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    Thio-.beta.-lactam penicillins
    3.
    发明授权
    Thio-.beta.-lactam penicillins 失效
    Thio- {62-内酰胺青霉素

    公开(公告)号：US3971776A

    公开(公告)日：1976-07-27

    申请号：US551221

    申请日：1975-02-19

    申请人： Christopher M. Cimarusti ,  Paul Wojtkowski ,  Joseph E. Dolfini

    发明人： Christopher M. Cimarusti ,  Paul Wojtkowski ,  Joseph E. Dolfini

    IPC分类号： C07D499/00 ,  C07D499/44 ,  C07D499/46 ,  C07D499/48

    CPC分类号： C07D499/00

    摘要： Thio-.beta.-lactam penicillins of the general formula ##EQU1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, trihaloethyl, alkali metal or alkaline earth metal; R.sub.1 is hydrogen, lower alkyl, cycloalkyl, phenyl, lower alkoxyphenyl, phenoxy, phenyl-lower alkyl or certain heterocyclic groups; R.sub.2 is hydrogen, amino, carboxy or ureido; and n is 0 or 1; are useful as antimicrobial agents.

    摘要翻译： 通式R2 | R1-CHn-CO-NH的硫代-β-内酰胺青霉素，其中R是氢，低级烷基，苯基 - 低级烷基，三卤代乙基，碱金属或碱土金属; R 1是氢，低级烷基，环烷基，苯基，低级烷氧基苯基，苯氧基，苯基 - 低级烷基或某些杂环基; R2是氢，氨基，羧基或脲基; 并且n为0或1; 作为抗微生物剂是有用的。

    NANOPARTICLES OF BETA-LACTAM DERIVATIVES
    5.
    发明申请
    NANOPARTICLES OF BETA-LACTAM DERIVATIVES 审中-公开
    BETA-LACTAM衍生物的纳米颗粒

    公开(公告)号：US20110269731A1

    公开(公告)日：2011-11-03

    申请号：US13126756

    申请日：2009-10-28

    申请人： Patrick Couvreur ,  Didier Demaele ,  Fatima Zouhiri

    发明人： Patrick Couvreur ,  Didier Demaele ,  Fatima Zouhiri

    IPC分类号： A61K31/43 ,  C07D499/48 ,  A61P31/04 ,  B82Y5/00 ,  B82Y99/00 ,  B82Y40/00

    CPC分类号： A61K47/54

    摘要： The present invention relates to a complex made up of at least one beta-lactam molecule covalently bonded to at least one hydrocarbon radical including at least 18 carbon atoms and containing at least one unit of 2-methyl-buta-2-ene, to nanoparticles of said complexes, and to a method for preparing same, said complex and/or said nanoparticles optionally being in the form of a lyophilisate. The present invention also relates to a pharmaceutical composition including at least said complex and/or said nanoparticles. The invention finally relates to said complex and/or to said nanoparticles for the treatment and/or prevention of bacterial infections, in particular caused by strains that are sensitive to beta-lactams.

    摘要翻译： 本发明涉及一种由至少一种共价结合至少一个包含至少18个碳原子并含有至少一个2-甲基丁-2-烯单元的烃基的β-内酰胺分子与纳米颗粒组成的复合物 的所述复合物，以及其制备方法，所述复合物和/或所述纳米颗粒任选地为冻干物形式。 本发明还涉及包含至少所述复合物和/或所述纳米颗粒的药物组合物。 本发明最终涉及用于治疗和/或预防细菌感染的所述复合物和/或所述纳米颗粒，特别是由对β-内酰胺类敏感的菌株引起的。

    Beta-lactamase inhibitor prodrug
    6.
    发明申请
    Beta-lactamase inhibitor prodrug 失效
    β-内酰胺酶抑制剂前药

    公开(公告)号：US20040110740A1

    公开(公告)日：2004-06-10

    申请号：US10648408

    申请日：2003-08-25

    申请人： Pfizer Inc

    发明人： Anthony Marfat ,  Dale G. McLeod

    IPC分类号： A61K031/43 ,  C07D499/48

    CPC分类号： C07D499/00

    摘要： Prodrugs of 6-null-hydroxymethylpenicillanic acid sulfone having the structure 1 wherein R is H or methyl, and solvates thereof, are disclosed. Also disclosed are pharmaceutical compositions comprising a prodrug of the present invention or a solvate thereof, an optional beta-lactam antibiotic and a pharmaceutically acceptable excipient. Further disclosed is a method for increasing the therapeutic effectiveness of a beta-lactam antibiotic in a mammal by administering an effective amount of a beta-lactam antibiotic and an effectiveness-increasing amount of a prodrug of the present invention, or a solvate thereof. Additionally disclosed is a method for treating a bacterial infection in a mammal by administering a therapeutically effective amount of a pharmaceutical composition of the present invention to a mammal in need thereof.

