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公开(公告)号：US20160022664A2
公开(公告)日：2016-01-28
申请号：US14629097
申请日：2015-02-23
发明人： 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分类号： A61K31/4709 , A61K31/404 , C12Q1/34 , A61K31/443
CPC分类号： A61K31/4709 , A61K31/404 , A61K31/443 , A61K31/4704 , A61K45/06 , C07D405/12 , C12Q1/34 , G01N2500/04 , G01N2500/20 , 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.
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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](/abs-image/US/2015/06/09/US09051303B2/abs.jpg.150x150.jpg)
22.发明授权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-YL）-N-（1-（2,3-二羟基丙基-6-氟-2-（1- 羟基-2-甲基丙-2-炔基）-1H-吲哚-5-YL） - 环丙烷甲酰胺公开(公告)号：US09051303B2
公开(公告)日：2015-06-09
申请号：US14318131
申请日：2014-06-27
发明人： Ali Keshavarz-Shokri , Beili Zhang , Tim Edward Alcacio , Elaine Chungmin Lee , Yuegang Zhang , Mariusz Krawiec
IPC分类号： A61K31/36 , C07D405/12 , A61K31/404 , A61K45/06 , A61K31/47
CPC分类号： C07D405/12 , A61K31/404 , A61K31/47 , A61K31/4709 , A61K45/06 , C07B2200/13 , A61K2300/00
摘要： 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.
摘要翻译： 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。
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![Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxo1-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl) benzoic acid](/abs-image/US/2014/09/30/US08846718B2/abs.jpg.150x150.jpg)
23.发明授权Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxo1-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl) benzoic acid 有权固体形式的3-（6-（1-（2,2-二氟苯并[d] [1,3]二氧杂环戊烯-5-基）环丙烷甲酰氨基）-3-甲基吡啶-2-基）苯甲酸公开(公告)号：US08846718B2
公开(公告)日：2014-09-30
申请号：US13933223
申请日：2013-07-02
IPC分类号： A61K31/443 , C07D405/12
CPC分类号： C07D405/12 , A61K31/4709 , C07B2200/13
摘要： The present invention relates to a substantially crystalline and free solid state form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Form I), pharmaceutical compositions thereof, and methods of treatment therewith.
摘要翻译： 本发明涉及3-（6-（1-（2,2-二氟苯并[d] [1,3]间二氧杂环戊烯-5-基）环丙烷甲酰氨基）-3-甲基吡啶-2-基的结晶和游离固体形式 - 基）苯甲酸（I型），其药物组合物及其处理方法。
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![Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid](/abs-image/US/2014/06/03/US08742122B2/abs.jpg.150x150.jpg)
24.发明授权Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid 有权固体形式的3-（6-（1-（2,2-二氟苯并[d] [1,3]二氧杂环戊烯-5-基）环丙烷甲酰氨基）-3-甲基吡啶-2-基）苯甲酸公开(公告)号：US08742122B2
公开(公告)日：2014-06-03
申请号：US13940361
申请日：2013-07-12
IPC分类号： A61K31/44 , C07D405/00
CPC分类号： A61K31/443 , A61K31/47 , A61K45/06 , C07D213/75 , C07D405/12 , C07D405/14 , C07D407/12 , Y10T428/2982
摘要： The present invention relates to a substantially a solid form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Compound 1, Solvate Form A and Compound 1, HCl Salt Form A), processes for making such forms, pharmaceutical compositions thereof, and methods of treatment therewith.
摘要翻译： 本发明涉及基本上固体形式的3-（6-（1-（2,2-二氟苯并[d] [1,3]二氧杂环戊烯-5-基）环丙烷甲酰氨基）-3-甲基吡啶-2-基） 苯甲酸（化合物1，溶剂化物形式A和化合物1，盐酸盐形式A），制备这种形式的方法，其药物组合物及其处理方法。
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公开(公告)号：US20130338188A9
公开(公告)日：2013-12-19
申请号：US13657321
申请日：2012-10-22
发明人： 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分类号： A61K31/47 , A61P11/00 , A61P1/18 , C12Q1/02 , A61P3/10 , A61P35/00 , A61P25/28 , A61P25/16 , A61P11/06 , A61P1/16
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.
