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    PROTEIN KINASE INHIBITORS COMPRISING ATP MIMETICS CONJUGATED TO PEPTIDES OR PEPTIDOMIMETICS
    1.
    发明申请
    PROTEIN KINASE INHIBITORS COMPRISING ATP MIMETICS CONJUGATED TO PEPTIDES OR PEPTIDOMIMETICS 审中-公开
    蛋白激酶抑制剂包含连接于肽或蛋白质的ATP

    公开(公告)号：US20080070843A1

    公开(公告)日：2008-03-20

    申请号：US11862542

    申请日：2007-09-27

    申请人： Nurit Livnah ,  Tamar Yechezkel ,  Yosef Salitra ,  Boris Perlmutter ,  Onsat Ohne ,  Ilana Cohen

    发明人： Nurit Livnah ,  Tamar Yechezkel ,  Yosef Salitra ,  Boris Perlmutter ,  Onsat Ohne ,  Ilana Cohen

    IPC分类号： A61K38/08 ,  A61P29/00 ,  A61P3/04 ,  A61P3/10 ,  A61P35/00 ,  A61P37/00 ,  A61P9/00 ,  C07K7/06

    CPC分类号： C07K7/06 ,  A61K38/00 ,  A61K47/64

    摘要： The present invention provides small molecules having high affinity to the ATP binding site of protein kinases, which are conjugated to apeptide or peptidomimetic moiety which mimics the substrate of PKB. The chimeric compounds according to the present invention preferably serve as PKB inhibitors with improved activity and selectivity. Novel ATP mimetic compounds, particularly isoquinoline derivatives, conjugated with peptides or peptidomimetics are useful as inhibitors of protein kinases for experimental, medical, and drug design purposes. Furthermore, pharmaceutical compositions comprising these protein kinase inhibitors, and methods of using such compositions for treatment and diagnosis of cancers, diabetes, cardiovascular pathologies, hemorrhagic shock, obesity, inflammatory diseases, diseases of the central nervous system, and autoimmune disease, are disclosed.

    摘要翻译： 本发明提供对蛋白激酶的ATP结合位点具有高亲和力的小分子，其与模仿PKB底物的肽或肽模拟部分缀合。 根据本发明的嵌合化合物优选用作具有改善的活性和选择性的PKB抑制剂。 与肽或肽模拟物缀合的新型ATP模拟化合物，特别是异喹啉衍生物，可用作实验，医学和药物设计目的的蛋白激酶抑制剂。 此外，公开了包含这些蛋白激酶抑制剂的药物组合物，以及使用这些组合物治疗和诊断癌症，糖尿病，心血管病变，出血性休克，肥胖症，炎性疾病，中枢神经系统疾病和自身免疫疾病的方法。

    Protein kinase inhibitors comprising ATP mimetics conjugated to peptides or peptidomimetics
    2.
    发明授权
    Protein kinase inhibitors comprising ATP mimetics conjugated to peptides or peptidomimetics 失效
    蛋白激酶抑制剂包含与肽或肽模拟物缀合的ATP模拟物

    公开(公告)号：US07407939B2

    公开(公告)日：2008-08-05

    申请号：US10764288

    申请日：2004-01-23

    申请人： Nurit Livnah ,  Tamar Yechezkel ,  Yosef Salitra ,  Boris Perlmutter ,  Onsat Ohne ,  Ilana Cohen ,  Pninit Litman ,  Hanoch Senderowitz

    发明人： Nurit Livnah ,  Tamar Yechezkel ,  Yosef Salitra ,  Boris Perlmutter ,  Onsat Ohne ,  Ilana Cohen ,  Pninit Litman ,  Hanoch Senderowitz

    IPC分类号： A61K38/08 ,  A61K31/47

    CPC分类号： C07K7/06 ,  A61K38/00 ,  A61K47/64

    摘要： The present invention provides small molecules having high affinity to the ATP binding site of protein kinases, which are conjugated to apeptide or peptidomimetic moiety which mimics the substrate of PKB. The chimeric compounds according to the present invention preferably serve as PKB inhibitors with improved activity and selectivity. Novel ATP mimetic compounds, particularly isoquinoline derivatives, conjugated with peptides or peptidomimetics are useful as inhibitors of protein kinases for experimental, medical, and drug design purposes. Furthermore, pharmaceutical compositions comprising these protein kinase inhibitors, and methods of using such compositions for treatment and diagnosis of cancers, diabetes, cardiovascular pathologies, hemorrhagic shock, obesity, inflammatory diseases, diseases of the central nervous system, and autoimmune disease, are disclosed.

