公开(公告)号：US20220313698A1

公开(公告)日：2022-10-06

申请号：US16992675

申请日：2020-08-13

申请人： Vertex Pharmaceuticals Incorporated

发明人： 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分类号： A61K31/529 ,  A61K31/404 ,  A61K31/47 ,  A61K31/4418 ,  A61K31/439 ,  C07D513/22

摘要： 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.

公开(公告)号：US11186566B2

公开(公告)日：2021-11-30

申请号：US16702891

申请日：2019-12-04

申请人： Vertex Pharmaceuticals Incorporated

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

IPC分类号： C07D401/14 ,  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.

公开(公告)号：US20210047345A1

公开(公告)日：2021-02-18

申请号：US16992419

申请日：2020-08-13

申请人： Vertex Pharmaceuticals Incorporated

发明人： 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分类号： C07D513/22 ,  C07D401/14 ,  C07D401/04 ,  C07D213/71 ,  C07D213/82 ,  C07D207/08 ,  C07D231/20

摘要： The disclosure provides processes for synthesizing Compound I, and pharmaceutically acceptable salts thereof.

公开(公告)号：US20210047323A1

公开(公告)日：2021-02-18

申请号：US16992441

申请日：2020-08-13

申请人： Vertex Pharmaceuticals Incorporated

发明人： 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分类号： C07D471/08

摘要： 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.

公开(公告)号：US10738009B2

公开(公告)日：2020-08-11

申请号：US16107109

申请日：2018-08-21

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： Sara Sabina Hadida Ruah ,  Corey Anderson ,  Vijayalaksmi Arumugam ,  Iuliana Luci Asgian ,  Brian Richard Bear ,  Andreas P. Termin ,  James Philip Johnson

IPC分类号： C07D213/75 ,  C07D405/12 ,  C07D401/12 ,  A61K31/4412

摘要： The invention relates to pyridone amide compounds of formula I and I′ or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium 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, including pain.

公开(公告)号：US20190248745A1

公开(公告)日：2019-08-15

申请号：US16107109

申请日：2018-08-21

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： Sara Sabina Hadida Ruah ,  Corey Anderson ,  Vijayalaksmi Arumugam ,  Iuliana Luci Asgian ,  Brian Richard Bear ,  Andreas P. Termin ,  James Philip Johnson

IPC分类号： C07D213/75 ,  A61K31/4412 ,  C07D405/12 ,  C07D401/12

摘要： The invention relates to pyridone amide compounds of formula I and I′ or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium 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, including pain.

公开(公告)号：US11866450B2

公开(公告)日：2024-01-09

申请号：US17323267

申请日：2021-05-18

申请人： Vertex Pharmaceuticals Incorporated

发明人： Jeremy J. Clemens ,  Alexander Russell Abela ,  Corey Don Anderson ,  Brett B. Busch ,  Weichao George Chen ,  Thomas Cleveland ,  Timothy Richard Coon ,  Bryan Frieman ,  Senait G. Ghirmai ,  Peter Grootenhuis ,  Anton V. Gulevich ,  Sara Sabina Hadida Ruah ,  Clara Kuang-Ju Hsia ,  Ping Kang ,  Haripada Khatuya ,  Jason McCartney ,  Mark Thomas Miller ,  Prasuna Paraselli ,  Fabrice Pierre ,  Sara E. Swift ,  Andreas Termin ,  Johnny Uy ,  Carl V. Vogel ,  Jinglan Zhou

IPC分类号： C07D513/22 ,  A61K31/439 ,  A61P11/00 ,  A61K31/47 ,  A61K31/404 ,  C07D515/22

CPC分类号： C07D513/22 ,  A61K31/404 ,  A61K31/439 ,  A61K31/47 ,  A61P11/00 ,  C07D515/22

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.

公开(公告)号：US20230382910A1

公开(公告)日：2023-11-30

申请号：US18305186

申请日：2023-04-21

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： Mark Thomas Miller ,  Dennis James Hurley ,  Timothy Donald Neubert ,  Elamprakash Nesan Savariar ,  Urvi Patel ,  Sara Sabina Hadida Ruah ,  Jason McCartney ,  Jinglan Zhou ,  Robert Martin Demoret ,  Roman Askatovich Valiulin ,  Alexander Frederik Kintzer ,  Peter Webb ,  David Robert Slochower ,  Kathleen Aertgeerts ,  Elizabeth Mary Beck ,  Ronald Marcellus Alphonsus Knegtel ,  Ewa Iwona Chudyk ,  Joanne Louise Pinder

IPC分类号： C07D471/04 ,  C07D215/233 ,  C07D215/22 ,  C07D215/60 ,  C07D215/48 ,  C07D401/04

CPC分类号： C07D471/04 ,  C07D215/233 ,  C07D215/22 ,  C07D215/60 ,  C07D215/48 ,  C07D401/04

摘要： Compounds, 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.

公开(公告)号：US20230373925A1

公开(公告)日：2023-11-23

申请号：US18137939

申请日：2023-04-21

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： Mark Thomas Miller ,  Dennis James Hurley ,  Timothy Donald Neubert ,  Vijayalaksmi Arumugam ,  Sara Sabina Hadida Ruah ,  Jason McCartney ,  Jinglan ZHOU ,  Jaclyn Chau ,  Robert Martin Demoret ,  Senait G. Ghirmai ,  Roman Askatovich Valiulin ,  Alexander Frederik Kintzer ,  David Robert Slochower ,  Kathleen Aertgeerts ,  Elizabeth Mary Beck ,  James Jun Bon Mui ,  Miranda Adele Wright ,  Ronald Marcellus Alphonsus Knegtel ,  Ewa Iwona Chudyk ,  Joanne Louise Pinder ,  James Dodd

IPC分类号： C07D215/233 ,  C07D471/04 ,  C07D239/91 ,  C07D401/14 ,  C07D401/04 ,  C07D519/00

CPC分类号： C07D215/233 ,  C07D471/04 ,  C07D239/91 ,  C07D401/14 ,  C07D401/04 ,  C07D519/00 ,  C07B2200/05

摘要： Compounds, 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.

公开(公告)号：US11066417B2

公开(公告)日：2021-07-20

申请号：US16276350

申请日：2019-02-14

申请人： Vertex Pharmaceuticals Incorporated

发明人： Jeremy J. Clemens ,  Alexander Russell Abela ,  Corey Don Anderson ,  Brett B. Busch ,  Weichao George Chen ,  Thomas Cleveland ,  Timothy Richard Coon ,  Bryan Frieman ,  Senait G. Ghirmai ,  Peter Grootenhuis ,  Anton V. Gulevich ,  Sara Sabina Hadida Ruah ,  Clara Kuang-Ju Hsia ,  Ping Kang ,  Haripada Khatuya ,  Jason McCartney ,  Mark Thomas Miller ,  Prasuna Paraselli ,  Fabrice Pierre ,  Sara E. Swift ,  Andreas Termin ,  Johnny Uy ,  Carl V. Vogel ,  Jinglan Zhou

IPC分类号： A61K31/44 ,  A61K31/435 ,  C07D513/22 ,  A61K31/439 ,  A61P11/00 ,  A61K31/47 ,  A61K31/404 ,  C07D515/22

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.