CAS: 850879-09-3; N-(Benzo[d][1,3]Dioxol-5-Ylmethyl)-4-(Benzofuro[3,2-D]Pyrimidin-4-yl)Piperazine-1-Carbothioamide

该化合物是一种针对多发性硬脉酶,包括c-Kit,PDGFR和FLT3的小型分子抑制剂,对突变形式,如c-Kit D816V进行更多的打击活动.主要调查了该物质在治疗由这些动脉驱动的癌症,特别是胃肠肿瘤和某些白血病方面的潜力.Amuvatinib的装置涉及破坏助长肿瘤扩散和生存的异常信号路径.其多目标抑制特征在克服单目标疗法所见的抗药性突变方面可能具有优势.临床早期和临床研究显示,如果与其他止血剂相结合,会产生协同效应.目前正在进行进一步的研究,以便在更广泛的肿瘤应用中评估其功效和安全性.

结构式图片

上下游产品

. 4-(Piperazin-1-yl)benzo[4,5]furo[3,2-d]pyrimidine N-benzo[1,3]dioxol-5-ylmethyl-thioformamide chloride

合成工艺路线路线简述

    . 4-(Piperazin-1-yl)Benzo[4,5]Furo[3,2-D]Pyrimidine置于. 4-(Piperazin-1-yl)Benzo[4,5]Furo[3,2-D]Pyrimidine体系中,用37的收率获得产物n-(1,3-苯并二氧戊环-5-基甲基)-4-苯并呋喃并[3,2-D]嘧啶-4-基-1-哌嗪硫代甲酰胺
    参考文献:Protein Kinase Inhibitors
    标题:Protein Kinase Inhibitors
    摘要:本发明揭示了具有在蛋白激酶介导的疾病和病症(如癌症)治疗中的用途的蛋白激酶抑制剂.本发明的化合物具有以下结构:包括立体异构体,前药和其药学上可接受的盐,其中a是从以下环基团中选择的环基团:其中r1,R2,R3,X,Z,L1,Cycl1,L2和cycl2如本文所定义.本发明还揭示了含有本发明化合物的组合物,以及与其使用相关的方法.

    海关参考信息

    专利信息


    专利号:US-2009076268-A1
    优先权日:2007-09-14
    标 题:Facile assembly of fused benzofuro-heterocycles
    发明人:FITZGERALD ANNE E; LIU JING; MANI NEELAKANDHA S
    权利人:FITZGERALD ANNE E; LIU JING; MANI NEELAKANDHA S
    摘要:This invention concerns the synthesis of polycyclic structural components of pharmacological compounds, including the synthesis of fused benzofuro-heterocycles, through selective palladium-catalyzed cross-coupling and intramolecular cyclization.

    专利号:WO-2025128098-A1
    优先权日:2023-12-13
    标 题 :Solid oral dosage forms, kits, and methods of using the same
    发明人:LI YING; LANGER ROBERT; TRAVERSO CARLO
    权利人:MASSACHUSETTS INST TECHNOLOGY; BRIGHAM & WOMENS HOSPITAL INC
    摘要:Provided herein are solid oral dosage forms, methods, and kits useful, e.g, for the extension of the residence time of active pharmaceutical agents in vivo by the synthesis of a polymer in situ in a subject. In particular, the solid oral dosage forms, methods, and kits disclosed herein are particularly useful for drugs that require more than once daily administration (e.g, drugs that have short half-lives).

    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-12180228-B2
    优先权日:2019-06-05
    标题:Compounds, conjugates, and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines and uses thereof
    发明人:MOVASSAGHI MOHAMMAD; OLSSON CHASE ROBERT; SCOTT TONY Z; CHEAH JAIME; PAYETTE JOSHUA NATHANIEL
    权利人:MASSACHUSETTS INST TECHNOLOGY
    摘要:The present disclosure provides, e.g., compounds, compositions, kits, methods of synthesis, and methods of use, involving epipolythiodiketopiperazines and polythiodiketopiperazines.

    专利号:US-2022411407-A1
    优先权日:2019-11-15
    标题:Aryl aminopyrimidines as dual mertk and tyro3 inhibitors and methods thereof
    发明人:WANG XIAODONG; ZHOU YUBAI; DING RANSHENG; KONG DEYU; FRYE STEPHEN
    权利人:UNIV NORTH CAROLINA CHAPEL HILL
    摘要:Aminopyrimidine containing compounds that inhibit both Mer tyrosine kinase (MerTK) activity and Tyro3 kinase activity are disclosed herein. Additionally disclosed are methods of synthesis and use of the aminopyrimidine containing compounds as anti-cancer agents, immunostimulatory and immunomodulatory agents, anti-platelet agents, anti-infective agents, and as adjunctive agents.
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    主要参考文献


    1: Marciano R, David HB, Akabayov B, Rotblat B. The Amuvatinib Derivative, N-(2H -1,3-Benzodioxol-5-yl)-4-{thieno[3,2-d]pyrimidin-4-yl}piperazine-1-carboxamide, Inhibits Mitochondria and Kills Tumor Cells under Glucose Starvation. Int J Mol Sci. 2020 Feb 4;21(3):1041. doi: 10.3390/ijms21031041.
    2: Huynh TTX, Pham TX, Lee GH, Lee JB, Lee SG, Tark D, Lim YS, Hwang SB. Amuvatinib Blocks SARS-CoV-2 Infection at the Entry Step of the Viral Life Cycle. Microbiol Spectr. 2023 Mar
    30:e0510522. doi: 10.1128/spectrum.05105-22. Epub ahead of print. 24(5):448-53. doi: 10.1097/CMR.0000000000000103.

    合成参考文献


    参考文献:10.1007/s10565-019-09483-7
    摘要:Lee CH, Decker AM, Cackowski FC, Taichman RS. Bone microenvironment signaling of cancer stem cells as a therapeutic target in metastatic prostate cancer. Cell Biology and Toxicology. 2019 Jun 27;36(2):115–30. doi: 10.1007/s10565-019-09483-7.
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