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    Process for preparing pergolide
    1.
    发明授权
    Process for preparing pergolide 失效
    昂高尔德的制备方法

    公开(公告)号：US06388079B1

    公开(公告)日：2002-05-14

    申请号：US09651381

    申请日：2000-08-29

    申请人： Edwin S. C. Wu ,  Mark Wu

    发明人： Edwin S. C. Wu ,  Mark Wu

    IPC分类号： C07D47104

    CPC分类号： C07D457/02

    摘要： This invention relates to a process for preparing pergolide, which comprises the steps of reacting 9,10-dihydrolysergol with an acid anhydride at an elevated temperature in the presence of a catalyst to form a triacylated product intermediate; reducing the triacylated product intermediate with a reducing agent in a solvent to form a primary amino alcohol intermediate; and reacting the amino alcohol intermediate with dimethyl disulfide and trialkyl phosphine, aryl phosphine or the polymeric derivatives of phosphine analogs thereof in a polar solvent to obtain pergolide; or the steps of reacting 9,10-dihydrolysergol with dimethyl disulfide and trialkyl phosphine, aryl phosphine or the polymeric derivatives of phosphine analogs thereof in a polar solvent to form a methylsulfide intermediate; reacting the methylsulfide intermediate with an acid anhydride at an elevated temperature in the presence of a catalyst to form a diacylated amide intermediate; and reducing the diacylated amide intermediate with a reducing agent in a solvent to obtain pergolide.

    摘要翻译： 本发明涉及一种制备昂热胶的方法，其包括以下步骤：在催化剂存在下，在升高的温度下使9,10-二氢赖氨酸与酸酐反应，形成三酰化产物中间体; 用还原剂在溶剂中还原三酰化产物中间体以形成伯氨基醇中间体; 并使氨基醇中间体与二甲基二硫醚和三烷基膦，芳基膦或其膦类似物的聚合衍生物在极性溶剂中反应，得到百戈来; 或使9,10-二氢赖氨酸与二甲基二硫醚和三烷基膦，芳基膦或其膦类似物的聚合衍生物在极性溶剂中反应以形成甲基硫化物中间体的步骤; 在升高的温度下，在催化剂存在下使甲硫醚中间体与酸酐反应，形成二酰化酰胺中间体; 并用还原剂在溶剂中还原二酰化酰胺中间体以获得百戈来（pergolide）。

    Spirofurane derivatives
    4.
    发明授权
    Spirofurane derivatives 失效
    螺呋喃衍生物

    公开(公告)号：US5594000A

    公开(公告)日：1997-01-14

    申请号：US469791

    申请日：1995-06-06

    申请人： Edwin S.-C. Wu ,  Ronald C. Griffith

    发明人： Edwin S.-C. Wu ,  Ronald C. Griffith

    IPC分类号： C07D491/10 ,  C07D491/107 ,  C07D471/10 ,  A61K31/445 ,  C07D211/44 ,  C07D405/06

    CPC分类号： C07D491/10

    摘要： Compounds of general formula I, ##STR1## wherein R.sup.1 represents hydrogen or alkyl C.sub.1-3,R.sup.2 represents hydrogen, alkyl C.sub.1-6, alkenyl C.sub.3-6 or alkynyl C.sub.3-6,n and m are integers from 1 to 3, provided that n+m=4, andone of X and Y represents CH.sub.2 and the other represents CHR.sup.3, C=CHR.sup.4 or C=NR.sup.5, in whichR.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13, R.sup.14, R.sup.15, R.sup.16 and R.sup.17 are as defined in the specification,and their saltsare useful as pharmaceuticals, in particular as central muscarinic acetylcholine receptors. The compounds are therefore useful in the treatment of diseases such as presenile and senile dementia, Huntington's chorea, tardive dyskinesia, hyperkinesia, mania and Tourette Syndrome, and also as analgesic agents for use in the treatment of severe painful conditions such as rheumatism, arthritis, and terminal illness.

    摘要翻译： 通式I的化合物，其中R 1表示氢或烷基C 1-3，R 2表示氢，烷基C 1-6，烯基C 3-6或炔基C 3-6，n和m是1至3的整数， n + m = 4，X和Y中的一个表示CH 2，另一个表示CHR 3，C = CHR 4或C = NR 5，其中R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 10，R 11，R 12 R13，R14，R15，R16和R17如说明书中所定义，并且它们的盐可用作药物，特别是作为中毒毒蕈碱乙酰胆碱受体。 因此，这些化合物可用于治疗诸如老年痴呆和老年痴呆，亨廷顿舞蹈病，迟发性运动障碍，运动过度，躁狂症和图雷特综合征等疾病，也可用作治疗严重疼痛病症如镇痛，关节炎， 和末期疾病。

    Opioid and opioid-like compounds and uses thereof
    5.
    发明授权
    Opioid and opioid-like compounds and uses thereof 有权
    阿片样物质和阿片样物质化合物及其用途

