CAS: 1227158-85-1; 5-(1-((2-(4-Cyclopropylpiperazin-1-yl)Pyridin-4-yl)Methyl)-5-Methyl-1H-Pyrazol-3-yl)-3-(4-(Trifluoromethoxy)Phenyl)-1,2,4-Oxadiazole

该化合物是一个复杂的有机化合物,其特点是多循环结构以及各种功能组的存在.该物质具有环状丙基环的特点,有助于其独特的消毒和电子特性.分子还含有一种以其生物活动而闻名的管状细胞,以及一种可增强溶性和再活动性的状环.此外,三氟甲氧基化合物的存在表明有可能增加脂性及代谢稳定性.氧化二氮和丙烯成分往往与药用活动有关,因此对药用化学产生兴趣.

结构式图片

物理性质

MSDS等安全信息

上下游产品

[(1-Ethoxycyclopropyl)oxy]trimethylsilane 1-{4-[(5-methyl-3-{3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl}-1H-pyrazol-1-yl)-methyl]pyridin-2-yl}piperazine 2-Chloro-4-[(5-methyl-3-{3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl}-1H-pyrazol-1-yl)-methyl]pyridine1-cyclopropyl-4-{4-[(5-methyl-3-{3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl}-1H-pyrazol-1-yl)methyl]pyridin-2-yl}piperazine hydr°Chloride 1-cyclopropyl-4-{4-[(5-methyl-3-{3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl}-1H-pyrazol-1-yl)methyl]pyridin-2-yl}piperazine 4-sulfamoylbenzoate

合成工艺路线路线简述

  • 合成目标产物 Bay 87-2243 主要起始原料 (1-Ethoxycyclopropoxy)Trimethylsilane And Ethanamine, N-[(3,5-Dichlorophenyl)Methylene]-2,2-Diethoxy-
  • (文献来源)合成步骤主要原料 (1-Ethoxycyclopropoxy)Trimethylsilane 和 Ethanamine, N-[(3,5-Dichlorophenyl)Methylene]-2,2-Diethoxy-
📜2-Chloro-4-[(5-Methyl-3-{3-[4-(Trifluoromethoxy)Phenyl]-1,2,4-Oxadiazol-5-Yl}-1H-Pyrazol-1-yl)-Methyl]Pyridine置于溶剂黄146体系中,化学反应 17.17H,反应生成1-环丙基-4-[4-[[5-甲基-3-[3-[4-(三氟甲氧基)苯基]-1,2,4-恶二唑-5-基]-1H-吡唑-1-基]甲基]-2-吡啶基]哌嗪
参考文献:Heterocyclically Substituted Aryl Compounds As Hif Inhibitors
标题:Heterocyclically Substituted Aryl Compounds As Hif Inhibitors
摘要:本申请涉及具有杂环取代基的新型芳基化合物,其制备方法,它们用于治疗和/或预防疾病以及用于制备治疗和/或预防疾病的药物,特别是用于治疗和/或预防过度增殖和血管生成性疾病以及那些由于代谢适应缺氧状态而引起的疾病.这种治疗可以作为单独治疗进行,也可以与其他药物或进一步治疗措施结合使用.

海关参考信息

专利信息


专利号:US-11612610-B2
优先权日:2018-12-14
标题:Mito-magnolol compounds and methods of synthesis and use thereof
发明人：KALYANARAMAN BALARAMAN; ZIELONKA JACEK MICHAL; CHENG GANG; HARDY MICAEL JOËL; OUARI OLIVIER
权利人:MEDICAL COLLEGE WISCONSIN INC; AIX MARSEILLE UNIV; MEDICAL COLLEGE OF WISCONSIN INC
摘要:The present invention provides mito-magnolol compounds, pharmaceutical compositions thereof, and methods of using the mito-magnolol compounds in the treatment of cancer, especially anti-cancer therapy or kinase resistant cancers.

专利号:US-11897910-B2
优先权日:2015-06-11
标 题:Mito-honokiol compounds and methods of synthesis and use thereof
发明人：KALYANARAMAN BALARAMAN; ZIELONKA JACEK MICHAL; CHENG GANG; HARDY MICAEL J; OUARI OLIVIER; YOU MING
权利人:MEDICAL COLLEGE WISCONSIN INC; AIX MARSEILLE UNIV
摘要:The present invention provides mito-honokiol or mito-magnolol compounds, pharmaceutical compositions thereof, and methods of using the mito-honokiol or mito-magnolol compounds in the treatment of cancer.

专利号:US-2022211727-A1
优先权日:2018-12-14
标 题 :Mito-Magnolol Compounds and Methods of Synthesis and Use Thereof

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主要参考文献


1: Kurelac I, Cavina B, Sollazzo M, Miglietta S, Fornasa A, De Luise M, Iorio M, Lama E, Traversa D, Nasiri HR, Ghelli A, Musiani F, Porcelli AM, Iommarini L, Gasparre G. NDUFS3 knockout cancer cells and molecular docking reveal specificity and mode of action of anti-cancer respiratory complex I inhibitors. Open Biol. 2022 Nov;12(11):220198. doi: 10.1098/rsob.220198. Epub 2022 Nov 9.
2: Philip M, Karakka Kal AK, Mathew B, Subhahar MB, Karatt TK, Perwad Z. Metabolic study of hypoxia-inducible factor stabilizers BAY 87-2243, MK-8617, and PT-2385 in equine liver microsomes for doping control. Drug Test Anal. 2022 Oct;14(10):1703-1723. doi: 10.1002/dta.3348. Epub 2022 Jul 26.
12:906494. doi: 10.3389/fonc.2022.906494.

合成参考文献


参考文献:10.1021/acs.jmedchem.0c01013
摘要:Xu Y, Xue D, Bankhead A, Neamati N. Why All the Fuss about Oxidative Phosphorylation (OXPHOS) J. Med. Chem. 2020 Oct 26;63(23):14276–307. doi: 10.1021/acs.jmedchem.0c01013.
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