CAS: 747412-49-3; 5-(2,4-Dihydroxy-5-Isopropylphenyl)-N-Ethyl-4-(4-(Morpholinomethyl)Phenyl)Isoxazole-3-Carboxamide

该化合物是一个小分子抑制剂,主要针对热冲击蛋白90(Hsp90),一种涉及各种客户蛋白适当折叠和稳定(其中许多与癌症的演变有关)的护身符蛋白质;该化合物是被称为Hsp90抑制剂的一类药物的一部分,由于它们能够扰乱多种诱导信号路径的功能,因此对癌症治疗产生了兴趣;AUY 922在临床研究前研究中显示,它对各种类型癌症,包括固体肿瘤和血癌的功效具有潜力;其行动机制涉及与受ATP约束的Hsp90网站具有约束力,导致客户蛋白退化和随后肿瘤生长抑制;此外,AUY 922在临床试验中受到评价,强调其药理基因特性和安全特征;作为研究的继续,AUY 922的治疗潜力及其在综合疗法中的作用可能进一步阐明其在肿瘤方面的效力.

结构式图片

上下游产品

5-(2,4-Bis(Benzyloxy)-5-Isopropylphenyl)-N-Ethyl-4(4(Morpholinomethyl)Phenyl)Isoxazole-3 Carboxamide
5-(2,4-Bis(Benzyloxy)-5-Isopropylphenyl)-4-(4-Formylphenyl)Isoxazole-3-Carboxylic Acid Ethylamide 747414-23-9
5-(2,4-双(苄氧基)-5-异丙基苯基)-N-乙基异噁唑-3-羧酰胺 5-(2,4-Bis(Benzyloxy)-5-Isopropyl-Phenyl)-N-Ethyl-Isoxazole-3-Carboxamide 747414-21-7
5-(2,4-双(苄氧基)-5-异丙基苯基)异噁唑-3-羧酸乙酯 Ethyl 5-(2,4-Bis(Benzyloxy)-5-Isopropylphenyl)Isoxazole-3-Carboxylate 747414-20-6

合成工艺路线路线简述

    📜5-(2,4-Bis(Benzyloxy)-5-Isopropylphenyl)-N-Ethyl-4(4(Morpholinomethyl)Phenyl)Isoxazole-3 Carboxamide置于三氯化硼体系中,用 二氯甲烷 作为反应溶剂,化学反应生成 5-[2,4-二羟基-5-异丙基苯基]-N-乙基-4-[4-(4-吗啉基甲基)苯基]-3-异恶唑甲酰胺
    参考文献:开发异恶唑作为用于光亲和标记和化学蛋白质组学的天然光交联剂
    标题:开发异恶唑作为用于光亲和标记和化学蛋白质组学的天然光交联剂
    摘要:异恶唑是药物发现中必不可少的药效团.在这项研究中,我们研究了异恶唑与生物分子的光化学,并将其开发为一种天然嵌入的光交联剂,用于化学蛋白质组学和药物发现.通过这种策略,两种含异恶唑的药物成功应用于化学蛋白质组学平台,以揭示它们的细胞靶点和相互作用.
    DOI:10.1002/anie.202209947

    海关参考信息

    专利信息


    专利号:US-10772971-B2
    优先权日:2017-06-22
    标 题:Methods of producing drug-carrying polymer scaffolds and protein-polymer-drug conjugates
    发明人:GURIJALA VENU REDDY; BOLLU SATYANARAYAN REDDY; LEBLANC JACQUES; LOWINGER TIMOTHY B; MCGILLICUDDY DENNIS; YIN MAO; YURKOVETSKIY ALEKSANDR V
    权利人:MERSANA THERAPEUTICS INC; MERSANA THERPEUTICS INC
    摘要:The disclosure provides methods of synthesis of polymeric scaffolds, e.g., those useful for conjugating with a protein based recognition-molecule (PBRM) to form PBRM-polymer-drug conjugates, and PBRM-polymer-drug conjugates thereof. The methods according to the disclosure allow for large-scale preparation of polymeric scaffolds having a high purity. In some embodiments, the methods according to the disclosure also allow for the preparation of scaffolds and conjugates thereof in better yield than previously used methods for preparing same. Also disclosed are methods of purifying polymeric scaffolds.

    专利号:WO-2014018862-A1
    优先权日:2012-07-27
    标 题 :Pharmaceutical compositions comprising a heat shock protein inhibitor and a; purine de novo synthesis inhibitor for treating rheumatoid arthritis or cancer
    发明人:FANG YE
    权利人:CORNING INC; FANG YE
    摘要:A pharmaceutical composition including an effective amount of the combination of: an heat shock protein (HSP) inhibitor, and a purine de novo biosynthesis inhibitor, or a pharmaceutically acceptable salt thereof. Also disclosed is a method of treating rheumatoid arthritis or cancer including administering an effective amount of the above mentioned pharmaceutical composition to a patient in need of such treatment, as defined herein.

