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公开(公告)号：US20140243332A1
公开(公告)日：2014-08-28
申请号：US14190246
申请日：2014-02-26
申请人： Monika A. Davare , Brian J. Druker
发明人： Monika A. Davare , Brian J. Druker
IPC分类号： C12Q1/68 , A61K31/5377
CPC分类号： C12Q1/6886 , A61K31/47 , C12Q2600/106
摘要： Disclosed herein are methods of treating cancers characterized by aberrant ROS1 activity by administering an effective amount of foretinib (N1′-[3-fluoro-4-[[6-methoxy-7-(3-morpholinopropoxy)-4-quinolyl]oxy]phenyl]-N1-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide), including methods of identifying mutations in the kinase domain of ROS1 that indicate resistance to crizotinib, but sensitivity to foretinib.
摘要翻译： 本文公开了通过施用有效量的前列肽（N1' - [3-氟-4 - [[6-甲氧基-7-（3-吗啉代丙氧基）-4-喹啉基]氧基]苯甲酰胺处理以异常ROS1活性为特征的癌症的方法， 苯基] -N1-（4-氟苯基）环丙烷-1,1-二羧酰胺），包括识别ROS1的激酶结构域突变的方法，该突变表明对crizotinib的抗性，但对前列腺素的敏感性。
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公开(公告)号：US07592142B2
公开(公告)日：2009-09-22
申请号：US12178926
申请日：2008-07-24
申请人： Brian J. Druker , Amie Corbin
发明人： Brian J. Druker , Amie Corbin
IPC分类号： C12Q1/68
CPC分类号： C12Q1/6886 , C07K14/82 , C12N9/12 , C12Q1/485 , C12Q2600/106 , G01N33/57426 , G01N2333/82
摘要： The present invention relates to isolated polypeptides which comprise an amino acid sequence consisting of a mutated functional Abl kinase domain, said mutated functional kinase domain being resistant to inhibition of its tyrosine kinase activity by N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-4-(4-methyl-piperazin-1-ylmethyl)-benzamide or a salt thereof, to the use of such polypeptides to screen for compounds which inhibit the tyrosine kinase activity of such polypeptides, to nucleic acid molecules encoding such polypeptides, to recombinant vectors and host cells comprising such nucleic acid molecules and to the use of such nucleic acid molecules in the production of such polypeptides for use in screening for compounds which inhibit the tyrosine kinase activity of such polypeptides.
摘要翻译： 本发明涉及分离的多肽，其包含由突变的功能性Ab1激酶结构域组成的氨基酸序列，所述突变的功能性激酶结构域对N- [4-甲基-3-（4-吡啶基） 吡啶-3-基 - 嘧啶-2-基氨基） - 苯基] -4-（4-甲基 - 哌嗪-1-基甲基） - 苯甲酰胺或其盐，用于筛选抑制酪氨酸激酶的化合物 这种多肽的活性，编码这种多肽的核酸分子，重组载体和包含此类核酸分子的宿主细胞，以及这种核酸分子在制备这些多肽中的用途，用于筛选抑制酪氨酸激酶的化合物 这些多肽的活性。
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公开(公告)号：US07326534B2
公开(公告)日：2008-02-05
申请号：US11524626
申请日：2006-09-20
申请人： Brian J. Druker , Amie Corbin
发明人： Brian J. Druker , Amie Corbin
CPC分类号： C12Q1/6886 , C07K14/82 , C12N9/12 , C12Q1/485 , C12Q2600/106 , G01N33/57426 , G01N2333/82
摘要： The present invention relates to isolated polypeptides which comprise an amino acid sequence consisting of a mutated functional Abl kinase domain, said mutated functional kinase domain being resistant to inhibition of its tyrosine kinase activity by N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-4-(4-methyl-piperazin-1-ylmethyl)-benzamide or a salt thereof, to the use of such polypeptides to screen for compounds which inhibit the tyrosine kinase activity of such polypeptides, to nucleic acid molecules encoding such polypeptides, to recombinant vectors and host cells comprising such nucleic acid molecules and to the use of such nucleic acid molecules in the production of such polypeptides for use in screening for compounds which inhibit the tyrosine kinase activity of such polypeptides.
