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    Cephalosporin and pharmaceutical preparations containing the same
    4.
    发明授权
    Cephalosporin and pharmaceutical preparations containing the same 失效
    头孢菌素和含有相同的药物制剂

    公开(公告)号：US3935204A

    公开(公告)日：1976-01-27

    申请号：US340673

    申请日：1973-03-13

    申请人： Sven Erik Dahlen ,  Bertil Ake Ekstrom ,  Odon Kalman Jozsef Kovacs ,  Berndt Olof Harald Sjoberg

    发明人： Sven Erik Dahlen ,  Bertil Ake Ekstrom ,  Odon Kalman Jozsef Kovacs ,  Berndt Olof Harald Sjoberg

    IPC分类号： C07D501/36 ,  A61K31/51 ,  A61K31/545 ,  C07D499/21 ,  C07D501/02 ,  C07D501/04 ,  C07D501/16 ,  C07D501/20 ,  C07D501/24

    CPC分类号： C07D501/04 ,  C07D499/21 ,  Y02P20/55

    摘要： New esters of cephalosporins of the formula ##EQU1## wherein R.sup.1 is a substituted or unsubstituted alkyl, cycloalkyl, aryl or heterocyclic group, R.sup.2 is S--R.sup.4 wherein R.sup.4 is a methyl, ethyl, benzyl or heterocyclic group, a xanthate, dithiocarbamate, thiouronium, azido, alkoxy, hydrogen, substituted or unsubstituted alkanoyloxy, carbonyloxy or 1-pyridinium group, R.sup.3 is ##EQU2## wherein R.sup.5 is hydrogen, methyl or ethyl, X.sup.2 is O or NH, R.sup.6 is a basic group, R.sup.7 is a substituted or unsubstituted alkyl, cycloalkyl, aryl, aralkyl or heterocyclic group, X.sup.1 is O or S, Y.sup.1 is hydrogen, a hydroxy, alkyloxycarbonyl, halogen, azido, a substituted or unsubstituted amino group, a carboxyl group, the group --COOR.sup.3, or a nitrite group, n is 0 or 1 and m is 0 or 1, useful as active ingredients of pharmaceutical preparations; processes for their preparation; and methods for the treatment of infectious diseases.

    摘要翻译： 新的式S的头孢菌素S ANGLE R1-（X1）n-CH-CO-NH-CH-CHCH2 ||| Y2CO-NCH2-R2 m ANGLE C | COOR3其中R1是取代或未取代的烷基，环烷基， 芳基或杂环基，R2是S-R4，其中R4是甲基，乙基，苄基或杂环基，黄原酸酯，二硫代氨基甲酸酯，硫脲，叠氮基，烷氧基，氢，取代或未取代的烷酰氧基，羰基氧基或1-吡啶鎓基，R3是 CH3OC2H5OR5O |并行的|并行的|平行的-CH-OC-R6，-CH-OC-R6，-CH-X2-C-OR7，其中R5是氢，甲基或乙基，X2是O或NH，R6是碱性基团， R7是取代或未取代的烷基，环烷基，芳基，芳烷基或杂环基，X1是O或S，Y1是氢，羟基，烷氧基羰基，卤素，叠氮基，取代或未取代的氨基，羧基， COOR3或亚硝酸酯基，n为0或1，m为0或1，可用作药物制剂的活性成分; 其准备过程; 以及治疗感染性疾病的方法。

    HIGH PENETRATION PRODRUG COMPOSITIONS OF ANTIMICROBIALS AND ANTIMICROBIAL-RELATED COMPOUNDS
    5.
    发明申请
    HIGH PENETRATION PRODRUG COMPOSITIONS OF ANTIMICROBIALS AND ANTIMICROBIAL-RELATED COMPOUNDS 审中-公开

    公开(公告)号：US20180222921A1

    公开(公告)日：2018-08-09

    申请号：US15947983

    申请日：2018-04-09

    申请人： Techfields Pharma Co., Ltd.

    发明人： Chongxi YU ,  Lina XU ,  Yuhua CHEN ,  Binbing YAN ,  Shiqian TU

    IPC分类号： C07D499/21

    CPC分类号： C07D499/21

    摘要： The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of antimicrobials and antimicrobial-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

    6-substituted penicillanic acid and derivatives thereof
    7.
    发明授权
    6-substituted penicillanic acid and derivatives thereof 失效
    6-取代的槟榔酸及其衍生物

    公开(公告)号：US3855233A

    公开(公告)日：1974-12-17

    申请号：US18364271

    申请日：1971-09-24

    申请人： SQUIBB & SONS INC

    发明人： DOLFINI J ,  BOHME E ,  SLUSARCHYK W

    IPC分类号： C07D499/21 ,  C07D499/42 ,  C07D99/14

    CPC分类号： C07D499/42 ,  C07D499/21

    摘要： Disclosed herein are penicillanic acids and derivatives thereof which are substituted in the 6-position, processes for preparing such compounds and the utility thereof. The compounds of the invention have been found to be useful as antibacterial agents.

    摘要翻译： 本文公开了在6-位取代的青霉烷酸及其衍生物，制备这些化合物的方法及其用途。 已经发现本发明的化合物可用作抗菌剂。

    High penetration prodrug compositions of antimicrobials and antimicrobial-related compounds
    8.
    发明授权
    High penetration prodrug compositions of antimicrobials and antimicrobial-related compounds 有权

    公开(公告)号：US09969751B2

    公开(公告)日：2018-05-15

    申请号：US13323556

    申请日：2011-12-12

    申请人： Chongxi Yu ,  Lina Xu ,  Yuhua Chen ,  Binbing Yan ,  Shiqian Tu

    发明人： Chongxi Yu ,  Lina Xu ,  Yuhua Chen ,  Binbing Yan ,  Shiqian Tu

    IPC分类号： C07D499/21

    CPC分类号： C07D499/21

    摘要： The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of antimicrobials and antimicrobial-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.