CAS: 49697-38-3; Rimexolone

该化合物是一种合成的可理可乐机器人,主要用于眼科配方,其强效抗炎和免疫抑制特性,其主要优势在于高溶胶受体感应度,能够有效管理后性炎和内脏肠炎,同时减少系统性吸收.Rimexolone的分子结构可以提高角膜渗透,同时最大限度地减少内部压力升高,这是其他类固醇的共同关切.它展示了一种有利的安全特征,适合短期眼科治疗.该化合物的快速行动以及可预测的药用植物遗传学进一步支持其在定向眼科应用中的临床作用.其功效与传统的花生类动物相似,但可能较少产生不良效应.

结构式图片

欧盟法规

C&L通报

上下游产品

11β-(Trimethylsiloxy)-16α,17α,21-Trimethylpregna-1,4-Dien-3,20-Dione 220983-31-3
11β-Hydroxy-1,4,16-Trienepregna-3,20-Dione 60124-50-7
迪普罗酮 11β,17α-Dihydroxypregna-1,4-Diene-3,20-Dione 20423-99-8
泼尼松龙 Prednisolon 50-24-8
21-Methyl-11β-(Trimethylsiloxy)-Pregna-1,4,16-Trien-3,20-Dione 207346-24-5
11β-(Trimethylsiloxy)-Pregna-1,4,16-Trien-3,20-Dione 60124-51-8
16α,21-Dimethyl-11β,20-Bis(Trimethylsiloxy)-Pregna-1,4,17(20)-Trien-3-One 226712-41-0

合成工艺路线路线简述

  • 合成目标产物 Rimexolone (100 Mg) 主要起始原料 Prednisolone
  • (文献来源)合成步骤主要原料 Prednisolone
📜泼尼松龙置于吡啶,盐酸,4-二甲氨基吡啶,4 A Molecular Sieve,盐酸氨基脲,苄基三甲基氟化铵,溶剂黄146,Sodium Iodide,Lithium Hexamethyldisilazane体系中,用 四氢呋喃,甲醇,六甲基磷酰三胺,水,溶剂黄146,丙酮 作为反应溶剂,化学反应 38.37H,反应生成 瑞美松龙
参考文献:Synthesis Of The 16α,17α,21-Trimethyl Corticosteroid Rimexolone From Prednisolone
标题:Synthesis Of The 16α,17α,21-Trimethyl Corticosteroid Rimexolone From Prednisolone
摘要:
DOI:10.1021/jo981848X

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-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:US-8697730-B2
优先权日:2007-10-26
标题 :5-lipoxygenase activating protein (FLAP) inhibitor
发明人:REWOLINSKI MELISSA VIRGINIA; SCHAAB KEVIN MURRAY; KING CHRISTOPHER DAVID; STOCK NICHOLAS SIMON
权利人:REWOLINSKI MELISSA VIRGINIA; SCHAAB KEVIN MURRAY; KING CHRISTOPHER DAVID; STOCK NICHOLAS SIMON; PANMIRA PHARMACEUTICALS LLC
摘要:Described herein are methods for the synthesis of 3-[5-(pyridin-2-ylmethoxy)-3-(2-methyl-2-propylthio)-1-[4-(2-methoxypyridin-5-yl)benzyl]-indol-2-yl]-2,2-dimethyl-propionic acid, pharmaceutically acceptable salts, pharmaceutically acceptable solvates thereof. Also described are pharmaceutical compositions suitable for oral administration to a mammal that include, as well as methods of using such oral pharmaceutical compositions for treating respiratory conditions or diseases, as well as other leukotriene-dependent or leukotriene mediated conditions or diseases.

专利号:WO-2012014114-A1
优先权日:2010-07-30
标 题:Matrix metalloproteinase inhibitors
发明人:KHERA MANOJ KUMAR; SATTIGERI JITENDRA; SATTIGERI VISWAJANANI; YADAV NEERAJ KUMAR; KUMAR KEWAL; RAUF ABDUL REHMAN ABDUL; CLIFFE IAN A; BHATNAGAR PRADIP KUMAR; RAY ABHIJIT; SRIVASTAVA PUNIT; DASTIDAR SUNANDA GHOSH
权利人:RANBAXY LAB LTD; KHERA MANOJ KUMAR; SATTIGERI JITENDRA; SATTIGERI VISWAJANANI; YADAV NEERAJ KUMAR; KUMAR KEWAL; RAUF ABDUL REHMAN ABDUL; CLIFFE IAN A; BHATNAGAR PRADIP KUMAR; RAY ABHIJIT; SRIVASTAVA PUNIT; DASTIDAR SUNANDA GHOSH
摘要:The present invention relates to certain hydroxy propionic acid derivatives and the processes for the synthesis of the same. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, dry eye, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by over-expression and over activation of a matrix metalloproteinase using the compounds.

专利号:CN-1908003-A
优先权日:2006-08-15
标 题:Synthesis of 9α-bromo-11β-hydroxypregna-1,4,16-triene-3,20-dione

专利号:EP-4058432-A1
优先权日:2019-11-14
标 题:Improved synthesis of kras g12c inhibitor compound

供应商参考报价(招募中)

品牌试剂参考报价(招募中)

📌 第三方产品分析报告

✅ COA系统入驻 | 共享模式

主要参考文献


1: Spies CM, Gaber T, Hahne M, Naumann L, Tripmacher R, Schellmann S, Stahn C, Burmester GR, Radbruch A, Buttgereit F. Rimexolone inhibits proliferation, cytokine expression and signal transduction of human CD4+ T-cells. Immunol Lett. 2010 Jun 15;131(1):24-32. doi: 10.1016/j.imlet.2010.03.009. Epub 2010 Apr 2. Spanish. Epub 2007 Aug 31. Epub 2005 Mar 9. Spanish. Review.

合成参考文献


参考文献:10.3341/kjo.2010.24.1.57
摘要:Lee H, Kim CY, Seong GJ, Ma KT. A case of decreased visual field after uneventful cataract surgery: nonarteritic anterior ischemic optic neuropathy. Korean J Ophthalmol. 2010 Feb;24(1):57–61.
参考文献:10.2147/opth.s7633
摘要:Reddy R, Kim SJ. Critical appraisal of ophthalmic ketorolac in treatment of pain and inflammation following cataract surgery. Clin Ophthalmol. 2011;5():751–8.
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