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![Solid Forms of (R)-1(2,2-Difluorobenzo[D][1,3]Dioxol-5-yl)-N-(1-(2,3-Dihydroxypropyl)-6-Fluoro-2-(1-Hydroxy-2-Methylpropan-2-yl)-1H-Indol-5-yl)Cyclopropanecarboxamide](data:image/svg+xml,%3Csvg xmlns='http://www.w3.org/2000/svg' width='200' height='200' viewBox='0 0 200 200'%3E%3Crect width='100%25' height='100%25' fill='%23eee'%3E%3C/rect%3E%3Ctext x='50%25' y='50%25' dominant-baseline='middle' text-anchor='middle' fill='%23333333' font-family='Helvetica' font-size='20' font-weight='bold'%3ENo Pic%3C/text%3E%3C/svg%3E)
公开(公告)号：US20210340128A1
公开(公告)日：2021-11-04
申请号：US17104903
申请日：2020-11-25
Applicant: Vertex Pharmaceuticals Incorporated
Inventor： Ali Keshavarz-Shokri , Beili Zhang , Tim Edward Alcacio , Elaine Chungmin Lee , Yuegang Zhang , Mariusz Krawiec
IPC: C07D405/12 , A61K31/404 , A61K45/06 , A61K31/47 , A61K31/4709
Abstract: The present invention relates to solid forms of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1) in substantially crystalline form (Form A) or amorphous form, pharmaceutical compositions thereof, and methods of treatment therewith.
![Solid Forms of (R)-1(2,2-Difluorobenzo[D][1,3]Dioxol-5-yl)-N-(1-(2,3-Dihydroxypropyl)-6-Fluoro-2-(1-Hydroxy-2-Methylpropan-2-yl)-1H-Indol-5-yl)Cyclopropanecarboxamide](/docs/US/2021-11-04/US20210340128A1/abs.jpg.600x600.jpg)
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公开(公告)号：US10716789B2
公开(公告)日：2020-07-21
申请号：US16038696
申请日：2018-07-18
Applicant: Vertex Pharmaceuticals Incorporated
Inventor： Kwame Wiredu Nti-Addae , Simon Adam O'Neil , Yuegang Zhang , Michael P. Waldo , Praveen Mudunuri , Bin Song , John Gregg Van Alsten , Mark Strohmeier , Kathy Stavropoulos , Irina Nikolaevna Kadiyala , Mettachit Navamal
IPC: A61K31/506 , C07D401/14 , A61P35/00 , A61K31/337 , A61K31/5025 , A61K31/513 , A61K31/517 , A61K31/555 , A61K31/704 , A61K31/7048 , A61K33/24 , A61K38/14 , A61K39/395 , A61K45/06 , C07B59/00 , C07C55/10 , C07C55/14 , C07C57/145 , C07C57/15 , C07C59/265 , C07C63/08 , C07K16/28 , A61N5/10
Abstract: The present invention relates to compositions and co-crystals each comprising a compound of formula I having the structure: 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：US20150164881A1
公开(公告)日：2015-06-18
申请号：US14629097
申请日：2015-02-23
Applicant: Vertex Pharmaceuticals Incorporated
Inventor： Fredrick F. Van Goor , Rossitza Gueorguieva Alargova , Tim Edward Alcacio , Hayley Marie Binch , Martyn Curtis Botfield , Lev Tyler Dewey Fanning , Peter Diederik Jan Grootenhuis , Dennis James Hurley , Irina Nikolaevna Kadiyala , Ritu Rohit Kaushik , Ali Keshavarz-Shokri , Mariusz Krawiec , Elaine Chungmin Lee , Brian Luisi , Ales Medek , Mehdi Numa , Urvi Jagdishbhai Sheth , Alina Silina , Marinus Jacobus Verwijs , Xiaoqing Yang , Christopher Ryan Young , Noreen Tasneem Zaman , Beili Zhang , Yuegang Zhang , Gregor Zlokarnik
IPC: A61K31/4709 , A61K31/404 , C12Q1/34 , A61K31/443
CPC classification number: A61K31/4709 , A61K31/404 , A61K31/443 , A61K31/4704 , A61K45/06 , C07D405/12 , C12Q1/34 , G01N2500/04 , G01N2500/20 , A61K2300/00
Abstract: 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.
