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19 条记录 (耗时 0.024 秒)

    Method of preparing sodium salts of imidazoledicarboxylic acid substituted cephalosporin derivatives
    11.
    发明授权
    Method of preparing sodium salts of imidazoledicarboxylic acid substituted cephalosporin derivatives 失效
    制备咪唑二羧酸取代头孢菌素衍生物的钠盐的方法

    公开(公告)号：US4423215A

    公开(公告)日：1983-12-27

    申请号：US353809

    申请日：1982-03-02

    申请人： Naohiko Yasuda ,  Hisao Iwagami ,  Yasuo Irie ,  Eiji Nakanishi ,  Hideomi Saito

    发明人： Naohiko Yasuda ,  Hisao Iwagami ,  Yasuo Irie ,  Eiji Nakanishi ,  Hideomi Saito

    IPC分类号： C07D501/04 ,  C07D501/38 ,  C07D501/46

    CPC分类号： C07D501/46

    摘要： A method of preparing sodium salts of an imidazoledicarboxylic acid derivative of a substituted cephalosporin represented by the general formula of ##STR1## where X is a radical selected from the group consisting of hydrogen, halogen, hydroxyl, alkyl, aryl, aralkyl, alkoxy, aryloxy, aralkyloxy, mercapto, alkylthio, arylthio, aralkylthio, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, alkylsulfinyl, arylsulfinyl, aralkylsulfinyl, amino, mono- or dialkylamino, mono- or diarylamino, mono- or diaralkylamino, acylamino, sulfonic acid, nitro or heterocyclic group;and where R is a radical selected from hydrogen, an organic radical such as alkyl, aryl or aralkyl or a heterocyclic group, said organic radical and heterocyclic group being optionally substituted;said method comprising reacting a compound represented by the following formula: ##STR2## with 4-pyridineethanesulfonic acid in an aqueous solution of sodium iodide and subsequently recovering the salt.The compounds are useful in the treatment of bacterial infections, particularly Pseudomonas aeruginosa, in man and other animals.

    摘要翻译： 一种制备由通式（I）＆lt; IMAGE＆gt;表示的取代头孢菌素的咪唑二羧酸衍生物的钠盐的方法，其中X是选自氢，卤素，羟基，烷基，芳基 芳烷氧基，烷氧基，芳氧基，芳烷硫基，芳烷硫基，烷基磺酰基，芳基磺酰基，芳烷基磺酰基，烷基亚磺酰基，芳基亚磺酰基，芳烷基亚磺酰基，氨基，一烷基氨基或二芳基氨基，单或二芳基氨基， ，硝基或杂环基; 并且其中R是选自氢，有机基团如烷基，芳基或芳烷基或杂环基的基团，所述有机基团和杂环基团任选被取代; 所述方法包括将由下式表示的化合物与4-吡啶乙磺酸在碘化钠水溶液中反应，随后回收盐。 这些化合物可用于治疗人和其他动物中细菌感染，特别是铜绿假单胞菌（Pseudomonas aeruginosa）。

    5-Substituted-3-isoxazolecarboxylic acid derivatives
    15.
    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。

    Formation of peptide bonds in the presence of isonitriles
    19.
    发明授权
    Formation of peptide bonds in the presence of isonitriles 失效
    在存在亚硝酸盐的情况下形成肽键

    公开(公告)号：US3933783A

    公开(公告)日：1976-01-20

    申请号：US530494

    申请日：1974-12-09

    申请人： Naohiko Yasuda ,  Yasuo Ariyoshi ,  Koji Toi

    发明人： Naohiko Yasuda ,  Yasuo Ariyoshi ,  Koji Toi

    IPC分类号： C07K1/10 ,  C07C103/52

    CPC分类号： C07C251/00 ,  C07K1/10

    摘要： Amino acids having masked amino groups react with amino acids having masked carboxyl groups to form peptide derivatives in good yields if the reaction medium contains an isonitrile. Isonitriles also are effective in causing condensation of amino acids having masked amino groups with compounds having active hydroxyl groups to the corresponding amino acid esters. The yields of the first-mentioned reaction are enhanced if the reaction mixture additionally contains one of the compounds having active hydroxyl groups. Both the peptide derivatives and the amino acid esters of the compounds having active hydroxyl groups are useful for peptide synthesis.

    摘要翻译： 如果反应介质含有异腈，具有掩蔽的氨基的氨基酸与具有掩蔽的羧基的氨基酸反应以以良好的产率形成肽衍生物。 异腈还有效地使具有掩蔽氨基的氨基酸与具有活性羟基的化合物缩合成相应的氨基酸酯。 如果反应混合物另外含有具有活性羟基的化合物之一，则提高反应​​的产率。 肽衍生物和具有活性羟基的化合物的氨基酸酯都可用于肽合成。