Patents Assigned to Vertex Pharmaceuticals, Incorporated
  • Inhibitors of influenza viruses replication
    Patent number: 10039762
    Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A compound is represented by Structural Formula (IA) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.
    Type: Grant
    Filed: September 28, 2017
    Date of Patent: August 7, 2018
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Paul S. Charifson, Michael P. Clark, Upul K. Bandarage, Randy S. Bethiel, John J. Court, Hongbo Deng, Ioana Davies, John P. Duffy, Luc J. Farmer, Huai Gao, Wenxin Gu, Dylan H. Jacobs, Joseph M. Kennedy, Mark W. Ledeboer, Brian Ledford, Francois Maltais, Emanuele Perola, Tiansheng Wang, M. Woods Wannamaker, Randal Byrn, Yi Zhou, Chao Lin, Min Jiang, Steven Jones, Ursula A. Germann, Francesco G. Salituro, Ann Dak-Yee Kwong
  • Imidazopyridazines useful as inhibitors of the PAR-2 signaling pathway
    Patent number: 10030024
    Abstract: The present invention relates to compounds useful as inhibitors of the PAR-2 signaling pathway. 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 GPCRs in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such GPCRs; and the comparative evaluation of new inhibitors of the PAR-2 signaling pathway. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Grant
    Filed: March 25, 2016
    Date of Patent: July 24, 2018
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Luc J. Farmer, Pierre-Andre Fournier, Stephanie Lessard, Bingcan Liu, Miguel St-Onge, Claudio Sturino, Janek Szychowski, Constantin Yannopoulos, Frederic Vallee, Jean-Eric Lacoste, Julien Martel, Monica Bubenik, Yeeman Ramtohul, Camil Elie Sayegh
  • Methods of preparing inhibitors of influenza viruses replication
    Patent number: 10023569
    Abstract: A method of preparing Compound (1) or a pharmaceutically acceptable salt thereof: comprises: (a) reacting Compound (X): or a pharmaceutically acceptable salt thereof with Compound (Y): in the presence of a palladium catalyst and a carbonate or phosphate base to form compound (Z): or a pharmaceutically acceptable salt thereof; and (b) deprotecting the Ts group of Compound (Z) to form Compound (1) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 10, 2016
    Date of Patent: July 17, 2018
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Gerald J. Tanoury, William Aloysius Nugent, Vadims Dvornikovs, Peter Jamison Rose
  • Modulators of ATP-binding cassette transporters
    Patent number: 10022352
    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.
    Type: Grant
    Filed: March 23, 2016
    Date of Patent: July 17, 2018
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Sabina Hadida Ruah, Peter Diederik Jan Grootenhuis, Fredrick F. Van Goor, Jinglan Zhou, Brian Richard Bear, Mark Thomas Miller, Jason McCartney, Mehdi Michel Djamel Numa
  • MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
    Publication number: 20180185364
    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.
    Type: Application
    Filed: August 11, 2017
    Publication date: July 5, 2018
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Mark Thomas Miller, Corey Anderson, Vijayalaksmi Arumugam, Brian Richard Bear, Hayley 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
  • Methods of regioselective synthesis of 2,4-disubstituted pyrimidines
    Patent number: 10005737
    Abstract: The present invention relates to the novel regioselective syntheses of 2,4-disubstituted pyrimidines through sequential nucleophilic aromatic substitutions.
    Type: Grant
    Filed: November 22, 2016
    Date of Patent: June 26, 2018
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Michael Edward O'Donnell
  • DNA-PK INHIBITORS
    Publication number: 20180161336
    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: July 25, 2017
    Publication date: June 14, 2018
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: John Patrick Maxwell, Paul S. Charifson, Qing Tang, Steven M. Ronkin, Katrina Lee Jackson, Albert Charles Pierce, David J. Lauffer, Pan Li, Simon Giroux, Jinwang Xu, Kevin Michael Cottrell, Mark A. Morris, Nathan D. Waal, John J. Court, Wenxin Gu, Hongbo Deng
  • Prodrug of an ICE inhibitor
    Patent number: 9994613
    Abstract: This invention describes an ICE inhibitor prodrug (I) having good bioavailability. Compound I is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, myocardial infarction, congestive heart failure, Huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.
    Type: Grant
    Filed: October 7, 2016
    Date of Patent: June 12, 2018
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Marion W. Wannamaker, Robert J. Davies
  • PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF
    Publication number: 20180153874
    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.
    Type: Application
    Filed: July 6, 2017
    Publication date: June 7, 2018
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: 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
  • Substituted benzooxadiazole DNA-PK inhibitors
    Patent number: 9987284
    Abstract: Provided are compounds of Formula (I): wherein R1, R2, X, Ring A, Ring B, and Ring C are as defined herein. Compounds of Formula (I) are useful as inhibitors of DNA-PK. Also provided are pharmaceutical compositions comprising said compounds and methods of using the compounds and compositions in the treatment of various diseases, conditions, and disorders.
