C.Sub.1 C.Sub.2键可以饱和或不饱和,特别是公式##str2##中的化合物,其中y和r.Sub.2具有上述给定的意义,通过将相应的9.Beta.,11.Beta.-环氧化合物与氟化氢或氯化氢反应制备而成.
专利号:US-8546532-B2 优先权日:2008-04-17 标题:Synthesis of directed sequence polymer compositions and antibodies thereof for the treatment of protein conformational disorders 发明人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS 权利人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS; DECLION PHARMACEUTICALS INC 摘要:The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the treatment and diagnosis of protein conformational disorders, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use. The invention also pertains to the process of generating antibodies using the directed epitope peptide mixtures as the antigens, and antibodies generated by such process, useful in the treatment and diagnostics of the said protein conformational disorder.
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.
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合成参考文献
参考文献:10.1177/1087057116635503 摘要:Voter AF, Manthei KA, Keck JL. A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. J Biomol Screen. 2016 Jul;21(6):626–33.