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公开(公告)号：US10030033B2
公开(公告)日：2018-07-24
申请号：US15227527
申请日：2016-08-03
Applicant: Gilead Sciences, Inc.
Inventor： Amy Cagulada , Johann Chan , Lina Chan , Denise A. Colby , Kapil Kumar Karki , Darryl Kato , Katie Ann Keaton , Sudha Kondappally , Chris Levins , Adam Littke , Ruben Martinez , Dominika Pcion , Troy Reynolds , Bruce Ross , Michael Sangi , Adam J. Schrier , Pamela Seng , Dustin Siegel , Nathan Shapiro , Donald Tang , James G. Taylor , Jonathan Tripp , Andrew W. Waltman , Lawrence Yu
IPC: C07D498/16 , C07D403/12 , C07D498/18 , C07C271/34 , C07D241/44 , C07C205/57 , C07C233/09 , C07C251/12 , C07C255/61
Abstract: The present disclosure provides processes for the preparation of a compound of formula I: which is useful as an antiviral agent. The disclosure also provides compounds and processes for the preparation of the compounds that are synthetic intermediates to the compound of formula I.
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![CRYSTALLINE FORMS OF (2R,5S,13AR)-8-HYDROXY-7,9-DIOXO-N-(2,4,6-TRIFLUOROBENZYL)-2,3,4,5,7,9,13,13A-OCTAHYDRO-2,5-METHANOPYRIDO[1',2':4,5]PYRAZINO[2,1-B][1,3]OXAZEPINE-10-CARBOXAMIDE](/abs-image/US/2017/11/23/US20170333438A1/abs.jpg.150x150.jpg)
公开(公告)号：US20170333438A1
公开(公告)日：2017-11-23
申请号：US15588346
申请日：2017-05-05
Applicant: Gilead Sciences, Inc.
Inventor： Ernest A. Carra , Irene Chen , Katie Ann Keaton , Scott E. Lazerwith , Vahid Zia
IPC: A61K31/5365 , A61K9/20 , A61K45/06 , C07D498/18 , C07D498/14 , A61K31/537
CPC classification number: A61K31/5365 , A61K9/20 , A61K31/513 , A61K31/537 , A61K31/553 , A61K31/675 , A61K31/683 , A61K45/06 , C07B2200/13 , C07D498/14 , C07D498/18 , Y02A50/395 , A61K2300/00
Abstract: The present invention relates to crystalline forms and co-crystals of (2R,5S,13aR)-8-hydroxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide, the pharmaceutical formulations, and the therapeutic uses thereof. The present invention also relates to novel crystalline forms of sodium (2R,5S,13aR)-7,9-dioxo-10-((2,4,6-trifluorobenzyl)carbamoyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazepin-8-olate Form I.
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![Crystalline forms of (2R,5S,13AR)-8-hydroxy-7,9,-dioxo-N-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide](/abs-image/US/2017/06/20/US09682084B2/abs.jpg.150x150.jpg)
公开(公告)号：US09682084B2
公开(公告)日：2017-06-20
申请号：US14745121
申请日：2015-06-19
Applicant: Gilead Sciences, Inc.
Inventor： Ernest A. Carra , Irene Chen , Katie Ann Keaton , Scott E. Lazerwith , Vahid Zia
IPC: A61K31/5365 , C07D498/18 , A61K45/06 , A61K9/20 , C07D498/14 , A61K31/537
CPC classification number: A61K31/5365 , A61K9/20 , A61K31/513 , A61K31/537 , A61K31/553 , A61K31/675 , A61K31/683 , A61K45/06 , C07B2200/13 , C07D498/14 , C07D498/18 , Y02A50/395 , A61K2300/00
Abstract: The present invention relates to crystalline forms and co-crystals of (2R,5S,13aR)-8-hydroxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide, the pharmaceutical formulations, and the therapeutic uses thereof. The present invention also relates to novel crystalline forms of sodium (2R,5S,13aR)-7,9-dioxo-10-((2,4,6-trifluorobenzyl)carbamoyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazepin-8-olate Form I.
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![Crystalline forms of (2R,5S,13AR)-8-hydroxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13A- octahydro-2,5-methanopyrido[1′,2′:4,5]pyrazino[2,1-B] [1,3] oxazepine-10-carboxamide](/abs-image/US/2018/10/16/US10098886B2/abs.jpg.150x150.jpg)
公开(公告)号：US10098886B2
公开(公告)日：2018-10-16
申请号：US15588346
申请日：2017-05-05
Applicant: Gilead Sciences, Inc.
