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    • 12. 发明授权
    • Penicillin derivatives
    • 青霉素衍生物
    • US4529592A
    • 1985-07-16
    • US501560
    • 1983-06-06
    • Ronald G. MicetichShigeru YamabeTomio YamazakiNaobumi IshidaTakeshi Ishizawa
    • Ronald G. MicetichShigeru YamabeTomio YamazakiNaobumi IshidaTakeshi Ishizawa
    • C07D499/87A61K31/425A61K31/43A61P31/04A61P43/00C07D499/00C07D499/86C07D499/897C07F7/10
    • C07D499/00C07F7/10
    • A penicillin derivative represented by the following formula ##STR1## wherein R.sub.1 and R.sub.2 are each the same or different and represent hydrogen, C.sub.1-18 alkyl, mononitro-substituted benzyl or group for forming a pharmaceutically acceptable salt and R.sub.3 is selected from the group consisting of hydrogen, C.sub.1-6 alkyl, C.sub.2-7 alkoxymethyl, C.sub.3-8 alkylcarbonyloxymethyl, C.sub.4-9 alkylcarbonyloxyethyl, (C.sub.5-7 cycloalkyl)carbonyloxymethyl, C.sub.9-14 benzylcarbonyloxyalkyl, C.sub.3-8 alkoxycarbonylmethyl, C.sub.4-9 alkoxycarbonylethyl, phthalidyl, crotonolacton-4-yl, .gamma.-butyrolacton-4-yl, halogenated C.sub.1-6 alkyl substituted with 1 to 3 halogen atoms, C.sub.1-6 alkoxy- or nitro-substituted or unsubstituted benzyl, benzhydryl, tetrahydropyranyl, dimethylaminoethyl, dimethylchlorosilyl, trichlorosilyl, (5-substituted C.sub.1-6 alkyl or phenyl or unsubstituted-2-oxo-1,3-dioxoden-4-yl)methyl, C.sub.8-13 benzoyloxyalkyl and group for forming a pharmaceutically acceptable salt.
    • 由下式(IMAGE)表示的青霉素衍生物,其中R 1和R 2各自相同或不同,表示氢,C 1-18烷基,一硝基取代的苄基或用于形成药学上可接受的盐的基团,R 3选自 氢,C 1-6烷基,C 2-7烷氧基甲基,C 3-8烷基羰基氧基甲基,C 4-9烷基羰基氧基乙基,(C 5-7环烷​​基)羰基氧基甲基,C 9-14苄基羰氧基烷基,C 3-8烷氧基羰基甲基,C 4-9烷氧基羰基乙基, 吡啶-4-基,γ-丁内酯-4-基,被1至3个卤素原子取代的卤代C 1-6烷基,C 1-6烷氧基或硝基取代或未取代的苄基,二苯甲基,四氢吡喃基,二甲基氨基乙基,二甲基氯甲硅烷基,三氯硅烷基(5 取代的C 1-6烷基或苯基或未取代的-2-氧代-1,3-二氧杂环己烯-4-基)甲基,C 13-13苯甲酰氧基烷基和用于形成药学上可接受的盐的基团。