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    Penicillins
    1.
    发明授权
    Penicillins 失效
    PENICILLINS

    公开(公告)号：US4001218A

    公开(公告)日：1977-01-04

    申请号：US547208

    申请日：1975-02-05

    申请人： Gunter Schmidt ,  Karl Georg Metzger

    发明人： Gunter Schmidt ,  Karl Georg Metzger

    IPC分类号： C07D499/00 ,  C07D499/64 ,  C07D499/68 ,  C07D499/70

    CPC分类号： C07D499/00

    摘要： Penicillins of the formula: ##SPC1##And their pharmaceutically acceptable nontoxic salts whereinR.sub.1 is hydrogen, halogen, lower alkyl, hydroxy, nitro or A-NH; ##EQU1## wherein R.sub.3 is hydrogen; lower alkyl; halo-(lower alkyl); cycloalkyl of 3 to 11 carbon atoms, unsubstituted or substituted by hydroxy or alkyl of 1 or 2 carbon atoms; cycloalkenyl of 3 to 11 carbon atoms; bicycloalkyl of up to 8 carbon atoms; bicycloalkenyl of up to 8 carbon atoms; aryl of 6 to 10 carbon atoms, unsubstituted or substituted by 1 to 3 substituents selected from the group consisting of alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen, trifluoromethyl, nitro, amino, alkylsulphonyl of 1 to 4 carbon atoms, and methylenedioxy azidoaryl of 6 to 10 carbon atoms, azido-(lower alkyl); amino; or thienyl;R.sub.4 is lower alkylamino or arylamino of 6 to 10 carbon atoms;B is a direct bond; CH.sub.2 ; S--CH.sub.2 ; CH=CH; or CO--NH--CH.sub.2 ;E is phenyl or phenyl or thenyl, substituted by hydroxy, azido, lower alkyl, lower alkoxy, lower alkylthio or chlorine; andC* is an asymmetric carbon atom,Are useful for their antibacterial activity against both Gram-positive and Gram-negative bacteria.

    Penicillins
    2.
    发明授权
    Penicillins 失效
    青霉素

    公开(公告)号：US3982011A

    公开(公告)日：1976-09-21

    申请号：US585890

    申请日：1975-06-11

    申请人： Gunter Schmidt ,  Karl Georg Metzger

    发明人： Gunter Schmidt ,  Karl Georg Metzger

    IPC分类号： C07D499/00 ,  C07D499/64 ,  C07D499/68 ,  C07D499/70

    CPC分类号： C07D499/00

    摘要： Penicillins of the formula: ##SPC1##And their pharmaceutically acceptable nontoxic salts whereinR.sub.1 is hydrogen, halogen, lower alkyl, hydroxy, nitro or A--NH;A is R.sub.2, ##EQU1## wherein R.sub.2 is hydrogen, lower alkyl or arylsulphenyl of 6 to 10 carbon atoms;R.sub.3 is hydrogen; lower alkyl; halo-(lower alkyl); cycloalkyl of 3 to 11 carbon atoms, unsubstituted or substituted by hydroxy or alkyl of 1 or 2 carbon atoms; cycloalkenyl of 3 to 11 carbon atoms; bicycloalkyl of up to 8 carbon atoms; bicycloalkenyl of up to 8 carbon atoms; aryl of 6 to 10 carbon atoms, unsubstituted or substituted by 1 to 3 substituents selected from the group consisting of alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen, trifluoromethyl, nitro, amino, alkylsulphonyl of 1 to 4 carbon atoms, and methylenedioxy; azidoaryl of 6 to 10 carbon atoms, azido-(lower alkyl); amino; or thienyl;R.sub.4 is lower alkylamino or arylamino of 6 to 10 carbon atoms;B is a direct bond; CH.sub.2 ; S--CH.sub.2 ; CH=CH; or CO--NH--CH.sub.2 ;E is phenyl or phenyl or thenyl, substituted by hydroxy, azido, lower alkyl, lower alkoxy, lower alkylthio or chlorine; andC* is an asymmetric carbon atom,Are useful for their antibacterial activity against both Gram-positive and Gram-negative bacteria.

