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    Kavalactone profile
    22.
    发明申请
    Kavalactone profile 失效
    Kavalactone简介

    公开(公告)号：US20040072897A1

    公开(公告)日：2004-04-15

    申请号：US10273943

    申请日：2002-10-18

    发明人： Robert Gow ,  John Pierce ,  Brian Pierce ,  William Birdsall

    IPC分类号： A61K031/366

    CPC分类号： C07D407/06 ,  A61K31/365 ,  A61K31/366 ,  A61K36/185 ,  A61K36/21 ,  A61K36/258 ,  A61K36/28 ,  A61K36/41 ,  A61K36/46 ,  A61K36/48 ,  A61K36/481 ,  A61K36/67 ,  A61K36/74 ,  A61K36/76 ,  A61K36/888 ,  A61K36/889 ,  A61K36/8988 ,  A61K36/9066 ,  A61K45/06 ,  C07D309/32 ,  C07D309/38 ,  C07D309/40 ,  A61K2300/00

    摘要： A method of producing a processed kava product involves using an extraction solvent, such as liquid CO2, to preferentially extract different kavalactones from the source material at different rates. By controlling the extraction parameters and stopping the extraction before all of the kavalactones have been extracted or allowing the extracted kavalactones to be preferentially precipitated in one or more collection environments, a processed kava product can be produced that has a kavalactone distribution profile that can differ substantially from that of the source material. As a result, roots from a less desirable kava cultivar can be used to produce a processed kava product which has a kavalactone distribution profile that is similar to that of a highly desired cultivar. A material having a preferred kavalactone distribution profile is also disclosed. The kava paste can be further processed to produce a dry flowable powder suitable for use in, e.g., a tableting formula. A rapid dissolve tablet formulation for use in the delivery of kavalactones is also disclosed.

    摘要翻译： 生产加工的卡瓦产品的方法涉及使用诸如液体CO 2的提取溶剂以不同的速率从源材料中优先提取不同的卡维乳糖。 通过控制提取参数并在所有的Kavalactone已被提取之前停止提取，或允许提取的kavalactones在一个或多个收集环境中优先沉淀，可以生产具有可以显着差异的Kavalactone分布分布的加工的卡瓦产品 从源材料。 结果，来自较不理想的卡拉品种的根可以用于生产加工的卡瓦产品，其具有与高度期望的品种相似的考卡内酯分布轮廓。 还公开了具有优选的卡维内酯分布特性的材料。 可以进一步处理卡瓦酱以产生适用于例如压片配方的干燥可流动粉末。 还公开了一种用于投放kavalactones的快速溶解片剂制剂。

    2-phenylpyran-4-one derivatives
    29.
    发明申请
    2-phenylpyran-4-one derivatives 失效
    2-苯基吡喃-4-酮衍生物

    公开(公告)号：US20020045644A1

    公开(公告)日：2002-04-18

    申请号：US09809645

    申请日：2001-03-16

    发明人： Maria Isabel Crespo Crespo ,  Juan Miguel Jimenez Mayorga ,  Carles Puig Duran ,  Lidia Soca Pueyo

    IPC分类号： C07D47/02 ,  C07D49/02 ,  A61K031/4433 ,  A61K031/351

    CPC分类号： C07D405/04 ,  C07C311/29 ,  C07C317/24 ,  C07D309/38 ,  C07D309/40 ,  C07D409/04

    摘要： 2-Phenylpyran-4-one derivatives of formula (I): 1 wherein: R1 represents an alkyl or nullNR4R5 group, wherein R4 and R5 each independently represents a hydrogen atom or an alkyl group; R2 represents an alkyl, C3-C7 cycloalkyl, pyridyl, thienyl, naphthyl, tetrahydronaphthyl or indanyl group, or a phenyl group which may be unsubstituted or substituted by one or more halogen atoms or alkyl, trifluoromethyl, hydroxy, alkoxy, methylthic, amino, mono- or dialkylamino, hydroxalkyl or hydroxycarbonyl groups; R3 represents a methyl, hydroxymethyl, alkoxymethyl, C3-C7 cycloalkoxymethyl, benzyloxymethyl, hydroxycarbonyl, nitrile, trifluoromethyl or difluoromethyl group or a CH2nullR6 group wherein R6 represents an alkyl group; and X represents a single bond, an oxygen atom, a sulfur atom or a methylene group; or pharmaceutically acceptable salts thereof, processes for their production and synthetic intermediates used in said processes, pharmaceutical compositions containing them and their use in medical treatment.

    摘要翻译： 式（I）的2-苯基吡喃-4-酮衍生物：其中：R 1表示烷基或-NR 4 R 5基团，其中R 4和R 5各自独立地表示氢原子或烷基; R 2表示烷基，C 3 -C 7环烷基，吡啶基，噻吩基，萘基，四氢萘基或茚满基，或可以未被取代或被一个或多个卤素原子或烷基，三氟甲基，羟基，烷氧基，甲基，氨基， 单或二烷基氨基，羟烷基或羟基羰基; R3表示甲基，羟甲基，烷氧基甲基，C3-C7环烷氧基甲基，苄氧基甲基，羟基羰基，腈，三氟甲基或二氟甲基或CH2-R6基团，其中R6表示烷基; X表示单键，氧原子，硫原子或亚甲基; 或其药学上可接受的盐，其生产方法和用于所述方法的合成中间体，含有它们的药物组合物及其在医疗中的用途。