公开(公告)号：US20120029213A1

公开(公告)日：2012-02-02

申请号：US13171971

申请日：2011-06-29

申请人： Brian Austad ,  Farid Benayoud ,  Trevor Calkins ,  Silvio Campagna ,  Charles E. Chase ,  William Christ ,  Francis G. Fang ,  Yongbo Hu ,  Bryan M. Lewis ,  Marc Pesant ,  Matthew Schnaderbeck ,  Gordon Wilkie ,  Xiaojie Zhu

发明人： Brian Austad ,  Farid Benayoud ,  Trevor Calkins ,  Silvio Campagna ,  Charles E. Chase ,  William Christ ,  Francis G. Fang ,  Yongbo Hu ,  Bryan M. Lewis ,  Marc Pesant ,  Matthew Schnaderbeck ,  Gordon Wilkie ,  Xiaojie Zhu

IPC分类号： C07D407/14 ,  C07D493/20 ,  C07D493/10 ,  C07F7/08 ,  C07D307/28

摘要： Intermediates and methods of their use in the synthesis of analogs of halichondrin B are provided.

摘要翻译： 提供了中间体及其用于合成类软绵母B的方法。

公开(公告)号：US06723716B1

公开(公告)日：2004-04-20

申请号：US09668722

申请日：2000-09-21

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

发明人： Scott J. Hecker ,  Aesop Cho ,  Tomasz W. Glinka ,  Trevor Calkins ,  Ving J. Lee

IPC分类号： C07D50159

CPC分类号： C07D213/70 ,  C07D285/08 ,  C07D501/00 ,  C07F9/6506

摘要： The present invention relates to a cephem prodrug having formula III or formula IV: or a pharmaceutically acceptable salt thereof, wherein R′1 is selected from the group consisting of hydrogen and —C(O)CH(NH2)CH3 and R′2 is selected from the group consisting of hydrogen and an acyl group that is cleaved by an enzyme found in mammals, with the proviso that, when either R′1 or R′2 is hydrogen, the other is not. A, B, L, G, E, and J are each independently nitrogen or carbon such that the respective rings are selected from the group consisting of provided that the group —CH2—S—CH2CH2NHR′2 is attached only to a carbon atom of said heterocyclic group, and Q is selected from the group consisting of nitrogen and —CX, wherein X is selected from the group consisting of hydrogen and chlorine.

摘要翻译： 本发明涉及具有式III或式IV的头孢烯前药或其药学上可接受的盐，其中R'1选自氢和-C（O）CH（NH 2）CH 3和R' <2>选自氢和由哺乳动物中发现的酶切割的酰基，条件是当R'1或R'2都是氢时，另一个不是 。 A，B，L，G，E和J各自独立地为氮或碳，使得各个环选自提供基团-CH 2 -S-CH 2 CH 2 NHR'2仅与碳原子连接 的所述杂环基，Q选自氮和-CX，其中X选自氢和氯。