Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
Type:
Grant
Filed:
November 3, 2006
Date of Patent:
October 26, 2010
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Hayley Binch, Michael Mortimore, Damien Fraysse, Alistair Rutherford
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:
Application
Filed:
March 19, 2010
Publication date:
October 21, 2010
Applicant:
VERTEX PHARMACEUTICALS INCORPORATED
Inventors:
John DeMattei, Adam R. Looker, Bobbianna Neubert-Langille, Martin Trudeau, Stefanie Roeper, Michael P. Ryan, Dahrika Milfred Lao Yap, Brian R. Krueger, Peter D.J. Grootenhuis, Fredrick F. van Goor, Martyn C. Botfield, Gregor Zlokarnik
Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated 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:
July 2, 2004
Date of Patent:
October 19, 2010
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Dean Mitchell Wilson, Esther Martinborough, Timothy Donald Neubert, Andreas Peter Termin, Jesus E. Gonzalez, III, Nicole Zimmerman
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:
Application
Filed:
March 12, 2010
Publication date:
October 14, 2010
Applicant:
VERTEX PHARMACEUTICALS INCORPORATED
Inventors:
Hayley Binch, Peter D.J. Grootenhuis, Sara S. Hadida Ruah, Jinglan Zhou, Anna Hazlewood, Lev T.D. Fanning
Abstract: This invention describes novel pyrazole compounds of formula IV: wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-8 membered ring having 1-3 ring heteroatoms selected from oxygen, sulfur, or nitrogen; and R2, R2?, T, and R3 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
Type:
Application
Filed:
January 4, 2010
Publication date:
October 7, 2010
Applicant:
VERTEX PHARMACEUTICALS INCORPORATED
Inventors:
David Bebbington, Hayley Binch, Ronald Knegtel, Julian Golec, Sanjay Patel, Jean-Damien Charrier, David Kay, Robert Davies, Pan Li, Marion Wannamaker, Cornelia Forster, Albert Pierce
Abstract: The present invention relates to pharmaceutical compositions comprising a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, methods of manufacturing pharmaceutical compositions of the present invention, and methods of administering pharmaceutical compositions of the present invention.
Type:
Application
Filed:
February 18, 2010
Publication date:
October 7, 2010
Applicant:
Vertex Pharmaceuticals Incorporated
Inventors:
William Rowe, Patricia Hurter, Christopher R. Young, Kirk Dinehart, Marinus Jacobus Verwijs, Kirk Overhoff, Peter D.J. Grootenhuis, Martyn Botfield, Alfredo Grossi, Gregor Zlokarnik, Fredrick F. Van Goor
Abstract: The present invention provides methods for stimulating naive T-cells or memory T-cells to produce IL-17, methods for identifying modulators of IL-17 production, and methods for treating IL-17 mediated disorders.
Abstract: The present invention relates to novel classes of compounds of formula I which are caspase and TNF-alpha inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase and TNF-alpha activity and consequently, can be advantageously used as agents against caspase-, interleukin-1-(“IL-1”), apoptosis-, interferon-? inducing factor-(IGIF), interferon-?-(“IFN-?”), or TNF-alpha mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to processes for preparing the compounds of this invention.
Type:
Grant
Filed:
September 14, 2006
Date of Patent:
October 5, 2010
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Anita Diu-Hercend, Julian Golec, Thierry Hercend, Ronald Knegtel, Paul Lang, Andrew Miller, Karen Miller, Michael Mortimore, Peter Weber
Abstract: The present invention provides crystalline molecules or molecular complexes which comprise binding pockets of Aurora-2 or its homologues. The invention also provides crystals comprising Aurora-2. The present invention also relates to a computer comprising a data storage medium encoded with the structural coordinates of Aurora-2 binding pockets and methods of using a computer to evaluate the ability of a compound to bind to the molecule or molecular complex. This invention also provides methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. In addition, this invention provides methods of using the structure coordinates to screen for and design compounds, including inhibitory compounds, that bind to Aurora-2 or homologues thereof.
