CAS: 202914-84-9; N-(2,2,2-Trifluoroethyl)-9-(4-(4-(4'-(Trifluoromethyl)-[1,1'-Biphenyl]-2-Ylcarboxamido)Piperidin-1-yl)Butyl)-9H-Fluorene-9-Carboxamide Methanesulfonate

该化合物是一种主要用于治疗超脂性贫血的药物化合物,特别是用于家庭超胆固醇血清患者的药物,它作为抑制微生物三相转移蛋白质的抑制剂,在肝脏脂蛋白的组装和分泌中起着关键作用.Lomitapide通过抑制MTP,减少了极低密度脂蛋白质(VLDL)的生产,随后降低了血液中低密度脂蛋白胆固醇(LDL)的含量.该物质通常通过口服施用,其特点是以微量盐形式进行,这增加了其溶性性和生物利用率.Lomitapide mesylate因其潜在副作用而闻名,包括胃肠扰动和肝酶升高,因此在治疗期间必须定期监测肝功能.其化学结构包括有助于其药理活动的具体功能组安排.

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合成工艺路线路线简述

    📜4-三氟甲基-联苯-2-甲酸置于草酰氯,三乙胺体系中,用 二氯甲烷,乙酸乙酯 用作溶剂,化学反应 5.75H,反应生成甲磺酸洛美他派
    参考文献: Crystalline Polymorph Of N-(2,2,2-Trifluoroethyl-9-[4-[r4-R[[[i4'-(Trifluoromethyl) [ 1,1 '-Biphenyl]-2-Yl] Carbonyl] Amino]-1-Piperidinyl] Butyl]-9H-Fluorene-9-Carboxamide Methanesulfonate And Process For Preparation Thereof[fr] Polymorphe Cristallin De N-(2,2,2-Trifluoroéthyl-9-[4-[r4-R[[[i4'-(Trifluorométhyl)[ 1,1'-Biphényl]-2-Yl]Carbonyl]Amino]-1-Pipéridinyl]Butyl]-9H-Fluorène-9-Carboxamide Méthanesulfonate Et Procédé Pour Sa Préparation
    标题: Crystalline Polymorph Of N-(2,2,2-Trifluoroethyl-9-[4-[r4-R[[[i4'-(Trifluoromethyl) [ 1,1 '-Biphenyl]-2-Yl] Carbonyl] Amino]-1-Piperidinyl] Butyl]-9H-Fluorene-9-Carboxamide Methanesulfonate And Process For Preparation Thereof[fr] Polymorphe Cristallin De N-(2,2,2-Trifluoroéthyl-9-[4-[r4-R[[[i4'-(Trifluorométhyl)[ 1,1'-Biphényl]-2-Yl]Carbonyl]Amino]-1-Pipéridinyl]Butyl]-9H-Fluorène-9-Carboxamide Méthanesulfonate Et Procédé Pour Sa Préparation
    摘要:本发明涉及下式(Ia)所示的n-(2,2,2-三氟乙基)-9-[4-[4-[[(4'-三氟甲基)[1,1'-联苯基]-2-基]甲酰基]氨基]-1-哌啶基]丁基]-9H-芴-9-甲酰胺甲磺酸盐的结晶多态以及其制备方法.

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    主要参考文献


    1: Marbach JA, Thapa J, Goldenberg E, Duffy D. Pharmacogenetics in the Development of Lipid Lowering Medications: Lomitapide & Mipomersen in Clinical Practice. Del Med J. 2015 Aug;87(8):238-43. doi: 10.1016/j.jacl.2015.05.001. Epub 2015 May 14. doi: 10.1016/j.atherosclerosissup.2015.02.005. The lipid-lowering effects of lomitapide are unaffected by adjunctive apheresis in patients with homozygous familial hypercholesterolaemia - a post-hoc analysis of a Phase 3, single-arm, open-label trial. Atherosclerosis. 2015 Jun;240(2):408-14. doi: 10.1016/j.atherosclerosis.2015.03.014. Epub 2015 Mar 14.
    6: Goulooze SC, Cohen AF, Rissmann R. Lomitapide. Br J Clin Pharmacol. 2015 Aug;80(2):179-81. doi: 10.1111/bcp.12612. Epub 2015 Jul 2.
    7: Alonso R, Mata P, Alonso Y Gregorio M, de Andrés R. [Homozygous familial hypercholesterolemia. First case in Spain treated with lomitapide, an inhibitor of the synthesis of lipoproteins with apolipoprotein B]. Med Clin (Barc). 2015 Sep 7;145(5):229-30. doi: 10.1016/j.medcli.2014.11.002. Epub 2014 Dec 24. Spanish. doi: 10.1016/j.atherosclerosissup.2014.07.001. Review. doi: 10.1016/j.atherosclerosissup.2014.07.005. Review. doi: 10.1001/jamainternmed.2014.1528. doi: 10.1001/jamainternmed.2014.1538. Review. doi: 10.2146/ajhp130592. Review. doi: 10.1161/CIRCULATIONAHA.113.001292. Review. doi: 10.1001/jamainternmed.2013.13309. doi: 10.1097/JCN.0000000000000104. Review. doi: 10.1331/JAPhA.2013.13538. doi: 10.1111/anec.12103. Epub 2013 Sep 30.

    合成参考文献


    参考文献:10.1177/2168479017720248
    摘要:Kondo H, Saint-Raymond A, Yasuda N. What to Know About Medicines With New Active Ingredients Approved in FY 2016 / 2016 in Japan and EU: A Brief Comparison of New Medicines Approved in Japan and the EU in 2016. Ther Innov Regul Sci. 2018 Mar;52(2):214–9. doi: 10.1177/2168479017720248.
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