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1. 发明专利

JP2005330284A Substituted arylacylthiourea, its related compound, and inhibitor of virus replication 有权
标题翻译：取代的氨基乙酸酯，其相关化合物和病毒复制物的抑制剂
公开(公告)号：JP2005330284A
公开(公告)日：2005-12-02
申请号：JP2005144790
申请日：2005-05-17
申请人： Achillion Pharmaceuticals Inc , アチリオンファーマシューティカルズ, インコーポレイテッドAchillion Pharmaceuticals, Inc.
发明人： PHADKE AVINASH , CHEN DAWEI , DESHPANDE MILIND , THURKAUF ANDREW , WANG XIANGZHU , SHEN YIPING , LIU CUIXIAN , QUINN JESSE , OHKANDA JUNKO , LI SHOUMING
IPC分类号： C07D249/06 , A61K31/17 , A61K31/277 , A61K31/341 , A61K31/343 , A61K31/351 , A61K31/352 , A61K31/381 , A61K31/415 , A61K31/4155 , A61K31/4164 , A61K31/4192 , A61K31/42 , A61K31/421 , A61K31/423 , A61K31/4245 , A61K31/426 , A61K31/428 , A61K31/429 , A61K31/433 , A61K31/4355 , A61K31/437 , A61K31/4375 , A61K31/4406 , A61K31/4412 , A61K31/443 , A61K31/445 , A61K31/455 , A61K31/47 , A61K31/4725 , A61K31/496 , A61K31/498 , A61K31/50 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/53 , A61K31/5375 , A61K31/5377 , A61P31/12 , C07C335/18 , C07C335/20 , C07C335/26 , C07D211/20 , C07D211/22 , C07D211/46 , C07D211/60 , C07D211/64 , C07D211/78 , C07D213/56 , C07D213/75 , C07D213/82 , C07D213/84 , C07D213/85 , C07D215/54 , C07D231/14 , C07D233/54 , C07D233/60 , C07D233/90 , C07D237/24 , C07D239/28 , C07D241/24 , C07D241/42 , C07D241/44 , C07D253/06 , C07D253/07 , C07D261/18 , C07D263/34 , C07D263/58 , C07D265/30 , C07D271/12 , C07D277/20 , C07D277/56 , C07D277/68 , C07D285/06 , C07D295/10 , C07D295/14 , C07D295/15 , C07D307/68 , C07D307/84 , C07D307/85 , C07D309/38 , C07D311/04 , C07D311/58 , C07D333/38 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07D419/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D491/048 , C07D495/04 , C07D513/04
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： PROBLEM TO BE SOLVED: To provide an arylthiourea derivative and its related compound, useful as an antiviral agent. SOLUTION: This compound of formula I (A 1 , A 2 , R 1 , R 2 , V, W, X, Y and Z are each specifically defined) and its pharmaceutically acceptable salt have strong antiviral activity and, especially, are each a strong and/or selective inhibitor of hepatitis C virus replication. A pharmaceutical composition contains one or more kinds of the compounds of formula I, salts of the compound, solvates thereof, or acylated prodrugs thereof, and one or more kinds of pharmaceutically acceptable carriers, vehicles, or diluents. COPYRIGHT: (C)2006,JPO&NCIPI
摘要翻译：待解决的问题：提供可用作抗病毒剂的芳基硫脲衍生物及其相关化合物。解决方案：该式I化合物（A 1 ，A 2 ，R SB 1，R SB 2，，V，W，X，Y和Z各自具体定义），其药学上可接受的盐具有强的抗病毒活性，特别是各自是丙型肝炎病毒复制的强和/或选择性抑制剂。药物组合物含有一种或多种式I化合物，化合物的盐，其溶剂合物或其酰化前体药物，以及一种或多种药学上可接受的载体，赋形剂或稀释剂。版权所有（C）2006，JPO＆NCIPI

