CAS: 722544-51-6; 2-(5-((7-(3-(Ethyl(2-Hydroxyethyl)Amino)Propoxy)Quinazolin-4-yl)Amino)-1H-Pyrazol-3-yl)-N-(3-Fluorophenyl)Acetamide

该化合物是复杂的有机化合物,具有多功能结构,具有五氯苯基核心,具有以生物活动,特别是药用化学生物活动而闻名的双环化合物,存在一个丙诺尔环和各种替代物,包括乙基(2-羟乙基)氨基组和三氟苯基混合物,表明与生物目标可能发生相互作用,使其成为药物应用的候选体.该化合物的结构表明,它可能具有诸如有机溶剂溶解性,氢基合金组的氢联结潜力以及由于氨和氨基功能的存在而可能产生的再活动等特性,其具体特性,包括熔点,溶性以及生物活动等,需要实证性调查才能充分了解其在不同环境中的行为.

结构式图片

上下游产品

CAS号722544-46-9 2-(5-{[7-(3-chl... | CAS号110-73-6 乙基羟乙胺 | CAS号174891-10-2 (5-氨基-2H-吡唑-3-基)乙酸 | CAS号557770-89-5 7-(3-羟基-丙氧基)-3H... | CAS号557770-90-8 7-(3-氯丙氧基)-4-氯喹唑啉 | CAS号557770-91-9 [5-[7-(3-氯丙氧基)喹... | CAS号16499-57-3 7-氟-4-喹唑啉酮 | CAS号957881-03-7 3-[[7-[3-[乙基[2-...

合成工艺路线路线简述

    4-Amino-7-{3-[ethyl(2-Hydroxyethyl)Amino]Propoxy}Quinazoline置于四丁基硫酸氢铵,Sodium Hydroxide体系中,用 水 作为反应溶剂,化学反应生成 5-[[7-[3-[乙基(2-羟基乙基)氨基]丙氧基]-4-喹唑啉]氨基]-N-(3-氟苯基)-1H-吡唑-3-乙酰胺
    参考文献:巴拉塞替的制备方法
    标题:巴拉塞替的制备方法
    摘要:本发明公开了巴拉塞替的制备方法,所述巴拉塞替化学名称为2‑{5‑[(7‑{3‑[乙基(2‑羟基乙基)氨基]丙氧基}喹唑啉‑4‑基)氨基]‑1H‑吡唑‑3‑基}‑n‑(3‑氟苯基)乙酰胺,其化学式为c26H30Fn7O3;本发明制备工艺过程简洁,原料易得,经济环保,有利于实现工业化,可促进巴拉塞替原料药的经济技术发展,降低了反应生成成本,适于大批量生产.

    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: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

    专利号:EP-4396189-B1
    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
    发明人:RODRIGUEZ RAPHAËL; CAÑEQUE TATIANA; MÜLLER SEBASTIAN; ANTOSZCZAK MICHAL
    权利人:CENTRE NAT RECH SCIENT; INST CURIE; INST NAT SANTE RECH MED
    上海泽涵生物医药科技有限公司
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    主要参考文献


    1: Helfrich BA, Kim J, Gao D, Chan DC, Zhang Z, Tan AC, Bunn PA. Barasertib,(AZD1152)a small molecule Aurora B inhibitor, inhibits the growth of SCLC cell lines in vitro and in vivo. Mol Cancer Ther. 2016 Aug 5. pii: molcanther.0298.2016. [Epub ahead of print] doi: 10.1002/jlcr.3376. doi: 10.1007/s00277-016-2670-6. Epub 2016 Apr 19. doi: 10.1007/s12035-015-9139-9. Epub 2015 Mar 11. doi: 10.1111/bjh.13333. Epub 2015 Feb 26. doi: 10.1007/s13277-014-2664-8. Epub 2014 Oct 3. doi: 10.1016/j.clml.2013.03.019. Epub 2013 Jun 10.
    8: Kantarjian HM, Martinelli G, Jabbour EJ, Quintás-Cardama A, Ando K, Bay JO, Wei A, Gröpper S, Papayannidis C, Owen K, Pike L, Schmitt N, Stockman PK, Giagounidis A; SPARK-AML1 Investigators. Stage I of a phase 2 study assessing the efficacy, safety, and tolerability of barasertib (AZD1152) versus low-dose cytosine arabinoside in elderly patients with acute myeloid leukemia. Cancer. 2013 Jul 15;119(14):2611-9. doi: 10.1002/cncr.28113. Epub 2013 Apr 19.
    9: Ma YX, Li XZ. [Effect of aurora kinase B inhibitor AZD1152 in the treatment of cisplatin-resistant ovarian carcinoma]. Zhonghua Fu Chan Ke Za Zhi. 2013 Jan;48(1):46-50. Chinese. doi: 10.1007/s00404-013-2719-x. Epub 2013 Feb 7. doi: 10.1007/s00280-012-1939-2. Epub 2012 Aug 4.

    合成参考文献


    参考文献:10.1124/mol.119.115964
    摘要:Lee TD, Lee OW, Brimacombe KR, Chen L, Guha R, Lusvarghi S, Tebase BG, Klumpp-Thomas C, Robey RW, Ambudkar SV, Shen M, Gottesman MM, Hall MD. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular Pharmacology. 2019 Nov;96(5):629–40. doi: 10.1124/mol.119.115964.
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