申请人:Imperial Chemical Industries PLC
公开号:US04490382A1
公开(公告)日:1984-12-25
A penicillin derivative of the formula I: ##STR1## in which R.sup.1 is any one of the C-3 substituents from antibacterially-active penicillins known in the art; X is a nitrogen atom or a radical of the formula N.sup..sym. --R.sup.3 ; R.sup.2 and R.sup.3, which may be the same or different, are hydrogen atoms or 1-6C alkyl, 1-6C alkanoyl, hydroxy, 1-6C alkoxy, amino, 1-6C alkanoylamino, 1-6C alkylamino, 1-6C aminoalkyl, 1-6C hydroxyalkyl, 2-6C carboxyalkyl, 2-6C alkenyl, 3-6C alkoxyalkyl, 3-8C alkoxycarbonylalkyl, furylmethyl, phenyl or 7-11C phenylalkyl radicals, in the latter two of which the phenyl ring is optionally substituted by a halogen atom or by a methyl, methoxy, nitro, hydroxy, amino, carboxy or methoxy-carbonyl radical; A< is a radical of the formula II or III: ##STR2## in which R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are as described in the specification; and the pharmaceutically-acceptable acid- or base-addition salts thereof. Pharmaceutical compositions and manufacturing processes are also described.
公式I的青霉素衍生物:##STR1## 其中R.sup.1是艺术上已知的具有抗菌活性的青霉素的C-3取代基之一; X是一个氮原子或公式N.sup..sym. --R.sup.3的基团; R.sup.2和R.sup.3可以相同也可以不同,是氢原子或1-6C烷基,1-6C烷酰基,羟基,1-6C烷氧基,氨基,1-6C烷酰胺基,1-6C烷基氨基,1-6C氨基烷基,1-6C羟基烷基,2-6C羧基烷基,2-6C烯基,3-6C烷氧基烷基,3-8C烷氧羰基烷基,呋喃甲基,苯基或7-11C苯基烷基基团,在后两个基团中,苯环可以选择性地被卤素原子或甲基,甲氧基,硝基,羟基,氨基,羧基或甲氧羰基基团取代; A<是公式II或III的基团:##STR2## 其中R.sup.4,R.sup.5,R.sup.6,R.sup.7,R.sup.8和R.sup.9如说明书中所述;以及其药学上可接受的酸或碱盐。同时还描述了制药组合物和制造工艺。