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    2 beta-substituted-6-alkylidene penicillanic acid derivatives as beta-lactamase inhibitors
    5.
    发明申请
    2 beta-substituted-6-alkylidene penicillanic acid derivatives as beta-lactamase inhibitors 有权
    2个β-取代-6-亚烷基青霉烷酸衍生物作为β-内酰胺酶抑制剂

    公开(公告)号：US20010021706A1

    公开(公告)日：2001-09-13

    申请号：US09725611

    申请日：2000-11-29

    申请人： Research Corporation Technologies, Inc.

    发明人： John D. Buynak ,  Akireddy Srinivasa Rao ,  Venkata Ramana Doppalapudi

    IPC分类号： A61K031/655 ,  C07D499/40 ,  A61K031/43

    CPC分类号： C07D499/00

    摘要： Compound of formula I: 1 wherein R1, R2, R3, R4 and n have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting null-lactamase enzymes, for enhancing the activity of null-lactam antibiotics, and for treating null-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I, and novel intermediates useful for the synthesis of compounds of formula I.

    摘要翻译： 式I化合物：其中R1，R2，R3，R4和n具有说​​明书中定义的任何值及其药学上可接受的盐，可用于抑制β-内酰胺酶，用于增强β-内酰胺抗生素的活性， 并用于治疗哺乳动物中的β-内酰胺抗性细菌感染。 本发明还提供药物组合物，制备式I化合物的方法和可用于合成式I化合物的新中间体。

    Method and kit for detecting, or determining the quantity of, beta-lactam penicillins
    8.
    发明申请
    Method and kit for detecting, or determining the quantity of, beta-lactam penicillins 有权
    用于检测或确定β-内酰胺青霉素数量的方法和试剂盒

    公开(公告)号：US20030143653A1

    公开(公告)日：2003-07-31

    申请号：US10211411

    申请日：2002-07-31

    发明人： Robert Ivan McConnell ,  Elouard Benchikh ,  Stephen Peter Fitzgerald ,  John Victor Lamont

    IPC分类号： G01N033/554 ,  G01N033/569 ,  G01N033/53 ,  G01N033/537 ,  G01N033/543 ,  C07D499/40 ,  C07K016/44 ,  C07K014/435

    CPC分类号： C07D499/00 ,  C07K16/44 ,  G01N33/9446 ,  G01N2415/00

    摘要： The invention provides a hapten comprising a 6-nullD-null-aminoacetamidonullpenicillin derivative crosslinked at the null-amino group with a substituted or unsubstituted phenyldicarbaldehyde. In addition, the invention provides an immunogen comprising the aforementioned hapten coupled to an antigenicity-conferring carrier material, a conjugate comprising the aforementioned hapten coupled to a labelling agent, as well as, antibodies raised against the aforementioned immunogen and capable of binding with at least one structural epitope of an intact null-lactam ring. The invention further provides a method and a kit for detecting, or determining the quantity of, null-lactam antibiotics, as well as, use of the aforementioned conjugate with the aforementioned antibodies for detecting, or determining the quantity of, null-lactam antibiotics. The present invention has broad specificity across the main first generation null-lactams and can be used to test milk and meat and the like for the presence of residual null-lactam antibiotics.

    摘要翻译： 本发明提供了包含在α-氨基与交联的取代或未取代的苯基二甲醛的6- [D-α-氨基乙酰胺基]青霉素衍生物的半抗原。 此外，本发明提供了一种免疫原，其包含与产生抗原性的载体材料偶联的上述半抗原，包含与标记试剂偶联的上述半抗原的缀合物，以及针对上述免疫原产生并能够至少结合的抗体 完整β-内酰胺环的一个结构表位。 本发明还提供了用于检测或确定β-内酰胺抗生素的量的方法和试剂盒，以及上述与上述抗体结合物用于检测或确定β-内酰胺抗生素的量的用途。 本发明在主要的第一代β-内酰胺类中具有广泛的特异性，并且可用于测试牛奶和肉类等残留β-内酰胺抗生素的存在。

    Process for the production of semi-synthetic penicillin intermediate
    9.
    发明授权
    Process for the production of semi-synthetic penicillin intermediate 失效
    生产半合成青霉素中间体的方法

    公开(公告)号：US3669978A

    公开(公告)日：1972-06-13

    申请号：US3669978D

    申请日：1970-05-28

    申请人： AMERICAN HOME PROD

    发明人： DEIST ROBERT P

    IPC分类号： C07D499/00 ,  C07D499/40 ,  C07D99/10 ,  C07D99/16

    CPC分类号： C07D499/00

    摘要： A novel process for the preparation of an intermediate mixture which is useful in the production of penicillanic acid derivatives is described. The main component of the intermediate mixture is 2-((6-amino-3,3-dimethyl-7-oxo-4-thia-1azabicyclo(3,2,O)hept-2-yl)carbonyl) -1,2-benzisothiazol-3(2H)one-1,1-dioxide hydrochloride.

    摘要翻译： 描述了一种制备可用于生产青霉烷酸衍生物的中间体混合物的新方法。 中间体混合物的主要组分是2 - [（6-氨基-3,3-二甲基-7-氧代-4-硫杂-1-氮杂双环[3,2，O]庚-2-基）羰基] - 1,2-二苯并异噻唑-3（2H） - 酮-1,1-二氧化物盐酸盐。