专利号:US-2005186197-A1 优先权日:2002-08-29 标 题:Peptide inhibitors of beta lactamases 发明人:PALZKILL TIMOTHY; HUANG WANZHI 摘要:Peptide inhibitors of β-lactamases have been identified by the synthesis of peptide arrays using synthesis SPOT technology. These peptide inhibitors of β-lactamase have activity against a broad spectrum of β-lactamases and are useful in a variety of applications.
专利号:US-8557979-B2 优先权日:2004-06-10 标题 :Carbapenem antibacterials with gram-negative activity and processes for their preparation 发明人:CHOI WOO-BAEG; KOWALIK EWA 权利人:CHOI WOO-BAEG; KOWALIK EWA; FOB SYNTHESIS INC 摘要:The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents.
专利号:US-10933051-B2 优先权日:2017-06-09 标 题 :Carbapenem compounds and compositions for the treatment of bacterial infections 发明人:CHOI WOO-BAEG; TOMIOKA TAKASHI; JOO HYUNG-YEUL; TRUONG PHONG; MIN BRIAN 权利人:FOB SYNTHESIS INC 摘要:The present invention provides carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections, including drug resistant or multiple-drug resistant bacterial infections, and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment.
专利号:WO-9964032-A1 优先权日:1998-06-08 标题 :Combinatorial synthesis of multibinding libraries 发明人:CHRISTENSEN BURTON G; GRIFFIN JOHN H; JENKINS THOMAS E; JUDICE J KEVIN 权利人:ADVANCED MEDICINE INC; CHRISTENSEN BURTON G; GRIFFIN JOHN H; JENKINS THOMAS E; JUDICE J KEVIN 摘要:Disclosed are methods for synthesizing large collections of diverse multimeric compounds as well as iterative processes for evaluating key molecular constraints imparting multibinding properties to multimeric compounds. Also disclosed are libraries of multimeric compounds which can be evaluated for imparting multibinding properties.
专利号:US-9693999-B2 优先权日:2011-01-26 标题:Small molecule RNase inhibitors and methods of use 发明人:DUNMAN PAUL M; OLSON PATRICK D; CHILDERS WAYNE 权利人:UNIV ROCHESTER; UNIV NEBRASKA; Temple University—Of the Commonwealth System of Higher Education 摘要:Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease. Also described herein are methods of identifying compounds for treating or preventing a microbial infection.
专利号:US-2009111737-A1 优先权日:1999-05-24 标题:Novel antibacterial agents 发明人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES 权利人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES 摘要:This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall. In particular the multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands hasn a ligand domain capable of binding to penicillin binding proteins, a transpeptidase enzyme, a substrate of a transpeptidase enzyme, a beta-lactamase enzyme, pencillinase enzyme, cephalosporinase enzyme, a transglycoslase enzyme, or a transglycosylase enzyme substrate; Preferably, the ligands are selected from the beta lactam or glycopeptide class of antibacterial agents.
Items 1-10 of 10 (Display the 10 citations in Bethesda (MD): National Library of Medicine (US); 2006–. Cefotetan. 2018 Oct 31. 32(6):679-682. doi: 10.1177/0897190018798198. Epub 2018 Sep 6. 155(5A):16-23. doi: 10.1016/s0002-9610(88)80207-1. 30(5):382-426. doi: 10.2165/00003495-198530050-00002. 81(3):186-8. doi: 10.1002/ajh.20459. 19(5):504-509. doi: 10.1089/sur.2017.296. Epub 2018 May 2. 21(1-2):101-7. doi: 10.1007/BF03256184. 26(4):248-58. doi: 10.2165/00003088-199426040-00002. 23(1):99-106. doi: 10.1093/jac/23.1.99. 19(4):388-396. doi: 10.1089/sur.2018.010. Epub 2018 Apr 24.
合成参考文献
参考文献:10.1007/s10350-005-0274-7 摘要:Kumar RR, Kim JT, Haukoos JS, Macias LH, Dixon MR, Stamos MJ, Konyalian VR. Factors Affecting the Successful Management of Intra-Abdominal Abscesses With Antibiotics and the Need for Percutaneous Drainage. Diseases of the Colon & Rectum. 2005 Dec 08;49(2):183–9. doi: 10.1007/s10350-005-0274-7.