    摘要翻译： 本发明提供对蛋白激酶的ATP结合位点具有高亲和力的小分子，其与模仿PKB底物的肽或肽模拟部分缀合。 根据本发明的嵌合化合物优选用作具有改善的活性和选择性的PKB抑制剂。 与肽或肽模拟物缀合的新型ATP模拟化合物，特别是异喹啉衍生物，可用作实验，医学和药物设计目的的蛋白激酶抑制剂。 此外，公开了包含这些蛋白激酶抑制剂的药物组合物，以及使用这些组合物治疗和诊断癌症，糖尿病，心血管病变，出血性休克，肥胖症，炎性疾病，中枢神经系统疾病和自身免疫疾病的方法。

    Cell permeable conjugates of peptides for inhibition of protein kinases
    4.
    发明申请
    Cell permeable conjugates of peptides for inhibition of protein kinases 审中-公开
    用于抑制蛋白激酶的肽的细胞渗透性缀合物

    公开(公告)号：US20070078092A1

    公开(公告)日：2007-04-05

    申请号：US11295793

    申请日：2005-12-06

    申请人： Nurit Livnah ,  Alexander Levitzki ,  Hanoch Senderovitz ,  Tamar Yechezkel ,  Yosef Salitra ,  Pninit Litman ,  Osnat Ohne

    发明人： Nurit Livnah ,  Alexander Levitzki ,  Hanoch Senderovitz ,  Tamar Yechezkel ,  Yosef Salitra ,  Pninit Litman ,  Osnat Ohne

    IPC分类号： A61K38/55 ,  A61K38/08 ,  C12N9/99

    CPC分类号： A61K47/62

    摘要： The present invention provides inhibitors of protein kinases comprising a molecule having at least a first moiety competent for penetration of the molecule into cells, and a second moiety for having a protein kinase inhibiting effect within the cells. The first moiety is joined to the second moiety through a linker or a spacer. The complex molecules are preferably peptide conjugates having improved cell-permeability, serum stability and kinase selectivity compared to known protein kinase inhibitors. Pharmaceutical compositions that include these protein kinase inhibitors, and methods of using such compositions for treatment of cancers and other diseases associated with protein kinase activity are also disclosed.

    摘要翻译： 本发明提供了蛋白激酶抑制剂，其包含具有至少第一部分的分子的分子的分子进入细胞的分子，以及在细胞内具有蛋白激酶抑制作用的第二部分。 第一部分通过接头或间隔物连接到第二部分。 与已知的蛋白激酶抑制剂相比，复合分子优选是具有改善的细胞渗透性，血清稳定性和激酶选择性的肽缀合物。 还公开了包括这些蛋白激酶抑制剂的药物组合物，以及使用这些组合物治疗癌症和与蛋白激酶活性相关的其它疾病的方法。

    Photo-active backbone cyclized somatostatin analogs for photodynamic therapy and imaging
    5.
    发明申请
    Photo-active backbone cyclized somatostatin analogs for photodynamic therapy and imaging 有权
    光动力骨架环化生长抑素类似物用于光动力治疗和成像

    公开(公告)号：US20050090429A1

    公开(公告)日：2005-04-28

    申请号：US10950378

    申请日：2004-09-24

    申请人： Thomas Bonasera ,  Nurit Livnah ,  Yoseph Salitra ,  Tamar Yechezkel

    发明人： Thomas Bonasera ,  Nurit Livnah ,  Yoseph Salitra ,  Tamar Yechezkel

    IPC分类号： A61K38/00 ,  A61K38/16 ,  A61K41/00 ,  A61K49/00 ,  C07K14/655

    CPC分类号： A61K41/0057 ,  A61K38/00 ,  A61K41/0071 ,  A61K49/0036 ,  A61K49/0041 ,  A61K49/0043 ,  A61K49/0056 ,  C07K14/6555

    摘要： Novel photo-active labeled diagnostic and therapeutic peptides which are conformationally constrained backbone cyclized somatostatin analogs, having improved somatostatin receptor subtype affinity and selectivity are disclosed. The backbone cyclized peptide analogs disclosed possess unique and superior properties over other analogs, such as chemical and metabolic stability, selectivity, increased bioavailability and improved pharmacokinetics. Furthermore, the unique patterns of receptor subtype selectivity provide compounds having improved diagnostic and therapeutic utilities. Pharmaceutical compositions comprising the photo-active backbone cyclized somatostatin analogs, reagents for synthesizing same, and methods of using such compositions for diagnostic and therapeutic purposes including optical imaging and photodynamic therapy are also disclosed.