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公开(公告)号：US07416873B2
公开(公告)日：2008-08-26
申请号：US11873985
申请日：2007-10-17
申请人： Brian J. Druker , Amie Corbin
发明人： Brian J. Druker , Amie Corbin
CPC分类号： C12Q1/6886 , C07K14/82 , C12N9/12 , C12Q1/485 , C12Q2600/106 , G01N33/57426 , G01N2333/82
摘要： The present invention relates to isolated polypeptides which comprise an amino acid sequence consisting of a mutated functional Abl kinase domain, said mutated functional kinase domain being resistant to inhibition of its tyrosine kinase activity by N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-4-(4-methyl-piperazin-1-ylmethyl)-benzamide or a salt thereof, to the use of such polypeptides to screen for compounds which inhibit the tyrosine kinase activity of such polypeptides, to nucleic acid molecules encoding such polypeptides, to recombinant vectors and host cells comprising such nucleic acid molecules and to the use of such nucleic acid molecules in the production of such polypeptides for use in screening for compounds which inhibit the tyrosine kinase activity of such polypeptides.
摘要翻译： 本发明涉及分离的多肽，其包含由突变的功能性Ab1激酶结构域组成的氨基酸序列，所述突变的功能性激酶结构域对N- [4-甲基-3-（4-吡啶基） 吡啶-3-基 - 嘧啶-2-基氨基） - 苯基] -4-（4-甲基 - 哌嗪-1-基甲基） - 苯甲酰胺或其盐，用于筛选抑制酪氨酸激酶的化合物 这种多肽的活性，编码这种多肽的核酸分子，重组载体和包含此类核酸分子的宿主细胞，以及这种核酸分子在制备这些多肽中的用途，用于筛选抑制酪氨酸激酶的化合物 这些多肽的活性。
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公开(公告)号：US20110065107A1
公开(公告)日：2011-03-17
申请号：US12803962
申请日：2010-07-09
申请人： Brian J. Druker , Amie Corbin
发明人： Brian J. Druker , Amie Corbin
CPC分类号： C12Q1/6886 , C07K14/82 , C12N9/12 , C12Q1/485 , C12Q2600/106 , G01N33/57426 , G01N2333/82
摘要： The present invention relates to isolated polypeptides which comprise an amino acid sequence consisting of a mutated functional Abl kinase domain, said mutated functional kinase domain being resistant to inhibition of its tyrosine kinase activity by N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-4-(4-methyl-piperazin-1-ylmethyl)-benzamide or a salt thereof, to the use of such polypeptides to screen for compounds which inhibit the tyrosine kinase activity of such polypeptides, to nucleic acid molecules encoding such polypeptides, to recombinant vectors and host cells comprising such nucleic acid molecules and to the use of such nucleic acid molecules in the production of such polypeptides for use in screening for compounds which inhibit the tyrosine kinase activity of such polypeptides.
摘要翻译： 本发明涉及分离的多肽，其包含由突变的功能性Ab1激酶结构域组成的氨基酸序列，所述突变的功能性激酶结构域对N- [4-甲基-3-（4-吡啶基） 吡啶-3-基 - 嘧啶-2-基氨基） - 苯基] -4-（4-甲基 - 哌嗪-1-基甲基） - 苯甲酰胺或其盐，用于筛选抑制酪氨酸激酶的化合物 这种多肽的活性，编码这种多肽的核酸分子，重组载体和包含此类核酸分子的宿主细胞，以及这种核酸分子在制备这些多肽中的用途，用于筛选抑制酪氨酸激酶的化合物 这些多肽的活性。
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公开(公告)号：US20130273542A1
公开(公告)日：2013-10-17
申请号：US13924369
申请日：2013-06-21
申请人： Brian J. Druker , Amie Corbin
发明人： Brian J. Druker , Amie Corbin
IPC分类号： C12Q1/68
CPC分类号： C12Q1/6886 , C07K14/82 , C12N9/12 , C12Q1/485 , C12Q2600/106 , G01N33/57426 , G01N2333/82
摘要： The present invention relates to isolated polypeptides which comprise an amino acid sequence consisting of a mutated functional Abl kinase domain, said mutated functional kinase domain being resistant to inhibition of its tyrosine kinase activity by N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-4-(4-methyl-piperazin-1-ylmethyl)-benzamide or a salt thereof, to the use of such polypeptides to screen for compounds which inhibit the tyrosine kinase activity of such polypeptides, to nucleic acid molecules encoding such polypeptides, to recombinant vectors and host cells comprising such nucleic acid molecules and to the use of such nucleic acid molecules in the production of such polypeptides for use in screening for compounds which inhibit the tyrosine kinase activity of such polypeptides.
