CAS: 958852-01-2; (Z)-5-((4-(Pyridin-4-yl)Quinolin-6-yl)Methylene)Thiazolidine-2,4-Dione

该化合物是化学化合物,主要针对其潜在的治疗用途进行研究,被归类为小分子,并被视为某些生物途径的选择性抑制物,特别是那些涉及炎症和免疫反应的路径;该化合物是针对各种疾病,包括自免疫障碍和某些类型的癌症进行调查的;其行动机制通常包括调节特定的酶或受体,导致改变细胞信号. GSK1059615的特点是其独特的分子结构,有助于其生物活动和选择性.与许多调查化合物一样,该化合物的安全性,功效和药用基因特性也是持续研究的主题.

结构式图片

上下游产品

thiazoline-2,4-dione 4-(4-pyridinyl)-6-quinolinecarbaldehyde 4-chloroquinoline-6-carbaldehyde 4-pyridylboronic acid

合成工艺路线路线简述

  • 2295-31-0 + 958852-13-6 = 958852-01-2
    反应条件:1.1 Reagents: Acetic Acid,Piperidine Solvents: Ethanol; 30 Min,150 °C; 150 °C -> Rt
    标题:Thiazolidinedione Derivatives As Pi3 Kinase Inhibitors And Their Preparation And Use In The Treatment Of Diseases
    参考文献:World Intellectual Property Organization]

    = 958852-01-2 [标题:Reaction Conditions
    标题:Discovery Of Gsk2126458,A Highly Potent Inhibitor Of Pi3K And The Mammalian Target Of Rapamycin
    作者:Knight,Steven D.; Adams,Nicholas D.; Burgess,Joelle L.; Chaudhari,Amita M.; Darcy,Michael G.; Et Al
    参考文献:Acs Medicinal Chemistry Letters 日期:2010 卷标:1(1) 页码:39-43
📜6-溴-4-氯喹啉置于四氧化锇,四(三苯基膦)钯 哌啶,2,6-二甲基吡啶,Sodium Periodate,水,Potassium Carbonate,溶剂黄146体系中,用 1,4-二氧六环,乙醇,水,N,N-二甲基甲酰胺,叔丁醇 作为反应溶剂,化学反应 9.0H,反应生成 Gsk 1059615; (5Z)-5-[[4-(4-吡啶基)-6-喹啉基]亚甲基]-2,4-噻唑烷二酮
参考文献:Wo2007/136940
标题:Wo2007/136940

海关参考信息

专利信息


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: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.

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:US-2023192681-A1
优先权日:2019-11-14
标 题 :Improved synthesis of kras g12c inhibitor compound

专利号:US-11299491-B2
优先权日:2018-11-16
标 题:Synthesis of key intermediate 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. Xie J, Li Q, Ding X, Gao Y. GSK1059615 kills head and neck squamous cell carcinoma cells possibly via activating mitochondrial programmed necrosis pathway. Oncotarget. 2017 Feb 7;8(31):50814-50823. doi: 10.18632/oncotarget.15135.

合成参考文献


参考文献:10.1007/s10555-009-9192-9
摘要:Dovedi SJ, Davies BR. Emerging targeted therapies for bladder cancer: a disease waiting for a drug. Cancer Metastasis Rev. 2009 Dec;28(3-4):355–67. doi: 10.1007/s10555-009-9192-9.
参考文献:10.1021/ml900028r
摘要:Knight SD, Adams ND, Burgess JL, Chaudhari AM, Darcy MG, Donatelli CA, Luengo JI, Newlander KA, Parrish CA, Ridgers LH, Sarpong MA, Schmidt SJ, Van Aller GS, Carson JD, Diamond MA, Elkins PA, Gardiner CM, Garver E, Gilbert SA, Gontarek RR, Jackson JR, Kershner KL, Luo L, Raha K, Sherk CS, Sung CM, Sutton D, Tummino PJ, Wegrzyn RJ, Auger KR, Dhanak D. Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin. ACS Med Chem Lett. 2010 Apr 08;1(1):39–43.
摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749
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