Methods and compositions for converting taxane amides to paclitaxel or other taxanes
    5.
    发明授权
    Methods and compositions for converting taxane amides to paclitaxel or other taxanes 有权
    将紫杉烷酰胺转化为紫杉醇或其他紫杉烷的方法和组合物

    公开(公告)号:US07605278B2

    公开(公告)日:2009-10-20

    申请号:US10522696

    申请日:2003-08-04

    IPC分类号: C07D305/14 C07D493/00

    摘要: The invention relates to methods and compositions for converting taxane amides to paclitaxel or other taxanes. In one alternative embodiment, the present invention comprises; (i) selectively protecting at least one OH group of a taxane amide; (ii) contacting the taxane amide with a transition metal compound to reduce the amide; (iii) contacting the reduced amide with an agent capable of substantially removing the transition metal; (iv) contacting the reduced amide with a hydrolyzing amount of acid to form a taxane amine salt in solution; (v) adding a sufficient amount of solvent to solidify the amine salt; and (vi) converting the taxane amine salt into paclitaxel or other taxanes.

    摘要翻译: 本发明涉及将紫杉烷酰胺转化为紫杉醇或其他紫杉烷的方法和组合物。 在一个替代实施例中,本发明包括: (i)选择性保护紫杉烷酰胺的至少一个OH基团; (ii)使紫杉烷酰胺与过渡金属化合物接触以还原酰胺; (iii)使还原酰胺与能够基本除去过渡金属的试剂接触; (iv)使还原酰胺与水解量的酸接触以在溶液中形成紫杉烷胺盐; (v)加入足够量的溶剂以固化胺盐; 和(vi)将紫杉烷胺盐转化成紫杉醇或其他紫杉烷。

    Methods And Compositions For Converting Taxane Amides To Paclitaxel Or Other Taxanes
    7.
    发明申请
    Methods And Compositions For Converting Taxane Amides To Paclitaxel Or Other Taxanes 有权
    将紫杉烷酰胺转化为紫杉醇或其他紫杉烷的方法和组合物

    公开(公告)号:US20080051589A1

    公开(公告)日:2008-02-28

    申请号:US10522696

    申请日:2003-08-04

    IPC分类号: C07D305/14

    摘要: The invention relates to methods and compositions for converting taxane amides to paclitaxel or other taxanes. In one alternative embodiment, the present invention comprises; (i) selectively protecting at least one OH group of a taxane amide; (ii) contacting the taxane amide with a transition metal compound to reduce the amide; (iii) contacting the reduced amide with an agent capable of substantially removing the transition metal; (iv) contacting the reduced amide with a hydrolyzing amount of acid to form a taxane amine salt in solution; (v) adding a sufficient amount of solvent to solidify the amine salt; and (vi) converting the taxane amine salt into paclitaxel or other taxanes.

    摘要翻译: 本发明涉及将紫杉烷酰胺转化为紫杉醇或其他紫杉烷的方法和组合物。 在一个替代实施例中,本发明包括: (i)选择性保护紫杉烷酰胺的至少一个OH基团; (ii)使紫杉烷酰胺与过渡金属化合物接触以还原酰胺; (iii)使还原酰胺与能够基本除去过渡金属的试剂接触; (iv)使还原酰胺与水解量的酸接触以在溶液中形成紫杉烷胺盐; (v)加入足够量的溶剂以固化胺盐; 和(vi)将紫杉烷胺盐转化成紫杉醇或其他紫杉烷。

    Selective acylation of secondary hydroxyl groups
    9.
    发明授权
    Selective acylation of secondary hydroxyl groups 有权
    仲羟基的选择性酰化

    公开(公告)号:US07176325B2

    公开(公告)日:2007-02-13

    申请号:US10510063

    申请日:2003-04-05

    CPC分类号: C07D305/14

    摘要: The invention provides methods and compositions for selectively acylating a specific hydroxyl group in a molecule of interest containing at least two unprotected secondary hydroxyl groups. Although the methods and compositions of the invention have general applicability, they are particularly useful in the selective acylation of taxane molecules.

    摘要翻译: 本发明提供用于选择性酰化目标分子中特定羟基的方法和组合物,其含有至少两个未被保护的仲羟基。 尽管本发明的方法和组合物具有一般适用性,但它们在紫杉烷分子的选择性酰化中特别有用。

    Process for large-scale isolation and purification of hypothalamic inhibitory factor
    10.
    发明授权
    Process for large-scale isolation and purification of hypothalamic inhibitory factor 失效
    大规模分离和纯化下丘脑抑制因子的方法

    公开(公告)号:US06998470B1

    公开(公告)日:2006-02-14

    申请号:US09506246

    申请日:2000-02-17

    CPC分类号: C07H15/24

    摘要: The present invention relates to a method of isolating and/or purifying hypothalamic inhibitory factor (HIF) from a sample (e.g., tissue fluid) containing HIF. The present invention provides for isolation of large amounts of HIF using diafiltration, solid phase extraction and immunoaffinity techniques. In one embodiment, the invention relates to a method of purifying hypothalamic inhibitory factor from a sample containing hypothalamic inhibitory factor comprising subjecting the sample to diafiltration, solid phase extraction and immunoaffintiy chromatography. In a particular embodiment, the invention relates to subjecting the sample to diafiltration to produce a diafiltrate of HIF; subjecting the diafiltrate to a first solid phase extraction (SPE) to produce a first fraction of HIF; subjecting the first fraction to immunoaffinity chromatography, wherein an antibody which binds to HIF is coupled to an immunoaffinity column, to produce a second fraction of HIF; subjecting the second fraction of HIF to reverse phase HPLC chromatography to produce a third fraction of HIF; and recovering purified HIF from the third fraction.

    摘要翻译: 本发明涉及从含有HIF的样品(例如组织液)中分离和/或纯化下丘脑抑制因子(HIF)的方法。 本发明提供使用渗滤,固相萃取和免疫亲和技术分离大量HIF。 在一个实施方案中,本发明涉及从含有下丘脑抑制因子的样品中纯化下丘脑抑制因子的方法,包括使样品进行渗滤,固相萃取和免疫亲和层析。 在一个具体实施方案中,本发明涉及对样品进行渗滤以产生HIF的渗滤液; 对渗滤液进行第一固相萃取(SPE)以产生HIF的第一部分; 使第一级分进行免疫亲和层析,其中结合HIF的抗体与免疫亲和柱偶联以产生HIF的第二级分; 使HIF的第二部分反相HPLC色谱以产生第三部分HIF; 并从第三级分回收纯化的HIF。