📜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.
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.
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