CAS: 23674-86-4; (6S,8S,9R,10S,11S,13S,14S,17R)-17-(2-Acetoxyacetyl)-6,9-Difluoro-11-Hydroxy-10,13-Dimethyl-3-Oxo-6,7,8,9,10,11,12,13,14,15,16,17-Dodecahydro-3H-Cyclopenta[a]Phenanthren-17-Yl Butyrate (Fluocortolone Impurity)

该化合物是作为独立化学化合物."pitope"一词是指免疫系统,特别是抗体,T细胞受体或B细胞受体承认的抗原的具体部分.眼部可以是线性或相容性的,对于免疫反应的特殊性至关重要.在研究和治疗应用方面,与顶部有关的物质可能涉及疫苗的开发,诊断和自动免疫疾病研究.这些物质的特性通常包括它们获得免疫反应的能力,结构多样性以及它们改变以加强免疫性的潜力.虽然作为化学实体的Epipotic的具体特性可能没有广泛的文献记载,但在生物和医学领域的相关性强调了了解免疫系统相互作用方面的顶部的重要性.

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

6A,9-二氟-11B,17,21-三羟基孕甾-1,4-二烯-3,20-二酮17-丁酸酯 6Alpha,9-Difluoro-11Beta,17,21-Trihydroxypregna-1,4-Diene-3,20-Dione 17-Butyrate 23640-96-2

合成工艺路线路线简述

    (6S,8S,9R,10S,11S,13S,14S,17R)-17-(2-Acetoxyacetyl)-6,9-Difluoro-11-Hydroxy-10,13-Dimethyl-3-Oxo-2,3,6,7,8,9,10,11,12,13,14,15,16,17-Tetradecahydro-1H-Cyclopenta[a]Phenanthren-17-Yl Butyrate 以70的收率获得二氟孕甾丁酯
    参考文献:一种制备二氟泼尼酯的方法
    标题:一种制备二氟泼尼酯的方法
    摘要:本发明公开了二氟泼尼酯的一种新型制备方法.以市场上常见且价格低廉的氢化可的松-21-醋酸酯为原料,通过羟基消除成9,11位双键,17位丁酸酯化,6,9位氟代以及1,2位脱氢最终得到二氟泼尼酯,共九步反应.其中17位丁酸酯化可以一步定量得到关键中间体化合物iv,从而大大简化了原有工艺;两步氟代反应采用的试剂环保低毒,反应条件温和,适合工业化生产.该方法与文献报道方法相比,路线更短,操作更简便,收率和成本等方面都具有明显的优势.

    海关参考信息

    专利信息


    专利号:US-11964965-B2
    优先权日:2020-05-08
    标题 :Methods of manufacture and synthesis of fluorescent dye compounds and uses thereof
    发明人:KULARATNE SUMITH A; GAGARE PRAVIN
    权利人:ON TARGET LABORATORIES LLC
    摘要:The present disclosure relates to synthesizing and utilizing fluorescent dye compounds or pharmaceutically acceptable salts thereof. Conjugation of amino acid groups to the fluorescent dyes increase specificity and detection of the compound. Methods of manufacture and synthesis of the compounds for use thereof in diagnostic imaging are contemplated.

    专利号:US-12391691-B2
    优先权日:2018-11-16
    标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
    发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
    权利人:AMGEN INC
    摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

    专利号:US-2025206736-A1
    优先权日:2019-11-14
    标题 :Synthesis of kras g12c inhibitor compound
    发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
    权利人:AMGEN INC
    摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

    专利号:WO-2022226312-A1
    优先权日:2021-04-22
    标 题:Combination nucleotide pool depletion for treatment of viral infections and cancers
    发明人:KUMAR VIKRAM; HESSON DAVID; DEMAREST JAMES
    权利人:CLEAR CREEK BIO INC
    摘要:The invention provides methods of treating cancers and viral infections by providing a combination of agents that inhibit both nucleotide synthesis and nucleotide salvage in the cells of a subject to prevent cancer proliferation and viral replication. The invention provides methods of depleting nucleotide pools by using both inhibitors of dihydroorotate dehydrogenase (DHODH), such as brequinar, which block synthesis of pyrimidine-based nucleotides, in combination of one or more nucleotide salvage inhibitors, for example deoxycytidine kinase (dCK) inhibitors, Equilibrative nucleoside transporter (ENT) inhibitors, and Uridine-cytidine kinase (UCK) inhibitors, which inhibit salvage of purine and/or pyrimidine-based nucleotides or nucleosides

