公开(公告)号：US07365068B2

公开(公告)日：2008-04-29

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： A61K31/496 ,  A61K31/444 ,  A61K31/5377 ,  C07D211/78 ,  C07D401/02 ,  C07D401/06 ,  C07D413/02 ,  C07D413/06

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。

公开(公告)号：US20090023730A1

公开(公告)日：2009-01-22

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： A61K31/5377 ,  C07C69/00 ,  A61K31/216 ,  C07D213/02 ,  A61K31/44 ,  C07D295/00 ,  A61K31/5375 ,  C07D285/06 ,  A61K31/433 ,  C07D241/36 ,  A61K31/498 ,  C07D211/06 ,  A61K31/445 ,  C07D239/02 ,  A61K31/505 ,  C07D215/00 ,  A61K31/47 ,  C07D471/02 ,  A61P31/12 ,  A61K31/53 ,  C07D253/06 ,  A61K31/437 ,  C07D401/02 ,  A61K31/496 ,  C07D487/02 ,  A61K31/519 ,  C07D413/02

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。

公开(公告)号：US07476686B2

公开(公告)日：2009-01-13

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： A61K31/44 ,  C07D213/46

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.

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。

公开(公告)号：US07094807B2

公开(公告)日：2006-08-22

申请号：US10716175

申请日：2003-11-18

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 ,  C07C335/02

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.

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。

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。

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.

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。

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。

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。

公开(公告)号：US20060167269A1

公开(公告)日：2006-07-27

申请号：US10483096

申请日：2002-07-11

申请人： Andrew Hamilton ,  Wesley Van Voorhis ,  Kohei Yokoyama ,  Fredericks Bucker ,  Junko Ohkanda ,  Michael Gelb ,  Jeffrey Lockman

发明人： Andrew Hamilton ,  Wesley Van Voorhis ,  Kohei Yokoyama ,  Fredericks Bucker ,  Junko Ohkanda ,  Michael Gelb ,  Jeffrey Lockman

IPC分类号： C07D233/61 ,  A61K31/4172

CPC分类号： C07D233/64 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

摘要： The present invention relates to compounds according to the formula (I): Where RA is a C1-C10 substituted or unsubstituted linear, branch-chained or cyclic alkyl or alkenyl group or a phenyl group according to the formula (II): RB is a C1-C10 substituted or unsubstituted linear, branch-chained or cyclic alkyl or alkenyl group or a phenyl group of the formula (III): R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are each independently selected from H, C1-C10 (preferably a C1-C4) alkyl or alkenyl group, CF3, F, Cl, Br, I, CN, NO2, NH2, NHR, NRR, COR (acyl group), OR (hydroxyl or ether group), CO2R (carboxylic acid or ester group), or COSR (thioester group) where R is H or a C1-C10 (preferably a C1-C4) alkyl or alkenyl group, an unsubstituted or substituted aryl (preferably, phenyl) or heterocycle group, or a (IV) group, where R3 is H, a C1-C10 (preferably a C1-C4) alkyl, alkenyl, ether or a thioether group; and R11 and R12 are independently selected from H or a C1-C3 alkyl or alkenyl group, or a pharmaceutically acceptable salt thereof and methods for treating infections caused by protozoal, fungal and/or bacterial agents such as Trypanosoma cruzi, Mycobacterium spp., Leishmania spp., Cryptococcus spp., Aspergillus spp., Histoplasma spp., Candida spp., especially Candida albicans, Pneumocystis carinii, Trichophyton spp., Microsporum spp., Malassezia spp., Rhizopus spp., Pseudallescheria spp., Blastomyces dermatitidis and Coccidiodes spp., among others.