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1. 发明授权

US08759353B2 Co-crystals and pharmaceutical compositions comprising the same 失效
标题翻译：包含其的共晶体和药物组合物
公开(公告)号：US08759353B2
公开(公告)日：2014-06-24
申请号：US12528977
申请日：2008-02-27
申请人： Patrick R. Connelly , Irina Kadiyala , Kathy Stavropoulos , Yuegang Zhang , Steven C. Johnston , Govinda Rao Bhisetti , Valdas Jurkauskas , Peter Rose
发明人： Patrick R. Connelly , Irina Kadiyala , Kathy Stavropoulos , Yuegang Zhang , Steven C. Johnston , Govinda Rao Bhisetti , Valdas Jurkauskas , Peter Rose
IPC分类号： A61K31/497 , A61P31/14
CPC分类号： C07K5/0812 , C07D403/12
摘要： The invention relates to compositions and co-crystals each comprising VX-950 and a co-crystal former selected from the group consisting of 4-hydroxybenzoic acid, 4-amino salicylic acid, phenylalanine, threonline, tartaric acid, adipic acid, succinic acetate, proline, methyl 4-hydroxybenzoate, anthranilic acid, and d-Biotin. Also within the scope of this invention are methods of making and using the same.
摘要翻译：本发明涉及各自包含VX-950和选自4-羟基苯甲酸，4-氨基水杨酸，苯丙氨酸，苏氨酸，酒石酸，己二酸，琥珀酸乙酯，脯氨酸，4-羟基苯甲酸甲酯，邻氨基苯甲酸和d-生物素。在本发明的范围内也是制造和使用本发明的方法。

2. 发明授权

US5990155A Oxygenated-heterocycle containing sulfonamide inhibitors of aspartyl protease 失效
标题翻译：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
申请人： Roger D. Tung , Govinda Rao Bhisetti
发明人： Roger D. Tung , Govinda Rao Bhisetti
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。

3. 发明申请

US20110172238A1 BENZIMIDAZOLE ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS 失效
标题翻译：用于治疗或预防感染病毒的苯唑咪唑类似物
公开(公告)号：US20110172238A1
公开(公告)日：2011-07-14
申请号：US12838350
申请日：2010-07-16
申请人： James A. Henderson , John Maxwell , Louis Vaillancourt , Mark Morris , Ronald Grey, JR. , Simon Giroux , Laval Chan Chun Kong , Sanjoy Kumar Das , Bingcan Liu , Carl Poisson , Caroline Cadilhac , Monica Bubenik , T. Jagadeeswar Reddy , Guy Falardeau , Constantin Yannopoulos , Jian Wang , Oswy Z. Pereira , Youssef L. Bennani , Albert C. Pierce , Govinda Rao Bhisetti , Kevin M. Cottrell , Valerie Marone
发明人： James A. Henderson , John Maxwell , Louis Vaillancourt , Mark Morris , Ronald Grey, JR. , Simon Giroux , Laval Chan Chun Kong , Sanjoy Kumar Das , Bingcan Liu , Carl Poisson , Caroline Cadilhac , Monica Bubenik , T. Jagadeeswar Reddy , Guy Falardeau , Constantin Yannopoulos , Jian Wang , Oswy Z. Pereira , Youssef L. Bennani , Albert C. Pierce , Govinda Rao Bhisetti , Kevin M. Cottrell , Valerie Marone
IPC分类号： A61K31/496 , C07D403/14 , A61K31/4184 , C07D401/14 , A61K31/4545 , A61K31/506 , A61K31/4439 , A61P31/14
CPC分类号： C07K5/06052 , C07D401/14 , C07D403/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D495/04
摘要： Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B′, X, Y, R1, R1′, R2, R2′, R3, R3′, R5, R5′, R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.
摘要翻译：其中A，B，B'，X，Y，R1，R1'，R2，R2'，R3，R3'，R5，R5'，R6，m， n或p如本文所定义，可用于治疗黄病毒科病毒感染。

