CAS: 1440964-89-5; 6-(1-Cyclopropyl-1H-Pyrazol-4-yl)-3-(Difluoro(6-Fluoro-2-Methyl-2H-Indazol-5-yl)Methyl)-[1,2,4]Triazolo[4,3-B]Pyridazine

结构式图片

合成工艺路线路线简述

    5-氟-2-甲基苯胺置于盐酸,甲烷磺酸,18-冠醚-6,丙二醇甲醚,水,碘,Potassium Acetate,过氧化脲素,铜,肼,亚硝酸异戊酯体系中,用 四氢呋喃,甲醇,乙醇,氯仿,二甲基亚砜,乙酸乙酯 用作溶剂,化学反应 75.0H,反应生成伯瑞替尼
    参考文献: Highly Selective C-Met Inhibitors As Anticancer Agents[fr] Inhibiteurs Hautement Sélectifs De C-Met Utilisés Comme Agents Anticancéreux
    标题: Highly Selective C-Met Inhibitors As Anticancer Agents[fr] Inhibiteurs Hautement Sélectifs De C-Met Utilisés Comme Agents Anticancéreux
    摘要:本文披露了新型含氮,杂环,C-Met抑制剂化合物,其制备方法和配方.这些化合物可用作治疗剂,用于抑制,调节和控制c-Met激酶信号通路,并用于治疗受c-Met介导的主体细胞增殖紊乱或疾病.

    海关参考信息

    专利信息


    专利号:US-12351573-B2
    优先权日:2019-05-09
    标 题:Compounds for use in synthesis of peptidomimetics
    发明人:AL-ABED YOUSEF; CHENG KAI FAN
    权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
    摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.

    专利号:US-2023159450-A1
    优先权日:2020-05-08
    标 题 :Dimers for use in synthesis of peptidomimetics
    发明人:AL-ABED YOUSEF; ALTITI AHMAD
    权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
    摘要:Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.

    专利号:US-2020354404-A1
    优先权日:2019-05-09
    标 题 :Peptidomimetic agents, synthesis and uses thereof
    发明人:AL-ABED YOUSEF
    权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
    摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.

    专利号:US-11440881-B2
    优先权日:2019-05-09
    标题 :Thiosemicarbazates and uses thereof
    发明人:AL-ABED YOUSEF; ALTITI AHMAD
    权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
    摘要:Thioesters, thiocarbamates, thiocarbazates, semithiocarbazates, peptides, aza-amino acid conjugates, and azapeptides; and a chemoselective and site-specific functionalization protocol of protected thiocarbazates and semithiocarbazates are described. The protocol features the use of Mitsunobu reaction to alkylate specifically the nitrogen atom close to the acylthiol moiety with alcohols to produce protected mono-substituted thiocarbazates that can be stored for months, activated under mild conditions at low temperature using halonium reagents and integrated orthogonally to make substituted semicarbazides that can be used, e.g., as synthons in synthesis of aza-amino acid conjugates, azapeptides and other peptidomimetics. Methods for preparing and using ureases, carbazides, semicarbazides, beta-peptides, azapeptides, and other peptidomimetics and azapeptide conjugates, and uses of ureases, carbazides, semicarbazides, beta-peptides, azapeptides in drug discovery, diagnosis, inhibition, prevention and treatment of diseases are also described.

    专利号:US-2022372022-A1
    优先权日:2019-05-09
    标 题:Compounds for use in synthesis of peptidomimetics

    专利号:US-10919882-B2
    优先权日:2019-05-09
    标题:Compounds for use in synthesis of peptidomimetics
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    主要参考文献


    1: Hu H, Mu Q, Bao Z, Chen Y, Liu Y, Chen J, Wang K, Wang Z, Nam Y, Jiang B, Sa JK, Cho HJ, Her NG, Zhang C, Zhao Z, Zhang Y, Zeng F, Wu F, Kang X, Liu Y, Qian Z, Wang Z, Huang R, Wang Q, Zhang W, Qiu X, Li W, Nam DH, Fan X, Wang J, Jiang T. Mutational Landscape of Secondary Glioblastoma Guides MET-Targeted Trial in Brain Tumor. Cell. 2018 Nov 29;175(6):1665-1678.e18. doi: 10.1016/j.cell.2018.09.038. Epub 2018 Oct 18. 9(10):e002451. doi: 10.1136/jitc-2021-002451.

    合成参考文献


    参考文献:10.1038/s42003-025-07490-5
    摘要:Lin H, Qu L, Wei H, Guo M, Chen X, Lin Q, Zhang H, Dai S, Chen Y. Characterization of Bozitinib as a potential therapeutic agent for MET-amplified gastric cancer. Commun Biol. 2025 Jan 28;8(1):134.
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