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公开(公告)号：US06436989B1
公开(公告)日：2002-08-20
申请号：US08998050
申请日：1997-12-24
IPC分类号： A61K31665
CPC分类号： C07D405/12 , C07C311/18 , C07D307/20 , C07F9/65515 , C07F9/65844 , C07H15/04
摘要： The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.
摘要翻译： 本发明涉及作为天冬氨酰蛋白酶抑制剂的一类磺酰胺的前药。 在一个实施方案中，本发明涉及HIV天冬氨酰蛋白酶抑制剂的新一类前药，其特征在于有利的水溶性，高口服生物利用度和活性成分的体内易生成。 本发明还涉及包含这些前药的药物组合物。 本发明的前药和药物组合物特别适用于降低药丸负担并增加患者依从性。 本发明还涉及用这些前药和药物组合物治疗哺乳动物的方法。
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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：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：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：USD429190S
公开(公告)日：2000-08-08
申请号：US112892
申请日：1999-10-26
申请人： Christopher T. Baker
设计人： Christopher T. Baker
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公开(公告)号：USD430828S
公开(公告)日：2000-09-12
申请号：US116198
申请日：1999-12-28
申请人： Christopher T. Baker
设计人： Christopher T. Baker
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公开(公告)号：USD429191S
公开(公告)日：2000-08-08
申请号：US116194
申请日：1999-12-28
申请人： Christopher T. Baker
设计人： Christopher T. Baker
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公开(公告)号：USD449801S1
公开(公告)日：2001-10-30
申请号：US29126207
申请日：2000-07-11
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公开(公告)号：USD432060S
公开(公告)日：2000-10-17
申请号：US116796
申请日：2000-01-11
申请人： Christopher T. Baker
设计人： Christopher T. Baker
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