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1.发明授权Compounds and compositions for inhibiting the activity of ABL1, ABL2 and BCR-ABL1 有权用于抑制ABL1，ABL2和BCR-ABL1活性的化合物和组合物公开(公告)号：US09278981B2
公开(公告)日：2016-03-08
申请号：US14400987
申请日：2013-05-09
申请人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Brynley Jones , Paul William Manley , Andreas Marzinzik , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer , Erich Alois Spieser
发明人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Brynley Jones , Paul William Manley , Andreas Marzinzik , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer , Erich Alois Spieser
IPC分类号： A61K31/4439 , C07D498/08 , C07D401/14 , C07D405/14 , C07D413/14 , C07D401/04 , C07D401/10 , C07D403/10 , C07D413/10 , C07D471/04 , C07D487/04 , C07D487/10 , C07D491/10 , A61K31/444 , A61K31/4545 , A61K31/4725 , A61K31/498 , A61K31/5025 , A61K31/506 , A61K31/551 , A61K31/553 , A61K45/06 , C07D491/107
CPC分类号： C07D498/08 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4725 , A61K31/498 , A61K31/5025 , A61K31/506 , A61K31/551 , A61K31/553 , A61K45/06 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/14 , C07D413/10 , C07D413/14 , C07D471/04 , C07D487/04 , C07D487/10 , C07D491/10 , C07D491/107
摘要： The present invention relates to compounds of formula (I): in which Y, Y, R, R 2, R 3 and R 4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
摘要翻译： 本发明涉及式（I）化合物：其中Y，Y，R，R 2，R 3和R 4在发明概述中定义; 能够抑制BCR-ABL1及其突变体的活性。 本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂和使用这些化合物治疗癌症的方法。
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2.发明申请COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF ABL1, ABL2 AND BCR-ABL1 有权抑制ABL1，ABL2和BCR-ABL1活性的化合物和组合物公开(公告)号：US20150183801A1
公开(公告)日：2015-07-02
申请号：US14400987
申请日：2013-05-09
申请人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Brynley Jones , Paul William Manley , Andreas Marzinzik , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer , Erich Alois Spieser
发明人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Brynley Jones , Paul William Manley , Andreas Marzinzik , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer , Erich Alois Spieser
IPC分类号： C07D498/08 , A61K31/506 , C07D401/10 , A61K31/4439 , C07D401/14 , C07D487/04 , C07D487/10 , C07D471/04 , C07D405/14 , A61K31/444 , A61K31/4725 , A61K31/498 , C07D491/107 , A61K31/4545 , A61K31/551 , A61K31/553 , A61K45/06 , A61K31/5025 , C07D403/10
CPC分类号： C07D498/08 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4725 , A61K31/498 , A61K31/5025 , A61K31/506 , A61K31/551 , A61K31/553 , A61K45/06 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/14 , C07D413/10 , C07D413/14 , C07D471/04 , C07D487/04 , C07D487/10 , C07D491/10 , C07D491/107
摘要： The present invention relates to compounds of formula (I): in which Y, Y, R, R 2, R 3 and R 4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
摘要翻译： 本发明涉及式（I）化合物：其中Y，Y，R，R 2，R 3和R 4在发明概述中定义; 能够抑制BCR-ABL1及其突变体的活性。 本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂和使用这些化合物治疗癌症的方法。
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3.发明授权Benzamide derivatives for inhibiting the activity of ABL1, ABL2 and BCR-ABL1 有权用于抑制ABL1，ABL2和BCR-ABL1活性的苯甲酰胺衍生物公开(公告)号：US09340537B2
公开(公告)日：2016-05-17
申请号：US14400992
申请日：2013-05-09
申请人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Brynley Jones , Paul William Manley , Andreas Marzinzik , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
发明人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Brynley Jones , Paul William Manley , Andreas Marzinzik , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
IPC分类号： C07D417/10 , C07D417/14 , C07D401/14 , C07D405/14 , C07D413/14 , C07D401/04 , C07D403/10 , C07D409/14 , A61K31/4025 , A61K31/427 , A61K31/4439 , A61K31/5377 , A61K45/06
