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公开(公告)号：US07456190B2
公开(公告)日：2008-11-25
申请号：US10798766
申请日：2004-03-11
IPC分类号： A61K31/506 , A61K31/4439 , A61K31/401 , C07D403/04 , C07D401/14 , C07D207/34
CPC分类号： C07D405/04 , C07D207/34 , C07D403/04
摘要： The present invention relates to compounds useful of 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： 本发明涉及可用于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。
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公开(公告)号：US07407962B2
公开(公告)日：2008-08-05
申请号：US10771165
申请日：2004-02-03
申请人： Alex Aronov , Michael R. Hale , Francois Maltais , Qing Tang
发明人： Alex Aronov , Michael R. Hale , Francois Maltais , Qing Tang
IPC分类号： C07D487/04 , C07D403/04 , A61K31/4025 , A61K31/517 , A61K31/519 , A61P9/10 , A61P11/06 , A61P25/28 , A61P35/00 , A61K31/506 , A61K31/53
CPC分类号： C07D487/04 , C07D401/14 , C07D403/04
摘要： The present invention provides compounds that are inhibitors of protein kinase, particularly inhibitors of ERK2, GSK3, PKA, CDK2 protein kinases, mammalian protein kinases involved in proliferative and neurodegenerative disorders. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of utilizing those compositions in the treatment of various disorders.
摘要翻译： 本发明提供了作为蛋白激酶抑制剂的化合物，特别是ERK2，GSK3，PKA，CDK2蛋白激酶的抑制剂，参与增殖性和神经变性疾病的哺乳动物蛋白激酶。 本发明还提供包含本发明化合物的药物组合物和利用这些组合物治疗各种疾病的方法。
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公开(公告)号：US07304071B2
公开(公告)日：2007-12-04
申请号：US10639784
申请日：2003-08-12
申请人： John Cochran , Jeremy Green , Michael R. Hale , Brian Ledford , Francois Maltais , Suganthini Nanthakumar
发明人： John Cochran , Jeremy Green , Michael R. Hale , Brian Ledford , Francois Maltais , Suganthini Nanthakumar
IPC分类号： C07D239/42 , A61K31/505
CPC分类号： C07D213/74 , C07D239/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： Described herein are compounds that are useful as protein kinase inhibitors having the formulae I and V: or a pharmaceutically acceptable salt thereof, wherein Ring B, Z1, Z2, U, T, m, n, p, Q, Q′, R1, R2, Rx, R3, and R6 are as defined herein. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including stroke, inflammatory disorders, autoimmune diseases such as SLE lupus and psoriasis, proliferative disorders such as cancer, and conditions associated with organ transplantation.
摘要翻译： 本文描述了可用作具有式I和V的蛋白激酶抑制剂的化合物：
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公开(公告)号：US06962936B2
公开(公告)日：2005-11-08
申请号：US10134122
申请日：2002-04-26
申请人： Michael R. Hale , Francois Maltais
发明人： Michael R. Hale , Francois Maltais
IPC分类号： A61K31/4192 , A61K31/4196 , A61K31/428 , A61K31/4439 , A61K31/506 , A61K31/5377 , A61K45/00 , A61P1/16 , A61P3/10 , A61P5/00 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/00 , A61P17/06 , A61P19/08 , A61P21/00 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/04 , A61P37/06 , A61P37/08 , A61P43/00 , C07D249/06 , C07D249/08 , C07D249/10 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D417/14 , C07D521/00 , A01N43/64 , A61K31/41
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D249/06 , C07D249/10 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D417/14
摘要： Described herein are compounds that are useful as protein kinase inhibitors having the formula: where Ht, R2, T, and m are as described in the specification. The compounds are useful for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.
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公开(公告)号：US20090042973A1
公开(公告)日：2009-02-12
申请号：US12217517
申请日：2008-07-02
申请人： Michael R. Hale , Christopher T. Baker , Timothy A. Stammers , Ronald George Sherrill , Andrew Spaltenstein , Eric Steven Furfine , Francois Maltais , Clarence Webster Andrews, III , John Franklin Miller , Vicente Samano
发明人： Michael R. Hale , Christopher T. Baker , Timothy A. Stammers , Ronald George Sherrill , Andrew Spaltenstein , Eric Steven Furfine , Francois Maltais , Clarence Webster Andrews, III , John Franklin Miller , Vicente Samano
IPC分类号： A61K31/343 , C07C255/03 , C07D307/78 , A61K31/352 , A61P31/18 , C07D319/16 , A61K31/277
CPC分类号： C07C311/19 , C07C311/29 , C07C311/42 , C07C311/46 , C07C317/18 , C07D307/20 , C07D319/06 , C07D493/04 , C07F9/6561
摘要： The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
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公开(公告)号：US07919523B2
公开(公告)日：2011-04-05
申请号：US12217517
申请日：2008-07-02
申请人： Michael R. Hale , Christopher T. Baker , Timothy A. Stammers , Ronald George Sherrill , Andrew Spaltenstein , Eric Steven Furfine , Francois Maltais , Clarence Webster Andrews, III , John Franklin Miller , Vicente Samano
发明人： Michael R. Hale , Christopher T. Baker , Timothy A. Stammers , Ronald George Sherrill , Andrew Spaltenstein , Eric Steven Furfine , Francois Maltais , Clarence Webster Andrews, III , John Franklin Miller , Vicente Samano
IPC分类号： A61K31/357 , C07D319/06
CPC分类号： C07C311/19 , C07C311/29 , C07C311/42 , C07C311/46 , C07C317/18 , C07D307/20 , C07D319/06 , C07D493/04 , C07F9/6561
摘要： The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
摘要翻译： 本发明涉及一类新型的磺酰胺，它们是天冬氨酰蛋白酶抑制剂。 在一个实施方案中，本发明涉及以特定结构和物理化学特征为特征的新型HIV天冬氨酰蛋白酶抑制剂。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于抑制HIV-1和HIV-2蛋白酶活性，因此可有利地用作针对HIV-1和HIV-2病毒的抗病毒剂。 本发明还涉及使用本发明化合物抑制HIV天冬氨酰蛋白酶活性的方法和用于筛选抗HIV活性化合物的方法。
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公开(公告)号：US07354919B2
公开(公告)日：2008-04-08
申请号：US10626356
申请日：2003-07-24
IPC分类号： A61K31/535 , A61K31/42 , A61K31/497 , A61K31/47 , A61K31/445 , C07D413/14
CPC分类号： C07D413/14 , C07D413/04 , C07D417/14
摘要： Described herein are compounds that are useful as protein kinase inhibitors, especially inhibitors of ERK, having the formula: where A, B, R1, R2, T and Ht are described in the specification. The compounds are useful for treating diseases in mammals that are alleviated by a protein, kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.