2. 发明专利

JP2007084548A Substituted aryl thiourea, related compound and inhibitor for viral replication 审中-公开
标题翻译：取代的芳基硫脲，相关化合物和抑制剂用于病毒复制
公开(公告)号：JP2007084548A
公开(公告)日：2007-04-05
申请号：JP2006272359
申请日：2006-10-03
申请人： Achillion Pharmaceuticals Inc , アチリオンファーマシューティカルズ, インコーポレイテッドAchillion Pharmaceuticals, Inc.
发明人： CHEN DAWEI , DESHPANDE MILIND , THURKAUF ANDREW , PHADKE AVINASH , WANG XIANGZHU , SHEN YIPING , LIU CUIXIAN , QUINN JESSE , OHKANDA JUNKO , LI SHOUMING
IPC分类号： C07C335/26 , A61K31/17 , A61K31/24 , A61K31/245 , A61K31/277 , A61K31/341 , A61K31/343 , A61K31/352 , A61K31/357 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/401 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/415 , A61K31/4162 , A61K31/4164 , A61K31/4192 , A61K31/42 , A61K31/422 , A61K31/423 , A61K31/4245 , A61K31/427 , A61K31/428 , A61K31/433 , A61K31/437 , A61K31/44 , A61K31/4406 , A61K31/443 , A61K31/4439 , A61K31/445 , A61K31/4453 , A61K31/4525 , A61K31/47 , A61K31/472 , A61K31/4965 , A61K31/498 , A61K31/519 , A61K31/5375 , A61K31/55 , A61P1/16 , A61P31/12 , C07D207/16 , C07D207/34 , C07D209/42 , C07D209/48 , C07D211/62 , C07D211/70 , C07D211/86 , C07D213/65 , C07D213/81 , C07D215/06 , C07D215/38 , C07D215/48 , C07D217/04 , C07D217/14 , C07D231/14 , C07D233/42 , C07D233/90 , C07D239/26 , C07D241/24 , C07D241/44 , C07D249/06 , C07D257/04 , C07D261/18 , C07D263/34 , C07D263/56 , C07D271/08 , C07D271/12 , C07D277/56 , C07D277/62 , C07D277/66 , C07D277/68 , C07D285/06 , C07D295/04 , C07D295/135 , C07D295/14 , C07D295/15 , C07D307/52 , C07D307/68 , C07D307/85 , C07D311/24 , C07D311/66 , C07D317/68 , C07D319/20 , C07D333/20 , C07D333/34 , C07D333/70 , C07D401/04 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D487/04 , C07D495/04
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： PROBLEM TO BE SOLVED: To provide a method of treating patients suffering from certain infectious diseases. SOLUTION: Specific acyl thiourea derivatives have potent antiviral activity. The compounds of the derivatives are a potent and/or selective inhibitor of Hepatitis C virus replication. The patients suffering from the certain diseases, can be treated with administration of a pharmaceutical composition comprising at least one of the same compounds, their salts, solvates or acylated prodrugs and at least one of a pharmaceutically acceptable carrier, excipient or diluent. The infectious diseases involve viral infection, more particular, HCV infection. COPYRIGHT: (C)2007,JPO&INPIT
摘要翻译：待解决的问题：提供治疗患有某些感染性疾病的患者的方法。解决方案：具体的酰基硫脲衍生物具有很强的抗病毒活性。衍生物的化合物是丙型肝炎病毒复制的有效和/或选择性抑制剂。患有某些疾病的患者可以通过给药包含至少一种相同化合物，其盐，溶剂合物或酰化前药的药物组合物和药学上可接受的载体，赋形剂或稀释剂中的至少一种来治疗。感染性疾病涉及病毒感染，特别是HCV感染。版权所有（C）2007，JPO＆INPIT

