📜9-(Methyl 9(S)-(((Tert-Butyloxy)Carbonyl)Amino)-6-Cyano-5,6,7,8,9-Pentadeoxy-2,3-O-Isopropylidene-β-D-Ribo-Decafuranosyluronate)Adenine置于吡啶,Sodium Hydroxide,甲酸,双氧水,Potassium Carbonate,三乙胺,三氟乙酸,[双(三氟乙酰氧基)碘]苯体系中,用 甲醇,水,二甲基亚砜,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 6.02H,反应生成 西奈芬净 参考文献:Synthesis Of Sinefungin And Its C-6' Epimer 标题:Synthesis Of Sinefungin And Its C-6' Epimer 摘要: DOI:10.1021/ja00364A028
专利号:US-2005080260-A1 优先权日:2003-04-22 标 题 :Preparation of prodrugs for selective drug delivery 发明人:MILLS RANDELL L; WU GUO-ZHANG 摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.
专利号:US-11980630-B2 优先权日:2017-07-31 标 题 :Flex-nucleoside analogues, novel therapeutics against filoviruses and flaviviruses 发明人:RADTKE KATHERINE L 权利人:UNIV MARYLAND 摘要:The present invention is directed to compounds, methods and compositions for treating or preventing viral infections using nucleosides analogs. Specifically, the present invention provides for the design and synthesis of acyclic fleximer nucleoside analogues having increased flexibility and ability to alter their conformation structures to provide increased antiviral activity potential with the result of inhibiting flaviviruses, filoviruses and/or coronaviruses.
专利号:US-11766412-B2 优先权日:2016-09-29 标 题:Methods of treating or alleviating adenylosuccinatelyase (ADSL) deficiency using spermidine or a pharmaceutically acceptable salt of spermidine 发明人:PAN WUGUANG; ZHU WEI 权利人:GENEHEAL BIOTECHNOLOGY CO LTD 摘要:Provided are compounds reducing SAICAR accumulation, and applications. On the basis of existing protein structure data and small molecule structure data, calculations and analysis are performed using software to screen and obtain compounds capable of effectively interfering with PAICS activity, reducing SAICAR synthesis, and ultimately reducing SAICAR accumulation, in order to achieve the goal of treating or improving ADSL deficiency. A better effect in the treatment or improvement of ADSL deficiency is expected from the joint use of at least two of the described compounds.
专利号:WO-2009058800-A2 优先权日:2007-10-29 标题:Synthesis of nucleosides
专利号:US-6723321-B2 优先权日:1998-07-31 标题:Autoinducer synthase modulating compounds and uses thereof 发明人:GREENBERG E PETER; CRONAN JR JOHN E; PLAPP BRYCE V; PARSEK MATTHEW R 权利人:UNIV ILLINOIS; UNIV IOWA RES FOUND 摘要:Provided are compositions and methods useful for modulating the activity of autoinducer synthase catalysts. A method for identifing modulators of the autoinducer synthesis reaction is also provided. Such modulators are useful for controlling bacterial growth and can be used for therapeutic treatment of bacterial infections particularly in immunocompromised subjects. They are also useful in treating disease states associated with autoinducer synthesis and biofilm development.
专利号:EP-1834645-A1 优先权日:1998-07-31 标 题:Autoinducer synthase modulating compounds and uses therefor 发明人:CRONAN JOHN E JR; PLAPP BRYCE V; GREENBERG E PETER; PARSEK MATTHEW R 权利人:UNIV IOWA RES FOUND 摘要:Provided are compositions and methods useful for modulating the activity of autoinducer synthase catalysts. A method for identifying modulators of the autoinducers synthesis reaction is also provided. Such modulators are useful for controlling bacterial growth and can be used for therapeutic treatment of bacterial infections particularly in immunocompromised subjects. They are also useful in treating disease states associated with autoinducer synthesis and biofilm development.
1: Meshnick SR. Recent studies on inhibitors of macromolecular synthesis and function in trypanosomes. Pharmacol Ther. 1984;25(2):239-54. Review.
合成参考文献
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