Abstract translation: 本发明涉及药物组合物，其包含与式II化合物和/或式III化合物中的一种或两种结合的式I化合物。 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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4.发明授权Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide 有权（R）-1（2,2-二氟苯并[D] [1,3]二氧代-5-基）-N-（1-（2,3-二羟基丙基-6-氟-2-（1- -2-羟基-2-甲基丙烷-2-基）-1H-吲哚-5-基） - 环丙烷甲酰胺
公开(公告)号：US08802868B2
公开(公告)日：2014-08-12
申请号：US13624241
申请日：2012-09-21
Applicant: Vertex Pharmaceuticals Incorporated
Inventor： Ali Keshavarz-Shokri , Beili Zhang , Tim Edward Alcacio , Elaine Chungmin Lee , Yuegang Zhang , Mariusz Krawiec
IPC: C07D405/12 , A61K31/36
CPC classification number: C07D405/12 , A61K31/404 , A61K31/47 , A61K31/4709 , A61K45/06 , C07B2200/13 , A61K2300/00
Abstract: The present invention relates to solid forms of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1) in substantially crystalline form (Form A) or amorphous form, pharmaceutical compositions thereof, and methods of treatment therewith.
Abstract translation: 本发明涉及（R）-1-（2,2-二氟苯并[d] [1,3]间二氧杂环戊烯-5-基）-N-（1-（2,3-二羟丙基）-6- （A型）或无定形形式的2-氟-2-（1-羟基-2-甲基丙-2-基）-1H-吲哚-5-基）环丙烷甲酰胺（化合物1）及其药物组合物，以及 治疗。
![Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide](/docs/US/2014-08-12/US08802868B2/abs.jpg.600x600.jpg)
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公开(公告)号：US20130143919A1
公开(公告)日：2013-06-06
申请号：US13657321
申请日：2012-10-22
Applicant: Vertex Pharmaceuticals Incorporated
Inventor： Fredrick F. Van Goor , Rossitza Gueorguieva Alargova , Tim Edward Alcacio , Sneha G. Arekar , Steven C. Johnston , Irina Nikolaevna Kadiyala , Ali Keshavarz-Shokri , Mariusz Krawiec , Elaine Chungmin Lee , Ales Medek , Praveen Mudunuri , Mark Jeffrey Sullivan , Noreen Tasneem Zaman , Beili Zhang , Yuegang Zhang , Gregor Zlokarnik
IPC: A61K31/47 , A61P11/00 , A61P1/18 , C12Q1/02 , A61P3/10 , A61P35/00 , A61P25/28 , A61P25/16 , A61P11/06 , A61P1/16
CPC classification number: A61K31/47 , A61K31/404 , A61K31/443 , A61K31/4433 , A61K31/4704 , G01N33/5032 , G01N2500/04 , A61K2300/00
Abstract: 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.
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6.发明申请Solid Forms of (R)-1(2,2-Difluorobenzo[D][1,3]Dioxol-5-yl)-N-(1-(2,3-Dihydroxypropyl-6-Fluoro-2-(1-Hydroxy-2-Methylpropan-2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide 有权（R）-1（2,2-二氟苯并[D] [1,3]二氧杂环戊烯-5-基）-N-（1-（2,3-二羟基丙基）-6-氟-2-（1- -2-羟基-2-甲基丙-2-基）-1H-吲哚-5-基） - 环丙烷甲酰胺
公开(公告)号：US20130143918A1
公开(公告)日：2013-06-06
申请号：US13624241
申请日：2012-09-21
Applicant: Vertex Pharmaceuticals Incorporated
Inventor： Ali Keshavarz-Shokri , Beili Zhang , Tim Edward Alcacio , Elaine Chungmin Lee , Yuegang Zhang , Mariusz Krawiec
IPC: A61K31/404 , C07D405/12 , A61K31/47 , A61K45/06 , C07D495/04
CPC classification number: C07D405/12 , A61K31/404 , A61K31/47 , A61K31/4709 , A61K45/06 , C07B2200/13 , A61K2300/00
Abstract: The present invention relates to solid forms of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1) in substantially crystalline form (Form A) or amorphous form, pharmaceutical compositions thereof, and methods of treatment therewith.