4. 发明授权

US06608067B1 Inhibitors of serine proteases, particularly HCV NS3 protease 失效
标题翻译：丝氨酸蛋白酶抑制剂，特别是HCV NS3蛋白酶
公开(公告)号：US06608067B1
公开(公告)日：2003-08-19
申请号：US09677382
申请日：2000-09-29
申请人： Roger D. Tung , Govinda Rao Bhisetti , Luc J. Farmer
发明人： Roger D. Tung , Govinda Rao Bhisetti , Luc J. Farmer
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。

5. 发明授权

US06392046B1 Sulfonamide inhibitors of aspartyl protease 有权
标题翻译：天冬氨酰蛋白酶的磺酰胺抑制剂
公开(公告)号：US06392046B1
公开(公告)日：2002-05-21
申请号：US09409808
申请日：1999-09-30
申请人： Roger D. Tung , Mark A. Murcko , Govinda Rao Bhisetti
发明人： Roger D. Tung , Mark A. Murcko , Govinda Rao Bhisetti
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。

6. 发明授权

US5691372A Oxygenated-Heterocycle containing sulfonamide inhibitors of aspartyl protease 失效
标题翻译：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
申请人： Roger D. Tung , Govinda Rao Bhisetti
发明人： Roger D. Tung , Govinda Rao Bhisetti
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。

7. 发明授权

US08354419B2 Benzimidazole analogues for the treatment or prevention of flavivirus infections 失效
标题翻译：苯并咪唑类似物用于治疗或预防黄病毒感染
公开(公告)号：US08354419B2
公开(公告)日：2013-01-15
申请号：US12838350
申请日：2010-07-16
申请人： James A. Henderson , John Maxwell , Louis Vaillancourt , Mark Morris , Ronald Grey, Jr. , Simon Giroux , Laval Chan Chun Kong , Sanjoy Kumar Das , Bingcan Liu , Carl Poisson , Caroline Cadilhac , Monica Bubenik , T. Jagadeeswar Reddy , Guy Falardeau , Constantin Yannopoulos , Jian Wang , Oswy Z. Pereira , Youssef L. Bennani , Albert C. Pierce , Govinda Rao Bhisetti , Kevin M. Cottrell , Valerie Marone
发明人： James A. Henderson , John Maxwell , Louis Vaillancourt , Mark Morris , Ronald Grey, Jr. , Simon Giroux , Laval Chan Chun Kong , Sanjoy Kumar Das , Bingcan Liu , Carl Poisson , Caroline Cadilhac , Monica Bubenik , T. Jagadeeswar Reddy , Guy Falardeau , Constantin Yannopoulos , Jian Wang , Oswy Z. Pereira , Youssef L. Bennani , Albert C. Pierce , Govinda Rao Bhisetti , Kevin M. Cottrell , Valerie Marone
IPC分类号： A61K31/506 , A61K31/4439 , A61K31/4184 , C07D403/14 , C07D401/14
CPC分类号： C07K5/06052 , C07D401/14 , C07D403/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D495/04
摘要： Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B′, X, Y, R1, R1′, R2, R2′, R3, R3′, R5, R5′, R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.
摘要翻译：由式I表示的化合物或其药学上可接受的盐和溶剂化物，其中A，B，B'，X，Y，R1，R1'，R2，R2'，R3，R3'，R5，R5'，R6， n或p如本文所定义，可用于治疗黄病毒科病毒感染。

