CAS: 443-48-1; Metronidazole

相似化合物

13182-89-3 1010-93-1 4812-40-2

上下游产品

oxirane 2-methyl-5-nitro-1H-imidazole metronidazole phosphate glycine ester of metronidaxoleH-imidazole2-(4-[1,3]dioxolan-2-yl-styryl)-5-nitro-1-vinyl-1H-imidazole 3,4,5-trimethoxy-benzoic acid 2-(2-methyl-5-nitro-imidazol-1-yl)-ethyl ester 27H18N6O12C27H18N6O12 2-(5-nitro-2-methyl-1-imidazolyl)ethyl methanesulfonate

2-甲基-5-硝基-1H-咪唑-1-乙醇 1-(磷酸二氢酯)置于human Serum体系中,用 水 作为反应溶剂,化学反应生成 甲硝唑
参考文献:磷酸甲硝唑-甲硝唑肠胃外溶液的水溶性前药.
标题:磷酸甲硝唑-甲硝唑肠胃外溶液的水溶性前药.
摘要:为了开发相对水不溶性甲硝唑(2-甲基-5-硝基-1H-咪唑-1-乙醇)的肠胃外溶液,可通过两种途径合成其磷酸酯.一种途径是使用2-氰基乙基磷酸酯,另一种途径是使用焦磷酸四氯化磷.第一种方法使用二环己基碳二亚胺作为偶联剂,并在弱碱性条件下除去氰基乙基.第二种方法是一步法,其中分离出甲硝唑磷酸酯的游离酸为结晶固体.在25度下测定甲硝唑在各种溶剂中的溶解度.根据其水溶性的ph依赖性,甲硝唑共轭酸的pka估计为2.62,与其他硝基咪唑的pka值非常吻合.磷酸甲硝唑在酸性介质中表现为两性离子化合物,在ph 2.0下的溶解度最小.在ph 7时,其溶解度约为甲硝唑的50倍.磷酸酯在高于7的ph值下是如此可溶,以致于难以准确测量其溶解度.在人血清中,甲硝唑磷酸酯的水解在初始浓度为0.25 Mg / Ml或更高时遵循零级动力学,这可能是由于酶饱和(37度下为0.035 Mg / Ml / Hr)引起的.采用
DOI:10.1002/jps.2600710409

专利信息

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-11059835-B2
优先权日:2014-08-15
标 题 :Synthesis of cephalosporin compounds
发明人：WALLER DAVID; GAZDA GREGORY; MINDEN ZACHARY; BARTON LISA; LEIGH CLIFTON
权利人:MERCK SHARP & DOHME
摘要:Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising a palladium-catalyzed coupling reaction.

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-2015198107-A1
优先权日:2014-06-24
标 题:Synthesis of metronidazole
发明人：KIANY FARD TAGHI; KIANIFARD TOKTAM; SARVI IRAJ; KOWSAR KASRA
权利人:KIANY FARD TAGHI
摘要:The producers utilize costly and unique active ingredients to produce metronidazole synthesis which has to be imported from other countries; consequently the cost of its production rises greatly. Furthermore, this drug has side effect in the present methods of production. Overusing usual samples leads to kidney stone in the patient's body. The purpose of this invention is to remove the mentioned defects. Producing metronidazole using the new method does not require utilizing costly and unique active ingredients for the producer and production process can be done with a lower cost. In addition, its production using the new method has fewer side effects rather than the previous methods.