CPC分类号： C07D417/14 , A61K31/4025 , A61K31/4155 , A61K31/427 , A61K31/4439 , A61K31/5377 , A61K45/06 , C07D401/04 , C07D401/14 , C07D403/10 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/10 , C07D487/10
摘要： The present invention relates to compounds of formula (I): in which Y, Y, R, R 2, R 3 and R 4 are defined in the Summary of the Invention; capable of inhibiting the tyrosine kinase enzymatic activity of the Abelson protein (ABL1), the Abelson-related protein (ABL2) and related chimeric proteins, in particular BCR-ABL1. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
摘要翻译： 本发明涉及式（I）化合物：其中Y，Y，R，R 2，R 3和R 4在发明概述中定义; 能够抑制Abelson蛋白（ABL1），Abelson相关蛋白（ABL2）和相关嵌合蛋白（特别是BCR-ABL1）的酪氨酸激酶酶活性。 本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂和使用这些化合物治疗癌症的方法。
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4.发明授权Compounds and compositions for inhibiting the activity of ABL1, ABL2 and BCR-ABL1 有权用于抑制ABL1，ABL2和BCR-ABL1活性的化合物和组合物公开(公告)号：US09315489B2
公开(公告)日：2016-04-19
申请号：US14400990
申请日：2013-05-09
申请人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Brynley Jones , Paul William Manley , Andreas Marzinzik , Saliha Moussaoui , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
发明人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Brynley Jones , Paul William Manley , Andreas Marzinzik , Saliha Moussaoui , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
IPC分类号： C07D401/04 , A61K31/4427 , C07D403/04 , C07D213/81 , C07D213/85 , C07D317/60 , C07D231/12 , C07D233/38 , C07D233/54 , C07D239/26 , C07D239/30 , C07D239/34 , C07D407/14 , C07D241/12 , C07D241/20 , C07D277/22 , A61K31/381 , A61K31/4025 , A61K31/4418 , A61K31/4965 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D333/38
CPC分类号： C07D239/26 , A61K31/36 , A61K31/381 , A61K31/4025 , A61K31/415 , A61K31/4164 , A61K31/426 , A61K31/4418 , A61K31/4439 , A61K31/4965 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D213/81 , C07D213/85 , C07D231/12 , C07D233/38 , C07D233/54 , C07D233/56 , C07D239/30 , C07D239/34 , C07D241/12 , C07D241/20 , C07D277/22 , C07D277/30 , C07D317/60 , C07D333/22 , C07D333/38 , C07D401/04 , C07D403/04 , C07D405/14 , C07D407/14 , C07D409/06
摘要： The present invention relates to compounds of formula I: in which Y, Y1, Y4, Y5, Y6, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
摘要翻译： 本发明涉及式I化合物：其中Y，Y 1，Y 4，Y 5，Y 6，R 1，R 2，R 3和R 4在发明概述中定义; 能够抑制BCR-ABL1及其突变体的活性。 本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂和使用这些化合物治疗癌症的方法。
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5.发明申请COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF ABL1, ABL2 AND BCR-ABL1 有权抑制ABL1，ABL2和BCR-ABL1活性的化合物和组合物公开(公告)号：US20150141427A1
公开(公告)日：2015-05-21
申请号：US14400990
申请日：2013-05-09
申请人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Brynley Jones , Paul William Manley , Andreas Marzinzik , Saliha Moussaoui , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
发明人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Brynley Jones , Paul William Manley , Andreas Marzinzik , Saliha Moussaoui , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
IPC分类号： C07D403/04 , A61K31/505 , C07D239/34 , C07D213/85 , A61K31/4418 , C07D241/20 , A61K31/4965 , C07D241/12 , C07D333/38 , A61K31/381 , A61K31/4025 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D239/26
CPC分类号： C07D239/26 , A61K31/36 , A61K31/381 , A61K31/4025 , A61K31/415 , A61K31/4164 , A61K31/426 , A61K31/4418 , A61K31/4439 , A61K31/4965 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D213/81 , C07D213/85 , C07D231/12 , C07D233/38 , C07D233/54 , C07D233/56 , C07D239/30 , C07D239/34 , C07D241/12 , C07D241/20 , C07D277/22 , C07D277/30 , C07D317/60 , C07D333/22 , C07D333/38 , C07D401/04 , C07D403/04 , C07D405/14 , C07D407/14 , C07D409/06
