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![CRYSTALLINE FORMS OF (S)-2-ETHYLBUTYL 2-(((S)-(((2R,3S,4R,5R)-5- (4-AMINOPYRROLO[2,1-F] [1,2,4]TRIAZIN-7-YL)-5-CYANO-3,4-DIHYDROXYTETRAHYDROFURAN-2-YL)METHOXY) (PHENOXY) PHOSPHORYL)AMINO)PROPANOATE](/abs-image/US/2023/11/02/US20230348519A1/abs.jpg.150x150.jpg)
公开(公告)号：US20230348519A1
公开(公告)日：2023-11-02
申请号：US18099477
申请日：2023-01-20
发明人： Katrien Brak , Ernest A. Carra , Lars V. Heumann , Nate Larson
IPC分类号： C07H19/00 , A61P31/14 , C07F9/6561
CPC分类号： C07H19/00 , A61P31/14 , C07F9/6561 , C07B2200/13
摘要： The present invention relates to novel salts and crystalline forms of (S)-2-ethylbutyl 2-(((S)-(((2R,3S,4R,5R)-5-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-5-cyano-3,4-dihydroxytetrahydrofuran-2-yl)methoxy)(phenoxy)phosphoryl)amino)propanoate for use in treating viral infections. In some embodiments, the viral infection is caused by a virus selected from the group consisting of Arenaviridae, Coronaviridae, Filoviridae, Flaviviridae, and Paramyxoviridae.
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公开(公告)号：US20210179570A1
公开(公告)日：2021-06-17
申请号：US17100107
申请日：2020-11-20
发明人： Katrien Brak , Kae M. Bullock , Greg Cizio , Kathy Dao , Darryl D. Dixon , Joshua R. Dunetz , Luke D. Humphreys , Valerie Huynh , Michael A. Ischay , Trevor C. Johnson , Jeffrey E. Merit , Christopher S. Regens , Eric A. Standley , Dietrich P. Steinhuebel , Justin Y. Su , Tao Wu , Marshall D. Young
IPC分类号： C07D267/16 , C07C311/13 , C07D317/30 , C07D319/06 , C07D513/04 , C07D413/12
摘要： The present disclosure provides methods for preparing MCL1 inhibitors or a salt thereof and related key intermediates.
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![CRYSTALLINE FORMS OF (S)-2-ETHYLBUTYL 2-(((S)-(((2R,3S,4R,5R)-5- (4-AMINOPYRROLO[2,1-F] [1,2,4]TRIAZIN-7-YL)-5-CYANO-3,4-DIHYDROXYTETRAHYDROFURAN-2-YL)METHOXY) (PHENOXY) PHOSPHORYL)AMINO)PROPANOATE](/abs-image/US/2018/12/06/US20180346504A1/abs.jpg.150x150.jpg)
公开(公告)号：US20180346504A1
公开(公告)日：2018-12-06
申请号：US15964597
申请日：2018-04-27
发明人： Katrien Brak , Ernest A. Carra , Lars V. Heumann , Nate Larson
CPC分类号： A61P31/14 , C07F9/6561
摘要： The present invention relates to novel salts and crystalline forms of (S)-2-ethylbutyl 2-(((S)-(((2R,3S,4R,5R)-5-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-5-cyano-3,4-dihydroxytetrahydrofuran-2-yl)methoxy)(phenoxy)phosphoryl)amino)propanoate for use in treating viral infections. In some embodiments, the viral infection is caused by a virus selected from the group consisting of Arenaviridae, Coronaviridae, Filoviridae, Flaviviridae, and Paramyxoviridae.
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![Crystalline forms of (s)-2-ethylbutyl 2-(((s)-(((2r,3s,4r,5r)-5-(4-aminopyrrolo[2,1-f] [1,2,4]triazin-7-yl)-5-cyano-3,4-dihydroxytetrahydrofuran-2-yl)methoxy) (phenoxy) phosphoryl)amino)propanoate](/abs-image/US/2024/07/09/US12030906B2/abs.jpg.150x150.jpg)
公开(公告)号：US12030906B2
公开(公告)日：2024-07-09
申请号：US18099477
申请日：2023-01-20
发明人： Katrien Brak , Ernest A. Carra , Lars V. Heumann , Nate Larson
IPC分类号： C07H19/00 , A61P31/14 , C07F9/6561
CPC分类号： C07H19/00 , A61P31/14 , C07F9/6561 , C07B2200/13
摘要： The present invention relates to novel salts and crystalline forms of (S)-2-ethylbutyl 2-(((S)-(((2R,3S,4R,5R)-5-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-5-cyano-3,4-dihydroxytetrahydrofuran-2-yl)methoxy)(phenoxy)phosphoryl)amino)propanoate for use in treating viral infections. In some embodiments, the viral infection is caused by a virus selected from the group consisting of Arenaviridae, Coronaviridae, Filoviridae, Flaviviridae, and Paramyxoviridae.
