Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention, processes for preparing the compounds and methods of using the compositions in the treatment of various disorders.
Type:
Grant
Filed:
August 6, 2004
Date of Patent:
June 5, 2007
Assignee:
Vertex Pharmaceuticals Inc.
Inventors:
Michael J. Arnost, Guy W. Bemis, Robert J. Davies, Cornelia J. Forster, Ronald Grey, Jr., Mark W. Ledeboer, Brian Ledford, Craig Marhefka, David Messersmith, Albert C. Pierce, Francesco G. Salituro, Jian Wang
Abstract: The present invention provides a compound of formula (I): or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK-3, JAK-3, FLT-3, PIM-1, SYK, or PDK-1 mammalian protein kinases. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.
Type:
Grant
Filed:
December 17, 2003
Date of Patent:
June 5, 2007
Assignee:
Vertex Pharmaceuticals Inc.
Inventors:
Mark Ledeboer, Robert Davies, David Messersmith, Young-Choon Moon, Michael Mullican
Abstract: A liquid level sensor comprises a plurality of electrodes arranged in a defined relationship with respect to a container filling trajectory, a signal generator coupled to one or more of the plurality of electrodes, a signal receiver coupled to one or more of the plurality of electrodes, and a sensing circuit coupled to at least one of the signal generator and signal receiver. The sensing circuit is configured to produce an output indicative of electrical resistance between at least one pair of the plurality of electrodes. The sensing circuit may be associated with the signal receiver and/or with the signal generator.
Type:
Grant
Filed:
July 28, 2004
Date of Patent:
May 22, 2007
Assignee:
Vertex Pharmaceuticals, Inc.
Inventors:
Philip E. Salzmann, Alec T. Harootunian, Michael P. Emery, Javier H. Flores, Todd N. Bennett, Minh Vuong
Abstract: The present invention relates to compounds of formula I that are useful as GSK-3 inhibitors. The invention also relates to methods of using compounds of formula I or pharmaceutical compositions comprising compounds of formula I to inhibit GSK-3 activity. The invention further provides methods of utilizing these compounds and pharmaceutical compositions in the treatment and prevention of various GSK-3-mediated disorders, such as diabetes and Alzheimer's disease.
Abstract: The present invention relates to a data storage medium encoded with the corresponding structure coordinates of molecules and molecular complexes which comprise the active site binding pockets of IMPDH. Such data storage material is capable of displaying such molecules and molecular complexes, or their structural homologues, as a graphical three-dimensional representation on a computer screen. This invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. In addition, this invention relates to methods of using the structure coordinates to screen and design compounds, including inhibitory compounds, that bind to IMPDH or homologues thereof. This invention also relates to molecules and molecular complexes which comprise the active site binding pockets of IMPDH or close structural homologues of the active site binding pockets. This invention also relates to compounds and pharmaceutical compositions which are inhibitors of IMPDH.
Type:
Grant
Filed:
October 2, 2000
Date of Patent:
May 8, 2007
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Keith P. Wilson, Michael D. Sintchak, Mark Andrew Fleming, David M. Armistead
Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3–NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection and to processes for preparing the compounds. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.
Type:
Grant
Filed:
October 12, 2004
Date of Patent:
April 24, 2007
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Kevin M. Cottrell, Robert B. Perni, Janos Pitlik
Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
Type:
Grant
Filed:
July 17, 2003
Date of Patent:
April 17, 2007
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Guy W Bemis, Francesco G Salituro, John P Duffy, John E Cochran, Edmund M Harrington, Mark A Murcko, Keith P Wilson, Michael Su, Vincent P Galullo
Abstract: This invention provides caspase inhibitors having the formula: wherein R1 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R2 and R3 are each independently selected from hydrogen or an optionally substituted C1–C6 aliphatic group; and R4 and R5 are each independently selected from hydrogen, an optionally substituted C1–C6 aliphatic group, or R4 and R5 taken together with the ring to which they are attached form an optionally substituted bicyclic ring. The caspase inhibitors are useful for treating a number of diseases such as cancer, acute inflammatory and autoimmune disorders, ischemic diseases and certain neurodegenerative disorders.
Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
Type:
Application
Filed:
May 8, 2006
Publication date:
March 15, 2007
Applicant:
VERTEX PHARMACEUTICALS INCORPORATED
Inventors:
Francesco Salituro, Vincent Galullo, Steven Bellon, Guy Bemis, John Cochran
Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to inhibitors of ZAP70. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
Type:
Grant
Filed:
February 11, 2003
Date of Patent:
March 6, 2007
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
John Cochran, Vincent Galullo, Guy W. Bemis
Abstract: The present invention is directed to a splice variant of a human sodium channel alpha subunit and methods and compositions for making and using the same.
Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein B, R1, n, R3, Q and R4 are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.
Type:
Grant
Filed:
May 3, 2004
Date of Patent:
February 27, 2007
Assignee:
Vertex Pharmaceuticals Incroporated
Inventors:
Michael Robin Hale, James Walter Janetka, Francois Maltais, Qing Tang
Abstract: The present invention relates to compounds useful as 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:
March 14, 2003
Date of Patent:
February 20, 2007
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
David Bebbington, Hayley Binch, Jean-Damien Charrier, Simon Everitt, Julian M. C. Golec, David Kay, Ronald Knegtel, Andrew Miller, Francoise Pierard
Abstract: Drug candidate screening methods are applied to discover compounds with activity against ion channel targets. The method may include modulating the transmembrane potential of host cells in a plurality of sample wells with a repetitive application of electric fields so as to set the transmembrane potential to a level corresponding to a pre-selected voltage dependent state of a target ion channel.
Type:
Grant
Filed:
February 2, 2004
Date of Patent:
February 13, 2007
Assignee:
Vertex Pharmaceuticals (San Diego) LLC
Inventors:
Michael P. Maher, Jesus E. Gonzalez, III
Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides processes for preparing the compounds of this invention, pharmaceutically acceptable compositions comprising the compounds of the invention, and methods of using the compositions in the treatment of various disorders.
Type:
Grant
Filed:
September 24, 2004
Date of Patent:
January 30, 2007
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Alex Aronov, David J. Lauffer, Pan Li, Ronald C. Tomlinson
Abstract: The present invention provides compounds of formula I: where R1 is H, CONH2, T(n)-R, or T(n)-Ar2, n may be zero or one, and G, XYZ, and Q are as described below. These compounds are inhibitors of protein kinase, particularly inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
Type:
Grant
Filed:
February 13, 2004
Date of Patent:
January 30, 2007
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Jeremy Green, Guy Bemis, Anne-Laure Grillot, Mark Ledeboer, Francesco G. Salituro, Edmund Harrington, Huai Gao, Christopher Baker, Jingrong Cao, Michael Hale
Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
Type:
Grant
Filed:
September 8, 2003
Date of Patent:
January 30, 2007
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Francesco Salituro, Guy Bemis, Huai Gao, Ghotas Evindar
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 20, 2004
Date of Patent:
January 2, 2007
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Jon H. Come, Jeremy Green, Craig Marhefka, Scott L. Harbeson, Ly Pham
Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved in cell proliferation, cell death and response to extracellular stimuli. The invention relates to compounds having the formula: or pharmaceutically acceptable salts thereof, wherein R1, Q1, Q2, and X are as described in the specification. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment end prevention of various disorders.
Type:
Grant
Filed:
September 27, 2004
Date of Patent:
December 19, 2006
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Francesco Salituro, Guy Bemis, John Cochran
Abstract: The present invention provides a facile process for the preparation of tri- and tetra-substituted pyrimidines. The process is useful for preparing inhibitors of protein kinases, especially Aurora kinase. These inhibitors are useful for treating or lessening the severity of Aurora-mediated diseases or conditions.
Type:
Application
Filed:
August 9, 2006
Publication date:
November 30, 2006
Applicant:
Vertex Pharmaceuticals Incorporated
Inventors:
Jean-Damien Charrier, Francesca Mazzei, David Kay, Andrew Miller