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1. 发明公开

EP2539348A4 CEPHALOSPORIN DERIVATIVES USEFUL AS -LACTAMASE INHIBITORS AND COMPOSITIONS AND METHODS OF USE THEREOF 审中-公开
标题翻译：作为β-内酰胺酶抑制剂的头孢类衍生物及其组合物及其使用方法
公开(公告)号：EP2539348A4
公开(公告)日：2013-07-24
申请号：EP11746805
申请日：2011-02-25
申请人： DMITRIENKO GARY IGOR , GHAVAMI AHMAD , GOODFELLOW VALERIE JOY , JOHNSON JARROD W , KRISMANICH ANTHONY PAUL , MARRONE LAURA , VISWANATHA SUNDARAMMA
发明人： DMITRIENKO GARY IGOR , GHAVAMI AHMAD , GOODFELLOW VALERIE JOY , JOHNSON JARROD W , KRISMANICH ANTHONY PAUL , MARRONE LAURA , VISWANATHA THAMMAIAH
IPC分类号： C07D501/36 , A61K31/545 , A61P31/04 , C07D501/26 , C07D501/28
CPC分类号： C07D501/36 , A61K31/545 , C07D501/26 , C07D501/28
摘要： The present invention relates to cephalosporin derivatives having &bgr;-lactamase inhibitory activity. The compounds are useful in preventing or treating bacterial resistance to an antibiotic, e.g. a &bgr;-lactam antibiotic. Disclosed herein are compounds that are inhibitors of class B metallo-&bgr;-lactamases, as well as class A, C, and D serine &bgr;-lactamases. In some preferred embodiments, the compounds are 3′-thiobenzoate derivatives of a cephalosporin. Pharmaceutical compositions, methods, uses, kits and commercial packages comprising the compounds are also disclosed.

2. 发明公开

EP1660506A2 ORAL NEUROTHERAPEUTIC CEFAZOLIN COMPOSITIONS 审中-公开
标题翻译：口服NEUROTHERAPEUTIC CEFAZOLIN组合物
公开(公告)号：EP1660506A2
公开(公告)日：2006-05-31
申请号：EP04782021.2
申请日：2004-08-24
申请人： Revaax Pharmaceuticals LLC
发明人： KOPPEL, Gary, A. , CHANEY, Michael, O.
IPC分类号： C07D501/36 , A61K31/545 , A61K31/546 , A61K31/43 , A61K31/431 , A61P25/28
CPC分类号： A61K31/43 , A61K31/431 , A61K31/545 , A61K31/546 , C07D501/36 , C07D501/60
摘要： The treatment of neurological disorders using cefazolin compositions and pharmaceutical compositions including oral dosage forms that include cefazolin compositions are described.
摘要翻译：描述了使用头孢唑啉组合物和包括包含头孢唑啉组合物的口服剂型的药物组合物治疗神经障碍。

3. 发明授权

EP0817785B1 SUBSTRATES FOR BETA-LACTAMASE AND USES THEREOF 失效
标题翻译：底物，β-内酰胺酶及其用途
公开(公告)号：EP0817785B1
公开(公告)日：2001-04-04
申请号：EP96912454.4
申请日：1996-03-20
申请人： The Regents of The University of California
发明人： TSIEN, Roger, Y. , ZLOKARNIK, Gregor
IPC分类号： C07D471/04
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 β-lactamase of general formula (I) 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); R' 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; R' is selected from the group consisting of H, physiologically acceptable metal and ammonium cations, -CHR2OCO(CH¿2?)nCH3, -CHR?2¿OCOC(CH¿3?)3, acylthiomethyl, acyloxy-alpha-benzyl, delta-butyrolactonyl, methoxycarbonyloxymethyl, phenyl, methylsulphinylmethyl, beta-morpholinoethyl, dialkylaminoethyl, acyloxyalkyl, dialkylaminocarbonyloxymethyl and aliphatic, in which R?2¿ is selected from the group consisting of H and lower alkyl; A is selected from the group consisting of S, O, SO, SO¿2? and CH2; and Z' and Z' are linkers for the fluorescent donor and quencher moieties. Methods of assaying β-lactamase activity and monitoring expression in systems using β-lactamase as a reporter gene also are disclosed.

4. 发明授权

EP0397511B1 Novel cephalosporin compounds and processes for preparation thereof 失效
标题翻译：头孢菌素及其制备化合物和方法
公开(公告)号：EP0397511B1
公开(公告)日：1996-09-04
申请号：EP90305079.7
申请日：1990-05-11
申请人： LUCKY, LTD.
发明人： Kim, Yong Zu , Oh, Hun Seung , Yeo, Jae Hong , Lim, Jong Chan , Kim, Won Sup , Bang, Chan Sik , Yim, Hyeon Joo
IPC分类号： C07D501/36 , A61K31/545
CPC分类号： C07D501/36

5. 发明授权

EP0329286B1 Zinc ceftiofur complexes 失效
标题翻译： Zinkceftiofurkomplexe。
公开(公告)号：EP0329286B1
公开(公告)日：1995-04-12
申请号：EP89300589.2
申请日：1989-01-23
申请人： THE UPJOHN COMPANY
发明人： Cazers, Alexander R. , Koshy, K. Thomas
IPC分类号： C07D501/36 , A61K31/545
CPC分类号： C07D501/36

