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公开(公告)号：US20100021920A1
公开(公告)日：2010-01-28
申请号：US12545113
申请日：2009-08-21
申请人： Christophe Barthe , Susan Branford , Amie Corbin , Brian Jay Druker , Justus Duyster , Andreas Hochhaus , Timothy Hughes , Sebastian Kreil , Thlbaut Leguay , Francois-Xavier Mahon , Gèrald Marit , Martin Müller , Christian Peschel , Claude Preudhomme , Catherine Roche Lestienne , Zbigniew Rudzki
发明人： Christophe Barthe , Susan Branford , Amie Corbin , Brian Jay Druker , Justus Duyster , Andreas Hochhaus , Timothy Hughes , Sebastian Kreil , Thlbaut Leguay , Francois-Xavier Mahon , Gèrald Marit , Martin Müller , Christian Peschel , Claude Preudhomme , Catherine Roche Lestienne , Zbigniew Rudzki
CPC分类号： C12N9/1205
摘要： The present invention relates to isolated polypeptides which comprise a functional kinase domain comprising the amino acid sequence of the native human Abl kinase domain or an essentially similar sequence thereof in which at least one amino acid selected from Met244, Leu248, Gly250, Glu252, Tyr253, Val256, Glu258, Phe311, Ile313, Phe317, Met318, Met351, Glu355, Glu359, Ile360, His361, Leu370, Asp381, Phe382, His396, Ser417, Glu459 and Phe486 is replaced by another amino acid, 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：US20100021921A1
公开(公告)日：2010-01-28
申请号：US12545133
申请日：2009-08-21
申请人： Christophe Barthe , Susan Branford , Amie Corbin , Brian Jay Druker , Justus Duyster , Andreas Hochhaus , Timothy Hughes , Sebastian Kreil , Thibaut Leguay , Francois-Xavier Mahon , Gerald Marit , Martin Muller , Christian Peschel , Claude Preudhomme , Catherine Roche Lestienne , Zbigniew Rudzki
发明人： Christophe Barthe , Susan Branford , Amie Corbin , Brian Jay Druker , Justus Duyster , Andreas Hochhaus , Timothy Hughes , Sebastian Kreil , Thibaut Leguay , Francois-Xavier Mahon , Gerald Marit , Martin Muller , Christian Peschel , Claude Preudhomme , Catherine Roche Lestienne , Zbigniew Rudzki
CPC分类号： C12N9/1205
摘要： The present invention relates to isolated polypeptides which comprise a functional kinase domain comprising the amino acid sequence of the native human Abl kinase domain or an essentially similar sequence thereof in which at least one amino acid selected from Met244, Leu248, Gly250, Glu252, Tyr253, Val256, Glu258, Phe311, Ile313, Phe317, Met318, Met351, Glu355, Glu359, Ile360, His361, Leu370, Asp381, Phe382, His396, Ser417, Glu459 and Phe486 is replaced by another amino acid, 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，其包含功能性激酶结构域，所述功能性激酶结构域包含天然人Abl激酶结构域的氨基酸序列或其基本相似的序列，其中至少一种选自Met244，Leu248，Gly250，Glu252，Tyr253， Val256，Glu258，Phe311，Ile313，Phe317，Met318，Met351，Glu355，Glu359，Ile360，His361，Leu370，Asp381，Phe382，His396，Ser417，Glu459和Phe486被另一个氨基酸取代，所述突变的功能性激酶结构域对 通过N- [4-甲基-3-（4-吡啶-3-基 - 嘧啶-2-基氨基） - 苯基] -4-（4-甲基 - 哌嗪-1-基甲基） - 苯甲酰胺抑制其酪氨酸激酶活性 或其盐使用这样的多肽筛选抑制这种多肽的酪氨酸激酶活性的化合物，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，以及使用其 核酸分子 生产这样的多肽用于筛选抑制这些多肽的酪氨酸激酶活性的化合物。
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公开(公告)号：US20090117641A1
公开(公告)日：2009-05-07
申请号：US12165217
申请日：2008-06-30
申请人： Christophe Barthe , Susan Bradford , Amie Corbin , Brian Jay Druker , Justus Duyster , Andreas Hochhaus , Timothy Hughes , Sebastian Kreil , Thibaut Leguay , Francios-Xavier Mahon , Gerald Marit , Martin Muller , Christian Peschel , Claude Preudhomme , Catherine Roche Lestienne , Zbigniew Rudzki
发明人： Christophe Barthe , Susan Bradford , Amie Corbin , Brian Jay Druker , Justus Duyster , Andreas Hochhaus , Timothy Hughes , Sebastian Kreil , Thibaut Leguay , Francios-Xavier Mahon , Gerald Marit , Martin Muller , Christian Peschel , Claude Preudhomme , Catherine Roche Lestienne , Zbigniew Rudzki
