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    Substrates for beta-lactamase and uses thereof
    3.
    发明申请
    Substrates for beta-lactamase and uses thereof 有权
    β-内酰胺酶底物及其用途

    公开(公告)号：US20030119085A1

    公开(公告)日：2003-06-26

    申请号：US10280482

    申请日：2002-10-24

    申请人： The Regents of the University of California

    发明人： Roger Y. Tsien ,  Gregor Zlokarnik

    IPC分类号： C12Q001/18 ,  C07D55/16 ,  C07D51/14 ,  C07D487/04

    CPC分类号： C07D501/36 ,  C07D501/00 ,  C07D505/00 ,  C07D519/00 ,  C12N9/86 ,  C12N15/85 ,  C12N2800/90 ,  C12N2830/002 ,  C12P17/184 ,  C12P17/188 ,  C12P35/00 ,  C12Q1/18 ,  C12Q1/34 ,  C12Q1/6897 ,  C12Q2334/00 ,  G01N2333/986 ,  G01N2415/00 ,  Y10S435/805

    摘要： Substrates for null-lactamase of the general formula I 1 in which one of X and Y is a fluorescent donor moiety and the other is a quencher (which may or may not re-emit); Rnull is selected from the group consisting of H, lower (i.e., alkyl of 1 to about 5 carbon atoms) and (CH2)nOH, in which n is 0 or an integer from 1 to 5; Rnull is selected from the group consisting of H, physiologically acceptable metal and ammonium cations, nullCHR2OCO(CH2)nCH3, nullCHR2OCOC(CH3)3, acylthiomethyl, acyloxy-alpha-benzyl, delta-butyrolactonyl, methoxycarbonyloxymethyl, phenyl, methylsulphinylmethyl, beta-morpholinoethyl, dialkylaminoethyl, acyloxyalkyl, dialkylaminocarbonyloxymethyl and aliphatic, in which R2 is selected from the group consisting of H and lower alkyl; A is selected from the group consisting of S, O, SO, SO2 and CH2; and Znull and Znull are linkers for the fluorescent donor and quencher moieties. Methods of assaying null-lactamase activity and monitoring expression in systems using null-lactamase as a reporter gene also are disclosed.

    摘要翻译： 通式I的β-内酰胺酶底物，其中X和Y中的一个是荧光供体部分，另一个是猝灭剂（其可以或不再发射）; R'选自H，低级（即1至约5个碳原子的烷基）和（CH 2）nOH，其中n为0或1至5的整数; R“选自H，生理学上可接受的金属和铵阳离子，-CHR2OCO（CH2）nCH3，-CHR2OCOC（CH3）3，酰基硫代甲基，酰氧基-α-苄基，δ-丁基内酰基，甲氧基羰氧基甲基，苯基，甲基亚磺酰基甲基 ，β-吗啉代乙基，二烷基氨基乙基，酰氧基烷基，二烷基氨基羰氧基甲基和脂族基，其中R2选自H和低级烷基; A选自S，O，SO，SO 2和CH 2; Z'和Z“是荧光供体和猝灭剂部分的接头。 公开了使用β-内酰胺酶作为报道基因的体内测定β-内酰胺酶活性和监​​测表达的方法。

    Process for the preparation of ceftriaxone
    4.
    发明授权
    Process for the preparation of ceftriaxone 失效
    头孢曲松的制备方法

    公开(公告)号：US5026843A

    公开(公告)日：1991-06-25

    申请号：US416627

    申请日：1989-10-03

    申请人： Monguzzi Riccardo ,  Menaspace Silvano ,  Anzaghi Piergiorgio

    发明人： Monguzzi Riccardo ,  Menaspace Silvano ,  Anzaghi Piergiorgio

    IPC分类号： C07D501/00 ,  A61K20060101 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/02 ,  C07D501/04 ,  C07D501/36

    CPC分类号： C07D501/36

    摘要： An improved process for the preparation of an antibiotic substance, more specifically 7{[2-(2-aminothiazol-4-yl)-2-synmethoxyimino]acetamido}-3-{[(2,5-dihydro-6-hydroxy-2-methyl-5-oxo-1,2,4-triazin-3-yl)thio]methyl}-3-cephem-4-carboxylic acid in the form of disodium salt hemieptahydrate is described, where 7-amino-3-{[(2,5-dihydro-6-hydroxy-2-methyl-5-oxo-1,2,4-triazin-3-yl)thio]methyl}-3-cephem-4-carboxylic acid is made to react with 2-mercaptobenzothiazole 2-(2-aminothiazol-4-yl)-2-syn-methoxyiminoacetate in an aqueous solution in suitable solvents, in the presence of an amine selected from the group consisting of trimethylamine, triethylamine, 1,4-dimethylpiperazine, N-ethylpiperidine, pyridine and dimethylaminopyridine and the obtained aqueous solution is treated with a base selected from the group consisting of dicyclohexylamine, diphenylamine, diisopropylamine, N-tert-butylcyclohexylamine and N,N-dibenzylethylendiamine, in a suitable form, and the thus formed precipitate is reacted in suitable solvents with sodium 2-ethylhexanoate to give the desired compound.

