Cephem compounds, processes for their preparation and pharmaceutical compositions containing them
申请人:FUJISAWA PHARMACEUTICAL CO., LTD.
公开号:EP0027599A2
公开(公告)日:1981-04-29
New cephem compounds of the formula:
wherein R1 is amino or a protected amino group;
R2 is hydrogen, lower alkyl which may be substituted with suitable substituent(s), lower alkenyl, lower alkynyl, cyclo(lower)-alkyl, cyclo(lower)alkenyl, or O containing 5-membered heterocyclic group substituted with oxo group(s); R3 is a group of the formula:
wherein X is hydrogen or carbamoyl; and
R' is -COO-; or
R3 is 2-lower alkyl-5-oxo-6-hydroxy-2,5-dihydro-1,
2,4-triazinylthio; and
R4 is carboxy or protected carboxy, and pharmaceutically acceptable salts thereof, and process for their preparation, and also a pharmaceutical composition comprising, as an effective ingredient, the above compound in association with a pharmaceutically acceptable, substantially nontoxic carrier or excipient. The invention also relates to the inter. mediate compounds
and
and their preparation,
新的 cephem 化合物式:
其中 R1 是氨基或受保护的氨基;
R2 是氢、可被适当取代基取代的低级烷基、低级烯基、低级炔基、环(低)烷基、环(低)烯基或被氧代基取代的含 O 的 5 元杂环基团; R3 是式中的基团:
其中 X 是氢或氨基甲酰基;以及
R' 是 -COO-;或
R3 是 2-低级烷基-5-氧代-6-羟基-2,5-二氢-1、
2,4-三嗪硫基;以及
R4是羧基或受保护的羧基,及其药学上可接受的盐和制备方法,以及一种药物组合物,其有效成分包括上述化合物与药学上可接受的、基本上无毒的载体或赋形剂。本发明还涉及中间体化合物
和
及其制备、