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15 条记录 (耗时 0.028 秒)

    Process for the preparation of quinoline carboxylic acids
    12.
    发明授权
    Process for the preparation of quinoline carboxylic acids 失效
    制备喹啉羧酸的方法

    公开(公告)号：US5294712A

    公开(公告)日：1994-03-15

    申请号：US583296

    申请日：1990-09-14

    申请人： Istvan Hermecz ,  Geza Keresturi ,  Lelle V. Debreczy ,  Agnes Horvath ,  Maria Balogh ,  Gabor Kovacs ,  Tamas Szuts ,  Peter Ritli ,  Judit Sipos ,  Aniko Pajor

    发明人： Istvan Hermecz ,  Geza Keresturi ,  Lelle V. Debreczy ,  Agnes Horvath ,  Maria Balogh ,  Gabor Kovacs ,  Tamas Szuts ,  Peter Ritli ,  Judit Sipos ,  Aniko Pajor

    IPC分类号： C07D215/56 ,  C07F5/02 ,  C07D401/04

    CPC分类号： C07D215/56 ,  C07F5/022

    摘要： The invention relates to a new process for the preparation of compounds of the Formula I ##STR1## (wherein R stands for hydrogen or methyl) and pharmaceutically acceptable salts thereof which comprises reacting a compound of the Formula V ##STR2## (wherein R.sup.1 and R.sup.2 stand for an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen: or for an aromatic acyloxy group comprising 7-11 carbon atoms) with an amine of the Formula VI ##STR3## (wherein R has the same meaning as stated above) or a salt thereof and subjecting the compound of the Formula VII ##STR4## thus obtained (wherein R, R.sup.1 and R.sup.2 are as stated above) to hydrolysis after or without isolation and if desired converting the compound of the Formula I thus obtained into a salt thereof or setting free the same from its salt.The compounds of the Formula I are known antibacterial agents.

    摘要翻译： 本发明涉及制备式I化合物（I）（其中R代表氢或甲基）及其药学上可接受的盐的新方法，其包括使式V化合物（V ）（其中R 1和R 2表示包含2-6个碳原子并且任选被卤素取代的脂族酰氧基或用于包含7-11个碳原子的芳族酰氧基）与式VI的胺（VI） （其中R具有与上述相同的含义）或其盐，并且如此获得的式VII（VII）化合物（其中R，R 1和R 2如上所述）在分离之后或在不分离之前进行水解，以及 如果需要将由此获得的式I的化合物转化成其盐或使其与其盐相同。 式I的化合物是已知的抗菌剂。

    Process for the preparation of quinoline carboxyolic acids
    13.
    发明授权
    Process for the preparation of quinoline carboxyolic acids 失效
    喹啉羧酸的制备方法

    公开(公告)号：US5284950A

    公开(公告)日：1994-02-08

    申请号：US691633

    申请日：1991-04-25

    申请人： Istvan Hermecz ,  Geza Kereszturi ,  Lelle Vasvari nee Debreczy ,  Agnes Horvath ,  Maria Balogh ,  Gabor Kovacs ,  Tamas Szuts ,  Peter Ritli ,  Judit Sipos ,  Aniko Pajor

    发明人： Istvan Hermecz ,  Geza Kereszturi ,  Lelle Vasvari nee Debreczy ,  Agnes Horvath ,  Maria Balogh ,  Gabor Kovacs ,  Tamas Szuts ,  Peter Ritli ,  Judit Sipos ,  Aniko Pajor

    IPC分类号： C07D215/56 ,  C07F5/02 ,  C07F5/04 ,  C07D403/04

    CPC分类号： C07D215/56 ,  C07F5/022 ,  C07F5/04

    摘要： A method of using a compound of the Formula (V) ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, wherein R.sup.1 and R.sup.2 are each C.sub.1 to C.sub.6 aliphatic acyloxy, unsubstituted or substituted by halogen, or are each C.sub.7 to C.sub.11 aromatic acyloxy,for preventing amination of the 6-position when a compound of the Formula (I) ##STR2## or a pharmaceutically acceptable salt thereof is to be formed, which comprises the steps of:(a) aminating the compound of the Formula (V) or a pharmaceutically acceptable salt thereof with piperazine in an inert organic solvent to yield a compound of the Formula (VII) ##STR3## or a pharmaceutically acceptable salt thereof, and (b) hydrolyzing the compound of the Formula (VII) or a pharmaceutically acceptable salt thereof, after or without isolation, to obtain the compound of the Formula (I), and if desired, converting the compound of the Formula (I) into a pharmaceutically acceptable salt thereof, or setting free the compound of the Formula (I) from its pharmaceutically acceptable salt.

    摘要翻译： 公开了使用式（V）的化合物或其药学上可接受的盐的方法，其中R 1和R 2各自是未被取代或被卤素取代的C 1至C 6脂族酰氧基，或各自为C7至 C11芳族酰氧基，用于防止当式（I）化合物或其药学上可接受的盐形成时，6-位的胺化，其包括以下步骤：（a）胺化化合物 （VII）化合物或其药学上可接受的盐，和（b）将式（Ⅴ）化合物或其药学上可接受的盐与哌嗪在惰性有机溶剂中反应，得到式 式（VII）化合物或其药学上可接受的盐在得到式（I）化合物后，如果需要，将式（I）化合物转化为其药学上可接受的盐，或设定 释放式的化合物 （I）的药学上可接受的盐。

    Stable aqueous solutions of prymicin and pharmaceutical and cosmetic compositions containing these solutions
    14.
    发明授权
    Stable aqueous solutions of prymicin and pharmaceutical and cosmetic compositions containing these solutions 失效
    稳定的含有这些溶液的蛋白质水溶液和药物和化妆品组合物

    公开(公告)号：US5244880A

    公开(公告)日：1993-09-14

    申请号：US835097

    申请日：1992-02-11

    申请人： Peter Szentmiklosi ,  Tamas Szuts ,  Gyorgy Hidasi ,  Istvan Juhasz

    发明人： Peter Szentmiklosi ,  Tamas Szuts ,  Gyorgy Hidasi ,  Istvan Juhasz

    IPC分类号： A61K47/22

    CPC分类号： A61K31/70 ,  A61K47/22 ,  A61K8/602 ,  A61K9/0014 ,  A61Q17/005 ,  A61K2800/52 ,  Y10S514/844 ,  Y10S514/97

    摘要： The invention relates to novel stable aqueous primycin solutions containing 0.5 to 1.75% by mass/volume of primycin sulfate or 2.5 to 9% by mass/volume of a complex of primycin N-methylpyrrolidone and 2 to 15% by mass/volume of pyroglutamic acid, preferably L-pyroglutamic acid or a soluble salt, preferably the sodium salt thereof as calculated for the volume of the solution to be prepared and 40 to 60% by volume of isopropanol as calculated for the volume of the solution to be prepared as well as water in an amount adding up to 100%. The stable, aqueous primycin solutions are topical antibiotics.

    摘要翻译： 本发明涉及含有0.5〜1.75质量％/体积的硫酸伯霉素或2.5〜9质量％体积的伯霉素N-甲基吡咯烷酮和2〜15质量％的焦谷氨酸复合物的新型稳定含水伯霉素溶液 ，优选L-焦谷氨酸或可溶性盐，优选其钠盐，根据制备溶液的体积计算，和40至60体积％的异丙醇，根据所制备的溶液的体积计算，以及 水量达100％。 稳定的含水伯霉素溶液是局部抗生素。