摘要翻译： 本文描述了可用作蛋白激酶抑制剂，特别是ERK抑制剂的化合物，其具有下式：其中A，B，R 1，R 2，T和Ht为 在说明书中描述。 该化合物可用于治疗由蛋白质，激酶抑制剂，特别是癌症，炎症性疾病，再狭窄和心血管疾病等疾病缓解的哺乳动物中的疾病。
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公开(公告)号：US06319946B1
公开(公告)日：2001-11-20
申请号：US09500781
申请日：2000-02-09
申请人： Michael R. Hale , Christopher T. Baker , Timothy A. Stammers , Ronald George Sherrill , Andrew Spaltenstein , Eric Steven Furfine , Francois Maltais , Clarence Webster Andrews, III , John Franklin Miller , Vicente Samano
发明人： Michael R. Hale , Christopher T. Baker , Timothy A. Stammers , Ronald George Sherrill , Andrew Spaltenstein , Eric Steven Furfine , Francois Maltais , Clarence Webster Andrews, III , John Franklin Miller , Vicente Samano
IPC分类号： A61K31357
CPC分类号： C07C311/19 , C07C311/29 , C07C311/42 , C07C311/46 , C07C317/18 , C07D307/20 , C07D319/06 , C07D493/04 , C07F9/6561
摘要： The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
摘要翻译： 本发明涉及一类新型的磺酰胺，它们是天冬氨酰蛋白酶抑制剂。 在一个实施方案中，本发明涉及以特定结构和物理化学特征为特征的新型HIV天冬氨酰蛋白酶抑制剂。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于抑制HIV-1和HIV-2蛋白酶活性，因此可有利地用作针对HIV-1和HIV-2病毒的抗病毒剂。 本发明还涉及使用本发明化合物抑制HIV天冬氨酰蛋白酶活性的方法和用于筛选抗HIV活性化合物的方法。
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公开(公告)号：US08455497B2
公开(公告)日：2013-06-04
申请号：US12370175
申请日：2009-02-12
申请人： Michael R. Hale , Roger Tung , Stephen Price , Robin David Wilkes , Wayne Carl Schairer , Ashley Nicholas Jarvis , Andrew Spaltenstein , Eric Steven Furfine , Vicente Samano , Istvan Kaldor , John Franklin Miller , Michael Stephen Brieger , Ronald George Sherrill
发明人： Michael R. Hale , Roger Tung , Stephen Price , Robin David Wilkes , Wayne Carl Schairer , Ashley Nicholas Jarvis , Andrew Spaltenstein , Eric Steven Furfine , Vicente Samano , Istvan Kaldor , John Franklin Miller , Michael Stephen Brieger , Ronald George Sherrill
IPC分类号： C07D493/04 , A61K31/34 , A61K31/357 , A61K31/36 , A61P31/18 , C07C311/16 , C07C311/29
CPC分类号： C07D493/04 , A61K31/352 , A61K31/36 , A61K45/06 , C07D317/46 , A61K2300/00
摘要： The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
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公开(公告)号：US06878728B1
公开(公告)日：2005-04-12
申请号：US09591464
申请日：2000-06-09
申请人： Michael R. Hale , Roger Tung , Stephen Price , Robin David Wilkes , Wayne Carl Schairer , Ashley Nicholas Jarvis , Andrew Spaltenstein , Eric Steven Furfine , Vicente Samano , Istvan Kaldor , John Franklin Miller , Michael Stephen Brieger
发明人： Michael R. Hale , Roger Tung , Stephen Price , Robin David Wilkes , Wayne Carl Schairer , Ashley Nicholas Jarvis , Andrew Spaltenstein , Eric Steven Furfine , Vicente Samano , Istvan Kaldor , John Franklin Miller , Michael Stephen Brieger
IPC分类号： A61K31/352 , A61K31/36 , A61K45/06 , A61K31/454 , A61K31/422 , C07D413/14 , C07D417/12
CPC分类号： C07D493/04 , A61K31/352 , A61K31/36 , A61K45/06 , C07D277/24 , C07D317/62 , C07D407/12 , A61K2300/00
摘要： The invention provides novel compounds of formula (I) wherein all variables are as defined in the specification, that are useful as inhibitors of aspartyl proteases.
摘要翻译： 本发明提供新的式（I）化合物，其中所有变量如说明书中所定义，可用作天冬氨酰蛋白酶抑制剂。
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