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31. 发明授权

US07671049B2 Pyrrole based inhibitors of glycogen synthase kinase 3 失效
标题翻译：基于吡咯的糖原合酶激酶抑制剂3
公开(公告)号：US07671049B2
公开(公告)日：2010-03-02
申请号：US11761937
申请日：2007-06-12
申请人： Manoj C. Desai , Simon Ng , Zhi-Jie Ni , Keith B. Pfister , Savithri Ramurthy , Sharadha Subramanian , Allan S. Wagman
发明人： Manoj C. Desai , Simon Ng , Zhi-Jie Ni , Keith B. Pfister , Savithri Ramurthy , Sharadha Subramanian , Allan S. Wagman
IPC分类号： A61K31/44 , A61K31/445 , A61K31/497
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D453/02 , C07D487/08
摘要： New pyrrole based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.
摘要翻译：提供了新的基于吡咯的化合物，组合物和抑制糖原合酶激酶（GSK3）活性并在体内治疗GSK3介导的病症的方法。本发明的方法，化合物和组合物可以单独使用或与其它药理活性剂组合用于治疗由GSK3活性介导的病症，例如糖尿病，阿尔茨海默病和其他神经变性疾病，肥胖症，动脉粥样硬化性心血管疾病，必需的高血压，多囊卵巢综合征，X综合征，缺血，创伤性脑损伤，双相情感障碍，免疫缺陷或癌症。

32. 发明授权

US09546173B2 Substituted pyrrolo[3,4-d]pyrimidines as kinase inhibitors 有权
标题翻译：取代的吡咯并[3,4-d]嘧啶作为激酶抑制剂
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

33. 发明申请

US20150274733A1 DIHYDROPYRROLIDINO-PYRIMIDINES AS KINASE INHIBITORS 有权
标题翻译：作为激酶抑制剂的二氢吡咯烷酮
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

34. 发明申请

US20070299039A1 Substituted benz-azoles and methods of their use as inhibitors of Raf kinase 失效
标题翻译：取代的苯并唑及其用作Raf激酶抑制剂的方法
公开(公告)号：US20070299039A1
公开(公告)日：2007-12-27
申请号：US11282939
申请日：2005-11-18
申请人： Payman Amiri , Wendy Fantl , Teresa Hansen , Barry Levine , Christopher McBride , Daniel Poon , Savithri Ramurthy , Paul Renhowe , Cynthia Shafer , Sharadha Subramanian , Leonard Sung
发明人： Payman Amiri , Wendy Fantl , Teresa Hansen , Barry Levine , Christopher McBride , Daniel Poon , Savithri Ramurthy , Paul Renhowe , Cynthia Shafer , Sharadha Subramanian , Leonard Sung
IPC分类号： A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/5377 , A61K31/55 , A61K31/665 , A61P35/00 , C07D401/10 , C07D401/14 , C07D413/10 , C07D413/14 , C07D417/10
CPC分类号： C07D401/14 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/12 , C07D417/14 , C07D453/02
摘要： New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
摘要翻译：提供了新的取代的苯并唑化合物，抑制人或动物受试者中Raf激酶活性的组合物和方法。新化合物组合物可以单独使用或与至少一种另外的药物组合使用，用于治疗Raf激酶介导的病症，例如癌症。

35. 发明申请

US20070244109A1 PYRROLE BASED INHIBITORS OF GLYCOGEN SYNTHASE KINASE 3 失效
标题翻译：吡咯基合成酶抑制剂3
公开(公告)号：US20070244109A1
公开(公告)日：2007-10-18
申请号：US11761937
申请日：2007-06-12
申请人： Manoj Desai , Simon Ng , Zhi-Jie Ni , Keith Pfister , Savithri Ramurthy , Sharadha Subramanian , Allan Wagman
发明人： Manoj Desai , Simon Ng , Zhi-Jie Ni , Keith Pfister , Savithri Ramurthy , Sharadha Subramanian , Allan Wagman
IPC分类号： A61K31/44 , A61K31/445 , A61K31/497 , A61K31/535 , A61P25/28 , A61P3/10
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D453/02 , C07D487/08
摘要： New pyrrole based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.
摘要翻译：提供了新的基于吡咯的化合物，组合物和抑制糖原合酶激酶（GSK3）活性并在体内治疗GSK3介导的病症的方法。本发明的方法，化合物和组合物可以单独使用或与其它药理活性剂组合用于治疗由GSK3活性介导的病症，例如糖尿病，阿尔茨海默病和其他神经变性疾病，肥胖症，动脉粥样硬化性心血管疾病，必需的高血压，多囊卵巢综合征，X综合征，缺血，创伤性脑损伤，双相情感障碍，免疫缺陷或癌症。

36. 发明申请

US20050085482A1 2,6-Disubstituted quinazolines, quinoxalines, quinolines and isoquinolines and methods of their use as inhibitors of RAF kinase 失效
标题翻译： 2,6-二取代喹唑啉，喹喔啉，喹啉和异喹啉及其作为RAF激酶抑制剂的方法
公开(公告)号：US20050085482A1
公开(公告)日：2005-04-21
申请号：US10966358
申请日：2004-10-15
申请人： Savithri Ramurthy , Paul Renhowe , Sharadha Subramanian
发明人： Savithri Ramurthy , Paul Renhowe , Sharadha Subramanian
IPC分类号： A61K31/4709 , A61K31/498 , A61K31/502 , A61K31/517 , C07D401/12 , C07D401/14 , G10H7/00
CPC分类号： C07D401/12 , C04B35/632 , C07D401/14
摘要： New substituted quinazoline, quinoxaline, quinoline and isoquinoline compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
摘要翻译：提供新的取代喹唑啉，喹喔啉，喹啉和异喹啉化合物，抑制人或动物受试者中Raf激酶活性的组合物和方法。新化合物组合物可以单独使用或与至少一种另外的药物组合使用，用于治疗Raf激酶介导的病症，例如癌症。

