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61. 发明授权

US08410133B2 Aminopyridines useful as inhibitors of protein kinases 失效
标题翻译：可用作蛋白激酶抑制剂的氨基吡啶
公开(公告)号：US08410133B2
公开(公告)日：2013-04-02
申请号：US12792044
申请日：2010-06-02
申请人： Juan-Miguel Jimenez , Philip Collier , Jeremy Green , Gregory Henkel , Michael Liu , Timothy Neuberger
发明人： Juan-Miguel Jimenez , Philip Collier , Jeremy Green , Gregory Henkel , Michael Liu , Timothy Neuberger
IPC分类号： C07D513/02 , C07D515/02 , A01N43/42 , A61K31/44
CPC分类号： C07D471/04 , A61K31/437 , A61K31/4439 , A61K45/06 , C07D417/12
摘要： The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds, the methods of using the aforementioned compounds, and compounds in the treatment of various diseases, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
摘要翻译：本发明涉及可用作蛋白激酶抑制剂的化合物。本发明还提供包含那些化合物的药学上可接受的组合物，使用上述化合物的方法和化合物治疗各种疾病，病症和障碍。本发明还提供了制备本发明化合物的方法。

62. 发明申请

US20120232275A1 PROCESS FOR PREPARING 5-FLUORO-1H-PYRAZOLO [3,4-B] PYRIDIN-3-AMINE AND DERIVATIVES THEREOF 失效
标题翻译：制备5-氟-L-吡唑并[3,4-B]吡啶-3-胺及其衍生物的方法
公开(公告)号：US20120232275A1
公开(公告)日：2012-09-13
申请号：US13347926
申请日：2012-01-11
申请人： Juan-Miguel Jimenez , Philip Collier , Jeremy Green , Andrew Miller , Huai Gao , Sylvain Loic Jean-Luc Hamon , Albert Cornelis Dros
发明人： Juan-Miguel Jimenez , Philip Collier , Jeremy Green , Andrew Miller , Huai Gao , Sylvain Loic Jean-Luc Hamon , Albert Cornelis Dros
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The present invention relates to a process for the synthesis of 5-fluoro-1H-pyrazolo[3,4-b]pyridin-3-amine in high yield and purity. The present invention also relates to processes for the synthesis of 5-fluoro-1H-pyrazolo[3,4-b]pyridin-3-amine derivatives. These processes are useful for preparing biologically active compounds, particularly certain GSK-3 inhibitors, or derivatives thereof.
摘要翻译：本发明涉及以高产率和纯度合成5-氟-1H-吡唑并[3,4-b]吡啶-3-胺的方法。本发明还涉及5-氟-1H-吡唑并[3,4-b]吡啶-3-胺衍生物的合成方法。这些方法可用于制备生物活性化合物，特别是某些GSK-3抑制剂或其衍生物。

63. 发明授权

US07883881B2 Inhibitors of GSK-3 and crystal structures of GSK-3β protein and protein complexes 有权
标题翻译： GSK-3的抑制剂和GSK-3＆bgr的晶体结构; 蛋白质和蛋白质复合物
公开(公告)号：US07883881B2
公开(公告)日：2011-02-08
申请号：US12652152
申请日：2010-01-05
申请人： Ernst ter Haar , Lovorka Swenson , Jeremy Green , Michael J. Arnost
发明人： Ernst ter Haar , Lovorka Swenson , Jeremy Green , Michael J. Arnost
IPC分类号： C12N9/00 , C12N9/10 , C12N9/12 , C12P21/04 , C07K14/00 , A61K38/17 , A61K38/45
CPC分类号： C07D487/04 , C07K2299/00 , C12N9/1205 , G06F19/16
摘要： The present invention relates to inhibitors of GSK-3 and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors and methods of utilizing those compositions in the treatment and prevention of various disorders, such as diabetes and Alzheimer's disease. In addition, the invention relates to molecules or molecular complexes which comprise binding pockets of GSK-3β or its homologues. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to GSK-3β protein or homologues thereof. The invention also relates to crystallizable compositions and crystals comprising GSK-3β protein or GSK-3β protein complexes.
摘要翻译：本发明涉及GSK-3抑制剂及其制备方法。本发明还提供包含抑制剂的药物组合物和利用这些组合物治疗和预防各种疾病如糖尿病和阿尔茨海默氏病的方法。此外，本发明涉及包含GSK-3和bgr的结合口袋的分子或分子复合物。或其同系物。本发明涉及一种计算机，包括用这种结合口袋的结构坐标编码的数据存储介质。本发明还涉及使用结构坐标来解决同源蛋白质或蛋白质复合物的结构的方法。本发明涉及使用结构坐标筛选和设计结合GSK-3和bgr的化合物的方法; 蛋白质或其同系物。本发明还涉及可结晶组合物和包含GSK-3和bgr的晶体; 蛋白质或GSK-3＆bgr; 蛋白复合物。

