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25 条记录 (耗时 0.02 秒)

    Process for penicillin epimerization
    2.
    发明公开
    Process for penicillin epimerization 失效
    哌嗪类化合物的方法

    公开(公告)号：EP0037729A3

    公开(公告)日：1981-12-30

    申请号：EP81301479

    申请日：1981-04-06

    申请人： ELI LILLY AND COMPANY

    发明人： Blaszczak, Larry Chris

    IPC分类号： C07D499/04

    CPC分类号： C07D499/00 ,  Y02P20/55

    摘要： There is described a process for the preparation of a compound of the formula I A process for the preparation of a compound of the formula I
    which comprises reacting at least about 0.1 mole of triethylamine and at least about 0.1 mole of chlorotrimethylsilane per mole of 6β-acylaminopenicillin- 1β-sulfoxide compound of the following formula (II)
    in a substantially anhydrous ether or hydrocarbon solvent, in which solvent the above 6β-acyhaminopenicillin-1β-sulfoxide (II) is present in a concentration of about 0.7 molar or greater, in a substantially anhydrous atmosphere at a temperature between about -20°C and about 20°C where in the above formulas R 1 is hydrogen or an acyl group derived from a carboxylic acid; and R 2 is an acyl group derived from a carboxylic acid; or R 1 and R 2 taken together with the nitrogen atom to which they are attached form a group of the formula wherein R 4 is the residue of an acyl group derived from a dicarboxylic acid; and R 3 is hydrogen or a conventional carboxylic acid protecting group.

    Halogenating compounds and a process for their production
    3.
    发明公开
    Halogenating compounds and a process for their production 失效
    Halogenisier-Verbindungen und Verfahren zu ihrer Herstellung。

    公开(公告)号：EP0015079A1

    公开(公告)日：1980-09-03

    申请号：EP80300282.3

    申请日：1980-01-31

    申请人： ELI LILLY AND COMPANY

    发明人： Hatfield, Lowell Deloss ,  Blaszczak, Larry Chris ,  Fisher, Jack Wayne

    IPC分类号： C07F9/14 ,  C07F9/12

    CPC分类号： C07F9/145 ,  C07F9/062

    摘要： A halogenating compound is described of the general formula
    which is the kinetically controlled product of the reaction of equivalent amounts of a triaryl phosphite of the formula
    and chlorine or bromine in a substantially anhydrous inert organic solvent wherein in the above formulas Z is hydrogen, halo, C 1 -C 4 alkyl or C 1 -C 4 alkoxy, and X is Cl or Br.

    摘要翻译： 卤化化合物描述为通式... ...，其是在基本上无水的惰性有机溶剂中等当量的式... ... CHCl 3与亚甲基亚磷酸酯和氯或溴的反应的动力学控制产物，其中 在上式中，Z是氢，卤素，C 1 -C 4烷基或C 1 -C 4烷氧基，X是Cl或Br。

    Penicllin binding protein 2A from staphylococcus aureus strain 27R and derivatives for use in purification therefor and assay for compounds effective against methicillin resistant organisms
    4.
    发明公开
    Penicllin binding protein 2A from staphylococcus aureus strain 27R and derivatives for use in purification therefor and assay for compounds effective against methicillin resistant organisms 失效
    青霉素的衍生物从金黄色葡萄球菌菌株27R结合蛋白2A用于其纯化并测定耐甲氧西林的微生物有效化合物的

    公开(公告)号：EP0875578A2

    公开(公告)日：1998-11-04

    申请号：EP98200530.8

    申请日：1992-03-18

    申请人： ELI LILLY AND COMPANY

    发明人： Blaszczak, Larry Chris ,  Skatrud, Paul Luther ,  Smith, Michele Ceceil ,  Wu, Chyun-Yey Earnest

