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1. 发明授权

US08809313B2 Substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes useful for treating HCV infections 有权
标题翻译：用于治疗HCV感染的取代的aliphanes，cyclophanes，heteraphanes，heterophanes，异质异烟肼和金属茂
公开(公告)号：US08809313B2
公开(公告)日：2014-08-19
申请号：US13482558
申请日：2012-05-29
申请人： Jason Allan Wiles , Qiuping Wang , Akihiro Hashimoto , Godwin Pais , Xiangzhu Wang , Venkat Gadhachanda , Avinash Phadke , Milind Deshpande , Dawei Chen
发明人： Jason Allan Wiles , Qiuping Wang , Akihiro Hashimoto , Godwin Pais , Xiangzhu Wang , Venkat Gadhachanda , Avinash Phadke , Milind Deshpande , Dawei Chen
IPC分类号： A61P31/14 , C07D471/08 , A61K31/439 , A61K31/496 , C07D403/14 , A61K31/555
CPC分类号： A61K31/4184 , A61K9/0053 , A61K9/20 , A61K31/4178 , A61K31/422 , A61K31/427 , A61K31/439 , A61K31/454 , A61K31/496 , A61K31/555 , A61K45/06 , A61K2300/00 , C07D209/42 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/14 , C07D417/14 , C07D453/06 , C07D471/08 , C07D491/10 , C07D491/113 , C07D519/00 , C07F5/025 , C07F15/02 , C07F17/02
摘要： The present disclosure provides substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes, of Formula I D-M-D (Formula I) useful as antiviral agents. In certain embodiments disclosed herein M is a group —P-A-P— where A is Certain substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions/and combinations containing one or more substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes and a pharmaceutically acceptable carrier are also provided by this disclosure. Methods for treating viral infections, including Hepatitis C viral infections are provided by the disclosure.
摘要翻译：本公开提供了可用作抗病毒剂的式I D-M-D（式I）的取代的阿片，环戊烷，异烟肼，杂异烟肼，杂异烟草和金属茂。在本文公开的某些实施方案中，M是基团-P-A-P-，其中A是本文公开的某些取代的阿氨苯酯，环戊烷，异烟肼，杂异烟肼，杂异烟草和金属茂是有效和/或选择性的病毒复制抑制剂，特别是丙型肝炎病毒复制。本公开内容还提供药物组合物和/或含有一种或多种取代的阿利膦，环戊二烯，异aph烷，异han嗪，杂异烟草和金属茂的药物组合物和药学上可接受的载体。通过本公开提供了治疗病毒感染的方法，包括丙型肝炎病毒感染。

2. 发明授权

US08614180B2 4-amino-4-oxobutanoyl peptides as inhibitors of viral replication 有权
公开(公告)号：US08614180B2
公开(公告)日：2013-12-24
申请号：US12635270
申请日：2009-12-10
申请人： Avinash Phadke , Dawei Chen , Venkat Gadhachanda , Akihiro Hashimoto , Godwin Pais , Xiangzhu Wang , Atul Agarwal , Ha Young Kim , Shouming Li , Cuixian Liu , Suoming Zhang , Milind Deshpande
发明人： Avinash Phadke , Dawei Chen , Venkat Gadhachanda , Akihiro Hashimoto , Godwin Pais , Xiangzhu Wang , Atul Agarwal , Ha Young Kim , Shouming Li , Cuixian Liu , Suoming Zhang , Milind Deshpande
IPC分类号： A01N37/18
CPC分类号： C07D207/16 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/08 , C07D487/08 , C07D487/18 , C07D491/113
摘要： The invention provides 4-amino-4-oxobutanoyl peptides of Formula I and the pharmaceutically salts and hydrates thereof. The variables R, R1, R6-R8, R16, R18, R19, M, n, T, Y, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. The 4-amino-4-oxobutanoyl peptides disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptides and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a 4-amino-4-oxobutanoyl peptides as the only active agent or may contain a combination of a 4-amino-4-oxobutanoyl peptides and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections.