摘要： The present invention relates to compounds of formula I: in which Y, Y1, Y4, Y5, Y6, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
摘要翻译： 本发明涉及式I化合物：其中Y，Y 1，Y 4，Y 5，Y 6，R 1，R 2，R 3和R 4在发明概述中定义; 能够抑制BCR-ABL1及其突变体的活性。 本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂和使用这些化合物治疗癌症的方法。
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6.发明申请BENZAMIDE DERIVATIVES FOR INHIBITING THE ACTIVITY OF ABL1, ABL2 AND BCR-ABL1 有权用于抑制ABL1，ABL2和BCR-ABL1活性的苯扎明星衍生物公开(公告)号：US20150126485A1
公开(公告)日：2015-05-07
申请号：US14400992
申请日：2013-05-09
申请人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Brynley Jones , Paul William Manley , Andreas Marzinzik , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
发明人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Brynley Jones , Paul William Manley , Andreas Marzinzik , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
IPC分类号： C07D417/14 , A61K31/427 , A61K45/06 , C07D401/14 , A61K31/4439 , A61K31/4025 , C07D413/14 , C07D409/14 , C07D401/04 , A61K31/5377 , C07D403/10 , C07D417/10 , C07D405/14
CPC分类号： C07D417/14 , A61K31/4025 , A61K31/4155 , A61K31/427 , A61K31/4439 , A61K31/5377 , A61K45/06 , C07D401/04 , C07D401/14 , C07D403/10 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/10 , C07D487/10
摘要： The present invention relates to compounds of formula (I): in which Y, Y, R, R 2, R 3 and R 4 are defined in the Summary of the Invention; capable of inhibiting the tyrosine kinase enzymatic activity of the Abelson protein (ABL1), the Abelson-related protein (ABL2) and related chimeric proteins, in particular BCR-ABL1. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
摘要翻译： 本发明涉及式（I）化合物：其中Y，Y，R，R 2，R 3和R 4在发明概述中定义; 能够抑制Abelson蛋白（ABL1），Abelson相关蛋白（ABL2）和相关嵌合蛋白（特别是BCR-ABL1）的酪氨酸激酶酶活性。 本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂和使用这些化合物治疗癌症的方法。
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7.发明授权Compounds and compositions for inhibiting the activity of ABL1, ABL2 and BCR-ABL1 有权用于抑制ABL1，ABL2和BCR-ABL1活性的化合物和组合物公开(公告)号：US08829195B2
公开(公告)日：2014-09-09
申请号：US13892769
申请日：2013-05-13
申请人： Stephanie Kay Dodd , Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Brynley Jones , Paul William Manley , Andreas Marzinzik , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
发明人： Stephanie Kay Dodd , Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Brynley Jones , Paul William Manley , Andreas Marzinzik , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
IPC分类号： C07D401/00 , C07D211/72 , C07D211/84 , C07D211/56 , A01N43/40 , A61K31/44 , C07D405/14 , C07D401/10 , C07D401/04 , C07D213/82 , A61K45/06 , C07D403/10 , C07F9/58 , A61K31/4439 , A61K31/506 , C07D401/14
CPC分类号： C07D213/82 , A61K31/4439 , A61K31/506 , A61K45/06 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/14 , C07F9/58
摘要： The present invention relates to compounds of formula (I): in which Y, Y1, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
摘要翻译： 本发明涉及式（I）化合物：其中Y，Y 1，R 1，R 2，R 3和R 4在发明概述中定义; 能够抑制BCR-ABL1及其突变体的活性。 本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂和使用这些化合物治疗癌症的方法。
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公开(公告)号：US20160185733A1
公开(公告)日：2016-06-30
申请号：US15060723
申请日：2016-03-04
申请人： Pascal FURET , Robert Martin GROTZFELD , Wolfgang JAHNKE , Darryl JONES , Paul William Manley , Andreas MARZINZIK , Saliha MOUSSAOUI , Xavier Francois Andre PELLE , Bahaa SALEM , Joseph SCHOEPFER
发明人： Pascal FURET , Robert Martin GROTZFELD , Wolfgang JAHNKE , Darryl JONES , Paul William Manley , Andreas MARZINZIK , Saliha MOUSSAOUI , Xavier Francois Andre PELLE , Bahaa SALEM , Joseph SCHOEPFER