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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](/abs-image/US/2021/02/02/US10906891B2/abs.jpg.150x150.jpg)
公开(公告)号：US10906891B2
公开(公告)日：2021-02-02
申请号：US16109931
申请日：2018-08-23
发明人： Ali Keshavarz-Shokri , Beili Zhang , Tim Edward Alcacio , Elaine Chungmin Lee , Yuegang Zhang , Mariusz Krawiec
IPC分类号： C07D405/12 , A61K45/08 , A61K31/4709 , A61K31/47 , A61K31/404 , A61K45/06
摘要： 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.
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公开(公告)号：US10787472B2
公开(公告)日：2020-09-29
申请号：US16283904
申请日：2019-02-25
发明人： Corey Anderson , Sara Sabina Hadida Ruah , Julian Marian Charles Golec , Beili Zhang , Benjamin Joseph Littler , Ali Keshavarz-Shokri , Tim Edward Alcacio , Daniel T. Belmont
IPC分类号： C07F9/58 , C07F9/59 , C07F9/576 , A61K31/675 , A61K45/06
摘要： The invention relates to prodrug compounds of formula I: wherein R2, R3, R5, R7 and X are as defined herein. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain. The compounds of formula I possess advantageous solubility and physicochemical properties.
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![Solid forms of 3-(6-(1-(2,2-difluorobenzo[D][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl) benzoic acid](/abs-image/US/2020/03/24/US10597384B2/abs.jpg.150x150.jpg)
公开(公告)号：US10597384B2
公开(公告)日：2020-03-24
申请号：US15807663
申请日：2017-11-09
IPC分类号： C07D405/12 , A61K31/4709
摘要： The present invention relates to a substantially crystalline and free solid state form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methypyridin-2-yl)benzoic acid (Form I), pharmaceutical compositions thereof, and methods of treatment therewith.
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公开(公告)号：US10570115B2
公开(公告)日：2020-02-25
申请号：US15721390
申请日：2017-09-29
发明人： Timothy Alcacio , Minson Baek , Peter Grootenhuis , Sara Sabina Hadida Ruah , Robert M. Hughes , Ali Keshavarz-Shokri , Rachel McAuley-Aoki , Jason McCartney , Mark Thomas Miller , Fredrick Van Goor , Beili Zhang , Corey Anderson , Thomas Cleveland , Bryan A. Frieman , Haripada Khatuya , Pramod Virupax Joshi , Paul John Krenitsky , Vito Melillo , Fabrice Jean Denis Pierre , Andreas P. Termin , Johnny Uy , Jinglan Zhou , Alexander Russell Abela , Brett Bradley Busch , Prasuna Paraselli , David Andrew Siesel
IPC分类号： C07D401/14 , A61K31/465 , A61K31/455 , A61K31/4155 , A61K31/4025 , C07D471/14 , C07D498/14 , C07B59/00
摘要： Compounds of Formula I: pharmaceutically acceptable salts thereof, deuterated derivatives of any of the foregoing, and metabolites of any of the foregoing are disclosed. Pharmaceutical compositions comprising the same, methods of treating cystic fibrosis using the same, and methods for making the same are also disclosed.
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公开(公告)号：US20180153874A1
公开(公告)日：2018-06-07
申请号：US15643182
申请日：2017-07-06
发明人： Fredrick F. Van Goor , Rossitza Gueorguieva Alargova , Tim Edward Alcacio , Sneha G. Arekar , Steven C. Johnston , Irina Nicolaevna 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分类号： A61K31/47 , A61K31/443 , A61K31/4433 , A61K31/4704 , A61K31/404 , G01N33/50
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.
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