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    Process for preparation of maytansinol
    4.
    发明申请
    Process for preparation of maytansinol 有权
    美登素的制备方法

    公开(公告)号：US20070112188A1

    公开(公告)日：2007-05-17

    申请号：US11594156

    申请日：2006-11-08

    申请人： Wayne Widdison ,  Ravi Chari

    发明人： Wayne Widdison ,  Ravi Chari

    IPC分类号： C07D491/14

    CPC分类号： C07D498/14 ,  C07D491/14

    摘要： The present invention describes the preparation of maytansinol by methods that minimize processing steps, and reduce solvent volumes, making the process more efficient, and scaleable. This process comprises a step of converting bridged acetals of maytansinol to maytansinol. The simplified processing also aids in lowering the potential for human exposure to chemicals. Also provided is an isolated C3 to C9 bridged acetal of maytansinol.

    摘要翻译： 本发明描述了通过使加工步骤最小化并减少溶剂体积，使该方法更有效和可扩缩的方法制备美登素的方法。 该方法包括将美登醇的桥联缩醛转化为美登素。 简化的处理也有助于降低人类接触化学品的可能性。 还提供了美登醇的分离的C3至C9桥连缩醛。

    CYTOTOXIC AGENTS COMPRISING NEW MAYTANSINOIDS
    6.
    发明申请
    CYTOTOXIC AGENTS COMPRISING NEW MAYTANSINOIDS 有权

    公开(公告)号：US20070269447A1

    公开(公告)日：2007-11-22

    申请号：US11778451

    申请日：2007-07-16

    申请人： Ravi Chari ,  Wayne Widdison

    发明人： Ravi Chari ,  Wayne Widdison

    IPC分类号： A61K39/00 ,  A61P35/00

    CPC分类号： A61K39/39558 ,  A61K31/5365 ,  A61K47/6803 ,  A61K2039/505 ,  C07D498/16

    摘要： New thiol and disulfide-containing maytansinoids bearing a mono or di-alkyl substitution on the α-carbon atom bearing the sulfur atom are disclosed. Also disclosed are methods for the synthesis of these new maytansinoids and methods for the linkage of these new maytansinoids to cell-binding agents. The maytansinoid-cell-binding agent conjugates are useful as therapeutic agents, which are delivered specifically to target cells and are cytotoxic. These conjugates display vastly improved therapeutic efficacy in animal tumor models compared to the previously described agents.

    CYTOTOXIC AGENTS COMPRISING NEW MAYTANSINOIDS
    7.
    发明申请
    CYTOTOXIC AGENTS COMPRISING NEW MAYTANSINOIDS 有权
    包含新的可待因腺苷的细胞毒性剂

    公开(公告)号：US20070264266A1

    公开(公告)日：2007-11-15

    申请号：US11778437

    申请日：2007-07-16

    申请人： Ravi Chari ,  Wayne Widdison

    发明人： Ravi Chari ,  Wayne Widdison

    IPC分类号： A61K39/395 ,  A61P35/04 ,  C07D491/08 ,  C07K16/00

    CPC分类号： A61K39/39558 ,  A61K31/5365 ,  A61K47/6803 ,  A61K2039/505 ,  C07D498/16

    摘要： New thiol and disulfide-containing maytansinoids bearing a mono or di-alkyl substitution on the α-carbon atom bearing the sulfur atom are disclosed. Also disclosed are methods for the synthesis of these new maytansinoids and methods for the linkage of these new maytansinoids to cell-binding agents. The maytansinoid-cell-binding agent conjugates are useful as therapeutic agents, which are delivered specifically to target cells and are cytotoxic. These conjugates display vastly improved therapeutic efficacy in animal tumor models compared to the previously described agents.

    摘要翻译： 公开了在带有硫原子的α-碳原子上带有单或二烷基取代的新的含硫醇和二硫化物的美登木素生物碱。 还公开了合成这些新的美登木素生物碱的方法和将这些新的美登木素生物素连接到细胞结合剂的方法。 美登木素生物碱 - 细胞结合剂缀合物可用作治疗剂，其特异性递送至靶细胞并且是细胞毒性的。 与先前描述的试剂相比，这些缀合物在动物肿瘤模型中显示出显着改善的治疗功效。

    CYTOTOXIC AGENTS COMPRISING NEW MAYTANSINOIDS
    8.
    发明申请
    CYTOTOXIC AGENTS COMPRISING NEW MAYTANSINOIDS 有权

    公开(公告)号：US20070270585A1

    公开(公告)日：2007-11-22

    申请号：US11778464

    申请日：2007-07-16

    申请人： Ravi Chari ,  Wayne Widdison

    发明人： Ravi Chari ,  Wayne Widdison

    IPC分类号： C07D491/14

    CPC分类号： A61K39/39558 ,  A61K31/5365 ,  A61K47/6803 ,  A61K2039/505 ,  C07D498/16

    摘要： New thiol and disulfide-containing maytansinoids bearing a mono or di-alkyl substitution on the α-carbon atom bearing the sulfur atom are disclosed. Also disclosed are methods for the synthesis of these new maytansinoids and methods for the linkage of these new maytansinoids to cell-binding agents. The maytansinoid-cell-binding agent conjugates are useful as therapeutic agents, which are delivered specifically to target cells and are cytotoxic. These conjugates display vastly improved therapeutic efficacy in animal tumor models compared to the previously described agents.

    Method for the preparation of maytansinoid esters
    9.
    发明申请
    Method for the preparation of maytansinoid esters 有权
    美登木素生物酯酯的制备方法

    公开(公告)号：US20060167245A1

    公开(公告)日：2006-07-27

    申请号：US11334478

    申请日：2006-01-19

    申请人： Wayne Widdison ,  Ravi Chari

    发明人： Wayne Widdison ,  Ravi Chari

    IPC分类号： C07D491/04

    CPC分类号： C07D498/18

    摘要： Improved processes for the preparation and purification of maytansinoid esters, especially thiol and disulfide-containing maytansinoids are described. In one aspect the process comprises a process of making a maytansinoid ester comprising forming an anion of maytansinol or a maytansinoid bearing a free C-3 hydroxyl moiety and reacting the anion with an activated carboxyl compound to thereby produce the maytansinoid ester.

    摘要翻译： 描述了用于制备和纯化美登木素生物碱酯，特别是硫醇和二硫化物的美登木素生物碱的改进方法。 在一个方面，该方法包括制备美登木素生物碱酯的方法，其包括形成美登醇的阴离子或含有游离C-3羟基部分的美登木素生物碱，并使阴离子与活化的羧基化合物反应，从而产生美登木酯生物酯。