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公开(公告)号：EP2560649A1
公开(公告)日：2013-02-27
申请号：EP11718596.7
申请日：2011-04-22
发明人： VAN GOOR, Fredrick, F. , ALARGOVA, Rossitza, Gueorguieva , ALCACIO, Tim, Edward , AREKAR, Sneha, G. , JOHNSTON, Steven, C. , KADIYALA, Irina, Nikolaevna , KESHAVARZ-SHOKRI, Ali , KRAWIEC, Mariusz , LEE, Elaine, Chungmin , MEDEK, Ales , MUDUNURI, Praveen , SULLIVAN, Mark, Jeffrey , ZAMAN, Noreen, Tasneem , ZHANG, Beili , ZHANG, Yuegang , ZLOKARNIK, Gregor
IPC分类号： A61K31/4704 , A61K31/404 , A61K31/443
CPC分类号： A61K31/47 , A61K31/404 , A61K31/443 , A61K31/4433 , A61K31/4704 , G01N33/5032 , G01N2500/04 , A61K2300/00
摘要： The present invention relates to pharmaceutical compositions comprising a compound of Formula I in combination with one or both of a Compound of Formula II and/or a Compound of Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis.
摘要翻译： 本发明涉及药物组合物，其包含式I化合物与式II化合物和/或式III化合物中的一种或两种的组合。 本发明还涉及固体形式及其药物制剂，以及使用这些组合物治疗CFTR介导的疾病，特别是囊性纤维化的方法。
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公开(公告)号：EP3068776A1
公开(公告)日：2016-09-21
申请号：EP14802787.3
申请日：2014-11-12
发明人： NTI-ADDAE, Kwame, W. , WALDO, Michael , O'NEIL, Simon, Adam , VAN ALSTEN, John, Gregg , MACIKENAS, Dainius , MUDUNURI, Praveen , SHI, Yi , LEDEBOER, Mark, Willem , JURKAUSKAS, Valdas , MEDEK, Ales , JONES, Steven , BYRN, Randal , ASMAL, Mohammed , ROBERTSON, Sarah, Marie , TSAI, Wanjung
IPC分类号： C07D403/04 , C07D471/04 , A61K31/506 , A61P31/16
CPC分类号： C07D471/04 , A61K31/16 , A61K31/351 , A61K31/4965 , A61K31/506 , A61K45/06 , C07C309/30 , C07D403/04
摘要： Polymorphic forms of Compound (1) or a pharmaceutically acceptable salt thereof, wherein Compound (1) is represented by the following structural formula: are Form A of HCl salt of Compound (1).½H2O, Form F of HCl salt of Compound (1).3H2O, Form D of HCl salt of Compound (1), Form A of Compound (1), and Form A of tosylate salt of Compound (1). Such polymorphic forms are employed for treating influenza, inhibiting the replication of influenza viruses, or reducing the amount of influenza viruses in a biological sample or in a subject.
