会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 5. 发明授权
    • 7.alpha.-Methoxycephalosporin derivatives and their pharmaceutical
compositions having antibacterial activity
    • 7α-甲氧基头孢菌素衍生物及其具有抗菌活性的药物组合物
    • US4247548A
    • 1981-01-27
    • US28707
    • 1979-04-10
    • Masafumi YoshimotoHachio MiyazawaTakuzo NishimuraAkiko AndoNorio NakamuraHideo Nakao
    • Masafumi YoshimotoHachio MiyazawaTakuzo NishimuraAkiko AndoNorio NakamuraHideo Nakao
    • A61K31/545A61K31/546A61P31/04C07D261/12C07D501/57
    • C07D261/12Y02P20/55
    • 7.alpha.-Methoxycephalosporin derivatives of general formula (I): ##STR1## wherein: R.sup.1 represents a hydroxy group; a C.sub.1 -C.sub.4 alkoxy group; a C.sub.2 -C.sub.5 aliphatic acyloxy group; a benzoyloxy group which is unsubstituted or has one or more C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, nitro or halogen substituents; a benzenesulphonyloxy group which is unsubstituted or has one or more C.sub.1 -C.sub.4 alkyl substituents; or a C.sub.1 -C.sub.3 alkanesulphonyloxy group which is unsubstituted or has one or more C.sub.1 -C.sub.3 alkoxy, cyano, nitro, halogen or C.sub.2 -C.sub.4 alkoxycarbonyl substituents;R.sup.2 represents a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, a halogen atom, a carboxyl group, a C.sub.2 -C.sub.5 alkoxycarbonyl group, a carbamoyl group, an alkylcarbamoyl group in which the alkyl moiety has from 1 to 3 carbon atoms, a di(C.sub.1 -C.sub.3 alkyl)carbamoyl group or a cyano group;R.sup.3 represents a hydrogen atom; an acetoxy group; a carbamoyloxy group; or a tetrazolylthio, thiadiazolylthio or oxadiazolylthio group which is unsubstituted or has one or more C.sub.1 -C.sub.3 alkyl, sulphomethyl or di(C.sub.1 or C.sub.2 alkyl)amino(C.sub.1 -C.sub.3 alkyl) substituents;m is 0 or 1; andn is 0 or 2exhibit potent antibacterial activity and are thus useful as medicines. The derivatives can be prepared by reacting the corresponding 7.alpha.-methoxycephalosporin derivative having an amino group at the 7.beta.-position with an acid halide corresponding to the substituted acetyl group which it is desired to attach to the amino group at the 7.beta.-position or by reacting Cephamycin C with the same acid halide.
    • 7,通式(I)的α-甲氧基头孢菌素衍生物:其中:R1表示羟基; C1-C4烷氧基; C2-C5脂族酰氧基; 未取代或具有一个或多个C 1 -C 4烷基,C 1 -C 4烷氧基,硝基或卤素取代基的苯甲酰氧基; 未取代或具有一个或多个C 1 -C 4烷基取代基的苯磺酰氧基; 或未取代或具有一个或多个C 1 -C 3烷氧基,氰基,硝基,卤素或C 2 -C 4烷氧羰基取代基的C 1 -C 3烷磺酰氧基; R2表示氢原子,C1-C4烷基,卤素原子,羧基,C2-C5烷氧基羰基,氨基甲酰基,烷基部分具有1至3个碳原子的烷基氨基甲酰基,二 (C 1 -C 3烷基)氨基甲酰基或氰基; R3表示氢原子; 乙酰氧基; 氨基甲酰氧基; 或未取代的或具有一个或多个C 1 -C 3烷基,磺基甲基或二(C 1或C 2烷基)氨基(C 1 -C 3烷基)取代基的四唑基硫代噻二唑基硫代或恶二唑基硫基; m为0或1; n为0或2表示有效的抗菌活性,因此可用作药物。 衍生物可以通过使7β位具有氨基的相应的7α-甲氧基头孢菌素衍生物与对应于取代的乙酰基的酰基卤反应而制备,希望在7β位上附着氨基 或通过使Cephamycin C与相同的酰卤反应。