    专利号:WO-0136626-A9
    优先权日:1999-11-15
    标 题 :Pentraxin i and pentraxin receptor, inhibitors of said proteins and pharmaceutical compositions containing said compounds
    发明人:MESSEGUER PEYPOCH RAMON; ROSELL VIVES ELISABET; MARTINEZ ESCOLA JOSEP MA; RODES GUBERN BLANCA; ADAN PLANA JAUME; PUIG CALVO NURIA; CARCELLER ROSA ANA; MASA ALVAREZ MARC; PIULATS XANCO JAUME; DEN DAAS IZAAK; TRULLAS OLIVA RAMON; DE GREGORIO-ROCASOLANO BARBANY
    权利人:MERCK PATENT GMBH; MESSEGUER PEYPOCH RAMON; ROSELL VIVES ELISABET; MARTINEZ ESCOLA JOSEP MA; RODES GUBERN BLANCA; ADAN PLANA JAUME; PUIG CALVO NURIA; CARCELLER ROSA ANA; MASA ALVAREZ MARC; PIULATS XANCO JAUME; DEN DAAS IZAAK; TRULLAS OLIVA RAMON; DE GREGORIO-ROCASOLANO BARBANY
    摘要:Described are nucleic acid sequences encoding the human Pentraxin receptor and related proteins and pharmaceutical composition comprising a therapeutically effective amount of (a) Pentraxin I or the human Pentraxin receptor, (b) a nonfunctional variant of the protein of (a), (c) an antibody to the protein of (a) or (b), (d) a nucleic acid sequence encoding the protein of (a) or (b), (e) an antisense RNA sequence, said sequence being capable of inhibiting the synthesis of Pentraxin 1 or the human Pentraxin receptor, or (f) a ribozyme characterized in that it is complementary to a Pentraxin I or human Pentraxin receptor mRNA and can selectively bind to and cleave said mRNA, thus inhibiting the synthesis of Pentraxin I or the human Pentraxin receptor.

    专利号:US-11649285-B2
    优先权日:2016-08-03
    标题 :Identification of VSIG3/VISTA as a novel immune checkpoint and use thereof for immunotherapy
    发明人:KALABOKIS VASSILIOS; WANG JINGHUA; WU GUOPING; BAZAN JOSE FERNANDO; VALLEY CHRISTOPHER CARLIN
    权利人:BIO TECHNE CORP
    摘要:The ligand for VISTA is identified (VSIG3) as well as the use of this ligand and receptor interaction in the identification or synthesis of a VSIG3 agonist or antagonist compounds, preferably antibodies, polypeptides and fusion proteins which agonize or antagonize the effects of VSIG3 and/or VISTA and/or the VSIG3/VISTA interaction. These antagonists may be used to suppress VSIG3/VISTA's suppressive effects on T cell immunity, and more particularly used in the treatment of cancer, or infectious disease. These agonist compounds may be used to potentiate or enhance VSIG3/VISTA's suppressive effects on T cell immunity and thereby suppress T cell immunity, such as in the treatment of autoimmunity, allergy or inflammatory conditions. Screening assays for identifying these agonists and antagonist compounds are also provided.
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    主要参考文献


    1: Symes RJ, Forooghian F. Topical difluprednate monotherapy for uveitic macular edema. Can J Ophthalmol. 2016 Feb;51(1):47-9. doi: 10.1016/j.jcjo.2015.10.007. doi: 10.2147/OPTH.S72955. eCollection 2015.
    4: Giacobbe C, Palmisano G, Giovenzana GB, Giovannelli L, Negri R, Masciocchi N. Difluprednate: more than meets the eye. J Pharm Biomed Anal. 2015 Jan;102:305-13. doi: 10.1016/j.jpba.2014.09.028. Epub 2014 Sep 30. doi: 10.1097/IAE.0000000000000215. doi: 10.1167/iovs.13-12660.
    7: Yamamoto T, Nakano Goto S, Abe S, Kirii E, Yamashita H. Difluprednate ophthalmic emulsion 0.05% as adjunctive treatment to panretinal photocoagulation for proliferative diabetic retinopathy with clinically significant macular edema. Retin Cases Brief Rep. 2012 Summer;6(3):228-31. doi: 10.1097/ICB.0b013e318224776f. doi: 10.1016/j.ajo.2011.10.008. Epub 2012 Jan 20. doi: 10.2147/OPTH.S28151. Epub 2012 Jan 24.

    合成参考文献


    参考文献:10.1159/000089030
    摘要:Kawada K, Maeda N, Kobayashi S, Sowa J, Tsuruta D, Kawada N. Injection site with generalized rash caused by pegylated interferon alpha 2a injection. Dermatology. 2006;212(1):82–3. doi: 10.1159/000089030.
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