3. 发明专利

JP2006225394A SUBSTITUTED ARYL ACYLTHIOUREA AND RELATED COMPOUND; INHIBITOR OF VIRAL REPLICATION 审中-公开
公开(公告)号：JP2006225394A
公开(公告)日：2006-08-31
申请号：JP2006051358
申请日：2006-02-27
申请人： ACHILLION PHARMACEUTICALS INC
发明人： PHADKE AVINASH , CHEN DAWEI , DESHPANDE MILIND , THURKAUF ANDREW , WANG XIANGZHU , SHEN YIPING , LIU CUIXIAN , QUINN JESSE , OHKANDA JUNKO , LI SHOUMING
IPC分类号： C07C335/26 , C07D249/06 , A61K9/06 , A61K9/08 , A61K9/10 , A61K9/12 , A61K9/20 , A61K9/48 , A61K9/70 , A61K31/17 , A61K31/245 , A61K31/277 , A61K31/341 , A61K31/343 , A61K31/351 , A61K31/352 , A61K31/366 , A61K31/381 , A61K31/415 , A61K31/4155 , A61K31/4162 , A61K31/4164 , A61K31/4192 , A61K31/42 , A61K31/421 , A61K31/423 , A61K31/4245 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/429 , A61K31/433 , A61K31/4355 , A61K31/437 , A61K31/4375 , A61K31/4406 , A61K31/4412 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K31/445 , A61K31/451 , A61K31/4545 , A61K31/455 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/498 , A61K31/50 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/53 , A61K31/5375 , A61K31/5377 , A61K31/655 , A61P1/16 , A61P31/12 , A61P31/14 , C07C335/18 , C07C335/20 , C07D211/20 , C07D211/22 , C07D211/34 , C07D211/46 , C07D211/60 , C07D211/64 , C07D211/78 , C07D213/56 , C07D213/75 , C07D213/82 , C07D213/84 , C07D213/85 , C07D215/54 , C07D231/14 , C07D233/54 , C07D233/56 , C07D233/60 , C07D233/90 , C07D237/24 , C07D239/28 , C07D241/24 , C07D241/42 , C07D241/44 , C07D253/06 , C07D253/07 , C07D261/18 , C07D263/34 , C07D263/58 , C07D265/30 , C07D271/08 , C07D271/12 , C07D277/20 , C07D277/56 , C07D277/68 , C07D285/06 , C07D295/10 , C07D295/14 , C07D295/15 , C07D307/68 , C07D307/84 , C07D307/85 , C07D309/38 , C07D311/04 , C07D311/58 , C07D333/38 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07D419/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D491/048 , C07D495/04 , C07D513/04
摘要： PROBLEM TO BE SOLVED: To provide aryl thiourea derivatives and related compounds which are useful as antiviral agents. SOLUTION: Compounds of formula I and pharmaceutically acceptable salts there of: wherein 1-(4-(pentyloxy) phenyl)-3-(4-phenylbutanoyl) thiourea is specifically exemplified, possess potent antiviral activity. The above compounds are particularly potent and/or selective inhibitors for Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compounds of formula I, or a salt, solvate, or acylated prodrug of such a compound, and one or more pharmaceutically acceptable carriers, excipients, or diluents. COPYRIGHT: (C)2006,JPO&NCIPI

4. 发明申请

WO2006083271A2 SUBSTITUTED ARYL ACYLTHIOUREAS AND RELATED COMPOUNDS; INHIBITORS OF VIRAL REPLICATION 审中-公开
标题翻译：取代的芳基乙二醇和相关化合物; VIRAL REPLICATION的抑制剂
公开(公告)号：WO2006083271A2
公开(公告)日：2006-08-10
申请号：PCT/US2005017308
申请日：2005-05-17
申请人： ACHILLION PHARMACEUTICALS INC , PHADKE AVINASH , CHEN DAWEI , DESHPANDE MILIND , THURKAUF ANDREW , WANG XIANGZHU , SHEN YIPING , LIU CUIXIAN , QUINN JESSE , LI SHOUMING , OHKANDA JUNKO
发明人： PHADKE AVINASH , CHEN DAWEI , DESHPANDE MILIND , THURKAUF ANDREW , WANG XIANGZHU , SHEN YIPING , LIU CUIXIAN , QUINN JESSE , LI SHOUMING , OHKANDA JUNKO
IPC分类号： C07C335/26 , C07D249/06 , A61K31/17 , A61K31/277 , A61K31/341 , A61K31/343 , A61K31/351 , A61K31/352 , A61K31/381 , A61K31/415 , A61K31/4155 , A61K31/4164 , A61K31/4192 , A61K31/42 , A61K31/421 , A61K31/423 , A61K31/4245 , A61K31/426 , A61K31/428 , A61K31/429 , A61K31/433 , A61K31/4355 , A61K31/437 , A61K31/4375 , A61K31/4406 , A61K31/4412 , A61K31/443 , A61K31/445 , A61K31/455 , A61K31/47 , A61K31/4725 , A61K31/496 , A61K31/498 , A61K31/50 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/53 , A61K31/5375 , A61K31/5377 , A61P31/12 , C07C335/18 , C07C335/20 , C07D211/20 , C07D211/22 , C07D211/46 , C07D211/60 , C07D211/64 , C07D211/78 , C07D213/56 , C07D213/75 , C07D213/82 , C07D213/84 , C07D213/85 , C07D215/54 , C07D231/14 , C07D233/54 , C07D233/60 , C07D233/90 , C07D237/24 , C07D239/28 , C07D241/24 , C07D241/42 , C07D241/44 , C07D253/06 , C07D253/07 , C07D261/18 , C07D263/34 , C07D263/58 , C07D265/30 , C07D271/12 , C07D277/20 , C07D277/56 , C07D277/68 , C07D285/06 , C07D295/10 , C07D295/14 , C07D295/15 , C07D307/68 , C07D307/84 , C07D307/85 , C07D309/38 , C07D311/04 , C07D311/58 , C07D333/38 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07D419/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D491/048 , C07D495/04 , C07D513/04
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 A 1 , A 2 , R 1 , R 2 , 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， 2，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。治疗方法包括施用式（I）化合物作为单一活性剂或与一种或多种其它治疗剂组合施用式（I）化合物。

