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21. 发明授权

US07718671B2 Substituted arylthiourea derivatives useful as inhibitors of viral replication 失效
标题翻译：用作病毒复制抑制剂的取代的芳基硫脲衍生物
公开(公告)号：US07718671B2
公开(公告)日：2010-05-18
申请号：US10887227
申请日：2004-07-08
申请人： Avinash Phadke , Jesse Quinn , Junko Ohkanda , Andrew Thurkauf , Yiping Shen , Cuixian Liu , Dawei Chen , Shouming Li , Xiangzhu Wang
发明人： Avinash Phadke , Jesse Quinn , Junko Ohkanda , Andrew Thurkauf , Yiping Shen , Cuixian Liu , Dawei Chen , Shouming Li , Xiangzhu Wang
IPC分类号： A61K31/47 , C07D217/02 , A61K31/445 , C07D211/32 , C07C335/00
CPC分类号： C07D211/64 , C07C335/12 , C07C335/14 , C07C335/16 , C07C335/18 , C07C335/20 , C07C335/22 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/44 , C07D211/14 , C07D211/62 , C07D215/06 , C07D217/04 , C07D295/135 , C07D317/66
摘要： Substituted arylthiourea compounds of Formula I, and the pharmaceutically acceptable salts of such compounds, useful as antiviral agents, are provided herein. Certain substituted arylthioureas disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions containing one or more substituted arylthiourea compounds and one or more pharmaceutically acceptable carriers, excipients, or diluents are provided herein. Such pharmaceutical compositions may contain a substituted arylthiourea as the only active agent or may contain a combination of a substituted arylthiourea derivative and one or more other pharmaceutically active agents. Methods of treating Hepatitis C viral infections in mammals are also provided herein.
摘要翻译：本文提供了式I的取代的芳基硫脲化合物和可用作抗病毒剂的这类化合物的药学上可接受的盐。本文公开的某些取代的芳基硫脲是有效和/或选择性的病毒复制抑制剂，特别是丙型肝炎病毒复制。本文提供了含有一种或多种取代的芳基硫脲化合物和一种或多种药学上可接受的载体，赋形剂或稀释剂的药物组合物。这样的药物组合物可以含有取代的芳基硫脲作为唯一的活性剂，或者可以含有取代的芳基硫脲衍生物和一种或多种其它药物活性剂的组合。本文还提供了治疗哺乳动物中丙型肝炎病毒感染的方法。

22. 发明申请

US20100292219A1 TERTIARY AMINE SUBSTITUTED PEPTIDES USEFUL AS INHIBITORS OF HCV REPLICATION 失效
标题翻译：作为丙型肝炎病毒复制的抑制剂的有用的胺替代物
公开(公告)号：US20100292219A1
公开(公告)日：2010-11-18
申请号：US12597380
申请日：2008-02-26
申请人： Atul Agarwal , Xiangzhu Wang , Dawei Chen , Suoming Zhang , Avinash Phadke
发明人： Atul Agarwal , Xiangzhu Wang , Dawei Chen , Suoming Zhang , Avinash Phadke
IPC分类号： A61K31/403 , C07D401/06 , C07D403/06 , C07D417/06 , A61K31/454 , A61K31/55 , A61K31/541 , A61K31/496 , A61P31/14
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/06026 , C07K5/06034 , C07K5/0806 , C07K5/0808 , C07K5/0812
摘要： The present invention provides tertiary amine substituted peptides of Formula (I) useful as inhibitors of HCV replication. The variables R and R1-R12 in Formula I are described herein. The invention also includes methods for preparing such compounds. The present invention further includes pharmaceutical compositions containing tertiary amine substituted peptides and methods for using such compounds, including methods for using the compounds to treat hepatitis C infection.
摘要翻译：本发明提供可用作HCV复制抑制剂的式（I）的叔胺取代肽。本文描述了式I中的变量R和R 1 -R 12。本发明还包括制备这些化合物的方法。本发明还包括含有叔胺取代肽的药物组合物和使用这些化合物的方法，包括使用该化合物治疗丙型肝炎感染的方法。

