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公开(公告)号：EP2343367A1
公开(公告)日：2011-07-13
申请号：EP10186259.7
申请日：2002-10-04
申请人： Novartis AG , Université Victor Segalen Bordeaux 2 , Oregon Health and Science University , Technische Universität München , University of Heidelberg , Centre Hospitalier Regional Universitaire de Lille , MEDVET SCIENCE PTY. LTD.
发明人： Barthe, Christophe , Branford, Susan , Corbin, Amie , Druker, Brian Jay , Duyster, Justus , Hochhaus, Andreas , Hughes, Timothy , Kreil, Sebastian , Leguay, Thibaut , Mahon, Francois-Xavier , Marit, Gerald , Mueller, Martin , Peschel, Christian , Preudhomme, Claude , Roche Lestienne, Catherine , Rudzki, Zbigniew
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，其包含天然人类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来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，重组载体和包含这种核酸分子的宿主细胞，以及使用这种 核酸分子 这些多肽的制备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：EP2017335A1
公开(公告)日：2009-01-21
申请号：EP08166771.9
申请日：2002-10-04
申请人： NOVARTIS AG , Université Victor Segalen Bordeaux 2 , Oregon Health and Science University , Technische Universität München , University of Heidelberg , Centre Hospitalier Regional Universitaire de Lille , MEDVET SCIENCE PTY. LTD.
发明人： Barthe, Christophe , Branford, Susan , Corbin, Amie , Druker, Brian Jay , Duyster, Justus , Hochhaus, Andreas , Hughes, Timothy , Kreil, Sebastian , Leguay, Thibaut , Mahon, Francois-Xavier , Marit, Gerald , Mueller, Martin , Peschel, Christian , Preudhomme, Claude , Roche Lestienne, Catherine , Rudzki, Zbigniew
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-yl m ethyl)-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，其包含天然人类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m乙基）对其酪氨酸激酶活性的抑制， 苯甲酰胺或其盐，使用这种多肽来筛选抑制这些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，重组载体和包含该核酸分子的宿主细胞，以及使用 的这种核酸痣 制备此类多肽的细胞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：EP2341133A1
公开(公告)日：2011-07-06
申请号：EP10186089.8
申请日：2002-10-04
申请人： Novartis AG , Université Victor Segalen Bordeaux 2 , Oregon Health and Science University , Technische Universität München , University of Heidelberg , Centre Hospitalier Regional Universitaire de Lille , MEDVET SCIENCE PTY. LTD.
发明人： Barthe, Christophe , Branford, Susan , Corbin, Amie , Druker, Brian Jay , Duyster, Justus , Hochhaus, Andreas , Hughes, Timothy , Kreil, Sebastian , Leguay, Thibaut , Mahon, Francois-Xavier , Marit, Gerald , Mueller, Martin , Peschel, Christian , Preudhomme, Claude , Roche Lestienne, Catherine , Rudzki, Zbigniew
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, IIe313, Phe317, Met318, Met351, Glu355, Glu359, IIe360, 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，其包含功能激酶结构域，所述功能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上相似的序列，其中至少一个选自Met244，Leu248，Gly250，Glu252，Tyr253， Val256，Glu258，Phe311，IIe313，Phe317，Met318，Met351，Glu355，Glu359，IIe360，His361，Leu370，Asp381，Phe382，His396，Ser417，Glu459和Phe486被另一氨基酸取代，所述突变的功能性激酶结构域是抗性 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 涉及使用这样的多肽筛选抑制这些多肽的酪氨酸激酶活性的化合物，编码这些多肽的核酸分子，包含这些核酸分子的重组载体和宿主细胞，以及涉及这样的多肽 核酸分子 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：EP2246416A1
公开(公告)日：2010-11-03
申请号：EP10155600.9
申请日：2002-10-04
申请人： Novartis AG , Université Victor Segalen Bordeaux 2 , Oregon Health and Science University , Technische Universität München , University of Heidelberg , Centre Hospitalier Regional Universitaire de Lille , MEDVET SCIENCE PTY. LTD.
发明人： Barthe, Christophe , Branford, Susan , Corbin, Amie , Druker, Brian Jay , Duyster, Justus , Hochhaus, Andreas , Hughes, Timothy , Kreil, Sebastain , Leguay, Thibaut , Mahon, Francois-Xavier , Marit, Gerald , Mueller, Martin , Peschel, Christian , Preudhomme, Claude , Roche Lestienne, Christine , Rudzki, Zbigniew
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-yl m ethyl)-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，其包含天然人类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m乙基）对其酪氨酸激酶活性的抑制， 苯甲酰胺或其盐，使用这种多肽来筛选抑制这些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，重组载体和包含该核酸分子的宿主细胞，以及使用 的这种核酸痣 制备此类多肽的细胞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：EP2343366A1
公开(公告)日：2011-07-13
申请号：EP10186180.5
申请日：2002-10-04
申请人： Novartis AG , Université Victor Segalen Bordeaux 2 , Oregon Health and Science University , Technische Universität München , University of Heidelberg , Centre Hospitalier Regional Universitaire de Lille , MEDVET SCIENCE PTY. LTD.