Inventor： Ernest A. Carra , Irene Chen , Katie Ann Keaton , Scott E. Lazerwith , Vahid Zia
IPC: C07D498/18 , A61K31/5365 , A61K45/06 , A61K9/20 , C07D498/14 , A61K31/513 , A61K31/553 , A61K31/675 , A61K31/683 , A61K31/537
Abstract: The present invention relates to crystalline forms and co-crystals of (2R,5S,13aR)-8-hydroxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide, the pharmaceutical formulations, and the therapeutic uses thereof. The present invention also relates to novel crystalline forms of sodium (2R,5S,13aR)-7,9-dioxo-10-((2,4,6-trifluorobenzyl)carbamoyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazepin-8-olate Form I.
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公开(公告)号：US20180022757A1
公开(公告)日：2018-01-25
申请号：US15639833
申请日：2017-06-30
Applicant: Gilead Sciences, Inc.
Inventor： Anna Chiu , John Enquist, JR. , Nolan Griggs , Christopher Hale , Norihiro Ikemoto , Katie Ann Keaton , Matt Kraft , Scott E. Lazerwith , Michel Leeman , Zhihui Peng , Kate Schrier , Jonathan Trinidad , Jochem Van Herpt , Andrew W. Waltman
IPC: C07D498/14 , C07D213/82 , C07C237/20 , C07D319/06 , C07C237/16 , C07D309/40 , C07C235/80 , C07C231/02 , C07D498/22 , C07C231/12
Abstract: Methods of making compounds of Formula I are disclosed:
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Patent Agency Ranking
公开(公告)号：US20170210756A1
公开(公告)日：2017-07-27
申请号：US15227527
申请日：2016-08-03
Applicant: Gilead Sciences, Inc.
Inventor： Amy Cagulada , Johann Chan , Lina Chan , Denise A. Colby , Kapil Kumar Karki , Darryl Kato , Katie Ann Keaton , Sudha Kondapally , Christopher Levins , Adam Littke , Ruben Martinez , Dominika Pcion , Troy Reynolds , Bruce Ross , Michael Sangi , Adam J. Schrier , Pamela Seng , Dustin Siegel , Nathan Shapiro , Donald Tang , James G. Taylor , Jonathan Tripp , Andrew W. Waltman , Lawrence Yu
IPC: C07D498/18 , C07C271/34 , C07C255/61 , C07C205/57 , C07C233/09 , C07C251/12 , C07D403/12 , C07D241/44
CPC classification number: C07D498/18 , C07C51/09 , C07C205/57 , C07C209/00 , C07C227/02 , C07C233/09 , C07C251/12 , C07C255/61 , C07C271/34 , C07C2601/02 , C07D241/44 , C07D403/12 , C07D453/02 , C07D498/16 , C07K5/0808
Abstract: The present disclosure provides processes for the preparation of a compound of formula I: which is useful as an antiviral agent. The disclosure also provides compounds and processes for the preparation of the compounds that are synthetic intermediates to the compound of formula I.
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公开(公告)号：US20200223866A1
公开(公告)日：2020-07-16
申请号：US16686912
申请日：2019-11-18
Applicant: Gilead Sciences, Inc.
Inventor： Anna Chiu , John Enquist, JR. , Nolan Griggs , Christopher Hale , Norihiro Ikemoto , Katie Ann Keaton , Matt Kraft , Scott E. Lazerwith , Michel Leeman , Zhihui Peng , Kate Schrier , Jonathan Trinidad , Jochem Van Herpt , Andrew W. Waltman
IPC: C07D498/14 , C07D319/06 , C07C237/20 , C07D213/82 , C07D309/40 , C07C235/80 , C07D498/22 , C07C231/02 , C07C231/12
Abstract: Methods of making compounds of Formula I are disclosed:
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![CRYSTALLINE FORMS OF (2R,5S,13AR)-8-HYDROXY-7,9-DIOXO-N-(2,4,6-TRIFLUOROBENZYL)-2,3,4,5,7,9,13,13A-OCTAHYDRO-2,5-METHANOPYRIDO[1',2':4,5]PYRAZINO[2,1-B][1,3]OXAZEPINE-10-CARBOXAMIDE](/abs-image/US/2015/12/24/US20150366872A1/abs.jpg.150x150.jpg)
8.发明申请CRYSTALLINE FORMS OF (2R,5S,13AR)-8-HYDROXY-7,9-DIOXO-N-(2,4,6-TRIFLUOROBENZYL)-2,3,4,5,7,9,13,13A-OCTAHYDRO-2,5-METHANOPYRIDO[1',2':4,5]PYRAZINO[2,1-B][1,3]OXAZEPINE-10-CARBOXAMIDE 有权（2R，5S，13AR）-8-羟基-7,9-二氧代-N-（2,4,6-三氟硼酸）-2,3,4,5,7,9,13,13a-八氢噻吩的结晶形式 -2,5-甲基吡咯并[1'，2'：4,5]吡咯并[2,1-B] [1,3]氧杂氮杂-10-羧酰胺公开(公告)号：US20150366872A1
公开(公告)日：2015-12-24
申请号：US14745121
申请日：2015-06-19
Applicant: Gilead Sciences, Inc.
