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    Heterocyclic-substituted bis-1,8 naphthalimide compounds, antibody drug conjugates, and methods of use
    1.
    发明申请
    Heterocyclic-substituted bis-1,8 naphthalimide compounds, antibody drug conjugates, and methods of use 有权
    杂环取代的双-1,8萘二甲酰亚胺化合物，抗体药物共轭物和使用方法

    公开(公告)号：US20060182751A1

    公开(公告)日：2006-08-17

    申请号：US11342937

    申请日：2006-01-30

    申请人： Lewis Gazzard ,  Edward Ha ,  David Jackson ,  Joann Um

    发明人： Lewis Gazzard ,  Edward Ha ,  David Jackson ,  Joann Um

    IPC分类号： A61K39/395 ,  C07K16/46 ,  C07D413/14 ,  C07D403/14

    CPC分类号： C07D221/14 ,  A61K47/6803 ,  A61K47/6875 ,  C07D401/14 ,  C07D471/04 ,  C07D491/04 ,  C07K16/32

    摘要： The invention relates to bis 1,8 naphthalimide compounds including antibody drug conjugate (ADC) compounds represented by Formula I: Ab-(L-D)p   I where one or more 1,8 bis-naphthalimide drug moieties (D) having Formulas IIa and IIb are covalently linked, through the wavy line, by a linker (L) to an antibody (Ab). The invention also relates to heterocyclic-substituted 1,8 bis-naphthalimide compounds having Formula XV The invention also relates to pharmaceutical compositions comprising an effective amount of a Formula I ADC or Formula XV heterocyclic-substituted 1,8 bis-naphthalimide compound for treatment of hyperproliferative disorders and other disorders. The invention also relates to methods for killing or inhibiting the proliferation of tumor cells or cancer cells including administering to a patient an effective amount of a Formula I ADC or Formula XV compound.

    摘要翻译： 本发明涉及包含由式I表示的抗体药物偶联物（ADC）化合物的双1,8萘二甲酰亚胺化合物：<？in-line-formula description =“In-line Formulas”end =“lead”？> Ab-（LD） 其中一个或多个具有式IIa和（VIII）的1,8-双萘二甲酰亚胺药物部分（D）的化合物 IIb通过波浪线通过连接体（L）与抗体（Ab）共价连接。 本发明还涉及具有式XV的杂环取代的1,8-双萘二甲酰亚胺化合物。本发明还涉及药物组合物，其包含有效量的式I ADC或式XV杂环取代的1,8-双萘二甲酰亚胺化合物，用于治疗 过度增殖性疾病和其他疾病。 本发明还涉及杀死或抑制肿瘤细胞或癌细胞增殖的方法，包括向患者施用有效量的式I ADC或式XV化合物。

    Antibody drug conjugates and methods
    2.
    发明申请
    Antibody drug conjugates and methods 审中-公开
    抗体药物偶联物和方法

    公开(公告)号：US20070134243A1

    公开(公告)日：2007-06-14

    申请号：US11311591

    申请日：2005-11-29

    申请人： Lewis Gazzard ,  Edward Ha ,  David Jackson ,  Joann Um

    发明人： Lewis Gazzard ,  Edward Ha ,  David Jackson ,  Joann Um

    IPC分类号： A61K39/395 ,  C07K16/46 ,  C07K16/28 ,  C07K16/24

    CPC分类号： C07D221/14 ,  A61K47/6803 ,  A61K47/6849 ,  A61K47/6855 ,  A61K47/6867 ,  A61K47/6875 ,  A61K47/6889 ,  C07D401/14 ,  C07D471/04 ,  C07D491/04 ,  C07K16/32

    摘要： The invention relates to antibody drug conjugate (ADC) compounds represented by Formula I: Ab-(L-D)p  I where one or more 1,8 bis-naphthalimide drug moieties (D) having Formulas IIa and IIb are covalently linked by a linker (L) to an antibody (Ab). The invention also relates to pharmaceutical compositions comprising an effective amount of a Formula I ADC for treatment of hyperproliferative disorders and other disorders. The invention also relates to methods for killing or inhibiting the multiplication of a tumor cell or cancer cell including administering to a patient an effective amount of a Formula I ADC.

    摘要翻译： 本发明涉及由式I表示的抗体药物偶联物（ADC）化合物：<？in-line-formula description =“In-line Formulas”end =“lead”？> Ab-（LD） > I <？in-line-formula description =“In-line Formulas”end =“tail”？>其中一个或多个具有式IIa和IIb的1,8-双萘二甲酰亚胺药物部分（D）通过连接体共价连接 （L）至抗体（Ab）。 本发明还涉及药物组合物，其包含有效量的用于治疗过度增殖性疾病和其它疾病的式IADC。 本发明还涉及杀死或抑制肿瘤细胞或癌细胞增殖的方法，包括向患者施用有效量的式I ADC。

    Caspase Activated Prodrugs Therapy
    4.
    发明申请
    Caspase Activated Prodrugs Therapy 审中-公开
    胱天蛋白酶活化前药治疗

    公开(公告)号：US20070104719A1

    公开(公告)日：2007-05-10

    申请号：US11537578

    申请日：2006-09-29

    申请人： Paul Carter ,  Lewis Gazzard

    发明人： Paul Carter ,  Lewis Gazzard

    IPC分类号： A61K39/395

    CPC分类号： C07K16/32 ,  A61K47/6899 ,  B82Y5/00 ,  C07K2317/24 ,  C07K2317/55

    摘要： The invention provides novel method for the localized delivery of pharmaceutical agents by the administration of a caspase conjugate that targets a cell type of interest and the additional administration of a pro-agent that is locally converted, in the presence of the caspase, to an active agent. The invention further provides novel tageting agents comprising a caspase as well as novel prodrugs comprising a caspase cleavable prodrug moiety. The invention also provides pharmaceutical compositions as well as methods of treatment comprising the caspase conjugates and prodrugs of the invention

    摘要翻译： 本发明提供了通过施用靶向感兴趣的细胞类型的半胱天冬酶缀合物来局部递送药物的新方法，并且在半胱天冬酶的存在下局部转化的前药的另外施用为活性 代理商 本发明进一步提供了包含胱天蛋白酶的新型标签试剂以及包含半胱天冬酶可切割前药部分的新型前体药物。 本发明还提供药物组合物以及包含本发明的半胱天冬酶缀合物和前药的治疗方法