23. 发明授权

US08435984B2 Tertiary amine substituted peptides useful as inhibitors of HCV replication 失效
标题翻译：可用作HCV复制抑制剂的叔胺取代肽
公开(公告)号：US08435984B2
公开(公告)日：2013-05-07
申请号：US12597380
申请日：2008-02-26
申请人： Atul Agarwal , Xiangzhu Wang , Dawei Chen , Suoming Zhang , Avinash Phadke
发明人： Atul Agarwal , Xiangzhu Wang , Dawei Chen , Suoming Zhang , Avinash Phadke
IPC分类号： C07D401/00 , C07D405/00 , C07D403/00 , C07D217/00 , A01N43/40 , A61K31/445 , A61K31/55
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/06026 , C07K5/06034 , C07K5/0806 , C07K5/0808 , C07K5/0812
摘要： The present invention provides tertiary amine substituted peptides of Formula (I) useful as inhibitors of HCV replication. The variables R and R1-R12 in Formula I are described herein. The invention also includes methods for preparing such compounds. The present invention further includes pharmaceutical compositions containing tertiary amine substituted peptides and methods for using such compounds, including methods for using the compounds to treat hepatitis C infection.
摘要翻译：本发明提供可用作HCV复制抑制剂的式（I）的叔胺取代肽。本文描述了式I中的变量R和R 1 -R 12。本发明还包括制备这些化合物的方法。本发明还包括含有叔胺取代肽的药物组合物和使用这些化合物的方法，包括使用该化合物治疗丙型肝炎感染的方法。

24. 发明申请

US20050032849A1 Substituted arylthiourea derivatives useful as inhibitors of viral replication 失效
标题翻译：用作病毒复制抑制剂的取代的芳基硫脲衍生物
公开(公告)号：US20050032849A1
公开(公告)日：2005-02-10
申请号：US10887227
申请日：2004-07-08
申请人： Avinash Phadke , Jesse Quinn , Junko Ohkanda , Andrew Thurkauf , Yiping Shen , Cuixian Liu , Dawei Chen , Shouming Li
发明人： Avinash Phadke , Jesse Quinn , Junko Ohkanda , Andrew Thurkauf , Yiping Shen , Cuixian Liu , Dawei Chen , Shouming Li
IPC分类号： A61K31/17 , A61K31/44 , C07C15/00 , C07C335/14 , C07C335/16 , C07D213/54
CPC分类号： C07D211/64 , C07C335/12 , C07C335/14 , C07C335/16 , C07C335/18 , C07C335/20 , C07C335/22 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/44 , C07D211/14 , C07D211/62 , C07D215/06 , C07D217/04 , C07D295/135 , C07D317/66
摘要： Substituted arylthiourea compounds of Formula I, and the pharmaceutically acceptable salts of such compounds, useful as antiviral agents, are provided herein. Certain substituted arylthioureas disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions containing one or more substituted arylthiourea compounds and one or more pharmaceutically acceptable carriers, excipients, or diluents are provided herein. Such pharmaceutical compositions may contain a substituted arylthiourea as the only active agent or may contain a combination of a substituted arylthiourea derivative and one or more other pharmaceutically active agents. Methods of treating Hepatitis C viral infections in mammals are also provided herein.
摘要翻译：本文提供了式I的取代的芳基硫脲化合物和可用作抗病毒剂的这类化合物的药学上可接受的盐。本文公开的某些取代的芳基硫脲是有效和/或选择性的病毒复制抑制剂，特别是丙型肝炎病毒复制。本文提供了含有一种或多种取代的芳基硫脲化合物和一种或多种药学上可接受的载体，赋形剂或稀释剂的药物组合物。这样的药物组合物可以含有取代的芳基硫脲作为唯一的活性剂，或者可以含有取代的芳基硫脲衍生物和一种或多种其它药物活性剂的组合。本文还提供了治疗哺乳动物中丙型肝炎病毒感染的方法。

