CAS: 1948229-21-7; 3-(5-Methylthiazol-2-yl)-5-(((R)-Tetrahydrofuran-3-yl)Oxy)-N-((R)-1-(2-(Trifluoromethyl)Pyrimidin-5-yl)Ethyl)Benzamide

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    专利信息


    专利号:EP-4630405-A1
    优先权日:2022-12-06
    标题 :Process for the synthesis of substituted tetrahydrofuran modulators of sodium channels

    专利号:WO-2024123815-A1
    优先权日:2022-12-06
    标 题:Process for the synthesis of substituted tetrahydrofuran modulators of sodium channels

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    主要参考文献


    1: Morice A, Smith JA, McGarvey L, Birring SS, Parker SM, Turner A, Hummel T, Gashaw I, Fels L, Klein S, Francke K, Friedrich C. Eliapixant (BAY 1817080), a P2X3 receptor antagonist, in refractory chronic cough: a randomised, placebo- controlled, crossover phase 2a study. Eur Respir J. 2021 Nov 18;58(5):2004240. doi: 10.1183/13993003.04240-2020.
    2: Davenport AJ, Neagoe I, Bräuer N, Koch M, Rotgeri A, Nagel J, Laux-Biehlmann A, Machet F, Coelho AM, Boyce S, Carty N, Gemkow MJ, Hess SD, Zollner TM, Fischer OM. Eliapixant is a selective P2X3 receptor antagonist for the treatment of disorders associated with hypersensitive nerve fibers. Sci Rep. 2021 Oct 6;11(1):19877. doi: 10.1038/s41598-021-99177-0.
    3: Klein S, Gashaw I, Baumann S, Chang X, Hummel T, Thuß U, Friedrich C. First- in-human study of eliapixant (BAY 1817080), a highly selective P2X3 receptor antagonist: Tolerability, safety and pharmacokinetics. Br J Clin Pharmacol. 2022 Oct;88(10):4552-4564. doi: 10.1111/bcp.15358. Epub 2022 May 22.

    合成参考文献


    参考文献:10.1183/13993003.04240-2020
    摘要:Morice A, Smith JA, McGarvey L, Birring SS, Parker SM, Turner A, Hummel T, Gashaw I, Fels L, Klein S, Francke K, Friedrich C. Eliapixant (BAY 1817080), a P2X3 receptor antagonist, in refractory chronic cough: a randomised, placebo-controlled, crossover phase 2a study. Eur Respir J. 2021 May 13;58(5):2004240. doi: 10.1183/13993003.04240-2020.
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