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11. 发明授权

US09125904B1 Biphenyl imidazoles and related compounds useful for treating HCV infections 有权
标题翻译：联苯咪唑和可用于治疗HCV感染的相关化合物
公开(公告)号：US09125904B1
公开(公告)日：2015-09-08
申请号：US13105504
申请日：2011-05-11
申请人： Jason Allan Wiles , Venkat Gadhachanda , Dawei Chen , Qiuping Wang , Akihiro Hashimoto , Godwin Pais , Xiangzhu Wang , Milind Deshpande , Avinash Phadke
发明人： Jason Allan Wiles , Venkat Gadhachanda , Dawei Chen , Qiuping Wang , Akihiro Hashimoto , Godwin Pais , Xiangzhu Wang , Milind Deshpande , Avinash Phadke
IPC分类号： A61K31/44 , A61K31/47 , A61K38/05 , A61K31/439 , A61K31/4709
CPC分类号： A61K31/439 , A61K31/4709 , A61K38/05 , A61K38/55 , A61K31/436 , A61K2300/00
摘要： Biphenyl imidazoles and related compounds of Formula I, useful as antiviral agents, are provided herein. Pharmaceutical compositions containing a compound of Formula I, together with a second active agent, such as an NS3a protease inhibitor are provided herein. Methods for treating viral infections, including Hepatitis C infections, are included herein by providing a compound of Formula I together with an additional active agent. In certain embodiments the additional active agent is an NS3a protease inhibitor.
摘要翻译：本文提供联苯基咪唑和可用作抗病毒剂的式I的相关化合物。本文提供了含有式I化合物的药物组合物，以及第二活性剂，例如NS3a蛋白酶抑制剂。本文通过提供式I化合物与另外的活性剂一起包括治疗病毒感染（包括丙型肝炎感染）的方法。在某些实施方案中，另外的活性剂是NS3a蛋白酶抑制剂。

12. 发明申请

US20120302538A1 SUBSITUTED ALIPHANES, CYCLOPHANES, HETERAPHANES, HETEROPHANES, HETERO-HETERAPHANES AND METALLOCENES USEFUL FOR TREATING HCV INFECTIONS 有权
标题翻译：用于治疗HCV感染的有用的二醇，环磷酰胺，异黄酮，异黄酮，异黄酮和金属
公开(公告)号：US20120302538A1
公开(公告)日：2012-11-29
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： A61K31/4178 , A61K31/4184 , C07F17/02 , 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。

13. 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。

14. 发明申请

US20060235041A1 New isothiazoloquinolones and related compounds as anti-infective agents 失效
标题翻译：新异噻唑并喹啉酮和相关化合物作为抗感染剂
公开(公告)号：US20060235041A1
公开(公告)日：2006-10-19
申请号：US11354521
申请日：2006-02-15
申请人： Barton Bradbury , Godwin Pais , Qiuping Wang , Milind Deshpande , Michael Pucci , Yongsheng Song , Edlaine Lucien , Jason Wiles , Akihiro Hashimoto
发明人： Barton Bradbury , Godwin Pais , Qiuping Wang , Milind Deshpande , Michael Pucci , Yongsheng Song , Edlaine Lucien , Jason Wiles , Akihiro Hashimoto
IPC分类号： C07D498/02 , A61K31/4745
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. Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.
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A 1，R 2，R 3，R 5，R 6，/或 >，R 7，A 8和R 9在本文中定义。本文公开的某些式I和式II化合物是细菌DNA合成和细菌复制的有效和选择性抑制剂。本发明还提供包含一种或多种式I或式II化合物和一种或多种载体，赋形剂或稀释剂的抗微生物组合物，包括药物组合物。这样的组合物可以含有式I或式II的化合物作为唯一的活性剂或可以含有式I或式II的化合物与一种或多种其它活性剂的组合。本发明还提供了治疗动物微生物感染的方法。

15. 发明申请

US20060100215A1 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones and related compounds as anti-infective agents 审中-公开
标题翻译： 8A，9-二氢-4a-异噻唑并[5,4-b]喹啉-3,4-二酮和相关化合物作为抗感染剂
公开(公告)号：US20060100215A1
公开(公告)日：2006-05-11
申请号：US11271556
申请日：2005-11-10
申请人： Barton Bradbury , Milind Deshpande , Michael Pucci , Qiuping Wang , Jason Wiles , Yongsheng Song , Akihiro Hashimoto , Edlaine Lucien
发明人： Barton Bradbury , Milind Deshpande , Michael Pucci , Qiuping Wang , Jason Wiles , Yongsheng Song , Akihiro Hashimoto , Edlaine Lucien
IPC分类号： A61K31/496 , A61K31/4745 , C07D498/02
CPC分类号： C07D513/04 , C07D513/14
摘要： The invention provides 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 n, m, p, RA, RB, A1, R2, R3, R5, R6, R7, A8 and R9 are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and/or selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in eukaryotes.
摘要翻译：本发明提供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n，m，p，R a，R B，A 1，R 2，R 2， R 3，R 5，R 6，R 7，A 8和R 8，本文定义了SUB> 9 。本文公开的某些式I和式II化合物是细菌DNA合成和细菌复制的有效和/或选择性抑制剂。本发明还提供包含一种或多种式I或式II化合物和一种或多种载体，赋形剂或稀释剂的抗微生物组合物，包括药物组合物。这样的组合物可以含有式I或式II的化合物作为唯一的活性剂或可以含有式I或式II的化合物与一种或多种其它活性剂的组合。本发明还提供了用于治疗真核生物中的微生物感染的方法。

