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公开(公告)号：US09802960B2
公开(公告)日：2017-10-31
申请号：US14596052
申请日：2015-01-13
发明人： Indu T. Bharathan , Chris Blackburn , Jeffrey P. Ciavarri , Jouhara Chouitar , Courtney A. Cullis , Natalie D'Amore , Paul E. Fleming , Kenneth M. Gigstad , Krista E. Gipson , Mario Girard , Yongbo Hu , Janice Lee , Gang Li , Mansoureh Rezaei , Michael D. Sintchak , Francois Soucy , Stephen G. Stroud , Tricia J. Vos , Tzu-Tshin Wong , He Xu , Tianlin Xu , Yingchun Ye
IPC分类号： A61K31/506 , C07D513/04 , C07D401/04 , A61K31/444 , A61K45/06 , C07D417/14 , C07D401/14 , C07D471/04 , A61K31/437 , A61K31/549 , A61K31/497
CPC分类号： C07D513/04 , A61K31/437 , A61K31/444 , A61K31/497 , A61K31/506 , A61K31/549 , A61K45/06 , C07D401/04 , C07D401/14 , C07D417/14 , C07D471/04 , A61K2300/00
摘要： The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
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2.发明申请PYRAZOLOPYRIMIDINYL INHIBITORS OF UBIQUITIN-ACTIVATING ENZYME 有权UBIQUITIN-ACTIVATING ENZYME的吡唑并嘧啶类抑制剂公开(公告)号：US20140088096A9
公开(公告)日：2014-03-27
申请号：US13767314
申请日：2013-02-14
发明人： Roushan Afroze , Indu T. Bharathan , Jeffrey P. Ciavarri , Paul E. Fleming , Jeffrey L. Gaulin , Mario Girard , Steven P. Langston , Francois Soucy , Tzu-Tshin Wong , Yingchun Ye
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Disclosed are chemical entities that inhibit ubiquitin-activating enzyme (UAE), each of which is a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein Y is and W, Z, XY, RY1, RY2 and RY3 are defined herein; pharmaceutical compositions comprising the chemical entities; and methods of using the chemical entities. These chemical entities are useful for treating disorders, particularly cell proliferation disorders, including cancers.
摘要翻译： 公开了抑制泛素活化酶（UAE）的化学实体，其各自是式I的化合物或其药学上可接受的盐，其中Y是且W，Z，XY，RY1，RY2和RY3在本文中定义; 包含化学实体的药物组合物; 以及使用化学实体的方法。 这些化学实体可用于治疗疾病，特别是细胞增殖障碍，包括癌症。
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公开(公告)号：US09663525B2
公开(公告)日：2017-05-30
申请号：US15048007
申请日：2016-02-19
发明人： Roushan Afroze , Indu T. Bharathan , Jeffrey P. Ciavarri , Paul E. Fleming , Jeffrey L. Gaulin , Marlo Girard , Steven P. Langston , Francois Soucy , Tzu-Tshin Wong , Yingchun Ye
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Disclosed are chemical entities that inhibit ubiquitin-activating enzyme (UAE), each of which is a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein Y is and W, Z, XY, RY1, RY2 and RY3 are defined herein; pharmaceutical compositions comprising the chemical entities; and methods of using the chemical entities. These chemical entities are useful for treating disorders, particularly cell proliferation disorders, including cancers.
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公开(公告)号：US09290500B2
公开(公告)日：2016-03-22
申请号：US13767314
申请日：2013-02-14
发明人： Roushan Afroze , Indu T. Bharathan , Jeffrey P. Ciavarri , Paul E. Fleming , Jeffrey L. Gaulin , Mario Girard , Steven P. Langston , Francois Soucy , Tzu-Tshin Wong , Yingchun Ye
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Disclosed are chemical entities that inhibit ubiquitin-activating enzyme (UAE), each of which is a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein Y is and W, Z, XY, RY1, RY2 and RY3 are defined herein; pharmaceutical compositions comprising the chemical entities; and methods of using the chemical entities. These chemical entities are useful for treating disorders, particularly cell proliferation disorders, including cancers.
摘要翻译： 公开了抑制泛素活化酶（UAE）的化学实体，其各自是式I的化合物或其药学上可接受的盐，其中Y是且W，Z，XY，RY1，RY2和RY3在本文中定义; 包含化学实体的药物组合物; 以及使用化学实体的方法。 这些化学实体可用于治疗疾病，特别是细胞增殖障碍，包括癌症。
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公开(公告)号：US10202389B2
公开(公告)日：2019-02-12
申请号：US15699818
申请日：2017-09-08
发明人： Roushan Afroze , Indu T. Bharathan , Jeffrey P. Ciavarri , Paul E. Fleming , Jeffrey L. Gaulin , Mario Girard , Steven P. Langston , Francois Soucy , Tzu-Tshin Wong , Yingchun Ye
IPC分类号： C07D487/04
摘要： Disclosed are chemical entities that inhibit ubiquitin-activating enzyme (UAE), each of which is a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein Y is and W, Z, XY, RY1, RY2 and RY3 are defined herein; pharmaceutical compositions comprising the chemical entities; and methods of using the chemical entities. These chemical entities are useful for treating disorders, particularly cell proliferation disorders, including cancers.
