CAS: 593960-11-3; N-(5-(4-Chloro-3-(N-(2-Hydroxyethyl)Sulfamoyl)Phenyl)-4-Methylthiazol-2-yl)Acetamide

该化合物是一个合成有机化合物,其结构复杂,包括一个硫酸盐环,一个磺酰胺组和一个乙酰胺细胞.该化合物通常具有诸如极地溶剂中溶性等特性,因为存在可进行氢结合的氢氧和氨基功能组.氯和硫酸替代组可能有助于其生物活动,有可能影响其与生物目标的互动.经常对其药用特性进行研究,特别是在药物开发方面,评估其功效和安全特征.多种功能组的存在表明,它可能参与各种化学反应,使其成为医药化学中的一种灵敏性化合物.与许多合成化合物一样,处理应谨慎,遵循适当的安全议定书,以减少与使用该物质有关的潜在危害.

结构式图片

合成工艺路线路线简述

    4-氯苯基丙酮置于氯磺酸,Tribromure De Carboxyethyl-2 Triphenylphosphonium体系中,用 四氢呋喃,乙醇 作为反应溶剂,化学反应 3.5H,反应生成 N-[5-[4-氯-3-[[(2-羟基乙基)氨基]磺酰基]苯基]-4-甲基-2-噻唑基]乙酰胺
    参考文献:磷脂酰肌醇4激酶iiiβ的有效和选择性抑制剂的设计和结构表征
    标题:磷脂酰肌醇4激酶iiiβ的有效和选择性抑制剂的设计和结构表征
    摘要:Iii型磷脂酰肌醇4激酶(pi4Kiiiβ)是介导膜运输的必不可少的酶,与多种致病过程有关.它是介导rna病毒复制的关键宿主因子.该酶的有效和特异性抑制剂的设计对于定义其细胞作用至关重要,并可能导致新型抗病毒治疗.我们先前曾报道过pi4K抑制剂pik93,并且该化合物具有pi4Kiiiβ的关键功能.然而,该化合物显示出与i和iii类pi3K的高交叉反应性.使用基于结构的药物设计,我们设计了新颖的有效和选择性(比i和iii类pi3K高1000倍以上)的pi4Kiiiβ抑制剂.这些化合物显示出抗丙型肝炎病毒的抗病毒活性.与最有效的化合物之一结合的pi4Kiiiβ的共晶体结构揭示了特异性的分子基础.这项工作对于新型pi4Kiiiβ抑制剂的设计至关重要,而pi4Kiiiβ抑制剂可能起着重要的抗病毒治疗作用.
    DOI:10.1021/acs.Jmedchem.5B01311

    海关参考信息

    专利信息


    专利号:US-2025289827-A1
    优先权日:2022-12-02
    标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
    发明人:YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
    权利人:C4 THERAPEUTICS INC
    摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.
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    主要参考文献

