Ether compounds
    1.
    发明申请

    公开(公告)号:US20030065195A1

    公开(公告)日:2003-04-03

    申请号:US10205939

    申请日:2002-07-26

    摘要: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

    Fermentation and purification of mycolactones
    2.
    发明申请
    Fermentation and purification of mycolactones 失效
    霉菌内酯的发酵和纯化

    公开(公告)号:US20020086375A1

    公开(公告)日:2002-07-04

    申请号:US09921666

    申请日:2001-08-03

    IPC分类号: C12P017/02 C07D35/12

    CPC分类号: C12P17/08

    摘要: Fermentation based methods for producing mycolactones allows one to produce large quantities of mycolactones, which can be purified by extraction and chromatography to yield pure preparations of mycolactones A, B, C, and D.

    摘要翻译: 用于生产霉菌内酯的基于发酵的方法允许产生大量的霉菌内酯,其可以通过萃取和色谱法纯化以产生霉菌内酯A,B,C和D的纯制剂。

    Method for purification of paclitaxel from paclitaxel-containing materials
    3.
    发明申请
    Method for purification of paclitaxel from paclitaxel-containing materials 有权
    从含紫杉醇的材料中纯化紫杉醇的方法

    公开(公告)号:US20050154218A1

    公开(公告)日:2005-07-14

    申请号:US11028487

    申请日:2004-12-30

    IPC分类号: C07D305/14 C07D35/12

    CPC分类号: C07D305/14

    摘要: This invention relates to methods for purification of paclitaxel from a paclitaxel-containing material. The method comprises the following steps: (a) extracting a paclitaxel-containing material with an organic solvent to obtain an extract, and concentrating the extract; (b) adding the concentrate with an organic solvent which is not mixed with water to separate an organic solvent phase and then concentrating; (c) subjecting the concentrate to normal phase chromatography to obtain an eluate; (d) dissolving the eluate in an acetone or dichloromethane followed by adding pentane or hexane to form a precipitate; and (e) subjecting the precipitate to high performance liquid chromatography. According to the method of the present invention, paclitaxel of over 99.5% purity can be easily obtained from a Taxus genus plant with a high yield.

    摘要翻译: 本发明涉及从含紫杉醇的材料中纯化紫杉醇的方法。 该方法包括以下步骤:(a)用有机溶剂萃取含有紫杉醇的材料,得到提取物,浓缩提取物; (b)将浓缩物与不与水混合的有机溶剂加入以分离有机溶剂相,然后浓缩; (c)使浓缩物进行正相色谱以获得洗脱液; (d)将洗脱液溶解在丙酮或二氯甲烷中,然后加入戊烷或己烷以形成沉淀物; 和(e)使沉淀物进行高效液相色谱。 根据本发明的方法,可以容易地从具有高收率的紫杉属植物获得纯度超过99.5%的紫杉醇。

    Semi-synthesis of taxane intermediates from 9-dihydro-13-acetylbaccatin III
    6.
    发明申请
    Semi-synthesis of taxane intermediates from 9-dihydro-13-acetylbaccatin III 有权
    紫杉烷中间体半合成由9-二氢-13-乙酰浆果赤霉素III

    公开(公告)号:US20050101789A1

    公开(公告)日:2005-05-12

    申请号:US10695416

    申请日:2003-10-27

    申请人: Ragina Naidu

    发明人: Ragina Naidu

    IPC分类号: C07D305/14 C07D35/12

    CPC分类号: C07D305/14

    摘要: A method is provided for the semi-synthesis of taxane intermediates useful in the preparation of paclitaxel and docetaxel from 9-dihydro-13-acetylbaccatin III. The preparation of a suitably protected baccatin III backbone from 9-dihydro-13-acetylbaccatin III, and the insertion of the phenylisoserine side chain onto the protected baccatin III from 9-dihydro-13-acetylbaccatin III to form the taxane derivatives, paclitaxel and docetaxel is disclosed.

    摘要翻译: 提供了可用于制备9-二氢-13-乙酰浆果赤霉素III的紫杉醇和多西他赛的紫杉烷中间体的半合成方法。 从9-二氢-13-乙酰浆果赤霉素III制备适当保护的浆果赤霉素III主链,并将苯基异丝氨酸侧链从9-二氢-13-乙酰浆果赤霉素III插入到保护的浆果赤霉素III上以形成紫杉烷衍生物,紫杉醇和多西紫杉醇 被披露。

    Process for the preparation of hydroxylactones
    7.
    发明申请
    Process for the preparation of hydroxylactones 失效
    制备羟基内酯的方法

    公开(公告)号:US20020038040A1

    公开(公告)日:2002-03-28

    申请号:US09935770

    申请日:2001-08-24

    IPC分类号: C07D35/12

    CPC分类号: C07D307/33

    摘要: The present invention is directed towards a process for the preparation of enantiomerically enriched 4-hydroxymethyl-null-butyrolactone (I). By kinetic racemate cleavage of racemic epoxide of the general formula (II) 1 wherein R represents a (C1-C8)-alkyl radical, a (C8-C16)-aryl radical, with a nucleophile and a Jacobsen catalyst there is obtained enantiomerically enriched (I). 2 Use of the lactone so prepared.

    摘要翻译: 本发明涉及制备对映体富集的4-羟甲基-γ-丁内酯(I)的方法。 通过动力学外消旋物裂解通式(II)的外消旋环氧化物,其中R表示(C 1 -C 8) - 烷基,(C 8 -C 16) - 芳基,与亲核试剂和Jacobsen催化剂,得到对映体富集 一世)。 使用内酯如此准备。