专利号:US-4271172-A 优先权日:1979-06-25 标 题 :6-Amino-spiro[penam-2,4'-piperidine]-3-carboxylic acids, antibacterial compositions thereof and method of use thereof 发明人:RODRIGUEZ LUDOVIC; LECLERCQ JACQUES; YKMAN PIERRE; COSSEMENT ERIC 权利人:UCB SA 摘要:6-Amino-spiro[penam-2,4'-piperidine]-3-carboxylic acids, salts and esters thereof of the formula ##STR1## wherein R 1 is hydrogen, benzyl or an alkali metal or ammonium ion and R 2 is methyl, phenyl or benzyl and process for preparing the same. n These compounds are useful as intermediates in the synthesis of a new group of antibiotics having properties similar to penicillins, besides own antibiotic activity with a broad antibacterial spectrum. Therefore, they are useful as antibacterials agents and as therapeutic agents for humans and for animals in the treatment of infectious diseases caused by Gram-positive and Gram-negative bacteria.
专利号:US-4348264-A 优先权日:1980-05-14 标 题 :Photocatalyzed process for producing carbapenams and carbapen-2-ems 发明人:ROSATI ROBERT L 权利人:PFIZER 摘要:Carbapenam-3-carboxylic acids and carbapen-2-em-3-carboxylic acids substituted at the 1-position with an oxo, a hydroxy or an acetoxy group, variously substituted at the 2-position with such groups as methyl, acetoxymethyl, methanesulfonyloxy, alkoxy, alkylthio, aminoalkylthio or amidinoalkylthio and optionally substituted at the 6-position with a hydroxyalkyl group, an acetoxyalkyl group or a conventional penicillin side-chain, pharmaceutically-acceptable salts thereof and various esters thereof wherein the esterifying group is selectively removed in the laboratory, or hydrolyzed under physiological conditions. n These compounds are useful either systemically or topically in the treatment of diseases caused by susceptible microorganisms, as animal feed additives for promotion of growth, or in the preservation of biodegradable materials, or as intermediates to compounds having such antibacterial activity. n Key to the synthesis of these compounds is the light catalyzed rearrangement of 2-diazo-1-oxoceph-3-em-4-carboxylates to 1-oxocarbapen-2-em-3-carboxylates, a newly discovered reaction determined to be of general applicability.
专利号:US-4429128-A 优先权日:1981-02-09 标题 :Carbapenams and carbapen-2-ems and process therefor 发明人:ROSATI ROBERT L 权利人:PFIZER 摘要:Carbapenam-3-carboxylic acids and carbapen-2-em-3-carboxylic acids substituted at the 1-position with an oxo, a hydroxy or an acetoxy group, variously substituted at the 2-position with such groups as methyl, acetoxymethyl, methanesulfonyloxy, alkoxy, alkylthio, aminoalkylthio or amidinoalkylthio and optionally substituted at the 6-position with a hydroxyalkyl group, an acetoxyalkyl group or a conventional penicillin side-chain, pharmaceutically-acceptable salts thereof and various esters thereof wherein the esterifying group is selectively removed in the laboratory, or hydrolyzed under physiological conditions. n These compounds are useful either systemically or topically in the treatment of diseases caused by susceptible microorganisms, as animal feed additives for promotion of growth, or in the preservation of biodegradable materials, or as intermediates to compounds having such antibacterial activity. n Key to the synthesis of these compounds is the light catalyzed rearrangement of 2-diazo-1-oxoceph-3-em-4-carboxylates to 1-oxocarbapen-2-em-3-carboxylates, a newly discovered reaction determined to be of general applicability.
专利号:US-4137236-A 优先权日:1977-01-18 标 题:Amino-spiro[oxa(or thia)cycloalkane-penam]-carboxylic 发明人:RODRIGUEZ LUDOVIC; LECLERCA JACQUES; YKMAN PIERRE; COSSEMENT ERIC 权利人:UCB SA 摘要:Amino-spiro[oxa(or thia)cycloalkane-penam]-carboxylic acid, a salt or an ester thereof, of the formula ##STR1## wherein Z is a hydrogen or an alkali metal atom, or a group protecting the carboxylic function, X is a sulfur or oxygen atom, n is 1 or 2, m is 1 or 2, and process of preparing the same. n These compounds are useful as intermediates in the synthesis of a new group of antibiotics having properties similar to penicillins, besides own antibiotic activity with a broad antibacterial spectrum.
专利号:US-4091027-A 优先权日:1976-05-25 标 题 :6'-Amino-spiro(cycloalkane-1,2'-penam)-3'-carboxylic acids 发明人:RODRIGUEZ LUDOVIC; LECLERCQ JACQUES 权利人:UCB SA 摘要:6'-Amino-spiro[cycloalkane-1,2'-penam]-3'-carboxylic acids of the formula ##STR1## WHEREIN Z is a hydrogen or an alkali metal atom, or a protective group, and n a whole number of from 3 to 6, and process of preparing the same. n These compounds are useful as intermediates in the synthesis of a new group of antibiotics having properties similar to the penicillins.
专利号:US-3989685-A 优先权日:1972-06-29 标题 :Process for making a 2'-halopenicillin 发明人:TANIDA HIROSHI; TSUJI TERUJI 权利人:SHINOGI CO 摘要:A 2'-halopenicillin compound is prepared from a penicillin-1-oxide compound by the action of an acid halide in the presence of a base. The product on heating rearranges to a 3-halo-3-methylcepham compound which itself gives a 3-methyl-3-cephem compound on further heating. A 2'-halopenicillin compound gives a 3-methyl-3-cephem compound on heating. The 2'-halopenicillin compounds, 3-halo-3-methylcepham compound and 3-methyl-3-cephem compounds are antibacterials which are also useful as intermediates for the synthesis of other penicillins and cephalosporins.
参考文献:10.1074/jbc.ra119.010201 摘要:Clausse V, Tao D, Debnath S, Fang Y, Tagad HD, Wang Y, Sun H, LeClair CA, Mazur SJ, Lane K, Shi Z, Vasalatiy O, Eells R, Baker LK, Henderson MJ, Webb MR, Shen M, Hall MD, Appella E, Appella DH, Coussens NP. Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. Journal of Biological Chemistry. 2019 Nov;294(46):17654–68. doi: 10.1074/jbc.ra119.010201. 参考文献:10.1177/2472555219873068 摘要:Lee OW, Austin S, Gamma M, Cheff DM, Lee TD, Wilson KM, Johnson J, Travers J, Braisted JC, Guha R, Klumpp-Thomas C, Shen M, Hall MD. Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. SLAS Discov. 2020 Jan;25(1):9–20.