5. 发明申请

WO2005067900A3 AZABENZOFURAN SUBSTITUTED THIOUREAS AS INHIBITORS OF VIRAL REPLICATION 审中-公开
标题翻译：作为病毒复制的抑制剂的AZABENZOFURAN替代THI
公开(公告)号：WO2005067900A3
公开(公告)日：2005-09-29
申请号：PCT/US2005000339
申请日：2005-01-05
申请人： ACHILLION PHARMACEUTICALS INC , THURKAUF ANDREW , CHEN DAWEI , PHADKE AVINASH , LI SHOUMING , DESHPANDE MILIND
发明人： THURKAUF ANDREW , CHEN DAWEI , PHADKE AVINASH , LI SHOUMING , DESHPANDE MILIND
IPC分类号： A61K31/00 , A61K31/4355 , A61K31/4741 , A61K38/21 , C07D471/04 , C07D491/02 , C07D491/04 , A61P31/14
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，A1，A2，A3，A4，R5，R6，R7，V，W，X和Y在本文中定义。某些本文所述的式（1）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。本发明还提供了含有一种或多种式（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）化合物或将式（1）的化合物与一种或多种其它治疗剂组合施用。

6. 发明申请

WO2005007601A3 SUBSTITUTED ARYLTHIOUREA DERIVATIVES USEFUL AS INHIBITORS OF VIRAL REPLICATION 审中-公开
标题翻译：作为病毒复制的抑制剂有用的替代芳香酶衍生物
公开(公告)号：WO2005007601A3
公开(公告)日：2005-06-23
申请号：PCT/US2004022599
申请日：2004-07-08
申请人： ACHILLION PHARMACEUTICALS INC , PHADKE AVINASH , QUINN JESSE , OHKANDA JUNKO , THURKAUF ANDREW , SHEN YIPING , LIU CUIXIAN , CHEN DAWEI , LI SHOUMING
发明人： PHADKE AVINASH , QUINN JESSE , OHKANDA JUNKO , THURKAUF ANDREW , SHEN YIPING , LIU CUIXIAN , CHEN DAWEI , LI SHOUMING
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。