Abstract translation: 本发明涉及（R）-1-（2,2-二氟苯并[d] [1,3]间二氧杂环戊烯-5-基）-N-（1-（2,3-二羟丙基）-6- （A型）或无定形形式的2-氟-2-（1-羟基-2-甲基丙-2-基）-1H-吲哚-5-基）环丙烷甲酰胺（化合物1）及其药物组合物，以及 治疗。
![Solid Forms of (R)-1(2,2-Difluorobenzo[D][1,3]Dioxol-5-yl)-N-(1-(2,3-Dihydroxypropyl-6-Fluoro-2-(1-Hydroxy-2-Methylpropan-2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide](/docs/US/2013-06-06/US20130143918A1/abs.jpg.600x600.jpg)
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公开(公告)号：US11578062B2
公开(公告)日：2023-02-14
申请号：US17104903
申请日：2020-11-25
Applicant: Vertex Pharmaceuticals Incorporated
Inventor： Ali Keshavarz-Shokri , Beili Zhang , Tim Edward Alcacio , Elaine Chungmin Lee , Yuegang Zhang , Mariusz Krawiec
IPC: C07D405/12 , A61K31/404 , A61K31/47 , A61K31/4709 , A61K45/06
Abstract: The present invention relates to solid forms of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1) in substantially crystalline form (Form A) or amorphous form, pharmaceutical compositions thereof, and methods of treatment therewith.
![Solid forms of (R)-1(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide](/docs/US/2023-02-14/US11578062B2/abs.jpg.600x600.jpg)
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公开(公告)号：US11485739B2
公开(公告)日：2022-11-01
申请号：US16994968
申请日：2020-08-17
Applicant: Vertex Pharmaceuticals Incorporated
Inventor： Jean-Damien Charrier , Christopher John Davis , Damien Fraysse , Gorka Etxebarria I Jardi , Simon Pegg , Francoise Pierard , Joanne Pinder , John Studley , Carl Zwicker , Tapan Sanghvi , Michael Waldo , Ales Medek , David Matthew Shaw , Maninder Panesar , Yuegang Zhang , Naziha Alem
IPC: C07D487/04 , C07C45/00 , C07C45/63 , C07B59/00 , A61K31/519
Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and solid forms of the compounds of this invention.
The compounds of this invention have formula I-A or I-B: wherein the variables are as defined herein.
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公开(公告)号：US10160760B2
公开(公告)日：2018-12-25
申请号：US14561368
申请日：2014-12-05
Applicant: Vertex Pharmaceuticals Incorporated
Inventor： Jean-Damien Charrier , Christopher John Davis , Damien Fraysse , Gorka Etxebarria I Jardi , Simon Pegg , Francoise Pierard , Joanne Pinder , John Studley , Carl Zwicker , Tapan Sanghvi , Michael Waldo , Ales Medek , David Matthew Shaw , Maninder Panesar , Yuegang Zhang , Naziha Alem
IPC: C07D487/04 , A61K31/519 , C07C45/00 , C07C45/63 , C07B59/00 , A61P35/00
Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and solid forms of the compounds of this invention.The compounds of this invention have formula I-A or I-B: wherein the variables are as defined herein.
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公开(公告)号：US10081621B2
公开(公告)日：2018-09-25
申请号：US14676205
申请日：2015-04-01
Applicant: Vertex Pharmaceuticals Incorporated
Inventor： Ali Keshavarz-Shokri , Beili Zhang , Tim Edward Alcacio , Elaine Chungmin Lee , Yuegang Zhang , Mariusz Krawiec
IPC: C07D405/12 , A61K31/404 , A61K45/06 , A61K31/47 , A61K31/4709
CPC classification number: C07D405/12 , A61K31/404 , A61K31/47 , A61K31/4709 , A61K45/06 , C07B2200/13 , A61K2300/00
Abstract: The present invention relates to solid forms of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1) in substantially crystalline form (Form A) or amorphous form, pharmaceutical compositions thereof, and methods of treatment therewith.
![Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide](/docs/US/2018-09-25/US10081621B2/abs.jpg.600x600.jpg)
