Process for the preparation of quinoline-carboxylic acid derivatives
    1.
    发明授权
    Process for the preparation of quinoline-carboxylic acid derivatives 失效
    喹啉羧酸衍生物的制备方法

    公开(公告)号:US4935512A

    公开(公告)日:1990-06-19

    申请号:US273853

    申请日:1988-06-03

    CPC分类号: C07D215/56

    摘要: The invention relates to a new and simple process for the preparation of quinoline-carboxylic acid derivatives of the general formula (I) ##STR1## as well as hydrates and therapeutically acceptable salts thereof. In the formula the meaning of the substituents is as follows:R is hydrogen atom or a formyl group,R.sup.1 is a hydrogen atom or a straight or branched chain alkyl group having 1 to 4 carbon atoms, which may be substituted by a hydroxyl group, a halogen atom or an amino group; or a CH.sub.3 --NH-group,R.sup.2 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms.According to the invention the compound of the general formula (II) ##STR2## or an acid addition salt thereof is reacted with piperazine in dimethylformamide and--if desired--the compound of the general formula (III) ##STR3## thus obtained is subjected to an acidic or alkaline treatment, or is reacted advantageously with hydrazine or preferably with hydrazine-hydrate.

    摘要翻译: PCT No.PCT / HU87 / 00044 Sec。 371日期:1988年6月3日 102(e)日期1988年6月3日PCT提交1987年10月14日PCT公布。 出版物WO88 / 02748 日本时间1988年04月21日。本发明涉及一种制备通式(I)的喹啉羧酸衍生物的新的和简单的方法,其水合物及其可治疗的盐。 在该式中,取代基的含义如下:R是氢原子或甲酰基,R 1是氢原子或可被羟基取代的具有1至4个碳原子的直链或支链烷基, 卤原子或氨基; 或CH 3 -NH基,R 2为氢原子或碳原子数1〜4的烷基。 根据本发明,通式(II)的化合物或其酸加成盐与二甲基甲酰胺中的哌嗪反应,如果需要,将通式(III)的化合物(III) )进行酸性或碱性处理,或有利地与肼反应或优选与肼水合物反应。

    Antimicrobial pharmaceutical composition
    7.
    发明授权
    Antimicrobial pharmaceutical composition 失效
    抗微生物药物组成

    公开(公告)号:US4904647A

    公开(公告)日:1990-02-27

    申请号:US222056

    申请日:1988-07-20

    CPC分类号: A61K31/65

    摘要: The invention relates to a synergistic, antimicrobial pharmaceutical composition containing 0.01 to 50% by weight of a quinolinecarboxylic acid derivative or a naphthyridinecarboxylic acid derivative of the formula (I), ##STR1## wherein X is carbon or nitrogen;R.sup.1 is hydrogen or fluorine;R.sup.2 is methyl, piperazino or methylpiperazino group; orR.sup.1 and R.sup.2 together are a methylenedioxy group; and 0.01 to 95% by weight of a tetracycline derivative of the formula (II), ##STR2## wherein R.sup.3 and R.sup.4 are hydrogen; orR.sup.3 and R.sup.4 together represent an additional chemical bond,in 20:1 to 1:50 ratio of the compound of the formula (I) to the compound of the formula (II), optionally in an admixture with an amount required to 100% by weight of an inert, solid or liquid carrier such as magnesium carbonate, magnesium stearate, starch, talc, cyclodextrine or water and other additives such as filling, disintegrating, sliding and emulsifying agents.

    Process for preparing primycin salts
    8.
    发明授权
    Process for preparing primycin salts 失效
    伯霉素盐的制备方法

    公开(公告)号:US4782141A

    公开(公告)日:1988-11-01

    申请号:US751624

    申请日:1985-07-02

    CPC分类号: C07H17/08

    摘要: This invention relates to salts of primycin formed with an organic acid--preferably a C.sub.1-16 aliphatic carboxylic acid, a halogenated carboxylic acid, an aliphatic dicarboxylic acid, an aromatic carboxylic acid, a substituted aromatic carboxylic acid or an organic sulfonic acid--or an inorganic acid--preferably a hydrohalogenic acid.There is furtheron provided a process for the preparation of new primycin salts which comprises reacting a suspension of primycin sulfate formed with an aliphatic alcohol containing 1-4 carbon atoms with a barium salt.The new primycin salts of the present invention possess excellent antibiotic properties.

    摘要翻译: 本发明涉及用有机酸 - 优选C 1-16脂族羧酸,卤代羧酸,脂族二羧酸,芳族羧酸,取代的芳族羧酸或有机磺酸形成的伯霉素的盐或 - 无机酸 - 优选氢卤酸。 还提供了制备新的伯霉素盐的方法,其包括使形成的伯霉素硫酸盐与含有1-4个碳原子的脂肪醇的悬浮液与钡盐反应。 本发明的新的伯霉素盐具有优异的抗生素特性。