公开(公告)号：US20140113890A1

公开(公告)日：2014-04-24

申请号：US14139196

申请日：2013-12-23

Applicant: 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

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

CPC classification number: 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

Abstract: 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.

Abstract translation: 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

Applicant: Suoming Zhang ,  Avinash Phadke ,  Milind Deshpande ,  Venkat Gadhachanda

Inventor： Suoming Zhang ,  Avinash Phadke ,  Milind Deshpande ,  Venkat Gadhachanda

IPC: A61K38/00 ,  A01N37/18

CPC classification number: C07K5/0808 ,  C07K5/0819

Abstract: 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.

Abstract translation: 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：US08183263B2

公开(公告)日：2012-05-22

申请号：US12125554

申请日：2008-05-22

Applicant: Xiangzhu Wang ,  Suoming Zhang ,  Venkat Gadhachanda ,  Cuixian Liu ,  Jesse Quinn ,  Shouming Lee ,  Dawei Chen ,  Milind Deshpande ,  Avinash Phadke

Inventor： Xiangzhu Wang ,  Suoming Zhang ,  Venkat Gadhachanda ,  Cuixian Liu ,  Jesse Quinn ,  Shouming Lee ,  Dawei Chen ,  Milind Deshpande ,  Avinash Phadke

IPC: A01N43/40 ,  A61K31/44 ,  C07D417/04 ,  C07D417/14

CPC classification number: C07D417/04

Abstract: 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.

Abstract translation: 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

Applicant: Suoming Zhang ,  Avinash Phadke ,  Cuixian Liu ,  Xiangzhu Wang ,  Jesse Quinn ,  Dawei Chen ,  Venkat Gadhachanda ,  Shouming Li ,  Milind Deshpande

Inventor： Suoming Zhang ,  Avinash Phadke ,  Cuixian Liu ,  Xiangzhu Wang ,  Jesse Quinn ,  Dawei Chen ,  Venkat Gadhachanda ,  Shouming Li ,  Milind Deshpande

IPC: A61K31/426 ,  A61K31/44

CPC classification number: C07D487/04 ,  C07D277/38 ,  C07D277/42 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D513/04

Abstract: 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.

Abstract translation: 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：US08697641B2

公开(公告)日：2014-04-15

申请号：US12635049

申请日：2009-12-10

Applicant: Avinash Phadke ,  Xiangzhu Wang ,  Godwin Pais ,  Akihiro Hashimoto ,  Venkat Gadhachanda ,  Dawei Chen ,  Atul Agarwal ,  Suoming Zhang ,  Cuixian Liu ,  Shouming Li ,  Milind Deshpande

Inventor： Avinash Phadke ,  Xiangzhu Wang ,  Godwin Pais ,  Akihiro Hashimoto ,  Venkat Gadhachanda ,  Dawei Chen ,  Atul Agarwal ,  Suoming Zhang ,  Cuixian Liu ,  Shouming Li ,  Milind Deshpande

IPC: A01N37/18

Abstract: 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.

公开(公告)号：US20100152103A1

公开(公告)日：2010-06-17

申请号：US12635049

申请日：2009-12-10

Applicant: Avinash Phadke ,  Xiangzhu Wang ,  Godwin Pais ,  Akihiro Hashimoto ,  Venkat Gadhachanda ,  Dawei Chen ,  Atul Agarwal ,  Suoming Zhang ,  Cuixian Liu ,  Shouming Li ,  Milind Deshpande

Inventor： Avinash Phadke ,  Xiangzhu Wang ,  Godwin Pais ,  Akihiro Hashimoto ,  Venkat Gadhachanda ,  Dawei Chen ,  Atul Agarwal ,  Suoming Zhang ,  Cuixian Liu ,  Shouming Li ,  Milind Deshpande

IPC: A61K38/12 ,  C07K5/12 ,  A61P31/12

CPC classification number: C07K5/12 ,  A61K38/00 ,  C07K5/06165

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20070004711A1

公开(公告)日：2007-01-04

申请号：US11431155

申请日：2006-05-09

Applicant: Suoming Zhang ,  Avinash Phadke ,  Cuixian Liu ,  Xiangzhu Wang ,  Jesse Quinn ,  Dawei Chen ,  Venkat Gadhachanda ,  Shouming Li ,  Milind Deshpande