摘要翻译： 化合物（1）的多晶型或其药学上可接受的盐，其中化合物（1）由以下结构式表示：化合物（1）的HCl盐的形式A。化合物（1）的HCl盐的形式F ）.3H 2 O，化合物（1）的HCl盐的形式D，化合物（1）的形式A和化合物（1）的甲苯磺酸盐的形式A. 这样的多晶型用于治疗流感，抑制流感病毒的复制，或减少生物样品或受试者中流感病毒的数量。
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公开(公告)号：EP3424920A1
公开(公告)日：2019-01-09
申请号：EP18188034.5
申请日：2014-10-17
发明人： NTI-ADDAE, Kwame, Wiredu , O'NEIL, Simon Adam , ZHANG, Yuegang , MUDUNURI, Praveen , VAN ALSTEN, John Gregg , SONG, Bin , STAVROPOULOS, Kathy , STROHMEIER, Mark , WALDO, Michael , NAVAMAL, Mettachit , KADIYALA, Irina Nikolaevna
IPC分类号： C07D401/14 , A61K31/506 , A61P35/00
摘要： The present invention relates to compositions and co-crystals each comprising a compound of formula I having the structure:
wherein each of R 1 and R 2 is H or 2 H and a co-crystal former selected from adipic acid, citric acid, fumaric acid, maleic acid, succinic acid, or benzoic acid. Also within the scope of this invention are methods of making and using the same.-
4.发明公开
公开(公告)号：EP2828277A1
公开(公告)日：2015-01-28
申请号：EP13712046.5
申请日：2013-03-11
发明人： KULDIPKUMAR, Anuj, K. , MEDEK, Ales , FERRIS, Lori, Ann , MUDUNURI, Praveen , JUNG, Young, Chun , WILLCOX, David, Richard , WALDO, Michael , NUGENT, William, Aloysius
IPC分类号： C07H19/06 , A61K31/7072 , A61P31/14
CPC分类号： C07H19/10 , A61K31/7056 , A61K31/706 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K38/00 , A61K45/06 , C07B2200/13 , C07H19/06 , A61K2300/00
摘要： The present application relates to solid state forms, for example, crystalline forms of 2′-C-methyluridine-5′-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, pharmaceutical compositions that can include one or more solid forms of 2′-C-methyluridine-5′-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, and methods of treating or ameliorating diseases and/or conditions with one or more solid forms of 2′-C-methyluridine-5′-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate. Also disclosed herein are methods of treating diseases and/or conditions with one or more solid forms of 2′-C-methyluridine-5′-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate in combination with one or more other agents.
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5.发明公开SOLID FORMS OF N-[2,4-BIS(1,1-DIMETHYLETHYL)-5-HYDROXYPHENYL]-1,4-DIHYDRO-4-OXOQUINOLINE-3-CARBOXAMIDE 审中-公开N-固体形式[2,4-双（1,1-二甲基乙基）-5-羟基苯基] -1,4-二氢-4-氧喹啉-3-甲酰胺
公开(公告)号：EP2222304A2
公开(公告)日：2010-09-01
申请号：EP08832069.2
申请日：2008-09-15
发明人： DEMATTEI, John , FENG, Yushi , HARRISON, Cristian , LOOKER, Adam , MUDUNURI, Praveen , ROEPER, Stefanie , ZHANG, Yuegang
CPC分类号： C07D215/56 , A61K31/47 , A61K45/06 , C07D215/233
摘要： Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide are described herein, including crystalline forms thereof.
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公开(公告)号：EP3424920B1
公开(公告)日：2020-04-15
申请号：EP18188034.5
申请日：2014-10-17
发明人： NTI-ADDAE, Kwame, Wiredu , O'NEIL, Simon Adam , ZHANG, Yuegang , MUDUNURI, Praveen , VAN ALSTEN, John Gregg , SONG, Bin , STAVROPOULOS, Kathy , STROHMEIER, Mark , WALDO, Michael , NAVAMAL, Mettachit , KADIYALA, Irina Nikolaevna
IPC分类号： C07D401/14 , A61K31/506 , A61P35/00
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公开(公告)号：EP3578554A1
公开(公告)日：2019-12-11
申请号：EP19165859.0
申请日：2014-11-12
发明人： NTI-ADDAE, Kwame W. , WALDO, Michael , O'NEIL, Simon Adam , VAN ALSTEN, John Gregg , MACIKENAS, Dainius , MUDUNURI, Praveen , SHI, Yi , LEDEBOER, Mark Willem , JURKAUSKAS, Valdas , MEDEK, Ales , JONES, Steven , BYRN, Randal , ASMAL, Mohammed , ROBERTSON, Sarah Marie , TSAI, Wanjung
