CAS: 372151-71-8; Telavancin

该化合物是一种来自vancomycin的脂质氯丙烯酸抗生素,它展示了抗克菌病原体(包括抗甲虫菌)的有力细菌杀菌活动,包括抗甲状腺素抗体血清球菌(MRSA),其双重行动机制是,通过与Peptidogycan前体D-alanil-D-alanine终点系结合,抑制细胞壁合成,以及破坏细菌膜的完整.Telavancin表现出依赖浓度的杀戮和长期抗生素后效应,提高了其在皮肤和皮肤结构复杂感染(cSSSI)和医院肺炎(HAP)等严重感染中的效力.它曾经使用甲状腺素和可靠的组织渗透进一步支持其临床功能.Telavancancan用于那些由于其目标频谱和潜在肾毒性风险而不适合替代疗法的病例.

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    N3-Decylaminoethylvancomycin

    合成工艺路线路线简述

      📜聚合甲醛,氨甲基膦酸,N3-Decylaminoethylvancomycin置于n,N-二异丙基乙胺体系中,用 水,乙腈 用作溶剂,化学反应 1.0H,以57%的收率获得特拉万星
      参考文献:Development And Preclinical Evaluation Of New Inhaled Lipoglycopeptides For The Treatment Of Persistent Pulmonary Methicillin-Resistant Staphylococcus Aureus Infections
      标题:Development And Preclinical Evaluation Of New Inhaled Lipoglycopeptides For The Treatment Of Persistent Pulmonary Methicillin-Resistant Staphylococcus Aureus Infections
      摘要:耐甲氧西林慢性肺病 金黄色葡萄球菌 (囊性纤维化(cf)中的慢性肺部耐甲氧西林金黄色葡萄球菌(mrsa)疾病在接受标准抗生素治疗后复发的可能性很高,这是一个与预期寿命缩短相关的未满足需求领域.我们开发了一种专为肺部给药而定制的脂聚糖肽疗法,它不仅对浮游的 Mrsa 具有强效活性,而且还对生物膜和细胞内的 Mrsa 受保护菌落具有强效活性,后者与临床抗生素失效有关.
      Doi:10.1128/aac.00316-21

      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-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-12221452-B2
      优先权日:2017-10-04
      标题:Synthesis of cantharidin
      发明人:DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R
      权利人:VERRICA PHARMACEUTICALS INC
      摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).

      专利号:US-12377186-B2
      优先权日:2018-01-19
      标 题:Antimicrobial biopolymer compositions, methods of synthesis, and applications of use
      发明人:KIM MINKYU; CAMP CHRISTOPHER P
      权利人:UNIV ARIZONA
      摘要:Biopolymer compositions comprising antimicrobial peptides (AMPs) for treating infections such as bacterial infections, viral infections, fungal infections, and parasitic infections. The compositions herein may also be used for treating infections associated with antibiotic-resistant bacteria, antifungal-resistant fungi, antiviral-resistant viruses, or for treating biological warfare agents (BWAs) such as Bacillus anthracis and Yersenia pestis. The present invention also provides methods of synthesis of said biopolymer compositions, wherein AMP biopolymers can be synthesized as an artificially engineered protein by genetically fusing an AMP; a protein that behaves similarly to polymer tethers; and a protein as a modifiable material platform that can transform to self-assembled nanoparticles, self-standing films, or adhesives to easily attach tethered AMPs onto any biomaterial surface for various clinical applications.

      专利号:WO-2013034675-A1
      优先权日:2011-09-09
      标 题:Process for the synthesis of telavancin and its pharmaceutically acceptable salts as well as n-protected derivatives thereof
      发明人:BENITO-GARAGORRI DAVID
      权利人:SANDOZ AG; BENITO-GARAGORRI DAVID
      摘要:The invention relates to a process for the preparation of telavancin, or a pharmaceutically acceptable salt thereof, wherein said process comprises a reductive alkylation of vancomycin which provides N-protected-decylaminoethylvancomycin, followed by aminomethyiation to obtain N-protected-telavancin, which is then deprotected to provide telavancin, or a pharmaceutically acceptable salt thereof. Another embodiment refers to N-protected-telavancin and pharmaceutically acceptable salts thereof, which are formed during the process of the invention.

      专利号:US-2015158809-A9
      优先权日:2013-02-26
      标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
      发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
      权利人:XENOPORT INC
      摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

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      主要参考文献


      1: Schroeder CP, Van Anglen LJ, Dretler RH, Adams JS, Prokesch RC, Luu Q, Krinsky AH. Outpatient treatment of osteomyelitis with telavancin. Int J Antimicrob Agents. 2017 Jul;50(1):93-96. doi: 10.1016/j.ijantimicag.2017.01.034. Epub 2017 Apr 26. doi: 10.1177/2049936117690501. Epub 2017 Mar 8. Review. Erratum in: Ther Adv Infect Dis. 2017 Nov;4(6):193.
      3: Al Jalali V, Zeitlinger M. Clinical Pharmacokinetics and Pharmacodynamics of Telavancin Compared with the Other Glycopeptides. Clin Pharmacokinet. 2018 Jul;57(7):797-816. doi: 10.1007/s40262-017-0623-4. Review.
      4: Liu Y, Wang J. A comparison of telavancin and vancomycin for treatment of methicillin-resistant Staphylococcus aureus infections: A meta-analysis. Int J Clin Pharmacol Ther. 2017 Nov;55(11):839-845. doi: 10.5414/CP202996. Review. doi: 10.1093/jac/dkx437.

      合成参考文献


      摘要:National Library of Medicine's Medical Subject Headings. Telavancin. Online file (MeSH, 2014). Available from, as of May 2, 2014:
      摘要:
      摘要:European Medicines Agency (EMA), Committee for Medicinal Products for Human Use (CHMP), European Public Assessment Report (EPAR): Vibativ (Telavancin) p.15 (2011). Available from, as of May 29, 2014:
      摘要:European Medicines Agency (EMA), Committee for Medicinal Products for Human Use (CHMP), European Public Assessment Report (EPAR): Vibativ (Telavancin) p.17 (2011).
      摘要:
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