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-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:WO-2014097257-A1 优先权日:2012-12-21 标 题:A method of preparation of (1'r,3r,4r)-4-acetoxy-3-(1'-(tert-butyldimethylsilyloxy)ethyl)-2-azetidinone, a precursor for carbapenem antibiotics synthesis 发明人:GRZESZCZYK BARBARA; STECKO SEBASTIAN; FURMAN BARTÅ?OMIEJ; CHMIELEWSKI MAREK 权利人:INST CHEMII ORGANICZNEJ PAN 摘要:The subject of the present invention is a method of preparation of (1'R,3R,4R)-4-acetoxy-3-(1'- (tert-butyl-dimethylsilyloxy)ethyl)-2-azetidinone defined by the formula (1) which is a basic chiral building block in the synthesis of carbapenem antibiotics.
专利号:US-9663771-B2 优先权日:2013-01-18 标题 :Engineered biocatalysts useful for carbapenem synthesis 发明人:SUKUMARAN JOLY; SMITH DEREK; YANG HONG; YEO WAN LIN; MOORE JEFFREY C 权利人:CODEXIS INC 摘要:The present disclosure provides engineered pNB esterase polypeptides useful for the synthesis of the carbapenem antibiotic, imipenem. The disclosure also provides polynucleotides encoding the engineered pNB esterases, host cells capable of expressing the engineered pNB esterases, and methods of using the engineered pNB esterases in the production of imipenem.
专利号:US-6566525-B1 优先权日:1998-09-17 标 题:Preparation of N-substituted-hydroxycycloalkylamine derivatives 发明人:KIM SEONG JIN; KIM KEON IL; YANG KYOUNG YOUL 权利人:SAMSUNG FINE CHEMICALS CO LTD 摘要:A process for the preparation of N-substituted-hydroxycycloalkylamine derivatives, that are useful intermediates for the synthesis of various organic chemicals including pharmaceutical and agrochemical compounds, represented by formula (1), by reacting a 1,2-dihydroxalkyl alcohol, represented by the following formula (2), with a thionyl halide to produce an intermediate 1,2-cyclosulfinylalkyl halide represented by the following formula (3); and then cyclizing that intermediate with an amine compounds represented by the following formula (4).In the above structural formuli, * represents an asymmetric carbon atom; R1 is hydrogen or an amino-protecting group; m is an integer of 1-3; and X is halogen. The reactant compounds as well as the compounds made according to this invention have the following substitution pattern:n=1, R2=OH, R3=H and m=1; n=1, R2=H, R3=CH2OH and m=2;n=2, R2=OH, R3=H; and m=2; and n=2, R2=H, R3=CH2OH and m=3.
专利号:US-12221646-B2 优先权日:2013-07-04 标 题:Method for the rapid determination of susceptibility or resistance of bacteria to antibiotics 发明人:FERNÃ?NDEZ GARCÃ?A JOSÉ LUIS; GOSÃ?LVEZ BERENGUER JAIME; SANTISO BRANDARIZ REBECA; TAMAYO NOVAS MARIA; BOU ARÉVALO GERMÃ?N 权利人:ABM TECH LLC 摘要:A method of rapidly evaluating the susceptibility of a strain of bacteria to a cell wall synthesis inhibiting antibiotic based on an assessment of cell enlargement in response to doses of the cell wall synthesis inhibiting antibiotic which are correlated to breakpoints of bacterial susceptibility.
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