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1. 发明申请

WO2010068760A2 NEW 4-AMINO-4-OXOBUTANOYL PEPTIDES AS INHIBITORS OF VIRAL REPLICATION 审中-公开
标题翻译：作为病毒复制的新型4-氨基-4-氧代戊酸酯
公开(公告)号：WO2010068760A2
公开(公告)日：2010-06-17
申请号：PCT/US2009/067506
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 , C07D413/14 , A61P31/12 , A61K31/437
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, R 1 , R 6 -R 8 , R 16 , R 18 , R 19 , 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。

2. 发明申请

WO2010068761A2 4-AMINO-4-OXOBUTANOYL PEPTIDE CYCLIC ANALOGUES, INHIBITORS OF VIRAL REPLICATION 审中-公开
标题翻译： 4-氨基-4-氧代丁酰基肽类环化类似物，病毒复制抑制剂
公开(公告)号：WO2010068761A2
公开(公告)日：2010-06-17
申请号：PCT/US2009/067507
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：本发明提供式I的4-氨基-4-氧代丁酰基肽及其环状类似物及其药用盐。变量在此定义。式I的某些化合物可用作抗病毒剂。如本文所公开的4-氨基-4-氧代丁酰基肽环类似物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-氧代丁酰基肽环类似物和一种或多种药学上可接受的载体的药物组合物。此类药物组合物可含有4-氨基-4-氧代丁酰基肽环状类似物作为唯一活性剂，或可含有4-氨基-4-氧代丁酰基肽环状类似物与一种或多种其他药物活性剂的组合。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。

3. 发明申请

WO2008147557A2 HETEROARYL SUBSTITUTED THIAZOLES 审中-公开
标题翻译： HETEROARYL取代THIAZOLES
公开(公告)号：WO2008147557A2
公开(公告)日：2008-12-04
申请号：PCT/US2008/006676
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 R 3 to R 7 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。

4. 发明申请

WO2006122011A2 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：WO2006122011A2
公开(公告)日：2006-11-16
申请号：PCT/US2006/017692
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 , C07D487/04
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。

5. 发明申请

WO2008106130A2 TERTIARY AMINE SUBSTITUTED PEPTIDES USEFUL AS INHIBITORS OF HCV REPLICATION 审中-公开
标题翻译：用于复制HCV的三价胺取代肽
公开(公告)号：WO2008106130A2
公开(公告)日：2008-09-04
申请号：PCT/US2008/002524
申请日：2008-02-26
申请人： ACHILLION PHARMACEUTICALS, INC. , AGARWAL, Atul , WANG, Xiangzhu , CHEN, Dawei , ZHANG, Suoming , PHADKE, Avinash
发明人： AGARWAL, Atul , WANG, Xiangzhu , CHEN, Dawei , ZHANG, Suoming , PHADKE, Avinash
IPC分类号： A61P31/14 , A61K38/06 , C07K5/08
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 R 1 -R 12 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）的叔胺取代的肽。本文描述式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的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。

6. 发明申请

WO2010059937A1 CYCLIC CARBOXAMIDE COMPOUNDS AND ANALOGUES THEREOF AS OF HEPATITIS C VIRUS 审中-公开
标题翻译：周期性羧酰胺化合物及其与乙型肝炎病毒的模拟物
公开(公告)号：WO2010059937A1
公开(公告)日：2010-05-27
申请号：PCT/US2009/065328
申请日：2009-11-20
申请人： ACHILLION PHARMACEUTICALS, INC. , ZHANG, Suoming , PHADKE, Avinash , DESHPANDE, Milind , GADHACHANDA, Venkat
发明人： ZHANG, Suoming , PHADKE, Avinash , DESHPANDE, Milind , GADHACHANDA, Venkat
IPC分类号： C07K5/02 , A61K38/00
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, R 1 , R 6 -R 8 , R 16 , R 18 , R 19 , 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，或者可以含有环状甲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。

7. 发明申请

WO2007103550A3 SUBSTITUTED AMINOTHIAZOLE DERIVATIVES WITH ANTI-HCV ACTIVITY 审中-公开
公开(公告)号：WO2007103550A3
公开(公告)日：2007-09-13
申请号：PCT/US2007/006023
申请日：2007-03-08
申请人： ACHILLION PHARMACEUTICALS, INC. , ZHANG, Suoming , PHADKE, Avinash , WANG, Xiangzhu , LIU, Cuixian
发明人： ZHANG, Suoming , PHADKE, Avinash , WANG, Xiangzhu , LIU, Cuixian
IPC分类号： C07D277/42 , C07D277/46 , C07D277/48 , C07D277/50 , C07D277/56 , C07D417/04 , C07D417/14 , C07F9/09 , A61K31/426 , A61K31/4436 , A61P31/14
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 R 1 to R 7 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.

