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    • 86. 发明授权
    • Process for the isolation of pseudomonic acid A from pseudomonic acid complex-containing culture broth
    • 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
    • US06245921B1
    • 2001-06-12
    • US09497806
    • 2000-02-03
    • Istvan BartaAniko TegdesValeria SzellCsaba SzaboEdit Nagy Nee ArvaiVilmos KeriDavid LeonovIIdiko LangMargit Bidlo Nee IgloyGyula JerkovichJanos Salat
    • Istvan BartaAniko TegdesValeria SzellCsaba SzaboEdit Nagy Nee ArvaiVilmos KeriDavid LeonovIIdiko LangMargit Bidlo Nee IgloyGyula JerkovichJanos Salat
    • C07D31500
    • C12P17/162
    • 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.
    • 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。
    • 87. 发明申请
    • 8-HYDROXY-QUINOLINE DERIVATIVES
    • 8-羟基喹啉衍生物
    • US20130131096A1
    • 2013-05-23
    • US13696541
    • 2011-05-06
    • Laszlo PuskasCsaba SzaboIvan KanizsaiMario GyurisRamona MadacsiBela OzsvariLiliana FeherGabor Tamas
    • Laszlo PuskasCsaba SzaboIvan KanizsaiMario GyurisRamona MadacsiBela OzsvariLiliana FeherGabor Tamas
    • C07D413/12C07D401/14C07D401/10C07D401/12C07D215/26
    • C07D413/12C07D215/26C07D401/06C07D401/10C07D401/12C07D401/14
    • 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.
    • 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。