    Cephalosporin derivatives
    5.
    发明授权
    Cephalosporin derivatives 失效
    头孢菌素衍生物

    公开(公告)号：US5017569A

    公开(公告)日：1991-05-21

    申请号：US117619

    申请日：1987-11-06

    申请人： Alain M. Bertrandie ,  Thomas G. C. Bird ,  Frederic H. Jung ,  Jean-Jacques M. Lohmann

    发明人： Alain M. Bertrandie ,  Thomas G. C. Bird ,  Frederic H. Jung ,  Jean-Jacques M. Lohmann

    IPC分类号： C07D501/38 ,  A61K20060101 ,  A61K9/00 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D471/00 ,  C07D501/00 ,  C07D501/18 ,  C07D501/34 ,  C07D501/36 ,  C07D501/46

    CPC分类号： C07D501/36 ,  C07D501/34 ,  C07D501/46

    摘要： Cephalosporin compounds having a 3-position substituent of the formula (I) are described:--CH.sub.2 --Y--Q (I)wherein Y is a linking group --NR.sup.4 CO--Y'--, --NR.sup.4 SO.sub.2 --Y'--, --OCO--Y;-- or --SCO--Y'-- wherein R.sup.4 is hydrogen, various optionally substituted alkyl groups or alkenyl and Y' is a bond or various optionally substituted alkylene or alkenylene groups; and Q is a benzene ring (optionally fused to a further benzene ring so forming a naphthyl group or optionally fused to a 5 or 6 membered heterocyclic aromatic group containing 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur), said benzene ring (or in the case of naphthyl either benzene ring) being substituted by groups R.sup.1 and R.sup.2 which are ortho with respect to one another, wherein R.sup.1 is hydroxy or an in vivo hydrolyzable ester thereof and R.sup.2 is hydroxy, an in vivo hydrolyzable ester thereof, carboxy, sulpho, hydroxymethyl, methanesulphonamido or ureido; or Q is a group of the formula (II) or (III): ##STR1## wherein M is oxygen or a group NR.sup.3 wherein R.sup.3 is hydrogen or C.sub.1-4 alkyl; ring Q being further optionally substituted.The use of such compounds as antibacterial agents is described as are processes for their preparation and intermediates therefor.

    摘要翻译： 描述了具有式（I）的3-位取代基的头孢菌素化合物：其中Y是连接基-NR4CO-Y'-，-NR4SO2-Y'-，-OCO-Y的-CH2-YQ（Ⅰ） 或-SCO-Y'-，其中R 4是氢，各种任选取代的烷基或烯基，Y'是一个键或各种任选取代的亚烷基或亚烯基; 并且Q是苯环（任选地与另外的苯环稠合形成萘基或任选地与含有1,2或3个选自氮，氧和硫的杂原子的5或6元杂环芳族基团稠合），所述苯环 （或萘基为苯环的情况）被相互相邻的基团R1和R2取代，其中R1是羟基或其体内可水解的酯，R2是羟基，其体内可水解的酯， 羧基，磺基，羟甲基，甲磺酰氨基或脲基; 或Q是式（II）或（III）的基团：其中M是氧或NR 3，其中R 3是氢或C 1-4烷基; 环Q进一步任选被取代。 这些化合物作为抗菌剂的使用被描述为它们的制备方法及其中间体。

    Cephalosporin derivatives, and their application as antibiotics
    7.
    发明授权
    Cephalosporin derivatives, and their application as antibiotics 失效
    头孢菌素衍生物及其作为抗生素的应用

    公开(公告)号：US4950661A

    公开(公告)日：1990-08-21

    申请号：US188073

    申请日：1988-04-28

    申请人： Dominique Olliero ,  Ali Salhi

    发明人： Dominique Olliero ,  Ali Salhi

    IPC分类号： C07D501/20 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/00 ,  C07D501/34 ,  C07D501/36 ,  C07D501/46 ,  C07D501/56

    CPC分类号： C07D501/36 ,  C07D501/34 ,  Y02P20/55

    摘要： The present invention relates to derivatives of the cephalosporin family, of formula: ##STR1## in which: X is an oxygen atom or a sulfur atomn is zero, 1 or 2.R.sub.1, R.sub.2 and R.sub.3 each designate, a hydrogen atom or else R.sub.1 and R.sub.2 designate a hydrogen atom or a methyl group, and R.sub.3 designates a carboxyl or cyclopropyl group, or elseR.sub.1 and R.sub.2 taken together with the carbon atom to which they are linked form a cyclobutyl or cyclopentyl group and R.sub.3 is a carboxyl group.B is the residue of a primary or secondary amine;their preparation process and application in therapeutics.

