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11. 发明申请

US20120165355A1 METHODS AND COMPOSITIONS FOR TREATING CANCERS 审中-公开
标题翻译：治疗癌症的方法和组合物
公开(公告)号：US20120165355A1
公开(公告)日：2012-06-28
申请号：US13411963
申请日：2012-03-05
申请人： Markus Warmuth , Christine Dierks
发明人： Markus Warmuth , Christine Dierks
IPC分类号： A61K31/506 , A61P35/02 , A61P35/00
CPC分类号： A61K31/675 , A61K31/352 , A61K31/4355 , A61K31/438 , A61K31/496 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/66 , A61K45/06 , A61K2300/00
摘要： This invention provides a combination of antagonists of the hedgehog signaling pathway with a BCR-ABL inhibitor. The combination of the present invention may be used for treating cancers known to be associated with protein tyrosine kinases such as, for example, Src, BCR-ABL and c-kit.
摘要翻译：本发明提供了刺猬蛋白信号传导途径的拮抗剂与BCR-ABL抑制剂的组合。本发明的组合可用于治疗已知与蛋白酪氨酸激酶（例如Src，BCR-ABL和c-kit）相关的癌症。

12. 发明申请

US20100197659A1 BIPHENYLCARBOXAMIDE DERIVATIVES AS HEDGEHOD PATHWAY MODULATORS 有权
标题翻译：苯二甲酰胺衍生物作为HEDGEHOD路径调节剂
公开(公告)号：US20100197659A1
公开(公告)日：2010-08-05
申请号：US12663490
申请日：2008-06-04
申请人： Christine Dierks , Markus Warmuth , Xu Wu
发明人： Christine Dierks , Markus Warmuth , Xu Wu
IPC分类号： A61K31/553 , C12N5/02 , A61K31/497 , A61K31/5377 , A61K31/4545 , A61K31/505 , A61K31/541 , A61K31/5513 , A61K31/55
CPC分类号： A61K31/165 , A61K31/18 , A61K31/277 , A61K31/40 , A61K31/44 , A61K31/4433 , A61K31/4453 , A61K31/4545 , A61K31/496 , A61K31/505 , A61K31/5375 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/551 , A61K31/553
摘要： The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I.
摘要翻译：本发明提供了一种调节刺猬蛋白信号通路活性的方法。特别地，本发明提供了一种抑制由诸如Ptc功能丧失，hedgehog功能增益，平滑增益功能或Gli功能增益等表现形成的异常生长状态的方法，包括使细胞接触与足量的式I化合物反应。

13. 发明申请

US20090191606A1 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
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
IPC分类号： C12N9/12 , C07H21/00 , C12N15/63 , C12N5/10
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。

