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    Process for manufacturing oxycodone
    2.
    发明授权
    Process for manufacturing oxycodone 有权
    制造羟考酮的方法

    公开(公告)号：US06864370B1

    公开(公告)日：2005-03-08

    申请号：US10455202

    申请日：2003-06-05

    申请人： Zhaiwei Lin ,  Charles Auxilium Francis ,  Christopher Arne Kaldahl ,  Kazimierz Grzegorz Antczak ,  Vijai Kumar

    发明人： Zhaiwei Lin ,  Charles Auxilium Francis ,  Christopher Arne Kaldahl ,  Kazimierz Grzegorz Antczak ,  Vijai Kumar

    IPC分类号： A61K20060101 ,  C07D489/02 ,  C07D515/06 ,  C07D515/08

    CPC分类号： C07D489/08

    摘要： Oxycodone is manufactured in high yields and with a high purity using codeine or a salt of codeine as the starting material. The manufacturing process involves the following steps: (a) codeine or a codeine salt (e.g., codeine phosphate) is converted into the intermediate N-carboalkoxy- or N-carboaryloxynorcodeine, (b) the intermediate N-carboalkoxy- or N-carboaryloxynorcodeine resulting from step (a) is oxidized to yield the intermediate N-carboalkoxy- or N-carboaryloxynorcodeinone; (c) the intermediate N-carboalkoxy- or N-carboaryloxynorcodeinone resulting from step (b) is enolized with a base and the resultant enolate is thereafter methylated to yield the intermediate N-carboalkoxy- or N-carboaryloxynorthebaine; (d) the intermediate N-carboalkoxy- or N-carboaryloxynorthebaine resulting from step (c) is reduce to yield thebaine; (e) the thebaine resulting from step (d) is oxidized to yield the intermediate 14-hydroxycodeinone; and (f) the intermediate 14-hydroxycodeinone resulting from step (e) is hydrogenated to yield oxycodone.

    摘要翻译： 以可待因或可待因盐为起始原料，以高产率和高纯度制造羟考酮。 制备方法包括以下步骤：（a）可待因或可待因盐（例如，磷酸可待因）被转化为中间体N-烷氧羰基或N-碳酰氧可卡因，（b）中间体N-烷氧羰基或N-碳酰氧可啡碱，得到 从步骤（a）中被氧化得到中间体N-烷氧羰基或N-碳酰氧可可醋酮;（c）步骤（b）得到的中间体N-烷氧羰基或N-碳酰氧可的可乐碱用碱碱化，然后将所得的烯醇化物 甲基化以产生中间体N-烷氧羰基或N-碳酰氧基异硫乙烯;（d）由步骤（c）得到的中间体N-烷氧羰基或N-碳酰氧基异硫乙烯被还原以产生蒂巴因;（e）由步骤（d） 被氧化得到中间体14-羟可待因酮; 和（f）将步骤（e）得到的中间体14-羟可待因酮氢化得到羟考酮。

    Process for manufacturing thebaine
    3.
    发明授权
    Process for manufacturing thebaine 有权
    制造蒂巴尼的工艺

    公开(公告)号：US06790959B1

    公开(公告)日：2004-09-14

    申请号：US10455197

    申请日：2003-06-05

    申请人： Zhaiwei Lin ,  Charles Auxilium Francis ,  Christopher Arne Kaldahl ,  Kazimierz Grzegorz Antczak ,  Vijai Kumar

    发明人： Zhaiwei Lin ,  Charles Auxilium Francis ,  Christopher Arne Kaldahl ,  Kazimierz Grzegorz Antczak ,  Vijai Kumar

    IPC分类号： C07D47108

    CPC分类号： C07D489/02 ,  C07D489/04

    摘要： Thebaine is manufactured in high yields and with a high purity using codeine or a salt of codeine as the starting material. The manufacturing process involves the following steps: (a) codeine or a codeine salt (e.g., codeine phosphate) is converted into the intermediate N-carboalkoxy- or N-carboaryloxynorcodeine; (b) the intermediate N-carboalkoxy- or N-carboaryloxynorcodeine resulting from step (a) is oxidized to yield the intermediate N-carboalkoxy- or N-carboaryloxynorcodeine; (c) the intermediate N-carboalkoxy- or N-carboaryloxynorcodeinone resulting from step (b) is enolized with a base and the resultant enolate is thereafter methylated to yield the intermediate N-carboalkoxy- or N-carboaryloxynorthebaine; and (d) the intermediate N-carboalkoxy- or N-carboaryloxynorthebaine resulting from step (c) is reduced to yield thebaine.

    摘要翻译： 蒂巴因以可待因或可待因盐作为起始原料，以高产率和高纯度制造。 制造过程包括以下步骤：（a）可待因或可待因盐（例如磷酸可待因）被转化为中间体N-烷氧羰基或N-碳酰氧可卡因;（b）中间体N-烷氧羰基或N-碳酰氧可啡碱，得到 从步骤（a）中被氧化得到中间体N-烷氧羰基或N-碳酰氧可卡因;（c）步骤（b）得到的中间体N-烷氧羰基或N-碳酰氧可的可乐碱用碱碱化，然后将所得的烯醇化物 甲基化产生中间体N-烷氧羰基或N-碳酰氧基异硫乙烯; 和（d）由步骤（c）得到的中间体N-烷氧基 - 或N-碳酰氧基去硫敌
    啶减少得到蒂巴因。

    Hydrazones, hydrazines, semicarbazones and thiosemicarbazones derived from pyridyl ketones as anticonvulsant drugs and excitatory amino acid antagonists
    5.
    发明授权
    Hydrazones, hydrazines, semicarbazones and thiosemicarbazones derived from pyridyl ketones as anticonvulsant drugs and excitatory amino acid antagonists 失效
    衍生自吡啶酮的腙，肼，缩氨基脲和缩氨基硫脲作为抗惊厥药物和兴奋性氨基酸拮抗剂

    公开(公告)号：US5942527A

    公开(公告)日：1999-08-24

    申请号：US917925

    申请日：1997-08-27

    申请人： Pankaja K. Kadaba ,  Zhaiwei Lin

    发明人： Pankaja K. Kadaba ,  Zhaiwei Lin

    IPC分类号： C07D213/53 ,  C07D213/02 ,  A61K31/44

    CPC分类号： C07D213/53

    摘要： Pharmaceutical compositions comprise as the active ingredient potent orally active, nonneurotoxic anticonvulsant compounds that are highly effective in the MES animal model and are excitatory amino acid antagonists, and that are selected from the groups of hydrazones, hydrazines and semicarbazones consisting of those of the formulae: ##STR1## wherein R.sup.1 is 4-pyridyl or 3-pyridyl, R.sup.2 is methyl, ethyl or phenyl, R.sup.3 is 3,4-dichloro, p-chloro or m-chloro and R.sup.4 is oxygen. The compositions are administered to mammals in an amount to provide a dosage amount ranging from about 10 mg/kg to 200 mg/kg of body weight.

    摘要翻译： 药物组合物包含作为活性成分的有效的口服活性的非神经毒性抗惊厥化合物，其在MES动物模型中是高度有效的，并且是兴奋性氨基酸拮抗剂，并且选自由以下结构式组成的腙，肼和缩氨基脲类： 其中R1是4-吡啶基或3-吡啶基，R2是甲基，乙基或苯基，R3是3,4-二氯，对氯或间氯，R4是氧。 组合物以提供约10mg / kg至200mg / kg体重的剂量的量施用于哺乳动物。