    IPC分类号： C12N15/57 ,  C12N9/52 ,  C12N15/62 ,  C07K19/00

    CPC分类号： C12N9/52 ,  C07K14/31 ,  C07K2319/00 ,  C07K2319/02 ,  C12N15/625

    摘要： The invention provides a gene encoding a novel PBP2A penicillin binding protein isolated from the methicillin resistant S . aureus strain 27R. The invention further provides soluble forms of PBP2A proteins lacking the transmembrane association region yet retain their active site configuration of the PBP2A protein. The invention also provides a method of assaying for agents useful against methicillin resistant staphylococcus strains by creating a kinetically inert complex between a support-immobilized transition metal ion and a modified soluble form of the PBP2A protein incorporating a chelating agent. The invention further provides a cell free method of assaying for agents which bind the PBP2A-27R protein.

    摘要翻译： 本发明提供了编码来自耐甲氧西林金黄色葡萄球菌菌株27R分离的新颖的PBP2a青霉素结合蛋白的基因。 本发明提供了缺乏跨膜区的关联，但仍保留了蛋白质的PBP2a的其活性位点结构的PBP2a蛋白的进一步可溶形式。 因此本发明提供测定针对通过创建一个支撑固定化的过渡金属离子和蛋白质的PBP2a掺入的螯合剂修饰的可溶性形式之间的动力学惰性的复杂耐甲氧西林葡萄球菌菌株有用的试剂的方法。 本发明还提供测定用于结合所述的PBP2a-27R蛋白质剂的无细胞方法。

    Processes for preparation of beta-lactam compounds
    6.
    发明公开
    Processes for preparation of beta-lactam compounds 失效
    Verfahren zur Herstellung von Beta-Lactam-Verbindungen。

    公开(公告)号：EP0014567A1

    公开(公告)日：1980-08-20

    申请号：EP80300284.9

    申请日：1980-01-31

    申请人： ELI LILLY AND COMPANY

    发明人： Hatfield, Lowell Deloss ,  Blaszczak, Larry Chris ,  Fisher, Jack Wayne ,  Bunnell, Charles Arthur

    IPC分类号： C07D501/02 ,  C07D501/59 ,  C07D501/16 ,  C07D501/18 ,  C07D499/04 ,  C07D498/04

    CPC分类号： C07D513/04 ,  C07D499/00 ,  C07D505/00

    摘要： Kinetically controlled triaryl phosphite halogen compounds of the formula
    wherein X is Cl or Br, and Z is hydrogen, halo, C 1 -C 4 alkyl or C 1 -C 4 alkoxy, are used to effect

    a) halogenation of a C-6 or C-7 acylamine penicillin or cephalosporin,
    b) halogenation of a 3-hydroxy-3-cephem,
    c) one step halogenation of a C-7 acylamine-3-hydroxy- cephem
    d) reduction of a cephalosporin sulfoxide
    e) one step reduction/halogenation of a 3-hydroxy cephalosporin sulfoxide
    f) one step reduction/halogenation of a C-7 acylamine cephalosporin sulfoxide
    g) one step reduction/halogenation of a C-7 acylamino-3-hydroxy cephalosporin sulfoxide.

    摘要翻译： 其中X为Cl或Br，Z为氢，卤素，C 1 -C 4烷基或C 1 -C 4烷氧基的式（CHEM）的动力学受控的三芳基亚磷酸酯卤化物用于实现a）C-6或C的卤化 -7 accylamine青霉素或头孢菌素，b）3-羟基-3-头孢烯的卤化，c）C-7酰胺-3-羟基头孢烯的一步卤化d）还原头孢菌素亚砜e）一步还原/ 3-羟基头孢菌素亚砜的卤化f）C-7酰胺头孢菌素亚砜的一步还原/卤化g）C-7酰氨基-3-羟基头孢菌素亚砜的一步还原/卤化。