25. 发明申请

US20050228013A1 Azabenzofuran substituted thioureas; inhibitors of viral replication 失效
标题翻译：氮杂苯并呋喃取代的硫脲; 病毒复制抑制剂
公开(公告)号：US20050228013A1
公开(公告)日：2005-10-13
申请号：US11029910
申请日：2005-01-05
申请人： Andrew Thurkauf , Dawei Chen , Avinash Phadke , Shouming Li , Milind Deshpande
发明人： Andrew Thurkauf , Dawei Chen , Avinash Phadke , Shouming Li , Milind Deshpande
IPC分类号： A61K31/00 , A61K31/4355 , A61K31/4741 , A61K38/21 , C07D471/04 , C07D491/02 , C07D491/04
CPC分类号： A61K31/00 , A61K31/4355 , C07D491/04
摘要： The present invention provides compounds of Formula 1, wherein the variables Ar, A1, A2, A3, A4, R5, R6, R7, V, W. X, and Y are defined herein. Certain compounds of Formula 1 described herein possess potent antiviral activity. The invention also provides compounds of Formula 1 that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compounds of Formula 1, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula 1 effective to reduce signs or symptoms of the disease. These infectious diseases include viral infections, particularly HCV infections. The invention is particularly includes methods of treating human patients suffering from an infectious disease, but also encompasses methods of treating other animals, including livestock and domesticated companion animals, suffering from an infectious disease. Methods of treatment include administering a compound of Formula 1 as a single active agent or administering a compound of Formula 1 in combination with on or more other therapeutic agent.
摘要翻译：本发明提供式1的化合物，其中变量Ar，A 1，A 2，A 3，A 4， R 5，R 6，R 7，V，W，X和Y如本文所定义。某些本文所述的式1的化合物具有有效的抗病毒活性。本发明还提供了作为丙型肝炎病毒复制的有效和/或选择性抑制剂的式1化合物。本发明还提供含有一种或多种式1化合物或这些化合物的盐，溶剂化物或酰化前药以及一种或多种药学上可接受的载体，赋形剂或稀释剂的药物组合物。本发明还包括通过向这些患者施用一定量的有效减少疾病体征或症状的式1化合物来治疗患有某些感染性疾病的患者的方法。这些传染病包括病毒感染，特别是HCV感染。本发明特别包括治疗患有感染性疾病的人类患者的方法，还包括治疗其它动物（包括患有传染病的家畜和驯养的伴侣动物）的方法。治疗方法包括施用作为单一活性剂的式1化合物或与一种或多种其它治疗剂组合施用式1的化合物。

26. 发明授权

US08163693B2 Urea-containing peptides as inhibitors of viral replication 失效
标题翻译：含尿素肽作为病毒复制的抑制剂
公开(公告)号：US08163693B2
公开(公告)日：2012-04-24
申请号：US12236855
申请日：2008-09-24
申请人： Dawei Chen , Milind Deshpande , Avinash Phadke
发明人： Dawei Chen , Milind Deshpande , Avinash Phadke
IPC分类号： A61K38/00
CPC分类号： C07K5/0823 , A61K38/00 , C07K5/06165
摘要： The invention provides compounds urea-containing peptide compounds of Formula I and the pharmaceutically salts and hydrates thereof. The variables T, R1-R9, J, L, M, Y, Z, m, n, and t are defined herein. Certain compounds of Formula I are useful as antiviral agents. Certain urea-containing peptide compounds 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 urea containing peptides compounds and one or more pharmaceutically acceptable carriers, excipients, or diluents. Such pharmaceutical compositions may contain a urea containing peptides compound as the only active agent or may contain a combination of a urea containing peptides compound and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections, in mammals.
摘要翻译：本发明提供式I化合物的含脲的肽化合物及其药用盐和水合物。变量T，R1-R9，J，L，M，Y，Z，m，n和t在本文中定义。某些式I化合物可用作抗病毒剂。本文公开的某些含脲的肽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含尿素的肽化合物和一种或多种药学上可接受的载体，赋形剂或稀释剂的药物组合物。这样的药物组合物可以含有含有肽化合物作为唯一活性剂的尿素，或者可以含有含尿素的肽化合物和一种或多种其它药学活性剂的组合。本发明还提供了用于治疗哺乳动物中的病毒感染（包括丙型肝炎感染）的方法。

27. 发明申请

US20090082261A1 UREA-CONTAINING PEPTIDES AS INHIBITORS OF VIRAL REPLICATION 失效
标题翻译：作为病毒复制的抑制剂的尿素包含肽
公开(公告)号：US20090082261A1
公开(公告)日：2009-03-26
申请号：US12236855
申请日：2008-09-24
申请人： Dawei Chen , Milind Deshpande , Avinash Phadke
发明人： Dawei Chen , Milind Deshpande , Avinash Phadke
IPC分类号： A61K38/12 , C07K14/00 , C07K7/06 , C07K7/50 , C07K5/08 , C07K5/10 , A61P31/12 , C07K5/12 , A61K38/21 , A61K38/08 , A61K38/06 , A61K38/07
CPC分类号： C07K5/0823 , A61K38/00 , C07K5/06165
摘要： The invention provides compounds urea-containing peptide compounds of Formula I and the pharmaceutically salts and hydrates thereof.The variables T, R1-R9, J, L, M, Y, Z, m, n, and t are defined herein. Certain compounds of Formula I are useful as antiviral agents. Certain urea-containing peptide compounds 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 urea containing peptides compounds and one or more pharmaceutically acceptable carriers, excipients, or diluents. Such pharmaceutical compositions may contain a urea containing peptides compound as the only active agent or may contain a combination of a urea containing peptides compound and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections, in mammals.
摘要翻译：本发明提供式I化合物的含脲的肽化合物及其药用盐和水合物。变量T，R1-R9，J，L，M，Y，Z，m，n和t在本文中定义。某些式I化合物可用作抗病毒剂。本文公开的某些含脲的肽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含尿素的肽化合物和一种或多种药学上可接受的载体，赋形剂或稀释剂的药物组合物。这样的药物组合物可以含有含有肽化合物作为唯一活性剂的尿素，或者可以含有含尿素的肽化合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哺乳动物中的病毒感染（包括丙型肝炎感染）的方法。

