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公开(公告)号：US20150274733A1
公开(公告)日：2015-10-01
申请号：US14428546
申请日：2013-09-17
申请人： Michael Patrick DILLON , Mika LINDVALL , Daniel POON , Savithri RAMURTHY , Vivek RAUNIYAR , Cynthia SHAFER , Sharadha SUBRAMANIAN , Huw TANNER
发明人： Michael Patrick Dillon , Mika Lindvall , Daniel Poon , Savithri Ramurthy , Vivek Rauniyar , Cynthia Shafer , Sharadha Subramanian , Huw Rowland Tanner
IPC分类号： C07D487/04 , A61K45/06 , A61K31/527 , A61K31/519 , C07D487/10
CPC分类号： C07D487/04 , A61K31/519 , A61K31/527 , A61K45/06 , C07D207/36 , C07D487/10
摘要： The present invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof; as further described herein. The present invention further provides pharmaceutical compositions comprising these compounds, and combinations comprising these compounds combined with or used with a therapeutic co-agent, as well as therapeutic uses of these compounds and compositions. These are useful in the treatment of diseases such as cancer that are associated with activation of ERK1 and/or ERK2, and especially for MAPK pathway dependent cancers showing resistance to Raf and/or MEK inhibitory cancer therapeutics
摘要翻译： 本发明提供式（I）的化合物及其药学上可接受的盐; 如本文进一步描述的。 本发明还提供包含这些化合物的药物组合物，以及包含与治疗性助剂组合或与其一起使用的这些化合物的组合，以及这些化合物和组合物的治疗用途。 这些可用于治疗与ERK1和/或ERK2的激活相关的疾病，特别是对显示出对Raf和/或MEK抑制性癌症治疗剂的抗性的MAPK通路依赖性癌症的疾病的治疗
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![Substituted pyrrolo[3,4-d]pyrimidines as kinase inhibitors](/abs-image/US/2017/01/17/US09546173B2/abs.jpg.150x150.jpg)
公开(公告)号：US09546173B2
公开(公告)日：2017-01-17
申请号：US14428546
申请日：2013-09-17
申请人： Michael Patrick Dillon , Mika Lindvall , Daniel Poon , Savithri Ramurthy , Vivek Rauniyar , Cynthia Shafer , Sharadha Subramanian , Huw Rowland Tanner
发明人： Michael Patrick Dillon , Mika Lindvall , Daniel Poon , Savithri Ramurthy , Vivek Rauniyar , Cynthia Shafer , Sharadha Subramanian , Huw Rowland Tanner
IPC分类号： A61K31/519 , C07D239/70 , C07D487/04 , C07D207/36 , A61K31/527 , A61K45/06 , C07D487/10
CPC分类号： C07D487/04 , A61K31/519 , A61K31/527 , A61K45/06 , C07D207/36 , C07D487/10
摘要： The present invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof; as further described herein. The present invention further provides pharmaceutical compositions comprising these compounds, and combinations comprising these compounds combined with or used with a therapeutic co-agent, as well as therapeutic uses of these compounds and compositions. These are useful in the treatment of diseases such as cancer that are associated with activation of ERK1 and/or ERK2, and especially for MAPK pathway dependent cancers showing resistance to Raf and/or MEK inhibitory cancer therapeutics.
摘要翻译： 本发明提供式（I）的化合物及其药学上可接受的盐; 如本文进一步描述的。 本发明还提供包含这些化合物的药物组合物，以及包含与治疗性助剂组合或与其一起使用的这些化合物的组合，以及这些化合物和组合物的治疗用途。 这些可用于治疗与ERK1和/或ERK2的激活相关的疾病，特别是对显示出对Raf和/或MEK抑制性癌症治疗剂的抗性的MAPK通路依赖性癌症的疾病的治疗
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3.发明授权公开(公告)号：US09173861B2
公开(公告)日：2015-11-03
申请号：US13359330
申请日：2012-01-26
申请人： Li Chen , Lichun Feng , Minmin Yang , Michael Patrick Dillon , Yingjie Lai
发明人： Li Chen , Lichun Feng , Minmin Yang , Michael Patrick Dillon , Yingjie Lai
IPC分类号： A61K31/166 , A61K31/497 , A61K31/4427 , A61K31/444 , A61K31/4436 , A61K31/4439 , C07D417/14 , C07C233/69 , A61K31/433
CPC分类号： C07D417/14 , A61K31/166 , A61K31/433 , A61K31/4427 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/497 , C07D285/06 , C07D417/12
摘要： Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted thiadiazolyl, and R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
摘要翻译： 式I化合物或其药学上可接受的盐，其中R 1为任选取代的噻二唑基，R 2，R 3，R 4，R 5，R 6，R 7和R 8如本文所定义。 还公开了使用该化合物治疗与P2X3和/或P2X2 / 3受体拮抗剂相关疾病的方法和制备该化合物的方法。
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公开(公告)号：US08846705B2
公开(公告)日：2014-09-30
申请号：US12963413
申请日：2010-12-08
申请人： Chris Allen Broka , David Scott Carter , Michael Patrick Dillon , Ronald Charles Hawley , Alam Jahangir , Clara Jeou Jen Lin , Daniel Warren Parish
发明人： Chris Allen Broka , David Scott Carter , Michael Patrick Dillon , Ronald Charles Hawley , Alam Jahangir , Clara Jeou Jen Lin , Daniel Warren Parish
IPC分类号： A61K31/505 , A61K31/506 , C07D239/48 , C07D403/12
CPC分类号： C07D239/49 , A61K31/505 , A61K31/506 , C07D239/48 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Compounds and methods for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I): or a pharmaceutically acceptable salt, solvate or prodrug thereof, wherein D, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.
