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-6362009-B1 优先权日:1997-11-21 标 题 :Solid phase synthesis of heterocycles 发明人:MUNOZ BENITO; CHEN CHIXU 权利人:MERCK & CO INC 摘要:Methods for solid phase and combinatorial synthesis using a resin activation/capture approach are provided. In particular, methods for the production of dihydropyridones, N-acyidihydropyridones, tetrahydropyridones, pyridines, aminopyridines, N-acyltetrahydropyridines and tetrahydropyridines compounds and libraries containing such compounds are provided. Methods for screening the libraries and compounds and pharmaceutical compositions containing compounds prepared by the methods are provided.
专利号:US-9440948-B2 优先权日:2010-09-03 标题:Nicotine compounds and analogs thereof, synthetic methods of making compounds, and methods of use 发明人:KEM WILLIAM READE; SOTI FERENC; ROUCHAUD ANNE; XING HONG; LINDSTROM JON; ANDRUD KRISTIN MARIE 权利人:KEM WILLIAM READE; SOTI FERENC; ROUCHAUD ANNE; XING HONG; LINDSTROM JON; ANDRUD KRISTIN MARIE; UNIV FLORIDA; UNIV PENNSYLVANIA 摘要:Embodiments of the present disclosure provide for compounds such as those shown in FIG. 1.1 (compounds A, B, C, and D), 2′substituted nicotine compounds, azetidine compounds, ether linked nicotine compounds (FIG. 1.2 , compounds E, F, G, and H), methods of synthesis of the compounds, methods of treatment of a condition using compounds A, B, C, D, 2′substituted nicotine compounds, azetidine compounds, or ether linked nicotine compounds, methods of selectively stimulating alpha7 nAChR and/or alpha4beta2 receptors, and the like.
专利号:WO-2023010317-A1 优先权日:2021-08-04 标 题:Method for producing maackiain by means of plant cell fermentation technology 发明人:CAI XIANNENG; Lin Liangli; QIU YUNTING; WU JIAJIA 权利人:HAINAN XINOPEN SOURCE MEDICAL TECH CO LTD 摘要:Disclosed is a method for inducing the production of maackiain by means of a Millettia suspension cell. By means of the method, in a scaled-up culture process of the Millettia suspension cell, by adding two or more of methyl jasmonate, phenylalanine and chitosan glutamate, the shortcomings of existing Millettia suspension culture remaining at a shake flask level, the cell yield being low, and large-scale culture not being able to be carried out are overcome; an optimized culture medium and addition process, both of which are the most optimal for promoting product synthesis, are obtained by means of screening; and the synthesis rate of Millettia maackiain is greatly improved.
专利号:WO-2022213262-A1 优先权日:2021-04-06 标题:Cytisine derivative, and synthesis method therefor, pharmaceutical composition thereof and use thereof 发明人:LIN CHENG-WEN; TSYPYSHEVA INNA; KIU YAN-TUNG; KOVAL'SKAYA ALENA; SAFIULLIN RUSTAM 权利人:LIN CHENG WEN 摘要:The present invention provides a cytisine derivative represented by formula (I), and a synthesis method therefor, a pharmaceutical composition thereof and a use thereof. The cytisine derivative has a structure as shown in formula (I). Symbols in formula (I) are as defined in the description. The cytisine derivative can inhibit the cytopathic effect and infectivity of a dengue virus, and is suitable for use as a drug for preventing and treating the dengue virus.
专利号:US-2005020616-A1 优先权日:2003-07-21 标 题 :Aryl fused azapolycyclic compounds 发明人:COE JOTHAM W; O'DONNELL CHRISTOPHER J 权利人:PFIZER 摘要:This invention is directed to compounds of the formula (I): n n nand their pharmaceutically acceptable salts, wherein R 1 , R 2 , R 3 and Z are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of neurological and psychological disorders.
1: Walker N, Howe C, Glover M, McRobbie H, Barnes J, Nosa V, Parag V, Bassett B, Bullen C. Cytisine versus nicotine for smoking cessation. N Engl J Med. 2014 Dec 18;371(25):2353-62. doi: 10.1056/NEJMoa1407764. doi: 10.1016/j.neuropharm.2015.03.019. Epub 2015 Mar 31. doi: 10.1002/dta.1707. Epub 2014 Sep 17. doi: 10.1038/npp.2013.216. Epub 2013 Aug 21. 5: Leaviss J, Sullivan W, Ren S, Everson-Hock E, Stevenson M, Stevens JW, Strong M, Cantrell A. What is the clinical effectiveness and cost-effectiveness of cytisine compared with varenicline for smoking cessation? A systematic review and economic evaluation. Health Technol Assess. 2014 May;18(33):1-120. doi: 10.3310/hta18330. Review. 6: Vakhitova YV, Farafontova EI, Zainullina LF, Vakhitov VA, Tsypysheva IP, Yunusov MS. [Search of (-)-Cytisine Derivatives as Potential Inhibitors of NF-κB and STAT1]. Bioorg Khim. 2015 May-Jun;41(3):336-45. Russian. doi: 10.1016/j.jmgm.2015.11.003. Epub 2015 Nov 12. doi: 10.1136/thoraxjnl-2012-203035. Epub 2013 Feb 12. Review. doi: 10.1056/NEJMc1500342. doi: 10.1016/j.pbb.2013.07.012. Epub 2013 Jul 20.
合成参考文献
参考文献:10.1177/1087057116635503 摘要:Voter AF, Manthei KA, Keck JL. A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. J Biomol Screen. 2016 Jul;21(6):626–33.