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31. 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。

32. 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。

33. 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。

34. 发明授权

US08445430B2 Cyclic carboxamide compounds and analogues thereof as of hepatitis C virus 失效
标题翻译：环丙酰胺化合物及其类似物作为丙型肝炎病毒
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。

35. 发明授权

US08173636B2 Hydroxylthienoquinolones and related compounds as anti-infective agents 失效
标题翻译：羟基噻吩并喹啉酮和相关化合物作为抗感染剂
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。

36. 发明申请

US20050020560A1 Chlorins processing fused ring systems useful as photoselective compounds for photodynamic therapy 有权
标题翻译：用于光动力学治疗的紫杉烷加工稠环系统可用作光选择性化合物
公开(公告)号：US20050020560A1
公开(公告)日：2005-01-27
申请号：US10922974
申请日：2004-08-23
申请人： Byron Robinson , Dipanjan Sengupta , Avinash Phadke
发明人： Byron Robinson , Dipanjan Sengupta , Avinash Phadke
IPC分类号： A61K41/00 , C07D487/22 , A61K31/555
CPC分类号： C07D487/22 , A61K41/0057 , A61K41/0071
摘要： The present invention provides a process of preparation of naphthochlorins and other chlorins with annelated ring systems useful for photodynamic therapy and the compounds themselves. The method for producing naphthochlorin compounds include contacting compounds such as meso-(2′-hydroxymethyl)phenyl porphyrin or meso-(2′-N,N,N-trialkylaminomethyl)phenyl porphyrin precursors with at least one acid catalyst at sufficient temperature for a sufficient time to yield the desired conversion. In a similar manner chlorins possessing annelated ring systems may be made from compounds such as meso-(2′-hydroxymethyl)aryl porphyrins or meso-(2′-N,N,N-trialkylaminomethyl)phenyl porphyrin. The procedures described herein provide new routes for synthesizing naphthochlorins and chlorins with annelated ring systems.
摘要翻译：本发明提供了用于光动力学治疗和化合物本身的具有环状环系的萘并氯和其他二氢卟酚的制备方法。制造萘并二氢黄汞化合物的方法包括将内消旋 - （2'-羟甲基）苯基卟啉或中 - （2-N，N，N-三烷基氨基甲基）苯基卟啉前体的化合物与足够温度的至少一种酸催化剂接触，足够的时间产生所需的转化。类似地，具有环状环系的二氢卟酚可以由诸如中 - （2'-羟甲基）芳基卟啉或中 - （2-N，N，N-三烷基氨基甲基）苯基卟啉的化合物制备。本文所述的方法提供用于合成具有环状环系的萘并氯和二氢卟酚的新途径。

37. 发明授权

US06794505B1 Chlorins possessing fused ring systems useful as photoselective compounds for photodynamic therapy 有权
标题翻译：具有可用作光动力治疗的光选择性化合物的稠环体系的二氢卟酚
公开(公告)号：US06794505B1
公开(公告)日：2004-09-21
申请号：US09538980
申请日：2000-03-30
申请人： Byron C. Robinson , Dipanjan Sengupta , Avinash Phadke
发明人： Byron C. Robinson , Dipanjan Sengupta , Avinash Phadke
IPC分类号： C07D48722
CPC分类号： C07D487/22 , A61K41/0057 , A61K41/0071
摘要： The present invention provides a process of preparation of naphthochlorins and other chlorins with annelated ring systems useful for photodynamic therapy and the compounds themselves. The method for producing naphthochlorin compounds include contacting compounds such as meso-(2′-hydroxymethyl)phenyl porphyrin or meso-(2′-N,N,N-trialkylaminomethyl)phenyl porphyrin precursors with at least one acid catalyst at sufficient temperature for a sufficient time to yield the desired conversion. In a similar manner chlorins possessing annelated ring systems may be made from compounds such as meso-(2′-hydroxymethyl)aryl porphyrins or meso-(2′-N,N,N-trialkylaminomethyl)phenyl porphyrin. The procedures described herein provide new routes for synthesizing naphthochlorins and chlorins with annelated ring systems.
摘要翻译：本发明提供了用于光动力学治疗和化合物本身的具有环状环系的萘并氯和其他二氢卟酚的制备方法。制造萘并二氢黄汞化合物的方法包括将内消旋 - （2'-羟甲基）苯基卟啉或中 - （2-N，N，N-三烷基氨基甲基）苯基卟啉前体的化合物与足够温度的至少一种酸催化剂接触，足够的时间产生所需的转化。类似地，具有环状环系的二氢卟酚可以由诸如中 - （2'-羟甲基）芳基卟啉或中 - （2-N，N，N-三烷基氨基甲基）苯基卟啉的化合物制备。本文所述的方法提供用于合成具有环状环系的萘并氯和二氢卟酚的新途径。

38. 发明申请

US20130165471A1 2-SUBSTITUTED-THIENOQUINOLONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS 审中-公开
标题翻译：作为抗感染剂的2-取代的三硝基苯酚和相关化合物
公开(公告)号：US20130165471A1
公开(公告)日：2013-06-27
申请号：US13723860
申请日：2012-12-21
申请人： Avinash Phadke , Jason Allan Wiles
发明人： Avinash Phadke , Jason Allan Wiles
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： Disclosed herein are 2-substituted-thienoquinolones and related compounds and their pharmaceutically acceptable salts useful as antiviral agents and having the general formula in which the variables R2, R3, 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 2-substituted-thienoquinolone in combination with one or more other active agent, and methods of treating microbial infections in animals by administering an effective amount of a 2-substituted-thienoquinolone to an animal suffering from a microbial infection.
摘要翻译：本文公开了2-取代 - 噻吩并喹啉酮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，R3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2-取代 - 噻吩并喹啉酮与一种或多种其它活性剂的药物组合物，以及通过将有效量的2-取代噻吩并喹啉给予动物而治疗动物微生物感染的方法来自微生物感染。

39. 发明授权

US08106209B2 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药
公开(公告)号：US08106209B2
公开(公告)日：2012-01-31
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： C07D417/04 , A61K31/44
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。

40. 发明授权

US07906619B2 4-amino-4-oxobutanoyl peptides as inhibitors of viral replication 有权
标题翻译： 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：US07906619B2
公开(公告)日：2011-03-15
申请号：US11777745
申请日：2007-07-13
申请人： Avinash Phadke , Xiangzhu Wang , Suoming Zhang , Atul Agarwal
发明人： Avinash Phadke , Xiangzhu Wang , Suoming Zhang , Atul Agarwal
IPC分类号： A61K38/06
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 provides 4-amino-4-oxobutanoyl peptide compounds of Formula 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：本发明提供了式I的4-氨基-4-氧代丁酰基肽化合物及其药学上可接受的盐和水合物。变量R1-R9，R16，R18，R19，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。

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