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公开(公告)号:US08653088B2
公开(公告)日:2014-02-18
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: A01N43/90 , A61K31/52 , C07D473/00
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。
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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。
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公开(公告)号:US08501446B2
公开(公告)日:2013-08-06
申请号:US13441287
申请日:2012-04-06
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 , Albert Pierce
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 , Albert Pierce
IPC分类号: C12N9/99 , 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.
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公开(公告)号:US20090176763A1
公开(公告)日:2009-07-09
申请号:US12273799
申请日:2008-11-19
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 , Albert Pierce
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 , Albert Pierce
IPC分类号: A61K31/55 , C07D401/14 , A61K31/506 , C07D243/08 , A61K31/551 , C07D403/14 , A61K31/496 , C07D471/02 , A61K31/437 , C07D413/14 , A61K31/5377 , A61P37/00 , A61P29/00 , A61P25/00 , A61P35/00
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.
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公开(公告)号:US20050228005A1
公开(公告)日:2005-10-13
申请号:US10999128
申请日:2004-11-29
申请人: Young Moon , Jeremy Green , Robert Davies , Deb Choquette , Albert Pierce , Mark Ledeboer
发明人: Young Moon , Jeremy Green , Robert Davies , Deb Choquette , Albert Pierce , Mark Ledeboer
IPC分类号: A61K31/506 , A61K31/5377 , A61K31/551 , A61K31/635 , A61L27/00 , A61P1/16 , A61P3/10 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/06 , A61P19/02 , A61P25/00 , A61P25/02 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/28 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D413/04 , C07D413/14 , C07D43/02 , C07D43/14
CPC分类号: C07D413/04 , C07D413/14
摘要: Described herein are benzisoxazole compounds of formula I: or a pharmaceutically acceptable derivative or prodrug thereof, wherein A-B is N—O or O—N; Ar is an optionally substituted C5-10 aryl group; R1 is hydrogen or an optionally substituted group selected from C1-10 aliphatic, C5-10 aryl, C6-12 aralkyl, C3-10 heterocyclyl, or C4-12 heterocyclylalkyl; and T, n, R2 and R3 are as described in the specification. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK-3 and JAK mammalian protein kinases. 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: 本文描述的是式I的苯并异恶唑化合物:或其药学上可接受的衍生物或前药,其中A-B是N-O或O-N; Ar是任选取代的C 5-10 - 芳基; R 1是氢或任选取代的选自C 1-10 - 脂族基,C 5-10 - 芳基,C 6 - 12个芳烷基,C 3-10杂环基或C 4-12 - 杂环基烷基; 和T,n,R 2和R 3如说明书中所述。 这些化合物是蛋白激酶的抑制剂,特别是GSK-3和JAK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。
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公开(公告)号:US20050222237A1
公开(公告)日:2005-10-06
申请号:US11145356
申请日:2005-06-03
申请人: Jeremy Green , Michael Arnost , Albert Pierce
发明人: Jeremy Green , Michael Arnost , Albert Pierce
IPC分类号: A61P3/10 , A61P17/06 , A61P19/02 , A61P25/18 , A61P25/28 , A61P31/18 , A61P31/22 , A61P35/00 , A61P43/00 , C07D231/20 , C07D231/46 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , A61K31/4152 , A61K31/416
CPC分类号: C07D401/12 , C07D231/20 , C07D231/46 , C07D403/12 , C07D405/12 , C07D409/12
摘要: The present invention relates to compounds of formula I that are useful as GSK-3 inhibitors. The invention also relates to methods of using compounds of formula I or pharmaceutical compositions comprising compounds of formula I to inhibit GSK-3 activity. The invention further provides methods of utilizing these compounds and pharmaceutical compositions in the treatment and prevention of various disorders, such as diabetes and Alzheimer's disease. The invention also relates to methods for inhibiting Aurora-2 activity and for treating or preventing Aurora-2-mediated diseases using compounds of formula I or pharmaceutical compositions comprising compounds of formula I. The invention also relates to methods for inhibiting cyclin-dependent kinase-2 activity and for treating or preventing inhibiting cyclin-dependent kinase-2-mediated diseases using compounds of formula I or pharmaceutical compositions comprising compounds of formula I.
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公开(公告)号:US06916798B2
公开(公告)日:2005-07-12
申请号:US10212471
申请日:2002-08-02
申请人: Jeremy Green , Michael J. Arnost , Albert Pierce
发明人: Jeremy Green , Michael J. Arnost , Albert Pierce
IPC分类号: A61P3/10 , A61P17/06 , A61P19/02 , A61P25/18 , A61P25/28 , A61P31/18 , A61P31/22 , A61P35/00 , A61P43/00 , C07D231/20 , C07D231/46 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , A61K31/4152 , A61K31/655 , C07D231/08 , C07D401/02
CPC分类号: C07D401/12 , C07D231/20 , C07D231/46 , C07D403/12 , C07D405/12 , C07D409/12
摘要: The present invention relates to compounds of formula I that are useful as GSK-3 inhibitors. The invention also relates to methods of using compounds of formula I or pharmaceutical compositions comprising compounds of formula I to inhibit GSK-3 activity. The invention further provides methods of utilizing these compounds and pharmaceutical compositions in the treatment and prevention of various disorders, such as diabetes and Alzheimer's disease. The invention also relates to methods for inhibiting Aurora-2 activity and for treating or preventing Aurora-2-mediated diseases using compounds of formula I or pharmaceutical compositions comprising compounds of formula I. The invention also relates to methods for inhibiting cyclin-dependent kinase-2 activity and for treating or preventing inhibiting cyclin-dependent kinase-2-mediated diseases using compounds of formula I or pharmaceutical compositions comprising compounds of formula I.
摘要翻译: 本发明涉及可用作GSK-3抑制剂的式I化合物。 本发明还涉及使用式I化合物或包含式I化合物的药物组合物抑制GSK-3活性的方法。 本发明还提供了利用这些化合物和药物组合物治疗和预防各种疾病如糖尿病和阿尔茨海默病的方法。 本发明还涉及使用式I化合物或包含式I化合物的药物组合物抑制Aurora-2活性和治疗或预防Aurora-2介导的疾病的方法。本发明还涉及抑制细胞周期蛋白依赖性激酶 - 2活性,以及使用式I化合物或包含式I化合物的药物组合物治疗或预防抑制细胞周期蛋白依赖性激酶-2介导的疾病。
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8.
公开(公告)号:US20120258958A1
公开(公告)日:2012-10-11
申请号:US13441287
申请日:2012-04-06
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 , Albert Pierce
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 , Albert Pierce
IPC分类号: A61K31/551 , A61K31/55 , A61P37/08 , A61P11/06 , C12N9/99 , A61P29/00 , A61P25/00 , A61P25/28 , A61P35/00 , A61K31/506 , A61P37/06
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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9.
公开(公告)号:US08188281B2
公开(公告)日:2012-05-29
申请号:US12273799
申请日:2008-11-19
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 , Albert Pierce
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 , Albert Pierce
IPC分类号: 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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10.
公开(公告)号:US07507826B2
公开(公告)日:2009-03-24
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 , Albert Pierce
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 , Albert Pierce
IPC分类号: 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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