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1. 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。

2. 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。

3. 发明申请

WO2010068760A3 NEW 4-AMINO-4-OXOBUTANOYL PEPTIDES AS INHIBITORS OF VIRAL REPLICATION 审中-公开
标题翻译：新的4-氨基-4-氧代丁酰基肽作为病毒复制的抑制剂
公开(公告)号：WO2010068760A3
公开(公告)日：2010-10-14
申请号：PCT/US2009067506
申请日：2009-12-10
申请人： ACHILLION PHARMACEUTICALS INC , PHADKE AVINASH , CHEN DAWEI , GADHACHANDA VENKAT , HASHIMOTO AKIHIRO , PAIS GODWIN , WANG XIANGZHU , AGARWAL ATUL , KIM HA YOUNG , LI SHOUMING , LIU CUIXIAN , ZHANG SUOMING , DESHPANDE MILIND
发明人： PHADKE AVINASH , CHEN DAWEI , GADHACHANDA VENKAT , HASHIMOTO AKIHIRO , PAIS GODWIN , WANG XIANGZHU , AGARWAL ATUL , KIM HA YOUNG , LI SHOUMING , LIU CUIXIAN , ZHANG SUOMING , DESHPANDE MILIND
IPC分类号： C07D403/14 , A61K31/437 , A61P31/12 , C07D413/14
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用盐和水合物。变量R，R1，R6-R8，R16，R18，R19，M，n，T，Y和Z在本文中定义。式I的某些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。本发明还提供了含有一种或多种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。这种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可以含有4-氨基-4-氧代丁酰基肽和一种或多种其他药物活性剂的组合。本发明还提供了治疗病毒感染（包括丙型肝炎感染）的方法。

4. 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。

5. 发明申请

WO2010068761A3 4-AMINO-4-OXOBUTANOYL PEPTIDE CYCLIC ANALOGUES, INHIBITORS OF VIRAL REPLICATION 审中-公开
标题翻译： 4-氨基-4-氧杂多酚类环状类似物，病毒复制抑制剂
公开(公告)号：WO2010068761A3
公开(公告)日：2010-10-21
申请号：PCT/US2009067507
申请日：2009-12-10
申请人： ACHILLION PHARMACEUTICALS INC , PHADKE AVINASH , WANG XIANGZHU , PAIS GODWIN , HASHIMOTO AKIHIRO , GADHACHANDA VENKAT , CHEN DAWEI , AGARWAL ATUL , ZHANG SUOMING , LIU CUIXIAN , LI SHOUMING , DESHPANDE MILIND
发明人： PHADKE AVINASH , WANG XIANGZHU , PAIS GODWIN , HASHIMOTO AKIHIRO , GADHACHANDA VENKAT , CHEN DAWEI , AGARWAL ATUL , ZHANG SUOMING , LIU CUIXIAN , LI SHOUMING , DESHPANDE MILIND
IPC分类号： C07D403/14 , C07D403/12 , C07D417/14
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。

6. 发明申请

WO2008147557A3 HETEROARYL SUBSTITUTED THIAZOLES AND THEIR USE AS ANTIVIRAL AGENTS 审中-公开
标题翻译： HETEROARYL替代THIAZOLES及其作为抗病毒剂的使用
公开(公告)号：WO2008147557A3
公开(公告)日：2009-03-05
申请号：PCT/US2008006676
申请日：2008-05-22
申请人： ACHILLION PHARMACEUTICALS INC , WANG XIANGZHU , ZHANG SUOMING , GADHACHANDA VENKAT , LIU CUIXIAN , LI SHOUMING , QUINN JESSE , CHEN DAWEI , DESHPANDE MILIND , PHADKE AVINASH
发明人： WANG XIANGZHU , ZHANG SUOMING , GADHACHANDA VENKAT , LIU CUIXIAN , LI SHOUMING , QUINN JESSE , CHEN DAWEI , DESHPANDE MILIND , PHADKE AVINASH
IPC分类号： C07D417/04 , A61K31/4436 , A61P31/12
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，包括使用该化合物治疗丙型肝炎病毒的方法。

7. 发明申请

WO2006122011A3 THIAZOLE COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：噻唑化合物及其使用方法
公开(公告)号：WO2006122011A3
公开(公告)日：2007-05-03
申请号：PCT/US2006017692
申请日：2006-05-09
申请人： ACHILLION PHARMACEUTICALS INC , ZHANG SUOMING , PHADKE AVINASH , LIU CUIXIAN , WANG XIANGZHU , QUINN JESSE , CHEN DAWEI , GADHACHANDA VENKAT , LI SHOUMING , DESHPANDE MILIND
发明人： ZHANG SUOMING , PHADKE AVINASH , LIU CUIXIAN , WANG XIANGZHU , QUINN JESSE , CHEN DAWEI , GADHACHANDA VENKAT , LI SHOUMING , DESHPANDE MILIND
IPC分类号： A61K31/426 , A61K31/427 , A61P31/12 , C07D277/38 , C07D277/42 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D487/04 , C07D513/04
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 Ar 1 R 2 , R 3 , R 4 , 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Ar 1 R 2，R 3，R 4 本文中定义的是，r，q和t。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。

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