Inventor： Ernest A. Carra , Irene Chen , Katie Ann Keaton , Vahid Zia
IPC: A61K31/5365 , A61K45/06 , A61K9/20 , C07D498/18
CPC classification number: A61K31/5365 , A61K9/20 , A61K31/513 , A61K31/537 , A61K31/553 , A61K31/675 , A61K31/683 , A61K45/06 , C07B2200/13 , C07D498/14 , C07D498/18 , Y02A50/395 , A61K2300/00
Abstract: The present invention relates to crystalline forms and co-crystals of (2R,5S,13aR)-8-hydroxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide, the pharmaceutical formulations, and the therapeutic uses thereof. The present invention also relates to novel crystalline forms of sodium (2R,5S,13aR)-7,9-dioxo-10-((2,4,6-trifluorobenzyl)carbamoyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazepin-8-olate Form I.
Abstract translation: 本发明涉及（2R，5S，13aR）-8-羟基-7,9-二氧代-N-（2,4,6-三氟苄基）-2,3,4,5， 7,9,13,13a-八氢-2,5-甲基吡啶并[1'，2'：4,5]吡嗪并[2,1-b] [1,3]恶唑嘌呤-10-甲酰胺，药物制剂和 其治疗用途。 本发明还涉及（2R，5S，13aR）-7,9-二氧代-10 - （（2,4,6-三氟苄基）氨基甲酰基）-2,3,4,5,7， 9,13,13a-八氢-2,5-亚甲基吡啶并[1'，2'：4,5]吡嗪并[2,1-b] [1,3]氧氮杂-8-乙酸酯。
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![Crystalline forms of (2R,5S,13aR)-8-hydroxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide](/abs-image/US/2021/12/21/US11202780B2/abs.jpg.150x150.jpg)
公开(公告)号：US11202780B2
公开(公告)日：2021-12-21
申请号：US16740174
申请日：2020-01-10
Applicant: Gilead Sciences, Inc.
Inventor： Ernest A. Carra , Irene Chen , Katie Ann Keaton , Scott E. Lazerwith , Vahid Zia
IPC: A61K31/5365 , C07D498/18 , A61K45/06 , A61K9/20 , C07D498/14 , A61K31/513 , A61K31/553 , A61K31/675 , A61K31/683 , A61K31/537
Abstract: The present invention relates to crystalline forms and co-crystals of (2R,5S,13aR)-8-hydroxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide, the pharmaceutical formulations, and the therapeutic uses thereof. The present invention also relates to novel crystalline forms of sodium (2R,5S,13aR)-7,9-dioxo-10-(2,4,6-trifluorobenzyl)carbamoyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazepin-8-olate Form I.
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公开(公告)号：US20150368264A1
公开(公告)日：2015-12-24
申请号：US14740954
申请日：2015-06-16
Applicant: Gilead Sciences, Inc.
Inventor： Anna Chiu , John Enquist, JR. , Nolan Griggs , Christopher Hale , Norihiro Ikemoto , Katie Ann Keaton , Matt Kraft , Scott E. Lazerwith , Michel Leeman , Zhihui Peng , Kate Schrier , Jonathan Trinidad , Jochem Van Herpt , Andrew W. Waltman
IPC: C07D498/14 , C07D309/40 , C07C237/20 , C07D213/82 , C07D319/06 , C07C235/78
Abstract: Methods of making compounds of Formula I are disclosed:
Abstract translation: 公开了制备式I化合物的方法：
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