3. 发明授权

US08138346B2 Method for synthesis of 8-alkoxy-9H-isothiazolo[5,4-B]quinoline-3,4-diones 有权
标题翻译： 8-烷氧基-9H-异噻唑并[5,4-B]喹啉-3,4-二酮的合成方法
公开(公告)号：US08138346B2
公开(公告)日：2012-03-20
申请号：US13040369
申请日：2011-03-04
申请人： Barton James Bradbury , Jason Allan Wiles , Akihiro Hashimoto , Qiuping Wang , Edlaine Lucien , Godwin Pais , Ha Young Kim
发明人： Barton James Bradbury , Jason Allan Wiles , Akihiro Hashimoto , Qiuping Wang , Edlaine Lucien , Godwin Pais , Ha Young Kim
IPC分类号： C07D215/38
CPC分类号： C07D215/28 , C07D401/04 , C07D513/04
摘要： The present invention provides process for synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones of the Formula A. The substituents R, R5, R6, R7, R8 and R9 are defined herein. The invention also provides novel synthetic intermediates useful in the synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones.
摘要翻译：本发明提供8-甲氧基-9H-异噻唑并[5,4-b]喹啉-3,4-二酮和8A,9-二氢-4a-异噻唑并[5,4-b]喹啉-3的合成方法，取代基R，R 5，R 6，R 7，R 8和R 9在本文中定义。本发明还提供了用于合成8-甲氧基-9H-异噻唑并[5,4-b]喹啉-3,4-二酮和8A,9-二氢-4a-异噻唑并[5,4-b] 喹啉-3,4-二酮。

4. 发明授权

US07902365B2 Method for synthesis of 8-alkoxy-9H-isothiazolo[5,4-B]quinoline-3,4-diones 有权
标题翻译： 8-烷氧基-9H-异噻唑并[5,4-B]喹啉-3,4-二酮的合成方法
公开(公告)号：US07902365B2
公开(公告)日：2011-03-08
申请号：US11840006
申请日：2007-08-16
申请人： Barton James Bradbury , Jason Allan Wiles , Akihiro Hashimoto , Qiuping Wang , Edlaine Lucien , Godwin Pais , Ha Young Kim
发明人： Barton James Bradbury , Jason Allan Wiles , Akihiro Hashimoto , Qiuping Wang , Edlaine Lucien , Godwin Pais , Ha Young Kim
IPC分类号： C07D215/38
CPC分类号： C07D215/28 , C07D401/04 , C07D513/04
摘要： The present invention provides process for synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones of the Formula A. The substituents R, R5, R6, R7, R8 and R9 are defined herein. The invention also provides novel synthetic intermediates useful in the synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones.
摘要翻译：本发明提供8-甲氧基-9H-异噻唑并[5,4-b]喹啉-3,4-二酮和8A,9-二氢-4a-异噻唑并[5,4-b]喹啉-3的合成方法，取代基R，R 5，R 6，R 7，R 8和R 9在本文中定义。本发明还提供了用于合成8-甲氧基-9H-异噻唑并[5,4-b]喹啉-3,4-二酮和8A,9-二氢-4a-异噻唑并[5,4-b] 喹啉-3,4-二酮。

