CAS: 85-79-0; 2-Butoxy-N-(2-(Diethylamino)Ethyl)Quinoline-4-Carboxamide

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2-butoxy-quinoline-4-carboxylic acid amide 2-(n-butyloxy)-4-(n-butyloxycarbonyl)-quinoline N,N-diethylethylenediamine sodium butanolate

2-氯喹啉-4-甲酰氯置于sodium Hydride,三乙胺体系中,用 二氯甲烷 作为反应溶剂,化学反应 72.5H,反应生成 辛可卡因
参考文献:鉴定dibucaine衍生物作为新型有效肠病毒2C解旋酶抑制剂:体外,体内和联合治疗研究.
标题:鉴定dibucaine衍生物作为新型有效肠病毒2C解旋酶抑制剂:体外,体内和联合治疗研究.
摘要:肠病毒a71(ev-A71)是引起手足口病(hfmd)的人类病原体,严重威胁着婴幼儿的安全和生命.但是,没有获得许可的直接抗病毒药可以治愈手足口病.在这项研究中,开发了一系列喹啉甲酰胺类似物作为有效的肠病毒抑制剂,随后的系统结构活性关系(sar)研究表明,这些喹啉甲酰胺类似物表现出了非常好的治疗ev-A71感染的能力.如上所述,最有效的ev-A71抑制剂6I 在rd细胞中显示出非常好的抗ev-A71活性(ec 50 = 1.238μm).此外,化合物6I可以有效预防6 Mg / Kg剂量的病毒感染小鼠的死亡.当与依替丁(0.1 Mg / Kg)联合使用时,这种治疗可以完全预防病毒感染小鼠的临床症状和死亡.机制研究表明,化合物6I通过靶向2C解旋酶抑制ev-A71,从而阻碍rna重塑和代谢.综上所述,这些数据表明6I是一种有前途的ev-A71抑制剂,作为前导化合物值得进行广泛的临床前研究.
DOI:10.1016/j.Ejmech.2020.112310

专利信息

专利号:US-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人：BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

专利号:US-2004110228-A1
优先权日:2002-04-01
标 题:Combinatorial organic synthesis of unique biologically active compounds
发明人：MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M
摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.

专利号:US-4795828-A
优先权日:1983-01-03
标题 :Functionalized intermediate for the synthesis of alpha-functionalized derivatives and labeled conjugates of procaimamide and NAPA
发明人：BUCKLER ROBERT T; WARD FREDERICK E
权利人:MILES INC
摘要:Procainamide and N-acetylprocainamide (NAPA) immunogens, antibodies prepared therefrom, labeled conjugates, synthetic intermediates, and the use of such antibodies and labeled conjugates in immunoassays for determining the respective drugs. The immunogens comprise the drugs coupled at the alpha -position of the amide side chain to an immunogenic carrier material. The labeled conjugates and synthetic intermediates similarly are alpha -position derivatives of the drugs or precursors thereof. The antibodies and labeled conjugates are particularly useful in homogeneous nonradioisotopic immunoassays for measuring the respective drugs in biological fluids such as serum.

专利号:US-9327264-B2
优先权日:2011-01-31
标 题 :Containerless synthesis of amorphous and nanophase organic materials
发明人：BENMORE CHRIS J; WEBER JOHANN R
权利人:BENMORE CHRIS J; WEBER JOHANN R; UCHICAGO ARGONNE LLC
摘要:The invention provides a method for producing a mixture of amorphous compounds, the method comprising supplying a solution containing the compounds; and allowing at least a portion of the solvent of the solution to evaporate while preventing the solute of the solution from contacting a nucleation point. Also provided is a method for transforming solids to amorphous material, the method comprising heating the solids in an environment to form a melt, wherein the environment contains no nucleation points; and cooling the melt in the environment.

专利号:US-2015352230-A1
优先权日:2013-01-11
标 题:Synthesis and isolation of dendrimer based imaging systems
发明人：MULLEN DOUGLAS GURNETT; BAKER JR JAMES R; BANASZAK HOLL MARK M; HUANG BAOHUA; DOUGHERTY CASEY; BALL JACK
权利人:UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis and isolation of antibodies conjugated with modular dendrimer nanoparticles. In particular, the present invention is directed to antibodies conjugated with novel modular dendrimer nanoparticles having precise numbers of imaging agents, methods of synthesizing the same, compositions comprising such antibodies conjugated with such modular dendrimer nanoparticles, as well as systems and methods utilizing the conjugates (e.g., in imaging settings) (e.g., in diagnostic and/or therapeutic settings) (e.g., for the delivery of therapeutics, imaging, and/or targeting agents).

专利号:US-2012232225-A1
优先权日:2009-08-26
标 题:Synthesis and isolation of dendrimer systems
发明人：BAKER JR JAMES R; BANASZAK HOLL MARK M; MULLEN DOUGLAS GURNETT; ORR BRADFORD G; DESAI ANKUR; SANDER LEONARD M; WADDELL JACK NEEL
权利人:BAKER JR JAMES R; BANASZAK HOLL MARK M; MULLEN DOUGLAS GURNETT; ORR BRADFORD G; DESAI ANKUR; SANDER LEONARD M; WADDELL JACK NEEL; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis and isolation of dendrimer systems. In particular, the present invention is directed to novel dendrimer conjugates with defined and limited numbers of ligand conjugates and high levels of structural uniformity, methods of synthesizing the same, compositions comprising the conjugates, as well systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)).