📜对甲氧基苯乙酸置于氯化亚砜,Sodium Azide体系中,用 甲苯 作为反应溶剂,化学反应 1.0H,反应生成 4-甲氧苄基异氰酸酯 参考文献:Synthesis,Selective Aldose Reductase Inhibitory Profile And Antihyperglycaemic Potential Of Certain Parabanic Acid Derivatives 标题:Synthesis,Selective Aldose Reductase Inhibitory Profile And Antihyperglycaemic Potential Of Certain Parabanic Acid Derivatives 摘要:描述了某些对二氨基甲酸衍生物1A-P的合成和醛糖还原酶抑制剖面.此外,研究了这些化合物的抗高血糖潜力.在这个系列中,最活跃的抑制剂是化合物1G,1P和10,它们在浓度为1 X 10−4时分别显示出36.6%,90%和91%的抑制活性.它们的ic50分别为2 X 10−6,7.5 X 10-8和5 X 10-8.化合物10表现出明显的抗高血糖效果. DOI:10.3797/scipharm.Aut-01-204
专利号:EP-3515880-B1 优先权日:2017-03-17 标题:Methods and compositions for synthesis of encoded libraries 发明人:LI JIN; MORGAN BARRY A; Wan jinqiao; DOU DENGFENG; LIU GUANSAI; CHANG YONG; CHEN QIUXIA; WANG XING; XU YANSHAN; HU DONGYAN; LIU JIAN; CHENG XUEMIN 权利人:HITGEN INC
专利号:EP-1836163-B1 优先权日:2004-12-23 标题 :Pyrrolidine derivatives for the treatment of a disease depending on the activity of renin 发明人:BREITENSTEIN WERNER; COTTENS SYLVAIN; EHRHARDT CLAUS; JACOBY EDGAR; LORTHIOIS EDWIGE LILIANE JEANNE; MAIBAUM JUERGEN KLAUS; OSTERMANN NILS; SELLNER HOLGER; SIMIC OLIVER 权利人:NOVARTIS AG 摘要:Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula I wherein the substituents are as described in the specification.
专利号:US-2020149034-A1 优先权日:2017-03-17 标题:Methods and Compositions for Synthesis of Encoded Libraries
专利号:US-6660832-B1 优先权日:1999-08-20 标题:Macrocyclic compounds and preparation methods thereof 发明人:JEFFERSON ELIZABETH; SWAYZE ERIC EDWARD 权利人:ISIS PHARMACEUTICALS INC 摘要:The present invention is directed to macrocyclic compounds of the formula (I)wherein Q, X, R1 and R5 are as defined herein. Compounds of the invention are useful for therapeutic and prophylactic treatment of bacterial infection in mammals. Solid phase synthetic procedures are provided effecting synthesis of the macrocyclic rings attached to a solid support.
专利号:CN-102627657-A 优先权日:2012-03-09 标 题:Synthesis of 3-(4-methoxy-benzyl)-1H-pyrimidine-2,4-dione derivatives