64. 发明申请

US20110021559A1 AMINOPYRIDINES USEFUL AS INHIBITORS OF PROTEIN KINASES 失效
标题翻译：氨苄青霉素作为蛋白激酶的抑制剂有用
公开(公告)号：US20110021559A1
公开(公告)日：2011-01-27
申请号：US12792044
申请日：2010-06-02
申请人： Juan-Miguel Jimenez , Philip Collier , Jeremy Green , Gregory Henkel , Michael Liu , Timothy Neuberger
发明人： Juan-Miguel Jimenez , Philip Collier , Jeremy Green , Gregory Henkel , Michael Liu , Timothy Neuberger
IPC分类号： A61K31/444 , C07D471/04 , C07D417/12 , A61K31/454 , C12N5/071 , A61P29/00 , A61P35/00 , A61P37/02 , A61P37/06 , A61P25/00 , A61P9/00 , A61P3/10 , A61P37/04 , A61P25/28 , A61P19/10 , A61P25/16 , A61P25/18 , A61P19/02 , C12N5/0793
CPC分类号： C07D471/04 , A61K31/437 , A61K31/4439 , A61K45/06 , C07D417/12
摘要： The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
摘要翻译：本发明涉及可用作蛋白激酶抑制剂的化合物。本发明还提供包含这些化合物的药学上可接受的组合物和使用该化合物和组合物治疗各种疾病，病症和障碍的方法。本发明还提供了制备本发明化合物的方法。

65. 发明申请

US20100227814A1 INHIBITORS OF GSK-3 AND CRYSTAL STRUCTURES OF GSK-3BETA PROTEIN AND PROTEIN COMPLEXES 有权
标题翻译： GSK-3和GSK-3BETA蛋白和蛋白复合物的晶体结构的抑制剂
公开(公告)号：US20100227814A1
公开(公告)日：2010-09-09
申请号：US12652152
申请日：2010-01-05
申请人： Ernst ter Haar , Lovorka Swenson , Jeremy Green , Michael J. Arnost
发明人： Ernst ter Haar , Lovorka Swenson , Jeremy Green , Michael J. Arnost
IPC分类号： A61K38/16 , A61P37/00 , A61P25/28 , A61P25/16 , A61P11/06 , A61P3/10 , A61P9/00
CPC分类号： C07D487/04 , C07K2299/00 , C12N9/1205 , G06F19/16
摘要： The present invention relates to inhibitors of GSK-3 and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors and methods of utilizing those compositions in the treatment and prevention of various disorders, such as diabetes and Alzheimer's disease. In addition, the invention relates to molecules or molecular complexes which comprise binding pockets of GSK-3β or its homologues. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to GSK-3β protein or homologues thereof. The invention also relates to crystallizable compositions and crystals comprising GSK-3β protein or GSK-3β protein complexes.
摘要翻译：本发明涉及GSK-3抑制剂及其制备方法。本发明还提供包含抑制剂的药物组合物和利用这些组合物治疗和预防各种疾病如糖尿病和阿尔茨海默氏病的方法。此外，本发明涉及包含GSK-3和bgr的结合口袋的分子或分子复合物。或其同系物。本发明涉及一种计算机，包括用这种结合口袋的结构坐标编码的数据存储介质。本发明还涉及使用结构坐标来解决同源蛋白质或蛋白质复合物的结构的方法。本发明涉及使用结构坐标筛选和设计结合GSK-3和bgr的化合物的方法; 蛋白质或其同系物。本发明还涉及可结晶组合物和包含GSK-3和bgr的晶体; 蛋白质或GSK-3＆bgr; 蛋白复合物。

66. 发明授权

US07666647B2 Inhibitors of GSK-3 and crystal structures of GSK-3β protein and protein complexes 失效
标题翻译： GSK-3的抑制剂和GSK-3＆bgr的晶体结构; 蛋白质和蛋白质复合物
公开(公告)号：US07666647B2
公开(公告)日：2010-02-23
申请号：US12079917
申请日：2008-03-28
申请人： Ernst ter Haar , Lovorka Swenson , Jeremy Green , Michael J. Arnost
发明人： Ernst ter Haar , Lovorka Swenson , Jeremy Green , Michael J. Arnost
IPC分类号： C12N9/00 , C12N9/10 , C12N9/12 , C12P21/04 , C07K14/00 , A61K38/17 , A61K38/45
CPC分类号： C07D487/04 , C07K2299/00 , C12N9/1205 , G06F19/16
摘要： The present invention relates to inhibitors of GSK-3 and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors and methods of utilizing those compositions in the treatment and prevention of various disorders, such as diabetes and Alzheimer's disease. In addition, the invention relates to molecules or molecular complexes which comprise binding pockets of GSK-3β or its homologues. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to GSK-3β protein or homologues thereof. The invention also relates to crystallizable compositions and crystals comprising GSK-3β protein or GSK-3β protein complexes.
摘要翻译：本发明涉及GSK-3抑制剂及其制备方法。本发明还提供包含抑制剂的药物组合物和利用这些组合物治疗和预防各种疾病如糖尿病和阿尔茨海默氏病的方法。此外，本发明涉及包含GSK-3和bgr的结合口袋的分子或分子复合物。或其同系物。本发明涉及一种计算机，包括用这种结合口袋的结构坐标编码的数据存储介质。本发明还涉及使用结构坐标来解决同源蛋白质或蛋白质复合物的结构的方法。本发明涉及使用结构坐标筛选和设计结合GSK-3和bgr的化合物的方法; 蛋白质或其同系物。本发明还涉及可结晶组合物和包含GSK-3和bgr的晶体; 蛋白质或GSK-3＆bgr; 蛋白复合物。

