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70 条记录 (耗时 0.05 秒)

    Cytotoxic agents comprising new maytansinoids
    54.
    发明授权
    Cytotoxic agents comprising new maytansinoids 有权
    包含新的美登木素生物碱的细胞毒剂

    公开(公告)号：US07473796B2

    公开(公告)日：2009-01-06

    申请号：US11778464

    申请日：2007-07-16

    申请人： Ravi V. J. Chari ,  Wayne C. Widdison

    发明人： Ravi V. J. Chari ,  Wayne C. Widdison

    IPC分类号： C07C229/00 ,  C07C315/00 ,  C07D267/22

    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。

    Blocked lectins; methods and affinity support for making the same using affinity ligands; and method of killing selected cell populations having reduced non-selective cytotoxicity
    58.
    发明授权
    Blocked lectins; methods and affinity support for making the same using affinity ligands; and method of killing selected cell populations having reduced non-selective cytotoxicity 失效
    阻断凝集素; 方法和亲和力支持使用亲和配体进行相同; 以及杀死所选择的具有降低的非选择性细胞毒性的细胞群的方法

    公开(公告)号：US5395924A

    公开(公告)日：1995-03-07

    申请号：US19831

    申请日：1993-02-19

    申请人： Walter A. Blattler ,  John M. Lambert ,  Victor S. Goldmacher ,  Ravi V. J. Chari ,  Charles F. Scott, Jr. ,  Linda J. Kostuba ,  Simon E. Moroney ,  Albert R. Collison

    发明人： Walter A. Blattler ,  John M. Lambert ,  Victor S. Goldmacher ,  Ravi V. J. Chari ,  Charles F. Scott, Jr. ,  Linda J. Kostuba ,  Simon E. Moroney ,  Albert R. Collison

    IPC分类号： A61K47/48 ,  C07H21/00 ,  C07K3/00 ,  A61K39/00

    CPC分类号： C07H21/00 ,  A61K47/48438

    摘要： An activated affinity ligand is described comprising: a ligand having (a) a region with affinity for binding sites of a lectin; and (b) a reactive group capable of covalently linking the ligand to the lectin to thereby block one or more of the binding sites of the lectin. A blocked lectin is described comprising one or more affinity ligands covalently linked by means of a reactive group present on each of the ligands to a lectin such that one or more binding sites of the lectin is blocked. A cell-binding agent-blocked lectin conjugate is described comprising the above-described blocked lectin and a cell-binding agent covalently linked to: (a) one of the covalently linked affinity ligands; or (b) the lectin. A method of preparing the cell-binding agent-blocked lectin conjugate is described. An affinity support capable of binding to a lectin to form a blocked lectin is described comprising an activated affinity ligand covalently linked to a solid support. A method of preparing the affinity support capable of binding to a lectin to form a blocked lectin is described. A method of killing selected cell populations having reduced cytotoxicity to non-selected cell populations is described comprising contacting a cell population or tissue suspected of containing cells from said selected cell population with the above-described cell-binding agent-blocked lectin conjugate, wherein the lectin is a cytotoxic lectin. Medicaments and methods of treatment using the above-described cell-binding agent-blocked lectin conjugate also are described.

    摘要翻译： 描述了活化的亲和配体，其包括：具有（a）对凝集素的结合位点具有亲和力的区域的配体; 和（b）能够将配体与凝集素共价连接从而阻断凝集素的一个或多个结合位点的反应性基团。 描述了封闭的凝集素，其包含通过存在于每个配体上的反应性基团与凝集素共价连接的一个或多个亲和配体，使得凝集素的一个或多个结合位点被阻断。 描述了包含上述封闭凝集素和共价连接的细胞结合剂的细胞结合剂阻断的凝集素缀合物：（a）共价连接的亲和配体之一; 或（b）凝集素。 描述了制备细胞结合剂阻断的凝集素缀合物的方法。 描述了能够结合凝集素以形成封闭的凝集素的亲和载体，其包含与固体支持物共价连接的活化的亲和配体。 描述了制备能够结合凝集素形成封闭的凝集素的亲和载体的方法。 描述了杀死对未选择的细胞群体具有降低的细胞毒性的选定细胞群的方法，其包括使来自所述选择的细胞群的怀疑含有细胞的细胞群体或组织与上述细胞结合剂阻断的凝集素缀合物接触，其中 凝集素是一种细胞毒素凝集素。 还描述了使用上述细胞结合剂阻断的凝集素缀合物的药物和治疗方法。

    Cytotoxic benzodiazepine derivatives and methods of preparation
    59.
    发明授权
    Cytotoxic benzodiazepine derivatives and methods of preparation 有权
    细胞毒性苯二氮卓衍生物及其制备方法

    公开(公告)号：US09534000B2

    公开(公告)日：2017-01-03

    申请号：US13984762

    申请日：2012-02-15

    申请人： Ravi V. J. Chari

    发明人： Ravi V. J. Chari

    IPC分类号： A61K31/5517 ,  A61K47/48 ,  C07D519/00 ,  C07D487/04 ,  A61K45/06 ,  C07K16/30 ,  A61K39/00

    CPC分类号： C07K16/30 ,  A61K31/5517 ,  A61K45/06 ,  A61K47/545 ,  A61K47/6803 ,  A61K47/6849 ,  A61K47/6851 ,  A61K47/6867 ,  A61K2039/505 ,  C07D487/04 ,  C07D519/00 ,  C07K2317/24 ,  C07K2317/92 ,  C07K2317/94

    摘要： The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds, such as those in formulas (V)-(VII). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The present invention is further directed to methods of preparing a conjugate of a cell-binding agent and a cytotoxic compound. The methods comprise the use of an imine reactive compound to enable efficient conjugations of cytotoxic compounds with cell binding agents.

    摘要翻译： 本发明涉及具有抗增殖活性的新型苯并二氮杂衍生物，更具体地涉及新的苯并二氮杂化合物，如式（Ⅴ） - （Ⅶ）中的那些。 本发明还提供了与细胞结合剂连接的苯并二氮杂类化合物的缀合物。 本发明还提供了使用本发明的化合物或缀合物来抑制哺乳动物异常细胞生长或治疗增殖性病症的组合物和方法。 本发明还涉及制备细胞结合剂和细胞毒性化合物的缀合物的方法。 所述方法包括使用亚胺反应性化合物以使细胞毒性化合物与细胞结合剂的有效缀合。