Process for the isolation of pseudomonic acid A from pseudomonic acid complex-containing culture broth
    92.
    发明授权
    Process for the isolation of pseudomonic acid A from pseudomonic acid complex-containing culture broth 失效
    用于从含有假单胞菌酸的复合物的培养液中分离假单胞菌酸A的方法

    公开(公告)号:US06245921B1

    公开(公告)日:2001-06-12

    申请号:US09497806

    申请日:2000-02-03

    IPC分类号: C07D31500

    CPC分类号: C12P17/162

    摘要: A process for the isolation of the pseudomonic acid A antibiotic of pharmaceutical quality from the culture broth of one of the pseudomonic acid A-producing species of the Pseudomonas bacterium genus comprising the extraction of the biosynthesized pseudomonic acid A from the culture broth at acidic pH with a chlorinated aliphatic hydrocarbon or isobutyl acetate, followed by purification, is disclosed. The invention includes processes for purification of the isolated pseudomonic acid A, including (a) by the distribution of the evaporated extract residue between the aqueous-alcohol and some aliphatic or aromatic hydrocarbon, and then the extraction of the increased water-containing aqueous-alcoholic phase with methylene chloride, ethyl acetate, or isobutyl acetate; (b) by the extraction of the extract with aqueous ammonium hydrogen carbonate, alkali metal hydroxide or ammonium hydroxide solution and the acidification of the resulting alkaline aqueous extract, then reextraction again with a chlorinated aliphatic hydrocarbon or isobutyl acetate; and (c) by the concentration of the extract and the recrystallization of the crystalline pseudomonic acid A in a mixture of isobutyl acetate and petroleum ether, or acetonitrile, or aqueous acetonitrile.

    摘要翻译: 从假单胞菌属的假单胞菌素A产生物种之一的培养液中分离出假单胞菌A抗生素药物质量的方法,包括在酸性pH下从培养液中提取生物合成的假单胞菌酸A, 公开了氯化脂族烃或乙酸异丁酯,然后纯化。 本发明包括纯化分离的假单胞菌酸A的方法,包括(a)通过在含水醇和某些脂族或芳族烃之间分配蒸发的提取物残渣,然后提取含水的含水醇 与二氯甲烷,乙酸乙酯或乙酸异丁酯反应; (b)通过用碳酸氢铵水溶液,碱金属氢氧化物或氢氧化铵溶液萃取提取物,并将得到的碱性水提取物酸化,然后用氯化脂族烃或乙酸异丁酯再次萃取; 和(c)通过提取物的浓度和结晶假单胞菌酸A在乙酸异丁酯和石油醚或乙腈或乙腈水溶液的混合物中的重结晶。

    8-HYDROXY-QUINOLINE DERIVATIVES
    93.
    发明申请
    8-HYDROXY-QUINOLINE DERIVATIVES 有权
    8-羟基喹啉衍生物

    公开(公告)号:US20130131096A1

    公开(公告)日:2013-05-23

    申请号:US13696541

    申请日:2011-05-06

    摘要: The invention relates to compounds of the general formula (I) and their pharmaceutically acceptable salts (in which formula R1 represents a hydrogen atom, lower alkyl group, lower alkenyl group, lower cycloalkyl group, aryl group, aralkyl group or heterocyclic group, wherein, the above groups are optionally substituted in ortho, meta and/or para position with 1, 2, 3 or 4 electron withdrawing groups or electron donating groups; R2 represents a hydrogen atom, lower alkyl group, aryl group, aralkyl group or heterocyclic group wherein the above groups are optionally substituted with one or more halogen atoms; R3 represents a lower alkyl group, aryl group, aralkyl group or heterocyclic group wherein the above groups are optionally substituted in ortho, meta or para position with 1, 2, 3 or 4 electron withdrawing groups or electron donating groups; R4 represents a hydrogen atom, lower alkyl group or any acidic functional group; n is 1 or 2). The compounds according to the invention can be used in the medicine mainly for the treatment of diseases associated with neurological and/or oxidative stress.

