公开(公告)号：US4864023A

公开(公告)日：1989-09-05

申请号：US236822

申请日：1988-08-26

申请人： Kazuteru Yokose ,  Nobuo Shimma ,  Mikayo Kamata ,  Masahiro Aoki ,  Tatsuo Ohtsuka

发明人： Kazuteru Yokose ,  Nobuo Shimma ,  Mikayo Kamata ,  Masahiro Aoki ,  Tatsuo Ohtsuka

IPC分类号： C07D215/58 ,  C07D498/06 ,  C07D521/00

CPC分类号： C07D231/12 ,  C07D215/58 ,  C07D233/56 ,  C07D249/08

摘要： The invention is concerned with tricyclic compounds of the formula ##STR1## wherein R.sup.1 is a hydrogen atom or a carboxy-protecting radical; R.sup.2 is a hydrogen atom or a lower alkyl radical which may be substituted with a halogen atom; R.sup.3 and R.sup.4 independently are a hydrogen atom or a lower alkyl radical which may be substituted with a hydroxy radical or a substituted or unsubstituted amino radical; X is a halogen atom; and R.sup.5 and R.sup.6 are independently a hydrogen atom or a lower alkyl radical which may be substituted with a hydroxy radical, a lower alkoxy radical or a substituted or unsubstituted amino radical; or R.sup.5 and R.sup.6, taken together with the adjacent nitrogen atom, may form a 5 to 7 membered heterocyclic ring which may be substituted with one or more substituents at the carbon atom(s), and the heterocyclic ring may further contain --NR.sup.7 --, --O--, --S--, --SO--, --SO.sub.2 -- or --NR.sup.7 --CO--, and also R.sup.7 is a hydrogen atom, a lower alkenyl radical, a lower alkyl or aralkyl radical which may be substituted, or a radical represented by the formula--(CH.sub.2).sub.n COR.sup.8 (II)in which n is an integer from 0 to 4 and R.sup.8 is a hydrogen atom, a lower alkoxy radical, or an amino, lower alkyl or aryl radical which may be substituted, as well as pharmaceutically acceptable salts thereof, and hydrates or solvates of the compounds of the formula I or their salts.Also included is a process for the manufacture of these compounds, pharmaceutical preparations containing them, intermediates useful in said process, and methods of using them. The end products have antimicrobial activity.

摘要翻译： 本发明涉及式（I）的三环化合物，其中R 1是氢原子或羧基保护基; R2是氢原子或可被卤素原子取代的低级烷基; R3和R4独立地是氢原子或可以被羟基或取代或未取代的氨基取代的低级烷基; X是卤原子; R5和R6独立地是氢原子或可被羟基，低级烷氧基或取代或未取代的氨基取代的低级烷基; 或R 5和R 6与相邻的氮原子一起形成可以在一个或多个碳原子上被一个或多个取代基取代的5至7元杂环，杂环还可以含有-NR 7 - ， - -O - ， - S - ， - SO - ， - SO 2 - 或-NR 7 -CO-，并且R 7是氢原子，可以被取代的低级烯基，低级烷基或芳烷基或表示 其中n为0至4的整数，R8为氢原子，低级烷氧基或氨基，可被取代的低级烷基或芳基，以及 - （CH 2）n COR 8（II） 其药学上可接受的盐，以及式I化合物或其盐的水合物或溶剂化物。 还包括制备这些化合物的方法，含有它们的药物制剂，可用于所述方法的中间体以及使用它们的方法。 最终产品具有抗菌活性。