14. 发明申请

US20070149539A1 USE OF C-SRC INHIBITORS ALONE OR IN COMBINATION WITH STI571 FOR THE TREATMENT OF LEUKAEMIA 审中-公开
标题翻译：使用C-SRC抑制剂或与STI571组合用于治疗白血病
公开(公告)号：US20070149539A1
公开(公告)日：2007-06-28
申请号：US11679901
申请日：2007-02-28
申请人： Nicholas Donato , Doriano Fabbro , Paul Manley , Jurgen Mestan , Markus Warmuth , Michael Hallek , Moshe Talpaz , Ji Wu
发明人： Nicholas Donato , Doriano Fabbro , Paul Manley , Jurgen Mestan , Markus Warmuth , Michael Hallek , Moshe Talpaz , Ji Wu
IPC分类号： A61K31/506 , A61K31/497 , A61K31/519
CPC分类号： A61K35/02 , A61K31/506 , A61K31/519
摘要： The invention relates to a combination which comprises (a) at least one compound decreasing the c-Src activity and (b) N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamdio]-2-methylphenyl }-4-(3-pyridyl)-2-pyrimidine-amine or the monomethanesulfonate salt thereof; to pharmaceutical compositions comprising said combinations; and to a method of treating a warm-blooded animal having leukaemia, especially chronic myelogenous leukaemia, comprising administering to the animal at least one compound inhibiting the activity of a member of the Src kinase family, the Tec kinase family or a Raf kinase inhibitor, in particular inhibiting the c-Src protein tyrosine kinase activity or inhibiting simultaneously the c-Src protein tyrosine kinase activity and the Bcr-Abl tyrosine kinase activity, alone or in combination with a Bcr-Abl inhibitor, in particular N- {5- [4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl }-4-(3-pyridyl)-2-pyrimidine-amine.
摘要翻译：本发明涉及一种组合，其包含（a）至少一种降低c-Src活性的化合物和（b）N- {5- [4-（4-甲基 - 哌嗪基 - 甲基） - 苯甲酰氨基] -2-甲基苯基} -4-（3-吡啶基）-2-嘧啶胺或其单甲磺酸盐; 包含所述组合的药物组合物; 以及治疗具有白血病，特别是慢性骨髓性白血病的温血动物的方法，包括向动物施用至少一种抑制Src激酶家族成员，Tec激酶家族或Raf激酶抑制剂的活性的化合物，特别是抑制c-Src蛋白酪氨酸激酶活性或同时抑制c-Src蛋白酪氨酸激酶活性和Bcr-Abl酪氨酸激酶活性，单独或与Bcr-Abl抑制剂组合，特别是N- {5- [ 4-（4-甲基 - 哌嗪子基 - 甲基） - 苯甲酰氨基] -2-甲基苯基} -4-（3-吡啶基）-2-嘧啶胺。

15. 发明申请

US20110044991A1 METHODS AND COMPOSITIONS FOR TREATING LYMPHOMA AND MYELOMA 审中-公开
标题翻译：治疗LYMPHOMA和MYELOMA的方法和组合物
公开(公告)号：US20110044991A1
公开(公告)日：2011-02-24
申请号：US12439878
申请日：2006-09-27
申请人： Christine Dierks , Markus Warmuth
发明人： Christine Dierks , Markus Warmuth
IPC分类号： A61K39/395 , A61K31/438 , A61K31/352 , A61K31/713 , A61K31/711 , A61K31/7105 , C12N5/09 , A61P35/00
CPC分类号： A61K31/4355 , A61K31/35 , A61K31/7105 , A61K31/711 , C07K14/47 , C07K16/18
摘要： This invention relates to the use of antagonists of the hedgehog signaling pathway to induce apoptosis of lymphoma and myeloma cells and to treat subjects suffering from various forms of lymphoma or myeloma.
摘要翻译：本发明涉及刺猬蛋白信号传导途径的拮抗剂用于诱导淋巴瘤和骨髓瘤细胞凋亡以及治疗患有各种形式的淋巴瘤或骨髓瘤的受试者的用途。

16. 发明申请

US20100216828A1 METHODS AND COMPOSITIONS FOR TREATING CANCERS 审中-公开
标题翻译：治疗癌症的方法和组合物
公开(公告)号：US20100216828A1
公开(公告)日：2010-08-26
申请号：US12673178
申请日：2008-08-13
申请人： Christine Dierks , Markus Warmuth
发明人： Christine Dierks , Markus Warmuth
IPC分类号： A61K31/506 , A61P35/00
CPC分类号： A61K31/675 , A61K31/352 , A61K31/4355 , A61K31/438 , A61K31/496 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/66 , A61K45/06 , A61K2300/00
摘要： This invention provides a combination of antagonists of the hedgehog signaling pathway with a BCR-ABL inhibitor. The combination of the present invention may be used for treating cancers known to be associated with protein tyrosine kinases such as, for example, Src, BCR-ABL and c-kit.
摘要翻译：本发明提供了刺猬蛋白信号传导途径的拮抗剂与BCR-ABL抑制剂的组合。本发明的组合可用于治疗已知与蛋白酪氨酸激酶（例如Src，BCR-ABL和c-kit）相关的癌症。

