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    Penicillin derivatives
    2.
    发明授权
    Penicillin derivatives 失效
    青霉素衍生物

    公开(公告)号：US4529592A

    公开(公告)日：1985-07-16

    申请号：US501560

    申请日：1983-06-06

    申请人： Ronald G. Micetich ,  Shigeru Yamabe ,  Tomio Yamazaki ,  Naobumi Ishida ,  Takeshi Ishizawa

    发明人： Ronald G. Micetich ,  Shigeru Yamabe ,  Tomio Yamazaki ,  Naobumi Ishida ,  Takeshi Ishizawa

    IPC分类号： C07D499/87 ,  A61K31/425 ,  A61K31/43 ,  A61P31/04 ,  A61P43/00 ,  C07D499/00 ,  C07D499/86 ,  C07D499/897 ,  C07F7/10

    CPC分类号： C07D499/00 ,  C07F7/10

    摘要： 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.

    摘要翻译： 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。

    Penicillin derivatives
    3.
    发明授权
    Penicillin derivatives 失效
    青霉素衍生物

    公开(公告)号：US4496484A

    公开(公告)日：1985-01-29

    申请号：US487557

    申请日：1983-04-22

    申请人： Ronald G. Micetich ,  Shigeru Yamabe ,  Shoji Hirata ,  Naobumi Ishida

    发明人： Ronald G. Micetich ,  Shigeru Yamabe ,  Shoji Hirata ,  Naobumi Ishida

    IPC分类号： C07D499/00 ,  A61K31/425

    CPC分类号： C07D499/00

    摘要： This invention provides a penicillin derivative of the formula and a salt thereof ##STR1## wherein X represents chlorine atom or bromine atom and R represents hydrogen atom or penicillin carboxy-protecting radical, and a process for preparing the derivative of the formula (I) and a salt thereof by reacting a compound of the formula ##STR2## wherein R is as defined above with a chlorinating reagent or brominating reagent and, when required, forming a salt thereof.

    摘要翻译： 本发明提供一种下式的青霉素衍生物及其盐，其中X表示氯原子或溴原子，R表示氢原子或青霉素羧基保护基，以及制备式（I）的衍生物的方法 I）化合物及其盐，其中R为如上定义的式的化合物与氯化试剂或溴化试剂反应，并且当需要时，形成其盐。

    Penicillin derivatives
    4.
    发明授权
    Penicillin derivatives 失效
    青霉素衍生物

    公开(公告)号：US4668514A

    公开(公告)日：1987-05-26

    申请号：US658373

    申请日：1984-10-05

    申请人： Ronald G. Micetich ,  Shigeru Yamabe ,  Motoaki Tanaka ,  Tomio Yamazaki ,  Naobumi Ishida ,  Makoto Kajitani

    发明人： Ronald G. Micetich ,  Shigeru Yamabe ,  Motoaki Tanaka ,  Tomio Yamazaki ,  Naobumi Ishida ,  Makoto Kajitani

    IPC分类号： C07D499/86 ,  A61K31/43 ,  C07D499/00 ,  A61K31/425

    CPC分类号： C07D499/00 ,  A61K31/43 ,  Y02P20/55

    摘要： This invention provides a penicillin derivative of the formula ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and represent hydrogen, C.sub.1-6 alkyl, C.sub.1-6 hydroxyalkyl, C.sub.3-9 acyloxyalkyl, C.sub.8-13 benzyloxyalkyl, C.sub.2-7 alkoxyalkyl, C.sub.2-7 alkoxycarbonyl, C.sub.3-8 alkenyloxycarbonyl, C.sub.3-8 alkynyloxycarbonyl, phenyl, amino, cyano, formyl, trifluoromethyl, C.sub.2-6 acyl, carbamoyl, C.sub.2-7 alkylcarbamoyl, benzyloxycarbonylamino, C.sub.2-7 alkoxycarbonylamino; and R.sub.3 is hydrogen, a group for forming a pharmaceutically acceptable salt, or a penicillin carboxyl protecting group, with the proviso that both of R.sub.1 and R.sub.2 are not hydrogen or C.sub.2-7 alkoxycarbonyl at the same time and that when one of R.sub.1 and R.sub.2 is hydrogen, the other is not C.sub.2-7 alkoxycarbonyl, or a pharmaceutically acceptable acid addition salt, process for preparing the derivative, and a pharmaceutical composition containing the derivative.

    摘要翻译： 本发明提供了一种下式的青霉素衍生物，其中R1和R2相同或不同，代表氢，C1-6烷基，C1-6羟烷基，C3-9酰氧基烷基，C8-13苄氧基烷基，C2-7烷氧基烷基， C 2-8烷氧基羰基，C 3-8烯氧基羰基，C 3-8炔氧基羰基，苯基，氨基，氰基，甲酰基，三氟甲基，C 2-6酰基，氨基甲酰基，C 2-7烷基氨基甲酰基，苄氧基羰基氨基，C 2-7烷氧基羰基氨基; 并且R 3是氢，用于形成药学上可接受的盐的基团或青霉素羧基保护基，条件是R 1和R 2同时不是氢或C 2-7烷氧基羰基，并且当R 1和R 2之一 是氢，另一个不是C 2-7烷氧基羰基，或其药学上可接受的酸加成盐，制备衍生物的方法和含有该衍生物的药物组合物。

    Penicillin derivatives
    5.
    发明授权
    Penicillin derivatives 失效
    青霉素衍生物

    公开(公告)号：US4562073A

    公开(公告)日：1985-12-31

    申请号：US519491

    申请日：1983-08-01

    申请人： Ronald G. Micetich ,  Shigeru Yamabe ,  Motoaki Tanaka ,  Makoto Kajitani ,  Tomio Yamazaki ,  Naobumi Ishida

    发明人： Ronald G. Micetich ,  Shigeru Yamabe ,  Motoaki Tanaka ,  Makoto Kajitani ,  Tomio Yamazaki ,  Naobumi Ishida

    IPC分类号： C07D499/86 ,  C07D499/00 ,  C07F7/10 ,  A61K31/425

    CPC分类号： C07D499/00 ,  C07F7/10

    摘要： A penicillin derivative represented by the following formula ##STR1## wherein R.sub.1 is hydrogen or trialkylsilyl; R.sub.2 is hydrogen, trialkylsilyl or COOR.sub.2 ' wherein R.sub.2 ' is hydrogen, C.sub.1-18 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 or group for forming a pharmaceutically acceptable salt; and R.sub.3 has the same meaning as above R.sub.2 '.

    摘要翻译： 由下式（IMAGE）表示的青霉素衍生物，其中R1是氢或三烷基甲硅烷基; R2是氢，三烷基甲硅烷基或COOR2'，其中R2'是氢，C1-18烷基，C2-7烷氧基甲基，C3-8烷基羰氧基甲基，C4-9烷基羰氧基乙基，（C5-7环烷​​基）羰基氧基甲基，C9-14苄基羰氧基烷基，C3-8 烷氧基羰基甲基，C4-9烷氧基羰基乙基，苯酞基，巴豆酸内酯-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，三氯甲硅烷基，（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，C8-13苯甲酰氧基烷基或用于形成药学上可接受的盐 ; 和R3具有与上述R2'相同的含义。