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    Benzoxazinedione derivatives, method of producing them and uses thereof
    2.
    发明授权
    Benzoxazinedione derivatives, method of producing them and uses thereof 失效
    苯并恶嗪二酮衍生物，其制备方法和用途

    公开(公告)号：US6013647A

    公开(公告)日：2000-01-11

    申请号：US35344

    申请日：1998-03-05

    申请人： Lothar Heinisch ,  Steffen Wittmann ,  Ute Moellmann ,  Rolf Reissbrodt

    发明人： Lothar Heinisch ,  Steffen Wittmann ,  Ute Moellmann ,  Rolf Reissbrodt

    IPC分类号： C07D499/70 ,  A61K31/535 ,  A61K31/536 ,  A61K31/538 ,  A61K38/00 ,  A61K47/48 ,  A61P3/00 ,  A61P31/04 ,  A61P43/00 ,  C07D265/24 ,  C07D265/26 ,  C07D413/06 ,  C07D413/12 ,  C07D499/00 ,  C07D499/68 ,  C07D501/20 ,  C07K5/02 ,  C07K5/06 ,  C07K5/103 ,  C07K7/06

    CPC分类号： C07K7/06 ,  C07D265/26 ,  C07D499/00 ,  C07K5/02 ,  C07K5/06026 ,  C07K5/1008 ,  A61K38/00

    摘要： This invention relates to new benzoxazinedione derivatives corresponding to the formula I: ##STR1## wherein R.sup.1 =H or carboxyalkyl, R.sup.2 =H, alkyl or phenyl, and R.sup.3 represents different acid groups derived from amino acids, dipeptides and hydrazones or conjugates thereof with active ingredients, e.g. antibiotics. The compounds may be present as free acids, in the form of their salts or as readily cleavable esters. The compounds according to the invention constitute heterocyclically protected catechol derivatives and are effective as siderophores against gram-negative bacterial strains, particularly against Pseudomonads and strains of E. coli and Salmonella. In the form of their conjugates with active ingredients, e.g. antibiotics (as "siderophore-antibiotic conjugates"), they can transport the latter into bacterial cells and can improve or extend the antibacterial effect thereof, sometimes even in relation to bacterial strains which are resistant to other .beta.-lactams. In addition, said compounds, as potential prodrug forms for iron chelating agents, are suitable for use against diseases which are caused by a disorder of the iron metabolism. The invention can be employed in pharmaceutical research and in the pharmaceutical industry, and in agriculture.

    摘要翻译： 本发明涉及对应于式I的新的苯并恶嗪二酮衍生物：其中R1 = H或羧基烷基，R2 = H，烷基或苯基，R3代表衍生自氨基酸，二肽和腙的不同酸基或​​其与活性成分例如 抗生素。 化合物可以其盐形式或易裂解的酯的形式存在为游离酸。 根据本发明的化合物构成了杂环保护的邻苯二酚衍生物，并且作为抗革兰氏阴性细菌菌株的铁载体是有效的，特别是对假单胞菌和大肠杆菌和沙门氏菌菌株有效。 以它们与活性成分的缀合物的形式，例如 抗生素（作为“铁载体 - 抗生素共轭物”），它们可以将后者转运到细菌细胞中，并且可以改善或延长其抗菌作用，有时甚至与对其它β-内酰胺酶有抗性的细菌菌株有关。 此外，作为铁螯合剂的潜在前体药物形式的所述化合物适用于针对由铁代谢紊乱引起的疾病。 本发明可用于制药研究，制药工业和农业领域。

    Process for the preparation of sterile amoxycillin sodium salt
    4.
    发明授权
    Process for the preparation of sterile amoxycillin sodium salt 失效
    无菌阿莫西林钠盐的制备方法

    公开(公告)号：US5559241A

    公开(公告)日：1996-09-24

    申请号：US528546

    申请日：1995-09-15

    申请人： Giordano B. Corsi ,  Alberto Brandt ,  Loredana Cecchetelli

    发明人： Giordano B. Corsi ,  Alberto Brandt ,  Loredana Cecchetelli

    IPC分类号： C07B63/02 ,  C07D499/00 ,  C07D499/16 ,  C07D499/18 ,  C07D499/68 ,  C07D277/60

    CPC分类号： C07D499/00

    摘要： A process for the preparation of sterile sodium amoxycillin characterized by the fact that a solution of amoxycillin trihydrate in a mixture of methyl alcohol and a lower C.sub.2 -C.sub.5 alcohol is reacted in a sterile ambient, optionally in the presence of a suitable amine, with a solution of a suitable salifying agent selected from the group consisting of an alcoholate or carboxylate of sodium in methyl acetate followed by separation of the precipitate is described.