7. 发明申请

WO2005095345A3 HETEROARYL GUANIDINES AS INHIBITORS OF VIRAL REPLICATION 审中-公开
标题翻译：作为病毒复制抑制剂的异氟烷类药物
公开(公告)号：WO2005095345A3
公开(公告)日：2005-12-01
申请号：PCT/US2005009710
申请日：2005-03-23
申请人： ACHILLION PHARMACEUTICALS INC , CHEN XI , LIU CIUXAN , THURKAUF ANDREW , LOUISE-MAY SHIRLEY
发明人： CHEN XI , LIU CIUXAN , THURKAUF ANDREW , LOUISE-MAY SHIRLEY
IPC分类号： A61K31/44 , A61K31/505 , A61K31/517 , C07C279/18 , C07D213/75 , C07D213/82 , C07D239/54 , C07D239/545 , C07D239/84 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D417/12 , A61P31/14
CPC分类号： C07C279/18 , C07D213/75 , C07D213/82 , C07D239/42 , C07D239/47 , C07D239/545 , C07D239/84 , C07D401/12 , C07D403/12 , C07D405/12 , C07D417/12
摘要： Compounds of Formula (1), and pharmaceutically acceptable forms thereof, are provided wherein the variables X, Y, Z, Al, R2, R3, R4, R5 and R6 are defined herein. Certain compounds of Formula 1 described herein which possess potent antiviral activity. Certain compounds of Formula (1) that are potent and/ or selective inhibitors of Hepatitis C virus replication. 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 are also provided. 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 or disorder are disclosed. These infectious diseases include viral infections, particularly HCV infections. 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：提供式（1）的化合物及其药学上可接受的形式，其中变量X，Y，Z，Al，R 2，R 3，R 4，R 5和R 6在本文中定义。某些本文所述的具有强抗病毒活性的式1的化合物。某些式（1）化合物是丙型肝炎病毒复制的有效和/或选择性抑制剂。还提供了含有一种或多种式（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。公开了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（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。治疗患有感染性疾病的人类患者的方法，还包括治疗其他动物，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）化合物或将式（1）的化合物与一种或多种其它治疗剂组合施用。

8. 发明专利

DE602005023266D1 AZABENZOFURANSUBSTITUIERTE THIOHARNSTOFFE ALS INHIBITOREN DER VIRUSREPLIKATION 未知
公开(公告)号：DE602005023266D1
公开(公告)日：2010-10-14
申请号：DE602005023266
申请日：2005-01-05
申请人： ACHILLION PHARMACEUTICALS INC
发明人： THURKAUF ANDREW , CHEN DAWEI , PHADKE AVINASH , LI SHOUMING , DESHPANDE MILIND
IPC分类号： C07D471/04 , A61K31/00 , A61K31/4355 , A61K31/4741 , A61K38/21 , A61P31/14 , C07D491/02 , C07D491/04

9. 发明专利

NZ544674A Substituted arylthiourea derivatives useful as inhibitors of viral replication 未知
公开(公告)号：NZ544674A
公开(公告)日：2009-03-31
申请号：NZ54467404
申请日：2004-07-08
申请人： ACHILLION PHARMACEUTICALS INC
发明人： PHADKE AVINASH , QUINN JESSE , OHKANDA JUNKO , THURKAUF ANDREW , SHEN YIPING , LIU CUIXIAN , CHEN DAWEI , LI SHOUMING , WANG XIANGZHU
IPC分类号： A61K31/17 , A61K31/44 , C07C15/00 , C07C335/14 , C07C335/16 , C07D213/54 , A61P31/14 , C07C335/04
摘要： Disclosed is a substituted arylthiourea of formula I or a pharmaceutically acceptable salt thereof, wherein z is 0, 1, or 2; R is hydrogen, methyl, or ethyl; A1 is nitrogen or CR1, A2 is nitrogen or CR2, A3 is nitrogen or CR3, A4 is nitrogen or CR4, or A5 is nitrogen or CR5; where one or none of A1-5 is nitrogen and the rest are CR1-5 and the rest of the substituents are disclosed within the specification. Also disclosed is the use of the above compound in the manufacture of a medicament for treating Hepatitis C infections.

10. 发明专利

OA13357A Azabenzofuran substituted thioureas as inhibitors of viral replication. 未知
公开(公告)号：OA13357A
公开(公告)日：2007-04-13
申请号：OA1200600222
申请日：2005-01-05
申请人： ACHILLION PHARMACEUTICALS INC
发明人： CHEN DAWEI , DESHPANDE MILIND , LI SHOUMING , PHADKE AVINASH , THURKAUF ANDREW
IPC分类号： A61K31/00 , A61K31/4355 , A61K31/4741 , A61K38/21 , C07D471/04 , C07D491/02 , C07D491/04
摘要： The present invention provides compounds of Formula 1, wherein the variables Ar, A 1 , A 2 , A 3 , A 4 , R 5 , R 6 , R 7 , 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.

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