6. 发明授权

EP0393066B1 CEPHALOSPORIN ANTIBIOTICS 失效
标题翻译：头孢菌素类抗生素。
公开(公告)号：EP0393066B1
公开(公告)日：1994-02-02
申请号：EP88909037.9
申请日：1988-10-11
申请人： THE UPJOHN COMPANY
发明人： CAZERS, Alexander R. , KOSHY, K. Thomas , JAGLAN, Prem S. , YANCEY, Robert J. Jr. , GILBERTSON, Terry , ARNOLD, Thomas S. , JOHNSON, David B. , GATCHELL, Catherine L.
IPC分类号： C07D501/36 , A61K31/545
CPC分类号： C07D501/36
摘要： Cephalosporin compounds of formula (II), where R is hydrogen or a pharmaceutical cation, in which case R1 is not present, or R is hydrogen or a chemical bond when R1 is an acid addition salt anion, and R2 is (a) hydrogen, (b) a duplicate of formula (I) compound to form a dimer, (c) an aminocarbonylmethyl, or (d) an -SR3 group where R3 is alkyl, cyclohexyl, phenyl, chloro-substituted phenyl, nitro-substituted phenyl, benzyl or furfuryl, have been found to be valuable as antibiotics for treating warm-blooded animals to combat pathogenic bacterial infections which cause diseases such as the commonly known ''shipping fever''.

7. 发明公开

EP0399094A3 Improved process for the preparation of ceftriaxone 失效
标题翻译：改进CEFTRIAXONE的制备方法
公开(公告)号：EP0399094A3
公开(公告)日：1992-03-04
申请号：EP89117988.9
申请日：1989-09-28
申请人： S.B.D. SYNTHETIC AND BIOLOGICAL DEVELOPMENTS S.r.l.
发明人： Monguzzi, Riccardo , Menapace, Silvano , Anzaghi, Piergiorgio
IPC分类号： C07D501/36 , C07D501/02
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-syn-methoxyimino]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.

8. 发明授权

EP0145395B1 Crystals of sodium cephemcarboxylate 失效
标题翻译：碳酸钙晶体的晶体
公开(公告)号：EP0145395B1
公开(公告)日：1990-11-22
申请号：EP84308182.9
申请日：1984-11-26
申请人： Takeda Chemical Industries, Ltd. , LEDERLE (JAPAN) LTD.
发明人： Naito, Kenzo , Tsukamura, Kazuo , Aoyagi, Sakae
IPC分类号： C07D501/36
CPC分类号： C07D501/36

9. 发明公开

EP0391393A2 Verfahren zur Herstellung von Cefodizim-Dinatrium 失效
标题翻译： Verfahren zur Herstellung von Cefodizim-Dinatrium。
公开(公告)号：EP0391393A2
公开(公告)日：1990-10-10
申请号：EP90106443.6
申请日：1990-04-04
申请人： HOECHST AKTIENGESELLSCHAFT
发明人： Martin, Wolfgang, Dr.
IPC分类号： C07D501/36
CPC分类号： C07D501/36
摘要： Verfahren zur Herstellung von Cefodizim-Dinatrium, dadurch gekennzeichnet, daß man Cefodizim mittels 1,5 - 2,5 Mol einer organischen Aminbase in Ethanol mit einem Wassergehalt von 4 - 15 % in Lösung bringt und das Dinatriumsalz des Cefodizims durch Zugabe eines Natriumspenders auskristallisieren läßt.
摘要翻译：该方法的特征在于，使用1.5-2.5mol的有机胺碱在含水量为4-15％的乙醇中将头孢地嗪溶解，并通过加入钠供体将头孢地嗪的二钠盐结晶出来。

10. 发明公开

EP0295630A3 Cephalosporinderivate 失效
标题翻译：头孢菌素
公开(公告)号：EP0295630A3
公开(公告)日：1990-09-26
申请号：EP88109479.1
申请日：1988-06-14
申请人： F. HOFFMANN-LA ROCHE AG
发明人： Wei, Chung-Chen , West, Kevin Francis
IPC分类号： C07D501/36 , C07D501/26 , C07D501/38 , C07D501/18 , A61K31/545
CPC分类号： C07D501/36 , C07D501/26 , C07D501/34 , C07D501/38 , C07D501/46 , Y02P20/55
摘要： Acylderivate der allgemeinen Formel
in der X -OCO-, -SCO-, -NHCO- oder -OCONH-; R₁ eine Acylgruppe; R₂ Wasserstoff oder niederes Alkoxy; und R₃ die Gruppe
oder
oder
darstellen,
worin R₄, R 4′ und R 4˝ unabhängig voneinander Wasserstoff oder -COR₂₀₀ mit R₂₀₀ geradkettigem oder verzweigtem niederem Alkyl, A und B Halogen und a, b, x, y und z unabhängig voneinander Null (wobei in der entsprechenden Ringposition ein Wasserstoffatom vorliegt) oder 1 bedeuten, wobei mindestens zwei der Symbole x, y und z 1 darstellen, und m Null oder eine Zahl von 1 bis 8 bedeutet,
sowie leicht hydrolysierbare Ester und pharmazeutisch verträgliche Salze dieser Verbindungen und Hydrate der Verbindungen der Formel I bzw. von deren Estern und Salzen. Die Produkte sind antibakteriell wirksam.
摘要翻译：其中X是-OCO - ， - SCO - ， - NHCO-或-OCONH-的通式的酰基衍生物; R 1是酰基; R 2是氢或低级烷氧基; 和R 3为基团或代表或其中R 4，R 4“和R 4独立地为氢或具有R₂₀₀-COR₂₀₀直链或支链的低级烷基，A和B卤素以及a，b，x，y和z独立地为零（在该环上的一个氢原子存在于相应位置）或平均1其中符号X，Y中的至少两个，并且Z 1表示，并且m表示0或从1到8的整数，以及易于水解的酯和药学上可接受的化合物的这些化合物和水合物的盐式I或其酯和盐。该产品具有抗菌作用。

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