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    Aryl (ethanoic) propanoic acid ascorbyl ester, preparation method thereof and medicament containing the same
    4.
    发明授权
    Aryl (ethanoic) propanoic acid ascorbyl ester, preparation method thereof and medicament containing the same 有权
    （乙酸）丙酸抗坏血酸酯，其制备方法和含有它的药物

    公开(公告)号：US08703975B2

    公开(公告)日：2014-04-22

    申请号：US13320101

    申请日：2009-12-24

    申请人： Luhong Tang ,  Ajuan Dai ,  Ze Wang ,  Yang Sun ,  Xinning Liu ,  Lingyan Xu ,  Xin Fang ,  Shuang Qiu ,  Yaqing Cao ,  Xiaomin Xu ,  Ruixia Jiang ,  Chao Wu

    发明人： Luhong Tang ,  Ajuan Dai ,  Ze Wang ,  Yang Sun ,  Xinning Liu ,  Lingyan Xu ,  Xin Fang ,  Shuang Qiu ,  Yaqing Cao ,  Xiaomin Xu ,  Ruixia Jiang ,  Chao Wu

    IPC分类号： C07D307/62

    CPC分类号： C07D307/62 ,  C07D405/12 ,  C07D491/04 ,  C07D491/052 ,  C12P17/04 ,  C12P17/16 ,  C12P17/188 ,  C12Y301/01003

    摘要： The present invention designs and synthesizes the ascorbyl ester derivatives of the aryl (ethanoic) propanoic acid non-steroidal anti-inflammatory medicaments, such as ibuprofen, ketoprofen and naproxen, and addition salt of the derivatives with pharmaceutical acid or pharmaceutical alkaline. The non-steroidal anti-inflammatory medicament which takes the ibuprofen as the representative is a common antipyretic analgesic medicament. The invention has remarkable antipyretic and analgesic effects and good safety except for anti-inflammatory effect, thus being not only suitable for adults, but also suitable for the elderly people, infants and children. The aryl (ethanoic) propanoic acid ascorbyl ester can be converted into ascorbyl ester derivatives and the addition salts of the derivatives with pharmaceutical acid or pharmaceutical alkaline, which can improve the water solubility thereof, facilitate intravenously administration, reduce the onset time, improve the bioavailability, reduce the stimulation effect to gastrointestinal tract, and enhance the penetrating capacity to hemato encephalic barrier, and can be used as a novel medicament to be applied for antiphlogistic, antipyresis, analgesia, treatment of arthritis, dysmenorrheal, multiple sclerosis, pneumonia cystic fibrosis and patent ductus arteriosus of premature infants, and prevention and treatment of cerebral apoplexy, hypoxic-ischemic brain damage, senile dementia and certain cancers.

    摘要翻译： 本发明设计和合成芳基（乙酸）丙酸非甾体抗炎药物如布洛芬，酮洛芬和萘普生的抗坏血酸酯衍生物，以及衍生物与药物酸或药物碱的加成盐。 以布洛芬为代表的非甾体抗炎药是常见的解热止痛药。 本发明除抗炎作用外，具有明显的解热镇痛作用，安全性好，不仅适用于成人，而且适用于老年人，婴儿和儿童。 芳基（乙酸）丙酸抗坏血酸酯可以转化为抗坏血酸酯衍生物，并且衍生物的加成盐与药物酸或药物碱性可以改善其水溶性，有助于静脉内施用，减少发病时间，提高生物利用度 降低对胃肠道的刺激作用，增强血液渗透屏障的穿透能力，可用作新型药物，用于消炎止痛，止痛，止痛，治疗关节炎，痛经，多发性硬化，肺炎囊性纤维化，以及 早产儿动脉导管未闭，预防和治疗脑中风，缺氧缺血性脑损伤，老年性痴呆和某些癌症。

    Stereoselective process for the production of dioxolane nucleoside analogues
    5.
    发明授权
    Stereoselective process for the production of dioxolane nucleoside analogues 有权
    用于生产二氧戊环核苷类似物的立体选择性方法