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公开(公告)号：US10538533B2
公开(公告)日：2020-01-21
申请号：US15665506
申请日：2017-08-01
发明人： Indu T. Bharathan , Chris Blackburn , Jeffrey P. Ciavarri , Jouhara Chouitar , Courtney A. Cullis , Natalie D'Amore , Paul E. Fleming , Kenneth M. Gigstad , Krista E. Gipson , Mario Girard , Yongbo Hu , Janice Lee , Gang Li , Mansoureh Rezaei , Michael D. Sintchak , Francois Soucy , Stephen G. Stroud , Tricia J. Vos , Tzu-Tshin Wong , He Xu , Tianlin Xu , Yingchun Ye
IPC分类号： C07D513/04 , C07D401/04 , A61K31/444 , A61K45/06 , C07D417/14 , C07D401/14 , A61K31/506 , C07D471/04 , A61K31/437 , A61K31/549 , A61K31/497
摘要： The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
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公开(公告)号：US09796725B2
公开(公告)日：2017-10-24
申请号：US15488800
申请日：2017-04-17
发明人： Roushan Afroze , Indu T. Bharathan , Jeffrey P. Ciavarri , Paul E. Fleming , Jeffrey L. Gaulin , Mario Girard , Steven P. Langston , Francois Soucy , Tzu-Tshin Wong , Yingchun Ye
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Disclosed are chemical entities that inhibit ubiquitin-activating enzyme (UAE), each of which is a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein Y is and W, Z, XY, RY1, RY2 and RY3 are defined herein; pharmaceutical compositions comprising the chemical entities; and methods of using the chemical entities. These chemical entities are useful for treating disorders, particularly cell proliferation disorders, including cancers.
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公开(公告)号：US09751854B2
公开(公告)日：2017-09-05
申请号：US15347334
申请日：2016-11-09
发明人： Indu T. Bharathan , Chris Blackburn , Jeffrey P. Ciavarri , Jouhara Chouitar , Courtney A. Cullis , Natalie D'Amore , Paul E. Fleming , Kenneth M. Gigstad , Krista E. Gipson , Mario Girard , Yongbo Hu , Janice Lee , Gang Li , Mansoureh Rezaei , Michael D. Sintchak , Francois Soucy , Stephen G. Stroud , Tricia J. Vos , Tzu-Tshin Wong , He Xu , Tianlin Xu , Yingchun Ye
IPC分类号： C07D401/04 , C07D513/04 , A61K31/444 , A61K45/06 , C07D417/14 , C07D401/14 , A61K31/506 , C07D471/04 , A61K31/437 , A61K31/549 , A61K31/497
CPC分类号： C07D513/04 , A61K31/437 , A61K31/444 , A61K31/497 , A61K31/506 , A61K31/549 , A61K45/06 , C07D401/04 , C07D401/14 , C07D417/14 , C07D471/04 , A61K2300/00
摘要： The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
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公开(公告)号：US20150225422A1
公开(公告)日：2015-08-13
申请号：US14596052
申请日：2015-01-13
发明人： Indu T. Bharathan , Chris Blackburn , Jeffrey P. Ciavarri , Jouhara Chouitar , Courtney A. Cullis , Natalie D'Amore , Paul E. Fleming , Kenneth M. Gigstad , Krista E. Gipson , Mario Girard , Yongbo Hu , Janice Lee , Gang Li , Mansoureh Rezaei , Michael D. Sintchak , Francois Soucy , Stephen G. Stroud , Tricia J. Vos , Tzu-Tshin Wong , He Xu , Tianlin Xu , Yingchun Ye
IPC分类号： C07D513/04 , A61K31/444 , A61K45/06 , A61K31/549 , C07D401/14 , A61K31/506 , C07D471/04 , A61K31/437 , C07D401/04 , C07D417/14
CPC分类号： C07D513/04 , A61K31/437 , A61K31/444 , A61K31/497 , A61K31/506 , A61K31/549 , A61K45/06 , C07D401/04 , C07D401/14 , C07D417/14 , C07D471/04 , A61K2300/00
摘要： The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
摘要翻译： 本发明提供式I化合物及其药学上可接受的盐，其中X，R 1，R 2，R 3，R 4，R 5，L 1，L 2，m和n如说明书所述。 这样的化合物是VPS34的抑制剂，因此可用于治疗增殖性，炎性或心血管疾病。
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10.发明申请PYRAZOLOPYRIMIDINYL INHIBITORS OF UBIQUITIN-ACTIVATING ENZYME 有权UBIQUITIN-ACTIVATING ENZYME的吡唑并嘧啶类抑制剂公开(公告)号：US20130217682A1
公开(公告)日：2013-08-22
申请号：US13767314
申请日：2013-02-14
发明人： Roushan Afroze , Indu T. Bharathan , Jeffrey P. Ciavarri , Paul E. Fleming , Jeffrey L. Gaulin , Mario Girard , Steven P. Langston , Francois Soucy , Tzu-Tshin Wong , Yingchun Ye
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Disclosed are chemical entities that inhibit ubiquitin-activating enzyme (UAE), each of which is a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein Y is and W, Z, XY, RY1, RY2 and RY3 are defined herein; pharmaceutical compositions comprising the chemical entities; and methods of using the chemical entities. These chemical entities are useful for treating disorders, particularly cell proliferation disorders, including cancers.
摘要翻译： 公开了抑制泛素活化酶（UAE）的化学实体，其各自是式I的化合物或其药学上可接受的盐，其中Y是且W，Z，XY，RY1，RY2和RY3在本文中定义; 包含化学实体的药物组合物; 以及使用化学实体的方法。 这些化学实体可用于治疗疾病，特别是细胞增殖障碍，包括癌症。
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