IPC分类号： C07D403/04 , C07D471/04 , A61K31/506 , A61P31/16
摘要： Polymorphic forms of Compound (1) or a pharmaceutically acceptable salt thereof, wherein Compound (1) is represented by the following structural formula:
are Form A of HCl salt of Compound (1)· 1/2H 2 O, Form F of HCl salt of Compound (1)· 3H 2 O, Form D of HCl salt of Compound (1), Form A of Compound (1), and Form A of tosylate salt of Compound (1). Such polymorphic forms are employed for treating influenza, inhibiting the replication of influenza viruses, or reducing the amount of influenza viruses in a biological sample or in a subject.-
公开(公告)号：EP3068776B1
公开(公告)日：2019-05-29
申请号：EP14802787.3
申请日：2014-11-12
发明人： NTI-ADDAE, Kwame, W. , WALDO, Michael , O'NEIL, Simon, Adam , VAN ALSTEN, John, Gregg , MACIKENAS, Dainius , MUDUNURI, Praveen , SHI, Yi , LEDEBOER, Mark, Willem , JURKAUSKAS, Valdas , MEDEK, Ales , JONES, Steven , BYRN, Randal , ASMAL, Mohammed , ROBERTSON, Sarah, Marie , TSAI, Wanjung
IPC分类号： C07D403/04 , C07D471/04 , A61K31/506 , A61P31/16
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公开(公告)号：EP3057953B1
公开(公告)日：2018-08-15
申请号：EP14799578.1
申请日：2014-10-17
发明人： NTI-ADDAE, Kwame, Wiredu , O'NEIL, Simon, Adam , ZHANG, Yuegang , MUDUNURI, Praveen , VAN ALSTEN, John Gregg , SONG, Bin , STAVROPOULOS, Kathy , STROHMEIER, Mark , WALDO, Michael , NAVAMAL, Mettachit , KADIYALA, Irina Nikolaevna
IPC分类号： C07D401/14 , A61K31/506 , A61P35/00
CPC分类号： A61K31/506 , A61K31/337 , A61K31/5025 , A61K31/513 , A61K31/517 , A61K31/555 , A61K31/704 , A61K31/7048 , A61K33/24 , A61K38/14 , A61K39/39558 , A61K45/06 , A61N2005/1098 , A61P35/00 , C07B59/002 , C07B2200/05 , C07B2200/13 , C07C55/10 , C07C55/14 , C07C57/145 , C07C57/15 , C07C59/265 , C07C63/08 , C07D401/14 , C07K16/2863 , C07K2317/24
摘要： wherein each of R1 and R2 is H or 2H and a co-crystal former selected from adipic acid, citric acid, fumaric acid, maleic acid, succinic acid, or benzoic acid. Also within the scope of this invention are methods of making and using the same.
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公开(公告)号：EP2560650A1
公开(公告)日：2013-02-27
申请号：EP11718597.5
申请日：2011-04-22
发明人： VAN GOOR, Fredrick, F. , ALARGOVA, Rossitza, Gueorguieva , ALCACIO, Tim, Edward , AREKAR, Sneha, G. , BINCH, Hayley, Marie , BOTFIELD, Martyn, Curtis , FANNING, Lev, Tyler Dewey , GROOTENHUIS, Peter, Diederik Jan , HURLEY, Dennis, James , JOHNSTON, Steven, C. , KADIYALA, Irina, Nikolaevna , KAUSHIK, Ritu, Rohit , KESHAVARZ-SHOKRI, Ali , KRAWIEC, Mariusz , LEE, Elaine, Chungmin , LUISI, Brian , MEDEK, Ales , MUDUNURI, Praveen , NUMA, Mehdi , SHETH, Urvi Jagdishbhai , SILINA, Alina , SULLIVAN, Mark Jeffrey , VERWIJS, Marinus Jacobus , YANG, Xiaoqing , YOUNG, Christopher Ryan , ZAMAN, Noreen Tasneem , ZHANG, Beili , ZHANG, Yuegang , ZLOKARNIK, Gregor
IPC分类号： A61K31/4704 , A61K31/404 , A61K31/443
CPC分类号： A61K31/4709 , A61K31/404 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/4704 , G01N33/6872 , G01N2333/4703 , A61K2300/00
摘要： The present invention relates to pharmaceutical compositions comprising a compound of Formulas I and II, optionally in combination with a Compound of Formula III and/or a Compound of Formula IV. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis.
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