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公开(公告)号：EP2814791A1
公开(公告)日：2014-12-24
申请号：EP13748707.0
申请日：2013-02-14
发明人： AFROZE, Roushan , BHARATHAN, Indu, T. , CIAVARRI, Jeffrey, P. , FLEMING, Paul, E. , GAULIN, Jeffrey, L. , GIRARD, Mario , LANGSTON, Steven, P. , SOUCY, Francois, R. , WONG, Tzu-Tshin , YE, Yingchun
IPC分类号： C07B45/04
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, X Y , R Y1 , R Y2 and R Y3 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： 公开了抑制遍在蛋白活化酶（UAE）的化学实体，其各自为式（I）的化合物或其药学上可接受的盐，其中Y为式（II）且W，Z，XY，R Y1， 本文定义R Y2和R Y3; 包含化学实体的药物组合物; 和使用这些化学实体的方法。 这些化学实体可用于治疗疾病，特别是细胞增殖性疾病，包括癌症。
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公开(公告)号：EP3536692A1
公开(公告)日：2019-09-11
申请号：EP19170607.6
申请日：2013-02-14
发明人： AFROZE, Roushan , BHARATHAN, Indu, T. , CIAVARRI, Jeffrey, P. , FLEMING, Paul, E. , GAULIN, Jeffrey, L. , GIRARD, Mario , LANGSTON, Steven, P. , SOUCY, Francois, R. , WONG, Tzu-Tshin , YE, Yingchun
IPC分类号： C07D487/04 , A61P35/00 , A61K31/519
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, X Y , R Y1 , R Y2 and R Y3 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.-
公开(公告)号：EP2346882A1
公开(公告)日：2011-07-27
申请号：EP09789372.1
申请日：2009-09-25
发明人： FLEMING, Paul, E. , LI, Jing
CPC分类号： C07F5/025 , C07F5/04 , C07K5/06 , C07K5/06078 , C07K5/08
摘要： The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
摘要翻译： 本发明提供了可用作蛋白酶体抑制剂的新型化合物。 本发明还提供包含本发明化合物的药物组合物和使用该组合物治疗各种疾病的方法。
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公开(公告)号：EP1735311B1
公开(公告)日：2010-03-31
申请号：EP05779267.3
申请日：2005-04-08
发明人： HEPPERLE, Michael, E. , LIU, Julie, Fields , SOUCY, Francois , PRAKASH, Raman , LITTLE, Jeremy, D. , FLEMING, Paul, E. , REYNOLDS, Dominic , HARRIMAN, Geraldine, C., B.
IPC分类号： C07D471/04 , A61K31/5377 , A61P29/00 , A61P35/00
CPC分类号： C07D471/04
摘要： This invention provides beta-carboline compounds of formula III-A-aa, wherein Q, G, R1, R2, R3, and R6b are as described in the specification. The compounds are useful for treating diseases such as inflammatory diseases and cancer.
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公开(公告)号：EP3173413B1
公开(公告)日：2019-05-01
申请号：EP16205139.5
申请日：2013-02-14
发明人： AFROZE, Roushan , BHARATHAN, Indu, T. , CIAVARRI, Jeffrey, P. , FLEMING, Paul, E. , GAULIN, Jeffrey, L. , GIRARD, Mario , LANGSTON, Steven, P. , SOUCY, Francois, R. , WONG, Tzu-Tshin , YE, Yingchun
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
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公开(公告)号：EP2552216B1
公开(公告)日：2018-01-24
申请号：EP11763354.5
申请日：2011-03-30
发明人： FLEMING, Paul, E. , LI, Jing
摘要： The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
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公开(公告)号：EP1735311A1
公开(公告)日：2006-12-27
申请号：EP05779267.3
申请日：2005-04-08
发明人： HEPPERLE, Michael, E. , LIU, Julie, Fields , SOUCY, Francois , PRAKASH, Raman , LITTLE, Jeremy, D. , FLEMING, Paul, E. , REYNOLDS, Dominic , HARRIMAN, Geraldine, C., B.
IPC分类号： C07D471/04 , A61K31/5377 , A61P29/00 , A61P35/00
CPC分类号： C07D471/04
摘要： This invention provides beta-carboline compounds of formula III-A-aa, wherein Q, G, R1, R2, R3, and R6b are as described in the specification. The compounds are useful for treating diseases such as inflammatory diseases and cancer.
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公开(公告)号：EP2346882B1
公开(公告)日：2017-09-20
申请号：EP09789372.1
申请日：2009-09-25
发明人： FLEMING, Paul, E. , LI, Jing
CPC分类号： C07F5/025 , C07F5/04 , C07K5/06 , C07K5/06078 , C07K5/08
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9.发明授权2-(AMINO-SUBSTITUTED)-4-ARYL PYRAMIDINES AND RELATED COMPOUNDS USEFUL FOR TREATING INFLAMMATORY DISEASES 有权炎症性疾病的治疗2-（氨基 - 取代的）-4- ARYLPYRAMIDINE及相关化合物适合
公开(公告)号：EP1701944B1
公开(公告)日：2009-07-29
申请号：EP05726205.7
申请日：2005-01-10
发明人： FLEMING, Paul, E. , SHI, Zhan , CHEN, Shaowu , SCHMIDT, Jane, F. , READER, John C. , HONE, Neal D. , CIAVARRI, Jefrey P.
IPC分类号： C07D239/42 , C07D401/12 , C07D405/14
CPC分类号： C07D239/42 , C07D401/10 , C07D403/10
摘要： A heterocyclic inhibitor having the formula (I), with the variables defined herein, which is useful for treating inflammatory and other physiological disorders in which PKC-theta isoform plays a role.
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10.发明公开2-(AMINO-SUBSTITUTED)-4-ARYL PYRAMIDINES AND RELATED COMPOUNDS USEFUL FOR TREATING INFLAMMATORY DISEASES 有权炎症性疾病的治疗2-（氨基 - 取代的）-4- ARYLPYRAMIDINE及相关化合物适合
公开(公告)号：EP1701944A2
公开(公告)日：2006-09-20
申请号：EP05726205.7
申请日：2005-01-10
发明人： FLEMING, Paul, E. , SHI, Zhan , CHEN, Shaowu , SCHMIDT, Jane, F. , READER, John C. , HONE, Neal D. , CIAVARRI, Jefrey P.
IPC分类号： C07D239/42 , C07D401/12 , C07D405/14
CPC分类号： C07D239/42 , C07D401/10 , C07D403/10
摘要： A heterocyclic inhibitor having the formula (I), with the variables defined herein, which is useful for treating inflammatory and other physiological disorders in which PKC-theta isoform plays a role.
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