5. 发明申请

US20100216725A1 4-AMINO-4-OXOBUTANOYL PEPTIDES AS INHIBITORS OF VIRAL REPLICATION 有权
标题翻译：作为病毒复制抑制剂的4-氨基-4-氧代哌啶
公开(公告)号：US20100216725A1
公开(公告)日：2010-08-26
申请号：US12635270
申请日：2009-12-10
申请人： Avinash Phadke , Dawei Chen , Venkat Gadhachanda , Akihiro Hashimoto , Godwin Pais , Xiangzhu Wang , Atul Agarwal , Ha Young Kim , Shuoming Li , Cuixian Liu , Suoming Zhang , Milind Deshpande
发明人： Avinash Phadke , Dawei Chen , Venkat Gadhachanda , Akihiro Hashimoto , Godwin Pais , Xiangzhu Wang , Atul Agarwal , Ha Young Kim , Shuoming Li , Cuixian Liu , Suoming Zhang , Milind Deshpande
IPC分类号： A61K38/06 , C07K5/00 , A61P31/12
CPC分类号： C07D207/16 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/08 , C07D487/08 , C07D487/18 , C07D491/113
摘要： The invention provides 4-amino-4-oxobutanoyl peptides of Formula I and the pharmaceutically salts and hydrates thereof. The variables R, R1, R6-R8, R16, R18, R19, M, n, T, Y, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. The 4-amino-4-oxobutanoyl peptides disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptides and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a 4-amino-4-oxobutanoyl peptides as the only active agent or may contain a combination of a 4-amino-4-oxobutanoyl peptides and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections.
摘要翻译：本发明提供式I的4-氨基-4-氧代丁酰基肽及其药学上可接受的盐和水合物。变量R，R1，R6-R8，R16，R18，R19，M，n，T，Y和Z在本文中定义。某些式I化合物可用作抗病毒剂。本文公开的4-氨基-4-氧代丁酰基肽是有效和/或选择性的病毒复制抑制剂，特别是丙型肝炎病毒复制。本发明还提供含有一种或多种4-氨基-4-氧代丁酰基肽和一种或多种药学上可接受的载体的药物组合物。这样的药物组合物可以含有4-氨基-4-氧代丁酰基肽作为唯一的活性剂，或者可以含有4-氨基-4-氧代丁酰基肽和一种或多种其它药物活性剂的组合。本发明还提供了治疗病毒感染的方法，包括丙型肝炎感染。

6. 发明申请

US20090012071A1 4-SUBSTITUTED-1H-ISOTHIAZOLO[5,4-B][1,4]OXAZINO[2,3,4-IJ]QUINOLINE-7,8(2H,9H)-DIONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS 审中-公开
标题翻译： 4-取代的1H-异亮氨酸[5,4-B] [1,4]氧杂嗪[2,3,4-I]喹啉-7,8（2H，9H） - 和相关化合物作为抗感染剂
公开(公告)号：US20090012071A1
公开(公告)日：2009-01-08
申请号：US12108106
申请日：2008-04-23
申请人： Barton James Bradbury , Milind Deshpande , Akihiro Hashimoto , Ha Young Kim , Edlaine Lucien , Godwin Pais , Michael John Pucci , Qiuping Wang , Jason Allan Wiles
发明人： Barton James Bradbury , Milind Deshpande , Akihiro Hashimoto , Ha Young Kim , Edlaine Lucien , Godwin Pais , Michael John Pucci , Qiuping Wang , Jason Allan Wiles
IPC分类号： A61K31/5383 , C07D498/06 , A61P33/02 , A61P31/04
CPC分类号： C07D513/16
摘要： The present invention provides compounds of the formula that possess antimicrobial activity. Certain compounds provided herein possess potent antibacterial, antiprotozoal, or antifungal activity. Particular compounds provided herein are also potent and/or selective inhibitors of microbial DNA synthesis and reproduction. The invention provides anti-microbial compositions, including pharmaceutical compositions, containing a compound of the invention and one or more or more carriers. The invention provides pharmaceutical compositions containing a 4-substituted-1H-isothiazolo[5,4-b][1,4]oxazino[2,3,4-ij]quinoline-7,8(2H,9H)-dione or related compound as the only active agent or in combination with one or more other active agents. The invention provides methods for treating or preventing microbial infections, preferably animals, by administering an effective amount of a 4-substituted-1H-isothiazolo[5,4-b][1,4]oxazino[2,3,4-ij]quinoline-7,8(2H,9H)-dione or related compound to an organism suffering from or susceptible to microbial infection. The invention also provides methods of inhibiting microbial growth and survival by applying an effective amount of a 4-substituted-1H-isothiazolo[5,4-b][1,4]oxazino[2,3,4-ij]quinoline-7,8(2H,9H)-dione or related compound.
摘要翻译：本发明提供具有抗微生物活性的具有下式的化合物。本文提供的某些化合物具有有效的抗细菌，抗原生动物或抗真菌活性。本文提供的具体化合物也是微生物DNA合成和繁殖的有效和/或选择性抑制剂。本发明提供包含本发明化合物和一种或多种或多种载体的抗微生物组合物，包括药物组合物。本发明提供含有4-取代-1H-异噻唑并[5,4-b] [1,4]恶嗪并[2,3,4-ij]喹啉-7,8（2H，9H） - 二酮或相关化合物作为唯一的活性剂或与一种或多种其它活性剂组合。本发明通过施用有效量的4-取代的1H-异噻唑并[5,4-b] [1,4]恶嗪并[2,3,4-ij]，提供了治疗或预防微生物感染，优选动物的方法。喹啉-7,8（2H，9H） - 二酮或相关化合物与患有或易感微生物感染的生物体接触。本发明还提供了通过应用有效量的4-取代的1H-异噻唑并[5,4-b] [1,4]恶嗪并[2,3,4-ij]喹啉-7 ，8（2H，9H） - 二酮或相关化合物。

