CAS: 564-25-0; Doxycycline

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methacycline hydr°Chloride doxycycline hydr°Chloride doxycycline (1S,2R)-1,2-dihydroxycyclohexa-3,5-diene-1-carboxylic acid4-epidoxycycline (4S,4aR,5S,5aR,6R,12aS)-9-Amino-4-dimethylamino-3,5,10,12,12a-pentahydroxy-6-methyl-1,11-dioxo-8-phenyl-1,4,4a,5,5a,6,11,12a-°Ctahydro-naphthacene-2-carboxylic acid amide (4S,4aR,5S,5aR,6R,12aS)-9-Amino-4-dimethylamino-3,5,10,12,12a-pentahydroxy-6-methyl-8-(4-nitro-phenyl)-1,11-dioxo-1,4,4a,5,5a,6,11,12a-°Ctahydro-naphthacene-2-carboxylic acid amide doxycycline hydr°Chloride

Doxycycline Hydrochloride置于sodium Hydroxide体系中,用 水 作为反应溶剂,化学反应生成 强力霉素
参考文献:Solid State Chemistry Of The Antibiotic Doxycycline: Structure Of The Neutral Monohydrate And Insights Into Its Poor Water Solubility
标题:Solid State Chemistry Of The Antibiotic Doxycycline: Structure Of The Neutral Monohydrate And Insights Into Its Poor Water Solubility
摘要:活性药物成分多西环素(dox)是一种广谱抗生素,主要用于治疗呼吸道和泌尿道感染,与许多药物一样,其药效可能会受到晶体形态的影响.迄今为止,只有关于强力霉素(dox-Hyc)(doryx®,Periostat®,Atridox® 和 Vibramycin® 等品牌的通用名)晶体结构的报道.本研究介绍了另一种晶体形式--一水强力霉素(dox-H2O)(monodox® 和 Oracea® 等品牌的通用名称)的单晶 X 射线衍射结构表征.我们将 Dox-H2O 结构与已知的 Dox-Hyc 结构在分子内和分子间几何形状方面进行了比较,并测量了它们的熔化温度,水溶性和溶解速率.通过这些数据,我们首次建立了与这两种 Dox 晶体变体的制药性能有关的固态特性与其超分子结构之间的关系.环酸盐和一水合物都以齐聚物形式结晶 Dox 分子,其中二甲基胺基团质子化,羟基之一去质子化.在 Dox-Hyc 中观测到两种构象(即在其中一种构象(t1)中,胺基位于烯醇旁边,而在另一种构象(t2)中,胺基位于羰基旁边),而在 Dox-H2O 中只发现一种构象(t2).此外,在环酸盐形式中,晶格中乙醇的存在可能与围绕酰胺基团的 C-C 键旋转有关,在该固态相中存在的两种构象之一(t1)中,氧被引向胺基团.与此同时,在另一个晶体学上独立的分子(t2)中,酰胺氮与胺位于同一侧.然而,在 Dox-H2O 中只观测到与 Dox-Hyc 中 T1 相似的构象.dox-H2O 的晶体结构由多个分子间氢键稳定,每个药物实体与另外两个 Dox 分子和三个水分子相互作用,从而形成了一个紧密的超分子网络.这种结构在氢键方面处于饱和状态,这可能与其溶解度和溶解速率低于 Dox-Hyc 有关.
DOI:10.1039/c1Ce06181J

专利信息

专利号:WO-2012047907-A9
优先权日:2010-10-04
标题 :Synthesis of c5-substituted tetracyclines, uses thereof, and intermediates thereto
发明人：MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN
权利人:HARVARD COLLEGE; MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN
摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for a wide variety of substituents at position 5 of the tetracycline ring system.

专利号:US-9884830-B2
优先权日:2004-05-21
标题 :Synthesis of tetracyclines and analogues thereof
发明人：MYERS ANDREW G; CHAREST MARK G; LERNER CHRISTIAN D; BRUBAKER JASON D; SIEGEL DIONICIO R
权利人:HARVARD COLLEGE
摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.

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-2024197774-A1
优先权日:2021-04-16
标 题:Synthesis of Antimicrobial PVP-coated Bismuth Nanoparticles
发明人：LOPEZ-RIBOT JOSE; VAZQUEZ-MUNOZ ROBERTO
权利人:UNIV TEXAS
摘要:Described herein is a facile, fast, and economical method for the synthesis of BAL-mediated PVP-BiNPs, using basic laboratory instruments and reagents readily available in most laboratories.

专利号:US-8486921-B2
优先权日:2006-04-07
标 题:Synthesis of tetracyclines and analogues thereof
发明人：MYERS ANDREW G; BRUBAKER JASON D; SUN CUIXIANG; WANG QIU
权利人:MYERS ANDREW G; BRUBAKER JASON D; SUN CUIXIANG; WANG QIU; HARVARD COLLEGE
摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetra-cycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-pro liferative agents in the treatment of diseases of humans or other animals.

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.