CAS: 182431-12-5; N-(2,2,2-Trifluoroethyl)-9-(4-(4-(4'-(Trifluoromethyl)-[1,1'-Biphenyl]-2-Ylcarboxamido)Piperidin-1-yl)Butyl)-9H-Fluorene-9-Carboxamide

该化合物是微粒三相转移蛋白的一个小分子抑制器,主要用作同性动物家庭超胆固醇症(HOFH)的辅助疗法,其作用是减少肝脏中极低密度脂蛋白(VLDL)的集合和分泌,从而降低低密度脂蛋白胆固醇(LDL-C)的血浆水平;Lomitapide是口服的,通常保留给HoFH的病人,他们对其他低脂疗法反应不力;其主要优点包括有针对性的MTP抑制剂,直接解决HOFH的基本病理学,及其在耐药性情况下大幅降低LDL-C水平的能力.由于潜在的肝中毒,其使用需要仔细监测肝脏功能.

结构式图片

上下游产品

9-{4-[4-({[4'-(Trifluoromethyl)Biphenyl-2-Yl]Carbonyl}Amino)Piperidin-1-Yl]Butyl}-9H-Fluorene-9-Carboxylic Acid
9-(4-Hydroxybutyl)-N-(2,2,2-Trifluoroethyl)-9H-Fluorene-9-Carboxamide
9-(4-溴丁基)-N-(2,2,2-三氟乙基)-9H-芴-9-甲酰胺 9-(4-Bromobutyl)-N-(2,2,2-Trifluoroethyl)-9H-Fluorene-9-Carboxamide 182438-98-8
9-(4-Bromo-Butyl)-9H-Fluorene-9-Carboxylic Acid Chloride 331767-53-4
Methyl 9-(4-Bromobutyl)-9H-Fluorene-9-Carboxylate
9-(4-Hydroxybutyl)-9H-Fluorene-9-Carboxilic Acid
9-(4-溴丁基)-9H-芴-9-羧酸 9-(4-Bromo-Butyl)-9H-Fluorene-9-Carboxylic Acid 182438-97-7
4-Trifluoromethylbiphenyl-2-Carboxylic Acid (1-Benzylpiperidin-4-yl)Amide 182439-40-3

合成工艺路线路线简述

    📜4-三氟甲基-联苯-2-甲酸置于20% Palladium Hydroxide-Activated Charcoal,Potassium Carbonate体系中,用 甲醇,乙醇,N,N-二甲基甲酰胺,乙腈,环己烯 用作溶剂,化学反应 26.5H,反应生成N-(2,2,2-三氟乙基)-9-(4-[4-[4'-(三氟甲基)[1,1'-联苯]-2-甲酰氨基]哌啶-1-基]丁基)-9H-芴-9-甲酰胺
    参考文献: Process For The Preparation Of Lomitapide[fr] Procédé De Préparation De Lomitapide
    标题: Process For The Preparation Of Lomitapide[fr] Procédé De Préparation De Lomitapide
    摘要:本发明涉及一种制备具有可接受杂质水平的高纯度洛米他派或其药用可接受盐的方法.

    海关参考信息

    专利信息


    专利号:US-7956214-B2
    优先权日:2001-11-02
    标题 :Process for the preparation of aniline-derived thyroid receptor ligands
    发明人:CHIDAMBARAM RAMAKRISHNAN; KANT JOYDEEP; WEAVER RAYMOND E; YU JURONG; GHOSH ARUN
    权利人:KAROBIO AB; BRISTOL MYERS SQUIBB CO
    摘要:Provided are processes for the synthesis of aniline derivatives, specifically certain aniline derivatives which have activity as thyroid receptor ligands.

    专利号:US-2015139987-A1
    优先权日:2013-11-20
    标 题 :Treatment of homozygous familial hypercholesterolemia
    发明人:MARTIN ROBERT L; MCWHERTER CHARLES A; O'MARA PATRICK J
    权利人:CYMABAY THERAPEUTICS INC
    摘要:Treatment of homozygous familial hypercholesterolemia by administration of (R)-2-(4-((2-ethoxy-3-(4-(trifluoromethyl)phenoxy)propyl)thio)-2-methylphenoxy)acetic acid or a salt thereof, optionally in combination with an MTP inhibitor, an apoB-100 synthesis inhibitor, or a PCSK9 inhibitor.

    专利号:US-2014315720-A1
    优先权日:2012-10-24
    标 题 :Polysaccharide ester microspheres and methods and articles relating thereto
    发明人:FALLON DENIS G; GARRETT THOMAS S; KIZER LAWTON E; ZAZZARA KAREN L; COMBS MICHAEL T; JOHNSON RICHARD K; DEHART GARY
    权利人:CELANESE ACETATE LLC
    摘要:A method for producing a polysaccharide ester microsphere may include forming a polysaccharide ester product from a polysaccharide synthesis, wherein the polysaccharide ester product comprises a polysaccharide ester and a solvent; diluting the polysaccharide ester product, thereby yielding a polysaccharide ester dope; and forming a plurality of polysaccharide ester microspheres from the polysaccharide ester dope. Suitable polysaccharides may include, but are not limited to, starch, cellulose, hemicellulose, algenates, chitosan, and any combination thereof. Esters thereof may be organic esters (e.g., acetate and the like), inorganic esters (e.g., sulfonates and the like), or combinations thereof. Further, the solids conent of the polysaccharide ester dope, in some instances, may be greater than about 16 wt %.

    专利号:US-9198917-B2
    优先权日:2012-12-11
    标题:Hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
    发明人:BRODNEY MICHAEL AARON; BECK ELIZABETH MARY; BUTLER CHRISTOPHER RYAN; DAVOREN JENNIFER ELIZABETH; O'NEILL BRIAN THOMAS
    权利人:PFIZER
    摘要:The present invention provides compounds of Formula I, and the tautomers thereof, and the pharmaceutically acceptable salts of the compounds and tautomers, wherein the compounds have the structure n nwherein the variables R 1 , R 2 , R 3 , R 4 and x are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 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: 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


    摘要:
    摘要:DHHS/FDA; Electronic Orange Book-Approved Drug Products with Therapeutic Equivalence Evaluations. Available from, as of March 6, 2015:
    摘要:Health Canada; Product Monograph for Juxtapid (Lomitapide (as Lomitapide Mesylate), Drug Identification Number (DIN): 02420341 p.5 (Date of Preparation: August 27, 2014). Available from, as of March 24, 2015:
    摘要:Health Canada; Product Monograph for Juxtapid (Lomitapide (as Lomitapide Mesylate), Drug Identification Number (DIN): 02420341 p.4-5 (Date of Preparation: August 27, 2014). Available from, as of March 24, 2015:
    摘要:https://cdn.caymanchem.com/cdn/msds/10009610m.pdf
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