7. 发明授权

US08697641B2 4-amino-4-oxobutanoyl peptide cyclic analogues, inhibitors of viral replication 有权
公开(公告)号：US08697641B2
公开(公告)日：2014-04-15
申请号：US12635049
申请日：2009-12-10
申请人： Avinash Phadke , Xiangzhu Wang , Godwin Pais , Akihiro Hashimoto , Venkat Gadhachanda , Dawei Chen , Atul Agarwal , Suoming Zhang , Cuixian Liu , Shouming Li , Milind Deshpande
发明人： Avinash Phadke , Xiangzhu Wang , Godwin Pais , Akihiro Hashimoto , Venkat Gadhachanda , Dawei Chen , Atul Agarwal , Suoming Zhang , Cuixian Liu , Shouming Li , Milind Deshpande
IPC分类号： A01N37/18
摘要： The invention provides 4-amino-4-oxobutanoyl peptides and cyclic analogues thereof of Formula I and the pharmaceutically salts thereof. The variables are defined herein. Certain compounds of Formula I are useful as antiviral agents. 4-amino-4-oxobutanoyl peptide cyclic analogues as disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptide cyclic analogues and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a 4-amino-4-oxobutanoyl peptide cyclic analogue as the only active agent or may contain a combination of a 4-amino-4-oxobutanoyl peptide cyclic analogue and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections, in patients.

8. 发明授权

US08114888B2 Isothiazoloquinolones and related compounds as anti-infective agents 失效
标题翻译：异噻唑并喹啉酮和相关化合物作为抗感染剂
公开(公告)号：US08114888B2
公开(公告)日：2012-02-14
申请号：US11354521
申请日：2006-02-15
申请人： Barton James Bradbury , Godwin Pais , Qiuping Wang , Milind Deshpande , Michael Pucci , Yongsheng Song , Edlaine Lucien , Jason Allan Wiles , Akihiro Hashimoto
发明人： Barton James Bradbury , Godwin Pais , Qiuping Wang , Milind Deshpande , Michael Pucci , Yongsheng Song , Edlaine Lucien , Jason Allan Wiles , Akihiro Hashimoto
IPC分类号： A61K31/4365 , A61K31/4375 , C07D491/14
CPC分类号： C07D513/04 , C07D513/14
摘要： The invention provides certain compounds and salts of Formula I and Formula II: which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A1, R2, R3, R5, R6, R7, A8 and R9 are defined herein.
摘要翻译：本发明提供某些具有抗微生物活性的式I和式II化合物和盐。本发明还提供了可用于制备式I和式II化合物的新型合成中间体。变量A1，R2，R3，R5，R6，R7，A8和R9在本文中定义。

