CAS: 332012-40-5; 4-(((4-((4-Chlorophenyl)Amino)Furo[2,3-D]Pyridazin-7-yl)Oxy)Methyl)-N-Methylpicolinamide

该化合物是一种小分子抑制剂,主要以其在针对癌症细胞扩散和存活过程中涉及的特定强力抗体方面所发挥的作用而闻名,被归类为抗癌剂,特别侧重于抑制血管内皮生长因子受体(VeGFR)和血盘生长因子受体(PDGFR)的活动.这种双重抑制作用在肿瘤血管产生和生长过程中意义重大.Telatinib通常通过口服,并在各种临床试验中调查其治疗固体肿瘤的效果.该化合物的化学结构包括有助于其药理活动的职能组,并显示有机溶剂的溶性中等.其行动机制包括阻断促进肿瘤生长和转移的信号路径,使其成为肿瘤综合疗法的候选.与许多有针对性的疗法一样,副作用简介可能包括高血压和胃肠炎,因此需要在治疗期间进行仔细监测.

结构式图片

上下游产品

N-Methylformamide 4-(hydroxymethyl)-N-methylpyridine-2-carboxamide 4-chloroanilino-7-chlorofuro[2,3-d]pyridazine 4-chloro-7-[N-(4-chlorophenyl)amino]-[2,3-d]furopyridazine4-[({4-[(4-chlorophenyl)amino]furo[2,3-d]pyridazin-7-yl}oxy)methyl]-N-methyl-2-pyridinecarboxamide 4-methylbenzenesulfonate 4-[({4-[(4-chlorophenyl)amino]furan[2,3-d]pyridazin-7-yl}oxy)methyl]-N-methyl-2-pyridinecarboxamide methanesulfonate

合成工艺路线路线简述

    📜2-甲基氨基甲酰异烟酸乙酯置于氢氧化钾,Sodium Tetrahydroborate,18-冠醚-6体系中,用 乙醇,甲苯 用作溶剂,化学反应 18.0H,反应生成替拉替尼
    参考文献:Substituted Pyridines And Pyridazines With Angiogenesis Inhibiting Activity
    标题:Substituted Pyridines And Pyridazines With Angiogenesis Inhibiting Activity
    摘要:具有抑制血管生成活性的取代吡啶并呈现广义结构式的物质,其中包含a,B,D,E和l的环为苯或含氮杂环;基团x和y可以是多种定义的连接单元中的任意一种;R1和r2可以是定义独立取代基,或者一起可以是环定义的桥;环j可以是芳基,吡啶基或环烷基基团;G基团可以是多种定义的取代基之一.还公开了含有这些物质的药物组合物,以及使用这些物质治疗具有异常血管生成或高渗透性过程特征的哺乳动物的方法.

    海关参考信息

    专利信息


    专利号:US-2024400576-A1
    优先权日:2021-09-03
    标 题:Nitrogen-containing derivatives of salinomycin, synthesis and uses thereof
    发明人:RODRIGUEZ RAPHAËL; CZERWONKA DOMINIKA; ANTOSZCZAK MICHAL; HUCZYNSKI ADAM
    权利人:CENTRE NAT RECH SCIENT; INST CURIE; INST NAT SANTE RECH MED; ADAM MICKIEWICZ UNIV
    摘要:The present invention relates to nitrogen-containing derivatives of salinomycin having the formula (I), as well as pharmaceutically acceptable salt thereof, and synthesis and uses thereof, in particular for the treatment and/or prevention of cancer including for preventing cancer metastasis and/or for preventing cancer recurrence and/or for decreasing resistance to a chemotherapy in a subject.

    专利号:US-2025250280-A1
    优先权日:2021-09-03
    标 题 :Nitrogen-containing derivatives of narasin, synthesis and uses thereof
    发明人:RODRIGUEZ RAPHAËL; CAÑEQUE TATIANA; MÜLLER SEBASTIAN; ANTOSZCZAK MICHAL
    权利人:CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; INST CURIE
    摘要:The present invention relates to nitrogen-containing derivatives of narasin having the formula (I), as well as synthesis and uses thereof, in particular for the treatment and/or prevention of cancer. Also disclosed are medicaments including the nitrogen-containing derivatives of narasin, which include medicaments for preventing cancer metastasis and/or for preventing cancer recurrence and/or for decreasing resistance to a chemotherapy in a subject.

    专利号:US-9295731-B2
    优先权日:2013-04-01
    标题 :Cleavable drug conjugates, compositions thereof and methods of use
    发明人:NGUYEN MARK QUANG
    权利人:NGUYEN MARK QUANG
    摘要:Base-labile crosslinkers, base-labile conjugates comprising such crosslinkers, methods of their synthesis and use are disclosed.

    专利号:WO-2023031399-A1
    优先权日:2021-09-03
    标题 :Iron-activable nitrogen-containing derivatives of salinomycin and narasin, synthesis and use for the treatment of cancers

    专利号:WO-2023031402-A1
    优先权日:2021-09-03
    标 题 :Nitrogen-containing derivatives of salinomycin, synthesis and uses thereof

    专利号:WO-2023031362-A1
    优先权日:2021-09-03
    标题:Nitrogen-containing derivatives of narasin, synthesis and uses thereof

    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: Song Q, Wang P, Wu J, Lu M, Xia Q, Shi Y, Wang Z, Ma X, Zhao Q. Analysis of the role of CHPF in colorectal cancer tumorigenesis and immunotherapy based on bioinformatics and experiments. Discov Oncol. 2024 Sep 18;15(1):458. doi: 10.1007/s12672-024-01340-2.
    2: Ong SLM, Baelde HJ, van IJzendoorn DGP, Bovée JVMG, Szuhai K. Identification of stable housekeeping genes for induced pluripotent stem cells and -derived endothelial cells for drug testing. Sci Rep. 2022 Sep 28;12(1):16160. doi: 10.1038/s41598-022-20435-w.
    3: van IJzendoorn DGP, Sleijfer S, Gelderblom H, Eskens FALM, van Leenders GJLH, Szuhai K, Bovée JVMG. Telatinib Is an Effective Targeted Therapy for Pseudomyogenic Hemangioendothelioma. Clin Cancer Res. 2018 Jun 1;24(11):2678-2687. doi: 10.1158/1078-0432.CCR-17-3512. Epub 2018 Mar 6. 49(4):851-868. doi: 10.4143/crt.2016.176. Epub 2017 Jan 3.

    合成参考文献


    参考文献:10.1186/s13000-019-0846-9
    摘要:Sun Y, Wang J. Primary pseudomyogenic hemangioendothelioma of the vulva: a rare location for a rare entity. Diagnostic Pathology. 2019 Jun 26;14(1):66. doi: 10.1186/s13000-019-0846-9.
    参考文献:10.1158/1078-0432.ccr-07-5050
    摘要:Steeghs N, Gelderblom H, Roodt JO, Christensen O, Rajagopalan P, Hovens M, Putter H, Rabelink TJ, de Koning E. Hypertension and rarefaction during treatment with telatinib, a small molecule angiogenesis inhibitor. Clin Cancer Res. 2008 Jun 01;14(11):3470–6. doi: 10.1158/1078-0432.ccr-07-5050.
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