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公开(公告)号：US06392046B1
公开(公告)日：2002-05-21
申请号：US09409808
申请日：1999-09-30
IPC分类号： A61K31473
CPC分类号： C07D207/26 , A61K38/00 , C07C2601/08 , C07C2601/14 , C07D209/08 , C07D213/30 , C07D215/48 , C07D231/14 , C07D239/22 , C07D263/24 , C07D271/08 , C07D277/36 , C07D307/12 , C07D307/20 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/06139
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：US20080293727A1
公开(公告)日：2008-11-27
申请号：US12001993
申请日：2007-12-12
IPC分类号： A61K31/47 , C07D215/04 , C07C311/10 , A61K31/498 , A61P31/18 , A61K31/18 , C07D241/36
CPC分类号： C07D207/26 , A61K38/00 , C07C307/06 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/39 , C07C311/46 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D209/08 , C07D213/30 , C07D213/78 , C07D215/38 , C07D215/48 , C07D231/14 , C07D239/22 , C07D263/24 , C07D271/08 , C07D277/36 , C07D307/12 , C07D307/20 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/06139
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天冬氨酰蛋白酶的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：US5977137A
公开(公告)日：1999-11-02
申请号：US115394
申请日：1998-07-14
IPC分类号： A61K38/00 , C07D207/26 , C07D209/08 , C07D213/30 , C07D215/48 , C07D231/14 , C07D239/22 , C07D263/24 , C07D271/08 , C07D277/36 , C07D307/12 , C07D307/20 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/078 , A01N43/42 , C07D215/12 , C07D215/20 , C07D214/14
CPC分类号： C07D207/26 , C07D209/08 , C07D213/30 , C07D215/48 , C07D231/14 , C07D239/22 , C07D263/24 , C07D271/08 , C07D277/36 , C07D307/12 , C07D307/20 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/06139 , A61K38/00 , C07C2101/08 , C07C2101/14
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：US5783701A
公开(公告)日：1998-07-21
申请号：US393460
申请日：1995-02-23
IPC分类号： A61K38/00 , C07D207/26 , C07D209/08 , C07D213/30 , C07D215/48 , C07D231/14 , C07D239/22 , C07D263/24 , C07D271/08 , C07D277/36 , C07D307/12 , C07D307/20 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/078 , C07D215/12
CPC分类号： C07D207/26 , C07D209/08 , C07D213/30 , C07D215/48 , C07D231/14 , C07D239/22 , C07D263/24 , C07D271/08 , C07D277/36 , C07D307/12 , C07D307/20 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/06139 , A61K38/00 , C07C2101/08 , C07C2101/14
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：US06720335B2
公开(公告)日：2004-04-13
申请号：US10094763
申请日：2002-03-08
IPC分类号： C07D21516
CPC分类号： C07D207/26 , A61K38/00 , C07C2601/08 , C07C2601/14 , C07D209/08 , C07D213/30 , C07D215/48 , C07D231/14 , C07D239/22 , C07D263/24 , C07D271/08 , C07D277/36 , C07D307/12 , C07D307/20 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/06139
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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6.发明授权Oxygenated-heterocycle containing sulfonamide inhibitors of aspartyl protease 失效含有天冬氨酰蛋白酶磺酰胺抑制剂的含氧杂环
公开(公告)号：US5990155A
公开(公告)日：1999-11-23
申请号：US977365
申请日：1997-11-24
IPC分类号： A61K31/335 , A61K31/34 , A61K31/341 , A61K31/357 , A61P31/12 , A61P43/00 , C07D307/20 , C07D309/12 , C07D317/24 , C07D319/06 , C07D493/04 , A61K31/35 , C07D311/00
CPC分类号： C07D493/04 , C07D307/20 , C07D309/12 , C07D317/24 , C07D317/34 , C07D317/36 , C07D319/06
摘要： The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. 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.
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。 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来抑制HIV天冬氨酰蛋白酶活性的方法。
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公开(公告)号：US06608067B1
公开(公告)日：2003-08-19
申请号：US09677382
申请日：2000-09-29
IPC分类号： A61K31495
CPC分类号： C07D213/82 , C07C237/42 , C07D241/24
摘要： The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.
摘要翻译： 本发明涉及用于抑制蛋白酶，特别是丝氨酸蛋白酶，更特别是HCV NS3蛋白酶的化合物，方法和药物组合物。 化合物以及利用它们的组合物和方法可以单独使用或组合用于抑制病毒，特别是HCV病毒。
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8.发明授权Oxygenated-Heterocycle containing sulfonamide inhibitors of aspartyl protease 失效含有天冬氨酰蛋白酶磺酰胺抑制剂的含氧杂环
公开(公告)号：US5691372A
公开(公告)日：1997-11-25
申请号：US424810
申请日：1995-04-19
IPC分类号： A61K31/335 , A61K31/34 , A61K31/341 , A61K31/357 , A61P31/12 , A61P43/00 , C07D307/20 , C07D309/12 , C07D317/24 , C07D319/06 , C07D493/04 , A61K31/35
CPC分类号： C07D493/04 , C07D307/20 , C07D309/12 , C07D317/24 , C07D317/34 , C07D317/36 , C07D319/06
摘要： The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. 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.
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。 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。
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9.发明申请INHIBITORS OF SERINE PROTEASES, PARTICULARLY HEPATITIS C VIRUS NS3 PROTEASE 审中-公开丝氨酸蛋白酶抑制剂，特异性丙型肝炎病毒NS3蛋白公开(公告)号：US20110112114A1
公开(公告)日：2011-05-12
申请号：US12797250
申请日：2010-06-09
IPC分类号： A61K31/4965 , C07D241/24 , C07C237/52 , A61K31/167 , C07D213/82 , A61K31/44 , C07C231/14 , A61P31/14
CPC分类号： C07D213/82 , C07C237/42 , C07D241/24
摘要： The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.
摘要翻译： 本发明涉及用于抑制蛋白酶，特别是丝氨酸蛋白酶，更特别是HCV NS3蛋白酶的化合物，方法和药物组合物。 化合物以及利用它们的组合物和方法可以单独使用或组合用于抑制病毒，特别是HCV病毒。
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公开(公告)号：US20130012430A1
公开(公告)日：2013-01-10
申请号：US13534531
申请日：2012-06-27
申请人： Roger D. Tung , Scott L. Harbeson , David D. Deininger , Mark A. Murcko , Govinda R. Bhisetti , Luc J. Farmer
发明人： Roger D. Tung , Scott L. Harbeson , David D. Deininger , Mark A. Murcko , Govinda R. Bhisetti , Luc J. Farmer
CPC分类号： C07K7/06 , A61K38/00 , C07K5/0202 , C07K5/1024 , C07K5/1027 , C07K7/02
摘要： The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.
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