    摘要翻译： 一种制备无菌阿莫西林钠的方法，其特征在于将阿莫西林三水合物在甲醇和较低C 2 -C 5醇的混合物中的溶液在无菌环境中，任选地在合适的胺存在下与 描述了选自在乙酸甲酯中的醇化物或羧酸钠的合适的选矿剂溶液，然后分离沉淀物。

    .beta.-Lactam antibiotics
    7.
    发明授权
    .beta.-Lactam antibiotics 失效
    β-内酰胺抗生素

    公开(公告)号：US4540688A

    公开(公告)日：1985-09-10

    申请号：US489183

    申请日：1983-04-27

    申请人： Michael J. Driver

    发明人： Michael J. Driver

    IPC分类号： C07D499/08 ,  A61B8/12 ,  A61K31/43 ,  A61P31/04 ,  C07D241/08 ,  C07D499/00 ,  C07D499/64 ,  C07D499/68 ,  H01L21/027 ,  A61K31/495 ,  C07D499/54

    CPC分类号： C07D241/08 ,  C07D499/00 ,  H01L21/0276

    摘要： Compounds of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof have antibacterial activity: ##STR1## wherein R is hydrogen, C.sub.1-6 alkylcarbonyl or C.sub.1-6 alkyl; R.sup.1 is hydrogen or hydrocarbon; R.sup.2 is hydrogen, or optionally substituted hydrocarbon or optionally substituted heterocyclyl or CXR.sup.d, where X is O or S and R.sup.d is hydrogen or optionally substituted hydrocarbon or optionally substituted heterocyclyl; or R.sup.1 and R.sup.2 together with the nitrogen to which they are attached, form an optionally substituted heterocyclyl group. A process for the preparation of such compounds and compositions comprising them, are also described.

    摘要翻译： 式（I）化合物或其药学上可接受的盐或体内可水解的酯具有抗菌活性：其中R是氢，C 1-6烷基羰基或C 1-6烷基; R1是氢或烃; R2是氢或任选取代的烃或任选取代的杂环基或CXRd，其中X是O或S，Rd是氢或任选取代的烃或任选取代的杂环基; 或者R 1和R 2与它们所连接的氮一起形成任选取代的杂环基。 还描述了制备这些化合物的方法和包含它们的组合物。

    5-Substituted-3-isoxazolecarboxylic acid derivatives
    9.
    发明授权
    5-Substituted-3-isoxazolecarboxylic acid derivatives 失效
    5-取代的3-异恶唑羧酸衍生物

    公开(公告)号：US4465631A

    公开(公告)日：1984-08-14

    申请号：US482544

    申请日：1983-04-06

    申请人： Naohiko Yasuda ,  Hisao Iwagami ,  Eiji Nakanishi ,  Yukio Sasaki ,  Shigeru Yamanaka

    发明人： Naohiko Yasuda ,  Hisao Iwagami ,  Eiji Nakanishi ,  Yukio Sasaki ,  Shigeru Yamanaka

    IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D499/00 ,  C07D499/64 ,  C07D499/68 ,  C07D499/70 ,  C07D501/20 ,  C07D501/22 ,  C07D501/44

    CPC分类号： C07D499/00

    摘要： A 5-substituted-3-isoxazolecarboxylic acid derivative of the general formula: ##STR1## wherein X stands for a phenyl group, thienyl group, furyl group or pyridyl group, each of which optionally may carry at least one substituent group; R stands for a phenyl group or hydroxyphenyl group; and A stands for a group of the formula: ##STR2## wherein Y stands for ##STR3## in which the carbon atom with which the carboxyl group combines with the nitrogen atom in A, M stands for a hydrogen atom or a substituent group, and Z stands for a hydrogen atom, hydroxy group, acyloxy group, carbamoyloxy group, aromatic heterocycle thio group or aromatic nitrogen-containing heterocycle quaternary ammonium group, is disclosed along with methods for producing these compounds.

    摘要翻译： 其中X代表苯基，噻吩基，呋喃基或吡啶基，其中每一个可以任选地带有至少一个取代基;一个5-取代的3-异恶唑羧酸衍生物，其通式如下： R代表苯基或羟基苯基; A代表下式的基团：其中Y代表其中羧基与A中的氮原子结合的碳原子，M代表氢原子或取代基的，以及 Z表示氢原子，羟基，酰氧基，氨基甲酰氧基，芳香族杂环硫基或芳香族含氮杂环季铵基，同时也包括这些化合物的制造方法。