公开(公告)号：EP2753620A1

公开(公告)日：2014-07-16

申请号：EP12769045.1

申请日：2012-09-07

申请人： Sandoz AG

发明人： KREMMINGER, Peter ,  STURM, Hubert

IPC分类号： C07D417/04 ,  C07D501/59

CPC分类号： C07F9/65613 ,  C07C51/41 ,  C07C303/22 ,  C07D417/04 ,  C07D501/04 ,  C07D501/08 ,  C07D501/59

摘要： The present invention relates to a novel process for preparing ceftaroline fosamil as well as to a intermediates of formulae (1), (3) or (4) of this process.

公开(公告)号：EP1132391B1

公开(公告)日：2006-11-15

申请号：EP00956989.8

申请日：2000-09-07

申请人： OTSUKA KAGAKU KABUSHIKI KAISHA

发明人： KAMEYAMA, Yutaka, Otsuka Kagaku Kabushiki Kaisha

IPC分类号： C07D501/04 ,  C07D501/59 ,  C07D501/00 ,  C07D501/22

CPC分类号： C07D501/00

摘要： A process for the preparation of 3-sulfonyloxy-3-cephem compounds of general formula (3), characterized by reacting a 3-hydroxy-3-cephem compound of general formula (1) with a sulfonic acid halide of general formula (2) :R4SO2x, in an organic solvent in the presence of an alkali metal carbonate or an alkaline earth metal carbonate wherein R1 to R4 and X are each as defined in the description.

公开(公告)号：EP1333836A4

公开(公告)日：2004-07-07

申请号：EP01968147

申请日：2001-08-23

申请人： ESSENTIAL THERAPEUTICS INC

发明人： GLINKA TOMASZ W

IPC分类号： C07D501/59 ,  A61K31/546 ,  A61P31/04 ,  C07D501/00 ,  A61K31/545 ,  A61P31/00

CPC分类号： C07D501/00

公开(公告)号：EP0827961B1

公开(公告)日：2002-10-16

申请号：EP97905459.0

申请日：1997-03-07

申请人： OTSUKA KAGAKU KABUSHIKI KAISHA

发明人： TORII, Sigeru ,  TANAKA, Hideo ,  SASAOKA, Michio, Otsuka Kagaku K.K. ,  KAMEYAMA, Yutaka, Otsuka Kagaku K.K.

IPC分类号： C07D501/59 ,  C07D205/08 ,  C07D205/09 ,  C07D205/095 ,  C07D501/00 ,  C07D501/08

CPC分类号： C07D501/00 ,  C07D205/095 ,  Y02P20/55

摘要： A process for preparing allenyl-β-lactam compounds of general formula (II) or 3-halocephem compounds of general formula (III) from halogenated β-lactam compounds of general formula (I) under reaction conditions selected depending on the objective compound. In formula (I), R1 is hydrogen, amino or protected amino; R2 is optionally substituted aryl; n is 0 to 2; R3 is hydrogen or a carboxyl-protecting group; X is halogeno; and Y is halogeno or a leaving group. In formula (II), R1, R2, n and R3 are each as defined above. In formula (III), R1, R3 and X are each as defined above.

公开(公告)号：EP1077981B1

公开(公告)日：2002-08-07

申请号：EP99919695.9

申请日：1999-05-12

申请人： LG CHEMICAL LIMITED

发明人： LEE, Chang Seok ,  OH, Seong Ho ,  MOON, Kwang Yul ,  RYU, Eun Jung, Taeyoung Moogoonghwa ,  KIM, Yong Zu ,  KIM, Mu Yong ,  PAEK, Kyoung Sook ,  LEE, Sun Hwa, Chungkoonarae

IPC分类号： C07D501/00 ,  C07D501/59 ,  A61K31/545

CPC分类号： C07D501/00 ,  Y02P20/55

摘要： This invention relates to novel cephalosporin compounds of formula (I), wherein A, R1, R2, Q and B are each as defined in the specification, processes for preparation thereof and antimicrobial compositions containing the same.

公开(公告)号：EP1222194A1

公开(公告)日：2002-07-17

申请号：EP00966807.0

申请日：2000-09-21

申请人： Essential Therapeutics, Inc.

发明人： HECKER, Scott, J. ,  CHO, Aesop ,  GLINKA, Tomasz, W. ,  CALKINS, Trevor ,  LEE, Ving, J.

IPC分类号： C07D501/59 ,  A61K31/546 ,  A61P31/04 ,  C07D213/70 ,  C07D285/08 ,  C07F9/6506

CPC分类号： C07D213/70 ,  C07D285/08 ,  C07D501/00 ,  C07F9/65062

摘要： The present invention includes novel (7R)-7-acylamino-3-heteroarylthio-3-cephem-4-carboxylic acids or their pharmacologically acceptable salts and prodrugs thereof, which exhibit antibiotic activity against a wide spectrum of organisms including organisms which are resistant to β-lactam antibiotics and are useful as antibacterial agents. The invention also relates to novel intermediates useful for making the novel compounds of the present invention and to novel methods for producing the novel compounds and intermediate compounds.

