CAS: 32986-56-4; (2S,3R,4S,5S,6R)-4-Amino-2-(((1S,2S,3R,4S,6R)-4,6-Diamino-3-(((2R,3R,5S,6R)-3-Amino-6-(Aminomethyl)-5-Hydroxytetrahydro-2H-Pyran-2-yl)Oxy)-2-Hydroxycyclohexyl)Oxy)-6-(Hydroxymethyl)Tetrahydro-2H-Pyran-3,5-Diol

该化合物是一种有抗生素的稀疏球菌,其抗生素具有很强的杀菌作用,能对抗广泛的克氏阴性病原体和一些克氏阳性病原体,对30S的脊髓膜炎亚体有约束力,抑制蛋白合成,导致细菌细胞死亡.托布米辛对Pseudomonas aeruginosa特别有效,使它成为呼吸道感染(包括细胞纤维纤维化病人)的关键治疗选择.它的稳定性和低抗体发展进一步增强了它的临床用途.在注射,吸入溶液和眼科制剂等配方中,托巴米素广泛用于系统性和局部性感染,其药效特征允许可以预测剂量,尽管建议进行治疗性药物监测,以尽量减少肾毒性和毒性风险.

结构式图片

欧盟法规

ECHA物质ECHA物质C&L通报REACH预注册

上下游产品

CAS号23155-02-4 磷霉素

合成工艺路线路线简述

  • 合成目标产物 Tobramycin 主要起始原料 Fosfomycin
  • (文献来源)合成步骤主要原料 Fosfomycin
磷霉素 反应生成尼拉霉素
参考文献:Inhaled Fosfomycin/tobramycin For The Treatment Of Chronic Obstructive Pulmonary Disease
标题:Inhaled Fosfomycin/tobramycin For The Treatment Of Chronic Obstructive Pulmonary Disease
摘要:本发明提供了在治疗患有慢性阻塞性肺疾病(copd)并正在经历或有患急性加重的风险的患者中使用含有磷霉素和托布拉霉素的气雾剂配方.还提供了用于此类用途的配方和治疗copd患者的方法.

海关参考信息

专利信息


专利号:US-9353057-B2
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
权利人:XENOPORT INC
摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

专利号:US-12146136-B2
优先权日:2020-03-26
标题:Synthesis of modified oligonucleotides with increased stability
发明人:KHVOROVA ANASTASIA; ROUX LOÃ?C MAURICE RENÉ JEAN; YAMADA KEN
权利人:UNIV MASSACHUSETTS
摘要:This disclosure relates to the synthesis of novel modified oligonucleotides. The synthesis of novel phosphoramidites are also provided.

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-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-9982005-B2
优先权日:2013-04-04
标 题 :Macrolides and methods of their preparation and use
发明人:MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG
权利人:HARVARD COLLEGE
摘要:Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided.
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主要参考文献


1: Rosalia M, Chiesa E, Tottoli EM, Dorati R, Genta I, Conti B, Pisani S. Tobramycin Nanoantibiotics and Their Advantages: A Minireview. Int J Mol Sci. 2022 Nov 15;23(22):14080. doi: 10.3390/ijms232214080.
2: Fiel SB, Roesch EA. The use of tobramycin for Pseudomonas aeruginosa: a review. Expert Rev Respir Med. 2022 May;16(5):503-509. doi: 10.1080/17476348.2022.2057951. Epub 2022 Apr 4.
195:106778. doi: 10.1016/j.rmed.2022.106778. Epub 2022 Feb 25.

合成参考文献


摘要:S10 | SWISSPHARMA | Pharmaceutical List with Consumption Data | DOI:10.5281/zenodo.2623484
摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2003).
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