4,4'-pentanediyldioxy-bis-benzimidic acid diethyl esterisethionic acid ammonium salt
合成工艺路线路线简述
📜4,4'-Pentanediyldioxy-Bis-Benzimidic Acid Diethyl Ester,羟乙基磺酸铵盐 以 乙醇,水 用作溶剂,化学反应 24.0H,以83%的收率获得喷他脒羟乙磺酸盐 参考文献:Nandi,Gopa; Mukherjee,S.; Basu,M. K.,Journal Of The Indian Chemical Society,1993,Vol. 70,# 6,P. 527-532 标题:Nandi,Gopa; Mukherjee,S.; Basu,M. K.,Journal Of The Indian Chemical Society,1993,Vol. 70,# 6,P. 527-532
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-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: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.
专利号:WO-2012149093-A1 优先权日:2011-04-26 标 题 :2-guanidino-4-oxo-imidazoline derivatives as antimalarial agents, synthesis and methods of use thereof 发明人:LIN AI J; LIU XIANJUN; KOZAR MICHAEL P; O'NEIL MICHAEL T 权利人:US OF AMERICA AS REPRESENTED BY THE SECRETARY OF ARMY; LIN AI J; LIU XIANJUN; KOZAR MICHAEL P; O'NEIL MICHAEL T 摘要:The present invention relates to new 2-guanidino-4-oxo-imidazoline derivatives (deoxo-IZ), methods of making these compounds, compositions containing the same, and methods of using the same to prevent, treat, or inhibit malaria in a subject.
专利号:US-9056887-B2 优先权日:2011-07-26 标 题 :Minor groove binder phosphoramidites and methods of use 发明人:VOROBIEV ALEXEI; LUKHTANOV EUGENY A 权利人:VOROBIEV ALEXEI; LUKHTANOV EUGENY A; ELITECH HOLDING BV 摘要:Minor groove binder phosphoramidites having the formula M-L-PA, wherein M is a minor groove binder comprising a protected heteroaromatic amine, L is a linker, and PA is a phosphoramidite group, have been synthesized. Preferred methods of synthesis include synthesizing a minor groove binder intermediate containing a transiently protected hydroxyl group, protecting heteroaromatic amines of the corresponding minor groove binder intermediate as carbamate intermediates, reacting the carbamate intermediate to remove the transient protecting group to yield carbamate-protected minor groove binder agent as an intermediate with a free hydroxyl group, and converting the intermediate with a free hydroxyl group to the desired minor groove binder phosphoramidite. These minor groove binder phosphoramidites are useful in the preparation of oligonucleotide conjugates, particularly those for use as probes and primers. In preferred methods, an oligonucleotide sequence is synthesized using nucleoside phosphoramidites and the minor groove binder phosphoramidite is incorporated into the oligonucleotide sequence to form a protected oligonucleotide-minor groove binder conjugate. Then, deprotection produces the oligonucleotide-minor groove binder.
1: Mans DR, Kent AD, Hu RV, Lai A Fat EJ, Schoone GJ, Adams ER, Rood EJ, Alba S, Sabajo LO, Lai A Fat RF, de Vries HJ, Schallig HD. Monitoring the response of patients with cutaneous leishmaniasis to treatment with pentamidine isethionate by quantitative real-time PCR, and identification of Leishmania parasites not responding to therapy. Clin Exp Dermatol. 2015 Dec 9. doi: 10.1111/ced.12786. [Epub ahead of print] doi: 10.1371/journal.pntd.0003592. eCollection 2015 Mar. 3: Orgel E, Rushing T. Efficacy and tolerability of intravenous pentamidine isethionate for Pneumocystis jiroveci prophylaxis in a pediatric oncology population. Pediatr Infect Dis J. 2014 Mar;33(3):319-21. doi: 10.1097/INF.0000000000000044. doi: 10.1002/jps.23055. Epub 2012 Jan 23. Epub 2007 Nov 19. French. Epub 2003 Mar 28. French. French.
合成参考文献
摘要:Annals of Internal Medicine., 105(146), 1986 摘要:Cancer, 34(441), 1974 [] 摘要:S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (2021) DOI:10.1021/acsenvironau.1c00008. List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355