公开(公告)号：US5389627A

公开(公告)日：1995-02-14

申请号：US145228

申请日：1993-11-03

申请人： Choong S. Kim ,  Yang S. Ahn ,  Kang Y. Jung ,  Nam H. Lee ,  Rok L. Yun ,  Seong Y. Park ,  Yeo H. Yoon ,  Keon H. Lee ,  Chun S. Lyu ,  Kwang H. Lee

发明人： Choong S. Kim ,  Yang S. Ahn ,  Kang Y. Jung ,  Nam H. Lee ,  Rok L. Yun ,  Seong Y. Park ,  Yeo H. Yoon ,  Keon H. Lee ,  Chun S. Lyu ,  Kwang H. Lee

IPC分类号： C07D501/00 ,  C07D519/06 ,  C07D501/38 ,  A61K31/545

CPC分类号： C07D501/00

摘要： The present invention relates to novel cephem compounds having the formula: ##STR1## wherein, Q is a carbon or nitrogen atom; X is an oxygen atom, or a nitroalkyl or cyanoimine group, with the proviso that X cannot be an oxygen atom when Q is a carbon atom; R.sub.1 is a hydrogen atom, or a lower alkyl group, or a lower alkyl group which may be substituted by fluoro, or by a carboxylic group or an inorganic cation salt thereof; and R.sub.2 and R.sub.3 independently are a hydrogen atom or a lower alkyl group; or pharmaceutically acceptable salts thereof.The compounds of the present invention have potent antibacterial activities against gram-negative bacteria, especially Pseudomonas, and a longer half-life than conventional cephem compounds.

摘要翻译： 本发明涉及具有下式的新的头孢烯化合物：其中Q是碳或氮原子; X是氧原子或硝基烷基或氰基亚胺基，条件是当Q是碳原子时X不能是氧原子; R1是氢原子或低级烷基，或可被氟取代的低级烷基，或其羧基或无机阳离子盐; R2和R3独立地为氢原子或低级烷基; 或其药学上可接受的盐。 本发明的化合物对革兰氏阴性细菌，特别是假单胞菌具有有效的抗菌活性，并且比常规头孢烯化合物具有更长的半衰期。