{5-[(Z)-2-Methyl-3-phenyl-prop-2-en-(E)-ylidene]-4-oxo-2-thioxo-thiazolidin-3-yl}-acetic acidepalrestaterhodanine 3-acetic acidα-methyl-trans-cinnamaldehyde{5-[(Z)-2-Methyl-3-phenyl-prop-2-en-(E)-ylidene]-4-oxo-2-thioxo-thiazolidin-3-yl}-acetic acidepalrestate5-[(1Z,2Z)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acidepalrestat 1-(2-hydroxyethyl)-pyrrolidine salt
合成工艺路线路线简述
5718-83-2 + 15174-47-7 = 82159-09-9 反应条件:1.1 Reagents: Piperidine Solvents: Dimethylformamide; 8 Min,100 °C1.2 Reagents: Hydrochloric Acid Solvents: Water; Acidified 标题:Development Of Efficient Manufacturing Process For Active Pharmaceutical Ingredient Epalrestat And Its Derivatives In Continuous Flow Synthesis 作者:Naramsetti,Kiran Kumar; Et Al 参考文献:Asian Journal Of Chemistry 日期:2023 卷标:35(1) 页码:233-238]
5718-83-2 + 768-49-0 = 82159-09-9 反应条件:1.1 Reagents: Acetic Acid,Sodium Acetate 标题:Development Of Epalrestat (Kinedak),Aldose Reductase Inhibitor 作者:Kawamura,Masanori; Et Al 参考文献:Yuki Gosei Kagaku Kyokaishi 日期:1997 卷标:55(7) 页码:651-657]
专利号:US-5847150-A 优先权日:1996-04-24 标题 :Solid phase and combinatorial synthesis of substituted 2-methylene-2, 3-dihydrothiazoles and of arrays of substituted 2-methylene-2, 3-dihydrothiazoles 发明人:DORWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS 摘要:A solid phase method for the synthesis of a plurality of differently substituted 2-methylenethiazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 2-methylenethiazoles are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide under acidic conditions yields differently substituted, support-bound 2-methylene-2,3-dihydrothiazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 2-methylenethiazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:US-10005720-B2 优先权日:2013-04-05 标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same 发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L 权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL 摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
专利号:US-9315483-B2 优先权日:2007-09-13 标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof 发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT 权利人:CONCERT PHARMACEUTICALS INC 摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.
专利号:US-2005004225-A1 优先权日:2003-04-16 标题:Oxidoreductase inhibitors and methods of screening and using thereof 发明人:BALENDIRAN GANESARATNAM K 摘要:The present invention relates to 1) the design and synthesis of analogs to glutathione conjugates which bind to or interact with aldose reductase (AR) through unique conformations that are distinctly different from the substrates and inhibitors of AR which are members of sugar metabolism; 2) the screening of the analogs to identify those that interact with or inhibit or enhance the activity of AR; and 3) the use of AR ligands, AR inhibitors (AR antagonsits) or AR enhancer (AR agonists) in the detection of AR activity, the modulation of AR activity, and the treatment of conditions in a subject in need of modulating AR activity. Such conditions include but not limited to cardiovascular disease, diabetes, artheriosclerosis, cancer, neoplasm, obesity, cataract, retinopathy, keratopathy, nephropathy, neurosis, thrombosis, faulty union of corneal injury and neuropathy. Examples of the treatment include the use of fibrates as AR inhibitors to treat these conditions.
专利号:US-2025223262-A1 优先权日:2022-03-31 标 题 :Synthesis of morphinans with reduced herg activity and mop binding 发明人:LAMMERT ECKHARD; SCHOLZ OKKA; OTTER SILKE; HEREBIAN DIRAN; HOFFMANN TORSTEN; SANZ MIGUEL ANGEL; KRAMP LAURENZ; LEVY LAURA MARIANA; HRISTEVA STANIMIRA 权利人:HEINRICH HEINE UNIV DUESSELDORF; DEUTSCHE DIABETES FORSCHUNGSGESELLSCHAFT E V; TAROS CHEMICALS GMBH & CO KG 摘要:The invention relates to morphinan-derivatives, processes for their preparation, medicaments containing them and the use of these morphinan-derivatives for the preparation of medicaments.
专利号:US-2018370905-A1 优先权日:2013-04-05 标题:Compounds Useful for the Treatment of Metabolic Disorders and Synthesis of the Same
1: Bailly C. Moving toward a new horizon for the aldose reductase inhibitor epalrestat to treat drug-resistant cancer. Eur J Pharmacol. 2022 Sep 15;931:175191. doi: 10.1016/j.ejphar.2022.175191. Epub 2022 Aug 11. 23(7):571-583. doi: 10.2174/1389200223666220810152633. 624:122033. doi: 10.1016/j.ijpharm.2022.122033. Epub 2022 Jul 20. 14(5):3172-3179. 5: Kulkarni UD, Kumari Kamalkishore M, Vittalrao AM, Kumar Siraganahalli Eshwaraiah P. Cognition enhancing abilities of vitamin D, epalrestat and their combination in diabetic rats with and without scopolamine induced amnesia. Cogn Neurodyn. 2022 Apr;16(2):483-495. doi: 10.1007/s11571-021-09718-6. Epub 2021 Sep 15.
合成参考文献
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