公开(公告)号：US20050075363A1

公开(公告)日：2005-04-07

申请号：US10911406

申请日：2004-08-04

申请人： Barton Bradbury ,  Milind Deshphande ,  Michael Pucci ,  Qiuping Wang ,  Jason Wiles ,  Monishing Song ,  Akihiro Hashimoto ,  Edlaine Lucien

发明人： Barton Bradbury ,  Milind Deshphande ,  Michael Pucci ,  Qiuping Wang ,  Jason Wiles ,  Monishing Song ,  Akihiro Hashimoto ,  Edlaine Lucien

IPC分类号： C07D498/04 ,  C07D513/04 ,  C07D498/14 ,  A61K31/4745

CPC分类号： C07D513/04

摘要： The invention provides compounds and salts of Formula I and Formula II: which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A1, R2, R3, R5, R6, R7, A8 and R9 are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.

摘要翻译： 本发明提供具有抗微生物活性的式I和式II化合物和盐。 本发明还提供了可用于制备式I和式II化合物的新型合成中间体。 变量A1，R2，R3，R5，R6，R7，A8和R9在本文中定义。 本文公开的某些式I和式II化合物是细菌DNA合成和细菌复制的有效和选择性抑制剂。 本发明还提供包含一种或多种式I或式II化合物和一种或多种载体，赋形剂或稀释剂的抗微生物组合物，包括药物组合物。 这样的组合物可以含有式I或式II的化合物作为唯一的活性剂或可以含有式I或式II的化合物与一种或多种其它活性剂的组合。 本发明还提供了治疗动物微生物感染的方法。