Patents Assigned to Vertex Pharmaceuticals, Incorporated
  • Prodrugs of pyridone amides useful as modulators of sodium channels
    Patent number: 9464102
    Abstract: 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.
    Type: Grant
    Filed: September 18, 2015
    Date of Patent: October 11, 2016
    Assignee: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Corey Anderson, Sara Sabina Hadida-Ruah, Julian Marian Charles Golec, Beili Zhang, Benjamin Joseph Littler, Ali Keshavarz-Shokri, Tim Edward Alcacio, Daniel T. Belmont
  • COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
    Publication number: 20160271129
    Abstract: The present invention relates to pyrazine and pyridine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating 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 methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula IV: wherein the variables are as defined herein.
    Type: Application
    Filed: March 18, 2016
    Publication date: September 22, 2016
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven John Durrant, Ronald Marcellus Alphonsus Knegtel, Anisa Nizarali Virani, Philip Michael Reaper
  • Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl) benzoic acid
    Patent number: 9434717
    Abstract: 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.
    Type: Grant
    Filed: August 31, 2015
    Date of Patent: September 6, 2016
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Ali Keshavarz-Shokri, Beili Zhang, Mariusz Krawiec
  • DNA-PK INHIBITORS
    Publication number: 20160250212
    Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: February 29, 2016
    Publication date: September 1, 2016
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Paul S. Charifson, Kevin Michael Cottrell, Hongbo Deng, John P. Duffy, Huai Gao, Simon Giroux, Jeremy Green, Katrina Lee Jackson, Joseph M. Kennedy, David J. Lauffer, Mark Willem Ledeboer, Pan Li, John Patrick Maxwell, Mark A. Morris, Albert Charles Pierce, Nathan D. Waal, Jinwang Xu
  • Pyrimidine compounds as tuberculosis inhibitors
    Patent number: 9422271
    Abstract: The present invention relates to compounds useful as inhibitors of treating tuberculosis. The invention also provides processes for preparing compounds of the invention.
    Type: Grant
    Filed: October 31, 2013
    Date of Patent: August 23, 2016
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Tiansheng Wang, Brian Hanzelka, Ute Muh, Guy Bemis, Harmon J. Zuccola
  • Amides as modulators of sodium channels
    Patent number: 9421196
    Abstract: The invention relates to 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.
    Type: Grant
    Filed: July 27, 2015
    Date of Patent: August 23, 2016
    Assignee: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Sabina Hadida-Ruah, Corey Anderson, Vijayalaksmi Arumugam, Iuliana Luci Asgian, Brian Richard Bear, Andreas P. Termin, James Philip Johnson
  • SOLID FORMS OF N-[2,4-BIS(1,1-DIMETHYLETHYL)-5-HYDROXYPHENYL]-1,4-DIHYDRO-4-OXOQUINOLINE-3-CARBOXAMIDE
    Publication number: 20160229806
    Abstract: The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.
    Type: Application
    Filed: September 14, 2015
    Publication date: August 11, 2016
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Patricia Hurter, William Rowe, Christopher R. Young, Adriana Costache, Patrick R. Connelly, Mariusz Krawiec, Yuchuan Gong, Yushi Feng, Martin Trudeau
  • MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
    Publication number: 20160221952
    Abstract: This invention relates to a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein R is COOH or CH2OH.
    Type: Application
    Filed: December 31, 2015
    Publication date: August 4, 2016
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Xiaoqing Yang, Sara Sabina Hadida Ruah, Peter Diederik Jan Grootenhuis, Fredrick F. Van Goor, Martyn Curtis Botfield, Gregor Zlokarnik
  • SOLID FORMS OF 3-(6-(1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL)CYCLOPROPANECARBOXAMIDO)-3-METHYLPYRIDIN-2-YL) BENZOIC ACID
    Publication number: 20160221995
    Abstract: 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.
    Type: Application
    Filed: April 12, 2016
    Publication date: August 4, 2016
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Ali Keshavarz-Shokri, Beili Zhang, Mariusz Krawiec
  • Pyran-spirocyclic piperidine amides as modulators of ion channels
    Patent number: 9403839
    Abstract: The invention relates to pyran spirocyclic piperidine amide compounds 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.
    Type: Grant
    Filed: January 15, 2013
    Date of Patent: August 2, 2016
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Sabina Hadida-Ruah, Vijayalaksmi Arumugam, Michael Paul Deninno, Bryan A. Frieman, Edward Adam Kallel, Mark Thomas Miller, Johnny Uy, Jinglan Zhou
  • Isothiazolopyridinones useful for the treatment of (inter alia) cystic fibrosis
    Patent number: 9399648
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Grant
    Filed: June 27, 2014
    Date of Patent: July 26, 2016
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventor: Alejandra Gallardo-Godoy
  • Inhibitors of influenza viruses replication
    Patent number: 9394302
    Abstract: This invention provides methods of preparing 3-(pyrimidin-2-yl)-1H-pyrrolo[2,3-b]pyridines and 3-(pyrimidin-2-yl)-1H-pyrazolo[3,4-b]pyridines, or pharmaceutically acceptable salts thereof that are useful for inhibiting the replication of influenza viruses in a biological sample or patient, reducing the amount of influenza viruses in a biological sample or patient, and treating influenza in a patient.