    公开(公告)号：US07955835B2

    公开(公告)日：2011-06-07

    申请号：US10535235

    申请日：2003-11-18

    申请人： Alex Cimpoia ,  James Joseph LaLonde

    发明人： Alex Cimpoia ,  James Joseph LaLonde

    IPC分类号： C12P41/00

    CPC分类号： C12P17/16 ,  C07D317/32 ,  C12P17/04 ,  C12P17/188 ,  C12P41/005

    摘要： The present invention relates to a process for producing compounds of formula (I) and (VII); said process comprising the steps of: a) subjecting a compound of formula (II) to an enzymatic diastereomeric resolution in the presence of a suitable amount of enzyme chosen from Pig Liver Esterase or Porcine Pancreatic Lipase b) recovering said compounds of formula (I) and (VII). The invention also provides a process for producing compounds of formula (III) and (X); said process comprising the steps of: a) subjecting a compound of formula (IV) to an enzymatic diastereomeric resolution in the presence of a suitable amount of enzyme chosen from Candida Antarctica “A” lipase, Candida Antarctica “B” lipase, Candida Lypolitica Lipase or Rhizomucor Miehei Lipase b) recovering said compound of formula (III) and (X).

    摘要翻译： 本发明涉及制备式（I）和（VII）化合物的方法; 所述方法包括以下步骤：a）在合适量的选自猪肝酯酶或猪胰腺脂肪酶的酶的存在下，使式（II）化合物进行酶促非对映异构体拆分b）回收所述式（I）化合物， 和（Ⅶ）。 本发明还提供了制备式（III）和（X）化合物的方法; 所述方法包括以下步骤：a）在适当量的选自南极假丝酵母“A”脂肪酶，南极假丝酵母“B”脂酶，假单胞菌脂肪酶假丝酵母属脂肪酶的酶的存在下使式（IV）化合物进行酶促非对映异构体拆分 或根瘤菌Miehei脂肪酶b）回收所述式（III）和（X）化合物。

    Burkholderia rhizoxina micro-organisms, novel endosymbionts of rhizopus sp. and method for producing rhizoxin and/or rhizoxin-derivates using said micro-organisms
    6.
    发明申请
    Burkholderia rhizoxina micro-organisms, novel endosymbionts of rhizopus sp. and method for producing rhizoxin and/or rhizoxin-derivates using said micro-organisms 审中-公开
    伯克霍尔德菌根瘤菌微生物，新根内根霉属的根霉属。 以及使用所述微生物生产根瘤菌素和/或根瘤菌素衍生物的方法

    公开(公告)号：US20090209013A1

    公开(公告)日：2009-08-20

    申请号：US11921698

    申请日：2006-06-01

    申请人： Christian Hertweck ,  Laila P. Partida-Martinez

    发明人： Christian Hertweck ,  Laila P. Partida-Martinez

    IPC分类号： C12P17/18 ,  C12N1/20

    CPC分类号： C12P17/16 ,  C12R1/01

    摘要： The invention relates to a method for producing rhizoxin and derivates of rhizoxin.The aim of the invention is to produce novel novel micro-organisms that synthesise rhizoxin or derivates of rhizoxin, and to provide a method for producing rhizoxin oder derivates thereof, without the disadvantages of prior art and in a simpler manner with a higher yield. To this end, bacterial symbionts of Rhizopus sp., in the form of Burkholderia Rhizoxina DSM 17360 or other Burkholderia Rhizoxina strains, are isolated, cultivated and used for the fermentive production of rhizoxin and/or derivates of rhizoxin in a submerged culture, and the rhizoxin and/or the derivates thereof are subsequently isolated from the culture supernatant.

    摘要翻译： 本发明涉及根瘤菌素和根瘤菌素衍生物的制备方法。 本发明的目的是制备合成根瘤菌素或根瘤菌素衍生物的新型微生物，并提供一种生产根瘤菌素衍生物的方法，而不存在现有技术的缺点，并以更高的产率以更简单的方式。 为此，分离培养的根瘤菌（Burkholderia Rhizoxina DSM 17360）或其他伯克霍尔德杆菌（Rhkoxia Rhizoxina）菌株的根霉菌种的细菌共生体用于在浸没培养物中发酵生产根瘤菌素和/或根瘤菌素衍生物， 随后从培养上清中分离出根瘤菌素和/或其衍生物。