Inventor： Suoming Zhang ,  Avinash Phadke ,  Cuixian Liu ,  Xiangzhu Wang ,  Jesse Quinn ,  Dawei Chen ,  Venkat Gadhachanda ,  Shouming Li ,  Milind Deshpande

IPC: A61K31/541 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/426

CPC classification number: C07D487/04 ,  C07D277/38 ,  C07D277/42 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D513/04

Abstract: 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.

Abstract translation: 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 3， 4，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：US09125904B1

公开(公告)日：2015-09-08

申请号：US13105504

申请日：2011-05-11

Applicant: Jason Allan Wiles ,  Venkat Gadhachanda ,  Dawei Chen ,  Qiuping Wang ,  Akihiro Hashimoto ,  Godwin Pais ,  Xiangzhu Wang ,  Milind Deshpande ,  Avinash Phadke

Inventor： Jason Allan Wiles ,  Venkat Gadhachanda ,  Dawei Chen ,  Qiuping Wang ,  Akihiro Hashimoto ,  Godwin Pais ,  Xiangzhu Wang ,  Milind Deshpande ,  Avinash Phadke

IPC: A61K31/44 ,  A61K31/47 ,  A61K38/05 ,  A61K31/439 ,  A61K31/4709

CPC classification number: A61K31/439 ,  A61K31/4709 ,  A61K38/05 ,  A61K38/55 ,  A61K31/436 ,  A61K2300/00

Abstract: Biphenyl imidazoles and related compounds of Formula I, useful as antiviral agents, are provided herein. Pharmaceutical compositions containing a compound of Formula I, together with a second active agent, such as an NS3a protease inhibitor are provided herein. Methods for treating viral infections, including Hepatitis C infections, are included herein by providing a compound of Formula I together with an additional active agent. In certain embodiments the additional active agent is an NS3a protease inhibitor.

Abstract translation: 本文提供联苯基咪唑和可用作抗病毒剂的式I的相关化合物。 本文提供了含有式I化合物的药物组合物，以及第二活性剂，例如NS3a蛋白酶抑制剂。 本文通过提供式I化合物与另外的活性剂一起包括治疗病毒感染（包括丙型肝炎感染）的方法。 在某些实施方案中，另外的活性剂是NS3a蛋白酶抑制剂。

公开(公告)号：US20120302538A1

公开(公告)日：2012-11-29

申请号：US13482558

申请日：2012-05-29

Applicant: Jason Allan Wiles ,  Qiuping Wang ,  Akihiro Hashimoto ,  Godwin Pais ,  Xiangzhu Wang ,  Venkat Gadhachanda ,  Avinash Phadke ,  Milind Deshpande ,  Dawei Chen

Inventor： Jason Allan Wiles ,  Qiuping Wang ,  Akihiro Hashimoto ,  Godwin Pais ,  Xiangzhu Wang ,  Venkat Gadhachanda ,  Avinash Phadke ,  Milind Deshpande ,  Dawei Chen

IPC: A61K31/4178 ,  A61K31/4184 ,  C07F17/02 ,  A61P31/14 ,  C07D471/08 ,  A61K31/439 ,  A61K31/496 ,  C07D403/14 ,  A61K31/555

CPC classification number: 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

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20100124545A1

公开(公告)日：2010-05-20

申请号：US12622753

申请日：2009-11-20

Applicant: Suoming Zhang ,  Avinash Phadke ,  Milind Deshpande ,  Venkat Gadhachanda

Inventor： Suoming Zhang ,  Avinash Phadke ,  Milind Deshpande ,  Venkat Gadhachanda

IPC: A61K38/21 ,  A61K38/12 ,  A61K31/7056 ,  A61K31/47 ,  C07K5/12 ,  C07D215/233 ,  A61P31/12

CPC classification number: C07K5/0808 ,  C07K5/0819

Abstract: 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.

Abstract translation: 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。