    Type: Grant
    Filed: April 20, 2016
    Date of Patent: June 5, 2018
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: John Patrick Maxwell, Paul S. Charifson, Qing Tang, Steven M. Ronkin, Katrina Lee Jackson, Albert Charles Pierce, David J. Lauffer, Pan Li, Simon Giroux, Jinwang Xu, Kevin Michael Cottrell, Mark A. Morris, Nathan D. Waal, John J. Court, Wenxin Gu, Hongbo Deng
  • Modulators of ATP-binding cassette transporters
    Patent number: 9974781
    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.
    Type: Grant
    Filed: August 11, 2016
    Date of Patent: May 22, 2018
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Sabina Hadida Ruah, Peter Diederik Jan Grootenhuis, Fredrick F. Van Goor, Jinglan Zhou, Brian Richard Bear, Mark Thomas Miller, Jason McCartney, Mehdi Michel Djamel Numa
  • SOLID FORMS OF 3-(6-(1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL)CYCLOPROPANECARBOXAMIDO)-3-METHYLPYRIDIN-2-YL) BENZOIC ACID
    Publication number: 20180127398
    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-methypyridin-2-yl)benzoic acid (Form I), pharmaceutical compositions thereof, and methods of treatment therewith.
    Type: Application
    Filed: November 9, 2017
    Publication date: May 10, 2018
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Ali Keshavarz-Shokri, Beili Zhang, Mariusz Krawiec
  • Mannose derivatives for treating bacterial infections
    Patent number: 9963478
    Abstract: The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: The invention also provides pharmaceutically acceptable compositions containing the compounds and methods of using the compositions in the treatment of bacteria infections. Finally, the invention provides processes for making compounds of the invention.
    Type: Grant
    Filed: April 27, 2016
    Date of Patent: May 8, 2018
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Yeeman K. Ramtohul, Sanjoy Kumar Das, Caroline Cadilhac, Thumkunta Jagadeeswar Reddy, Louis Vaillancourt, Michel Gallant, Bingcan Liu, Evelyne Dietrich, Frederic Vallee, Julien Martel, Carl Poisson
  • Solid forms of N[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
    Patent number: 9931334
    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: Grant
    Filed: May 2, 2017
    Date of Patent: April 3, 2018
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Patricia Hurter, William Rowe, Christopher R. Young, Adriana Costache, Patrick R. Connelly, Mariusz Krawiec, Yuchuan Gong, Yushi Feng, Martin Trudeau
  • DNA-PK inhibitors and uses thereof
    Patent number: 9925188
    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: February 29, 2016
    Date of Patent: March 27, 2018
    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
  • Inhibitors of influenza viruses replication
    Patent number: 9908878
    Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.
    Type: Grant
    Filed: June 9, 2016
    Date of Patent: March 6, 2018
    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
  • Mannose derivatives for treating bacterial infections
    Patent number: 9890176
    Abstract: The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: The invention also provides processes for making the compounds described herein. Furthermore, the present invention provides a composition comprising the compounds described herein, and a pharmaceutically acceptable carrier, adjuvant, or vehicle. The present invention also provides methods of treating or preventing bacteria infection in a subject, comprising administering to the subject an effective amount of the compound or the composition described herein.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: February 13, 2018
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Evelyne Dietrich, Carl Poisson, Michel Gallant, Stephanie Lessard, Bingcan Liu, Sanjoy Kumar Das, Yeeman Ramtohul, Thumkunta Jagadeeswar Reddy, Julien Martel, Frederic Vallee, Jean-Francois Lévesque
  • DNA-PK inhibitors for treatment of cancer
    Patent number: 9878993
    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: May 19, 2016
    Date of Patent: January 30, 2018
    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
  • FORMULATIONS OF 3-(6-(1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL) CYCLOPROPANECARBOXAMIDO)-3-METHYLPYRIDIN-2-YL)BENZOIC ACID
    Publication number: 20180008546
    Abstract: A pharmaceutical composition comprising Compound 1, (3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid), and at least one excipient selected from: a filler, a disintegrant, a surfactant, a binder, and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Processes of preparing pharmaceutical compositions comprising Compound 1 are also disclosed.
    Type: Application
    Filed: July 20, 2017
    Publication date: January 11, 2018
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventor: Marinus Jacobus Verwijs
  • Processes for making compounds useful as inhibitors of ATR kinase
    Patent number: 9862709
    Abstract: The present invention relates to processes and intermediates for preparing compounds useful as inhibitors of ATR kinase, such as aminopyrazine-isoxazole derivatives and related molecules. The present invention also 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 or II: wherein the variables are as defined herein.
    Type: Grant
    Filed: April 3, 2015
    Date of Patent: January 9, 2018
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, John Studley, Francoise Yvonne Theodora Marie Pierard, Steven John Durrant, Benjamin Joseph Littler, Robert Michael Hughes, David Andrew Siesel, Paul Angell, Armando Urbina, Yi Shi