专利号:US-11059835-B2 优先权日:2014-08-15 标 题 :Synthesis of cephalosporin compounds 发明人:WALLER DAVID; GAZDA GREGORY; MINDEN ZACHARY; BARTON LISA; LEIGH CLIFTON 权利人:MERCK SHARP & DOHME 摘要:Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising a palladium-catalyzed coupling reaction.
专利号:US-2023286915-A1 优先权日:2020-10-07 标 题 :Synthesis of pyrrole acid derivatives 发明人:WILKINSON ANDREW; COOPER LAN; ORR DAVID; FINLAYSON JONATHAN; BUNT ADAM; KIRKHAM JAMES; LYTH DAVID; BLADES KEVIN 权利人:INFEX THERAPEUTICS LTD 摘要:This invention relates to the synthesis of compounds that can be used to treat bacterial infections in combination with other antibacterial agents, and more specifically in combination with a class of antibacterial agents known as carbapenems. The compounds resulting from the novel methods of the present invention are enzyme inhibitors and more particularly are metallo-β-lactamase inhibitors.
专利号:US-2025009786-A1 优先权日:2021-09-30 标 题 :Automated synthesis of polymeric dual drugs 发明人:MATRAY TRACY; VANBRUNT MICHAEL; MCCUTCHEON JOHN MICHAEL 权利人:SONY GROUP CORP 摘要:Compounds useful as biologically active compounds with or without fluorescent or colored dyes are disclosed. In some embodiments, the compounds have the following structure (I): (I) or a stereoisomer, tautomer or salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, L1, L2, L3, L4, L5, L6, L7, L8, L9, L10, L11, M1, M2, M3, l, m, n, p, and q are as defined herein. Additional compound, methods of preparation, pharmaceutical compositions, and methods of treatment related to compounds of Structure (I) are also provided.
专利号:US-10941161-B2 优先权日:2014-08-15 标 题:Intermediates in the synthesis of cephalosporin compounds 发明人:MOSHOS KRISTOS ADRIAN; JURKAUSKAS VALDAS; FOGLIATO GIOVANNI; SCANU MANUEL; HWANG YOU SEOK 权利人:MERCK SHARP & DOHME 摘要:Described herein are crystalline forms of a compound of formula (III′), including toluene solvates of TATD-CLE, as well as processes for the preparation thereof and use thereof in the preparation of cephalosporin compounds such as ceftolozane.
专利号:US-11542279-B2 优先权日:2016-06-06 标 题:Solid forms of ceftolozane and processes for preparing 发明人:MALONEY KEVIN MATTHEW; SIROTA ERIC M; VARSOLONA RICHARD J; GAUTHIER JR DONALD R; REN HONG 权利人:MERCK SHARP & DOHME; MERCK SHARP & DOHME LLC 摘要:The instant invention is related to a novel solid form of ceftolozane sulfate (the DMAc solvate of ceftolozane sulfate (Form 3)), compositions comprising ceftolozane sulfate DMAc solvate (Form 3), synthesis of Form 3 and an improved crystallization process using Form 3 to prepare ceftolozane sulfate Form 2. Novel compositions also include ceftolozane sulfate solid Form 3 and/or other crystalline and amorphous solid forms of ceftolozane.
专利号:WO-2025027521-A1 优先权日:2023-08-01 标题 :An improved process for the preparation of avibactam and intermediate thereof 发明人:DHAVARIA SANDEEP; HANDA VISHAL; SHARMA SUNEEL KUMAR; MEHTA ANSHU KUMAR; SINGH ADITYA NARAYAN; ABUL AZIM; GUPTA NITIN; SINGH GOVIND; CABRI WALTER 权利人:FRESENIUS KABI ONCOLOGY LTD 摘要:The present invention relates to an improved process for the preparation of Avibactam or a pharmaceutically acceptable salt thereof, particularly the present invention relates to process for the preparation of a bridged ester intermediate of Formula I, wherein R1 is a hydroxy protecting group which is a key intermediate for Avibactam or a pharmaceutically acceptable salt thereof. The present invention also relates to the crystalline form of intermediates used for the synthesis of Avibactam or a pharmaceutically acceptable salt thereof. The invention also provides improved processes for the preparation of Avibactam or a pharmaceutically acceptable salt, using the bridged ester compound of formula I prepared by the process of the present invention.
1: Das S, Li J, Riccobene T, Carrothers TJ, Newell P, Melnick D, Critchley IA, Stone GG, Nichols WW. Dose Selection and Validation for Ceftazidime-Avibactam in Adults with Complicated Intra-abdominal Infections, Complicated Urinary Tract Infections, and Nosocomial Pneumonia. Antimicrob Agents Chemother. 2019 Mar 27;63(4). pii: e02187-18. doi: 10.1128/AAC.02187-18. Print 2019 Apr. Review. 2: Giri P, Patel H, Srinivas NR. Review of Clinical Pharmacokinetics of Avibactam, A Newly Approved non-β lactam β-lactamase Inhibitor Drug, In Combination Use With Ceftazidime. Drug Res (Stuttg). 2019 May;69(5):245-255. doi: 10.1055/a-0748-5548. Epub 2018 Oct 8. Review. doi: 10.1007/s40262-018-0705-y. Review. doi: 10.1016/j.ijantimicag.2018.07.004. Epub 2018 Aug 31. Review. Available from http://www.ncbi.nlm.nih.gov/books/NBK500953/ doi: 10.1007/s40265-018-0902-x. Review. pii: e02446-17. doi: 10.1128/AAC.02446-17. Print 2018 Jun. Review. 8: Sherry N, Howden B. Emerging Gram negative resistance to last-line antimicrobial agents fosfomycin, colistin and ceftazidime-avibactam - epidemiology, laboratory detection and treatment implications. Expert Rev Anti Infect Ther. 2018 Apr;16(4):289-306. doi: 10.1080/14787210.2018.1453807. Epub 2018 Mar 21. Review. doi: 10.2174/1573396314666180308150908. Review. doi: 10.1080/17425255.2018.1434142. Epub 2018 Jan 31. Review. doi: 10.1007/s15010-017-1096-y. Epub 2017 Nov 7. Review. Review. doi: 10.18433/J3X31R. Review. eCollection 2016. Review.
合成参考文献
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