发明人： Barthe, Christophe , Branford, Susan , Corbin, Amie , Druker, Brian Jay , Duyster, Justus , Hochhaus, Andreas , Hughes, Timothy , Kreil, Sebastian , Leguay, Thibaut , Mahon, Francois-Xavier , Marit, Gerald , Mueller, Martin , Peschel, Christian , Preudhomme, Claude , Roche Lestienne, Catherine , Rudzki, Zbigniew
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, lle333, Phe317, Met318, Met351, Glu355, Glu359, lle360, 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，其包含功能激酶结构域，所述功能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上相似的序列，其中至少一个选自Met244，Leu248，Gly250，Glu252，Tyr253， Val256，Glu258，Phe311，Ile333，Phe317，Met318，Met351，Glu355，Glu359，Ile360，His361，Leu370，Asp381，Phe382，His396，Ser417，Glu459和Phe486被另一个氨基酸置换，所述突变的功能激酶结构域对 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 涉及使用这样的多肽筛选抑制这些多肽的酪氨酸激酶活性的化合物，编码这些多肽的核酸分子，包含这些核酸分子的重组载体和宿主细胞，以及涉及这样的多肽 核酸分子 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：EP2343365A1
公开(公告)日：2011-07-13
申请号：EP10186114.4
申请日：2002-10-04
申请人： Novartis AG , Université Victor Segalen Bordeaux 2 , Oregon Health and Science University , Technische Universität München , University of Heidelberg , Centre Hospitalier Regional Universitaire de Lille , MEDVET SCIENCE PTY. LTD.
发明人： Barthe, Christophe , Branford, Susan , Corbin, Amie , Druker, Brian Jay , Duyster, Justus , Hochhaus, Andreas , Hughes, Timothy , Kreil, Sebastian , Leguay, Thibaut , Mahon, Francois-Xavier , Marit, Gerald , Mueller, Martin , Peschel, Christian , Preudhomme, Claude , Roche Lestienne, Catherine , Rudzki, Zbigniew
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-y(methyl)-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，其包含功能激酶结构域，所述功能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上相似的序列，其中至少一个选自Met244，Leu248，Gly250，Glu252，Tyr253， Val256，Glu258，Phe311，Ile313，Phe317，Met318，Met351，Glu355，Glu359，Ile360，His361，Leu370，Asp381，Phe382，His396，Ser417，Glu459和Phe486被另一个氨基酸置换，所述突变的功能激酶结构域对 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） - 苯甲酰胺或其盐的用途，涉及这些多肽用于筛选抑制这些多肽的酪氨酸激酶活性的化合物，编码这些多肽的核酸分子，包含此类核酸分子的重组载体和宿主细胞以及用途 的这种核酸分子 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：EP2017335B1
公开(公告)日：2010-12-01
申请号：EP08166771.9
申请日：2002-10-04
申请人： Novartis AG , Université Victor Segalen Bordeaux 2 , Oregon Health and Science University , Technische Universität München , University of Heidelberg , Centre Hospitalier Regional Universitaire de Lille , MEDVET SCIENCE PTY. LTD.
发明人： Barthe, Christophe , Branford, Susan , Corbin, Amie , Druker, Brian Jay , Duyster, Justus , Hochhaus, Andreas , Hughes, Timothy , Kreil, Sebastian , Leguay, Thibaut , Mahon, Francois-Xavier , Marit, Gerald , Mueller, Martin , Peschel, Christian , Preudhomme, Claude , Roche Lestienne, Catherine , Rudzki, Zbigniew
CPC分类号： C12N9/1205
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公开(公告)号：EP2290056A3
公开(公告)日：2011-06-01
申请号：EP10174534.7
申请日：2002-10-04
申请人： Novartis AG , Centre Hospitalier Regional Universitaire de Lille , MEDVET SCIENCE PTY. LTD. , Oregon Health & Science University , Technische Universität München , University of Heidelberg , Université Victor Segalen Bordeaux 2
发明人： Barthe, Christophe , Branford, Susan , Corbin, Amie , Druker, Brian Jay , Duyster, Justus , Hochhaus, Andreas , Hughes, Timothy , Kreil, Sebastian , Leguay, Thibaut , Mahon, François-Xavier , Marit, Gérald , Müller, Martin , Peschel, Christian , Preudhomme, Claude , Roche Lestienne, Catherine , Rudzki, Zbigniew
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：EP2290056A2
公开(公告)日：2011-03-02
申请号：EP10174534.7
申请日：2002-10-04
申请人： Novartis AG , Centre Hospitalier Regional Universitaire de Lille , MEDVET SCIENCE PTY. LTD. , Oregon Health & Science University , Technische Universität München , University of Heidelberg , Université Victor Segalen Bordeaux 2
发明人： Barthe, Christophe , Branford, Susan , Corbin, Amie , Druker, Brian Jay , Duyster, Justus , Hochhaus, Andreas , Hughes, Timothy , Kreil, Sebastian , Leguay, Thibaut , Mahon, François-Xavier , Marit, Gérald , Müller, Martin , Peschel, Christian , Preudhomme, Claude , Roche Lestienne, Catherine , Rudzki, Zbigniew
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，其包含天然人类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来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，重组载体和包含这种核酸分子的宿主细胞，以及使用这种 核酸分子 这些多肽的制备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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