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公开(公告)号：US06617350B2
公开(公告)日：2003-09-09
申请号：US09927271
申请日：2001-08-09
申请人： Michael R. Hale , Christopher T. Baker , Timothy A. Stammers , Ronald George Sherrill , Andrew Spaltenstein , Eric Steven Furfine , François 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 , François Maltais , Clarence Webster Andrews, III , John Franklin Miller , Vicente Samano
IPC分类号： A61K3134
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：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：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：US20090274650A1
公开(公告)日：2009-11-05
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： A61K31/443 , C07D493/04 , C07D413/12 , C07D317/46 , A61K31/5377 , A61K31/357 , A61K31/34 , A61K31/52 , A61K31/522 , A61K31/496 , A61K31/427 , A61K31/472 , A61K31/513 , A61K31/708 , A61K38/21 , A61K38/20 , A61P31/12 , A61P31/18
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.
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：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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公开(公告)号：US20080103164A1
公开(公告)日：2008-05-01
申请号：US11573111
申请日：2005-07-27
申请人： Kristjan Gudmundsson , John Franklin Miller , Ronald George Sherrill , Elizabeth Madalena Turner
发明人： Kristjan Gudmundsson , John Franklin Miller , Ronald George Sherrill , Elizabeth Madalena Turner
IPC分类号： A61K31/437 , A61K31/506 , A61P31/12 , A61P31/20 , C07D471/04
CPC分类号： A61K31/437
摘要： The present invention relates to compounds that are useful in the treatment of human papillomaviruses, and also to the methods for the making and use of such compounds.
摘要翻译： 本发明涉及可用于治疗人乳头状瘤病毒的化合物，以及涉及制备和使用这些化合物的方法。
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公开(公告)号：US20080194554A1
公开(公告)日：2008-08-14
申请号：US11908305
申请日：2006-03-07
申请人： Ed W. McLean , John Franklin Miller
发明人： Ed W. McLean , John Franklin Miller
IPC分类号： A61K31/535 , A61K31/425 , A61K31/415 , A61K31/44
CPC分类号： C07D493/04
摘要： The present invention features compounds that are HIV protease inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.
摘要翻译： 本发明的特征在于是HIV蛋白酶抑制剂的化合物，因此可用于抑制HIV复制，预防和/或治疗HIV感染以及治疗AIDS和/或ARC。
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公开(公告)号：US20100280010A1
公开(公告)日：2010-11-04
申请号：US12161799
申请日：2007-01-24
IPC分类号： A61K31/551 , C07D401/04 , C07D471/04 , C07D243/08 , A61K31/497 , A61K31/437 , A61P31/18
CPC分类号： C07D471/04 , C07D519/00
摘要： The present invention provides compounds that demonstrate protective effects on target cells from HIV infection in a manner as to bind to chemokine receptor, and which affect the binding of the natural ligand or chemokine to a receptor such as CXCR4 of a target cell.
摘要翻译： 本发明提供以结合趋化因子受体的方式显示对HIV感染的靶细胞的保护作用并且影响天然配体或趋化因子与靶细胞的受体（例如CXCR4）的结合的化合物。
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