IPC分类号： C12N9/12
CPC分类号： C12N9/1205
摘要： The present invention relates to isolated polypeptides which comprise a functional kinase domain comprising the amino acid sequence of the native human Abl kinase domain or an essentially similar sequence thereof in which at least one amino acid selected from Met244, Leu248, Gly250, Glu252, Tyr253, Val256, Glu258, Phe311, Ile313, Phe317, Met318, Met351, Glu355, Glu359, Ile360, His361, Leu370, Asp381, Phe382, His396, Ser417, Glu459 and Phe486 is replaced by another amino acid, 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，其包含功能性激酶结构域，所述功能性激酶结构域包含天然人Abl激酶结构域的氨基酸序列或其基本相似的序列，其中至少一种选自Met244，Leu248，Gly250，Glu252，Tyr253， Val256，Glu258，Phe311，Ile313，Phe317，Met318，Met351，Glu355，Glu359，Ile360，His361，Leu370，Asp381，Phe382，His396，Ser417，Glu459和Phe486被另一个氨基酸取代，所述突变的功能性激酶结构域对 通过N- [4-甲基-3-（4-吡啶-3-基 - 嘧啶-2-基氨基） - 苯基] -4-（4-甲基 - 哌嗪-1-基甲基） - 苯甲酰胺抑制其酪氨酸激酶活性 或其盐使用这样的多肽筛选抑制这种多肽的酪氨酸激酶活性的化合物，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，以及使用其 核酸分子 生产这样的多肽用于筛选抑制这些多肽的酪氨酸激酶活性的化合物。
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公开(公告)号：US20110129852A1
公开(公告)日：2011-06-02
申请号：US12834628
申请日：2010-07-12
申请人： Christophe Barthe , Pascale Cony-Makhoul , Amie Corbin , Sven De Vos , Brian Jay Druker , Harald Gschaidmeier , Michael Hallek , Andreas Hochhaus , Dieter Hoelzer , Wolf-Karsten Hofmann , Phillip Koeffler , Sebastian Kreil , Francois-Xavier Mahon , Martin Müller , Oliver Gerhard Ottmann , Markus Warmuth
发明人： Christophe Barthe , Pascale Cony-Makhoul , Amie Corbin , Sven De Vos , Brian Jay Druker , Harald Gschaidmeier , Michael Hallek , Andreas Hochhaus , Dieter Hoelzer , Wolf-Karsten Hofmann , Phillip Koeffler , Sebastian Kreil , Francois-Xavier Mahon , Martin Müller , Oliver Gerhard Ottmann , Markus Warmuth
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：US20090191606A1
公开(公告)日：2009-07-30
申请号：US12337322
申请日：2008-12-17
申请人： Christophe Barthe , Pascale Cony-Makhoul , Amie Corbin , Sven De Vos , Brian Jay Druker , Harald Gschaidmeier , Michael Hallek , Andreas Hochhaus , Dieter Hoelzer , Wolf-Karsten Hofmann , Phillip Koeffler , Sebastian Kreil , Francois-Xavier Mahon , Martin Muller , Oliver Gerhard Ottmann , Markus Warmuth
发明人： Christophe Barthe , Pascale Cony-Makhoul , Amie Corbin , Sven De Vos , Brian Jay Druker , Harald Gschaidmeier , Michael Hallek , Andreas Hochhaus , Dieter Hoelzer , Wolf-Karsten Hofmann , Phillip Koeffler , Sebastian Kreil , Francois-Xavier Mahon , Martin Muller , Oliver Gerhard Ottmann , Markus Warmuth
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：US06958335B2
公开(公告)日：2005-10-25
申请号：US10415015
申请日：2001-10-26
申请人： Elisabeth Buchdunger , Renaud Capdeville , George Daniel Demetri , Sasa Dimitrijevic , Brian Jay Druker , Jonathan A. Fletcher , Michael C. Heinrich , Heikki Joensuu , Sandra Leta Silberman , David Tuveson
发明人： Elisabeth Buchdunger , Renaud Capdeville , George Daniel Demetri , Sasa Dimitrijevic , Brian Jay Druker , Jonathan A. Fletcher , Michael C. Heinrich , Heikki Joensuu , Sandra Leta Silberman , David Tuveson
IPC分类号： A61K31/506 , A61P35/00 , C07D401/04 , A61K31/497
CPC分类号： C07D401/04 , A61K31/506
摘要： 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide of the formula I or a pharmaceutically acceptable salt thereof can be used in the treatment of gastrointestinal stromal tumours.
摘要翻译： 4-（4-甲基哌嗪-1-基甲基）-N- [4-甲基-3-（4-吡啶-3-基）嘧啶-2-基氨基）苯基] - 苯甲酰胺或其药学上可接受的盐 可用于治疗胃肠道间质瘤。
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