申请人:ICI Pharma
公开号:US05017569A1
公开(公告)日:1991-05-21
Cephalosporin compounds having a 3-position substituent of the formula (I) are described: --CH.sub.2 --Y--Q (I) wherein Y is a linking group --NR.sup.4 CO--Y'--, --NR.sup.4 SO.sub.2 --Y'--, --OCO--Y;-- or --SCO--Y'-- wherein R.sup.4 is hydrogen, various optionally substituted alkyl groups or alkenyl and Y' is a bond or various optionally substituted alkylene or alkenylene groups; and Q is a benzene ring (optionally fused to a further benzene ring so forming a naphthyl group or optionally fused to a 5 or 6 membered heterocyclic aromatic group containing 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur), said benzene ring (or in the case of naphthyl either benzene ring) being substituted by groups R.sup.1 and R.sup.2 which are ortho with respect to one another, wherein R.sup.1 is hydroxy or an in vivo hydrolyzable ester thereof and R.sup.2 is hydroxy, an in vivo hydrolyzable ester thereof, carboxy, sulpho, hydroxymethyl, methanesulphonamido or ureido; or Q is a group of the formula (II) or (III): ##STR1## wherein M is oxygen or a group NR.sup.3 wherein R.sup.3 is hydrogen or C.sub.1-4 alkyl; ring Q being further optionally substituted. The use of such compounds as antibacterial agents is described as are processes for their preparation and intermediates therefor.
头孢菌素化合物具有式(I)的3位取代基,描述如下:--CH.sub.2 --Y--Q (I)其中Y是连接基--NR.sup.4 CO--Y'--,--NR.sup.4 SO.sub.2 --Y'--,--OCO--Y;--或--SCO--Y'--其中R.sup.4是氢,各种可选择取代的烷基或烯基,Y'是键或各种可选择取代的亚烷基或烯基基团;Q是苯环(可选择与另一苯环融合形成萘基或可选择与含有1、2或3个异原子(从氮、氧和硫中选择)的5或6成员杂环芳基团融合),所述苯环(或在萘基的情况下是任一苯环)被基团R.sup.1和R.sup.2取代,这些基团与彼此相对位,其中R.sup.1是羟基或其体内可水解酯,R.sup.2是羟基,其体内可水解酯,羧基,磺酸基,羟甲基,甲磺酰胺基或脲基;或Q是式(II)或(III)的基团:##STR1##其中M是氧或基团NR.sup.3,其中R.sup.3是氢或C.sub.1-4烷基;环Q进一步可选择取代。描述了这类化合物作为抗菌剂的用途,以及它们的制备方法和中间体。