    摘要翻译： 公开了具有改善的生长抑素受体亚型亲和性和选择性的新型光活性标记的诊断和治疗肽，其是构象约束的骨架环化生长抑素类似物。 所公开的骨架环化肽类似物具有优于其它类似物的独特且优异的性质，例如化学和代谢稳定性，选择性，增加的生物利用度和改善的药代动力学。 此外，受体亚型选择性的独特模式提供具有改进的诊断和治疗效用的化合物。 还公开了包含光活性骨架环化的生长抑素类似物的药物组合物，用于合成它们的试剂，以及使用这些组合物用于包括光学成像和光动力疗法在内的诊断和治疗目的的方法。

    Photo-active backbone cyclized somatostatin analogs for photodynamic therapy and imaging
    6.
    发明授权
    Photo-active backbone cyclized somatostatin analogs for photodynamic therapy and imaging 有权
    光动力骨架环化生长抑素类似物用于光动力治疗和成像

    公开(公告)号：US07700717B2

    公开(公告)日：2010-04-20

    申请号：US10950378

    申请日：2004-09-24

    申请人： Thomas A. Bonasera ,  Nurit Livnah ,  Yoseph Salitra ,  Tamar Yechezkel

    发明人： Thomas A. Bonasera ,  Nurit Livnah ,  Yoseph Salitra ,  Tamar Yechezkel

    IPC分类号： A61K38/16

    CPC分类号： A61K41/0057 ,  A61K38/00 ,  A61K41/0071 ,  A61K49/0036 ,  A61K49/0041 ,  A61K49/0043 ,  A61K49/0056 ,  C07K14/6555

    摘要： Novel photo-active labeled diagnostic and therapeutic peptides which are conformationally constrained backbone cyclized somatostatin analogs, having improved somatostatin receptor subtype affinity and selectivity are disclosed. The backbone cyclized peptide analogs disclosed possess unique and superior properties over other analogs, such as chemical and metabolic stability, selectivity, increased bioavailability and improved pharmacokinetics. Furthermore, the unique patterns of receptor subtype selectivity provide compounds having improved diagnostic and therapeutic utilities. Pharmaceutical compositions comprising the photo-active backbone cyclized somatostatin analogs, reagents for synthesizing same, and methods of using such compositions for diagnostic and therapeutic purposes including optical imaging and photodynamic therapy are also disclosed.

    摘要翻译： 公开了具有改善的生长抑素受体亚型亲和性和选择性的新型光活性标记的诊断和治疗肽，其是构象约束的骨架环化生长抑素类似物。 所公开的骨架环化肽类似物具有优于其它类似物的独特且优异的性质，例如化学和代谢稳定性，选择性，增加的生物利用度和改善的药代动力学。 此外，受体亚型选择性的独特模式提供具有改进的诊断和治疗效用的化合物。 还公开了包含光活性骨架环化的生长抑素类似物的药物组合物，用于合成它们的试剂，以及使用这些组合物用于包括光学成像和光动力疗法在内的诊断和治疗目的的方法。

    Protein kinase inhibitors
    7.
    发明授权
    Protein kinase inhibitors 失效
    蛋白激酶抑制剂

    公开(公告)号：US06949565B2

    公开(公告)日：2005-09-27

    申请号：US10296624

    申请日：2001-05-30

    申请人： Nurit Livnah ,  Alexander Levitzki ,  Hadas Reuveni

    发明人： Nurit Livnah ,  Alexander Levitzki ,  Hadas Reuveni

    IPC分类号： C07D217/22 ,  A61K31/472 ,  A61P3/04 ,  A61P3/10 ,  A61P7/04 ,  A61P9/00 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D217/02 ,  C07D217/24 ,  C07D401/12 ,  C07D405/12

    CPC分类号： C07D401/12 ,  C07D217/02 ,  C07D405/12

    摘要： Novel isoquinoline derivatives which are useful as inhibitors of protein kinases for experimental, medical, and drug design purposes are disclosed. Preferred compounds which are specific inhibitors of protein kinase B are also disclosed. Furthermore, pharmaceutical compositions comprising these protein kinase inhibitors, and methods of using such compositions for treatment and diagnosis of cancers, diabetes, cardiovascular pathologies, hemorrhagic shock, obesity, inflammatory diseases, diseases of the central nervous system, and autoimmune diseases, are also disclosed.

    摘要翻译： 公开了可用作实验，医学和药物设计目的的蛋白激酶抑制剂的新型异喹啉衍生物。 还公开了作为蛋白激酶B的特异性抑制剂的优选化合物。 此外，还公开了包含这些蛋白激酶抑制剂的药物组合物，以及使用这些组合物治疗和诊断癌症，糖尿病，心血管病变，出血性休克，肥胖症，炎性疾病，中枢神经系统疾病和自身免疫性疾病的方法 。