CAS: 143664-11-3; N-(4-(2-(6,7-Dimethoxy-3,4-Dihydroisoquinolin-2(1H)-yl)Ethyl)Phenyl)-5-Methoxy-9-Oxo-9,10-Dihydroacridine-4-Carboxamide

该化合物是一种化学化合物,主要因其作为P-gp(P-gp)和乳腺癌抗药性蛋白(BCRP)的强大抑制剂的作用而得到承认,被归类为小分子,并经常在药理学和药物开发方面进行研究,特别是因为它有可能通过防止各种治疗剂从细胞中抽取来来增加其生物利用率.Elacridar的特点是它能够跨越血液-脑屏障,从而在治疗...

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9,10-二氢-5-甲氧基-9-氧代-4-吖啶甲酸 4-Methoxy-9-Oxoacridan-5-Carboxylic Acid 88377-31-5

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    📜2-(4-硝基苯基)乙酰氯置于palladium On Activated Charcoal Lithium Aluminium Tetrahydride,氢气,碳酸氢钠,1-羟基苯并三唑一水物,N,N'-二环己基碳二亚胺体系中,用 四氢呋喃,乙醇,N,N-二甲基甲酰胺,丙酮 用作溶剂,25.0 °C,101.33 Kpa 条件下,反应 9.0H,反应生成依克立达
    参考文献:Synthesis And Activity Against Multidrug Resistance In Chinese Hamster Ovary Cells Of New Acridone-4-Carboxamides
    标题:Synthesis And Activity Against Multidrug Resistance In Chinese Hamster Ovary Cells Of New Acridone-4-Carboxamides
    摘要:A Number Of Tricyclic Carboxamides Have Been Synthesized And Tested To Evaluate Their Ability To Reverse Multidrug Resistance In The (Chc)-C-R/5 Cell Line. Among Them The Acridone Derivatives Were The Most Potent,A Key Feature Is The Presence Of A Dimethoxybenzyl Or Phenethylamine Cationic Site,Separated From The Tricyclic Lipophilic Part By A Carbamoylphenyl Chain. Optimization Led To Compounds 2 Orders Of Magnitude More Active Than The Prototype Inhibitors Verapamil And Amiodarone. On The Basis Of In Vitro And In Vivo Activities,9,10-Dihydro-5-Methoxy-9-Oxo-N-[4-[2-(1,2,3,4-Tetrahydro-6,7-Dimethoxyisoquinol-2-yl)Ethyl]Phenyl]-4-Acridinecarboxamide (84) Has Been Selected For Further Development.
    Doi:10.1021/jm00013A017

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    专利信息


    专利号:US-6248891-B1
    优先权日:1997-05-23
    标题:Synthesis of acridine derivative multidrug-resistant inhibitors
    发明人:SHARP MATTHEW JUDE; MADER CATHERINE J; STRACHAN CALUM
    权利人:GLAXO WELLCOME INC
    摘要:Synthesis of the MDRI of formula (I) from intermediates of acridone acid of formula (II) and aminophenethyl isoquinoline of formula (III), via steps including coupling and conversion to yield the MDRI of formula (I).

    专利号:US-2023002411-A1
    优先权日:2019-12-20
    标 题:Deuterated analogues of selenophenochromenes, synthesis thereof, and methods of using same agents
    发明人:ARSENJANS PAVELS
    权利人:LATVIAN INST ORGANIC SYNTHESIS
    摘要:The present invention relates to a novel cancer curing deuterated selenopheno [h] chromene derivatives, as well as methods of their manufacturing and use in different pharmaceutical compositions for the treatment of cancer by administration of such substances.

    专利号:US-2025241876-A1
    优先权日:2023-07-19
    标 题:Anti-tumor compounds and methods of use thereof and synthesis thereof
    发明人:QUAY STEVEN CARL
    权利人:ATOSSA THERAPEUTICS INC
    摘要:Described herein are pharmaceutical compounds and compositions and methods of making thereof. Methods of synthesis for the compounds are described herein. The compounds or compositions described herein may exhibit aromatase inhibition activity or estrogen receptor activity. The compounds and compositions described herein may be useful in the treatment of a condition in a subject.

    专利号:US-12304894-B2
    优先权日:2019-04-17
    标题 :Derivatives of adamantyl oxadiazoles and pharmaceutically acceptable solvates, hydrates and salts thereof, pharmaceutical composition comprising same, synthesis method, suitable for use as effective and selective inhibitors of the reductase activity of the enzyme 11-beta dehydrogenase type 1 (11β-HSD1)
    发明人:FARDELLA BELLO CARLOS ENRIQUE; LAGOS ARÉVALO CARLOS FERNANDO; VECCHIOLA CÃ?RDENAS ANDREA PAOLA; ALLENDE SANZANA FIDEL ALEJANDRO; DIETHELM VARELA BENJAMIN MANUEL; RECABARREN GAJARDO GONZALO IVAN; GONZÃ?LEZ CISTERNA PABLO MARCELO
    权利人:UNIV PONTIFICIA CATOLICA CHILE
    摘要:The present invention relates to compounds derived from adamantyl oxadiazoles and the pharmaceutically acceptable solvates, hydrates and salts of same. These compounds are suitable for use as effective and selective inhibitors of the reductase activity of the enzyme 11-beta dehydrogenase type 1 (11β-HSD1), as well as in the production of a drug for treating conditions and diseases such as high blood pressure, obesity, dyslipidaemia, type 2 diabetes, insulin resistance, glaucoma, metabolic syndrome, cognitive disorders, osteoporosis, immune disorders, depression and other conditions. Also provided is a pharmaceutical composition comprising the compounds and a method for preparing said composition.

    专利号:WO-9852923-A1
    优先权日:1997-05-23
    标题:Synthesis of acridine derivative multidrug-resistant inhibitors

    专利号:DE-69809733-T2
    优先权日:1997-05-23
    标 题:SYNTHESIS OF ACRIDINE DERIVATIVES AS INHIBITORS OF MULTIPLE MEDICINE RESISTANCE

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    合成参考文献


    参考文献:10.1124/dmd.30.5.479
    摘要:Savolainen J, Edwards JE, Morgan ME, McNamara PJ, Anderson BD. Effects of a P-glycoprotein inhibitor on brain and plasma concentrations of anti-human immunodeficiency virus drugs administered in combination in rats. Drug Metab Dispos. 2002 May;30(5):479–82. doi: 10.1124/dmd.30.5.479.
    摘要:Allen JD, Jackson SC, Schinkel AH. A mutation hot spot in the Bcrp1 (Abcg2) multidrug transporter in mouse cell lines selected for Doxorubicin resistance. Cancer Res. 2002 Apr 15;62(8):2294–9.
    参考文献:10.1007/s11095-006-0279-5
    摘要:Dirson G, Fernandez C, Hindlet P, Roux F, German-Fattal M, Gimenez F, Farinotti R. Efavirenz Does Not Interact with the ABCB1 Transporter at the Blood—Brain Barrier. Pharmaceutical Research. 2006 Jun 21;23(7):1525–32. doi: 10.1007/s11095-006-0279-5.
    参考文献:10.1016/j.ijpharm.2006.05.030
    摘要:Yao H, Chiou WL. The complexity of intestinal absorption and exsorption of digoxin in rats. International Journal of Pharmaceutics. 2006 Sep;322(1-2):79–86. doi: 10.1016/j.ijpharm.2006.05.030.
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