CAS: 3801-06-7; (6S,8S,9R,10S,11S,13S,14S,17R)-17-Acetyl-9-Fluoro-11-Hydroxy-6,10,13-Trimethyl-3-Oxo-6,7,8,9,10,11,12,13,14,15,16,17-Dodecahydro-3H-Cyclopenta[a]Phenanthren-17-Yl Acetate

该化合物是一种主要用于眼科配方的合成花生类固醇,主要用于其抗炎和免疫抑制特性的眼科配方,其特点是能够减少炎症并缓解与各种眼疾有关的症状,例如过敏结膜炎和手术后炎症.该化合物具有氟化类固醇结构的特点,与非氟化的花生类相比,这种结构增强了其药力并减少了系统性副作用.氟化聚醇乙酸酯通常作为一种眼滴溶液施用,允许进行局部化处理,而其系统吸收程度则最小.其行动机制包括抑制炎性调节器和免疫反应的调节.该物质一般都受到良好的调制,但潜在的副作用可能包括长期使用增加的内腔压力和白内酯形成.与任何花类固醇一样,仔细监测对于减轻与长期治疗有关的风险至关重要.

结构式图片

欧盟法规

ECHA物质C&L通报REACH预注册

上下游产品

[(6S,8S,10R,13S,14S,17R)-17-乙酰基-6,10,13-三甲基-3-氧代-7,8,12,14,15,16-六氢-6H-环戊二烯并[a]菲-17-基]乙酸酯 6-Methyl-3,20-Dioxo-1,4,9(11)-Pregnatrien-17-Acetate 130145-14-1
(9Beta,11Beta)-环氧氟米龙乙酸酯 17α-Acetoxy-6α-Methyl-9β,11β-Oxidopregna-1,4-Dien-3,20-Dione 83873-17-0

合成工艺路线路线简述

    (9Beta,11Beta)-环氧氟米龙乙酸酯置于氢氟酸体系中,用 水 作为反应溶剂,化学反应 4.0H,以84.7%的收率获得产物氟米龙醋酸酯
    参考文献:氟米龙及氟米龙醋酸酯与制备方法
    标题:氟米龙及氟米龙醋酸酯与制备方法
    摘要:本发明公开了一种氟米龙及氟米龙醋酸酯与制备方法.该制备方法以式ⅱ所示化合物为原料,依次经过脱氯反应,酯化反应,次甲基化反应,氢化反应,发酵脱氢反应,环氧反应,开环反应,制得氟米龙的衍生物,氟米龙的衍生物再经过水解反应,制得氟米龙,该制备方法合成路线短,收率高,原料成本低,原料易得,纯化方便简单,产品纯度高,工艺可操作性强,适合于工业化生产,具有很高的工业化价值.

    海关参考信息

    专利信息


    专利号:US-8734846-B2
    优先权日:2008-06-16
    标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles
    发明人:ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS
    权利人:BIND BIOSCIENCES INC
    摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

    专利号:US-9051302-B2
    优先权日:2008-01-15
    标 题 :Synthesis of resorcylic acid lactones useful as therapeutic agents
    发明人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN
    权利人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN; UNIV STRASBOURG
    摘要:Disclosed are macrocyclic compounds of formulae I, I′, II, II′, III, III′, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.

    专利号:US-2013035307-A1
    优先权日:2010-01-26
    标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers
    发明人:PRESTWICH GLENN D; KENNEDY THOMAS P
    权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P
    摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.

    专利号:WO-2010122096-A1
    优先权日:2009-04-23
    标题:Process for obtaining fluorometholone and intermediates therefor
    发明人:LORENTE BONDE-LARSEN ANTONIO; IGLESIAS RETUERTO JESUS MIGUEL; HERRAIZ SIERRA IGNACIO; BERMEJO GONZALEZ FRANCISCO; MARCOS ESCRIBANO JOSE ANDRES; GUTIERREZ FUENTES LUIS GERARDO
    权利人:CRYSTAL PHARMA S L U; LORENTE BONDE-LARSEN ANTONIO; IGLESIAS RETUERTO JESUS MIGUEL; HERRAIZ SIERRA IGNACIO; BERMEJO GONZALEZ FRANCISCO; MARCOS ESCRIBANO JOSE ANDRES; GUTIERREZ FUENTES LUIS GERARDO
    摘要:The present invention relates to a process for obtaining compounds of formula (I) and (V), wherein R 1 is C 1 -C 6 alkyl; and R 2 is OR 3 , OC(=O)R 4 or O-(HPG), wherein R 3 is H, C 1 -C 6 alkyl or C 6 -C 14 aryl; R 4 is H or C 1 -C 6 alkyl; and HPG is a hydro xyl protecting group, intermediates useful in the synthesis of some steroids, for example, fluorometholone and derivatives thereof. The invention also relates to other intermediates useful in synthesis.

    专利号:WO-2023096715-A9
    优先权日:2021-10-22
    标 题:Immunomodulatory glycosphingolipids and methods of use thereof
    发明人:KASPER DENNIS; OH SUNGWHAN
    权利人:HARVARD COLLEGE
    摘要:Provided herein are a subset of alpha-galactosylceramide (alpha-GC) compounds having improved immunomodulatory activity, particularly with respect to NKT cell number and activity. Also provided herein are methods of use of such compounds, including in the modulation of NKT cells and/or activity in vivo. Further provided are combinatorial synthesis methods for generating alpha-GC compounds of specifically defined structure and thereby generating pure preparations thereof.

    专利号:US-9982006-B2
    优先权日:2014-08-21
    标题:2′-chloro aminopyrimidinone and pyrimidine dione nucleosides
    发明人:CLARKE MICHAEL O'NEIL HANRAHAN; MACKMAN RICHARD L; SIEGEL DUSTIN
    权利人:GILEAD SCIENCES INC
    摘要:Provided herein are formulations, methods and substituted 2′-chloro aminopyrimidinone and pyrimidine dione compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of substituted 2′-chloro aminopyrimidinone and pyrimidine dione compounds.
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    主要参考文献


    1: Sohn S, Hur W, Choi YR, Chung YS, Ki CS, Kee C. Little evidence for association of the glaucoma gene MYOC with open-angle glaucoma. Br J Ophthalmol. 2010 May;94(5):639-42. Review. Portuguese. Epub 2008 Jul 9. Epub 2008 Mar 21.
    9: Rodrigues EB, Maia M, Meyer CH, Penha FM, Dib E, Farah ME. Vital dyes for chromovitrectomy. Curr Opin Ophthalmol. 2007 May;18(3):179-87. Review. Epub 2006 Dec 21.

    合成参考文献


    参考文献:10.1124/mol.119.115964
    摘要:Lee TD, Lee OW, Brimacombe KR, Chen L, Guha R, Lusvarghi S, Tebase BG, Klumpp-Thomas C, Robey RW, Ambudkar SV, Shen M, Gottesman MM, Hall MD. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular Pharmacology. 2019 Nov;96(5):629–40. doi: 10.1124/mol.119.115964.
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