9. 发明申请

US20100152103A1 4-AMINO-4-OXOBUTANOYL PEPTIDE CYCLIC ANALOGUES, INHIBITORS OF VIRAL REPLICATION 审中-公开
标题翻译： 4-氨基-4-氧杂多酚类环状类似物，病毒复制抑制剂
公开(公告)号：US20100152103A1
公开(公告)日：2010-06-17
申请号：US12635049
申请日：2009-12-10
申请人： Avinash Phadke , Xiangzhu Wang , Godwin Pais , Akihiro Hashimoto , Venkat Gadhachanda , Dawei Chen , Atul Agarwal , Suoming Zhang , Cuixian Liu , Shouming Li , Milind Deshpande
发明人： Avinash Phadke , Xiangzhu Wang , Godwin Pais , Akihiro Hashimoto , Venkat Gadhachanda , Dawei Chen , Atul Agarwal , Suoming Zhang , Cuixian Liu , Shouming Li , Milind Deshpande
IPC分类号： A61K38/12 , C07K5/12 , A61P31/12
CPC分类号： C07K5/12 , A61K38/00 , C07K5/06165
摘要： The invention provides 4-amino-4-oxobutanoyl peptides and cyclic analogues thereof of Formula I and the pharmaceutically salts thereof.The variables are defined herein. Certain compounds of Formula I are useful as antiviral agents. 4-amino-4-oxobutanoyl peptide cyclic analogues as disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptide cyclic analogues and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a 4-amino-4-oxobutanoyl peptide cyclic analogue as the only active agent or may contain a combination of a 4-amino-4-oxobutanoyl peptide cyclic analogue and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections, in patients.
摘要翻译：本发明提供了式I的4-氨基-4-氧代丁酰基肽及其环状类似物及其药学上可接受的盐。变量在此定义。某些式I化合物可用作抗病毒剂。本文公开的4-氨基-4-氧代丁酰基肽环类似物是病毒复制，特别是丙型肝炎病毒复制的有效和/或选择性抑制剂。本发明还提供含有一种或多种4-氨基-4-氧代丁酰基肽环状类似物和一种或多种药学上可接受的载体的药物组合物。这样的药物组合物可以含有4-氨基-4-氧代丁酰基肽环类似物作为唯一的活性剂，或者可以含有4-氨基-4-氧代丁酰基肽环类似物和一种或多种其它药物活性剂的组合。本发明还提供了用于治疗患者中的病毒感染（包括丙型肝炎感染）的方法。

10. 发明申请

US20140113890A1 NEW 4-AMINO-4-OXOBUTANOYL PEPTIDES AS INHIBITORS OF VIRAL REPLICATION 有权
标题翻译：作为病毒复制的新型4-氨基-4-氧代戊酸酯
公开(公告)号：US20140113890A1
公开(公告)日：2014-04-24
申请号：US14139196
申请日：2013-12-23
申请人： Avinash Phadke , Dawei Chen , Venkat Gadhachanda , Akihiro Hashimoto , Godwin Pais , Xiangzhu Wang , Atul Agarwal , Ha Young Kim , Shuoming Li , Cuixian Liu , Suoming Zhang , Milind Deshpande
发明人： Avinash Phadke , Dawei Chen , Venkat Gadhachanda , Akihiro Hashimoto , Godwin Pais , Xiangzhu Wang , Atul Agarwal , Ha Young Kim , Shuoming Li , Cuixian Liu , Suoming Zhang , Milind Deshpande
IPC分类号： C07D207/16 , C07D401/14 , C07D413/14 , C07D417/12 , C07D409/14 , C07D491/113 , C07D487/18 , C07D417/14 , C07D401/12 , C07D403/12
CPC分类号： C07D207/16 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/08 , C07D487/08 , C07D487/18 , C07D491/113
摘要： The invention provides 4-amino-4-oxobutanoyl peptides of Formula I and the pharmaceutically salts and hydrates thereof. The variables R, R1, R6-R8, R16, R18, R19, M, n, T, Y, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. The 4-amino-4-oxobutanoyl peptides disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptides and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a 4-amino-4-oxobutanoyl peptides as the only active agent or may contain a combination of a 4-amino-4-oxobutanoyl peptides and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections.
摘要翻译：本发明提供式I的4-氨基-4-氧代丁酰基肽及其药学上可接受的盐和水合物。变量R，R1，R6-R8，R16，R18，R19，M，n，T，Y和Z在本文中定义。某些式I化合物可用作抗病毒剂。本文公开的4-氨基-4-氧代丁酰基肽是有效和/或选择性的病毒复制抑制剂，特别是丙型肝炎病毒复制。本发明还提供含有一种或多种4-氨基-4-氧代丁酰基肽和一种或多种药学上可接受的载体的药物组合物。这样的药物组合物可以含有4-氨基-4-氧代丁酰基肽作为唯一的活性剂，或者可以含有4-氨基-4-氧代丁酰基肽和一种或多种其它药物活性剂的组合。本发明还提供了治疗病毒感染的方法，包括丙型肝炎感染。

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