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公开(公告)号：US20220313698A1
公开(公告)日：2022-10-06
申请号：US16992675
申请日：2020-08-13
Applicant: Vertex Pharmaceuticals Incorporated
Inventor： Alexander Russell Abela , Corey Don Anderson , Brett C. Bookser , Brett B. Busch , Jeremy J. Clemens , Thomas Cleveland , Timothy Richard Coon , Bryan Frieman , Senait G. Ghirmai , Peter Grootenhuis , Anton V. Gulevich , Sara Sabina Hadida Ruah , Yoshihiro Ishihara , Haripada Khatuya , Jason McCartney , Mark Thomas Miller , Prasuna Paraselli , Fabrice Pierre , Andreas Termin , Sara E. Swift , Johnny Uy , Carl V. Vogel , Jinglan Zhou
IPC: A61K31/529 , A61K31/404 , A61K31/47 , A61K31/4418 , A61K31/439 , C07D513/22
Abstract: This disclosure provides modulators of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR), pharmaceutical compositions containing at least one such modulator, methods of treatment of cystic fibrosis using such modulators and pharmaceutical compositions, and processes for making such modulators.
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公开(公告)号：US11186566B2
公开(公告)日：2021-11-30
申请号：US16702891
申请日：2019-12-04
Applicant: Vertex Pharmaceuticals Incorporated
Inventor： 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
IPC: C07D401/14 , C07D471/14 , C07D498/14 , C07B59/00
Abstract: 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：US20210047345A1
公开(公告)日：2021-02-18
申请号：US16992419
申请日：2020-08-13
Applicant: Vertex Pharmaceuticals Incorporated
Inventor： Paul Angell , John E. Cochran , Benjamin J. Littler , David Siesel , Armando Urbina , Corey Don Anderson , Jeremy J. Clemens , Thomas Cleveland , Timothy Richard Coon , Bryan Frieman , Peter Grootenhuis , Sara Sabina Hadida Ruah , Jason McCartney , Mark Thomas Miller , Prasuna Paraselli , Fabrice Pierre , Sara E. Swift , Jinglan Zhou
IPC: C07D513/22 , C07D401/14 , C07D401/04 , C07D213/71 , C07D213/82 , C07D207/08 , C07D231/20
Abstract: The disclosure provides processes for synthesizing Compound I, and pharmaceutically acceptable salts thereof.
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公开(公告)号：US20210047323A1
公开(公告)日：2021-02-18
申请号：US16992441
申请日：2020-08-13
Applicant: Vertex Pharmaceuticals Incorporated
Inventor： Yi Shi , Kevin J. Gagnon , Jicong Li , Jennifer Lu , Ales Medek , Muna Shrestha , Michael Waldo , Beili Zhang , Carl L. Zwicker , Corey Don Anderson , Jeremy J. Clemens , Thomas Cleveland , Timothy Richard Coon , Bryan Frieman , Peter Grootenhuis , Sara Sabina Hadida Ruah , Jason McCartney , Mark Thomas Miller , Prasuna Paraselli , Fabrice Pierre , Sara E. Swift , Jinglan Zhou
IPC: C07D471/08
Abstract: Crystalline forms of Compound I: pharmaceutically acceptable salts thereof, and solvates and hydrates thereof 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：US10738030B2
公开(公告)日：2020-08-11
申请号：US16089703
申请日：2017-03-31
Applicant: Vertex Pharmaceuticals Incorporated
Inventor： Brian Bear , Jeremy Clemens , Thomas Cleveland , Timothy Richard Coon , Peter Diederik Jan Grootenhuis , Bryan A. Frieman , Sara S. Hadida Ruah , Haripada Khatuya , Paul J. Krenitsky , Mark Thomas Miller , Alina Silina , Johnny Uy , Jinglan Zhou
IPC: C07D401/14 , C07D213/82 , A61P11/00 , C07D401/12 , C07D471/04
Abstract: The present disclosure features a compound of formula I: or a pharmaceutically acceptable salt thereof, where R1, R2, W, X, Z, n, p, and Rings A and B are defined herein, for the treatment of CFTR mediated diseases, such as cystic fibrosis. The present disclosure also features pharmaceutical compositions, method of treating, and kits thereof.
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公开(公告)号：US20190269683A1
公开(公告)日：2019-09-05
申请号：US16258024
申请日：2019-01-25
Applicant: Vertex Pharmaceuticals Incorporated
Inventor： Mark Thomas Miller , Corey Anderson , Vijayalaksmi Arumugam , Brian Richard Bear , Haley Marie Binch , Jeremy J. Clemens , Thomas Cleveland , Erica Conroy , Timothy Richard Coon , Bryan A. Frieman , Peter Diederik Jan Grootenhuis , Raymond Stanley Gross , Sara Sabina Hadida-Ruah , Haripada Khatuya , Pramod Virupax Joshi , Paul John Krenitsky , Chun-Chieh Lin , Gulin Erdogan Marelius , Vito Melillo , Jason McCartney , Georgia McGaughey Nicholls , Fabrice Jean Denis Pierre , Alina Silina , Andreas P. Termin , Johnny Uy , Jinglan Zhou
IPC: A61K31/506 , A61K31/4525 , C07D403/12 , A61K31/4709 , A61K31/4545 , C07D405/14 , C07D417/12 , A61K31/497 , C07D231/12 , C07D401/14 , A61K31/4439 , C07D401/12 , A61K31/404 , C07D209/42 , A61K31/415 , C07D231/14 , C07D213/84 , A61K31/44 , A61K31/444 , A61K31/4418 , C07D213/82 , A61J1/03 , C07D213/64 , C07D209/49 , C07D209/18 , C07D407/12 , C07D239/34 , C07D403/10 , C07D235/24 , C07D401/04 , C07D231/20 , C07D213/73 , C07D413/14 , A61K31/496
Abstract: The present invention features a compound of formula I: or a pharmaceutically acceptable salt thereof, where R1, R2, R3, W, X, Y, Z, n, o, p, and q are defined herein, for the treatment of CFTR mediated diseases, such as cystic fibrosis. The present invention also features pharmaceutical compositions, method of treating, and kits thereof.