67. 发明申请

US20090325968A1 Compositions Useful as Inhibitors of Protein Kinases 失效
标题翻译：可用作蛋白激酶抑制剂的组合物
公开(公告)号：US20090325968A1
公开(公告)日：2009-12-31
申请号：US12552003
申请日：2009-09-01
申请人： Jeremy Green , Ronald Grey, JR. , Albert Pierce
发明人： Jeremy Green , Ronald Grey, JR. , Albert Pierce
IPC分类号： A61K31/5025 , C07D487/04 , C12N9/99
CPC分类号： C07D487/04
摘要： The present invention provides a compound of formula I: or a pharmaceutically acceptable salt or mixtures thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK mammalian protein kinase, and more particularly inhibitors of GSK-3 mammalian protein kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.
摘要翻译：本发明提供式I化合物或其药学上可接受的盐或其混合物。这些化合物是蛋白激酶的抑制剂，特别是GSK哺乳动物蛋白激酶的抑制剂，特别是GSK-3哺乳动物蛋白激酶的抑制剂。本发明还提供包含本发明化合物的药学上可接受的组合物和利用这些化合物和组合物治疗各种蛋白激酶介导的病症的方法。

68. 发明授权

US07531556B2 Compositions useful as inhibitors of rock and other protein kinases 失效
标题翻译：可用作岩石和其他蛋白激酶抑制剂的组合物
公开(公告)号：US07531556B2
公开(公告)日：2009-05-12
申请号：US11115661
申请日：2005-04-27
申请人： Jeremy Green
发明人： Jeremy Green
IPC分类号： C07D403/04 , C07D413/02 , A61K31/415 , A61K31/4196 , A61K31/4245 , A61P3/10 , A61P11/06 , A61P27/06 , A61P27/14
CPC分类号： C07D401/04 , C07D413/04 , C07F9/65583
摘要： The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
摘要翻译：本发明涉及可用作蛋白激酶抑制剂的化合物。本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。

69. 发明授权

US07253187B2 Heterocyclic inhibitors of ERK2 and uses thereof 有权
标题翻译： ERK2的杂环抑制剂及其用途
公开(公告)号：US07253187B2
公开(公告)日：2007-08-07
申请号：US10770814
申请日：2004-02-03
申请人： Jingrong Cao , Jeremy Green , Michael Hale , Francois Maltais , Judy Straub , Qing Tang , Alex Aronov
发明人： Jingrong Cao , Jeremy Green , Michael Hale , Francois Maltais , Judy Straub , Qing Tang , Alex Aronov
IPC分类号： C07D401/04 , A61K31/4427
CPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D413/14
摘要： Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein Z1 and Z2 are each independently nitrogen or CH and Ring A, TmR1, QR2, UnR3, and Sp are as described in the specification. The compounds are especially useful as inhibitors of ERK2 and for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, diabetes, and cardiovascular disease.
摘要翻译：本文描述了可用作具有下式的蛋白激酶抑制剂的化合物：其中Z 1和Z 2各自独立地为氮或CH并且环A，T m 第二，第二，第二，第三，第三和第三，第二，如规范。该化合物特别可用作ERK2的抑制剂，并且用于治疗由蛋白激酶抑制剂，特别是癌症，炎性疾病，再狭窄，糖尿病和心血管疾病等疾病缓解的哺乳动物疾病。

70. 发明申请

US20070043063A1 Azaindoles useful as inhibitors of JAK and other protein kinases 有权
标题翻译：可用作JAK和其他蛋白激酶抑制剂的阿魏糖苷
公开(公告)号：US20070043063A1
公开(公告)日：2007-02-22
申请号：US11093821
申请日：2005-03-30
申请人： Francesco Salituro , Luc Farmer , Randy Bethiel , Edmund Harrington , Jeremy Green , John Court , Jon Come , David Lauffer , Alex Aronov , Hayley Binch , Dean Boyall , Jean-Damien Charrier , Simon Everitt , Damien Fraysse , Michael Mortimore , Francoise Pierard , Daniel Robinson , Jian Wang , Joanne Pinder , Tiansheng Wang
发明人： Francesco Salituro , Luc Farmer , Randy Bethiel , Edmund Harrington , Jeremy Green , John Court , Jon Come , David Lauffer , Alex Aronov , Hayley Binch , Dean Boyall , Jean-Damien Charrier , Simon Everitt , Damien Fraysse , Michael Mortimore , Francoise Pierard , Daniel Robinson , Jian Wang , Joanne Pinder , Tiansheng Wang
IPC分类号： A61K31/506 , A61K31/4745 , C07D471/02
CPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/695 , A61K45/06 , C07D519/00 , C07F7/0805
摘要： The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
摘要翻译：本发明涉及蛋白激酶抑制剂。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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