公开(公告)号：US20100029652A1

公开(公告)日：2010-02-04

申请号：US12519470

申请日：2007-12-17

申请人： Mingjun Huang ,  Joanne Fabrycki ,  Wengang Yang ,  Xingtie Nie ,  Avinash Phadke ,  Milind Deshpande

发明人： Mingjun Huang ,  Joanne Fabrycki ,  Wengang Yang ,  Xingtie Nie ,  Avinash Phadke ,  Milind Deshpande

IPC分类号： A61K31/5377 ,  A61K31/17 ,  A61K31/44 ,  A61K31/497 ,  A61K31/4965

CPC分类号： A61K31/17 ,  A61K45/06 ,  A61K2300/00

摘要： The invention provides a method of treating hepatitis C, by providing compound of Formula I (shown below) in combination with a second active agent to a patient infected with the hepatitis C virus. Also provided herein are pharmaceutical combinations comprising a compound of Formula I and a second active agent. The pharmaceutical combination may be a unit dosage form or a packaged pharmaceutical composition. Packaged pharmaceutical combinations include a compound of Formula I and a second active agent in a package with instructions for using the formulation to treat a hepatitis C infection.

摘要翻译： 本发明提供一种治疗丙型肝炎的方法，其通过向感染丙型肝炎病毒的患者提供式I化合物（如下所示）与第二活性剂的组合。 本文还提供包含式I化合物和第二活性剂的药物组合。 药物组合可以是单位剂型或包装的药物组合物。 包装的药物组合包括式I化合物和包装中的第二活性剂，其中使用该制剂治疗丙型肝炎感染的说明书。

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。

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。

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。

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：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。

公开(公告)号：US20140113890A1

公开(公告)日：2014-04-24

申请号：US14139196

申请日：2013-12-23

申请人： Avinash Phadke ,  Dawei Chen ,  Venkat Gadhachanda ,  Akihiro Hashimoto ,  Godwin Pais ,  Xiangzhu Wang ,  Atul Agarwal ,  Ha Young Kim ,  Shuoming Li ,  Cuixian Liu ,  Suoming Zhang ,  Milind Deshpande

发明人： Avinash Phadke ,  Dawei Chen ,  Venkat Gadhachanda ,  Akihiro Hashimoto ,  Godwin Pais ,  Xiangzhu Wang ,  Atul Agarwal ,  Ha Young Kim ,  Shuoming Li ,  Cuixian Liu ,  Suoming Zhang ,  Milind Deshpande

IPC分类号： C07D207/16 ,  C07D401/14 ,  C07D413/14 ,  C07D417/12 ,  C07D409/14 ,  C07D491/113 ,  C07D487/18 ,  C07D417/14 ,  C07D401/12 ,  C07D403/12

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学上可接受的盐和水合物。 变量R，R1，R6-R8，R16，R18，R19，M，n，T，Y和Z在本文中定义。 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。 本发明还提供含有一种或多种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。 这样的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，或者可以含有4-氨基-4-氧代丁酰基肽和一种或多种其它药物活性剂的组合。 本发明还提供了治疗病毒感染的方法，包括丙型肝炎感染。

公开(公告)号：US08445430B2

公开(公告)日：2013-05-21

申请号：US12622753

申请日：2009-11-20

申请人： Suoming Zhang ,  Avinash Phadke ,  Milind Deshpande ,  Venkat Gadhachanda

发明人： Suoming Zhang ,  Avinash Phadke ,  Milind Deshpande ,  Venkat Gadhachanda

IPC分类号： A61K38/00 ,  A01N37/18

CPC分类号： C07K5/0808 ,  C07K5/0819

摘要： The invention provides cyclic carboxamide compounds and analogues thereof 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. Certain cyclic carboxamide compounds and cyclic carboxamide analogues 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 cyclic carboxamide compounds or cyclic carboxamide analogues and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a cyclic carboxamide compound or cyclic carboxamide analogue as the only active agent or may contain a combination of a cyclic carboxamide compound or cyclic carboxamide analogue 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的环状羧酰胺化合物及其类似物及其药学上可接受的盐和水合物。 变量R，R1，R6-R8，R16，R18，R19，M，n，T，Y和Z在本文中定义。 某些式I化合物可用作抗病毒剂。 本文公开的某些环状羧酰胺化合物和环状羧酰胺类似物是有效和/或选择性的病毒复制抑制剂，特别是丙型肝炎病毒复制。 本发明还提供含有一种或多种环状羧酰胺化合物或环状甲酰胺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环状羧酰胺化合物或环状羧酰胺类似物作为唯一的活性剂，或者可以含有环状羧酰胺化合物或环状甲酰胺类似物和一种或多种其它药学活性剂的组合。 本发明还提供了治疗病毒感染的方法，包括丙型肝炎感染。

公开(公告)号：US08173636B2

公开(公告)日：2012-05-08

申请号：US12754057

申请日：2010-04-05

申请人： Barton James Bradbury ,  Milind Deshpande ,  Akihiro Hashimoto ,  Ha Young Kim ,  Edlaine Lucien ,  Godwin Pais ,  Michael Pucci ,  Qiuping Wang ,  Jason Allan Wiles ,  Avinash Phadke

发明人： Barton James Bradbury ,  Milind Deshpande ,  Akihiro Hashimoto ,  Ha Young Kim ,  Edlaine Lucien ,  Godwin Pais ,  Michael Pucci ,  Qiuping Wang ,  Jason Allan Wiles ,  Avinash Phadke

IPC分类号： C07D495/04 ,  A61K31/4743 ,  A61K31/496

CPC分类号： A61K31/4743 ,  A61K31/496 ,  C07D495/04 ,  C07D498/16 ,  C07D519/00

摘要： Disclosed herein are hydroxylthienoquinolones and related compounds and their pharmaceutically acceptable salts useful as antiviral agents and having the general formula in which the variables R2, R6, and R7 are defined herein. Certain compounds provided herein possess potent antibacterial, antiprotozoal, or antifungal activity and are particularly efficacious for the treatment of MRSA infections. The invention also provides pharmaceutical compositions, pharmaceutical compositions containing a hydroxylthienoquinolone in combination with one or more other active agent, and methods of treating microbial infections in animals by administering an effective amount of a hydroxylthienoquinolone or related compound to an animal suffering from a microbial infection.

摘要翻译： 本文公开的是羟基噻吩并喹啉酮和相关化合物及其药学上可接受的盐，其可用作抗病毒剂并具有通式，其中变量R2，R6和R7在本文中定义。 本文提供的某些化合物具有有效的抗细菌，抗原生动物或抗真菌活性，并且对于治疗MRSA感染特别有效。 本发明还提供药物组合物，含有羟基噻吩并喹啉与一种或多种其它活性剂的药物组合物，以及通过向有微生物感染的动物施用有效量的羟基噻吩并喹啉酮或相关化合物来治疗动物微生物感染的方法。