CAS: 1029872-54-5; (1R)-1-(4-Hydroxy-3-{[(1R)-6-Methoxy-1-(4-Methoxybenzyl)-2-Methyl-1,2,3,4-Tetrahydro-7-Isoquinolinyl]Oxy}Benzyl)-6-Methoxy-2-Methy L-1,2,3,4-Tetrahydro-7-Isoquinolinol

该化合物是用于治疗BRAF变异型黑皮瘤的定向活性抑制剂,它有选择地抑制许多黑皮瘤病例中表现过量的变异BRAFV600E蛋白. Vemurafenib通过具体针对诱因路径,在降低肿瘤生长和提高患者存活率方面提供了重大优势,从而最大限度地减少与广谱抑制剂相关的副作用.

结构式图片

欧盟法规

C&L通报

合成工艺路线路线简述

    专利信息


    专利号:US-12221452-B2
    优先权日:2017-10-04
    标题:Synthesis of cantharidin
    发明人:DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R
    权利人:VERRICA PHARMACEUTICALS INC
    摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).

    专利号:US-9695169-B2
    优先权日:2012-05-31
    标 题:Synthesis of heterocyclic compounds
    发明人:IBRAHIM PRABHA N
    权利人:PLEXXIKON INC
    摘要:Provided herein are intermediates and processes useful for facile synthesis of biologically active molecules.

    专利号:US-2024400519-A1
    优先权日:2023-06-01
    标 题 :Crystal forms a, b, c, d, e, f and g of selumetinib sulfate and preparation methods thereof
    发明人:HSU YAO-LUNG; HSIEH KUANG-CHAN; CHENG HUI-WEN; Yang zong-han
    权利人:CHUNGHWA CHEMICAL SYNTHESIS & BIOTECH CO LTD
    摘要:The present invention relates to crystal forms of A, B, C, D, E, F and G of selumetinib sulfate and the preparation method thereof. The crystal forms A, B and F of selumetinib sulfate are obtained by adding 6-(4-Bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-vinyloxy-ethoxy)-amide (SEL-3) into an organic solvent; further, crystal form A of selumetinib sulfate can be as a raw material to prepare crystal forms C, D and E of selumetinib sulfate, and crystal form C of selumetinib sulfate can be as a raw material to prepare crystal form G of selumetinib sulfate.

    专利号:US-11649285-B2
    优先权日:2016-08-03
    标题 :Identification of VSIG3/VISTA as a novel immune checkpoint and use thereof for immunotherapy
    发明人:KALABOKIS VASSILIOS; WANG JINGHUA; WU GUOPING; BAZAN JOSE FERNANDO; VALLEY CHRISTOPHER CARLIN
    权利人:BIO TECHNE CORP
    摘要:The ligand for VISTA is identified (VSIG3) as well as the use of this ligand and receptor interaction in the identification or synthesis of a VSIG3 agonist or antagonist compounds, preferably antibodies, polypeptides and fusion proteins which agonize or antagonize the effects of VSIG3 and/or VISTA and/or the VSIG3/VISTA interaction. These antagonists may be used to suppress VSIG3/VISTA's suppressive effects on T cell immunity, and more particularly used in the treatment of cancer, or infectious disease. These agonist compounds may be used to potentiate or enhance VSIG3/VISTA's suppressive effects on T cell immunity and thereby suppress T cell immunity, such as in the treatment of autoimmunity, allergy or inflammatory conditions. Screening assays for identifying these agonists and antagonist compounds are also provided.

    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-2022118094-A1
    优先权日:2019-02-21
    标题:Synthesis of biomimetic cell wall structure
    发明人:WANG YONG; SHI PENG
    权利人:PENN STATE RES FOUND
    摘要:The present invention relates generally to methods of generating a biomimetic cell wall (BCW) on a target surface, compositions comprising the BCW, and methods of use of the compositions, including biomedical applications of the BCW coated compositions.
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    ✅ COA系统入驻 | 共享模式

    合成参考文献


    参考文献:10.1038/jid.2011.177
    摘要:Metzner T, Bedeir A, Held G, Peter-Vörösmarty B, Ghassemi S, Heinzle C, Spiegl-Kreinecker S, Marian B, Holzmann K, Grasl-Kraupp B, Pirker C, Micksche M, Berger W, Heffeter P, Grusch M. Fibroblast Growth Factor Receptors as Therapeutic Targets in Human Melanoma: Synergism with BRAF Inhibition. Journal of Investigative Dermatology. 2011 Oct;131(10):2087–95. doi: 10.1038/jid.2011.177.
    参考文献:10.1007/s00280-011-1703-z
    摘要:Eroglu Z, Kong KM, Jakowatz JG, Samlowski W, Fruehauf JP. Phase II clinical trial evaluating docetaxel, vinorelbine and GM-CSF in stage IV melanoma. Cancer Chemotherapy and Pharmacology. 2011 Jul 19;68(4):1081. doi: 10.1007/s00280-011-1703-z.
    参考文献:10.2165/11591380-000000000-00000
    摘要:Natarajan N, Telang S, Miller D, Chesney J. Novel immunotherapeutic agents and small molecule antagonists of signalling kinases for the treatment of metastatic melanoma. Drugs. 2011 Jul 09;71(10):1233–50. doi: 10.2165/11591380-000000000-00000.
    参考文献:10.1186/1479-5876-9-115
    摘要:Ascierto PA, Marincola FM. Combination therapy: the next opportunity and challenge of medicine. Journal of Translational Medicine. 2011 Jul 21;9(1):115. doi: 10.1186/1479-5876-9-115.
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