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1.发明授权2-(amino-substituted)-4-aryl pyrimidines and related compounds useful for treating inflammatory diseases 失效2-（氨基取代的）-4-芳基嘧啶和可用于治疗炎性疾病的相关化合物公开(公告)号：US08268822B2
公开(公告)日：2012-09-18
申请号：US12767139
申请日：2010-04-26
申请人： Paul E. Fleming , Zhan Shi , Brendan Shaowu Chen , Jane F. Schmidt , John C. Reader , Neal D. Hone , Jeffrey P. Ciavarri
发明人： Paul E. Fleming , Zhan Shi , Brendan Shaowu Chen , Jane F. Schmidt , John C. Reader , Neal D. Hone , Jeffrey P. Ciavarri
IPC分类号： C07D239/42 , C07D401/12 , A61K31/506
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:
摘要翻译： 具有式I的杂环抑制剂，其具有本文定义的变量，其可用于治疗其中PKC-θ同种型起作用的炎性和其他生理障碍：
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公开(公告)号：US08664200B2
公开(公告)日：2014-03-04
申请号：US12586650
申请日：2009-09-25
申请人： Paul E. Fleming , Jing Li
发明人： Paul E. Fleming , Jing Li
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：US08569543B2
公开(公告)日：2013-10-29
申请号：US13221315
申请日：2011-08-30
IPC分类号： C07C311/15 , C07D213/02 , A61K31/18 , A61K31/44 , A61K31/50 , A61P1/00 , A61P29/00
CPC分类号： C07C311/29 , C07C311/21 , C07C311/44 , C07C311/46 , C07C317/34 , C07C323/49 , C07D213/46 , C07D213/50 , C07D213/65 , C07D213/70 , C07D213/71 , C07D213/75 , C07D213/76 , C07D213/80 , C07D213/89 , C07D237/08 , C07D239/26 , C07D239/42 , C07D333/34 , C07D333/62 , C07D401/06 , C07D405/06 , C07D409/04 , C07D409/06 , C07D413/04 , C07D413/14 , C07D513/04
摘要： The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
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公开(公告)号：US08513218B2
公开(公告)日：2013-08-20
申请号：US13075306
申请日：2011-03-30
申请人： Paul E. Fleming , Jing Li
发明人： Paul E. Fleming , Jing Li
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：US20110245203A1
公开(公告)日：2011-10-06
申请号：US13075306
申请日：2011-03-30
申请人： Paul E. Fleming , Jing Li
发明人： Paul E. Fleming , Jing Li
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：US07951801B2
公开(公告)日：2011-05-31
申请号：US11101998
申请日：2005-04-08
申请人： Michael E. Hepperle , Julie Fields Liu , Francois Soucy , Prakash Raman , Jeremy D. Little , Paul E. Fleming , Dominic Reynolds , Geraldine C. B. Harriman
发明人： Michael E. Hepperle , Julie Fields Liu , Francois Soucy , Prakash Raman , Jeremy D. Little , Paul E. Fleming , Dominic Reynolds , Geraldine C. B. Harriman
IPC分类号： A61K31/535 , C07D413/14
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.
摘要翻译： 本发明提供式III-A-aa的β-咔啉化合物：其中Q，G，R 1，R 2，R 3和R 6b如说明书中所述。 该化合物可用于治疗疾病如炎性疾病和癌症。
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公开(公告)号：US20100081633A1
公开(公告)日：2010-04-01
申请号：US12586650
申请日：2009-09-25
申请人： Paul E. Fleming , Jing Li
发明人： Paul E. Fleming , Jing Li
IPC分类号： A61K31/69 , C07F5/02 , C07D265/30 , C07F7/08
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：US20100093713A1
公开(公告)日：2010-04-15
申请号：US12640335
申请日：2009-12-17
申请人： Michael E. Hepperle , Julie Fields Liu , Francois Soucy , Yingchun Ye , Robert S. Murray , Raman Prakash , Jeremy D. Little , Alfredo Castro , Hormoz Mazdiyasni , Paul E. Fleming , Dominic Reynolds
发明人： Michael E. Hepperle , Julie Fields Liu , Francois Soucy , Yingchun Ye , Robert S. Murray , Raman Prakash , Jeremy D. Little , Alfredo Castro , Hormoz Mazdiyasni , Paul E. Fleming , Dominic Reynolds
IPC分类号： A61K31/541 , C07D471/04 , A61P35/04 , A61P37/00 , A61K31/5377 , A61P29/00 , A61K31/501 , A61K31/437 , C07D295/10
CPC分类号： C07D265/30 , C07D471/04
摘要： This invention provides beta-carboline compounds of formula wherein Ring A is a substituted pyridinyl, pyrimidinyl, morpholinyl, piperidinyl, piperazinyl, pyrrolidinyl, pyranyl, tetrahydrofuranyl, cyclohexyl, cyclopentyl or thiomorpholinyl ring and R1, R2 and R3 are as described in the specification. The compounds are IKK-2 inhibitors that are useful for treating IKK-2-mediated diseases such as inflammatory diseases and cancer.
摘要翻译： 本发明提供下式的β-咔啉化合物，其中环A是取代的吡啶基，嘧啶基，吗啉基，哌啶基，哌嗪基，吡咯烷基，吡喃基，四氢呋喃基，环己基，环戊基或硫代吗啉基，R1，R2和R3如说明书中所述。 这些化合物是可用于治疗IKK-2介导的疾病如炎性疾病和癌症的IKK-2抑制剂。
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公开(公告)号：US08030517B2
公开(公告)日：2011-10-04
申请号：US12630040
申请日：2009-12-03
IPC分类号： C07C311/15 , C07D213/02 , A61K31/18 , A61K31/44 , A61K31/50 , A61P1/00 , A61P29/00
CPC分类号： C07C311/29 , C07C311/21 , C07C311/44 , C07C311/46 , C07C317/34 , C07C323/49 , C07D213/46 , C07D213/50 , C07D213/65 , C07D213/70 , C07D213/71 , C07D213/75 , C07D213/76 , C07D213/80 , C07D213/89 , C07D237/08 , C07D239/26 , C07D239/42 , C07D333/34 , C07D333/62 , C07D401/06 , C07D405/06 , C07D409/04 , C07D409/06 , C07D413/04 , C07D413/14 , C07D513/04
摘要： The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
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公开(公告)号：US07999109B2
公开(公告)日：2011-08-16
申请号：US12640439
申请日：2009-12-17
IPC分类号： C07D213/02 , A61K31/44 , A61P1/00 , A61P29/00
CPC分类号： C07C311/29 , C07C311/21 , C07C311/44 , C07C311/46 , C07C317/34 , C07C323/49 , C07D213/46 , C07D213/50 , C07D213/65 , C07D213/70 , C07D213/71 , C07D213/75 , C07D213/76 , C07D213/80 , C07D213/89 , C07D237/08 , C07D239/26 , C07D239/42 , C07D333/34 , C07D333/62 , C07D401/06 , C07D405/06 , C07D409/04 , C07D409/06 , C07D413/04 , C07D413/14 , C07D513/04
摘要： The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
摘要翻译： 本发明涉及由结构式I表示的化合物，其可结合CCR9受体并阻断配体（例如TECK）与受体的结合。 本发明还涉及抑制CCR9的功能的方法，以及结构式I所示的使用化合物在研究，治疗，预防和诊断方法中的用途。
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