公开(公告)号：US5527910A

公开(公告)日：1996-06-18

申请号：US160821

申请日：1993-12-03

申请人： Choong S. Kim ,  Jin W. Kim ,  Jae M. Lee ,  Il H. Cho ,  Yong S. Youn ,  Young J. Shin ,  Ki H. Lee ,  Je H. Kim ,  Yong H. Jung ,  Seung H. An

发明人： Choong S. Kim ,  Jin W. Kim ,  Jae M. Lee ,  Il H. Cho ,  Yong S. Youn ,  Young J. Shin ,  Ki H. Lee ,  Je H. Kim ,  Yong H. Jung ,  Seung H. An

IPC分类号： C07D221/04 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/473 ,  A61P31/04 ,  C07D209/52 ,  C07D401/04 ,  C07D401/14 ,  C07D471/04 ,  C07D498/06

CPC分类号： C07D401/04 ,  A61K31/4375 ,  C07D471/04

摘要： Pyridone carboxylic acid compounds or physiologically hydrolyzable esters thereof are provided which are represented by the formula: ##STR1## wherein R.sub.1 is a lower alkyl, a halogen-substituted lower alkyl, a lower alkenyl, a cycloalkyl, or a substituted- or unsubstituted-phenyl group; R.sub.2 is a hydrogen atom, or a lower alkyl or an amino group; A is a nitrogen atom or the group C-X wherein X is a hydrogen or a halogen atom, or an alkoxy group; and Z is a group having the formula: ##STR2## wherein n is 1 or 2; R.sub.3 and R.sub.4 each represent a hydrogen atom or a lower alkyl group, with proviso that, if n is 2, one of R.sub.3 and R.sub.4 is a hydrogen atom; R.sub.5 and R.sub.6 each represent a hydrogen atom, or a hydroxy, a lower alkoxy or an amino group which is unsubstituted or substituted by a lower alkyl group, with proviso that one of R.sub.5 and R.sub.6 is a hydrogen atom; and R.sub.7 is a hydrogen atom or a lower alkyl group. The compounds of the present invention show potent and broad spectrum of antibacterial activities.

摘要翻译： 提供了由下式表示的吡啶酮羧酸化合物或其生理上可水解的酯：其中R 1是低级烷基，卤素取代的低级烷基，低级烯基，环烷基或取代或 未取代的苯基; R2是氢原子或低级烷基或氨基; A是氮原子或C-X基团，其中X是氢或卤素原子或烷氧基; Z为具有下式的基团：其中n为1或2; R3和R4各自表示氢原子或低级烷基，条件是如果n为2，则R3和R4中的一个为氢原子; R 5和R 6各自表示氢原子，或羟基，低级烷氧基或未被取代或被低级烷基取代的氨基，条件是R 5和R 6中的一个为氢原子; 并且R 7是氢原子或低级烷基。 本发明的化合物显示出有效和广谱的抗菌活性。