Process for the preparation of quinoline-carboxylic acid derivatives
    5.
    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.

    Miniature pulsed fiber laser source
    9.
    发明申请
    Miniature pulsed fiber laser source 有权
    微型脉冲光纤激光源

    公开(公告)号:US20050018715A1

    公开(公告)日:2005-01-27

    申请号:US10868668

    申请日:2004-06-14

    摘要: A pulsed fiber laser and associated electronics contained in a miniature package is disclosed. The Pulsed Fiber Laser Source (PFLS) can be a single-stage high gain master oscillator power amplifier (MOPA) type fiber laser source. The PFLS can include a distributed feedback (DFB) laser, a narrowband optical filter, a broad area high-power pump diode, and Erbium/Ytterbium (Er/Yb) double cladding doped fiber. Input electrical pulses drive the DFB laser diode to emit optical pulses that are then amplified by the optical amplifier. Active and passive cooling elements may be incorporated for continuous operation without rest time. Passive cooling for intermittent pulsed applications allows the laser source to be miniaturized by eliminating active cooling elements and associated power supplies and controllers. Low duty cycle relaxes drive requirements and further reduces the size. The PFLS can be used for long distance ranging, communication by retro-modulation, and communication in presence of atmospheric attenuation.

    摘要翻译: 公开了一种包含在微型封装中的脉冲光纤激光器和相关电子装置。 脉冲光纤激光源(PFLS)可以是单级高增益主振荡器功率放大器(MOPA)型光纤激光源。 PFLS可以包括分布式反馈(DFB)激光器,窄带滤光器,广域大功率泵浦二极管和铒/镱(Er / Yb)双包层掺杂光纤。 输入电脉冲驱动DFB激光二极管发出光脉冲,然后由光放大器放大。 主动和被动冷却元件可以并入,用于连续操作而不需要休息时间。 用于间歇脉冲应用的无源冷却允许通过消除主动冷却元件和相关电源和控制器来使激光源小型化。 低占空比减轻驱动要求,进一步减小尺寸。 PFLS可用于长距离测距,通过逆向调制进行通信,以及在存在大气衰减的情况下进行通信。

    Process for the preparation of water soluble primycin and its components
and pharmaceutical compositions containing them
    10.
    发明授权
    Process for the preparation of water soluble primycin and its components and pharmaceutical compositions containing them 失效
    制备水溶性伯霉素及其组分和含有它们的药物组合物的方法

    公开(公告)号:US5441940A

    公开(公告)日:1995-08-15

    申请号:US133795

    申请日:1993-10-08

    CPC分类号: C07H17/08

    摘要: The invention relates to a process for the preparation of water soluble primycin and to the separation of its components of formulae (A.sub.1) and (A.sub.3) either as single components or as a mixture of the two components. According to the invention(i) water insoluble primycin is reacted in a C.sub.1-3 alcohol with a condensable substance comprising a C--C--C bridge in the presence of sodium or potassium methoxide or ethoxide, the resulting product with a water solubility of 40-60 mg/ml is separated, and, if desired,(ii) the resulting substance is subjected to column chromatography on silica gel applying a 1% aqueous solution of Partridge mixture as eluting agent to obtain a mixture of components of formulae (A.sub.1) and (A.sub.3) with a water solubility of 50 mg/ml, and, if desired,(iii) the resulting two-component mixture is subjected to ion exchange chromatography applying carboxymethyl cellulose in ammonium cycle as adsorbent and eluting the adsorbent with aqueous ammonium hydrocarbonate solution to obtain the component of formula (A.sub.3) with a water solubility of 50 mg/ml in pure form, and, if desired,(iv) elution is continued with absolute methanol comprising 10 mmoles of acetic acid to obtain the component of formula (A.sub.1) with a water solubility of 10 mg/ml in pure form.

    摘要翻译: 本发明涉及一种用于制备水溶性伯霉素的方法,以及将其式(A1)和(A3)的组分分离为单一组分或作为两种组分的混合物。 根据本发明(i)水溶性伯霉素在甲醇钠或乙醇钠或甲醇钾存在下,在C 1-3醇与包含CCC桥的可冷凝物质反应,所得产物的水溶解度为40-60mg / ml,并且如果需要,(ii)将得到的物质在硅胶上进行柱色谱,用1%的鹧鸪混合物水溶液作为洗脱剂,得到式(A1)和(A3)的组分的混合物, 水溶解度为50mg / ml,如果需要,(iii)将得到的双组分混合物进行离子交换色谱,在铵循环中用羧甲基纤维素作为吸附剂,并用碳酸氢铵水溶液洗脱该吸附剂,得到 水溶性为纯净形式为50mg / ml的式(A3)组分,如果需要,(iv)用包含10mmol乙酸的无水甲醇继续洗脱,得到f (A1),水溶性为10mg / ml,纯净。