37. 发明授权

US07250443B2 Pyrrole based inhibitors of glycogen synthase kinase 3 失效
标题翻译：基于吡咯的糖原合成酶激酶抑制剂3
公开(公告)号：US07250443B2
公开(公告)日：2007-07-31
申请号：US10646625
申请日：2003-08-21
申请人： Manoj C. Desai , Simon Ng , Zhi-Jie Ni , Keith B. Pfister , Savithri Ramurthy , Sharadha Subramanian , Allan S. Wagman
发明人： Manoj C. Desai , Simon Ng , Zhi-Jie Ni , Keith B. Pfister , Savithri Ramurthy , Sharadha Subramanian , Allan S. Wagman
IPC分类号： A61K31/4025 , A61K31/401 , C07D43/02
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D453/02 , C07D487/08
摘要： New pyrrole based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.
摘要翻译：提供了新的基于吡咯的化合物，组合物和抑制糖原合酶激酶（GSK3）活性并在体内治疗GSK3介导的疾病的方法。本发明的方法，化合物和组合物可以单独使用或与其它药理活性剂组合用于治疗由GSK3活性介导的病症，例如糖尿病，阿尔茨海默病和其他神经变性疾病，肥胖症，动脉粥样硬化性心血管疾病，必需的高血压，多囊卵巢综合征，X综合征，缺血，创伤性脑损伤，双相情感障碍，免疫缺陷或癌症。

38. 发明申请

US20070161680A1 Substituted benzimidazoles and methods of their use 有权
标题翻译：取代的苯并咪唑及其使用方法
公开(公告)号：US20070161680A1
公开(公告)日：2007-07-12
申请号：US11513959
申请日：2006-08-30
申请人： Mina Alkawa , Payman Amiri , Jeffrey Dove , Barry Levine , Christopher McBride , Teresa Pick , Daniel Poon , Savithri Ramurthy , Paul Renhowe , Cynthia Shafer , Darrin Stuart , Sharadha Subramanian
发明人： Mina Alkawa , Payman Amiri , Jeffrey Dove , Barry Levine , Christopher McBride , Teresa Pick , Daniel Poon , Savithri Ramurthy , Paul Renhowe , Cynthia Shafer , Darrin Stuart , Sharadha Subramanian
IPC分类号： A61K31/4439 , C07D403/14
CPC分类号： C07D401/14 , Y02P20/55
摘要： New substituted benzimidazole compounds, compositions, and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
摘要翻译：提供了新的取代的苯并咪唑化合物，组合物和抑制与人或动物受试者的肿瘤发生相关的激酶活性的方法。在某些实施方案中，化合物和组合物有效地抑制至少一种丝氨酸/苏氨酸激酶或受体酪氨酸激酶的活性。新化合物和组合物可以单独使用或与至少一种另外的药剂组合使用，用于治疗丝氨酸/苏氨酸激酶或受体酪氨酸激酶介导的病症，例如癌症。

39. 发明申请

US20050192287A1 Substituted benzazoles and methods of their use as inhibitors of Raf kinase 失效
标题翻译：取代的苯并唑及其作为Raf激酶抑制剂的方法
公开(公告)号：US20050192287A1
公开(公告)日：2005-09-01
申请号：US10967089
申请日：2004-10-15
申请人： Abran Costales , Teresa Hansen , Barry Levine , Christopher McBride , Daniel Poon , Savithri Ramurthy , Paul Renhowe , Cynthia Shafer , Sharadha Subramanian , Joelle Verhagen
发明人： Abran Costales , Teresa Hansen , Barry Levine , Christopher McBride , Daniel Poon , Savithri Ramurthy , Paul Renhowe , Cynthia Shafer , Sharadha Subramanian , Joelle Verhagen
IPC分类号： A61K31/4439 , A61K31/4745 , A61K31/496 , A61K31/506 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/12
CPC分类号： C07D401/12 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/551 , A61K45/06 , C04B35/632 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14
摘要： New substituted benzazole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
摘要翻译：提供了新的取代的苯唑化合物，抑制人或动物受试者中的Raf激酶活性的组合物和方法。新化合物组合物可以单独使用或与至少一种另外的药物组合使用，用于治疗Raf激酶介导的病症，例如癌症。

40. 发明授权

US06989382B2 Carbocycle based inhibitors of glycogen synthase kinase 3 失效
标题翻译：基于碳循环的糖原合酶激酶抑制剂3
公开(公告)号：US06989382B2
公开(公告)日：2006-01-24
申请号：US10690497
申请日：2003-10-20
申请人： Allan S. Wagman , Sharadha Subramanian , John M. Nuss
发明人： Allan S. Wagman , Sharadha Subramanian , John M. Nuss
IPC分类号： C07D401/04 , A61K31/44
CPC分类号： C07D213/74 , C07D213/85 , C07D401/12
摘要： New carbocyclic compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease, other neurodegenerative disorders, such as Parkinson's disease and Huntington's disease, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.
摘要翻译：提供了新的碳环化合物，体外抑制糖原合酶激酶（GSK3）活性和体内GSK3介导的病症治疗的组合物和方法。本发明的方法，化合物和组合物可以单独使用或与其它药理活性剂组合用于治疗由GSK3活性介导的病症，例如治疗糖尿病，阿尔茨海默氏病，其他神经变性疾病如帕金森病疾病和亨廷顿舞蹈病，肥胖，动脉粥样硬化性心血管疾病，原发性高血压，多囊卵巢综合征，X综合征，缺血性脑损伤，双相情感障碍，免疫缺陷或癌症。

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