📜21-氯-9-Beta,11-Beta-环氧-17-羟基-16-Alpha-甲基孕甾-1,4-二烯-3,20-二酮置于盐酸体系中,用 溶剂黄146 用作溶剂,化学反应 3.0H,以83%的收率获得莫美他松 参考文献:Unusual Hydroxy--Sultone Byproducts Of Steroid 21-Methanesulfonylation. An Efficient Synthesis Of Mometasone 17-Furoate (Sch 32088) 标题:Unusual Hydroxy--Sultone Byproducts Of Steroid 21-Methanesulfonylation. An Efficient Synthesis Of Mometasone 17-Furoate (Sch 32088) 摘要:An Efficient Two Stage Synthesis Of The Steroid Anti-Inflammatory Agent Mometasone 17-Furoate (Sch 32088) 4 From 17 Alpha,21-Dihydroxy-16 Alpha-Methyl-9 Beta,11 Beta-Oxidopregna-1,4-Diene-3,20-Dione 6 Is Described And The Structures Of Unusual Delta-Hydroxy-Gamma-Sultone Byproducts Of 4-Dimethylaminopyridine Catalyzed Methanesulfonylation Of 21-Hydroxy-20-Ketosteroids Are Deduced. (C) 1999 Elsevier Science Ltd. All Rights Reserved. Doi:10.1016/s0040-4020(98)01146-6
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-2024082118-A1 优先权日:2021-05-19 标 题:Topical compositions and methods of preparing the same 发明人:ABRAMOVICH SAGI; AVIDOR GAL; LANDA BENZION 权利人:LANDA LABS 2012 LTD 摘要:There is disclosed a composition comprising a water-insoluble thermoplastic compound capable of stimulating collagen synthesis (CSSC), the CSSC having a molecular weight of more than 0.6 kDa and being dispersed in a polar carrier as nano-elements having an average diameter of 200 nm or less and a viscosity of 107 mPa·s or less. The nano-elements of CSSC can be capable of stimulating the synthesis of skin proteins and/or enabling the delivery of active agents upon their application to a surface to be treated therewith. Methods for preparing the compositions and uses thereof are also provided.
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-8802660-B2 优先权日:2007-03-12 标 题:De novo synthesis of glucocorticoids in the epidermis and its uses and applications 发明人:TOMIC-CANIC MARJANA; BREM HAROLD; SAMUELS HERBERT H 权利人:TOMIC-CANIC MARJANA; BREM HAROLD; SAMUELS HERBERT H; UNIV NEW YORK 摘要:The present invention relates to methods and compositions that control, i.e., antagonize/inhibit or agonize/stimulate, de novo glucocorticoid production in the skin. Such methods and compositions can be used for the prevention and/or treatment of a variety of skin conditions, including inflammation, acute wounds, chronic non-healing wounds, keloid, fibrotic or hypertrophic scars, and epithelial-derived cancer.
1. Cam, B., Sari, M., Midi, A., et al. Xylitol treats nasal mucosa in rhinitis medicamentosa: An experimental rat model study. Eur. Arch. Otorhinolaryngol. 6(11), 3123-3130 (2019). 2. Kim, D.H., Kim, B.-Y., Shin, J.-H., et al. Intranasal azelastine and mometasone exhibit a synergistic effect on a murine model of allergic rhinitis. Am. J. Otolaryngol. 38(2), 198-203 (2017). 3. Chen, J., Mo, Y., Schlueter, C.F., et al. Inhibition of chlorine-induced pulmonary inflammation and edema by mometasone and budesonide. Toxicol. Appl. Pharmacol. 272(2), 408-413 (2013).
合成参考文献
参考文献:10.1331/japha.2011.10044 摘要:Sega T, Sullivan DL. Assessment of pharmacists' opinions toward the behind-the-counter category of medications. Journal of the American Pharmacists Association. 2011 Jul;51(4):535–8. doi: 10.1331/japha.2011.10044. 参考文献:10.1155/2011/485402 摘要:Kim SH, Kim BK, Lee YC. Antiasthmatic effects of hesperidin, a potential Th2 cytokine antagonist, in a mouse model of allergic asthma. Mediators Inflamm. 2011;2011():485402.