17. 发明申请

US20060074094A1 Use of c-Src inhibitors alone or in combination with STI571 for the treatment of leukaemia 失效
标题翻译：单独或与STI571组合使用c-Src抑制剂治疗白血病
公开(公告)号：US20060074094A1
公开(公告)日：2006-04-06
申请号：US11285664
申请日：2005-11-22
申请人： Nicholas Donato , Doriano Fabbro , Paul Manley , Jurgen Mestan , Markus Warmuth , Michael Hallek , Moshe Talpaz , Ji Wu
发明人： Nicholas Donato , Doriano Fabbro , Paul Manley , Jurgen Mestan , Markus Warmuth , Michael Hallek , Moshe Talpaz , Ji Wu
IPC分类号： A61K31/519
CPC分类号： A61K35/02 , A61K31/506 , A61K31/519
摘要： The invention relates to a combination which comprises (a) at least one compound decreasing the c-Src activity and (b) N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine or the monomethanesulfonate salt thereof; to pharmaceutical compositions comprising said combinations; and to a method of treating a warm-blooded animal having leukaemia, especially chronic myelogenous leukaemia, comprising administering to the animal at least one compound inhibiting the activity of a member of the Src kinase family, the Btk kinase family, the Tec kinase family or a Raf kinase inhibitor, in particular inhibiting the c-Src protein tyrosine kinase activity or inhibiting simultaneously the c-Src protein tyrosine kinase activity and the Bcr-Abl tyrosine kinase activity, alone or in combination with a Bcr-Abl inhibitor, in particular N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine.
摘要翻译：本发明涉及一种组合，其包含（a）至少一种降低c-Src活性的化合物和（b）N- {5- [4-（4-甲基 - 哌嗪基 - 甲基） - 苯甲酰氨基] -2-甲基苯基} -4-（3-吡啶基）-2-嘧啶胺或其单甲磺酸盐; 包含所述组合的药物组合物; 以及治疗具有白血病，特别是慢性骨髓性白血病的温血动物的方法，包括向所述动物施用至少一种抑制Src激酶家族成员，Btk激酶家族，Tec激酶家族的活性的化合物或 Raf激酶抑制剂，特别是抑制c-Src蛋白酪氨酸激酶活性或同时抑制c-Src蛋白酪氨酸激酶活性和Bcr-Abl酪氨酸激酶活性，单独或与Bcr-Abl抑制剂组合，特别是N - {5- [4-（4-甲基 - 哌嗪子基 - 甲基） - 苯甲酰氨基] -2-甲基苯基} -4-（3-吡啶基）-2-嘧啶胺。

18. 发明授权

US08268837B2 Use of c-Src inhibitors alone or in combination with STI571 for the treatment of leukaemia 失效
标题翻译：单独或与STI571组合使用c-Src抑制剂治疗白血病
公开(公告)号：US08268837B2
公开(公告)日：2012-09-18
申请号：US11285664
申请日：2005-11-22
申请人： Nicholas J Donato , Doriano Fabbro , Paul W Manley , Jurgen Mestan , Markus Warmuth , Michael Hallek , Moshe Talpaz , Ji Wu
发明人： Nicholas J Donato , Doriano Fabbro , Paul W Manley , Jurgen Mestan , Markus Warmuth , Michael Hallek , Moshe Talpaz , Ji Wu
IPC分类号： A61K31/519
CPC分类号： A61K35/02 , A61K31/506 , A61K31/519
摘要： The invention relates to a combination which comprises (a) at least one compound decreasing the c-Src activity and (b) N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine or the monomethanesulfonate salt thereof; to pharmaceutical compositions comprising said combinations; and to a method of treating a warm-blooded animal having leukaemia, especially chronic myelogenous leukaemia, comprising administering to the animal at least one compound inhibiting the activity of a member of the Src kinase family, the Btk kinase family, the Tec kinase family or a Raf kinase inhibitor, in particular inhibiting the c-Src protein tyrosine kinase activity or inhibiting simultaneously the c-Src protein tyrosine kinase activity and the Bcr-Abl tyrosine kinase activity, alone or in combination with a Bcr-Abl inhibitor, in particular N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine.
摘要翻译：本发明涉及一种组合，其包含（a）至少一种降低c-Src活性的化合物和（b）N- {5- [4-（4-甲基 - 哌嗪基 - 甲基） - 苯甲酰氨基] -2-甲基苯基} -4-（3-吡啶基）-2-嘧啶胺或其单甲磺酸盐; 包含所述组合的药物组合物; 以及治疗具有白血病，特别是慢性骨髓性白血病的温血动物的方法，包括向所述动物施用至少一种抑制Src激酶家族成员，Btk激酶家族，Tec激酶家族的活性的化合物或 Raf激酶抑制剂，特别是抑制c-Src蛋白酪氨酸激酶活性或同时抑制c-Src蛋白酪氨酸激酶活性和Bcr-Abl酪氨酸激酶活性，单独或与Bcr-Abl抑制剂组合，特别是N - {5- [4-（4-甲基 - 哌嗪子基 - 甲基） - 苯甲酰氨基] -2-甲基苯基} -4-（3-吡啶基）-2-嘧啶胺。