    专利号:US-2017107577-A1
    优先权日:2014-03-11
    标题:Determining Cancer Aggressiveness, Prognosis and Responsiveness to Treatment
    发明人:AL-EJEH FARES
    权利人:THE COUNCIL OF THE QUEENSLAND INST OF MEDICAL RES
    摘要:The invention provides methods of determining the aggressiveness, prognosis and response to therapy for particular cancers, which include comparing the expression levels of one or a plurality of differentially expressed genes from one or more 5 functional metagenes, including a Carbohydrate/Lipid Metabolism metagene, a Cell Signalling metagene, a Cellular Development metagene, a Cellular Growth metagene, a Chromosome Segregation metagene, a DNA Replication/Recombination metagene, an Immune system metagene, a Metabolic Disease metagene, a Nucleic Acid Metabolism metagene, a Post-Translational Modification metagene, a Protein 10 Synthesis/Modification metagene and a Multiple Networks metagene. The method disclosed herein may be particularly suitable as a companion diagnostic for cancer therapies.

    专利号:US-11077116-B2
    优先权日:2017-07-18
    标题:Isoxazole derivatives as inducers of fetal hemoglobin in erythroid precursor cells from beta-thalassemic patients
    发明人:LAMPRONTI ILARIA; GAMBARI ROBERTO; SIMONI DANIELE
    权利人:RARE PARTNERS SRL
    摘要:The invention refers to the use of isoxazole derivatives to prepare medicament able to induce fetal hemoglobin (HbF) synthesis in β-thalassemia and sickle cell disease (SCD) patients.

    专利号:US-11312722-B2
    优先权日:2019-05-08
    标 题:Hsp90 inhibitors and uses thereof
    发明人:BROWN LAUREN ELAINE; HUANG DAVID S; COWEN LEAH E; WHITESELL LUKE; MARCYK PAUL
    权利人:UNIV BOSTON; GOVERNING COUNCIL UNIV TORONTO
    摘要:Herein is described the design and synthesis of resorcylate aminopyrazole compounds. These compounds show broad, potent and fungal-selective Hsp90 inhibitory activity. These compounds also find use in treating Hsp90 related diseases.

    专利号:US-2024066133-A1
    优先权日:2020-03-06
    标 题 :Therapeutic agents and conjugates thereof
    发明人:SONG YUNTAO; LI ANRONG; LI HUI; LI XIANFENG; YANG JUNBAO
    权利人:BEIJING XUANYI PHARMASCIENCES CO LTD
    摘要:The present disclosure provides a class of conjugates of general formula (X), a class of TLR9 agonist derivatives, such as formula (I), (XX), and (XXI), certain diastereomers of STING agonists, a class of STING agonist derivatives, such as formula (XXVIV), a class of heterocyclic compounds of general formula (II), a class of heterocyclic compounds of general formula (III), as defined herein. A 1 , A 2 , T, Z 1 , Z 2 , Z 3 , b 1 , and b 2 , in formula (X) are defined herein. The conjugate provides unique properties that are based upon the properties of the therapeutic agents that are part of the conjugate. Also provided are methods of synthesis and use of compounds.

    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: Gaykema SB, Schröder CP, Vitfell-Rasmussen J, Chua S, Oude Munnink TH, Brouwers AH, Bongaerts AH, Akimov M, Fernandez-Ibarra C, Lub-de Hooge MN, de Vries EG, Swanton C, Banerji U. 89Zr-trastuzumab and 89Zr-bevacizumab PET to Evaluate the Effect of the HSP90 Inhibitor NVP-AUY922 in Metastatic Breast Cancer Patients. Clin Cancer Res. 2014 Aug 1;20(15):3945-54. doi: 10.1158/1078-0432.CCR-14-0491. doi: 10.1007/s00280-014-2521-x. Epub 2014 Jul 25.
    3: Chiang NJ, Wu SN, Kao CA, Huang YM, Chen LT. Stimulation of Electroporation-Induced Inward Currents in Glioblastoma Cell Lines by the Heat Shock Protein Inhibitor AUY922. Clin Exp Pharmacol Physiol. 2014 Jun 7. doi: 10.1111/1440-1681.12273. [Epub ahead of print] doi: 10.3892/ijo.2013.2130. Epub 2013 Oct 4.
    7: Voruganti S, Lacroix JC, Rogers CN, Rogers J, Matts RL, Hartson SD. The anticancer drug AUY922 generates a proteomics fingerprint that is highly conserved among structurally diverse Hsp90 inhibitors. J Proteome Res. 2013 Aug 2;12(8):3697-706. doi: 10.1021/pr400321x. Epub 2013 Jun 27.

    合成参考文献


    参考文献:10.1111/j.1600-0609.2009.01403.x
    摘要:Kaiser M, Lamottke B, Mieth M, Jensen MR, Quadt C, Garcia-Echeverria C, Atadja P, Heider U, von Metzler I, Türkmen S, Sezer O. Synergistic action of the novel HSP90 inhibitor NVP-AUY922 with histone deacetylase inhibitors, melphalan, or doxorubicin in multiple myeloma. Eur J Haematol. 2010 Apr;84(4):337–44. doi: 10.1111/j.1600-0609.2009.01403.x.
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