Type:
Grant
Filed:
February 13, 2008
Date of Patent:
October 5, 2010
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Graham Cheetham, Ronald Knegtel, Lovorka Swenson, Joyce T. Coll, Suzanne Renwick, Peter Weber
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.
Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium 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:
Application
Filed:
March 29, 2010
Publication date:
September 30, 2010
Applicant:
VERTEX PHARMACEUTICALS INCORPORATED
Inventors:
Dean Wilson, Lev Fanning, Paul Krenitsky, Joshua Boger
Abstract: The present invention features vectors that contain a promoter effective for expression in bacterial cells and a promoter effective for expression in insect cells. The dual promoter system allows use of the same vector in both host cell systems so that construction of only a single vector is needed to express a polynucleotide inserted at a downstream cloning site. In preferred embodiments the vector is used to derive a recombinant baculovirus that is used to infect host cells. In particular vectors the promoters are a baculovirus polh promoter and a T7lac promoter. In particular vectors the promoter effective for expression in bacteria is positioned between the promoter effective for expression in insect cells and a cloning site. The invention also features various high throughput screening methods.
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:
Application
Filed:
February 12, 2010
Publication date:
September 30, 2010
Applicant:
VERTEX PHARMACEUTICALS INCORPORATED
Inventors:
Sara S. Hadida Ruah, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney
Abstract: The present invention relates to phenyl sulfonamides 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, including for example the treatment of pain.
Type:
Grant
Filed:
December 21, 2006
Date of Patent:
September 21, 2010
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Esther Martinborough, Lev T. D. Fanning, Urvi Sheth, Dean Wilson, Andreas Termin, Timothy Neubert, Nicole Zimmermann, Tara Knoll, Tara Whitney, Aarti Kawatkar, Danielle Lehsten, Dean Stamos, Jinglan Zhou, Vijayalaksmi Arumugam, Corey Gutierrez
Abstract: The present invention relates to processes for the preparation of compounds useful as inhibitors of p38 kinase. The processes of the present invention are amenable for large scale preparation and produce stable phenyl-6-(1-(phenyl)ureido)nicotinamides in high purity and yields.
Type:
Application
Filed:
February 12, 2010
Publication date:
September 16, 2010
Applicant:
Vertex Pharmaceuticals Incorporated
Inventors:
Stefanie Roeper, Adam R. Looker, Theodore A. Martinot, Bobbianna Neubert-Langille, Michael P. Ryan, John R. Snoonian
Abstract: The present invention relates to compound 1, which is useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising Compound 1 and methods of using the compositions in the treatment of proliferative disorders.
Type:
Application
Filed:
November 18, 2009
Publication date:
September 16, 2010
Applicant:
VERTEX PHARMACEUTICALS INCORPORATED
Inventors:
David Lauffer, Pan Li, Dean Shannon, Jianglin Liang
Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinase of the following formula: or a pharmaceutically acceptable salt thereof. 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. The invention also provides processes for preparing compounds of the inventions.
Type:
Grant
Filed:
November 22, 2005
Date of Patent:
September 14, 2010
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Hayley Binch, Daniel Robinson, Damien Fraysse, Andrew Miller
Abstract: The present invention relates to inhibitors of GSK-3 and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors and methods of utilizing those compositions in the treatment and prevention of various disorders, such as diabetes and Alzheimer's disease. In addition, the invention relates to molecules or molecular complexes which comprise binding pockets of GSK-3? or its homologues. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to GSK-3? protein or homologues thereof. The invention also relates to crystallizable compositions and crystals comprising GSK-3? protein or GSK-3? protein complexes.
Type:
Application
Filed:
January 5, 2010
Publication date:
September 9, 2010
Applicant:
Vertex Pharmaceuticals Incorporated
Inventors:
Ernst ter Haar, Lovorka Swenson, Jeremy Green, Michael J. Arnost
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 (“CFTC”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
Type:
Application
Filed:
May 19, 2010
Publication date:
September 9, 2010
Applicant:
VERTEX PHARMACEUTICALS INCORPORATED
Inventors:
Sara S. Hadida Ruah, Mark Miller, Brian Bear, Jinglan Zhou, Jason McCartney, Peter Grootenhuis