    摘要翻译： 本发明涉及头孢菌素家族的衍生物，其结构如下：其中：X是氧原子或硫原子，n是0,1或2.R 1，R 2和R 3各自表示氢 或者R 1和R 2表示氢原子或甲基，R 3表示羧基或环丙基，或者R 1和R 2与它们所连接的碳原子一起形成环丁基或环戊基，R 3为 羧基。 B是伯胺或仲胺的残基; 其制备方法和在治疗中的应用。

    Cephalosporin derivatives
    8.
    发明授权
    Cephalosporin derivatives 失效
    头孢菌素衍生物

    公开(公告)号：US4904791A

    公开(公告)日：1990-02-27

    申请号：US174518

    申请日：1988-03-28

    申请人： Haruo Ohnishi ,  Hiroshi Kosuzume ,  Masahiro Mizota ,  Yasuo Suzuki ,  Ei Mochida

    发明人： Haruo Ohnishi ,  Hiroshi Kosuzume ,  Masahiro Mizota ,  Yasuo Suzuki ,  Ei Mochida

    IPC分类号： C07D209/48 ,  C07D277/20 ,  C07D277/40 ,  C07D501/20 ,  C07D501/36 ,  C07D501/46 ,  C07D501/59 ,  C07D519/00

    CPC分类号： C07D209/48 ,  C07D277/587 ,  C07D501/36 ,  C07D501/46 ,  C07D519/00

    摘要： The present invention relates to novel cephalosporin derivatives, processes for preparing thereof, compositions for preventing and/or treating infectious diseases which comprise the novel cephalosporin derivatives as active components, and the intermediate compounds in the synthesis of cephalosporin derivatives and processes for producing thereof.The present invention is based on the selection of groups containing a condensed heterocyclic ring, particularly a triazolopyrimidine ring or a thiadiazolopyrimidine ring, as substituents at the 3-position of the cephem skeleton, and of groups containing a catechol moiety, particularly a catechol carboxymethyloxyimino moiety or a catechol carboxyimino moiety, as substituents at the 7-position of the cephem skeleton.The compounds of the present invention containing the aforementioned substituents have a strong antibacterial activity against Gram-negative bacteria and also against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus. These compounds are extremely useful for the treatment of infectious diseases.

    Process for the preparation of cefodizime
    9.
    发明授权
    Process for the preparation of cefodizime 失效
    头孢地嗪的制备方法

    公开(公告)号：US4868295A

    公开(公告)日：1989-09-19

    申请号：US936187

    申请日：1986-12-01

    申请人： Ottmar Jaenicke ,  Hans Wagner ,  Manfred Worm

    发明人： Ottmar Jaenicke ,  Hans Wagner ,  Manfred Worm

    IPC分类号： C07D501/06 ,  A61K20060101 ,  A61K31/545 ,  C07D20060101 ,  C07D501/00 ,  C07D501/04 ,  C07D501/36 ,  C07D501/46 ,  C07D501/56

    CPC分类号： C07D501/36 ,  Y02P20/55

    摘要： A process for the preparation of cefodizime of the formula ##STR1## wherein (a) a compound of the formula II (ATS) ##STR2## wherein R.sub.1 represents hydrogen or an aminoprotective group and A represents a hydrogen atom or one equivalent of an alkali metal or alkaline earth metal, of ammonium or of an organic nitrogen base, is first reacted with a compound of the formula IIIR--SO.sub.2 Hal wherein R represents an optionally substituted alkyl, aryl or aralkyl radical and Hal represents a halogen atom, in an organic solvent and, if appropriate, in the presence of a base,(b) a compound of the formula I (TACS) ##STR3## in which A has the above meaning, is reacted with a silylating agent in an organic solvent and, if appropriate, in the presence of a base, and(c) the two products formed in (a) and (b) are reacted in their reaction solutions, and any protective group R.sub.1 present in the end product of the formula I is eliminated.

    摘要翻译： 制备式（II）的化合物其中（a）式II（ATS）的化合物其中R 1表示氢或氨基保护基，A表示氢原子或一个 首先与式IIIR-SO2Hal的化合物反应，其中R表示任选取代的烷基，芳基或芳烷基，Hal表示卤素原子 在有机溶剂中，如果合适，在碱的存在下，（b）式（I）所示的化合物（TACS），其中A具有上述含义，与甲硅烷基化剂在有机溶剂中反应 和（c）在（a）和（b）中形成的两种产物在其反应溶液中反应，并且存在于式I的最终产物中的任何保护基R1是 消除了