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1. 发明申请

US20160016986A1 STABILIZED NUCLEOTIDES FOR MEDICAL TREATMENT 审中-公开
标题翻译：稳定的药物治疗核心
公开(公告)号：US20160016986A1
公开(公告)日：2016-01-21
申请号：US14805421
申请日：2015-07-21
申请人： Milind Deshpande , Jason Allan Wiles , Akihiro Hashimoto , Avinash Phadke
发明人： Milind Deshpande , Jason Allan Wiles , Akihiro Hashimoto , Avinash Phadke
IPC分类号： C07H19/10 , C07H19/056 , A61K31/7056 , A61K31/7072
CPC分类号： C07H19/10 , A61K31/7056 , A61K31/7072 , C07B59/005 , C07H19/056 , C07H19/11
摘要： 5′-Deuterated nucleosides and nucleotides and modifications thereof are provided for use in medical therapies, including as antiviral, anti-tumor and anti-neoplastic agents. In one embodiment, compounds, methods and uses are provided for the treatment of hepatitis C, RSV, HSV and other viral diseases in a host, including a human.
摘要翻译： 5'-脱唾液酸核苷及其核苷酸及其修饰被提供用于医学疗法，包括抗病毒，抗肿瘤和抗肿瘤剂。在一个实施方案中，提供化合物，方法和用途用于在宿主（包括人）中治疗丙型肝炎，RSV，HSV和其它病毒性疾病。

2. 发明授权

US08183263B2 Heteroaryl substituted thiazoles 失效
标题翻译：杂芳基取代的噻唑
公开(公告)号：US08183263B2
公开(公告)日：2012-05-22
申请号：US12125554
申请日：2008-05-22
申请人： Xiangzhu Wang , Suoming Zhang , Venkat Gadhachanda , Cuixian Liu , Jesse Quinn , Shouming Lee , Dawei Chen , Milind Deshpande , Avinash Phadke
发明人： Xiangzhu Wang , Suoming Zhang , Venkat Gadhachanda , Cuixian Liu , Jesse Quinn , Shouming Lee , Dawei Chen , Milind Deshpande , Avinash Phadke
IPC分类号： A01N43/40 , A61K31/44 , C07D417/04 , C07D417/14
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。

3. 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。

4. 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。

5. 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。

6. 发明申请

US20090304605A1 Substituted Aminothiazole Prodrugs of Compounds with Anti-HCV Activity 失效
标题翻译：具有抗HCV活性的化合物的取代的氨基噻唑前体药物
公开(公告)号：US20090304605A1
公开(公告)日：2009-12-10
申请号：US12479213
申请日：2009-06-05
申请人： Cuixan Liu , Avinash Phadke , Xiangzhu Wang , Suoming Zhang
发明人： Cuixan Liu , Avinash Phadke , Xiangzhu Wang , Suoming Zhang
IPC分类号： A61K9/12 , C07D417/04 , A61K31/4439 , A61K31/675 , C07F9/58 , A61P31/12
CPC分类号： C07D417/04 , C07D417/14
摘要： The invention provides amino-substituted aminothiazole compounds of Formula I and Formula II where A is a group of the formula: and the variables X, Y, R, and R1 to R7 are described herein. These compounds are prodrugs of compounds useful as inhibitors of viral replication. Compositions containing such compounds, and methods of treating viral infections with these compounds, as well as to processes and intermediates useful for preparing such compounds are also provided by the invention.
摘要翻译：本发明提供式I和式II的氨基取代的氨基噻唑化合物，其中A是下式的基团：变量X，Y，R 1和R 1至R 7在本文中描述。这些化合物是可用作病毒复制抑制剂的化合物的前药。含有这些化合物的组合物，以及用这些化合物治疗病毒感染的方法，以及可用于制备这些化合物的方法和中间体也由本发明提供。

