📜6-氨基青霉烷酸,2-苯氧基丁酸 反应生成 丙匹西林 参考文献:Derivatives Of 6-Aminopenicillanic Acid. I. Partially Synthetic Penicillins Prepared From α-Aryloxyalkanoic Acids 标题:Derivatives Of 6-Aminopenicillanic Acid. I. Partially Synthetic Penicillins Prepared From α-Aryloxyalkanoic Acids 摘要: DOI:10.1021/ja01500A036
专利号:US-4340672-A 优先权日:1979-09-19 标 题:Enzymatic synthesis of β-lactam antibacterials 发明人:KONDO EIJI; MITSUGI TAKASHI; FUJIWARA TAMIO; MUNEYUKI RYONOSUKE 权利人:SHIONOGI & CO 摘要:Penicillins and cephalosporins can be synthesized by the action of an acylase on a penicillin or cephalosporin nucleus amine as substrate and an ester (I) of the following formula as the acyl source: (I) (wherein RCO is an acyl group in penicillin or cephalosporin side chains; X is a hydrogen atom, lower alkyl group or hydroxy-lower alkyl group; Y is a hydrogen atom or a lower alkyl group; and n is a positive integer). The novel acyl source (I) is also disclosed.
专利号:EP-0024372-A1 优先权日:1979-08-03 标题:Derivatives of clavulanic acid, their preparation and pharmaceutical compositions containing them 发明人:DENERLEY PAUL MILLINGTON; EGLINGTON ALFRED JOHN; HARBRIDGE JOHN BARRY 权利人:BEECHAM GROUP PLC 摘要:The compounds of the formula (II):n and salts and esters thereof wherein the hydroxyl group occupies position 2 or 4 R 1 and R 2 may be the same or different and represent hydrogen, halogen, hydroxy, lower alkyl, cyclopentyl, cyclohexyl, lower alkoxy or R, and R 2 when an adjacent carbon atoms may together represent a 1,4-buta-1,3-dienylene group or a polymethylene group containing from 3 to 5 carbon atoms; have been found to be β-lactam antibiotics and synergists with penicillins and cephalosporins. Their preparation and use is described. The synthesis of intermediates useful in their preparation is also described.
专利号:US-2025002508-A1 优先权日:2020-05-05 标题 :Boronic acid derivatives and synthesis, polymorphic forms, and therapeutic uses thereof 发明人:HECKER SCOTT J; BOYER SERGE HENRI; BIO MATTHEW M; FANG YUANQING; GONZALES DE CASTRO ANGELA; LEFORT LAURENT; ZHU ZUOLIN; LINDER THOMAS 权利人:QPEX BIOPHARMA INC 摘要:Disclosed herein are antimicrobial compounds, polymorphic forms, compositions, pharmaceutical compositions, the method of use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents, for example, β-lactamase inhibitors (BLIs).
专利号:US-4452796-A 优先权日:1982-06-14 标题:6-Aminoalkylpenicillanic acid 1,1-dioxides as beta-lactamase inhibitors 发明人:BARTH WAYNE E 权利人:PFIZER 摘要:Beta-lactamase inhibitors which are 6-alpha- and 6-beta-(aminomethyl) and (1-aminoethyl)pencillanic acid 1,1-dioxides; pharmaceutically-acceptable salts thereof; conventional esters thereof which are hydrolyzable in vivo; bis-methanediol esters thereof; or mixed methanediol esters with said beta-lactamase inhibitors and sulbactam. Pharmaceutical compositions comprising said beta-lactamase inhibitors and a conventional beta-lactam antibiotic, used in the treatment of bacterial infections. Compounds useful as intermediates in the synthesis of said beta-lactamase inhibitors. Antibacterial mixed bis-methanediol esters of said aminoalkyl penicillanic acid 1,1-dioxides and ampicillin or amoxicillin, also used in the treatment of bacterial infections; and intermediates therefor.
专利号:US-9839642-B2 优先权日:2014-05-09 标 题:Beta-tetrazolyl-propionic acids as metallo-beta-lactamase inhibitors 发明人:TANG HAIFENG; YANG SHU-WEI; MANDAL MIHIR; SU JING; LI GUOQING; PAN WEIDONG; TANG HAIQUN; DEJESUS REYNALDA; PAN JIANPING; HAGMANN WILLIAM; DING FA-XIANG; XIAO LI; PASTERNAK ALEXANDER; HUANG YUHUA; DONG SHUZHI; YANG DEXI 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula I that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
专利号:US-9708336-B2 优先权日:2014-01-22 标题 :Metallo-beta-lactamase inhibitors 发明人:MANDAL MIHIR; TANG HAIFENG; XIAO LI; SU JING; LI GUOQING; YANG SHU-WEI; PAN WEIDONG; TANG HAIQUN; DEJESUS REYNALDA; HICKS JACQUELINE; LOMBARDO MATTHEW; CHU HONG; HAGMANN WILLIAM; PASTERNAK ALEX; GU XIN; JIANG JINLONG; DONG SHUZHI; DING FA-XIANG; LONDON CLARE; BISWAS DIPSHIKHA; YOUNG KATHERINE; HUNTER DAVID N; ZHAO ZHIQIANG; YANG DEXI 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664 参考文献:10.1007/s00063-004-1052-3 摘要:de With K, Bergner J, Bühner R, Dörje F, Gonnermann C, Haber M, Hartmann M, Rothe U, Strehl E, Steib-Bauert M, Kern WV. [Antibiotic Use at German University Hospitals (Project INTERUNI-II). Results for Medical Intensive Care, Hematology-Oncology, and Other Medical Service Areas]. Med Klin (Munich). 2004 Jul 15;99(7):347–54. doi: 10.1007/s00063-004-1052-3.