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31 条记录 (耗时 0.036 秒)

    Antibacterial compounds
    22.
    发明授权
    Antibacterial compounds 失效
    抗菌化合物

    公开(公告)号：US4216223A

    公开(公告)日：1980-08-05

    申请号：US962953

    申请日：1978-11-22

    申请人： John P. Clayton ,  Norman H. Rogers ,  Steven Coulton

    发明人： John P. Clayton ,  Norman H. Rogers ,  Steven Coulton

    IPC分类号： A61K31/35 ,  A61P31/04 ,  C07D407/06 ,  C07D309/06

    CPC分类号： C07D407/06

    摘要： A thiol acid and esters thereof of formula (II): ##STR1## wherein R is hydrogen, a salt forming ion or a pharmaceutically acceptable ester-forming radical, have antibacterial and antimycoplasmal activity and are therefore useful in the treatment of human and veterinary bacterial and mycoplasmal infections.

    摘要翻译： 式（II）的硫醇酸及其酯：其中R为氢，成盐离子或药学上可接受的成酯基团，具有抗菌和抗支原体活性，因此可用于治疗人和兽用细菌 和支原体感染。

    .beta.-Lactam antibiotics, their preparation and use
    25.
    发明授权
    .beta.-Lactam antibiotics, their preparation and use 失效
    β-内酰胺抗生素，其制备和使用

    公开(公告)号：US4410533A

    公开(公告)日：1983-10-18

    申请号：US345485

    申请日：1982-02-03

    申请人： Roger J. Ponsford ,  Pamela Brown ,  Steven Coulton

    发明人： Roger J. Ponsford ,  Pamela Brown ,  Steven Coulton

    IPC分类号： C07D477/00 ,  A61K31/397 ,  A61K31/505 ,  A61P31/04 ,  C07D239/46 ,  C07D477/20 ,  C07F9/568 ,  C07D487/04

    CPC分类号： C07D239/47 ,  C07D477/20 ,  C07F9/5683

    摘要： The present invention provides a compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt or in-vivo hydrolyzable ester thereof wherein R.sup.1 is a hydrogen atom, an .alpha.-sulphonato-oxyethyl group, an .alpha.-sulphonato-oxypropyl group or is a group CR.sup.3 R.sup.4 R.sup.5 wherein R.sup.3 is a hydrogen atom or a hydroxy group; R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl group; and R.sup.5 is a hydrogen atom or a C.sub.1-6 alkyl group, a benzyl group, a phenyl group or is joined to R.sup.4 to form together with the carbon atom to which they are joined a carbocyclic ring of 5 to 7 carbon atoms; R.sup.2 is a pyrimidinyl group substituted by one two or three groups selected from nitro, halo, amino or substituted amino, and in addition may be optionally substituted by one or two C.sub.1-6 alkyl groups as the degree of substitution permits; and x is zero or one.These compounds are antibacterial agents. Their preparation and use are described.

    摘要翻译： 本发明提供了式（I）化合物：其中R 1是氢原子，α-磺酰氧基乙基，α-磺酸根，或其药学上可接受的盐或体内可水解的酯 或是基团CR 3 R 4 R 5，其中R 3是氢原子或羟基; R4是氢原子或C1-6烷基; R5为氢原子或C1-6烷基，苄基，苯基或与R4结合形成与碳原子数5〜7个碳环的碳原子一起形成的基团。 R2是被一个选自硝基，卤素，氨基或取代的氨基的两个或三个基团取代的嘧啶基，并且另外可任选地被一个或两个C 1-6烷基取代，作为取代许可的程度; x为0或1。 这些化合物是抗菌剂。 描述了它们的制备和使用。

    2-(pyrazol-3-yl)carbapenem derivatives
    26.
    发明授权
    2-(pyrazol-3-yl)carbapenem derivatives 失效
    2-（吡唑-3-基）碳青霉烯衍生物

    公开(公告)号：US07045619B2

    公开(公告)日：2006-05-16

    申请号：US10324593

    申请日：2002-12-19

    申请人： Eric Hunt ,  Steven Coulton ,  Jeremy David Hinks ,  Stephen Frederick Moss ,  Stephen Christopher Martin Fell ,  Alfred John Eglington ,  George Burton

    发明人： Eric Hunt ,  Steven Coulton ,  Jeremy David Hinks ,  Stephen Frederick Moss ,  Stephen Christopher Martin Fell ,  Alfred John Eglington ,  George Burton

    IPC分类号： C07D477/14

    CPC分类号： C07D477/14 ,  C07D477/08 ,  Y02P20/55

    摘要： A compound of formula (I): wherein Rα is hydrogen, optionally substituted (C1-6)alkyl or optionally substituted aryl; Rβ is hydrogen, optionally substituted (C1-6)alkyl or optionally substituted aryl; or Rα and Rβ together form an optionally substituted 5 or 6 membered heterocyclic ring with or without additional heteroatoms; R1 is (C1-6)alkyl which is unsubstituted or substituted by fluoro, a hydroxy group which is optionally protected by a removable hydroxy protecting group, or by an amino group which is optionally protected by a removable amino protecting group; R2 is hydrogen or methyl; and —CO2R3 is carboxy or a carboxylate anion or the group R3 is a removable carboxy protecting group. This invention also relates to processes for its preparation, intermediates and pharmaceutical compositions comprising compounds of formula (I). Compounds of formula (I) which include pharmaceutically acceptable salts or pharmaceutically acceptable in vivo hydrolysable esters thereof have a broad spectrum of anti-bacterial activity and show good stability towards DHP-1.

    摘要翻译： 式（I）的化合物：其中R a为氢，任选取代的（C 1-6 - ）烷基或任选取代的芳基; R 6是氢，任选取代的（C 1-6 - ）烷基或任选取代的芳基; 或R aα和R b一起形成具有或不具有另外的杂原子的任选取代的5或6元杂环; R 1是未被取代或被氟取代的（C 1-6 - ）烷基，任选地被可除去的羟基保护基保护的羟基，或被氨基 任选被可除去的氨基保护基团保护的基团; R 2是氢或甲基; 并且-CO 2 R 3是羧基或羧酸根阴离子或基团R 3是可除去的羧基保护基。 本发明还涉及其制备方法，中间体和包含式（I）化合物的药物组合物。 包括其药学上可接受的盐或其药学上可接受的体内可水解的酯的式（I）化合物具有广谱的抗细菌活性，并显示出对DHP-1的良好的稳定性。

    2-(pyrazol-3-yl)carbapenem derivatives
    29.
    发明授权
    2-(pyrazol-3-yl)carbapenem derivatives 失效
    2-（吡唑-3-基）碳青霉烯衍生物

    公开(公告)号：US5606051A

    公开(公告)日：1997-02-25

    申请号：US457076

    申请日：1995-06-01

    申请人： Steven Coulton ,  Jeremy D. Hinks ,  Eric Hunt

    发明人： Steven Coulton ,  Jeremy D. Hinks ,  Eric Hunt

    IPC分类号： C07D477/14 ,  C07D487/00

    CPC分类号： C07D477/14

    摘要： Disclosed are 1-, 6- and 2-substituted-1-carba-2-penem-3-carboxylic acids, a process for their preparation, pharmaceutical compositions comprising said compounds and a method of using them to treat bacterial infections.

    摘要翻译： 公开了1-，6-和2-取代-1-碳代-2-青霉烯-3-羧酸，其制备方法，包含所述化合物的药物组合物及其用于治疗细菌感染的方法。