专利号:WO-2012047907-A9 优先权日:2010-10-04 标题 :Synthesis of c5-substituted tetracyclines, uses thereof, and intermediates thereto 发明人:MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN 权利人:HARVARD COLLEGE; MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN 摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for a wide variety of substituents at position 5 of the tetracycline ring system.
专利号:US-9688644-B2 优先权日:2009-04-30 标 题 :Synthesis of Tetracyclines and intermediates thereto 发明人:MYERS ANDREW G; KUMMER DAVID A; LI DERUN; HECKER EVAN; DION AMELIE; WRIGHT PETER M 权利人:HARVARD COLLEGE 摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.
专利号:US-11807883-B2 优先权日:2020-11-03 标 题:Polypeptide tag, highly soluble recombinant nitrilase and application thereof in synthesis of pharmaceutical chemicals 发明人:XUE YAPING; XIE DONG; XIONG NENG; ZHENG YUGUO 权利人:UNIV ZHEJIANG TECHNOLOGY 摘要:The present invention provides a polypeptide tag and its application in the synthesis of pharmaceutical chemicals, the recombinant nitrilase was obtained by connecting a polypeptide tag to the N-terminus of the amino acid sequence of the nitrilase; wherein amino acids at both ends of the polypeptide tag are uncharged glycine G, and the rest are a random combination of any one or more of glycine G, histidine H, glutamic acid E, aspartic acid D, lysine K and arginine R; The activity of the recombinant nitrilase in the preparation of 1-cyanocyclohexyl acetic acid is up to 3034.7 U/g dcw, the polypeptide tag significantly improves the soluble expression of nitrilase, and the whole cell catalyst hydrolyzes 1M substrate with the same concentration 30 minutes faster than the mother enzyme. The method provided by the present invention can also be used for the biocatalytic reaction of other pharmaceutical intermediates as the substrate catalyzed by the nitrilase, improving the activity of the whole cell catalyst in reaction, and also improving the solubility of other types of nitrilases and the activity of the corresponding whole cell catalysts.
专利号:US-2024308959-A1 优先权日:2021-06-29 标 题:Processes for the preparation of (s)-2-(4-chloro-2-methoxyphenyl)-2-((3 -methoxy-5-(m ethylsulfonyl)phenyl)amino)-1 -(1h-indol-3-yl)ethenone derivatives 发明人:WU KAI; OOST RIK; SCHWEITZER-CHAPUT BERTRAND; ERIKSSON CARL ARNE MAGNUS; COESEMANS ERWIN 权利人:JANSSEN PHARMACEUTICALS INC 摘要:The present invention relates to novel chiral synthesis of mono- or di-substituted indole compounds of formula (I) n n n n n n n n n n n n wherein: n R 1 is H, R 2 is F and R 3 is H or CH 3 , n R 1 is H, CH 3 or F, R 2 is OCH 3 and R 3 is H and n R 1 is H, R 2 is OCH 3 and R 3 is CH 3 , n R 1 is CH 3 , R 2 is F and R 3 is H, n R 1 is CF 3 or OCF 3 , R 2 is H and R 3 is H, n R 1 is OCF 3 , R 2 is OCH 3 and R 3 is H and n R 1 is OCF 3 , R 2 is H and R 3 is CH 3 .
专利号:US-2014349347-A1 优先权日:2011-12-15 标题:Synthesis of n-acetyl-d-neuraminic acid 发明人:SCHROVEN ANDREAS; DEKANY GYULA; VRASIDAS IONNIS 权利人:SCHROVEN ANDREAS; DEKANY GYULA; VRASIDAS IONNIS; GLYCOM AS 摘要:Method of making NANA from NAM, which may itself be made from fructose. The NAM is treated with pyruvic acid or a pyruvate in the presence of a NANA aldolase having at least 70% sequence similarity or homology to the amino acid sequence of SEQ. ID. NO. 1.
专利号:US-12031160-B2 优先权日:2018-12-28 标 题:Method for the production of glufosinate-ammonium 发明人:XUE YAPING; CHENG FENG; LI QINGHUA; ZHENG YUGUO; XU JIANMIAO 权利人:UNIV ZHEJIANG TECHNOLOGY 摘要:The present invention provides a glufosinate-ammonium dehydrogenase mutant and application in synthesis of L-glufosinate-ammonium thereof, the method uses 2-carbonyl-4-[(hydroxy)(methyl)phosphinoyl]-butyric acid or its salts as a substrate and the glufosinate-ammonium dehydrogenase or cells containing the glufosinate-ammonium dehydrogenase as a biocatalyst to carry out reductive amination, thereby obtaining L-glufosinate-ammonium. The method has features of high conversion rate of raw materials, high yield, easy separation and purification of the product, and high chiral purity; compared with other catalytic processes, the method in the present invention has features of relatively simple process and a conversion rate of raw materials up to 100%.
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