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公开(公告)号：US11760736B2
公开(公告)日：2023-09-19
申请号：US17701404
申请日：2022-03-22
发明人： Katrien Brak , Kae M. Bullock , Greg Cizio , Kathy Dao , Darryl D. Dixon , Joshua R. Dunetz , Luke D. Humphreys , Valerie Huynh , Michael A. Ischay , Trevor C. Johnson , Jeffrey E. Merit , Christopher S. Regens , Eric A. Standley , Dietrich P. Steinhuebel , Justin Y. Su , Tao Wu , Marshall D. Young
IPC分类号： C07D267/16 , C07C311/13 , C07D317/30 , C07D319/06 , C07D413/12 , C07D513/04
CPC分类号： C07D267/16 , C07C311/13 , C07D317/30 , C07D319/06 , C07D413/12 , C07D513/04
摘要： The present disclosure provides methods for preparing MCL1 inhibitors or a salt thereof and related key intermediates.
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公开(公告)号：US20160122356A1
公开(公告)日：2016-05-05
申请号：US14926063
申请日：2015-10-29
发明人： Steven Donald Axt , Pavel Robertovich Badalov , Katrien Brak , Silvio Campagna , Andrei Chtchemelinine , Edward Doerffler , Morin Mae Frick , Detian Gao , Lars V. Heumann , Brittanie Hoang , Willard Lew , Robert Ronald Milburn , Sean Timothy Neville , Bruce Ross , Erik Rueden , Robert William Scott , Dustin Siegel , Andrew C. Stevens , Clarissa Tadeus , Tiago Vieira , Andrew W. Waltman , Xianghong Wang , Mark Charles Whitcomb , Lydia Wolfe , Chia-Yun Yu
IPC分类号： C07D487/04 , C07F9/6561 , C07D519/00 , C07F9/24
CPC分类号： A61K31/685 , A61K31/00 , A61K31/53 , A61K31/6615 , A61K31/665 , A61K31/675 , A61K31/683 , A61K31/7056 , A61K31/706 , A61K45/06 , C07D487/04 , C07D519/00 , C07F9/2429 , C07F9/65616 , C07H1/00 , C07H1/02 , C07H11/00 , C07H15/18 , A61K2300/00
摘要： Provided are methods of preparing compounds and pharmaceutical compositions for treating Filoviridae virus infections The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.
摘要翻译： 提供制备用于治疗丝状病毒科病毒感染的化合物和药物组合物的方法所提供的化合物，组合物和方法特别可用于治疗马尔堡病毒，埃博拉病毒和Cueva病毒感染。
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公开(公告)号：US20220354873A1
公开(公告)日：2022-11-10
申请号：US17665724
申请日：2022-02-07
发明人： Steven Donald Axt , Pavel Robertovich Badalov , Katrien Brak , Silvio Campagna , Andrei Chtchemelinine , Edward Doerffler , Morin Mae Frick , Detian Gao , Lars V. Heumann , Brittanie Hoang , Willard Lew , Robert Ronald Milburn , Sean Timothy Neville , Bruce Ross , Erik Rueden , Robert William Scott , Dustin Siegel , Andrew C. Stevens , Clarissa Tadeus , Tiago Vieira , Andrew W. Waltman , Xianghong Wang , Mark Charles Whitcomb , Lydia Wolfe , Chia-Yun Yu
IPC分类号： A61K31/685 , A61K31/706 , A61K31/7056 , A61K31/53 , C07H1/00 , C07H1/02 , C07H11/00 , C07H15/18 , A61K31/6615 , A61K31/665 , A61K31/683 , C07D487/04 , C07D519/00 , C07F9/24 , C07F9/6561 , A61K31/675 , A61K45/06 , A61K31/00
摘要： Provided are methods of preparing compounds and pharmaceutical compositions for treating Filoviridae virus infections The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.
