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：EP1320533A1

公开(公告)日：2003-06-25

申请号：EP01918879.6

申请日：2001-03-20

申请人： Essential Therapeutics, Inc. ,  Hecker, Scott J. ,  Cho, Aesop ,  Glinka, Tomasz W. ,  Calkins, Trevor ,  Lee, Ving J.

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

CPC分类号： C07D501/00

摘要： The present invention relates to prodrugs of the antibiotic compound (7R)-7-[(Z)-2-(2-amino-5-chlorothiazol-4-yl)-2-(hydroxylimino)acetamido]acetamidol]-3-{3-(2-aminoethylthiomethyl]-pyrid-4-ylthio}-3-cephem-4-carbocyllic acid, where the prodrugs are substantially more water soluble at or near neutral pH than the parent compound.