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。

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。

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。

公开(公告)号：US08946422B2

公开(公告)日：2015-02-03

申请号：US13279852

申请日：2011-10-24

申请人： Barton James Bradbury ,  Jason Allan Wiles ,  Qiuping Wang ,  Akhiro Hashimoto ,  Edlaine Lucien ,  Godwin Clarence Gilroy Pais ,  Milind Deshpande ,  Micheal John Pucci ,  Ha Young Kim

发明人： Barton James Bradbury ,  Jason Allan Wiles ,  Qiuping Wang ,  Akhiro Hashimoto ,  Edlaine Lucien ,  Godwin Clarence Gilroy Pais ,  Milind Deshpande ,  Micheal John Pucci ,  Ha Young Kim

IPC分类号： A61K31/4375 ,  A61K31/496 ,  A61P33/02 ,  C07D513/14 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

CPC分类号： C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  C07D513/14

摘要： The invention provides compound and salts of Formula I and II, disclosed herein, which includes compounds of Formula A and Formula B: Such compounds possess useful antimicrobial activity. The variables R2, R3, R5, R6, R7, and R9 shown in Formula A and B 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 animals.

摘要翻译： 本发明提供本文公开的式I和II的化合物和盐，其包括式A和式B的化合物：这些化合物具有有效的抗微生物活性。 式A和B中所示的变量R2，R3，R5，R6，R7和R9如本文所定义。 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/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。 本发明还提供了治疗动物微生物感染的方法。

公开(公告)号：US08044204B2

公开(公告)日：2011-10-25

申请号：US11494205

申请日：2006-07-27

申请人： Barton James Bradbury ,  Jason Allan Wiles ,  Qiuping Wang ,  Akhiro Hashimoto ,  Edlaine Lucien ,  Godwin Clarence Gilroy Pais ,  Milind Deshpande ,  Michael John Pucci ,  Ha Young Kim

发明人： Barton James Bradbury ,  Jason Allan Wiles ,  Qiuping Wang ,  Akhiro Hashimoto ,  Edlaine Lucien ,  Godwin Clarence Gilroy Pais ,  Milind Deshpande ,  Michael John Pucci ,  Ha Young Kim

IPC分类号： C07D417/04 ,  C07D409/04 ,  A61K31/4365

CPC分类号： C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  C07D513/14

摘要： The invention provides compound and salts of Formula I and II, disclosed herein, which includes compounds of Formula A and Formula B: Such compounds possess useful antimicrobial activity. The variables R2, R3, R5, R6, R7, and R9 shown in Formula A and B 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 animals.

摘要翻译： 本发明提供本文公开的式I和II的化合物和盐，其包括式A和式B的化合物：这些化合物具有有效的抗微生物活性。 式A和B中所示的变量R2，R3，R5，R6，R7和R9如本文所定义。 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/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。 本发明还提供了治疗动物微生物感染的方法。

公开(公告)号：US20120040959A1

公开(公告)日：2012-02-16

申请号：US13279852

申请日：2011-10-24

申请人： Barton James Bradbury ,  Jason Allan Wiles ,  Qiuping Wang ,  Akhiro Hashimoto ,  Edlaine Lucien ,  Godwin Clarence Gilroy Pais ,  Milind Deshpande ,  Michael John Pucci ,  Ha Young Kim

发明人： Barton James Bradbury ,  Jason Allan Wiles ,  Qiuping Wang ,  Akhiro Hashimoto ,  Edlaine Lucien ,  Godwin Clarence Gilroy Pais ,  Milind Deshpande ,  Michael John Pucci ,  Ha Young Kim

IPC分类号： A61K31/4375 ,  A61K31/496 ,  A61K31/5377 ,  A61P33/02 ,  A61K31/438 ,  A61P31/00 ,  A61P31/04 ,  C07D513/14 ,  A61K31/541

CPC分类号： C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  C07D513/14

摘要： The invention provides compound and salts of Formula I and II, disclosed herein, which includes compounds of Formula A and Formula B: Such compounds possess useful antimicrobial activity. The variables R2, R3, R5, R6, R7, and R9 shown in Formula A and B 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 animals.

摘要翻译： 本发明提供本文公开的式I和II的化合物和盐，其包括式A和式B的化合物：这些化合物具有有效的抗微生物活性。 式A和B中所示的变量R2，R3，R5，R6，R7和R9如本文所定义。 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/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。 本发明还提供了治疗动物微生物感染的方法。

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.

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。

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.

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。