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    Methods of preparing substituted tetracyclines with transition metal-based chemistries
    2.
    发明申请
    Methods of preparing substituted tetracyclines with transition metal-based chemistries 有权
    用过渡金属化学制备取代四环素的方法

    公开(公告)号：US20050187198A1

    公开(公告)日：2005-08-25

    申请号：US11004559

    申请日：2004-12-03

    申请人： Mark Nelson ,  Glen Rennie ,  Darrell Koza

    发明人： Mark Nelson ,  Glen Rennie ,  Darrell Koza

    IPC分类号： C07C231/12 ,  C07C237/26 ,  C07D295/185 ,  C07D295/192 ,  A61K31/65

    CPC分类号： C07D295/185 ,  C07C231/12 ,  C07C237/26 ,  C07C2603/46 ,  C07D295/192

    摘要： The present invention relates to novel chemistries which allow for heretofore unobtainable substituted tetracycline compounds which exhibit significant activity in tetracycline responsive states. The methods disclosed herein utilize reactive tetracycline-based precursor compounds, reactive organic substituent precursors and transition metal catalysts under conditions such that a tetracycline compound substituted with the desired organic substituent is formed. In one embodiment of the invention, a substituted tetracycline compound may be prepared by combining a reactive tetracycline-based precursor compound such as an arene tetracycline diazonium salt, and a reactive organic substituent precursor, e.g., alkenes, substituted alkenes, vinyl monomers, aromatics and heteroaromatics, in the presence of a transition metal catalyst, such as palladium chloride, under conditions such that a tetracycline compound substituted with the organic substituent is formed. Such compounds may optionally act as intermediates for making other compounds, e.g., hydrogenation of unsaturated groups on the substituent.

    摘要翻译： 本发明涉及允许迄今为止在四环素反应状态下表现出显着活性的未获得的取代四环素化合物的新化学物质。 本文公开的方法在形成被所需有机取代基取代的四环素化合物的条件下使用基于活性四环素的前体化合物，反应性有机取代基前体和过渡金属催化剂。 在本发明的一个实施方案中，取代的四环素化合物可以通过将活性四环素类前体化合物如芳族四环素重氮盐和反应性有机取代基前体例如烯烃，取代的烯烃，乙烯基单体，芳族化合物和 在过渡金属催化剂如氯化钯存在下，在形成被有机取代基取代的四环素化合物的条件下，进行杂芳族化合物。 这样的化合物可以任选地用作制备其它化合物的中间体，例如取代基上不饱和基团的氢化。

    7, 8 And 9-substituted tetracycline compounds
    5.
    发明申请
    7, 8 And 9-substituted tetracycline compounds 有权
    7,8和9-取代四环素化合物

    公开(公告)号：US20060229282A1

    公开(公告)日：2006-10-12

    申请号：US11454221

    申请日：2006-06-16

    申请人： Mark Nelson ,  Darrell Koza ,  Glen Rennie

    发明人： Mark Nelson ,  Darrell Koza ,  Glen Rennie

    IPC分类号： A61K31/65

    CPC分类号： C07C237/26

    摘要： 7, 8 and 9-substituted tetracycline compounds, methods of treating tetracycline responsive states, and pharmaceutical compositions containing the 7, 8 and 9-substituted tetracycline compounds are described.

    摘要翻译： 7,8和9-取代的四环素化合物，治疗四环素应答状态的方法，以及含有7,8和9-取代的四环素化合物的药物组合物。

    Methods of preparing substituted tetracyclines with transition metal-based chemistries
    6.
    发明申请
    Methods of preparing substituted tetracyclines with transition metal-based chemistries 失效

    公开(公告)号：US20060166946A1

    公开(公告)日：2006-07-27

    申请号：US11390902

    申请日：2006-03-28

    申请人： Mark Nelson ,  Glen Rennie ,  Darrell Koza

    发明人： Mark Nelson ,  Glen Rennie ,  Darrell Koza

    IPC分类号： A61K31/65 ,  C07C237/26

    CPC分类号： C07C237/26 ,  C07C231/12 ,  C07C2603/46

    摘要： The present invention relates to novel chemistries which allow for heretofore unobtainable substituted tetracycline compounds which exhibit significant antibacterial activity. The methods disclosed herein utilize reactive tetracycline-based precursor compounds, reactive organic substituent precursors and transition metal catalysts under conditions such that a tetracycline compound substituted with the desired organic substituent is formed. In one embodiment of the invention, a substituted tetracycline compound may be prepared by combining a reactive tetracycline-based precursor compound such as an arene tetracycline diazonium salt, and a reactive organic substituent precursor, e.g., alkenes, substituted alkenes, vinyl monomers, aromatics and heteroaromatics, in the presence of a transition metal catalyst, such as palladium chloride, under conditions such that a tetracycline compound substituted with the organic substituent is formed. Such compounds may optionally act as intermediates for making other compounds, e.g., hydrogenation of unsaturated groups on the substituent.