    Preparation of the penicilline binding protein 2A from staphylococcus aureus 27R, purification and use in a resistant-assay
    7.
    发明公开
    Preparation of the penicilline binding protein 2A from staphylococcus aureus 27R, purification and use in a resistant-assay 失效
    产生从金黄色葡萄球菌27R，纯化和使用中，青霉素结合蛋白2A如在结合测定。

    公开(公告)号：EP0505151A2

    公开(公告)日：1992-09-23

    申请号：EP92302298.2

    申请日：1992-03-18

    申请人： ELI LILLY AND COMPANY

    发明人： Blaszczak, Larry Chris ,  Skatrud, Paul Luther ,  Smith, Michele Ceceil ,  Wu, Chyun-Yeh Earnest

    IPC分类号： C12N15/57 ,  C12N15/31 ,  C12N15/62 ,  C12N9/52 ,  C07K3/18 ,  C12Q1/37 ,  B01J20/32

    CPC分类号： C12N9/52 ,  C07K14/31 ,  C07K2319/00 ,  C07K2319/02 ,  C12N15/625

    摘要： The invention provides a gene encoding a novel PBP2A penicillin binding protein isolated from the methicillin resistant S. aureus strain 27R. The invention further provides soluble forms of PBP2A proteins lacking the transmembrane association region yet retain their active site configuration of the PBP2A protein. The invention also provides a method of assaying for agents useful against methicillin resistant staphylococcus strains by creating a kinetically inert complex between a support-mobilized transition metal ion and a modified soluble form of the PBP2A protein incorporating a chelating agent. The invention further provides a cell free method of assaying for agents which bind the PBP2A-27R protein.

    摘要翻译： 本发明提供了编码来自耐甲氧西林金黄色葡萄球菌菌株27R分离的新颖的PBP2a青霉素结合蛋白的基因。 本发明提供了缺乏跨膜区的关联，但仍保留了蛋白质的PBP2a的其活性位点结构的PBP2a蛋白的进一步可溶形式。 因此本发明提供测定针对通过创建支持动员的过渡金属离子和蛋白质的PBP2a掺入的螯合剂修饰的可溶性形式之间的动力学惰性的复杂耐甲氧西林葡萄球菌菌株有用的试剂的方法。 本发明还提供测定用于结合所述的PBP2a-27R蛋白质剂的无细胞方法。

    Process for 1-carba(dethia) cephalosporins
    8.
    发明公开
    Process for 1-carba(dethia) cephalosporins 失效
    1-卡巴（dethia）头孢菌素的工艺

    公开(公告)号：EP0359540A3

    公开(公告)日：1991-09-04

    申请号：EP89309281.7

    申请日：1989-09-13

    申请人： ELI LILLY AND COMPANY

    发明人： Blaszczak, Larry Chris

    IPC分类号： C07D463/00 ,  C07D501/14 ,  C07D205/085

    CPC分类号： C07D205/085 ,  C07D463/04 ,  C07D463/06

    摘要： The invention provides a free radical process for preparing 1-carba(1-dethia)cephalosporin antibiotics with 2-substituted methylcephalosporin 1,1-­dioxides wherein the substituent on the 2-methylene group is a free radical precursor group such as a phenyl or alkylseleno group. The latter dioxides are treated with a free radical initiator, e.g., a trialkyl­tin hydride or actinic radiation at 40°C to 150°C to provide the 1-carba-3-cephem and 1-carba-2-cephem products. The invention also provides free radical compounds formed as intermediates in the process.

    摘要翻译： 本发明提供了用2-取代甲基头孢菌素1,1-二氧化物制备1-卡巴（1-去硫）头孢菌素抗生素的自由基方法，其中2-亚甲基上的取代基是自由基前体基团，例如苯基或烷基硒基 组。 用自由基引发剂例如三烷基锡氢化物或光化辐射在40℃至150℃下处理后面的二氧化物，以提供1-碳-β-3-头孢烯和1-卡巴-2-头孢烯产物。 本发明还提供了在该方法中形成为中间体的自由基化合物。