CAS: 1333151-73-7; Kpt-185

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上下游产品

isopropyl propiolate 3-(3-methoxy-5-(trifluoromethyl)phenyl)-1H-1,2,4-triazole 3-methoxy-5-(trifluoromethyl)benzonitrile (Z)-3-(3-(3-methoxy-5-(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)acrylic acid (Z)-azetidin-3-yl 3-(3-(3-methoxy-5-(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)acrylate (Z)-1-(3,3-difluoroazetidin-1-yl)-3-(3-(3-methoxy-5-(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)prop-2-en-1-one

合成工艺路线路线简述

    📜3-甲氧基-5-三氟甲基苯甲腈置于sodium Hydrosulfide Hydrate,Magnesium(II) Chloride Hexahydrate,三乙胺体系中,用 乙醚,二氯甲烷,N,N-二甲基甲酰胺 用作溶剂,化学反应 16.5H,反应生成Kpt185抑制剂
    参考文献: Nuclear Transport Modulatiors And Uses Thereof[fr] Modulateurs De Transport Nucléaire Et Leurs Utilisations
    标题: Nuclear Transport Modulatiors And Uses Thereof[fr] Modulateurs De Transport Nucléaire Et Leurs Utilisations

    海关参考信息

    专利信息


    专利号:US-9550757-B2
    优先权日:2010-03-05
    标题:Nuclear transport modulators and uses thereof
    发明人:SHACHAM SHARON; KAUFFMAN MICHAEL; SANDANAYAKA VINCENT P; SHECHTER SHARON
    权利人:KARYOPHARM THERAPEUTICS INC
    摘要:The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic).

    专利号:US-9714226-B2
    优先权日:2011-07-29
    标题:Hydrazide containing nuclear transport modulators and uses thereof
    发明人:SANDANAYAKA VINCENT P; SHACHAM SHARON; MCCAULEY DILARA; SHECHTER SHARON
    权利人:KARYOPHARM THERAPEUTICS INC
    摘要:The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula I: n nor a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.

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    📌 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. Ranganathan, P., Yu, X., Na, C., et al. Preclinical activity of a novel CRM1 inhibitor in acute myeloid leukemia. Blood 120(9), 1765-1773 (2012). 2. Etchin, J., Sanda, T., Mansour, M.R., et al. KPT-330 inhibitor of CRM1 (XPO1)-mediated nuclear export has selective anti-leukaemic activity in preclinical models of T-cell acute lymphoblastic leukaemia and acute myeloid leukaemia. British Journal of Haematology 161(1), 117-127 (2013). 3. Wang, S., Han, X., Wang, J., et al. Antitumor effects of a novel chromosome region maintenance 1 (CRM1) inhibitor on non-small cell lung cancer cells in vitro and in mouse tumor xenografts. PLoS One 9(3), e89848 (2014).

    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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