    摘要翻译: 本发明涉及通式(I)的化合物及其药学上可接受的盐(式中R1表示氢原子,低级烷基,低级烯基,低级环烷基,芳基,芳烷基或杂环基,其中, 上述基团任选在邻位,间位和/或对位用1,2,3或4个吸电子基团或给电子基团取代; R 2表示氢原子,低级烷基,芳基,芳烷基或杂环基,其中 上述基团任选被一个或多个卤素原子取代; R 3表示低级烷基,芳基,芳烷基或杂环基,其中上述基团在邻位,间位或对位任选被取代1,2,3或4 吸电子基团或给电子基团; R 4表示氢原子,低级烷基或任何酸性官能团; n为1或2)。 根据本发明的化合物可用于药物中,主要用于治疗与神经和/或氧化应激有关的疾病。

    Methods for Treating or Preventing Radiocontrast Agent Induced Kidney Injury
    95.
    发明申请
    Methods for Treating or Preventing Radiocontrast Agent Induced Kidney Injury 审中-公开
    治疗或预防放射治疗剂诱发肾损伤的方法

    公开(公告)号:US20100183748A1

    公开(公告)日:2010-07-22

    申请号:US12690368

    申请日:2010-01-20

    IPC分类号: A61K33/04 A61P43/00

    摘要: Methods for treating or preventing radiocontrast agent induced kidney injury in a mammal are disclosed, the methods comprising administering to the mammal a first effective amount of a chalcogenide composition prior to administering a radiocontrast agent to the mammal.

    摘要翻译: 公开了用于治疗或预防放射性对比剂诱导的哺乳动物肾损伤的方法,所述方法包括在向哺乳动物施用放射性对比剂之前向哺乳动物施用第一有效量的硫族化物组合物。

    Processes for preparing crystalline and amorphous mupirocin calcium
    97.
    发明申请
    Processes for preparing crystalline and amorphous mupirocin calcium 审中-公开
    制备结晶和无定形莫匹罗星钙的方法

    公开(公告)号:US20080249322A1

    公开(公告)日:2008-10-09

    申请号:US11483418

    申请日:2006-07-07

    IPC分类号: C07D407/06

    CPC分类号: C07D407/06

    摘要: Processes are provided for preparing mupirocin calcium dihydrate from pseudomonic acid in a two phase system by using an organic carboxylate.A highly pure composition of amorphous mupirocin calcium is provided, and processes for its preparation by solvent removal, lyophilization and precipitation with use of an anti-solvent. Pharmaceutical compositions of amorphous form, and methods of using them to treat infections are also provided.Also provided are combined processes for preparing mupirocin calcium dihydrate and amorphous, by producing amorphous form first, followed by conversion of amorphous form into the dihydrate through crystallization from an aqueous solution. Also provided are processes for removing the water of crystallization of the dihydrate to obtain mupirocin calcium anhydrate.

    摘要翻译: 提供了通过使用有机羧酸盐在两相体系中由假单胞菌酸制备莫匹罗星二水合钙的方法。 提供了一种高纯度非晶莫匹罗星钙组合物,以及通过溶剂去除,冻干和使用抗溶剂沉淀制备的方法。 还提供了无定形形式的药物组合物,以及使用它们治疗感染的方法。 还提供了通过首先产生无定形形式,然后通过从水溶液中结晶将无定形形式转化为二水合物,制备莫匹罗星二水合物和无定形物的组合方法。 还提供了去除二水合物结晶水以获得莫匹罗星钙无水物的方法。

    Methods of preparing pimecrolimus
    100.
    发明授权

    公开(公告)号:US07279571B2

    公开(公告)日:2007-10-09

    申请号:US11293353

    申请日:2005-12-01

    IPC分类号: C07D498/18

    摘要: The present invention provides a process for the preparation of pimecrolimus from ascomycin in which ascomycin is reacted with a conversion reagent that converts ascomycin to its activated derivative at C-32. The activated ascomycin is then reacted with chloride ion. The process of the invention requires fewer process steps than prior art processes, and does not require the protection of the ascomycin C-24 hydroxyl group or the purification of the activated ascomycin derivative.