CAS: 1361030-48-9; N-(4-((6,7-Dimethoxyquinolin-4-yl)Oxy)-3-Fluorophenyl)-4-Ethoxy-1-(4-Fluoro-2-Methylphenyl)-1H-Pyrazole-3-Carboxamide

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    专利号:US-2024342244-A1
    优先权日:2021-07-28
    标 题:Isthmin Protein Therapeutics for the Treatment of Non-Alcoholic Fatty Liver Disease
    发明人:SVENSSON KATRIN JENNIFER; VOILQUIN LAETITIA
    权利人:UNIV LELAND STANFORD JUNIOR
    摘要:Compositions and methods are provided for the treatment of one or both of type 2 diabetes and fatty liver disease, e.g. non-alcoholic fatty liver disease (NAFLD) and nonalcoholic steatohepatitis (NASH). The adipokine Isthmin-1 (ISM1) protein increases adipose glucose uptake while suppressing hepatic lipid synthesis.

    专利号:US-2022411407-A1
    优先权日:2019-11-15
    标题:Aryl aminopyrimidines as dual mertk and tyro3 inhibitors and methods thereof
    发明人:WANG XIAODONG; ZHOU YUBAI; DING RANSHENG; KONG DEYU; FRYE STEPHEN
    权利人:UNIV NORTH CAROLINA CHAPEL HILL
    摘要:Aminopyrimidine containing compounds that inhibit both Mer tyrosine kinase (MerTK) activity and Tyro3 kinase activity are disclosed herein. Additionally disclosed are methods of synthesis and use of the aminopyrimidine containing compounds as anti-cancer agents, immunostimulatory and immunomodulatory agents, anti-platelet agents, anti-infective agents, and as adjunctive agents.

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    1: Paolino M, Choidas A, Wallner S, Pranjic B, Uribesalgo I, Loeser S, Jamieson AM, Langdon WY, Ikeda F, Fededa JP, Cronin SJ, Nitsch R, Schultz-Fademrecht C, Eickhoff J, Menninger S, Unger A, Torka R, Gruber T, Hinterleitner R, Baier G, Wolf D, Ullrich A, Klebl BM, Penninger JM. The E3 ligase Cbl-b and TAM receptors regulate cancer metastasis via natural killer cells. Nature. 2014 Mar 27;507(7493):508-12. doi: 10.1038/nature12998. Epub 2014 Feb 19.

    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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