    摘要翻译： 青霉素的配方：

    Penicillins
    3.
    发明授权
    Penicillins 失效

    公开(公告)号：US3931153A

    公开(公告)日：1976-01-06

    申请号：US419950

    申请日：1973-11-29

    申请人： Gunter Schmidt ,  Karl Georg Metzger

    发明人： Gunter Schmidt ,  Karl Georg Metzger

    IPC分类号： C07D499/66 ,  A23K20/195 ,  A61K31/43 ,  A61P31/04 ,  C07D249/18 ,  C07D317/68 ,  C07D333/38 ,  C07D409/04 ,  C07D499/00 ,  C07D499/64 ,  C07D499/68 ,  C07D499/70 ,  C07D499/44

    CPC分类号： C07D333/38 ,  C07D249/18 ,  C07D317/68 ,  C07D499/00

    摘要： Penicillins of the formula: ##SPC1##And their pharmaceutically acceptable nontoxic salts whereinR.sub.1 is hydrogen, halogen, lower alkyl, hydroxy, nitro or A--NH;A is ##EQU1## wherein R.sub.3 is hydrogen; lower alkyl; halo-(lower alkyl); cycloalkyl of 3 to 11 carbon atoms, unsubstituted or substituted by hydroxy or alkyl of 1 or 2 carbon atoms; cycloalkenyl of 3 to 11 carbon atoms; bicycloalkyl of up to 8 carbon atoms; bicycloalkenyl of up to 8 carbon atoms; aryl of 6 to 10 carbon atoms, unsubstituted or substituted by 1 to 3 substituents selected from the group consisting of alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen, trifluoromethyl, nitro, amino, alkylsulphonyl of 1 to 4 carbon atoms, and methylenedioxy; azidoaryl of 6 to 10 carbon atoms, azido-(lower alkyl); amino; or thienyl;R.sub.4 is lower alkylamino or arylamino of 6 to 10 carbon atoms;B is a direct bond; CH.sub.2 ; S--CH.sub.2 ; CH=CH; or CO--NH--CH.sub.2 ;E is phenyl or phenyl or thenyl, substituted by hydroxy, azido, lower alkyl, lower alkoxy, lower alkylthio or chlorine; andC* is an asymmetric carbon atom,Are useful for their antibacterial activity against both Gram-positive and Gram-negative bacteria.

    Antibacterial compositions containing a 4-amino-pyrimido-(4,5,b)-quinoxaline-5,10-dioxide and method of using same
    7.
    发明授权
    Antibacterial compositions containing a 4-amino-pyrimido-(4,5,b)-quinoxaline-5,10-dioxide and method of using same 失效
    含有4-氨基 - 嘧啶并 - （4,5，b） - 喹喔啉-5,10-二氧化物的抗菌组合物及其使用方法

    公开(公告)号：US3985879A

    公开(公告)日：1976-10-12

    申请号：US511175

    申请日：1974-10-02

    申请人： Florin Seng ,  Kurt Ley ,  Karl Georg Metzger

    发明人： Florin Seng ,  Kurt Ley ,  Karl Georg Metzger

    IPC分类号： A23K1/16 ,  A61K31/505

    CPC分类号： A23K20/116

    摘要： 4-amino-pyrimido-(4,5,b)-quinoxaline-5,10-dioxides of the formula: ##SPC1##WhereinR is hydrogen, a straight or branched chain saturated or partially unsaturated substituted or unsubstituted aliphatic moiety or a substituted or unsubstituted cycloaliphatic moiety, are produced by reacting quinoxaline-di-N-oxide of the formula: ##SPC2##With an amine of the general formula R--NH.sub.2, wherein R is as defined, above, in a diluent, at a temperature in the range of 20.degree. to 100.degree. C.These compounds are useful for their antimicrobial activity. They exhibit activity against both gram positive and gram negative bacteria.

    摘要翻译： 4-氨基 - 嘧啶并 - （4,5，b） - 喹喔啉-5,10-二氧化物，其结构如下：