    摘要翻译： 公开了具有其中R为H或甲基的结构及其溶剂合物的6-β-羟甲基青霉烷酸砜的前药。 还公开了包含本发明的前药或其溶剂合物，任选的β-内酰胺抗生素和药学上可接受的赋形剂的药物组合物。 进一步公开的是通过施用有效量的β-内酰胺抗生素和增加有效量的本发明的前药或其溶剂化物来增加哺乳动物中β-内酰胺抗生素的治疗有效性的方法。 另外公开了通过向有需要的哺乳动物施用治疗有效量的本发明药物组合物来治疗哺乳动物细菌感染的方法。

    Bis-esters of dicarboxylic acids with amoxicillin and certain hydroxymethylpenicillanate 1,1-dioxides
    8.
    发明授权
    Bis-esters of dicarboxylic acids with amoxicillin and certain hydroxymethylpenicillanate 1,1-dioxides 失效
    二羧酸与阿莫西林和某些羟甲基青霉素1,1-二氧化物的双酯

    公开(公告)号：US4462934A

    公开(公告)日：1984-07-31

    申请号：US481108

    申请日：1983-03-31

    申请人： Vytautas J. Jasys

    发明人： Vytautas J. Jasys

    IPC分类号： C07D519/06 ,  A61K31/43 ,  A61P31/04 ,  C07D499/00 ,  C07D499/32 ,  C07D499/68 ,  C07D499/86 ,  C07D499/861 ,  C07D499/87 ,  C07D499/897 ,  C07D519/00 ,  C07D499/48

    CPC分类号： C07D499/00

    摘要： Antibacterial bis-esters of 1,4-cyclohexanedicarboxylic acids and alkane dicarboxylic acids wherein the ester moieties are derived from different alcohols; one alcohol being hydroxymethylpenicillanate 1,1-dioxide, or the 6-beta-hydroxymethyl or the 6-alpha-aminomethyl derivative thereof; and the other being 6-[D-(2-amino-2-(p-hydroxyphenyl)acetamido)]penicillanic acid (amoxicillin); and pharmaceutically acceptable salts thereof; a method for the use of said esters and their salts, and methods for their preparation.

    摘要翻译： 1,4-环己烷二羧酸和烷二羧酸的抗菌双酯，其中酯部分衍生自不同的醇; 一种醇是羟甲基青霉素1,1-二氧化物，或6-β-羟甲基或其6-α-氨基甲基衍生物; 另一个是6- [D-（2-氨基-2-（对羟基苯基）乙酰氨基）]青霉烷酸（阿莫西林）; 及其药学上可接受的盐; 所述酯及其盐的使用方法及其制备方法。

    Penicillins
    10.
    发明授权
    Penicillins 失效
    青霉素

    公开(公告)号：US4008220A

    公开(公告)日：1977-02-15

    申请号：US495914

    申请日：1974-08-08

    申请人： Hisao Tobiki ,  Hirotada Yamada ,  Iwao Nakatsuka ,  Kozo Shimago ,  Shigeru Okano ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Hiroshi Noguchi ,  Yasuko Eda

    发明人： Hisao Tobiki ,  Hirotada Yamada ,  Iwao Nakatsuka ,  Kozo Shimago ,  Shigeru Okano ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Hiroshi Noguchi ,  Yasuko Eda

    IPC分类号： C07D499/00 ,  C07D499/68 ,  C07D499/48

    CPC分类号： C07D499/00 ,  Y02P20/55

    摘要： A penicillin of the formula: ##STR1## wherein ##STR2## is a six-membered heteroaromatic ring containing 1 or 2 nitrogen atoms as the hetero atom, Y is hydrogen, lower alkanoyl or lower alkoxycarbonyl, R.sub.1 and R.sub.2 are each hydrogen, lower alkyl, lower alkanoyl, benzoyl, lower alkylmercapto, hydroxyl, mercapto, hydroxy(lower)alkyl, halogen or cyano or R.sub.1 and R.sub.2 may link together to form a lower alkylene chain which may be substituted with an oxo group, and Z is phenyl, hydroxyphenyl, lower alkyl, cyclohexadienyl, thienyl or isothiazolyl, which is prepared by reacting a compound of the formula: ##STR3## wherein Z is as defined above or its derivative with a carboxylic acid of the formula: ##STR4## wherein ##STR5## and R.sub.2 are each as defined above or its reactive derivative, if necessary, followed by hydrolysis or acylation of the resulting product and/or elimination of any protective group and which is useful as an antimicrobial agent against various gram-positive and gram-negative bacteria including Pseudomonas.

    摘要翻译： 一种下式的青霉素：其中是含有1或2个氮原子作为杂原子的六元杂芳环，Y是氢，低级烷酰基或低级烷氧基羰基，R 1和R 2各自是氢，低级烷基 ，低级烷酰基，苯甲酰基，低级烷基巯基，羟基，巯基，羟基（低级）烷基，卤素或氰基，或者R 1和R 2可以连接在一起形成可被氧代基取代的低级亚烷基链，Z是苯基， 低级烷基，环己二烯基，噻吩基或异噻唑基，其通过使下式化合物：其中Z如上所定义或其衍生物与下式的羧酸反应制备：其中和R2 各自如上所定义，或其反应性衍生物，如果需要，随后水解或酰化所得产物和/或消除任何保护基团，并且其可用作针对各种革兰氏阳性和革兰氏阴性菌的抗微生物剂，包括 uding假单胞菌