19. 发明申请

US20110021524A1 COMPOSITIONS AND METHODS FOR TREATING CANCERS 审中-公开
标题翻译：用于治疗癌症的组合物和方法
公开(公告)号：US20110021524A1
公开(公告)日：2011-01-27
申请号：US12812740
申请日：2008-12-18
申请人： Francisco Adrian , Christine Dierks , Nathanael S. Gray , Markus Warmuth
发明人： Francisco Adrian , Christine Dierks , Nathanael S. Gray , Markus Warmuth
IPC分类号： A61K31/5377 , A61K31/506 , A61K31/505 , A61K31/52 , A61K31/497 , A61K31/5025 , A61P35/02 , A61P35/00
CPC分类号： A61K31/5377 , A61K31/506 , A61K2300/00
摘要： This invention provides a combination of ATP-competitive BCR-ABL inhibitor and a non-ATP competitive BCR-ABL inhibitor. The combination of the present invention may be used for treating cancers known to be associated with BCR-ABL.
摘要翻译：本发明提供ATP竞争性BCR-ABL抑制剂和非ATP竞争性BCR-ABL抑制剂的组合。本发明的组合可用于治疗已知与BCR-ABL相关的癌症。

20. 发明申请

US20060148058A1 Organic compounds 审中-公开
标题翻译：有机化合物
公开(公告)号：US20060148058A1
公开(公告)日：2006-07-06
申请号：US11343891
申请日：2006-01-31
申请人： Christophe Barthe , Pascale Cony-Makhoul , Amie Corbin , Sven De Vos , Brian Druker , Harald Gschaidmeier , Michael Hallek , Andreas Hochhaus , Dieter Hoelzer , Wolf-Karsten Hofmann , Phillip Koeffler , Sebastian Kreil , Francois-Xavier Mahon , Martin Muller , Oliver Ottmann , Markus Warmuth
发明人： Christophe Barthe , Pascale Cony-Makhoul , Amie Corbin , Sven De Vos , Brian Druker , Harald Gschaidmeier , Michael Hallek , Andreas Hochhaus , Dieter Hoelzer , Wolf-Karsten Hofmann , Phillip Koeffler , Sebastian Kreil , Francois-Xavier Mahon , Martin Muller , Oliver Ottmann , Markus Warmuth
IPC分类号： C12N9/12
CPC分类号： C12Q1/6886 , C07K14/82 , C12N9/12 , C12Q1/485 , C12Q2600/106 , G01N33/57426 , G01N2333/82
摘要： The tides 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 they 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 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：包含由突变的功能性Ab1激酶结构域组成的氨基酸序列的所述突变体，所述突变的功能性激酶结构域对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，用于筛选抑制这些多肽的酪氨酸激酶活性的化合物，涉及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，以及这些核酸分子在产生此类多肽中的用途，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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