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11. 发明申请

US20090041720A1 HETEROARYL SUBSTITUTED THIAZOLES 失效
标题翻译： HETEROARYL取代THIAZOLES
公开(公告)号：US20090041720A1
公开(公告)日：2009-02-12
申请号：US12125554
申请日：2008-05-22
申请人： Xiangzhu Wang , Souming Zhang , Venkat Gadhachanda , Cuixian Liu , Jesse Quinn , Shouming Li , Dawei Chen , Milind Deshpande , Avinash Phadke
发明人： Xiangzhu Wang , Souming Zhang , Venkat Gadhachanda , Cuixian Liu , Jesse Quinn , Shouming Li , Dawei Chen , Milind Deshpande , Avinash Phadke
IPC分类号： A61K38/21 , C07D417/04 , C07D401/04 , A61K31/443 , A61P31/12 , A61K31/7056 , A61K31/4439 , A61K31/496
CPC分类号： C07D417/04
摘要： The invention provides heteroaryl substituted thiazolo compounds of Formula I and II and pharmaceutically acceptable salts thereof. The variables A and R3 to R7 are defined herein. The invention also includes methods for preparing compounds and salts of Formula I and II. The present invention also includes pharmaceutical compositions containing heteroaryl substituted thiazolo compounds and methods for using heteroaryl substituted thiazolo compounds, including methods for using the compounds in the treatment of hepatitis C virus.
摘要翻译：本发明提供式I和II的杂芳基取代的噻唑烷化合物及其药学上可接受的盐。变量A和R3至R7在本文中定义。本发明还包括制备式I和II的化合物和盐的方法。本发明还包括含有杂芳基取代的噻唑烷化合物的药物组合物和使用杂芳基取代的噻唑烷化合物的方法，包括使用这些化合物治疗丙型肝炎病毒的方法。

12. 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。

13. 发明申请

US20060025416A1 Substituted aryl acylthioureas and related compounds; inhibitors of viral replication 失效
标题翻译：取代的芳基酰基硫脲和相关化合物; 病毒复制抑制剂
公开(公告)号：US20060025416A1
公开(公告)日：2006-02-02
申请号：US11131013
申请日：2005-05-17
申请人： Avinash Phadke , Dawei Chen , Milind Deshpande , Andrew Thurkauf , Xiangzhu Wang , Yiping Shen , Cuixian Liu , Jesse Quinn , Junko Ohkanda , Shouming Li
发明人： Avinash Phadke , Dawei Chen , Milind Deshpande , Andrew Thurkauf , Xiangzhu Wang , Yiping Shen , Cuixian Liu , Jesse Quinn , Junko Ohkanda , Shouming Li
IPC分类号： A61K31/537 , A61K31/498 , A61K31/47 , A61K31/421 , A61K31/17
CPC分类号： C07D295/15 , C07C335/26 , C07D211/22 , C07D211/46 , C07D211/60 , C07D211/64 , C07D211/78 , C07D213/56 , C07D213/82 , C07D215/54 , C07D231/14 , C07D233/54 , C07D233/64 , C07D233/90 , C07D237/24 , C07D239/28 , C07D241/24 , C07D241/44 , C07D249/06 , C07D253/07 , C07D261/18 , C07D263/34 , C07D263/58 , C07D265/30 , C07D271/12 , C07D277/56 , C07D277/68 , C07D285/06 , C07D307/68 , C07D307/84 , C07D307/85 , C07D309/38 , C07D311/58 , C07D333/38 , C07D401/04 , C07D401/12 , C07D405/04 , C07D409/04 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07D419/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04 , C07D513/04
摘要： The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, 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 I effective to reduce signs or symptoms of the disease or disorder. 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 I as a single active agent or administering a compound of Formula I in combination with on or more other therapeutic agent.
摘要翻译：本发明提供式I的化合物和药学上可接受的盐，其中变量A 1，A 2，R 1，R 2， / SUB>，V，W，X，Y和Z在本文中定义。某些本文所述的具有强抗病毒活性的式I化合物。本发明特别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I化合物。本发明还提供含有一种或多种式I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或病症的体征或症状的式I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。治疗方法包括给予式I化合物作为单一活性剂或将一种式I化合物与一种或多种其它治疗剂组合施用。

14. 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。

15. 发明授权

US08088806B2 Thiazole compounds and methods of use 失效
标题翻译：噻唑化合物和使用方法
公开(公告)号：US08088806B2
公开(公告)日：2012-01-03
申请号：US11431155
申请日：2006-05-09
申请人： Suoming Zhang , Avinash Phadke , Cuixian Liu , Xiangzhu Wang , Jesse Quinn , Dawei Chen , Venkat Gadhachanda , Shouming Li , Milind Deshpande
发明人： Suoming Zhang , Avinash Phadke , Cuixian Liu , Xiangzhu Wang , Jesse Quinn , Dawei Chen , Venkat Gadhachanda , Shouming Li , Milind Deshpande
IPC分类号： A61K31/426 , A61K31/44
CPC分类号： C07D487/04 , C07D277/38 , C07D277/42 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D513/04
摘要： The present invention provides compounds, salts and hydrates of Formula I, wherein the variables Ar1, R2, R3, R4, r, q, and t are defined herein. Certain compounds of Formula I described herein possess potent antiviral activity. The invention also provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. Certain compounds described herein inhibit assembly of the HCV replication complex. The invention also provides pharmaceutical compositions containing one or more compounds of Formula I, 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 I 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 I as a single active agent or administering a compound of Formula I in combination with on or more other therapeutic agent.
摘要翻译：本发明提供式I的化合物，盐和水合物，其中变量Ar1，R2，R3，R4，r，q和t在本文中定义。某些本文所述的式I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I化合物。本文所述的某些化合物抑制HCV复制复合物的组装。本发明还提供含有一种或多种式I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降低疾病体征或症状的式I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。治疗方法包括给予式I化合物作为单一活性剂或将一种式I化合物与一种或多种其它治疗剂组合施用。