    Type: Grant
    Filed: March 24, 2015
    Date of Patent: July 19, 2016
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Paul S. Charifson, Michael P. Clark, Upul K. Bandarage, Randy S. Bethiel, Michael J. Boyd, Ioana Davies, Hongbo Deng, John P. Duffy, Luc J. Farmer, Huai Gao, Wenxin Gu, Joseph M. Kennedy, Brian Ledford, Mark W. Ledeboer, Francois Maltais, Emanuele Perola, Tiansheng Wang
  • Pyridone amides as modulators of sodium channels
    Patent number: 9393235
    Abstract: 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.
    Type: Grant
    Filed: April 29, 2015
    Date of Patent: July 19, 2016
    Assignee: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Sabina Hadida-Ruah, Corey Anderson, Vijayalaksmi Arumugam, Iuliana Luci Asgian, Brian Richard Bear, Andreas P. Termin, James Philip Johnson
  • PROCESSES FOR PRODUCING CYCLOALKYLCARBOXAMIDO-PYRIDINE BENZOIC ACIDS
    Publication number: 20160200712
    Abstract: The present invention relates to a process of providing the 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid in substantially free form (Compound 1).
    Type: Application
    Filed: March 17, 2016
    Publication date: July 14, 2016
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventor: David Siesel
  • Pharmaceutical Compositions for the Treatment of CFTR-Mediated Disorders
    Publication number: 20160200684
    Abstract: The present invention relates to the use of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), solids forms, and pharmaceutical compositions thereof for the treatment of CFTR-mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations. The present invention also relates to the use of Compound 1 in combination with 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Compound 2), and Compound 1 in combination with (S)-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 3), for the treatment of CFTR-mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations.
    Type: Application
    Filed: November 26, 2014
    Publication date: July 14, 2016
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Fredrick F. Van Goor, William Lawrence Burton, Haihul Yu, Beth Jennifer Hoffman
  • DNA-PK inhibitors
    Patent number: 9376448
    Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Grant
    Filed: October 17, 2013
    Date of Patent: June 28, 2016
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Paul S. Charifson, Kevin Michael Cottrell, Hongbo Deng, John P. Duffy, Huai Gao, Simon Giroux, Jeremy Green, Katrina Lee Jackson, Joseph M. Kennedy, David J. Lauffer, Mark Willem Ledeboer, Pan Li, John Patrick Maxwell, Mark A. Morris, Albert Charles Pierce, Nathan D. Waal, Jinwang Xu
  • Process for making modulators of cystic fibrosis transmembrane conductance regulator
    Patent number: 9371287
    Abstract: The invention provides a process for the preparation of a compound of Formula 1, comprising coupling a carboxylic acid of Formula 2 with an aniline of Formula 3 in the presence of a coupling agent.
    Type: Grant
    Filed: May 23, 2014
    Date of Patent: June 21, 2016
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: John DeMattei, Adam R. Looker, Bobbianna Neubert-Langille, Martin Trudeau, Stefanie Roeper, Michael P. Ryan, Dahrika Milfred Yap Guerette, Brian R. Krueger, Peter D. J. Grootenhuis, Fredrick F. Van Goor, Martyn C. Botfield, Gregor Zlokarnik
  • Substituted pyrazin-2-amines as inhibitors of ATR kinase
    Patent number: 9365557
    Abstract: The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also 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 methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. Certain compounds of this invention have formula IA: wherein the variables are as defined herein.
    Type: Grant
    Filed: March 24, 2014
    Date of Patent: June 14, 2016
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven Durrant, David Kay, Ronald Knegtel, Somhairle MacCormick, Michael Mortimore, Michael O'Donnell, Joanne Pinder, Alistair Rutherford, Anisa Nizarali Virani, Stephen Young, Philip Michael Reaper
  • Benzoxazines as modulators of ion channels
    Patent number: 9365588
    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.
    Type: Grant
    Filed: November 2, 2012
    Date of Patent: June 14, 2016
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: 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
  • Pyrrole inhibitors of ERK protein kinase, synthesis thereof and intermediates thereto
    Patent number: RE46097
    Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Grant
    Filed: August 23, 2013
    Date of Patent: August 9, 2016
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Gabriel Martinez Botella, Michael Hale, Francois Maltais, Judith Straub, Qing Tang