摘要翻译： 本发明涉及分离的多肽，其包含由突变的功能性Ab1激酶结构域组成的氨基酸序列，所述突变的功能性激酶结构域对N- [4-甲基-3-（4-吡啶基） 吡啶-3-基 - 嘧啶-2-基氨基） - 苯基] -4-（4-甲基 - 哌嗪-1-基甲基） - 苯甲酰胺或其盐，用于筛选抑制酪氨酸激酶的化合物 这种多肽的活性，编码这种多肽的核酸分子，重组载体和包含此类核酸分子的宿主细胞，以及这种核酸分子在制备这些多肽中的用途，用于筛选抑制酪氨酸激酶的化合物 这些多肽的活性。
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公开(公告)号：US20130131139A1
公开(公告)日：2013-05-23
申请号：US13299245
申请日：2011-11-17
IPC分类号： A61K31/713 , A61K31/7105 , C40B30/04 , G01N33/573 , C12Q1/48 , C12Q1/68 , A61K31/506 , A61P35/02
CPC分类号： A61K31/506 , A61K31/7105 , A61K31/713 , C12Q1/6886 , C12Q2600/106 , C12Q2600/158 , G01N33/57426
摘要： Disclosed are methods of selecting a subject suspected of having or having leukemia, such as lymphoblast leukemia (B-ALL), for treatment with an agent that inhibits ROR1-regulated signaling activity. In some examples, cells obtained from the subject are screened for over expression of ROR1. In other examples, the cells are contacted with an agent that inhibits ROR1 signaling activity and a ROR1-regulated signaling activity is detected. An alteration in the ROR1-regulated signaling activity as compared to a control identifies the subject as one that would benefit from treatment with an agent that inhibits ROR1 signaling activity. Also disclosed are methods for identifying an agent for treating a subject with a ROR1-dependent leukemia or with a predisposition for developing a ROR1-dependent leukemia, and methods for treating or inhibiting a ROR1-dependent leukemia, such as B-ALL in a subject.
摘要翻译： 公开了选择疑似患有白血病或具有白血病的受试者（例如淋巴细胞白血病（B-ALL））用于用抑制ROR1调节的信号传导活性的药物治疗的方法。 在一些实施例中，筛选从受试者获得的细胞过度表达ROR1。 在其他实施例中，细胞与抑制ROR1信号传导活性的试剂接触并检测到ROR1调节的信号活性。 与对照相比，ROR1调节的信号传导活性的改变将该受试者识别为将受益于用抑制ROR1信号传导活性的药物治疗的受试者。 还公开了用于鉴定用于治疗患有ROR1依赖性白血病或具有发展ROR1依赖性白血病的倾向的受试者的方法，以及用于治疗或抑制ROR1依赖性白血病（例如受试者中的B-ALL）的方法 。
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公开(公告)号：US20080305492A1
公开(公告)日：2008-12-11
申请号：US12178926
申请日：2008-07-24
申请人： Brian J. Druker , Amie Corbin
发明人： Brian J. Druker , Amie Corbin
CPC分类号： C12Q1/6886 , C07K14/82 , C12N9/12 , C12Q1/485 , C12Q2600/106 , G01N33/57426 , G01N2333/82
摘要： The present invention relates to isolated polypeptides which comprise an amino acid sequence consisting of a mutated functional Abl kinase domain, said mutated functional kinase domain being resistant to inhibition of its tyrosine kinase activity by N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-4-(4-methyl-piperazin-1-ylmethyl)-benzamide or a salt thereof, to the use of such polypeptides to screen for compounds which inhibit the tyrosine kinase activity of such polypeptides, to nucleic acid molecules encoding such polypeptides, to recombinant vectors and host cells comprising such nucleic acid molecules and to the use of such nucleic acid molecules in the production of such polypeptides for use in screening for compounds which inhibit the tyrosine kinase activity of such polypeptides.
摘要翻译： 本发明涉及分离的多肽，其包含由突变的功能性Ab1激酶结构域组成的氨基酸序列，所述突变的功能性激酶结构域对N- [4-甲基-3-（4-吡啶基） 吡啶-3-基 - 嘧啶-2-基氨基） - 苯基] -4-（4-甲基 - 哌嗪-1-基甲基） - 苯甲酰胺或其盐，用于筛选抑制酪氨酸激酶的化合物 这种多肽的活性，编码这种多肽的核酸分子，重组载体和包含此类核酸分子的宿主细胞，以及这种核酸分子在制备这些多肽中的用途，用于筛选抑制酪氨酸激酶的化合物 这些多肽的活性。
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