专利号:WO-0032619-A1 优先权日:1998-11-30 标题:Methods and compositions for identification of inhibitors of ribosome assembly 发明人:DAMMEL CAROL S; WATSON JULIE C 权利人:RIBOGENE INC 摘要:The invention provides a means for identifying novel antibiotics by screening for compounds that inhibit bacterial ribosome assembly and ribosomal protein synthesis, which comprises the screening of test compounds to identify those that inhibit the activity of a bacterial ribosomal protein. The in vitro and in vivo assays detect (a) increased translation of a reporter mRNA that is normally repressed in the presence of a ribosomal protein, (b) increased growth in cells that over-express ribosomal protein, and (c) decreased binding of the ribosomal protein to its target RNA. The invention encompasses the (a) methods of screening and testing compounds by the above methods, (b) compounds that are identified in the assay which inhibit ribosome assembly and protein synthesis and (c) methods for treatment using said compounds.
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-6528631-B1 优先权日:1993-09-03 标题 :Oligonucleotide-folate conjugates 发明人:COOK PHILLIP DAN; MANOHARAN MUTHIAH; BHAT BALKRISHEN 权利人:ISIS PHARMACEUTICALS INC 摘要:Oligonucleotide-folate conjugates are described wherein folates are conjugated to one or more sites on an oligonucleotide including the 2′-, 3′-, 5′-, nucleobase and internucleotide linkage sites. The folate can be attached via the α- or γ-carboxylate, optionally through a linking group. Methods for the regiospecific synthesis of the conjugates are disclosed.
专利号:US-11135200-B2 优先权日:2014-12-20 标题:Antimicrobial drug synthesis and therapeutic compositions 发明人:GREGG JOHN MALCOLM HALL 权利人:GREGG JOHN MALCOLM HALL 摘要:This invention relates to the medical use of an antimicrobial agent, racemic Ornidazole, its (R) and (S) enantiomers, or pharmaceutically acceptable salts or esters thereof, and to methods of treatment which involve treating a subject with Ornidazole. The racemic (rac)-ornidazole, its enantiomers, or pharmaceutically acceptable salts or esters thereof, may be used in combination with other actives. The invention also relates to pharmaceutical formulations and compositions comprising (rac)-ornidazole, (R)-ornidazole, (S)-ornidazole, or pharmaceutically acceptable salts or esters thereof, and/or other actives as well as methods to stereoselectively manufacture the enantiomers.
专利号:US-9149445-B2 优先权日:2009-07-27 标 题:Inhibition of glycerol-3-phosphate acyltransferase (GPAT) and associated enzymes for treatment of viral infections 发明人:LIU SEAN; RABINOWITZ JOSHUA D; SHENK THOMAS 权利人:LIU SEAN; RABINOWITZ JOSHUA D; SHENK THOMAS; UNIV PRINCETON 摘要:A method of treating or preventing a viral infection in a mammal by administering a compound or pharmaceutically acceptable derivative thereof that inhibits a phosphatidic acid synthesis enzyme.
专利号:WO-2014017797-A1 优先权日:2012-07-25 标题:Novel method for preparing 1-oxacephalosporin derivative 发明人:LEE SANG GYUN; HA HONG JOO; CHU SO MI; AN JUNG GI 权利人:JE IL PHARMACEUTICAL CO LTD 摘要:The present invention relates to a novel method for preparing a 1-oxacephalosporin derivative, which is an intermediate for the synthesis of 1-oxacephalosporin which is useful as an antibacterial agent. The preparation method of the present invention uses a simple halogenating agent to show remarkable stability, have a simple reaction process, allow a reaction to be readily controlled, and reduce reaction time, and thus is very efficient and improves the production yield of 1-oxacephalosporin which is useful as an antibacterial agent.
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合成参考文献
参考文献:10.1128/aac.00259-11 摘要:Lee C, Liu J, Li C, Chien C, Tang Y, Su L. Spread of IS CR1 Elements Containing blaDHA-1 and Multiple Antimicrobial Resistance Genes Leading to Increase of Flomoxef Resistance in Extended-Spectrum-β-Lactamase-Producing Klebsiella pneumoniae. Antimicrob Agents Chemother. 2011 Sep;55(9):4058–63. doi: 10.1128/aac.00259-11.