申请人:F. HOFFMANN-LA ROCHE AG
公开号:EP0409081A1
公开(公告)日:1991-01-23
β-Lactam compounds of the formula
in which R₁ is a cyclic or secondary acyclic amino group which independently has antibacterial activity;
R₂ is hydrogen, lower alkoxy, lower alkylthio or formamido;
R₃ is hydrogen or an organic group bonded through carbon, oxygen, sulfur or nitrogen;
R₄ is an electronegative acidic group; or R₃ and R₄ together form a heterocycle; and
R₅ is hydrogen or lower alkyl, except when R₃ and R₄ form a heterocycle, in which case R₅ is hydrogen only;
and readily hydrolyzable esters and pharmaceutically acceptable salts of these compounds, and hydrates of any of the foregoing.
The products have antibacterial activity.
式中β-内酰胺化合物
其中 R₁ 是独立具有抗菌活性的环状或仲间无环氨基;
R₂ 是氢、低级烷氧基、低级烷硫基或甲酰胺基;
R₃ 是氢或通过碳、氧、硫或氮键合的有机基团;
R₄ 是电负性酸性基团;或 R₃ 和 R₄ 共同形成杂环;以及
R₅ 是氢或低级烷基,除非 R₃ 和 R₄ 构成杂环,在这种情况下,R₅ 仅是氢;
以及这些化合物的易水解酯和药学上可接受的盐,以及上述任何一种化合物的水合物。
这些产品具有抗菌活性。