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公开(公告)号：US09550761B2
公开(公告)日：2017-01-24
申请号：US13972151
申请日：2013-08-21
Applicant: Vertex Pharmaceuticals Incorporated
Inventor： Sara Sabina Hadida-Ruah , Peter Diederik Jan Grootenhuis , Mark Thomas Miller , Matthew Hamilton
IPC: C07D231/40 , C07D233/08 , C07D263/48 , C07D271/113 , C07D277/46 , C07D277/54 , C07D277/82 , C07D285/135 , C07D405/12 , C07D407/12 , C07D493/10 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D233/88
CPC classification number: C07D417/12 , C07D231/40 , C07D233/88 , C07D263/48 , C07D271/113 , C07D277/46 , C07D277/54 , C07D277/82 , C07D285/135 , C07D405/12 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/14 , C07D493/10
Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
Abstract translation: 本发明涉及ATP结合盒（“ABC”）转运体或其片段的调节剂，包括囊性纤维化跨膜电导调节剂（“CFTR”），其组合物及其方法。 本发明还涉及使用这种调节剂治疗ABC转运蛋白介导的疾病的方法。
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公开(公告)号：US20140309220A1
公开(公告)日：2014-10-16
申请号：US14355325
申请日：2012-11-02
Applicant: VERTEX PHARMACEUTICALS INCORPORATED
Inventor： Sara Sabina Hadida-Ruah , Peter Diederik Jan Grootenhuis , Mark Thomas Miller , Corey Anderson , Joseph Pontillo , Edward Adam Kallel , Mehdi Michael Djamel Numa , Bryan A. Frieman , Jason McCartney , Jennings Franklin Worley, III , Vijayalaksmi Arumugam , Johnny Uy , Nicole Hilgraf , Brian Richard Bear
IPC: C07D498/20 , C07D491/20
CPC classification number: C07D498/20 , C07D491/20
Abstract: The invention relates to benzoxazines useful as inhibitors of ion channels. 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.
Abstract translation: 本发明涉及可用作离子通道抑制剂的苯并恶嗪。 本发明还提供包含本发明化合物的药学上可接受的组合物和使用该组合物治疗各种疾病的方法。
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公开(公告)号：US20140080826A1
公开(公告)日：2014-03-20
申请号：US14036286
申请日：2013-09-25
Applicant: VERTEX PHARMACEUTICALS INCORPORATED
Inventor： SARA SABINA HADIDA RUAH , Peter Diederik Jan Grootenhuis , Frederick F. Van Goor , Jinglan Zhou , Brian Richard Bear , Mark Thomas Miller , Jason Mc Cartney , Mehdi Numa , Xiaoqing Yang
IPC: C07D405/12 , C07D405/14 , C07D403/12
CPC classification number: A61K31/47 , A61K31/404 , A61K31/4045 , A61K31/405 , A61K31/407 , A61K31/41 , A61K31/4184 , A61K31/4192 , A61K31/454 , A61K31/5377 , A61K45/06 , C07D209/08 , C07D233/64 , C07D403/12 , C07D405/12 , C07D405/14 , C07D471/04 , C07D487/04 , G01N33/5035 , G01N2333/705 , G01N2500/10
Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
Abstract translation: 本发明的化合物及其药学上可接受的组合物可用作ATP结合盒（“ABC”）转运蛋白或其片段的调节剂，包括囊性纤维化跨膜电导调节剂（“CFTR”）。 本发明还涉及使用本发明化合物治疗ABC转运蛋白介导的疾病的方法。
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10.发明申请
公开(公告)号：US20240400544A1
公开(公告)日：2024-12-05
申请号：US18566282
申请日：2022-06-03
Applicant: VERTEX PHARMACEUTICALS INCORPORATED
Inventor： Elizabeth Mary BECK , Robert PULLIN , Gorka ETXEBARRIA JARDI , Dean STAMOS , Yvonne SCHMIDT , Joseph PONTILLO , Stephen Andrew THOMSON , David Matthew SHAW , Nadia M. AHMAD , Lidio Marx CARVALHO MEIRELES , Sarah SKERRATT , Sara S. HADIDA RUAH , Timothy Donald NEUBERT , Dennis James HURLEY , Alexander KINTZER , Steven John DURRANT , Christopher WRAY , Anisa Nizarali VIRANI , Kiri NORTH , Reece JACQUES , Mark Thomas Miller , Jinglan ZHOU , Ronald Marcellus KNEGTEL , Ewa Iwona CHUDYK , Joanne Louise PINDER , Bruno Artur SOUSA , James DODD , Michael Edward O'DONNELL , Bhairavi GALAN , Rebecca E. STEVENS
IPC: C07D413/14 , A61K31/4355 , A61K31/443 , A61K31/506 , A61K31/5377 , C07D405/12 , C07D405/14 , C07D491/04
Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.