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公开(公告)号：US11344565B2
公开(公告)日：2022-05-31
申请号：US14926063
申请日：2015-10-29
发明人： Steven Donald Axt , Pavel Robertovich Badalov , Katrien Brak , Silvio Campagna , Andrei Chtchemelinine , Edward Doerffler , Morin Mae Frick , Detian Gao , Lars V. Heumann , Brittanie Hoang , Willard Lew , Robert Ronald Milburn , Sean Timothy Neville , Bruce Ross , Erik Rueden , Robert William Scott , Dustin Siegel , Andrew C. Stevens , Clarissa Tadeus , Tiago Vieira , Andrew W. Waltman , Xianghong Wang , Mark Charles Whitcomb , Lydia Wolfe , Chia-Yun Yu
IPC分类号： C07H5/06 , C07H7/06 , A61K31/685 , A61K31/706 , A61K31/7056 , A61K31/53 , C07H1/00 , C07H1/02 , C07H11/00 , C07H15/18 , A61K31/6615 , A61K31/665 , A61K31/683 , C07D487/04 , C07D519/00 , C07F9/24 , C07F9/6561 , A61K31/675 , A61K45/06 , A61K31/00
摘要： Provided are methods of preparing compounds and pharmaceutical compositions comprising a compound Formula VIII for treating Filoviridae virus infections. In one aspect, the compound of Formula VIII is formed from a reaction mixture comprising the compound of Formula IX, the compound of Formula X, a coupling agent such as magnesium chloride and a non-nucleophilic base such as diisopropylethylamine. The compound of Formula IX can be formed from a compound of Formula V and a cyanating agent. The compound of Formula V can be synthesized from a reaction mixture comprising a deprotonating agent such as phenylmagnesium chloride; a silylating agent such as chlorotrimethylsilane; a coupling agent such as isopropylmagnesium chloride, an additive such as LaCl3-2LiCl, LaCl3, CeCl3, NdCl3, or YCl3; a compound of Formula VI; and 7-iodopyrrolo[2,1-f][1,2,4]triazin-4-amine. The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.
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![CRYSTALLINE FORMS OF (S)-2-ETHYLBUTYL 2-(((S)-(((2R,3S,4R,5R)-5- (4-AMINOPYRROLO[2,1-F] [1,2,4]TRIAZIN-7-YL)-5-CYANO-3,4-DIHYDROXYTETRAHYDROFURAN-2-YL)METHOXY) (PHENOXY) PHOSPHORYL)AMINO)PROPANOATE](/abs-image/US/2021/06/03/US20210163523A1/abs.jpg.150x150.jpg)
公开(公告)号：US20210163523A1
公开(公告)日：2021-06-03
申请号：US17069248
申请日：2020-10-13
发明人： Katrien Brak , Ernest A. Carra , Lars V. Heumann , Nate Larson
IPC分类号： C07H19/00 , A61P31/14 , C07F9/6561
摘要： The present invention relates to novel salts and crystalline forms of (S)-2-ethylbutyl 2-(((S)-(((2R,3S,4R,5R)-5-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-5-cyano-3,4-dihydroxytetrahydrofuran-2-yl)methoxy)(phenoxy)phosphoryl)amino)propanoate for use in treating viral infections. In some embodiments, the viral infection is caused by a virus selected from the group consisting of Arenaviridae, Coronaviridae, Filoviridae, Flaviviridae, and Paramyxoviridae.
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公开(公告)号：US20240109851A1
公开(公告)日：2024-04-04
申请号：US18363585
申请日：2023-08-01
发明人： Katrien Brak , Kae M. Bullock , Greg Cizio , Kathy Dao , Darryl D. Dixon , Joshua R. Dunetz , Luke D. Humphreys , Valerie Huynh , Michael A. Ischay , Trevor C. Johnson , Jeffrey E. Merit , Christopher S. Regens , Eric A. Standley , Dietrich P. Steinhuebel , Justin Y. Su , Tao Wu , Marshall D. Young
IPC分类号： C07D267/16 , C07C311/13 , C07D317/30 , C07D319/06 , C07D413/12 , C07D513/04
CPC分类号： C07D267/16 , C07C311/13 , C07D317/30 , C07D319/06 , C07D413/12 , C07D513/04
摘要： The present disclosure provides methods for preparing MCL1 inhibitors or a salt thereof and related key intermediates.
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