IPC分类号： C07D239/26 , C07D239/34 , C07D401/04 , A61K31/506 , C07D241/20 , A61K31/4965 , C07D241/12 , C07D333/38 , A61K31/381 , C07D409/06 , A61K31/4025 , C07D233/56 , A61K31/4164 , C07D277/30 , A61K31/426 , C07D231/12 , A61K31/415 , C07D405/14 , A61K31/4439 , C07D403/04 , C07D317/60 , A61K31/36 , C07D333/22 , A61K31/5377 , A61K45/06 , A61K31/505
CPC分类号： C07D239/26 , A61K31/36 , A61K31/381 , A61K31/4025 , A61K31/415 , A61K31/4164 , A61K31/426 , A61K31/4418 , A61K31/4439 , A61K31/4965 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D213/81 , C07D213/85 , C07D231/12 , C07D233/38 , C07D233/54 , C07D233/56 , C07D239/30 , C07D239/34 , C07D241/12 , C07D241/20 , C07D277/22 , C07D277/30 , C07D317/60 , C07D333/22 , C07D333/38 , C07D401/04 , C07D403/04 , C07D405/14 , C07D407/14 , C07D409/06
摘要： The present invention relates to compounds of formula I: in which Y, Y1, Y4, Y5, Y6, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
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公开(公告)号：US09896444B2
公开(公告)日：2018-02-20
申请号：US15075620
申请日：2016-03-21
申请人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Jones , Paul William Manley , Andreas Marzinzik , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
发明人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Jones , Paul William Manley , Andreas Marzinzik , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
IPC分类号： C07D401/14 , C07D417/14 , A61K31/4155 , C07D487/10 , C07D405/14 , C07D413/14 , C07D401/04 , C07D403/10 , C07D409/14 , C07D417/10 , A61K31/4025 , A61K31/427 , A61K31/4439 , A61K31/5377 , A61K45/06
CPC分类号： C07D417/14 , A61K31/4025 , A61K31/4155 , A61K31/427 , A61K31/4439 , A61K31/5377 , A61K45/06 , C07D401/04 , C07D401/14 , C07D403/10 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/10 , C07D487/10
摘要： The present invention relates to compounds of formula (I): in which Y, Y1, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the tyrosine kinase enzymatic activity of the Abelson protein (ABL1), the Abelson-related protein (ABL2) and related chimeric proteins, in particular BCR-ABL1. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
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10.发明授权Compounds and compositions for inhibiting the activity of ABL1, ABL2 and BCR-ABL1 有权用于抑制ABL1，ABL2和BCR-ABL1活性的化合物和组合物公开(公告)号：US09458112B2
公开(公告)日：2016-10-04
申请号：US15060723
申请日：2016-03-04
申请人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Jones , Paul William Manley , Andreas Marzinzik , Saliha Moussaoui , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
发明人： Pascal Furet , Robert Martin Grotzfeld , Wolfgang Jahnke , Darryl Jones , Paul William Manley , Andreas Marzinzik , Saliha Moussaoui , Xavier Francois Andre Pelle , Bahaa Salem , Joseph Schoepfer
IPC分类号： C07D239/26 , C07D401/04 , A61K31/505 , C07D239/34 , A61K31/506 , C07D241/20 , A61K31/4965 , C07D241/12 , C07D333/38 , A61K31/381 , C07D409/06 , A61K31/4025 , C07D233/56 , A61K31/4164 , C07D277/30 , A61K31/426 , C07D231/12 , A61K31/415 , C07D405/14 , A61K31/4439 , C07D403/04 , C07D317/60 , A61K31/36 , C07D333/22 , A61K31/5377 , A61K45/06
CPC分类号： C07D239/26 , A61K31/36 , A61K31/381 , A61K31/4025 , A61K31/415 , A61K31/4164 , A61K31/426 , A61K31/4418 , A61K31/4439 , A61K31/4965 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D213/81 , C07D213/85 , C07D231/12 , C07D233/38 , C07D233/54 , C07D233/56 , C07D239/30 , C07D239/34 , C07D241/12 , C07D241/20 , C07D277/22 , C07D277/30 , C07D317/60 , C07D333/22 , C07D333/38 , C07D401/04 , C07D403/04 , C07D405/14 , C07D407/14 , C07D409/06
摘要： The present invention relates to compounds of formula I: in which Y, Y1, Y4, Y5, Y6, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
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