CAS: 59-87-0; 2-((5-Nitrofuran-2-yl)Methylene)Hydrazinecarboxamide

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CAS号698-63-5 5-硝基糠醛 | CAS号563-41-7 盐酸氨基脲 | CAS号92-55-7 5-硝基糠醛二乙酸酯 | CAS号624-46-4 methyl ethyl ke... | CAS号1574-10-3 苯甲醛缩氨基脲 | CAS号110-20-3 丙酮缩氨脲

Hydroxymethylnitrofurazone 以 Aq. Acetate Buffer 作为反应溶剂,化学反应 48.0H,反应生成 呋喃西林
参考文献:Pharmacokinetics Of Hydroxymethylnitrofurazone,A Promising New Prodrug For Chagas' Disease Treatment
标题:Pharmacokinetics Of Hydroxymethylnitrofurazone,A Promising New Prodrug For Chagas' Disease Treatment
摘要:摘要 羟甲基硝基呋喃酮(nfoh)是硝基呋喃酮(nf)的杀胰原药,无诱变毒性.这项工作的目的是研究 Nfoh 在醋酸钠缓冲液(ph 值为 1.2 和 7.4)和人体血浆中转化为 Nf 的化学过程,并确定大鼠的临床前药代动力学参数.在 Ph 值为 1.2 的条件下,48 小时后 Nfoh 完全转化为母药 Nf,而在 Ph 值为 7.4 的条件下,48 小时后的水解率为 20%.在人体血浆中,24 小时后 50%的 Nfoh 被水解. 与 曲线来计算单剂量给药后的药代动力学参数.nfoh 在血清中达到最大药物浓度的时间(t T 最大值)为 1 小时,表明吸收速度快于 Nf(4 小时).观测到的最重要结果是分布容积 (V Nfoh 在组织中的分布容积(v)比 Nf(17.64 升/千克体重)高出 20 倍(337.5 升/千克体重). 体内 Nfoh的体内代谢所产生的nf浓度大约低四倍(血清中的最大药物浓度[C C Max] = 0.83 μg/kg =0.83微克/毫升;0至12小时的浓度-时间曲线下面积[auc 0-12] = 5.683 μg/ml-H). C 最大值 = 2.78 μg/ml; Auc 0-12 = 54.49 μg/ml-H).这些发现可以解释原药 Nfoh 与母药相比具有更高的活性和更低的毒性,并证实 Nfoh 是一种很有前途的抗南美锥虫病候选药物.
DOI:10.1128/aac.02522-12

专利信息

专利号:US-2009299067-A1
优先权日:2008-05-30
标 题:New synthesis of 2,6-diamino-3,5-dinitropyrazine-1-oxide from 2,6-diaminopyrazine-1-oxide
发明人：PAGORIA PHILIP F; MITCHELL ALEXANDER R; BALA KASON
权利人:PAGORIA PHILIP F; MITCHELL ALEXANDER R; BALA KASON
摘要:A method for the synthesis of 2,6-Diamino-3,5-dinitropyrazine-1-oxide including nitration of 2,6-diaminopyrazine-1-oxide. The step of nitration may use nitrating agents 20% Oleum/100% HNO3, 100% HNO3 and conc. H2504/100% HNO3 or nitronium tetrfluoraoborate. The synthesis of 2,6-diaminopyrazine-1-oxide may involve both the oxidation of 2,6-diaminopyrazine, the amination of a precursor 2,6-disubstitutedpyrazine-1-oxide or direct formation of the 2,6-diaminopyrazine-l-oxide from the precursor, 2-amino-6-hydroxamino-pyrazine-1-oxide.

专利号:US-9284306-B2
优先权日:2012-05-11
标题 :(R)-Nifuratel, its use for the treatment of infections and synthesis of (R) and (S)-Nifuratel
发明人：GAGLIARDI STEFANIA; CONSONNI ALESSANDRA; MAILLAND FEDERICO; BULGHERONI ANNA
权利人:POLICHEM SA
摘要:(R)-Nifuratel is disclosed together with its use as bactericide and bacteriostatic agent as well as the pharmaceutical compositions containing the same; (R)-nifuratel has been surprisingly found to possess a better antimicrobial profile than either nifuratel racemate or (S)-nifuratel. A new procedure for the synthesis of both (R)-Nifuratel and (S)-Nifuratel is also disclosed.

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:US-2008280855-A1
优先权日:2005-06-22
标 题 :Process For the Production of Intermediates For the Preparation of Tricyclic Benzimidazoles
发明人：CHIESA MARIA VITTORIA; PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; SIMON WOLFGANG-ALEXANDER; POSTIUS STEFAN; KROMER WOLFGANG; ZANOTTI-GEROSA ANTONIO
权利人:NYCOMED GMBH
摘要:The invention relates to a process for the synthesis of compounds of the formula 1-a and compounds of the formula 1-b. n n n n n n n n n n The compounds of the formula 1-a and the compounds of the formula 1-b, in which the substituents R1, R2, R3, and Ar have the meanings indicated in the description, are valuable intermediates for the preparation of pharmaceutically active compounds.