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    Cytotoxic agents containing novel potent taxanes and their therapeutic use
    12.
    发明申请
    Cytotoxic agents containing novel potent taxanes and their therapeutic use 失效
    含有新型有效紫杉烷类及其治疗用途的细胞毒素

    公开(公告)号：US20050026997A1

    公开(公告)日：2005-02-03

    申请号：US10926192

    申请日：2004-08-26

    申请人： Erkan Baloglu ,  Michael Miller ,  Ravi Chari

    发明人： Erkan Baloglu ,  Michael Miller ,  Ravi Chari

    IPC分类号： A61K31/337 ,  A61P31/04 ,  A61P31/12 ,  A61P33/00 ,  A61P35/00 ,  A61P37/06 ,  A61P43/00 ,  C07D305/14 ,  C07D407/12 ,  C07D407/14 ,  C07D409/12 ,  C07

    CPC分类号： C07D407/12 ,  A61K31/337 ,  C07D305/14 ,  C07D407/14 ,  C07D409/12 ,  Y02A50/423 ,  Y02A50/491

    摘要： Included within the scope of the present invention are potent taxanes and taxanes containing a linking group. Also included is a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for inducing cell death in selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient is also included. A method for inducing cell death in selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent is included as well.

    摘要翻译： 包括在本发明范围内的有效的紫杉烷类和含有连接基团的紫杉烷类。 还包括细胞毒性剂，其包含与细胞结合剂连接的一种或多种紫杉烷类。 一种用于在所选细胞群体中诱导细胞死亡的治疗组合物，包括：（A）细胞毒量的一种或多种通过连接基团与细胞结合剂共价结合的紫杉烷，和（B）药学上可接受的载体，稀释剂或赋形剂 包括。 还包括诱导选择的细胞群体中的细胞死亡的方法，包括使靶细胞或含有靶细胞的组织与有效量的包含与细胞结合剂连接的一种或多种紫杉烷的细胞毒性试剂接触。

    CYTOTOXIC AGENTS COMPRISING NEW MAYTANSINOIDS
    13.
    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
    14.
    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 taxanes and their therapeutic use
    15.
    发明申请
    Cytotoxic agents comprising taxanes and their therapeutic use 失效
    包含紫杉烷及其治疗用途的细胞毒素

    公开(公告)号：US20070197775A1

    公开(公告)日：2007-08-23

    申请号：US11785483

    申请日：2007-04-18

    申请人： Ravi Chari ,  Walter Blattler

    发明人： Ravi Chari ,  Walter Blattler

    IPC分类号： C07K14/54 ,  C07K14/56 ,  C07K16/46

    CPC分类号： C07D305/14 ,  A61K31/337 ,  A61K47/6803 ,  A61K47/6849 ,  A61K47/6851 ,  A61K47/6881 ,  A61K2039/505 ,  C07K16/2863 ,  C07K16/32 ,  Y02A50/423 ,  Y02A50/491

    摘要： A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.

    摘要翻译： 包含与细胞结合剂连接的一种或多种紫杉烷类的细胞毒性剂。 一种用于杀死所选细胞群的治疗组合物，其包含：（A）细胞毒性量的一种或多种通过连接基团与细胞结合剂共价结合的紫杉烷，和（B）药学上可接受的载体，稀释剂或赋形剂。 一种杀死所选细胞群体的方法，包括使含有目标细胞的靶细胞或组织与有效量的细胞毒性剂接触，所述细胞毒剂包含与细胞结合剂连接的一种或多种紫杉烷类。 新型含硫紫杉烷。

    Prodrugs of CC-1065 analogs
    16.
    发明申请
    Prodrugs of CC-1065 analogs 失效
    CC-1065类似物的前药

    公开(公告)号：US20070135346A1

    公开(公告)日：2007-06-14

    申请号：US11649822

    申请日：2007-01-05

    申请人： Robert Zhao ,  Ravi Chari

    发明人： Robert Zhao ,  Ravi Chari

    IPC分类号： A61K31/496 ,  A61K31/4545 ,  A61K38/16 ,  C07K14/00 ,  C07D403/14

    CPC分类号： C07D307/85 ,  A61K31/407 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/496 ,  A61K31/675 ,  A61K47/545 ,  A61K47/548 ,  A61K47/60 ,  C07D209/42 ,  C07D209/60 ,  C07D403/14 ,  C07D405/12 ,  C07F9/5728 ,  C07F9/65583 ,  Y02A50/423 ,  Y02A50/491 ,  Y02P20/55

    摘要： Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytoxic drugs in a targeted fashion.

    摘要翻译： 具有可切割保护基的抗肿瘤抗生素CC-1065类似物的前药，例如哌嗪基氨基甲酸酯，4-哌啶子基 - 哌啶子基氨基甲酸酯或磷酸酯，其中保护基团赋予增强的水溶性和在前药上的稳定性， 其中前药还具有可与细胞结合试剂例如抗体缀合的部分，例如二硫化物。 还描述了这种前药缀合物的治疗用途; 这种细胞毒性药物的前药具有治疗用途，因为它们可以将细胞毒性前体药物递送至特定细胞群体，以靶向方式酶促转化为细胞毒性药物。

    Method and apparatus for optical spectroscopic detection of cell and tissue death
    18.
    发明申请
    Method and apparatus for optical spectroscopic detection of cell and tissue death 审中-公开
    光学检测细胞和组织死亡的方法和装置

    公开(公告)号：US20050119548A1

    公开(公告)日：2005-06-02

    申请号：US10955331

    申请日：2004-09-30

    申请人： Wei-Chiang Lin ,  Steven Toms ,  Anita Mahadevan-Jansen ,  Ravi Chari

    发明人： Wei-Chiang Lin ,  Steven Toms ,  Anita Mahadevan-Jansen ,  Ravi Chari

    IPC分类号： A61B20060101 ,  A61B5/00 ,  A61B6/00

    CPC分类号： A61B5/0071 ,  A61B5/0075 ,  A61B5/0084 ,  A61B5/4244

    摘要： A method for detecting death process of a cell or tissue of a living subject. In one embodiment, the method includes the steps of illuminating the cell or tissue of the living subject with a coherent light, collecting fluorescent light returned from the illuminated cell or tissue of the living subject, identifying a NAD(P)H peak of a spectrum of the collected fluorescent light with a wavelength, λpeak, and obtaining the intensity of the NAD(P)H peak of the spectrum of the collected fluorescent light substantially corresponding to the wavelength λpeak. These steps are repeated at sequential stages until the intensity of the NAD(P)H peak of the spectrum at a current stage is less than the intensity of the NAD(P)H peak of the spectrum at an earlier stage immediately prior to the current stage so as to detect death process of the cell of the living subject at the current stage using the intensity of the NAD(P)H peak of the spectrum.

    摘要翻译： 一种用于检测活体受试者的细胞或组织的死亡过程的方法。 在一个实施例中，该方法包括以相干光照射活体的细胞或组织的步骤，收集从活体受试者的照射细胞或组织返回的荧光，识别光谱的NAD（P）H峰 收集的具有波长λλ峰值的荧光，并且获得基本上对应于波长λ的峰的峰的收集的荧光的光谱的NAD（P）H峰的强度， / SUB>。 这些步骤在连续阶段重复，直到当前阶段的光谱的NAD（P）H峰的强度小于在电流之前的较早阶段的光谱的NAD（P）H峰的强度 使用光谱的NAD（P）H峰的强度来检测当前阶段的活体的细胞的死亡过程。