摘要翻译： 本发明包括对广谱的生物体具有抗生素活性的新型（7R）-7-酰氨基-3-杂芳硫基-3-头孢烯-4-羧酸或其药理学上可接受的盐和前药，所述生物体包括对 β-内酰胺抗生素并且可用作抗菌剂。 本发明还涉及可用于制备本发明新化合物的新颖中间体，并涉及制备该新化合物和中间体化合物的新方法。

公开(公告)号：EP0989132A4

公开(公告)日：2001-11-14

申请号：EP99910811

申请日：1999-04-02

申请人： OTSUKA KAGAKU KK

发明人： SHIMABAYASHI AKIHIRO ,  KAWAHARA ICHIROU ,  YAGUCHI SHIGETOSHI ,  ASAI HIROAKI

IPC分类号： C07D499/87 ,  C07D499/00 ,  C07D499/04 ,  C07D499/10 ,  C07D499/86 ,  C07D499/865 ,  C07D499/897 ,  C07D501/00 ,  C07D501/04 ,  C07D501/16 ,  C07D501/59

CPC分类号： C07D499/00 ,  C07D501/00

摘要： A process for producing a halogenated β-lactam compound represented by general formula (4), characterized by reacting a β-lactam-derived amino compound represented by general formula (1) with nitrous acid or a nitrite in the presence of halogen molecules under acid conditions while keeping the reactants in an aqueous slurry state to obtain the target compound. In formula (1) n is an integer of 0 to 2; and A represents formula (2) or (3), wherein R?1 and R2¿ are the same or different and each is hydrogen, halogeno, C¿1-3? alkyl, C2-4 alkenyl, C2-4 alkynyl, a nucleophilic group, or CH2R?3¿, where R3 represents halogeno or a nucleophilic group. In formula (4) A is the same as the above; X1 represents hydrogen or halogeno; and X2 represents halogeno.

公开(公告)号：EP1132391A1

公开(公告)日：2001-09-12

申请号：EP00956989.8

申请日：2000-09-07

申请人： OTSUKA KAGAKU KABUSHIKI KAISHA

发明人： KAMEYAMA, Yutaka, Otsuka Kagaku Kabushiki Kaisha

IPC分类号： C07D501/04 ,  C07D501/59

CPC分类号： C07D501/00

摘要： A method for producing a 3-sulfonyloxy-3-cephem compound shown by the formula (3) comprising reacting a 3-hydroxy-3-cephem compound shown by the formula (1) with a sulfonyl halide shown by the formula (2) in an organic solvent in the presence of an alkali metal carbonate or alkaline earth metal carbonate.


        R 4 SO 2 X     (2)


(R 1 to R 4 , and X are as defined in the specification)

摘要翻译： 一种制备式（3）所示的3-磺酰氧基-3-头孢烯化合物的方法，包括使式（1）所示的3-羟基-3-头孢烯化合物与式（2）所示的磺酰卤反应在 有机溶剂在碱金属碳酸盐或碱土金属碳酸盐存在下进行。 （CH 1）R 4 SO 2 X （R 1至R 4），X如说明书中所定义）n

公开(公告)号：EP0854875B1

公开(公告)日：2001-06-13

申请号：EP96932012.6

申请日：1996-09-27

申请人： FUJISAWA PHARMACEUTICAL CO., LTD.

发明人： KAWABATA, Kohji ,  YAMAMOTO, Hirofumi ,  EIKYU, Yoshiteru ,  OKUDA, Shinya ,  TAKASUGI, Hisashi

IPC分类号： C07D501/22 ,  C07D501/24 ,  C07D501/59 ,  A61K31/545

CPC分类号： C07D501/00 ,  Y02P20/55

摘要： A compound of general formula (I) wherein R1 is amino or protected amino, R2 is hydrogen or hydroxy protective group, R3 is carboxy or protected carboxy, R4 is hydrogen, lower alkenyl, acyloxy(lower)alkenyl, optionally substituted heterocyclic(lower)alkenyl, optionally substituted heterocyclic(lower)alkenylthio, optionally substituted heterocyclic(lower)alkylthio, or optionally substituted heterocyclic-thio(lower)alkylthio and R5 is halogen or lower alkyl and pharmaceutically acceptable salts thereof, which is useful as a medicament for prophylactic and therapeutic treatment of infectious diseases.

公开(公告)号：EP0780393A4

公开(公告)日：1997-12-10

申请号：EP95930705

申请日：1995-09-06

申请人： FUJISAWA PHARMACEUTICAL CO

发明人： KAWABATA KOHJI ,  TERASAWA TAKESHI ,  OHKI AYAKO ,  SHIRAI FUMIYUKI ,  YAMAMOTO HIROFUMI ,  KAWAKAMI RYOICHI ,  HAMAGUCHI CHIAKI

IPC分类号： C07D501/04 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07B63/00 ,  C07D501/00 ,  C07D501/59

CPC分类号： C07D501/00 ,  Y02P20/55

摘要： A novel crystal of 7β-[2-(2-aminothiazol-4-yl)-2-Z-(hydroxyimino)acetamido]-3-[(pyrazol-4-yl)-methylthio]-3-cephem-4-carboxylic acid or a salt thereof. The compound is a cephalosporin antibiotic having a potent antibacterial activity and is excellent in physical, chemical and pharmaceutical properties.