    1. Inhibitors of the PI3k/Akt/Ikk/NF-kb signalling pathway, pharmaceutically acceptable salts thereof and compositions containing said inhibitors for prophylaxis and treatment of viral diseases. By Fedichev, Petr Olegovich; Vinnik, Andrey Alexandrovich. From PCT Int. Appl. (2013), WO 2013147649 A2 20131003, 2. Phosphatidylinositol 4-kinase III beta is essential for replication of human rhinovirus and its inhibition causes a lethal phenotype in vivo. By Spickler, Catherine; Lippens, Julie; Laberge, Marie-Kristine; Desmeules, Sophie; Bellavance, Edith; Garneau, Michel; Guo, Tim; Hucke, Oliver; Leyssen, Pieter; Neyts, Johan; et al. From Antimicrobial Agents and Chemotherapy (2013), 57(7), 3358-3368. , 3. Autoimmune and inflammatory disorder therapy using inhibitors of phosphatidylinositol-4-kinase IIIβ and screening methods thereof By Herman, Jean; Louat, Thierry; Huang, Qiuya; Vanderhoydonck, Bart; Waer, Mark; Herdewijn, Piet From PCT Int. Appl. (2013), WO 2013034738 A1 20130314, 4. Methods for predicting cancer treatment responsiveness to phosphatidylinositol 3-kinase (PI3K) inhibitors. By Jane, Stephen M.; Darido, Charbel. From PCT Int. Appl. (2013), WO 2013029116 A1 20130307, 5. Coxsackievirus mutants that can bypass host factor PI4KIIIβ and the need for high levels of PI4P lipids for replication. By van der Schaar, Hilde M.; van der Linden, Lonneke; Lanke, Kjerstin H. W.; Strating, Jeroen R. P. M.; Puerstinger, Gerhard; de Vries, Erik; de Haan, Cornelis A. M.; Neyts, Johan; van Kuppeveld, Frank J. M. From Cell Research (2012), 22(11), 1576-1592. , DOI:10.1038/cr.2012.129 6. Methods for treating oncovirus positive cancers. By Jimeno, Antonio; Hausman, Diana F.; Peterson, Scott. From PCT Int. Appl. (2012), WO 2012118978 A1 20120907, 7. Methods and compositions targeting signaling pathways for the treatment of cancer By Brugge, Joan S.; Muranen, Taru; Mills, Gordon; Selfors, Laura. From PCT Int. Appl. (2011), WO 2011133668 A2 20111027, 8. Phosphatidylinositol 4-kinase III beta is a target of enviroxime-like compounds for antipoliovirus activity By Arita, Minetaro; Kojima, Hirotatsu; Nagano, Tetsuo; Okabe, Takayoshi; Wakita, Takaji; Shimizu, Hiroyuki. From Journal of Virology (2011), 85(5), 2364-2372. , DOI:10.1128/JVI.02249-10 9. Modification of proteins for detection in cellular assays By Treiber, Daniel Kelly; Lewis, Warren G.; Wodicka, Lisa M. From PCT Int. Appl. (2010), WO 2010124157 A1 20101028, 10. Shaping Development of Autophagy Inhibitors with the Structure of the Lipid Kinase Vps34 By Miller, Simon; Tavshanjian, Brandon; Oleksy, Arkadiusz; Perisic, Olga; Houseman, Benjamin T.; Shokat, Kevan M.; Williams, Roger L. From Science (Washington, DC, United States) (2010), 327(5973), 1638-1642. , 11. Discovery of drug-resistant and drug-sensitizing mutations in the oncogenic PI3K isoform p110α By Zunder, Eli R.; Knight, Zachary A.; Houseman, Benjamin T.; Apsel, Beth; Shokat, Kevan M. From Cancer Cell (2008), 14(2), 180-192. , DOI:10.1016/j.ccr.2008.06.014 12. Phosphoinositide modulation for the treatment of neurodegenerative diseases By Kim, Tae-Wan; Dipaolo, Gilbert; Kang, Min Suk; Berman, Diego; McIntire, Laura Beth Johnson From PCT Int. Appl. (2008), WO 2008064244 A2 20080529, 13. Design of Drug-Resistant Alleles of Type-III Phosphatidylinositol 4-Kinases Using Mutagenesis and Molecular Modeling By Balla, Andras; Tuymetova, Galina; Toth, Balazs; Szentpetery, Zsofia; Zhao, Xiaohang; Knight, Zachary A.; Shokat, Kevan; Steinbach, Peter J.; Balla, Tamas From Biochemistry (2008), 47(6), 1599-1607. , DOI:10.1021/bi7017927 14. A pharmacological map of the PI3-K family defines a role for p110α in insulin signaling By Knight, Zachary A.; Gonzalez, Beatriz; Feldman, Morri E.; Zunder, Eli R.; Goldenberg, David D.; Williams, Olusegun; Loewith, Robbie; Stokoe, David; Balla, Andras; Toth, Balazs; et al From Cell (Cambridge, MA, United States) (2006), 125(4), 733-747. , 15. A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma . By Fan, Qi-Wen; Knight, Zachary A.; Goldenberg, David D.; Yu, Wei; Mostov, Keith E.; Stokoe, David; Shokat, Kevan M.; Weiss, William A. From Cancer Cell (2006), 9(5), 341-349. 16. 5-Phenylthiazole derivatives and their use as phosphatidylinositol 3-kinase (Pi3K) inhibitors for the treatment of allergic and inflammatory diseases. By Bruce, Ian; Finan, Peter; Leblanc, Catherine; McCarthy, Clive; Whitehead, Lewis; Blair, Nicola Elaine; Bloomfield, Graham Charles; Hayler, Judy; Kirman, Louise; Oza, Mrinalini Sachin; et al. From PCT Int. Appl. (2003), WO 2003072557 A1 20030904,

    合成参考文献


    摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749
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