16. 发明授权

US07767706B2 Substituted aryl acylthioureas and related compounds; inhibitors of viral replication 失效
标题翻译：取代的芳基酰基硫脲和相关化合物; 病毒复制抑制剂
公开(公告)号：US07767706B2
公开(公告)日：2010-08-03
申请号：US12036728
申请日：2008-02-25
申请人： Avinash Phadke , Dawei Chen , Milind Deshpande , Andrew Thurkauf , Xiangzhu Wang , Yiping Shen , Cuixian Liu , Jesse Quinn , Junko Ohkanda , Shouming Li
发明人： Avinash Phadke , Dawei Chen , Milind Deshpande , Andrew Thurkauf , Xiangzhu Wang , Yiping Shen , Cuixian Liu , Jesse Quinn , Junko Ohkanda , Shouming Li
IPC分类号： A61K31/415 , C07D231/10
CPC分类号： C07D295/15 , C07C335/26 , C07D211/22 , C07D211/46 , C07D211/60 , C07D211/64 , C07D211/78 , C07D213/56 , C07D213/82 , C07D215/54 , C07D231/14 , C07D233/54 , C07D233/64 , C07D233/90 , C07D237/24 , C07D239/28 , C07D241/24 , C07D241/44 , C07D249/06 , C07D253/07 , C07D261/18 , C07D263/34 , C07D263/58 , C07D265/30 , C07D271/12 , C07D277/56 , C07D277/68 , C07D285/06 , C07D307/68 , C07D307/84 , C07D307/85 , C07D309/38 , C07D311/58 , C07D333/38 , C07D401/04 , C07D401/12 , C07D405/04 , C07D409/04 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07D419/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04 , C07D513/04
摘要： The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, 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 I effective to reduce signs or symptoms of the disease or disorder. 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 I as a single active agent or administering a compound of Formula I in combination with on or more other therapeutic agent.
摘要翻译：本发明提供式I的化合物和药学上可接受的盐，其中变量A1，A2，R1，R2，V，W，X，Y和Z在本文中定义。某些本文所述的具有强抗病毒活性的式I化合物。本发明特别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I化合物。本发明还提供含有一种或多种式I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或病症的体征或症状的式I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。治疗方法包括给予式I化合物作为单一活性剂或将一种式I化合物与一种或多种其它治疗剂组合施用。

17. 发明申请

US20060014836A1 Substituted aryl thioureas and related compounds; inhibitors of viral replication 失效
公开(公告)号：US20060014836A1
公开(公告)日：2006-01-19
申请号：US11015300
申请日：2004-12-17
申请人： Dawei Chen , Milind Deshpande , Andrew Thurkauf , Avinash Phadke , Xiangzhu Wang , Yiping Shen , Cuixian Liu , Jesse Quinn , Junko Ohkanda , Shouming Li
发明人： Dawei Chen , Milind Deshpande , Andrew Thurkauf , Avinash Phadke , Xiangzhu Wang , Yiping Shen , Cuixian Liu , Jesse Quinn , Junko Ohkanda , Shouming Li
IPC分类号： A61K31/17 , C07C335/26
CPC分类号： C07D209/48 , C07C335/26 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/12 , C07D207/16 , C07D207/34 , C07D207/416 , C07D209/42 , C07D211/14 , C07D211/62 , C07D211/70 , C07D211/86 , C07D213/64 , C07D213/65 , C07D213/81 , C07D215/06 , C07D215/48 , C07D217/04 , C07D231/14 , C07D233/42 , C07D233/90 , C07D239/26 , C07D241/24 , C07D241/44 , C07D249/06 , C07D257/04 , C07D261/18 , C07D263/34 , C07D263/57 , C07D271/08 , C07D271/12 , C07D277/56 , C07D277/66 , C07D277/68 , C07D285/06 , C07D295/135 , C07D295/15 , C07D307/52 , C07D307/68 , C07D307/85 , C07D311/24 , C07D311/66 , C07D317/66 , C07D319/20 , C07D333/20 , C07D333/34 , C07D333/38 , C07D333/70 , C07D405/04 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D487/04 , C07D495/04
摘要： The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, 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 I effective to reduce signs or symptoms of the disease or disorder. 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 I as a single active agent or administering a compound of Formula I in combination with on or more other therapeutic agent.

18. 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。

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