8. 发明申请

WO2008008502A1 4-AMINO-4-OXOBUTANOYL PEPTIDES AS INHIBITORS OF VIRAL REPLICATION 审中-公开
标题翻译：作为病毒复制抑制剂的4-氨基-4-氧代哌啶
公开(公告)号：WO2008008502A1
公开(公告)日：2008-01-17
申请号：PCT/US2007/016018
申请日：2007-07-13
申请人： ACHILLION PHARMACEUTICALS, INC. , PHADKE, Avinash , WANG, Xiangzhu , ZHANG, Suoming
发明人： PHADKE, Avinash , WANG, Xiangzhu , ZHANG, Suoming
IPC分类号： C07K5/02 , C07K5/06 , A61K38/00 , C07K5/08
CPC分类号： A61K38/05 , A61K38/00 , A61K38/12 , A61K45/06 , C07K5/02 , C07K5/06078 , C07K5/06139 , C07K5/06165 , C07K5/06191 , C07K5/0808 , C07K5/12
摘要： The invention rovides 4-amino-4-oxobutanoyl peptide compounds of Formula I (I) and the pharmaceutically salts and hydrates thereof. The variables R1-R9, R16, R18 R19, n, M,, n, M,, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. Certain 4-amino-4-oxobutanoyl peptide compounds 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 compounds and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain 4-amino-4-oxobutanoyl peptide compound as the only active agent or may contain a combination of 4-amino-4-oxobutanoyl peptide containing peptides compound and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections, in mammals.
摘要翻译：本发明涉及式I（I）的4-氨基-4-氧代丁酰基肽化合物及其药用盐和水合物。变量R1-R9，R16，R18R19，n，M ,, n，M ,,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4-氨基-4-氧代丁酰基肽化合物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。本发明还提供含有一种或多种4-氨基-4-氧代丁酰基肽化合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-氧代丁酰基肽化合物作为唯一的活性剂，或者可以含有含有4-氨基-4-氧代丁酰基肽的肽化合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哺乳动物中的病毒感染（包括丙型肝炎感染）的方法。

9. 发明申请

WO2009149436A1 SUBSTITUTED AMINOTHIAZOLE PRODRUGS OF COMPOUNDS WITH ANTI-HCV ACTIVITY 审中-公开
标题翻译：具有抗HCV活性的化合物的取代的氨基苯唑酸
公开(公告)号：WO2009149436A1
公开(公告)日：2009-12-10
申请号：PCT/US2009/046549
申请日：2009-06-08
申请人： ACHILLION PHARMACEUTICALS, INC. , LIU, Cuixan , PHADKE, Avinash , WANG, Xiangzhu , ZHANG, Suoming
发明人： LIU, Cuixan , PHADKE, Avinash , WANG, Xiangzhu , ZHANG, Suoming
IPC分类号： C07D417/04 , C07D417/14 , A61K31/4436 , A61P1/00
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 R 1 to R 7 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。

10. 发明申请

WO2011060196A1 BORON-CONTAINING SMALL MOLECULES 审中-公开
标题翻译：含硼的小分子
公开(公告)号：WO2011060196A1
公开(公告)日：2011-05-19
申请号：PCT/US2010/056420
申请日：2010-11-11
申请人： ANACOR PHARMACEUTICALS, INC. , HERNANDEZ, Vincent, S. , LI, Xianfeng , ZHANG, Suoming , AKAMA, Tsutomu , ZHANG, Yanchen , LIU, Yang , PLATTNER, Jacob, J. , ALLEY, Michael, Kevin Richard , ZHOU, Yasheen , NEIMAN, James, A.
发明人： HERNANDEZ, Vincent, S. , LI, Xianfeng , ZHANG, Suoming , AKAMA, Tsutomu , ZHANG, Yanchen , LIU, Yang , PLATTNER, Jacob, J. , ALLEY, Michael, Kevin Richard , ZHOU, Yasheen , NEIMAN, James, A.
IPC分类号： C07F5/02 , A61K31/69 , A61K31/04
CPC分类号： C07F5/025
摘要： This invention relates to 6-substituted benzoxaborole compounds of the following formula and their use for treating bacterial infections.
摘要翻译：本发明涉及下式的6-取代苯并恶唑化合物及其用于治疗细菌感染的用途。

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