28. 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。

29. 发明授权

US07439374B2 Azabenzofuran substituted thioureas; inhibitors of viral replication 失效
标题翻译：氮杂苯并呋喃取代的硫脲; 病毒复制抑制剂
公开(公告)号：US07439374B2
公开(公告)日：2008-10-21
申请号：US11029910
申请日：2005-01-05
申请人： Andrew Thurkauf , Dawei Chen , Avinash Phadke , Shouming Li , Milind Deshpande
发明人： Andrew Thurkauf , Dawei Chen , Avinash Phadke , Shouming Li , Milind Deshpande
IPC分类号： C07D401/02 , A61K31/44
CPC分类号： A61K31/00 , A61K31/4355 , C07D491/04
摘要： The present invention provides compounds of Formula 1, wherein the variables Ar, A1, A2, A3, A4, R5, R6, R7, V, W, X, and Y are defined herein. Certain compounds of Formula 1 described herein possess potent antiviral activity. The invention also provides compounds of Formula 1 that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compounds of Formula 1, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula 1 effective to reduce signs or symptoms of the disease. These infectious diseases include viral infections, particularly HCV infections. The invention is particularly includes methods of treating human patients suffering from an infectious disease, but also encompasses methods of treating other animals, including livestock and domesticated companion animals, suffering from an infectious disease.Methods of treatment include administering a compound of Formula 1 as a single active agent or administering a compound of Formula 1 in combination with on or more other therapeutic agent.
摘要翻译：本发明提供式1的化合物，其中变量Ar，A 1，A 2，A 3，A 4， R 5，R 6，R 7，V，W，X和Y在本文中定义。某些本文所述的式1的化合物具有有效的抗病毒活性。本发明还提供了作为丙型肝炎病毒复制的有效和/或选择性抑制剂的式1化合物。本发明还提供含有一种或多种式1化合物或这些化合物的盐，溶剂化物或酰化前药以及一种或多种药学上可接受的载体，赋形剂或稀释剂的药物组合物。本发明还包括通过向这些患者施用一定量的有效减少疾病体征或症状的式1化合物来治疗患有某些感染性疾病的患者的方法。这些传染病包括病毒感染，特别是HCV感染。本发明特别包括治疗患有感染性疾病的人类患者的方法，还包括治疗其它动物（包括患有传染病的家畜和驯养的伴侣动物）的方法。治疗方法包括施用作为单一活性剂的式1化合物或与一种或多种其它治疗剂组合施用式1的化合物。

30. 发明授权

US06412478B1 Breather for internal combustion engine 有权
标题翻译：内燃机呼吸器
公开(公告)号：US06412478B1
公开(公告)日：2002-07-02
申请号：US09753367
申请日：2001-01-02
申请人： Gerald C. Ruehlow , Edward M. Haworth , Dawei Chen
发明人： Gerald C. Ruehlow , Edward M. Haworth , Dawei Chen
IPC分类号： F02B2506
CPC分类号： F01M13/0416 , F01M2013/0433 , F01M2013/0461
摘要： A breather is provided for mounting on a cylinder head of a crankcase of an engine in order to separate oil from the crankcase blow-by. The breather includes a rocker cover mounted to the cylinder head of the crankcase. A plate is positioned within a cavity in the rocker cover for separating the cavity into first and second portions. The plate has an opening therein for allowing the crankcase blow-by to flow from the first portion into the second portion of the cavity. An oil separator is disposed in the second portion of the cavity and includes baffles projecting from each side thereof. It is contemplated that the oil in the crankcase blow-by cling to the oil separator and the first and second sets of baffles as the crankcase blow-by flows therepast.
摘要翻译：设置有用于安装在发动机的曲轴箱的气缸盖上的通气器，以将油与曲轴箱窜气分离。呼吸器包括安装在曲轴箱的气缸盖上的摇臂盖。板被定位在摇臂盖的空腔内，用于将空腔分成第一和第二部分。板上有一个开口，用于允许曲轴箱窜气从第一部分流入空腔的第二部分。油分离器设置在空腔的第二部分中，并且包括从其每侧突出的挡板。可以想到，随着曲轴箱窜流，曲轴箱窜流中的油粘附到油分离器和第一组和第二组挡板上。

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