16. 发明授权

US08835456B1 NS5A inhibitors useful for treating HCV 有权
标题翻译：用于治疗HCV的NS5A抑制剂
公开(公告)号：US08835456B1
公开(公告)日：2014-09-16
申请号：US13423935
申请日：2012-03-19
申请人： Jason Allan Wiles , Venkat Gadhachanada , Avinash Phadke , Milind Deshpande , Dawei Chen
发明人： Jason Allan Wiles , Venkat Gadhachanada , Avinash Phadke , Milind Deshpande , Dawei Chen
IPC分类号： A61K31/44 , C07D451/02
CPC分类号： C07D471/08 , A61K45/06
摘要： The invention provides compounds of Formula I and the pharmaceutically salts thereof. These compounds may be generally described as bridged-bicyclo indole-containing compounds. The variables shown in Formula I are defined herein. Certain compounds of Formula I are useful as antiviral agents. Compounds 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 compounds of Formula I and at least one pharmaceutically acceptable carrier. Such pharmaceutical compositions may contain a compound of Formula I as the only active agent or may contain a combination of a compound of Formula I 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：本发明提供式I化合物及其药学上可接受的盐。这些化合物通常可以被描述为含桥连双环吲哚的化合物。式I中所示的变量在本文中定义。某些式I化合物可用作抗病毒剂。本文公开的化合物是病毒复制的有效和/或选择性抑制剂，特别是丙型肝炎病毒复制。本发明还提供含有一种或多种式I化合物和至少一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式I化合物作为唯一的活性剂，或者可以含有式I化合物与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。

17. 发明申请

US20160016986A1 STABILIZED NUCLEOTIDES FOR MEDICAL TREATMENT 审中-公开
标题翻译：稳定的药物治疗核心
公开(公告)号：US20160016986A1
公开(公告)日：2016-01-21
申请号：US14805421
申请日：2015-07-21
申请人： Milind Deshpande , Jason Allan Wiles , Akihiro Hashimoto , Avinash Phadke
发明人： Milind Deshpande , Jason Allan Wiles , Akihiro Hashimoto , Avinash Phadke
IPC分类号： C07H19/10 , C07H19/056 , A61K31/7056 , A61K31/7072
CPC分类号： C07H19/10 , A61K31/7056 , A61K31/7072 , C07B59/005 , C07H19/056 , C07H19/11
摘要： 5′-Deuterated nucleosides and nucleotides and modifications thereof are provided for use in medical therapies, including as antiviral, anti-tumor and anti-neoplastic agents. In one embodiment, compounds, methods and uses are provided for the treatment of hepatitis C, RSV, HSV and other viral diseases in a host, including a human.
摘要翻译： 5'-脱唾液酸核苷及其核苷酸及其修饰被提供用于医学疗法，包括抗病毒，抗肿瘤和抗肿瘤剂。在一个实施方案中，提供化合物，方法和用途用于在宿主（包括人）中治疗丙型肝炎，RSV，HSV和其它病毒性疾病。

18. 发明申请

US20060173026A1 8-N-substituted-2H-isothiazolo[5,4-b]quinolizine-3,4-diones and related compounds as antiinfective agents 失效
标题翻译： 8-N-取代-2H-异噻唑并[5,4-b]喹嗪-3,4-二酮和相关化合物作为抗感染剂
公开(公告)号：US20060173026A1
公开(公告)日：2006-08-03
申请号：US11345201
申请日：2006-02-01
申请人： Barton Bradbury , Jason Wiles , Milind Deshpande , Quiping Wang , Akihiro Hashimoto , Edlaine Lucien
发明人： Barton Bradbury , Jason Wiles , Milind Deshpande , Quiping Wang , Akihiro Hashimoto , Edlaine Lucien
IPC分类号： A61K31/519 , A61K31/4745 , C07D491/14
CPC分类号： C07D513/14 , C07D498/14 , C07D513/22 , C07D519/00
摘要： The invention provides 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, A8, R2, R3, R5, R6, R7, and R9 are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of compounds of Formula I and/or Formula II and one or more other active agents. The invention also provides methods for treating microbial and protozoal infections in animals.
摘要翻译：本发明提供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A 1，A 8，R 2，R 3，R 5，/ 3 >，R 6，R 7和R 9在本文中定义。本文公开的某些式I和式II化合物是细菌DNA合成和细菌复制的有效和选择性抑制剂。本发明还提供包含一种或多种式I或式II化合物和一种或多种载体，赋形剂或稀释剂的抗微生物组合物，包括药物组合物。这样的组合物可以含有式I或式II的化合物作为唯一的活性剂或可以含有式I和/或式II化合物与一种或多种其它活性剂的组合。本发明还提供了用于处理动物中的微生物和原生动物感染的方法。

19. 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。

20. 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.

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