📜对三氟甲基苯酚置于lithium Hydroxide,四丁基氟化铵,Sodium Hydride体系中,用 四氢呋喃 作为反应溶剂,化学反应生成 司拉德帕 参考文献:Discovery Of Para-Alkylthiophenoxyacetic Acids As A Novel Series Of Potent And Selective Pparδ Agonists 标题:Discovery Of Para-Alkylthiophenoxyacetic Acids As A Novel Series Of Potent And Selective Pparδ Agonists 摘要:A Novel Series Of Potent And Selective Ppar Delta Agonists,Para-Alkylthiophenoxyacetic Acids,Was Identified. The Synthesis And Structure-Activity Relationships Are Described. (C) 2007 Elsevier Ltd. All Rights Reserved. DOI:10.1016/j.Bmcl.2007.05.007
专利号:US-11912647-B2 优先权日:2020-05-22 标 题:Diversity-oriented synthesis of N,N,O-trisubstituted hydroxylamines from alcohols and amines by N—O bond formation 发明人:CRICH DAVID; HETTIKANKANAMALAGE ASIRI; HILL JARVIS 权利人:UNIV GEORGIA 摘要:In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.
专利号:US-9908846-B2 优先权日:2014-02-21 标题:Composition, synthesis, and use of new arylsulfonyl isonitriles 发明人:FLEMING FRASER FERGUSSON; LUJAN MONTELONGO JESUS ARMANDO 权利人:DUQUESNE UNIV OF THE HOLY GHOST; UNIV HOLY GHOST DUQUESNE 摘要:This invention relates to novel isonitriles, including arylsulfonyl isonitriles, and methods for their synthesis. The isonitriles include a conjugated ring system. The structure is designed with the flexibility to have multiple substitution patterns. The isonitriles may be used in applications including, but not limited to, pharmaceutical compositions.
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-12358903-B2 优先权日:2016-06-13 标题 :FXR (NR1H4) modulating compounds 发明人:BLOMGREN PETER A; CURRIE KEVIN S; FARAND JULIE; GEGE CHRISTIAN; KROPF JEFFREY E; XU JIANJUN 权利人:GILEAD SCIENCES INC 摘要:The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
专利号:US-11739065-B2 优先权日:2016-06-13 标题 :FXR (NR1H4) modulating compounds 发明人:BLOMGREN PETER A; CURRIE KEVIN S; GEGE CHRISTIAN; KROPF JEFFREY E; XU JIANJUN 权利人:GILEAD SCIENCES INC 摘要:The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
专利号:CN-106045991-A 优先权日:2016-05-30 标题 :Application of chlorophyll as a photosensitizer in the synthesis of tetrahydroquinoline derivatives by visible light-catalyzed cyclization reaction
1: Vuppalanchi R, Kowdley KV. Editorial: The evolving paradigms and treatments for primary biliary cholangitis. Aliment Pharmacol Ther. 2024 Jan;59(2):280-281. doi: 10.1111/apt.17779. 59(2):186-200. doi: 10.1111/apt.17755. Epub 2023 Oct 30. 59(2):201-216. doi: 10.1111/apt.17762. Epub 2023 Oct 25. 12(8):1523. doi: 10.3390/antiox12081523. 7: Hirschfield GM, Shiffman ML, Gulamhusein A, Kowdley KV, Vierling JM, Levy C, Kremer AE, Zigmond E, Andreone P, Gordon SC, Bowlus CL, Lawitz EJ, Aspinall RJ, Pratt DS, Raikhelson K, Gonzalez-Huezo MS, Heneghan MA, Jeong SH, Ladrón de Guevara AL, Mayo MJ, Dalekos GN, Drenth JPH, Janczewska E, Leggett BA, Nevens F, Vargas V, Zuckerman E, Corpechot C, Fassio E, Hinrichsen H, Invernizzi P, Trivedi PJ, Forman L, Jones DEJ, Ryder SD, Swain MG, Steinberg A, Boudes PF, Choi YJ, McWherter CA; ENHANCE Study Group*. Seladelpar efficacy and safety at 3 months in patients with primary biliary cholangitis: ENHANCE, a phase 3, randomized, placebo-controlled study. Hepatology. 2023 Aug 1;78(2):397-415. doi: 10.1097/HEP.0000000000000395. Epub 2023 Apr 6. 8: Levy C, Manns M, Hirschfield G. New Treatment Paradigms in Primary Biliary Cholangitis. Clin Gastroenterol Hepatol. 2023 Jul;21(8):2076-2087. doi: 10.1016/j.cgh.2023.02.005. Epub 2023 Feb 19.
合成参考文献
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