CAS: 235114-32-6; Micafungin

该化合物是属于echinocandin类的抗风素药物,主要用于治疗侵入性真菌感染,特别是由Candida和Aspergills物种造成的真菌感染,它抑制了真菌细胞墙基本组成部分-(1,3,3)-D-glucan的合成,从而损害了真菌的结构性完整性,导致细胞解析.Micafungin通常通过静脉注射进行,其特点是蛋白质约束能力高,半衰期相对较长,允许每天一次服用.它一般是良好的,具有常见的副作用,包括发烧,恶心和与输血有关的反应.Micafungin没有从胃肠道中大量吸收,这就是为什么它被亲生地吸收.它的活动范围使得它特别有助于治疗白血和食道直线性丝,特别是在免疫共融化的病人中. 与任何抗反烟疗法一样,监测潜在的药物相互作用和抗药性对于有效治疗结果至关重要.

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    FR 179642 1-[[4-[5-(4-pentyloxyphenyl)isoxazol-3-yl]benzoyl]oxy]-1H-1,2,3-benzotriazole 21H20ClNO3C21H20ClNO3 27H28N3O9PC27H28N3O9P

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      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-10443047-B2
      优先权日:2014-05-01
      标题 :Increasing cellular lipid production by increasing the activity of diacylglycerol acyltransferase and decreasing the activity of triacylglycerol lipase
      发明人:TSAKRAKLIDES VASILIKI; BREVNOVA ELENA E
      权利人:NOVOGY INC
      摘要:Disclosed are methods and compositions for increasing the triacylglycerol content of a cell by up-regulating diacylglycerol acyltransferase and down-regulating triacylglycerol lipase. In some embodiments, a DGA1 protein is expressed and a native TGL3 gene is knocked out, thereby increasing the synthesis of triacylglycerol and decreasing its consumption, respectively.

      专利号:US-2023364251-A1
      优先权日:2020-08-06
      标 题:Methods for the synthesis of protein-drug conjugates
      发明人:BORCHARDT ALLEN; HUGHES ROBERT MICHAEL
      权利人:CIDARA THERAPEUTICS INC
      摘要:The present invention relates to intermediates and methods for synthesizing protein-drug conjugates that can be used for the treatment of diseases and related conditions.

      专利号:US-9695214-B2
      优先权日:2013-03-15
      标 题 :Solid phase peptide synthesis processes and associated systems
      发明人:SIMON MARK DAVID; PENTELUTE BRADLEY L; ADAMO ANDREA; HEIDER PATRICK LOUIS; JENSEN KLAVS F
      权利人:MASSACHUSETTS INST TECHNOLOGY
      摘要:Systems and processes for performing solid phase peptide synthesis are generally described. Solid phase peptide synthesis is a known process in which amino acid residues are added to peptides that have been immobilized on a solid support. In certain embodiments, the inventive systems and methods can be used to perform solid phase peptide synthesis quickly while maintaining high yields. Certain embodiments relate to processes and systems that may be used to heat, transport, and/or mix reagents in ways that reduce the amount of time required to perform solid phase peptide synthesis.

      专利号:US-2007099915-A1
      优先权日:2005-10-07
      标题 :Inhibitors of the hiv integrase enzyme
      发明人:DRESS KLAUS R; JOHNSON TED W; PLEWE MICHAEL B; TANIS STEVEN P; ZHU HUICHUN
      权利人:PFIZER
      摘要:The present invention is directed to compounds of formula (I), n nand pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus (“HIVâ€?) integrase enzyme.

      专利号:US-2023365629-A1
      优先权日:2018-06-15
      标题:Synthesis of echinocandin antifungal agent
      安润医药科技(苏州)有限公司
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      主要参考文献


      1: Spettel K, Galazka S, Kriz R, Camp I, Willinger B. Do Candida albicans Isolates with Borderline Resistant Micafungin MICs Always Harbor FKS1 Hot Spot Mutations? J Fungi (Basel). 2021 Jan 28;7(2):93. doi: 10.3390/jof7020093. 8(12):1867. doi: 10.3390/microorganisms8121867.
      6: Mullins C, Beaulac K, Sylvia L. Reply: Drug-Induced Liver Injury (DILI) With Micafungin: The Importance of Causality Assessment. Ann Pharmacother. 2020 Nov
      15:1060028020973607. doi: 10.1177/1060028020973607. Epub ahead of print. 76(2):418-422. doi: 10.1093/jac/dkaa419. Japan Febrile Neutropenia Study Group. Efficacy and safety of micafungin in empiric and D-index-guided early antifungal therapy for febrile neutropenia; A subgroup analysis of the CEDMIC trial. Int J Infect Dis. 2020 Nov;100:292-297. doi: 10.1016/j.ijid.2020.08.081. Epub 2020 Sep 3. 6(3):136. doi: 10.3390/jof6030136.

      合成参考文献


      参考文献:10.3109/13693780903471784
      摘要:Choi JH, Kwon EY, Park CM, Choi SM, Lee DG, Yoo JH, Shin WS, Stevens DA. Immunomodulatory effects of antifungal agents on the response of human monocytic cells to Aspergillus fumigatus conidia. Med Mycol. 2010 Aug;48(5):704–9. doi: 10.3109/13693780903471784.
      参考文献:10.1111/j.1442-200x.2009.02947.x
      摘要:Okamoto T, Koh K, Takita J, Furuya A, Kato M, Ida K. Voriconazole–micafungin combination therapy for acute lymphoblastic leukemia. Pediatrics International. 2010 Jan 25;52(1):137–41. doi: 10.1111/j.1442-200x.2009.02947.x.
      参考文献:10.3109/14767058.2011.604929
      摘要:Manzoni P, Benjamin DK, Hope W, Rizzollo S, Sordo PD, Stronati M, Jacqz-Aigrain E, Castagnola E, Farina D. The management ofCandidainfections in preterm neonates and the role of micafungin. The Journal of Maternal-Fetal & Neonatal Medicine. 2011 Jul 12;24(sup2):24–7. doi: 10.3109/14767058.2011.604929.
      参考文献:10.1089/jop.2011.0026
      摘要:Mochizuki K, Suemori S, Udo K, Komori S, Ohkusu K, Yamada N, Ogura S. Intraocular Penetration of Micafungin in Patient with Candida albicans Endophthalmitis. Journal of Ocular Pharmacology and Therapeutics. 2011 Oct;27(5):531–3. doi: 10.1089/jop.2011.0026.
      参考文献:10.1016/j.jbiosc.2011.06.002
      摘要:Ueda S, Kinoshita M, Tanaka F, Tsuboi M, Shimizu S, Oohata N, Hino M, Yamada M, Isogai Y, Hashimoto S. Strain selection and scale-up fermentation for FR901379 acylase production by Streptomyces sp. no. 6907. Journal of Bioscience and Bioengineering. 2011 Oct;112(4):409–14. doi: 10.1016/j.jbiosc.2011.06.002.
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