7. 发明申请

US20070213301A1 Substituted Aminothiazole Derivatives With Anti-HCV Activity 审中-公开
标题翻译：具有抗HCV活性的取代的氨基噻唑衍生物
公开(公告)号：US20070213301A1
公开(公告)日：2007-09-13
申请号：US11683749
申请日：2007-03-08
申请人： Souming Zhang , Xiangzhu Wang , Cuixian Liu , Avinash Phadke
发明人： Souming Zhang , Xiangzhu Wang , Cuixian Liu , Avinash Phadke
IPC分类号： A61K31/675 , A61K31/538 , A61K31/5377 , A61K31/53 , A61K31/506 , A61K31/497 , A61K31/4439 , C07D417/02
CPC分类号： C07D277/46 , C07D277/42 , C07D277/48 , C07D277/50 , C07D277/56 , C07D417/04 , C07D417/12 , C07D417/14 , C07F9/6539 , C07F9/65583
摘要： The invention provides amino-substituted aminothiazole compounds of Formula I in which A is a group of the formula: and the variables R and R1 to R7 are described herein. These compounds are useful as inhibitors of viral replication. Compositions containing such compounds, and methods of treating viral infections with these compounds, as well as to processes and intermediates useful for preparing such compounds are also provided by the invention.
摘要翻译：本发明提供式I的氨基取代的氨基噻唑化合物，其中A是下式的基团：变量R和R 1至R 7在本文中描述。这些化合物可用作病毒复制的抑制剂。含有这些化合物的组合物，以及用这些化合物治疗病毒感染的方法，以及可用于制备这些化合物的方法和中间体也由本发明提供。

8. 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.

9. 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。

10. 发明授权

US08809313B2 Substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes useful for treating HCV infections 有权
标题翻译：用于治疗HCV感染的取代的aliphanes，cyclophanes，heteraphanes，heterophanes，异质异烟肼和金属茂
公开(公告)号：US08809313B2
公开(公告)日：2014-08-19
申请号：US13482558
申请日：2012-05-29
申请人： Jason Allan Wiles , Qiuping Wang , Akihiro Hashimoto , Godwin Pais , Xiangzhu Wang , Venkat Gadhachanda , Avinash Phadke , Milind Deshpande , Dawei Chen
发明人： Jason Allan Wiles , Qiuping Wang , Akihiro Hashimoto , Godwin Pais , Xiangzhu Wang , Venkat Gadhachanda , Avinash Phadke , Milind Deshpande , Dawei Chen
IPC分类号： A61P31/14 , C07D471/08 , A61K31/439 , A61K31/496 , C07D403/14 , A61K31/555
CPC分类号： A61K31/4184 , A61K9/0053 , A61K9/20 , A61K31/4178 , A61K31/422 , A61K31/427 , A61K31/439 , A61K31/454 , A61K31/496 , A61K31/555 , A61K45/06 , A61K2300/00 , C07D209/42 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/14 , C07D417/14 , C07D453/06 , C07D471/08 , C07D491/10 , C07D491/113 , C07D519/00 , C07F5/025 , C07F15/02 , C07F17/02
摘要： The present disclosure provides substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes, of Formula I D-M-D (Formula I) useful as antiviral agents. In certain embodiments disclosed herein M is a group —P-A-P— where A is Certain substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions/and combinations containing one or more substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes and a pharmaceutically acceptable carrier are also provided by this disclosure. Methods for treating viral infections, including Hepatitis C viral infections are provided by the disclosure.
摘要翻译：本公开提供了可用作抗病毒剂的式I D-M-D（式I）的取代的阿片，环戊烷，异烟肼，杂异烟肼，杂异烟草和金属茂。在本文公开的某些实施方案中，M是基团-P-A-P-，其中A是本文公开的某些取代的阿氨苯酯，环戊烷，异烟肼，杂异烟肼，杂异烟草和金属茂是有效和/或选择性的病毒复制抑制剂，特别是丙型肝炎病毒复制。本公开内容还提供药物组合物和/或含有一种或多种取代的阿利膦，环戊二烯，异aph烷，异han嗪，杂异烟草和金属茂的药物组合物和药学上可接受的载体。通过本公开提供了治疗病毒感染的方法，包括丙型肝炎病毒感染。

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