    公开(公告)号：US08404706B2

    公开(公告)日：2013-03-26

    申请号：US13081179

    申请日：2011-04-06

    申请人： Edwin S. C. Wu ,  Mao-Hsiung Yen ,  Chin-Tsai Fan

    发明人： Edwin S. C. Wu ,  Mao-Hsiung Yen ,  Chin-Tsai Fan

    IPC分类号： A61K31/4748 ,  C07D221/28

    CPC分类号： A61K31/485 ,  C07D221/28 ,  C07D489/00 ,  C07D489/02 ,  C07D489/08

    摘要： The present invention relates to opioid and opioid-like compounds, and pharmaceutical formulations containing the same and methods of use thereof. Uses of the present invention include, but are not limited to, use for the prevention and treatment of septic shock and other disorders. The compounds described herein can be water soluble and can act through mechanisms mediated through pathways other than opiate receptors.

    摘要翻译： 本发明涉及阿片样物质和阿片样物质化合物，以及含有其的药物制剂及其使用方法。 本发明的用途包括但不限于用于预防和治疗败血性休克和其它疾病的用途。 本文所述的化合物可以是水溶性的，并且可以通过除阿片受体之外的途径介导的机制起作用。

    Chromones and chromone derivatives and uses thereof
    6.
    发明授权
    Chromones and chromone derivatives and uses thereof 有权
    色酮和色酮衍生物及其用途

    公开(公告)号：US08138165B2

    公开(公告)日：2012-03-20

    申请号：US10531506

    申请日：2003-10-22

    申请人： Mao-Hsiung Yen ,  Edwin S. C. Wu

    发明人： Mao-Hsiung Yen ,  Edwin S. C. Wu

    IPC分类号： A61K31/665 ,  C07D311/00

    CPC分类号： C07D311/30 ,  C07D311/02 ,  C07D407/12 ,  C07D493/04

    摘要： Certain 2- and/or 3-substituted 5,6,7 substituted chromones are of use in treatment of treating diseases associated with overproduction of TNF-α, diseases associated with overproduction of superoxide anion radical And the treatment of organ damage. Some of the compounds are novel.

    摘要翻译： 某些2-和/或3-取代的5,6,7取代的色酮可用于治疗与过量产生TNF-α相关的疾病，与超氧阴离子自由基过量生成相关的疾病和器官损害的治疗。 一些化合物是新的。

    Preparation of 7-(3-(propylamino)-2-hydroxypropoxy)flavone
    7.
    发明授权
    Preparation of 7-(3-(propylamino)-2-hydroxypropoxy)flavone 失效
    7-（3-（丙基氨基）-2-羟基丙氧基）黄酮的制备

    公开(公告)号：US4758679A

    公开(公告)日：1988-07-19

    申请号：US887757

    申请日：1986-07-18

    申请人： Hans F. Schmitthenner ,  Edwin S. C. Wu

    发明人： Hans F. Schmitthenner ,  Edwin S. C. Wu

    IPC分类号： C07D311/30

    CPC分类号： C07D311/30

    摘要： In a process for preparing 7-[3-(propylamino)-2-hydroxypropoxy]flavone by the reaction of 7-(2,3-epoxypropoxy)flavone and n-propylamine, the improvement which resides in treating the beta-aminochalcone by-product with a weak organic acid to convert the chalcone to the desired aminated flavone.

    摘要翻译： 在通过7-（2,3-环氧丙氧基）黄酮与正丙胺的反应制备7- [3-（丙基氨基）-2-羟基丙氧基]黄酮的方法中，改进在于处理β-氨基查尔酮 具有弱有机酸的产物将查耳酮转化成所需的胺化黄酮。

    Opioid and opioid-like compounds and uses thereof
    9.
    发明授权
    Opioid and opioid-like compounds and uses thereof 有权
    阿片样物质和阿片样物质化合物及其用途

    公开(公告)号：US07923454B2

    公开(公告)日：2011-04-12

    申请号：US10936431

    申请日：2004-09-08

    申请人： Edwin S. C. Wu ,  Mao-Hsiung Yen ,  Chin-Tsai Fan

    发明人： Edwin S. C. Wu ,  Mao-Hsiung Yen ,  Chin-Tsai Fan

    IPC分类号： A61K31/4748 ,  C07D221/28

    CPC分类号： A61K31/485 ,  C07D221/28 ,  C07D489/00 ,  C07D489/02 ,  C07D489/08

    摘要： The present invention relates to opioid and opioid-like compounds, and pharmaceutical formulations containing the same and methods of use thereof. Uses of the present invention include, but are not limited to, use for the prevention and treatment of septic shock and other disorders. The compounds described herein can be water soluble and can act through mechanisms mediated through pathways other than opiate receptors.

    摘要翻译： 本发明涉及阿片样物质和阿片样物质化合物，以及含有其的药物制剂及其使用方法。 本发明的用途包括但不限于用于预防和治疗败血性休克和其它疾病的用途。 本文所述的化合物可以是水溶性的，并且可以通过除阿片受体之外的途径介导的机制起作用。