申请人:Bristol-Myers Squibb Company
公开号:US05126336A1
公开(公告)日:1992-06-30
This invention relates to novel cephalosporin derivatives of the formula ##STR1## wherein R.sup.1 is hydrogen, a straight, branched, or cyclic lower alkyl group having up to six carbon atoms or a radical of the formula ##STR2## in which R.sup.3 and R.sup.4 are each independently hydrogen, methyl or ethyl, or R.sup.3 and R.sup.4, taken together with the carbon atom to which they are attached, may be a cycloalkylidene ring containing from 3 to 5 carbon atoms; R.sup.2 is a radical selected from the group consisting of ##STR3## wherein R.sup.5 is hydrogen or acetyl; R.sup.6, R.sup.7 and R.sup.8 each are independently C.sub.1-5 alkyl; n is 1 or 2; and y is 1 to 5. In another aspect, this invention relates to compounds of formula I and their nontoxic pharmaeutically acceptable salts, physiologically hydrolyzable esters or solvates. Representative compounds of this invention were selected for testing and were shown to display potent antibacterial activity.
本发明涉及一种新型头孢菌素衍生物,其化学式为##STR1##其中R.sup.1为氢,直链、支链或环状低碳原子烷基,碳原子数最多为6,或者为式子##STR2##中的基团,其中R.sup.3和R.sup.4各自独立地为氢、甲基或乙基,或者R.sup.3和R.sup.4与它们所连接的碳原子一起,可以是含有3到5个碳原子的环状烷基;R.sup.2是从##STR3##所选的基团,其中R.sup.5为氢或乙酰基;R.sup.6、R.sup.7和R.sup.8各自独立地为C.sub.1-5烷基;n为1或2;y为1到5。在另一个方面,本发明涉及化合物I及其无毒的药学上可接受的盐、生理水解酯或溶剂化合物。本发明的代表性化合物经过测试显示出强大的抗菌活性。