摘要翻译： 用于治疗由P2X3和/或P2X2 / 3受体拮抗剂介导的疾病的化合物和方法，所述方法包括向有需要的受试者施用有效量的式（I）化合物或其药学上可接受的盐，溶剂合物或 其前体药物，其中D，X，Y，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8如本文所定义。
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5.发明授权公开(公告)号：US08193368B2
公开(公告)日：2012-06-05
申请号：US12583325
申请日：2009-08-18
IPC分类号： C07D257/04
CPC分类号： A61K31/41 , A61K31/4439 , A61K31/497 , A61K31/5377 , C07D241/12 , C07D257/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/12 , C07D407/10 , C07D409/12 , C07D413/10 , C07D417/10 , C07D417/12 , C07D471/04 , C07D491/10 , C07D491/107 , C07D498/08
摘要： Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5 and R6 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.
摘要翻译： 式I化合物或其药学上可接受的盐，其中R 1为任选取代的四唑基，R 2为任选取代的苯基，任选取代的吡啶基或任选取代的噻吩基，R 3，R 4，R 5和R 6如本文所定义。 还提供了使用该化合物治疗与P2X3和/或P2X2 / 3受体拮抗剂相关疾病的方法和制备该化合物的方法。
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6.发明申请INDOLE, INDAZOLE AND BENZIMIDAZOLE ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS 有权吲哚，吲哚和苯并咪唑类亚胺基作为P2X3和P2X2 / 3拮抗剂公开(公告)号：US20100324070A1
公开(公告)日：2010-12-23
申请号：US12820748
申请日：2010-06-22
IPC分类号： A61K31/497 , C07D401/14 , A61P29/00 , A61P17/02 , A61P25/06 , A61P31/04 , A61P9/10 , A61P1/00 , A61P15/00
CPC分类号： C07D401/14 , A61K31/497 , C07D401/04 , C07D401/10
摘要： Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, Z, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
摘要翻译： 式I化合物或其药学上可接受的盐，其中X，Y，Z，R 1，R 2，R 3，R 4和R 5如本文所定义。 还公开了使用该化合物治疗与P2X3和/或P2X2 / 3受体拮抗剂相关疾病的方法和制备该化合物的方法。
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7.发明申请OXAZOLONE AND PYRROLIDINONE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS 有权OXAZOLONE和吡咯烷酮取代的ARYLAMIDES作为P2X3和P2X2 / 3拮抗剂公开(公告)号：US20100324069A1
公开(公告)日：2010-12-23
申请号：US12820660
申请日：2010-06-22
申请人： Li Chen , Michael Patrick Dillon , Lichun Feng , Minmin Yang
发明人： Li Chen , Michael Patrick Dillon , Lichun Feng , Minmin Yang
IPC分类号： A61K31/497 , C07D413/12 , A61P29/00
CPC分类号： A61K31/497 , C07D207/27 , C07D233/32 , C07D263/20 , C07D401/14 , C07D403/12 , C07D407/14 , C07D413/10 , C07D413/12 , C07D413/14 , C07D473/00
摘要： Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
摘要翻译： 式I化合物或其药学上可接受的盐，其中X，Y，R 1，R 2，R 3，R 4，R 5，R 6和R 7如本文所定义。 还公开了使用该化合物治疗与P2X3和/或P2X2 / 3受体拮抗剂相关疾病的方法和制备该化合物的方法。
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公开(公告)号：US07799796B2
公开(公告)日：2010-09-21
申请号：US11509890
申请日：2006-08-25
IPC分类号： C07D239/48 , C07D413/12 , A61K31/506
CPC分类号： C07D239/48 , C07D401/12 , C07D403/12 , C07D405/12
摘要： Compounds and methods for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the compounds being of formula (I): wherein D, X, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.
摘要翻译： 用于治疗由P2X3和/或P2X2 / 3受体拮抗剂介导的疾病的化合物和方法，所述化合物为式（I）：其中D，X，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8为 如本文所定义。
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公开(公告)号：US07776872B2
公开(公告)日：2010-08-17
申请号：US11510015
申请日：2006-08-25
IPC分类号： C07D239/48 , C07D401/12 , A61K31/506
CPC分类号： C07D401/12 , C07D239/48 , C07D471/04
摘要： Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein A, D, E, G, J, X, Y, Z R6, R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.
摘要翻译： 式I化合物或其药学上可接受的盐，其中A，D，E，G，J，X，Y，Z R6，R7和R8如本文所定义。 还提供了使用该化合物治疗由P2X3和/或P2X2 / 3受体拮抗剂介导的疾病的方法和制备该化合物的方法。
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10.发明申请公开(公告)号：US20090326220A1
公开(公告)日：2009-12-31
申请号：US12583325
申请日：2009-08-18
IPC分类号： C07D257/04 , C07D417/12 , C07D413/12 , C07D403/14 , C07D403/12 , C07D401/12 , C07D405/12
CPC分类号： A61K31/41 , A61K31/4439 , A61K31/497 , A61K31/5377 , C07D241/12 , C07D257/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/12 , C07D407/10 , C07D409/12 , C07D413/10 , C07D417/10 , C07D417/12 , C07D471/04 , C07D491/10 , C07D491/107 , C07D498/08
摘要： Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5 and R6 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.
摘要翻译： 式I化合物或其药学上可接受的盐，其中R 1为任选取代的四唑基，R 2为任选取代的苯基，任选取代的吡啶基或任选取代的噻吩基，R 3，R 4，R 5和R 6如本文所定义。 还提供了使用该化合物治疗与P2X3和/或P2X2 / 3受体拮抗剂相关疾病的方法和制备该化合物的方法。
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