8. 发明申请

US20120014914A1 INHIBITORS OF SERINE PROTEASES, PARTICULARLY HCV NS3-NS4A PROTEASES 失效
标题翻译：丝氨酸蛋白酶抑制剂，特别是HCV NS3-NS4A蛋白
公开(公告)号：US20120014914A1
公开(公告)日：2012-01-19
申请号：US13238386
申请日：2011-09-21
申请人： Luc J. Farmer , Robert B. Perni , Govinda Rao Bhisetti , Keith P. Wilson
发明人： Luc J. Farmer , Robert B. Perni , Govinda Rao Bhisetti , Keith P. Wilson
IPC分类号： A61K38/21 , C07D413/14 , C07D277/24 , C07D403/12 , A61P31/14 , A61K31/7056 , A61K31/427 , A61K31/497 , A61K31/5377 , A61K31/4178 , C07D401/12 , A61K38/22
CPC分类号： C07D403/12 , A61K38/00 , C07D417/12 , C07K5/0804 , C07K5/0808 , C07K5/0812
摘要： The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt, or mixtures thereof, that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are useful as antiviral agents. The invention further relates to pharmaceutically acceptable compositions comprising said compounds either for ex vivo use or for administration to a patient suffering from HCV infection and processes for preparing the compounds. The invention also relates to methods of treating an HCV infection in a patient by administering a pharmaceutical composition comprising a compound of this invention.
摘要翻译：本发明涉及抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒NS3-NS4A蛋白酶活性的式I化合物或其药学上可接受的盐或其混合物。因此，它们通过干扰丙型肝炎病毒的生命周期起作用，并且作为抗病毒剂是有用的。本发明还涉及包含用于离体使用或用于给予HCV感染的患者的所述化合物的药学上可接受的组合物和用于制备所述化合物的方法。本发明还涉及通过施用包含本发明化合物的药物组合物来治疗患者HCV感染的方法。

9. 发明授权

US07494988B2 Inhibitors of serine proteases, particularly hepatitis C virus NS3 protease 失效
标题翻译：丝氨酸蛋白酶抑制剂，特别是丙型肝炎病毒NS3蛋白酶
公开(公告)号：US07494988B2
公开(公告)日：2009-02-24
申请号：US10391932
申请日：2003-03-19
申请人： Robert Perni , John Court , Ethan O'Malley , Govinda Rao Bhisetti
发明人： Robert Perni , John Court , Ethan O'Malley , Govinda Rao Bhisetti
IPC分类号： A61K31/396 , A61K31/397 , C07D205/04 , C07D203/08
CPC分类号： C07K7/06 , A61K38/00 , C07K5/101
摘要： The present invention relates to compounds that are useful as protease inhibitors, particularly as serine protease inhibitors, and more particularly as hepatitis C NS3 protease inhibitors. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HCV NS3 protease activity and consequently, may be advantageously used as therapeutic agents against the hepatitis C virus and other viruses that are dependent upon a serine protease for proliferation. This invention also relates to methods for inhibiting the activity of proteases, including hepatitis C virus NS3 protease and other serine proteases, using the compounds of this invention and related compounds.
摘要翻译：本发明涉及可用作蛋白酶抑制剂的化合物，特别是作为丝氨酸蛋白酶抑制剂，特别是作为丙型肝炎NS3蛋白酶抑制剂。因此，它们通过干扰丙型肝炎病毒的生命周期起作用，也可用作抗病毒剂。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HCV NS3蛋白酶活性，因此可有利地用作针对依赖于丝氨酸蛋白酶增殖的丙型肝炎病毒和其它病毒的治疗剂。本发明还涉及使用本发明化合物和相关化合物来抑制蛋白酶（包括丙型肝炎病毒NS3蛋白酶和其它丝氨酸蛋白酶）的活性的方法。

10. 发明申请

US20080293727A1 Novel sulfonamide inhibitors of aspartyl protease 审中-公开
标题翻译：新型磺酰胺抑制剂天冬氨酰蛋白酶
公开(公告)号：US20080293727A1
公开(公告)日：2008-11-27
申请号：US12001993
申请日：2007-12-12
申请人： Roger D. Tung , Mark A. Murcko , Govinda Rao Bhisetti
发明人： Roger D. Tung , Mark A. Murcko , Govinda Rao Bhisetti
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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